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Mekinist trametinib .05 mg/mL Powder, For Solution, 90 mL — NDC 00078-1161-47 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

Mekinist trametinib .05 mg/mL Powder, For Solution, 90 mL — NDC 0078-1161-47 (Billing 00078-1161-47)

by Novartis Pharmaceuticals Corporation · 90 mL in 1 BOTTLE

This is a package of 90 mL of Mekinist trametinib .05 mg/mL Powder, For Solution from Novartis Pharmaceuticals Corporation, marketed since Mar 2023 and currently FDA-listed. It is this product's only package size.

NDC 00078-1161-47
🏷️ FDA NDC (as labeled) 0078-1161-47 billing pads the labeler segment with a zero
Rx only Brand On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

NDC database record

One package, one record: these facts belong to NDC 0078-1161-47 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
0078 labeler · 1161 product · 47 package
Package marketed since
Mar 16, 2023
Sample package
No — commercial package
Listing certified through
Dec 31, 2027
Billing quantity
90 mL per package
Barcode (UPC-A, from the NDC)
3 0078116147 2
Medicaid fills, this package
1,150 prescriptions in the last four reported quarters
FDA record last changed
Jul 24, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 0078-1161-47
Product NDC 0078-1161
11-digit billing NDC 00078116147
NCPDP billing unit ML — per mL (volume)
RxCUI 1425110, 1425116, 1425118, 2632560, 2632564, 1425104
UNII BSB9VJ5TUT
Application # NDA217513
SPL Set ID 0002ad27-779d-42ab-83b5-bc65453412a1
Established class (EPC) Kinase Inhibitor
Mechanism of action Protein Kinase Inhibitors
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2023-03-16
Route ORAL
Dosage form POWDER, FOR SOLUTION
Substance TRAMETINIB DIMETHYL SULFOXIDE

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 21533570102120
GCN Seq No 084528
GCN 53859
HICL code 040361
Ingredient (HICL) Trametinib Dimethyl Sulfoxide
HIC1 code V
Therapeutic class — broad (HIC1) Neoplasms
HIC2 code V3
Therapeutic class — intermediate (HIC2) Antineoplastic Drugs (Continued 1)
HIC3 code V3U
Therapeutic class — specific (HIC3) Antineoplastic - Mek Kinase Inhibitors
AHFS code 10:00.00.00
AHFS class Antineoplastic Agents
FDB label name MEKINIST 0.05 MG/ML SOLUTION
FDB brand name Mekinist
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 084528
  • GCN: 53859
  • GPI-14 (Medi-Span): 21533570102120
  • HICL (First Databank): 040361
  • AHFS class code: 10:00.00.00
  • RxCUI (RxNorm): 1425110
Why two NDCs? The FDA registers this code as 0078-1161-47 — a 4-4-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the labeler segment → 00078-1161-47. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Kinase Inhibitor class.

Pharmacologic class Kinase Inhibitor
Drug family (ATC) Mitogen-activated protein kinase (MEK) inhibitors
How it works Protein Kinase Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name MEKINIST 0.05 MG/ML SOLUTION Ingredient Trametinib Dimethyl Sulfoxide
📖 What it is MedlinePlus · NLM

Trametinib is used alone or in combination with dabrafenib (Tafinlar) to treat certain types of melanoma (a type of skin cancer). It is also used in combination with dabrafenib to prevent the return of a certain type of melanoma after surgery. Trametinib is also used in combination with dabrafenib to treat certain types of non-small-cell lung cancer (NSCLC) and thyroid cancer. It is also used in combination with dabrafenib to treat certain types of solid tumors in adults and children 6 years of age older and to treat a certain type of glioma (a certain type of cancerous brain tumor) in childre...

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • It treats cancers that carry a BRAF V600 mutation, such as melanoma, non-small cell lung cancer, anaplastic thyroid cancer, other solid tumors, and low-grade glioma in children. Yo...
  • Take Mekinist once a day at the same time. Tablets go on an empty stomach, at least 1 hour before or 2 hours after a meal, and should not be crushed or broken. If you vomit, don't...
  • Rash, diarrhea, swelling, fever, chills, nausea, vomiting and tiredness are common. Tell your care team about them, because many can be managed. A fever of 100.4°F or higher needs...
  • Call for unusual bleeding, chest pain, shortness of breath, leg or arm swelling, vision changes, a new or worse cough, severe skin reactions, or severe stomach pain. These can be s...
📖 Read our full Trametinib guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer mLPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo $19.67 $1,769.97 / 90 ml
Medicare drug plans payPart D · Q2 2026 $21.56 $1,940.00 / 90 ml
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
00078-1161-47 You're viewing this Main listing 90 mL in 1 BOTTLE 2023-03-16 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Mekinist .05 mg/mLthis 00078-1161-47 Novartis 90 ml — — FDA listed —
About this product: this is the brand-name version. We did not find an FDA-approved generic match for this exact strength, form and route.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2023
First FDA approval
Mar 2023
📍
2026
Currently FDA-listed
3 years listed
🛡️
2031
Latest patent/protection listed
not a guaranteed launch date
🔒No FDA-approved generic found

We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.

🛡️ Latest patent/protection date listed: FDA patent/protection data lists protections through Apr 2031. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Mar 16, 2023 RLD RS ⏳ ~4.5 yr to latest listed protection

Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.

Patents & exclusivity — FDA Orange Book
US 8703781 — drug substance (U-3564)
US 7378423 — drug substance
US 7378423*PED — drug product
US 8703781*PED — drug product
Exclusivity NP
Exclusivity ODE-428
Exclusivity PED
Exclusivity PED
2023 2025 2027 2029 2031
Today
LOE
Substance patent Formulation patent Method-of-use patent Exclusivity Pediatric +6mo
🏛️FDA exclusivity
FDA-granted marketing protection. It’s separate from patents and may be shorter than patent protection.
🧪Product / substance patents
Patents covering the active ingredient, product, formulation, or related drug features.
🎯Method-of-use patents
Patents covering specific approved uses. These can sometimes be carved out with a “skinny label,” but not always.
🛈 What do these terms mean?
Patent
Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
Substance patent
Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
Formulation (product) patent
Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
Method-of-use patent
A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
Skinny label
A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
Exclusivity
FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
Paragraph IV
A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
RLD / RS
Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
TE / AB rating
FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
LOE (loss of exclusivity)
The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.

Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.

Listed patents (4)
PatentTypeUse codeExpires
US 8703781 ↗ Drug substance U-3564 Oct 15, 2030
US 7378423 ↗ Drug substance — May 29, 2027
US 7378423*PED ↗ Drug product — Nov 29, 2027
US 8703781*PED ↗ Drug product — Apr 15, 2031
FDA exclusivity
CodeWhat it grantsExpires
NPNew ProductMar 16, 2026
ODE-428Orphan Drug Exclusivity (7-year)Mar 16, 2030
PEDPediatric Exclusivity (+6 months)Sep 16, 2030
PEDPediatric Exclusivity (+6 months)Sep 16, 2026
Common questions
Is there a generic version of MEKINIST 0.05 MG/ML SOLUTION?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for MEKINIST 0.05 MG/ML SOLUTION. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Apr 2031 — an estimate, not a guaranteed launch date.
The FDA approved a generic — why can’t I get it at my pharmacy yet?
FDA approval and pharmacy availability are two different things. The FDA can approve a generic years before it actually reaches pharmacies, because the brand company may still hold patents or have a settlement that delays the launch. A manufacturer also has to choose to make and sell it, and have supply ready. So a drug can be “FDA-approved generic exists” and still be brand-only at the counter today.
Why do different websites show different generic release dates?
Generic availability is not based on one single date. Some sources use the first exclusivity expiration, some use the last product patent, and others use the latest method-of-use patent. Patent challenges, settlements, licenses, and label carve-outs can also change the real-world launch date. This page shows the underlying Orange Book dates so you can see why estimates may differ.
What does “FDA listed” mean?
It means the product appears in the FDA’s official NDC directory. That’s a good sign a product exists and is intended for the U.S. market, but on its own it does not confirm a pharmacy can fill it today. Where we have recent retail pricing data (NADAC) for a product, we label it “Availability likely” instead.
What does a patent or protection date mean here?
It’s the latest date currently listed in the FDA Orange Book for a patent or exclusivity on the brand product. It can affect when a full generic version becomes widely available — but it is not a guaranteed generic launch date. Generics sometimes arrive earlier (through a settlement or patent challenge) or later (a manufacturer still has to make and sell one).
What does “current Orange Book estimate” mean?
It means we are using the latest patent and exclusivity dates currently listed in the FDA Orange Book. It is not a guaranteed launch date.
Can a generic come out before the last patent expires?
Sometimes. A generic company may challenge a patent, settle with the brand manufacturer, receive a license, or obtain approval with a narrower label that avoids a patented use. In other cases, the last listed protection may delay full-label generic competition.
Can a generic come out after the listed dates?
Yes. Even after patents or exclusivity expire, a generic still needs FDA approval and a manufacturer must choose to market it. Supply, litigation, business decisions, or regulatory issues can delay actual availability.
What is the difference between patents and exclusivity?
Patents are legal protections usually issued by the U.S. Patent and Trademark Office. FDA exclusivity is marketing protection granted by the FDA. They are separate, and either one can affect generic timing.
Why are there multiple patent dates?
One drug can have several patents covering different things: the active ingredient, a formulation, a manufacturing process, or a specific approved use. That is why a page may show several expiration dates instead of one simple generic date.
Built from FDA Orange Book patent and exclusivity data. Dates are refreshed from public FDA data when available; the marker is max(latest patent expiry, latest exclusivity expiry). Paragraph-IV settlements and first-filer 180-day exclusivity can shift the real date; a method-of-use patent may allow an earlier skinny-label generic for non-protected indications. Generic launch timing is an estimate, not a guarantee.
Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

What it looks like

Color Yellow / Pink
ShapeRound
ImprintIMPRINT;LL
Size8 mm
ScoringNot scored
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

🧪 Avoiding an ingredient? See Trametinib inactive ingredients by manufacturer: every current product's list side by side, so you can ask your pharmacy for the version that does not list it.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII 2PP9364507
    A modified form of beta-cyclodextrin, a natural sugar-like molecule. It helps dissolve and stabilize drugs in liquid medicines and improves how well the body absorbs certain medications.
  • UNII 2968PHW8QP
    A weak organic acid derived from citrus fruits or made through fermentation. It works as a buffer to control pH, a preservative to extend shelf life, and a flavoring agent in medications.
  • UNII A2I8C7HI9T
    Methylparaben is a preservative derived from benzoic acid that prevents growth of bacteria, fungi, and mold in medicines. It extends the product's shelf life and maintains safety during storage.
  • UNII 1VPU26JZZ4
    Potassium sorbate is a salt derived from sorbic acid, a naturally occurring preservative. It prevents growth of mold, yeast, and some bacteria, extending the medicine's shelf life.
  • UNII GR686LBA74
    Sodium phosphate, dibasic is a salt derived from phosphoric acid. It acts as a buffer to help maintain the medicine's pH balance and may serve as a binder or filler in tablets and capsules.
  • UNII 4J2TY8Y81V
    A natural flavoring derived from strawberries that gives the medicine its strawberry taste and smell. It helps make the medicine more pleasant to take, especially for children.
  • UNII 96K6UQ3ZD4
    Sucralose is a synthetic sweetener made from sugar. It's added to medicines to improve taste without adding calories, helping make bitter or unpleasant-tasting drugs easier to take.

7 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerNovartis Pharmaceuticals Corporation
Application holderNOVARTIS PHARMACEUTICALS CORP
FDA applicationNDA217513 (NDA)
Labeler code00078
First marketedMar 2023
Product typeHuman Prescription Drug
Portfolio209 products on file

More NDCs from Novartis Pharmaceuticals Corporation labeler code 00078

The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Patient Package Insert 📖 Instructions for Use 📄 Recent Major Changes 📄 Package Label / Principal Display Panel
🎯 Indications and Usage ~3 min read ▾

1 INDICATIONS AND USAGE MEKINIST is a kinase inhibitor indicated as a single agent for the treatment of BRAF-inhibitor treatment-naïve patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test. ( 1.1 , 2.1 ) MEKINIST is indicated, in combination with dabrafenib, for: the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test. ( 1.1 , 2.1 ) the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection.

( 1.2 , 2.1 ) the treatment of patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation as detected by an FDA-approved test. ( 1.3 , 2.1 ) the treatment of patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation, as detected by an FDA-approved test, and with no satisfactory locoregional treatment options. ( 1.4 , 2.1 ) the treatment of adult and pediatric patients 1 year of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options.

This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s). ( 1.5 , 2.1 ) the treatment of pediatric patients 1 year of age and older with low-grade glioma (LGG) with a BRAF V600E mutation who require systemic therapy.

( 1.6 , 2.1 ) Limitations of Use : MEKINIST is not indicated for treatment of patients with colorectal cancer because of known intrinsic resistance to BRAF inhibition. ( 1.7 , 12.1 )

1.1BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma MEKINIST ® is indicated, as a single agent in BRAF-inhibitor treatment-naïve patients or in combination with dabrafenib, for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test [see Dosage and Administration (2.1)] .

1.2Adjuvant Treatment of BRAF V600E or V600K Mutation-Positive Melanoma MEKINIST is indicated, in combination with dabrafenib, for the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection [see Dosage and Administration (2.1)].

1.3BRAF V600E Mutation-Positive Metastatic NSCLC MEKINIST is indicated, in combination with dabrafenib, for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation as detected by an FDA-approved test [see Dosage and Administration (2.1)] .

1.4BRAF V600E Mutation-Positive Locally Advanced or Metastatic Anaplastic Thyroid Cancer MEKINIST is indicated, in combination with dabrafenib, for the treatment of patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation, as detected by an FDA-approved test, and with no satisfactory locoregional treatment options [see Dosage and Administration (2.1)] .

1.5BRAF V600E Mutation-Positive Unresectable or Metastatic Solid Tumors MEKINIST is indicated, in combination with dabrafenib, for the treatment of adult and pediatric patients 1 year of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options [see Dosage and Administration (2.1)] . This indication is approved under accelerated approval based on overall response rate and duration of response [see Clinical Studies (14.6)] .

Continued approval for this indication may be contingent upon verification and description of clinical benefit in a co… [Excerpted — this section continues on DailyMed.]

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION The recommended dosage of MEKINIST in adult patients is 2 mg orally once daily. The recommended dosage for MEKINIST in pediatric patients is based on body weight. ( 2 )

2.1Patient Selection Melanoma Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to initiation of treatment with MEKINIST as a single agent or in combination with dabrafenib [see Clinical Studies (14.1, 14.2)] . Information on FDA-approved tests for the detection of BRAF V600 mutations in melanoma is available at: http://www.fda.gov/CompanionDiagnostics . NSCLC Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.3)] .

Information on FDA-approved tests for the detection of BRAF V600E mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics . ATC Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.4)] . Information on FDA-approved tests for the detection of BRAF V600E mutations in ATC is available at: http://www.fda.gov/CompanionDiagnostics .

Solid Tumors Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.6)] . An FDA-approved test for the detection of BRAF V600E mutation in solid tumors other than melanoma and NSCLC is not currently available. Low-Grade Glioma Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.7)] .

An FDA-approved test for the detection of BRAF V600E mutation in LGG is not currently available.

2.2Recommended Dosage MEKINIST Tablets Adult Patients The recommended dosage for MEKINIST tablets in adult patients is 2 mg orally taken once daily [see Dosage and Administration (2.3)] . Pediatric Patients The recommended dosage for MEKINIST tablets in pediatric patients who weigh at least 26 kg is based on body weight (Table 1) [see Dosage and Administration (2.3)] . A recommended dosage of MEKINIST tablets has not been established in patients who weigh less than 26 kg.

Table 1. Recommended Dosage for MEKINIST Tablets in Pediatric Patients (Weight-based) Body Weight Recommended Dosage 26 to 37 kg 1 mg orally once daily 38 to 50 kg 1.5 mg orally once daily 51 kg or greater 2 mg orally once daily MEKINIST for Oral Solution Adult and Pediatric Patients The recommended dosage for MEKINIST for oral solution for adult and pediatric patients is based on body weight (Table 2) [see Dosage and Administration (2.3)] . Table 2.

Recommended Dosage for MEKINIST for Oral Solution in Adult and Pediatric Patients (Weight-based) Body Weight Recommended Dosage Total Volume of Oral Solution Once Daily (Trametinib Content) 8 kg 0.3 mg (6 mL) 9 kg 0.35 mg (7 mL) 10 kg 0.35 mg (7 mL) 11 kg 0.4 mg (8 mL) 12 to 13 kg 0.45 mg (9 mL) 14 to 17 kg 0.55 mg (11 mL) 18 to 21 kg 0.7 mg (14 mL) 22 to 25 kg 0.85 mg (17 mL) 26 to 29 kg 0.9 mg (18 mL) 30 to 33 kg 1 mg (20 mL) 34 to 37 kg 1.15 mg (23 mL) 38 to 41 kg 1.25 mg (25 mL) 42 to 45 kg 1.4 mg (28 mL) 46 to 50 kg 1.6 mg (32 mL) ≥ 51 kg 2 mg (40 mL) Duration of Treatment The recommended duration of treatment for patients with unresectable or metastatic melanoma or solid tumors, metastatic NSCLC, or locally advanced or metastatic anaplastic thyroid cancer is until disease progression or unacceptable toxicity.

The recommended duration of treatment in the adjuvant melanoma setting is until disease recurrence or unacceptable toxicity for up to 1 year. The recommended duration of treatment for pediatric patients with LGG is until disease progression or until unacceptable toxicity. Combination Therapy with Dabrafenib Refer to the dabrafenib prescribing information for recommended dabrafenib dosing information.

2.3Administration Take MEKINIST at the same time each day, approx… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 107 words ▾

3 DOSAGE FORMS AND STRENGTHS MEKINIST tablets: 0.5 mg tablets: Yellow, ovaloid, biconvex, unscored film-coated tablets with beveled edges and with the Novartis logo debossed on one side and ‘TT’ on the other side. 2 mg tablets: Pink, round, biconvex, unscored film-coated tablets with beveled edges and with the Novartis logo debossed on one side and ‘LL’ on the other side. MEKINIST for oral solution: White to almost white powder containing 4.7 mg of trametinib per bottle.

Each mL of reconstituted strawberry-flavored trametinib solution contains 0.05 mg of trametinib. MEKINIST Tablets: 0.5 mg, 2 mg ( 3 ) MEKINIST for Oral Solution: 4.7 mg ( 3 )

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS New Primary Malignancies, Cutaneous and Non-Cutaneous : Can occur when MEKINIST is used with dabrafenib. Monitor patients for new malignancies prior to, or while on therapy, and following discontinuation of treatment. ( 5.1 ) Hemorrhage : Major hemorrhagic events can occur.

Monitor for signs and symptoms of bleeding. ( 5.2 ) Colitis and Gastrointestinal Perforation : Colitis and gastrointestinal perforation can occur in patients receiving MEKINIST. ( 5.3 ) Venous Thromboembolic Events : Deep vein thrombosis (DVT) and pulmonary embolism (PE) can occur in patients receiving MEKINIST.

( 5.4 , 2.4 ) Cardiomyopathy : Assess left ventricular ejection fraction (LVEF) before treatment, after one month of treatment, then every 2 to 3 months thereafter. ( 5.5 , 2.4 ) Ocular Toxicities : Perform ophthalmological evaluation for any visual disturbances. For Retinal Vein Occlusion (RVO), permanently discontinue MEKINIST.

( 5.6 , 2.4 ) Interstitial Lung Disease (ILD)/Pneumonitis : Withhold MEKINIST for new or progressive unexplained pulmonary symptoms. Permanently discontinue MEKINIST for treatment-related ILD or pneumonitis. ( 5.7 , 2.4 ) Serious Febrile Reactions : Can occur when MEKINIST is used with dabrafenib.

( 5.8 , 2.4 ) Serious Skin Toxicities : Monitor for skin toxicities and for secondary infections. Permanently discontinue MEKINIST for intolerable Grade 2 or for Grade 3 or 4 rash not improving within 3 weeks despite interruption of MEKINIST. Permanently discontinue for severe cutaneous adverse reactions (SCARs).

( 5.9 , 2.4 ) Hyperglycemia : Monitor serum glucose levels in patients with preexisting diabetes or hyperglycemia. ( 5.10 ) Hemophagocytic Lymphohistiocytosis (HLH) : Interrupt treatment for suspected HLH. Discontinue treatment if HLH is confirmed.

( 5.12 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of potential risk to a fetus and to use effective contraception. ( 5.13 , 8.1 , 8.3 )

5.1New Primary Malignancies Cutaneous Malignancies MEKINIST Administered with Dabrafenib (Adult) : In the pooled safety population [see Adverse Reactions (6.1)] , cutaneous squamous cell carcinomas (cuSCCs) and keratoacanthomas occurred in 2% of patients. Basal cell carcinoma and new primary melanoma occurred in 3% and < 1% of patients, respectively. MEKINIST Administered with Dabrafenib (Pediatric) : In the pooled safety population, new primary melanoma occurred in < 1% of patients.

Perform dermatologic evaluations prior to initiation of MEKINIST when used with dabrafenib, every 2 months while on therapy, and for up to 6 months following discontinuation of the combination. Non-Cutaneous Malignancies Based on its mechanism of action, dabrafenib may promote growth and development of malignancies with activation of RAS through mutation or other mechanisms; refer to the prescribing information for dabrafenib. In the pooled safety population of MEKINIST administered with dabrafenib, non-cutaneous malignancies occurred in 1% of patients.

Monitor patients receiving MEKINIST and dabrafenib closely for signs or symptoms of non-cutaneous malignancies. No dose modification is required for MEKINIST in patients who develop non-cutaneous malignancies.

5.2Hemorrhage Hemorrhages, including major hemorrhage defined as symptomatic bleeding in a critical area or organ, can occur with MEKINIST. Fatal cases have been reported. MEKINIST Administered with Dabrafenib (Adult) : In the pooled safety population [see Adverse Reactions (6.1)] , hemorrhagic events occurred in 17% of patients; gastrointestinal hemorrhage occurred in 3% of patients; intracranial hemorrhage occurred in 0.6% of patients; fatal hemorrhage occurred in 0.5% of patients.

The fatal events were cerebral hemorrhage and brainstem hemorrhage. MEKINIST Administered with Dabrafenib (Pediatric) : In the pooled safety population, hemorrhagic events occurred in 25% of patients; the most common type of bleeding was epistaxis (16%). Se… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: New Primary Malignancies [see Warnings and Precautions ( 5.1)] Hemorrhage [see Warnings and Precautions (5.2)] Colitis and Gastrointestinal Perforation [see Warnings and Precautions (5.3)] Venous Thromboembolic Events [see Warnings and Precautions (5. 4 )] Cardiomyopathy [see Warnings and Precautions (5. 5 )] Ocular Toxicities [see Warnings and Precautions (5.

6 )] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5. 7 )] Serious Febrile Reactions [see Warnings and Precautions (5. 8 )] Serious Skin Toxicities [see Warnings and Precautions (5.

9 )] Hyperglycemia [see Warnings and Precautions (5. 10 )] Hemophagocytic Lymphohistiocytosis [see Warnings and Precautions (5. 12 )] There are additional adverse reactions associated with dabrafenib.

Refer to the dabrafenib prescribing information for additional information. Most common adverse reactions (≥ 20%) for MEKINIST as a single agent include rash, diarrhea, and lymphedema. ( 6.1 ) Most common adverse reactions (≥ 20%) for MEKINIST in combination with dabrafenib include: Unresectable or metastatic melanoma: pyrexia, nausea, rash, chills, diarrhea, vomiting, hypertension, and peripheral edema.

( 6.1 ) Adjuvant treatment of melanoma: pyrexia, fatigue, nausea, headache, rash, chills, diarrhea, vomiting, arthralgia, and myalgia. ( 6.1 ) NSCLC: pyrexia, fatigue, nausea, vomiting, diarrhea, dry skin, decreased appetite, edema, rash, chills, hemorrhage, cough, and dyspnea. ( 6.1 ) Adult patients with solid tumors: pyrexia, fatigue, nausea, rash, chills, headache, hemorrhage, cough, vomiting, constipation, diarrhea, myalgia, arthralgia, and edema.

( 6.1 ) Pediatric patients with solid tumors: pyrexia, rash, vomiting, fatigue, dry skin, cough, diarrhea, dermatitis acneiform, headache, abdominal pain, nausea, hemorrhage, constipation, and paronychia. ( 6.1 ) Pediatric patients with LGG: pyrexia, rash, headache, vomiting, musculoskeletal pain, fatigue, diarrhea, dry skin, nausea, hemorrhage, abdominal pain, and dermatitis acneiform. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Novartis Pharmaceuticals Corporation at 1-888-669-6682 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adult Safety Pools The pooled safety population described in the WARNINGS AND PRECAUTIONS reflects exposure to MEKINIST 2 mg orally, once daily as a single agent in 329 patients with various solid tumors enrolled in METRIC, MEK113583, and MEK111054.

Among these 329 patients who received MEKINIST as a single agent, 33% were exposed for 6 months or longer and 9% were exposed for greater than one year. The pooled safety population described in the WARNINGS AND PRECAUTIONS reflects exposure to MEKINIST 2 mg orally, once daily, administered in combination with dabrafenib 150 mg orally, twice daily, in 1087 patients enrolled in COMBI-d, COMBI-v, COMBI-AD, and BRF113928 with unresectable or metastatic melanoma, adjuvant melanoma, or NSCLC. Among these 1087 patients who received MEKINIST administered with dabrafenib, 70% were exposed for 6 months or longer and 21% were exposed for greater than one year.

Pediatric Safety Pool The pediatric pooled safety population described in the WARNINGS AND PRECAUTIONS reflects exposure to weight-based MEKINIST orally, once daily administered in combination with dabrafenib in 166 pediatric patients across two trials: a multi-center, open-label, multi-cohort study in pediatric patients with BRAF V600E mutation-positive glioma requiring systemic therapy (Study G2201; n = 123) and a multi-center, open-label, multi-cohort study in pediatric patients with refr… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions 28 words ▾

7 DRUG INTERACTIONS MEKINIST is indicated for use in combination with dabrafenib. Refer to the dabrafenib prescribing information for additional risk information that applies to combination use treatment.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Do not breastfeed. ( 8.2 ) Females and Males of Reproductive Potential : May impair fertility. Counsel patients on pregnancy planning and prevention. ( 8.3 )

8.1Pregnancy Risk Summary Based on its mechanism of action [see Clinical Pharmacology (12.1)] and findings from animal reproduction studies, MEKINIST can cause fetal harm when administered to a pregnant woman. There is insufficient data in pregnant women exposed to MEKINIST to assess the risks. Trametinib was embryotoxic and abortifacient in rabbits at doses greater than or equal to those resulting in exposures approximately 0.3 times the human exposure at the recommended adult clinical dose (see Data) .

Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In reproductive toxicity studies, administration of trametinib to rats during the period of organogenesis resulted in decreased fetal weights at doses greater than or equal to 0.031 mg/kg/day [approximately 0.3 times the human exposure at the recommended adult dose based on area under the curve (AUC)].

In rats, at a dose resulting in exposures 1.8-fold higher than the human exposure at the recommended adult dose, there was maternal toxicity and an increase in post-implantation loss. In pregnant rabbits, administration of trametinib during the period of organogenesis resulted in decreased fetal body weight and increased incidence of variations in ossification at doses greater than or equal to 0.039 mg/kg/day (approximately 0.08 times the human exposure at the recommended adult dose based on AUC). In rabbits administered trametinib at 0.15 mg/kg/day (approximately 0.3 times the human exposure at the recommended adult dose based on AUC) there was an increase in post-implantation loss, including total loss of pregnancy, compared with control animals.

8.2Lactation Risk Summary There are no data on the presence of trametinib in human milk, or the effects of trametinib on the breastfed child or on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with MEKINIST and for 4 months following the last dose.

8.3Females and Males of Reproductive Potential Pregnancy Testing Verify pregnancy status in females of reproductive potential prior to initiating MEKINIST. Contraception Based on data from animal studies and its mechanism of action, MEKINIST can cause fetal harm when administered to pregnant women [see Use in Specific Populations (8.1 )]. Females Advise female patients of reproductive potential to use effective contraception during treatment with MEKINIST and for 4 months after the last dose.

Males To avoid potential drug exposure to pregnant partners and female partners of reproductive potential, advise male patients (including those who have had vasectomies) with female partners of reproductive potential to use condoms during treatment with MEKINIST and for 4 months after the last dose. Infertility Females Advise female patients of reproductive potential that MEKINIST may impair fertility. Increased follicular cysts and decreased corpora lutea were observed in female rats at dose exposures equivalent to 0.3 times the human exposure at the recommended adult dose [see Nonclinical Toxicology (13.1)] .

8.4Pediatric Use BRAF V600E Mutation-Positive Unresectable or Metastatic Solid Tumors and LGG The safety and effectiveness of MEKINIST in combination with dabrafenib have been established in pediatric patients 1 year of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options; or with LGG with BRAF V600E mutation who require systemic therapy. Use of MEKINIST in combination wi… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~1 min read ▾

8.1Pregnancy Risk Summary Based on its mechanism of action [see Clinical Pharmacology (12.1)] and findings from animal reproduction studies, MEKINIST can cause fetal harm when administered to a pregnant woman. There is insufficient data in pregnant women exposed to MEKINIST to assess the risks. Trametinib was embryotoxic and abortifacient in rabbits at doses greater than or equal to those resulting in exposures approximately 0.3 times the human exposure at the recommended adult clinical dose (see Data) .

Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In reproductive toxicity studies, administration of trametinib to rats during the period of organogenesis resulted in decreased fetal weights at doses greater than or equal to 0.031 mg/kg/day [approximately 0.3 times the human exposure at the recommended adult dose based on area under the curve (AUC)].

In rats, at a dose resulting in exposures 1.8-fold higher than the human exposure at the recommended adult dose, there was maternal toxicity and an increase in post-implantation loss. In pregnant rabbits, administration of trametinib during the period of organogenesis resulted in decreased fetal body weight and increased incidence of variations in ossification at doses greater than or equal to 0.039 mg/kg/day (approximately 0.08 times the human exposure at the recommended adult dose based on AUC). In rabbits administered trametinib at 0.15 mg/kg/day (approximately 0.3 times the human exposure at the recommended adult dose based on AUC) there was an increase in post-implantation loss, including total loss of pregnancy, compared with control animals.

🧒 Pediatric Use ~1 min read ▾

8.4Pediatric Use BRAF V600E Mutation-Positive Unresectable or Metastatic Solid Tumors and LGG The safety and effectiveness of MEKINIST in combination with dabrafenib have been established in pediatric patients 1 year of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options; or with LGG with BRAF V600E mutation who require systemic therapy. Use of MEKINIST in combination with dabrafenib for these indications is supported by evidence from studies X2101 and G2201 that enrolled 171 patients (1 to < 18 years of age) with BRAF V600 mutation-positive advanced solid tumors, of which 4 (2.3%) patients were 1 to < 2 years of age, 39 (23%) patients were 2 to < 6 years of age, 54 (32%) patients were 6 to < 12 years of age, and 74 (43%) patients were 12 to < 18 years of age [see Adverse Reactions (6.1), Clinical Pharmacology (12.3), Clinical Studies (14.6, 14.7)] .

The safety and effectiveness of MEKINIST in combination with dabrafenib have not been established for these indications in pediatric patients less than 1 year old. The safety and effectiveness of MEKINIST as a single agent in pediatric patients have not been established. Juvenile Animal Toxicity Data In a repeat-dose toxicity study in juvenile rats, decreased bone length and corneal dystrophy were observed at doses resulting in exposures as low as 0.3 times the human exposure at the recommended adult dose based on AUC.

Additionally, a delay in sexual maturation was noted at doses resulting in exposures as low as 1.6 times the human exposure at the recommended adult dose based on AUC.

🧓 Geriatric Use ~1 min read ▾

8.5Geriatric Use Of the 214 patients with melanoma who received single agent MEKINIST in the METRIC study, 27% were aged 65 years and older and 4% were over 75 years old [see Clinical Studies (14.1)] . This study of single agent MEKINIST in melanoma did not include sufficient numbers of geriatric patients to determine whether they respond differently from younger adults. Of the 994 patients with melanoma who received MEKINIST plus dabrafenib in the COMBI-d, COMBI-v, and COMBI-AD studies [see Clinical Studies (14.1, 14.2)] , 21% were aged 65 years and older and 5% were aged 75 years and older.

No overall differences in the effectiveness of MEKINIST plus dabrafenib were observed in geriatric patients as compared to younger adults across these melanoma studies. The incidences of peripheral edema (26% vs. 12%) and anorexia (21% vs.

9%) increased in geriatric patients as compared to younger adults in these studies. Of the 93 patients with NSCLC who received MEKINIST in Study BRF113928, there were insufficient numbers of geriatric patients aged 65 years and older to determine whether they respond differently from younger adults [see Clinical Studies (14.4)] . Of the 26 patients with ATC who received MEKINIST in Study BRF117019, 77% were aged 65 years and older and 31% were aged 75 years and older [see Clinical Studies (14.4)] .

This study in ATC did not include sufficient numbers of younger adults to determine whether they respond differently compared to geriatric patients.

🆘 Overdosage 76 words ▾

10 OVERDOSAGE The highest doses of MEKINIST evaluated in clinical trials were 4 mg orally once daily and 10 mg administered orally once daily on 2 consecutive days followed by 3 mg once daily. In seven patients treated on one of these two schedules, there were two cases of RPEDs for an incidence of 28%. Since trametinib is highly bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with MEKINIST.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Trametinib is a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2.

Trametinib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo. Trametinib and dabrafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Use of trametinib and dabrafenib in combination resulted in greater growth inhibition of BRAF V600 mutation-positive tumor cell lines in vitro and prolonged inhibition of tumor growth in BRAF V600 mutation-positive tumor xenografts compared with either drug alone.

In the setting of BRAF-mutant colorectal cancer, induction of EGFR-mediated MAPK pathway re-activation has been identified as a mechanism of intrinsic resistance to BRAF inhibitors [see Indications and Usage (1.7)] .

12.2Pharmacodynamics Administration of MEKINIST tablets 1 mg and 2 mg to patients with BRAF V600 mutation-positive melanoma resulted in dose-dependent changes in tumor biomarkers, including inhibition of phosphorylated ERK, inhibition of Ki67 (a marker of cell proliferation), and increases in p27 (a marker of apoptosis). Cardiac Electrophysiology The heart rate-corrected QT (QTc) prolongation potential of trametinib was assessed in a dedicated study in 32 patients who received placebo on Day 1 and MEKINIST tablets 2 mg once daily on Days 2-14 followed by MEKINIST tablets 3 mg on Day 15.

No large changes in the mean QTc interval (i.e., > 20 ms) were detected in the study. A decrease from baseline in HR by 9 beats/min (90% CI: -11.4 to -6.1) and an increase from baseline in PR by 20 ms (90% CI: 13.0 to 27.4) relative to placebo was observed at two hours post-dose in the same study. In clinical trials in patients who received MEKINIST with dabrafenib, QTc prolongation > 500 ms occurred in 0.8% of patients and QTc increased by > 60 ms from baseline in 3.8% of patients.

12.3Pharmacokinetics The pharmacokinetics of trametinib were characterized following a single dose and multiple doses in patients with solid tumors and BRAF V600 mutation-positive metastatic melanoma. Following administration of MEKINIST tablets 0.125 mg (0.0625 times the approved recommended adult dosage) to 4 mg (2 times the approved recommended adult dosage) daily, both C max and AUC increase proportionally with dose. Intersubject variability in AUC and C max at steady state is 22% and 28%, respectively.

Absorption The median time to achieve peak plasma concentrations (T max ) is 1.5 hours post-dose. The mean absolute bioavailability of MEKINIST tablets is 72% and MEKINIST for oral solution is 81%. Effect of Food Following administration of MEKINIST tablets, a high-fat, high-calorie meal (approximately 1000 calories) decreased trametinib AUC by 24%, C max by 70%, and delayed T max by approximately 4 hours as compared with fasted conditions.

Administration of a single 2 mg dose of MEKINIST for oral solution with a low-fat, low-calorie meal (approximately 500 calories, 14 grams fat, 80 grams carbohydrates, and 12 grams protein) showed no clinically significant changes on both AUC and C max of trametinib as compared with fasted conditions. Distribution Trametinib is 97.4% bound to human plasma proteins. The apparent volume of distribution (V c /F) is 214 L.

Elimination The estimated elimination half-life is 3.9 to 4.8 days. The apparent clearance is

4.9L/h. Metabolism Trametinib is metabolized predominantly via deacetylation alone or with mono-oxygenation or in combination with glucuronidation biotransformation pathways in vitro. Deacetylation is mediated by carboxylesterases (i.e., carboxylesterase 1b/c and 2) and may also be mediated by other hydrolytic enzymes.… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 153 words ▾

12.1Mechanism of Action Trametinib is a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2.

Trametinib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo. Trametinib and dabrafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Use of trametinib and dabrafenib in combination resulted in greater growth inhibition of BRAF V600 mutation-positive tumor cell lines in vitro and prolonged inhibition of tumor growth in BRAF V600 mutation-positive tumor xenografts compared with either drug alone.

In the setting of BRAF-mutant colorectal cancer, induction of EGFR-mediated MAPK pathway re-activation has been identified as a mechanism of intrinsic resistance to BRAF inhibitors [see Indications and Usage (1.7)] .

📦 How Supplied / Storage and Handling 215 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING MEKINIST Tablets : 0.5 mg tablets: Yellow, ovaloid, biconvex, unscored film-coated tablets with beveled edges and with the Novartis logo debossed on one side and ‘TT’ on the other side; available in bottles of 30 (NDC 0078-1105-15). 2 mg tablets: Pink, round, biconvex, unscored film-coated tablets with beveled edges and with the Novartis logo debossed on one side and ‘LL’ on the other side; available in bottles of 30 (NDC 0078-1112-15). Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature].

Dispense in original bottle. Do not remove desiccant. Protect from moisture and light.

Do not place medication in pill boxes. MEKINIST for Oral Solution : White or almost white powder in amber glass bottles, co-packaged with a press-in bottle adapter and an oral syringe. Each bottle contains 4.7 mg of trametinib equivalent to 5.3 mg trametinib dimethyl sulfoxide.

Each mL of reconstituted strawberry flavored trametinib solution contains 0.05 mg of trametinib non-solvated parent. (NDC 0078-1161-47). Store refrigerated at 2°C to 8°C (36°F to 46°F).

Store in the original carton to protect from light and moisture. After reconstitution, store in the original bottle below 25°C (77°F) and do not freeze. Discard any unused solution 35 days after reconstitution.

📋 Description ~1 min read ▾

11 DESCRIPTION Trametinib dimethyl sulfoxide is a kinase inhibitor. The chemical name is acetamide, N-[3-[3-cyclopropyl-5-[(2-fluoro-4- iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl- 2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]-, compound with 1,1’-sulfinylbis[methane] (1:1). It has a molecular formula C 26 H 23 FIN 5 O 4 •C 2 H 6 OS with a molecular mass of 693.53 g/mol.

Trametinib dimethyl sulfoxide has the following chemical structure: Trametinib dimethyl sulfoxide is a white to almost white powder. It is practically insoluble in the pH range of 2 to 8 in aqueous media. MEKINIST (trametinib) tablets for oral use are supplied as 0.5 mg and 2 mg tablets for oral administration.

Each 0.5 mg tablet contains 0.5635 mg trametinib dimethyl sulfoxide equivalent to 0.5 mg of trametinib non-solvated parent. Each 2 mg tablet contains 2.254 mg trametinib dimethyl sulfoxide equivalent to 2 mg of trametinib non-solvated parent. The inactive ingredients of MEKINIST tablets are: Tablet Core: colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate (vegetable source), mannitol, microcrystalline cellulose, and sodium lauryl sulfate.

Coating: hypromellose, iron oxide red (2 mg tablets), iron oxide yellow (0.5 mg tablets), polyethylene glycol, polysorbate 80 (2 mg tablets), and titanium dioxide. MEKINIST (trametinib) for oral solution is a white or almost white powder which produces a clear colorless solution when reconstituted with water. Each bottle contains 4.7 mg of trametinib equivalent to 5.3 mg trametinib dimethyl sulfoxide.

Each mL of reconstituted trametinib solution contains 0.05 mg of trametinib non-solvated parent. The inactive ingredients of MEKINIST for oral solution are betadex sulfobutyl ether sodium, citric acid monohydrate, dibasic sodium phosphate, methylparaben, potassium sorbate, sucralose, and strawberry flavor. Trametinib Structure-01

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information and Instructions for Use). New Primary Cutaneous and Non-cutaneous Malignancies Advise patients that MEKINIST administered with dabrafenib can result in the development of new primary cutaneous and non-cutaneous malignancies. Advise patients to contact their healthcare provider immediately for any new lesions, changes to existing lesions on their skin, or other signs and symptoms of malignancies [see Warnings and Precautions (5.1)] .

Hemorrhage Advise patients that MEKINIST administered with dabrafenib increases the risk of intracranial and gastrointestinal hemorrhage. Advise patients to contact their healthcare provider to seek immediate medical attention for signs or symptoms of unusual bleeding or hemorrhage [see Warnings and Precautions (5.2)] . Colitis and Gastrointestinal Perforation Advise patients that MEKINIST can cause colitis and gastrointestinal perforation and to contact their healthcare provider for signs or symptoms of colitis or gastrointestinal perforation [see Warnings and Precautions (5.3)] .

Venous Thromboembolic Events Advise patients that MEKINIST administered with dabrafenib increases the risks of PE and DVT. Advise patients to seek immediate medical attention for sudden onset of difficulty breathing, leg pain, or swelling [see Warnings and Precautions (5.4)] . Cardiomyopathy Advise patients that MEKINIST can cause cardiomyopathy and to immediately report any signs or symptoms of heart failure to their healthcare provider [see Warnings and Precautions (5.5)] .

Ocular Toxicities Advise patients that MEKINIST can cause severe visual disturbances that can lead to blindness and to contact their healthcare provider if they experience any changes in their vision [see Warnings and Precautions (5.6)] . Interstitial Lung Disease/Pneumonitis Advise patients that MEKINIST can cause ILD (or pneumonitis). Advise patients to contact their healthcare provider as soon as possible if they experience signs, such as cough or dyspnea [see Warnings and Precautions (5.7)] .

Serious Febrile Reactions Advise patients that MEKINIST administered with dabrafenib can cause serious febrile reactions. Instruct patients to contact their healthcare provider if they develop a fever while taking MEKINIST with dabrafenib [see Warnings and Precautions (5.8)] . Serious Skin Toxicities Advise patients that MEKINIST can cause serious skin toxicities, which may require hospitalization, and to contact their healthcare provider for progressive or intolerable rash.

Advise patients to contact their healthcare provider immediately if they develop signs and symptoms of a severe skin reaction [see Warnings and Precautions (5.9)] . Hypertension Advise patients that MEKINIST can cause hypertension and that they need to undergo blood pressure monitoring and to contact their healthcare provider if they develop symptoms of hypertension, such as severe headache, blurry vision, or dizziness [see Adverse Reactions (6.1)] . Diarrhea Advise patients that MEKINIST often causes diarrhea which may be severe in some cases.

Inform patients of the need to contact their healthcare provider if severe diarrhea occurs during treatment [see Adverse Reactions (6.1)] . Embryo-Fetal Toxicity Advise pregnant women and males of reproductive potential of the potential risk to a fetus [see Warnings and Precautions (5.13), Use in Specific Populations (8.1, 8.3)] . Advise females to contact their healthcare provider of a known or suspected pregnancy.

Advise females of reproductive potential to use effective contraception during treatment with MEKINIST and for 4 months after the last dose. Advise male patients with female partners of reproductive potential to use condoms during treatment with MEKINIST and for 4 months after the last dose. Lactation Advise women not to breastfeed during treatment with MEKINIST and for 4 months after the last dose [see Use in Specific… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics The pharmacokinetics of trametinib were characterized following a single dose and multiple doses in patients with solid tumors and BRAF V600 mutation-positive metastatic melanoma. Following administration of MEKINIST tablets 0.125 mg (0.0625 times the approved recommended adult dosage) to 4 mg (2 times the approved recommended adult dosage) daily, both C max and AUC increase proportionally with dose. Intersubject variability in AUC and C max at steady state is 22% and 28%, respectively.

Absorption The median time to achieve peak plasma concentrations (T max ) is 1.5 hours post-dose. The mean absolute bioavailability of MEKINIST tablets is 72% and MEKINIST for oral solution is 81%. Effect of Food Following administration of MEKINIST tablets, a high-fat, high-calorie meal (approximately 1000 calories) decreased trametinib AUC by 24%, C max by 70%, and delayed T max by approximately 4 hours as compared with fasted conditions.

Administration of a single 2 mg dose of MEKINIST for oral solution with a low-fat, low-calorie meal (approximately 500 calories, 14 grams fat, 80 grams carbohydrates, and 12 grams protein) showed no clinically significant changes on both AUC and C max of trametinib as compared with fasted conditions. Distribution Trametinib is 97.4% bound to human plasma proteins. The apparent volume of distribution (V c /F) is 214 L.

Elimination The estimated elimination half-life is 3.9 to 4.8 days. The apparent clearance is

4.9L/h. Metabolism Trametinib is metabolized predominantly via deacetylation alone or with mono-oxygenation or in combination with glucuronidation biotransformation pathways in vitro. Deacetylation is mediated by carboxylesterases (i.e., carboxylesterase 1b/c and 2) and may also be mediated by other hydrolytic enzymes.

Following a single dose of [ 14 C]-trametinib, approximately 50% of circulating radioactivity is represented as the parent compound; however, ≥ 75% of drug-related material in plasma is the parent compound based on metabolite profiling after repeat dosing of trametinib. Excretion Following oral administration of [ 14 C]-trametinib, greater than 80% of excreted radioactivity was recovered in the feces while less than 20% of excreted radioactivity was recovered in the urine with less than 0.1% of the excreted dose as parent.

Specific Populations Age (18 to 93 years), sex, body weight (36 to 170 kg), and renal impairment (eGFR 15 to 89 mL/min/1.73 m 2 ) have no clinically significant effect on the exposure of trametinib. There are insufficient data to evaluate potential differences in the exposure of trametinib by race or ethnicity. Pediatric Patients: The pharmacokinetics of trametinib in glioma and other solid tumors were evaluated in 244 patients aged 1 to < 18 years following a single dose or multiple doses.

Pharmacokinetic parameters in patients aged 1 to < 18 years are within range of values previously observed in adults given the same dose based on weight. Weight (6 to 156 kg) was found to have a statistically significant effect on trametinib oral clearance in this population. Patients with Hepatic Impairment: Hepatic impairment (defined by bilirubin and AST levels) had no significant effect in trametinib exposure or apparent drug clearance compared with patients with normal hepatic function.

Drug Interaction Studies Effect of Dabrafenib on Trametinib : Coadministration of MEKINIST tablets 2 mg daily with dabrafenib resulted in no change in AUC of trametinib. Effect of Trametinib on CYP Substrates: Coadministration of MEKINIST tablets 2 mg once daily with a sensitive CYP3A4 substrate had no clinically relevant effect on the AUC and C max of the sensitive CYP3A4 substrate. Based on in vitro studies, trametinib is an inhibitor of CYP2C8, but is not an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, or CYP2D6 at a clinically relevant systemic concentration.

Effect of Transporters on Trametinib: Trametinib is a substrate of P-glycoprotein (P-gp) and BSEP. Inh… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics 183 words ▾

12.2Pharmacodynamics Administration of MEKINIST tablets 1 mg and 2 mg to patients with BRAF V600 mutation-positive melanoma resulted in dose-dependent changes in tumor biomarkers, including inhibition of phosphorylated ERK, inhibition of Ki67 (a marker of cell proliferation), and increases in p27 (a marker of apoptosis). Cardiac Electrophysiology The heart rate-corrected QT (QTc) prolongation potential of trametinib was assessed in a dedicated study in 32 patients who received placebo on Day 1 and MEKINIST tablets 2 mg once daily on Days 2-14 followed by MEKINIST tablets 3 mg on Day 15.

No large changes in the mean QTc interval (i.e., > 20 ms) were detected in the study. A decrease from baseline in HR by 9 beats/min (90% CI: -11.4 to -6.1) and an increase from baseline in PR by 20 ms (90% CI: 13.0 to 27.4) relative to placebo was observed at two hours post-dose in the same study. In clinical trials in patients who received MEKINIST with dabrafenib, QTc prolongation > 500 ms occurred in 0.8% of patients and QTc increased by > 60 ms from baseline in 3.8% of patients.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES Figure 1. Kaplan-Meier Curves of Investigator-Assessed Progression-Free Survival (ITT Population) in the METRIC Study Figure 2. Kaplan-Meier Curves of Overall Survival in the COMBI-d Study Figure 3. Kaplan-Meier Curves for Investigator-Assessed Relapse-Free Survival in COMBI-AD in the Adjuvant Treatment of Melanoma Figure 4. Kaplan-Meier Curves for Progression-Free Survival in Study G2201 (LGG cohort)

14.1BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma MEKINIST as a Single Agent The safety and efficacy of MEKINIST were evaluated in an international, multi-center, randomized (2:1), open-label, active-controlled trial (the METRIC study; NCT01245062) in 322 patients with BRAF V600E or V600K mutation-positive, unresectable or metastatic melanoma. In the METRIC study, patients were not permitted to have more than one prior chemotherapy regimen for advanced or metastatic disease; prior treatment with a BRAF inhibitor or MEK inhibitor was not permitted.

Patients were randomized to receive MEKINIST 2 mg orally once daily (N = 214) or chemotherapy (N = 108) consisting of either dacarbazine 1000 mg/m 2 intravenously every 3 weeks or paclitaxel 175 mg/m 2 intravenously every 3 weeks. Treatment continued until disease progression or unacceptable toxicity. Randomization was stratified according to prior use of chemotherapy for advanced or metastatic disease (yes vs. no) and LDH level (normal vs. greater than ULN).

Tumor tissue was evaluated for BRAF mutations at a central testing site using a clinical trial assay. Tumor samples from 289 patients (196 patients treated with MEKINIST and 93 chemotherapy-treated patients) were also tested retrospectively using an FDA-approved companion diagnostic test, THxID ® -BRAF assay. The major efficacy outcome measure was progression-free survival (PFS) as assessed by the investigator.

The median age for randomized patients was 54 years, 54% were male, greater than 99% were White, and all patients had baseline ECOG performance status of 0 or 1. Most patients had metastatic disease (94%), had M1c disease (64%), had elevated LDH (36%), had no history of brain metastasis (97%), and received no prior chemotherapy for advanced or metastatic disease (66%). The distribution of BRAF V600 mutations was BRAF V600E (87%), V600K (12%), or both (less than 1%).

The median durations of follow-up prior to initiation of alternative treatment were 4.9 months for patients treated with MEKINIST and 3.1 months for patients treated with chemotherapy. Fifty-one (47%) patients crossed over from the chemotherapy arm at the time of disease progression to receive MEKINIST. The METRIC study demonstrated a statistically significant increase in PFS in the patients treated with MEKINIST.

Table 20 and Figure 1 summarize the PFS results. Table 20. Efficacy Results in the METRIC Study Abbreviations: CI, confidence interval; DoR, duration of response; HR, hazard ratio; NR, not reached. a Pike estimator.

Investigator - A ssessed Endpoints MEKINIST N = 214 Chemotherapy N = 108 P rogression- F ree S urvival Number of events (%) 117 (55%) 77 (71%) Progressive disease 107 (50%) 70 (65%) Death 10 (5%) 7 (6%) Median, months (95% CI) 4.8 (4.3, 4.9) 1.5 (1.4, 2.7) HR a (95% CI) 0.47 (0.34, 0.65) P -value (log-rank test) < 0.0001 Confirmed Tumor Responses Overall response rate (95% CI) 22% (17%, 28%) 8% (4%, 15%) Complete response, n (%) 4 (2%) 0 Partial response, n (%) 43 (20%) 9 (8%) Duration of Response Median DoR, months (95% CI) 5.5 (4.1, 5.9) NR (3.5, NR) Figure 1.

Kaplan-Meier Curves of Investigator-Assessed Progression-Free Survival (ITT Population) in the METRIC Study In supportive analyses based on independent radiologic review committee (IRRC) assessment, the PFS results were consistent with those of the primary efficacy analysis. MEKINIST with Dabrafenib COMBI-d Study The safety and efficacy of MEKINIST administered with dabrafenib were evaluated in an international, randomized, double-blin… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology 114 words ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies with trametinib have not been conducted. Trametinib was not genotoxic in studies evaluating reverse mutations in bacteria, chromosomal aberrations in mammalian cells, and micronuclei in the bone marrow of rats. Trametinib may impair fertility in humans.

In female rats given trametinib for up to 13 weeks, increased follicular cysts and decreased corpora lutea were observed at doses ≥ 0.016 mg/kg/day (approximately 0.3 times the human exposure at the recommended adult dose based on AUC). In rat and dog toxicity studies up to 13 weeks in duration, there were no treatment effects observed on male reproductive tissues [see Use in Specific Populations (8.3)] .

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 111 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies with trametinib have not been conducted. Trametinib was not genotoxic in studies evaluating reverse mutations in bacteria, chromosomal aberrations in mammalian cells, and micronuclei in the bone marrow of rats. Trametinib may impair fertility in humans.

In female rats given trametinib for up to 13 weeks, increased follicular cysts and decreased corpora lutea were observed at doses ≥ 0.016 mg/kg/day (approximately 0.3 times the human exposure at the recommended adult dose based on AUC). In rat and dog toxicity studies up to 13 weeks in duration, there were no treatment effects observed on male reproductive tissues [see Use in Specific Populations (8.3)] .

📄 Patient Package Insert ~3 min read ▾

This Patient Information has been approved by the U.S. Food and Drug Administration. Revised: March 2025 Patient Information MEKINIST ® (MEK-in-ist) (trametinib) tablets MEKINIST ® (MEK-in-ist) (trametinib) for oral solution Important information: If your healthcare provider prescribes MEKINIST to be taken or given with dabrafenib, also read the Medication Guide that comes with dabrafenib.

What is the most important information I should know about MEKINIST? MEKINIST may cause serious side effects, including: Risk of new skin cancers. MEKINIST, when used with dabrafenib, may cause skin cancers, called cutaneous squamous cell carcinoma, keratoacanthoma, basal cell carcinoma, or melanoma.

Talk to your healthcare provider about your risk for these cancers. Check your skin and tell your healthcare provider right away about any skin changes, including a: new wart skin sore or reddish bump that bleeds or does not heal change in size or color of a mole Your healthcare provider should check your skin before treatment with MEKINIST and dabrafenib, every 2 months during treatment with MEKINIST and dabrafenib, and for up to 6 months after you stop taking MEKINIST and dabrafenib to look for any new skin cancers.

Your healthcare provider should also check for cancers that may not occur on the skin. Tell your healthcare provider about any new symptoms that develop during treatment with MEKINIST with dabrafenib. See "What are the possible side effects of MEKINIST?" for more information about side effects.

What is MEKINIST? MEKINIST is a prescription medicine used: alone or in combination with a medicine called dabrafenib to treat a type of skin cancer called melanoma: ○ that has spread to other parts of the body or cannot be removed by surgery, and ○ that has a certain type of abnormal “BRAF” gene. MEKINIST should not be used to treat people who already have received a BRAF inhibitor for treatment of their melanoma, and it did not work or is no longer working. in combination with dabrafenib, to help prevent melanoma that has a certain type of abnormal “BRAF” gene from coming back after the cancer has been removed by surgery. in combination with dabrafenib to treat a type of lung cancer called non-small cell lung cancer (NSCLC): ○ that has spread to other parts of the body, and ○ that has a certain type of abnormal “BRAF” gene. in combination with dabrafenib to treat a type of thyroid cancer called anaplastic thyroid cancer (ATC): ○ that has spread to other parts of the body and you have no satisfactory treatment options, and ○ that has a certain type of abnormal “BRAF” gene. in combination with dabrafenib to treat solid tumors in adults and children 1 year and older: ○ that cannot be removed by surgery or have spread to other parts of the body, and that have gotten worse (progressed), and you have no satisfactory treatment options, and ○ that have a certain type of abnormal “BRAF” gene. in combination with dabrafenib to treat a type of brain tumor called glioma in children 1 year and older: ○ that is low-grade glioma (LGG), and ○ that have a certain type of abnormal “BRAF” gene, and ○ who require a medicine by mouth or injection (systemic therapy).

MEKINIST is not for use in treating people with colorectal cancer. Your healthcare provider will perform a test to make sure that MEKINIST is right for you. It is not known if MEKINIST used in combination with dabrafenib is safe and effective in children less than 1 year of age.

It is not known if MEKINIST used alone is safe and effective in children. Before you take or give MEKINIST, tell your healthcare provider about all of your medical conditions, including if you: have had bleeding problems or blood clots have stomach problems have inflammation of the colon have heart problems have eye problems have lung or breathing problems have high blood pressure (hypertension) have liver or kidney problems have diabetes are pregnant or plan to become pregnant. MEKINIST can harm your unborn baby.

Females w… [Excerpted — this section continues on DailyMed.]

📖 Instructions for Use ~3 min read ▾

This Instructions for Use has been approved by the U.S. Food and Drug Administration. Revised: March 2025 INSTRUCTIONS FOR USE MEKINIST ® (MEK-in-ist) (trametinib) for oral solution This “Instructions for Use” contains information on how to give MEKINIST oral solution.

Important information you need to know before giving MEKINIST oral solution MEKINIST oral solution should only be given by a caregiver. Read this “Instructions for Use” carefully before you give MEKINIST oral solution for the first time and each time you get a refill. There may be new information.

This “Instructions for Use” does not take the place of talking with your healthcare provider about your or your child’s medical condition and treatment. You will receive the MEKINIST oral solution in an amber-colored bottle that your pharmacist has already mixed. If you receive MEKINIST as a powder, contact your healthcare provider or pharmacist right away.

Do not mix the MEKINIST powder on your own. Your pharmacist prepared the MEKINIST oral solution to an exact concentration. Do not add more water to the oral solution you receive from the pharmacy.

Your healthcare provider or pharmacist should show the caregiver how to measure and give a dose of MEKINIST oral solution correctly. Always give MEKINIST oral solution exactly as your healthcare provider tells you to. If you have any questions about how to measure and give a dose of MEKINIST oral solution, talk to your healthcare provider or pharmacist.

If at any time MEKINIST oral solution gets on your or your child’s skin, wash the area well with soap and water. If at any time MEKINIST oral solution gets in your or your child’s eyes, rinse the eyes well with cool water. Ask your healthcare provider or pharmacist about how to safely throw away (dispose of) MEKINIST oral solution.

When MEKINIST is prepared as an oral solution, it can be used for 35 days. Throw away any remaining oral solution after 35 days. If you spill any MEKINIST oral solution, follow the instructions at the end of this "Instructions for Use" in the section called “How to clean up any spilled MEKINIST oral solution.” The MEKINIST pack should contain: Reusable oral syringe parts: Storage of MEKINIST oral solution Store the amber bottle of MEKINIST oral solution at room temperature below 77°F (25°C).

Do not freeze MEKINIST oral solution. Store the amber bottle of MEKINIST oral solution upright with the cap tightly closed. Keep MEKINIST oral solution in the carton it comes in and away from direct moisture and light.

When MEKINIST is prepared as an oral solution, it can be used for 35 days. Throw away any remaining oral solution after 35 days. Do not use MEKINIST oral solution after the expiration or “discard after” date written or printed on the label by the pharmacist.

Keep MEKINIST oral solution and all medicines out of the reach of children. Storage of oral syringe Store the oral syringe with the MEKINIST oral solution. Keep oral syringe out of the reach of children.

Section A. Measuring and giving a dose of MEKINIST oral solution Gather your supplies: To give a dose of MEKINIST oral solution, you will need: 1 bottle adapter (already inserted into the bottle neck) 1 amber bottle containing MEKINIST oral solution 1 reusable oral syringe Call your healthcare provider or pharmacist if you do not have one or more of these items. If any of the MEKINIST oral solution comes into contact with your skin or eyes when you are following the steps below, follow the instructions in the section “ Important information you need to know before giving MEKINIST oral solution ” above.

If any MEKINIST oral solution spills, follow the instructions in the section “ How to clean up any spilled MEKINIST oral solution ” at the end of this "Instructions for Use." Step 1. Wash and dry your hands before measuring and giving a dose of MEKINIST oral solution. Step 2.

Place your supplies on a clean, flat work surface. Step 3. Check if you have powder or solution in the amber bottle.

I… [Excerpted — this section continues on DailyMed.]

📄 Recent Major Changes 7 words ▾

Warnings and Precautions ( 5.6 ) 5/2026

📄 Package Label / Principal Display Panel 161 words ▾

PRINCIPAL DISPLAY PANEL NDC 0078-1105-15 Mekinist ® (trametinib) Tablets 0.5 mg* Rx only 30 Tablets NOVARTIS PRINCIPAL DISPLAY PANEL NDC 0078-1105-15 Mekinist® (trametinib) Tablets 0.5 mg* Rx only 30 Tablets NOVARTIS

PRINCIPAL DISPLAY PANEL NDC 0078-1112-15 Mekinist ® (trametinib) Tablets 2 mg* Rx only 30 Tablets NOVARTIS PRINCIPAL DISPLAY PANEL NDC 0078-1112-15 Mekinist® (trametinib) Tablets 2 mg* Rx only 30 Tablets NOVARTIS

PRINCIPAL DISPLAY PANEL NDC 0078-1161-47 Rx only Mekinist ® (trametinib) for Oral Solution 0.05 mg per mL* 90 mL (when reconstituted) To Pharmacist: Reconstitute before dispensing*. Dispense with the enclosed Patient Information and Instructions for Use. For administration by caregivers only.

Discard any unused solution 35 days after reconstitution. NOVARTIS PRINCIPAL DISPLAY PANEL NDC 0078-1161-47 Rx only Mekinist® (trametinib) for Oral Solution 0.05 mg per mL* 90 mL (when reconstituted) To Pharmacist: Reconstitute before dispensing*. Dispense with the enclosed Patient Information and Instructions for Use.

For administration by caregivers only. Discard any unused solution 35 days after reconstitution. NOVARTIS

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicaid utilization & spend

📍 This exact package only: Medicaid data is reported per full 11-digit NDC — labeler, product and pack size — so every number here is for this package alone, not the drug overall. Other pack sizes report separately.
💊 Pharmacy benefit only: These are Medicaid outpatient pharmacy claims, billed by NDC. They exclude the medical benefit — clinic- or hospital-administered drugs billed under HCPCS J-codes — so drugs used mostly that way (e.g. Avastin, Lucentis, Keytruda) can look low or missing here. That’s expected, not an error.
📅 Q1 2025 – Q4 2025 · 4 quarters of data
ⓘ The newest quarter is usually incomplete when first published; states restate recent quarters in later CMS releases, so the latest figures typically revise upward. State coverage-policy changes can also shift quarter-to-quarter totals.
Prescriptions last 4 qtrs
1.2K
Units reimbursed last 4 qtrs
356.1K
Gross reimbursed last 4 qtrs
$7M
Avg / prescription
$6,089.19
Avg / unit
$19.6663
Latest quarter Q4 2025
320Rx
Fee-for-service vs managed care ⓘ
51% FFS 49% MCO
Fee-for-service · 591 Rx Managed care · 559 Rx
State Medicaid map
Alaska: no data reported AK Maine: no data reported ME Washington: 14,940 units · 191 per 100k residents WA Idaho: no data reported ID Montana: no data reported MT North Dakota: no data reported ND Minnesota: no data reported MN Wisconsin: 8,370 units · 142 per 100k residents WI Michigan: 16,590 units · 165 per 100k residents MI New York: 69,120 units · 353 per 100k residents NY Vermont: no data reported VT New Hampshire: no data reported NH Oregon: no data reported OR Nevada: no data reported NV Wyoming: no data reported WY South Dakota: no data reported SD Iowa: no data reported IA Illinois: 2,610 units · 20.8 per 100k residents IL Indiana: 14,400 units · 210 per 100k residents IN Ohio: 4,500 units · 38.2 per 100k residents OH Pennsylvania: 19,080 units · 147 per 100k residents PA New Jersey: 7,020 units · 75.6 per 100k residents NJ Massachusetts: no data reported MA California: 83,250 units · 214 per 100k residents CA Utah: no data reported UT Colorado: 11,610 units · 198 per 100k residents CO Nebraska: no data reported NE Missouri: 11,430 units · 184 per 100k residents MO Kentucky: no data reported KY West Virginia: no data reported WV Virginia: no data reported VA Maryland: 990 units · 16.0 per 100k residents MD Connecticut: no data reported CT Rhode Island: no data reported RI Arizona: 25,110 units · 338 per 100k residents AZ New Mexico: no data reported NM Kansas: no data reported KS Arkansas: no data reported AR Tennessee: no data reported TN North Carolina: 23,310 units · 215 per 100k residents NC South Carolina: no data reported SC Delaware: no data reported DE Oklahoma: no data reported OK Louisiana: no data reported LA Mississippi: no data reported MS Alabama: no data reported AL Georgia: 3,600 units · 32.6 per 100k residents GA D.C.: no data reported DC Hawaii: no data reported HI Texas: 13,140 units · 43.1 per 100k residents TX Florida: 27,000 units · 119 per 100k residents FL
Units reimbursed · per 100k residents
16.0353
gray = no data reported ⓘ
Colors are per 100,000 residents, so big states don’t automatically dominate. Tap or hover a state for its actual totals.
Tap or hover a state
…for its Medicaid breakdown
🏆 Top states by units · per 100k residents
1 New York 353 /100k
2 Arizona 338 /100k
3 North Carolina 215 /100k
4 California 214 /100k
5 Indiana 210 /100k
6 Colorado 198 /100k
7 Washington 191 /100k
8 Missouri 184 /100k
National units — by quarter
💵 About the dollar figures: “reimbursed” is what Medicaid paid pharmacies before confidential manufacturer rebates, so the program’s real net cost is lower than these numbers. Fee-for-service and managed-care claims are combined unless split above. Source: CMS State Drug Utilization Data; per-100k rates use 2023 Census population estimates.

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Mekinist — the program that covers self-administered drugs. 1 manufacturer.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Mekinist. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$81.4M
Claims incl. refills
5.2K
Beneficiaries
2.2K
Spend / beneficiary
$36,211.30
Spend / claim
$15,714.86
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) ✓ Available
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Novartis Pharmaceuticals Corporation. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Novartis Pharmaceuticals Corporation is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
← 00078-1154-21 · Novartis 00078-1168-61 · Novartis →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.