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ZYKADIA ceritinib 150 mg Tablet, Film Coated, 21-count — NDC 00078-0694-48 package photo

ZYKADIA ceritinib 150 mg Tablet, Film Coated, 21-count

by Novartis Pharmaceuticals Corporation · 21 TABLET, FILM COATED in 1 BOTTLE (0078-0694-48)
NDC 00078-0694-48
🏷️ FDA NDC (as labeled) 0078-0694-48 billing pads the labeler segment with a zero
This package
Contains21-count Pack sizes2 compare ↓
Also priced by: Part D plans $180.97/unit — full pricing hub ↓
Also comes in: 84 tablets 00078-0694-84
Rx only Brand On market Non-controlled
🗂️ Data synced 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

🆔 Identity & classification

FDA NDC (as labeled) 0078-0694-48
Product NDC 0078-0694
11-digit billing NDC 00078069448
RxCUI 2121059, 2121061
UNII K418KG2GET
Application # NDA211225
SPL Set ID fff5d805-4ffd-4e8e-8e63-6f129697563e
Established class (EPC) Kinase Inhibitor
Mechanism of action Tyrosine Kinase Inhibitors; Cytochrome P450 3A Inhibitors; Cytochrome P450 2C9 Inhibitors
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2019-03-18
Route ORAL
Dosage form TABLET, FILM COATED
Substance CERITINIB
GPI-14 21530514000330
GPI class Zykadia
GCN Seq No 079591
GCN 46119
HICL code 041111
Ingredient (HICL) Ceritinib
HIC1 code V
Therapeutic class — broad (HIC1) Neoplasms
HIC2 code V1
Therapeutic class — intermediate (HIC2) Antineoplastic Drugs
HIC3 code V1Q
Therapeutic class — specific (HIC3) Antineoplastic Systemic Enzyme Inhibitors
AHFS code 10:00.00.00
AHFS class Antineoplastic Agents
FDB label name ZYKADIA 150 MG TABLET
FDB brand name Zykadia
Legend status F — Federal legend — prescription drug or device
Why two NDCs? The FDA registers this code as 0078-0694-48 — 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 → 00078-0694-48. 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) Anaplastic lymphoma kinase (ALK) inhibitors
How it works Tyrosine Kinase Inhibitors, Cytochrome P450 2C9 Inhibitors, Cytochrome P450 3A 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.

🏭 Manufacturer & labeler

LabelerNovartis Pharmaceuticals Corporation
Application holderNOVARTIS PHARMACEUTICALS CORP
FDA applicationNDA211225 (NDA)
Labeler code00078
First marketedMar 2019
Product typeHuman Prescription Drug
Portfolio209 products on file
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.

🩺 Clinical

Label name ZYKADIA 150 MG TABLET Ingredient Ceritinib
📖 What it is MedlinePlus · NLM

Ceritinib is used to treat a certain type of non-small cell lung cancer (NSCLC) that has spread to other parts of the body. Ceritinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • Zykadia (ceritinib) is a targeted therapy for a specific type of lung cancer. It's prescribed when your lung cancer has spread (metastatic) and your tumor tests positive for a gene...
  • What exactly is Zykadia and why has my doctor prescribed it for me?
  • Yes, you should take Zykadia with food — that's the recommended way to take the tablet form. Eating when you take it helps reduce stomach side effects like nausea, vomiting, and di...
  • Do I need to take Zykadia with food, and does it matter what I eat?
📖 Read our full Ceritinib 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.

💊 What it looks like

Color Blue
ShapeRound
ImprintNVR;ZY1
Size9 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.

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

  • UNII OP1R32D61U
    Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
  • UNII M28OL1HH48
    Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
  • UNII L06K8R7DQK
    A synthetic blue dye approved by the FDA for use in medications and foods. It serves as a colorant to make pills and liquids visually distinct and easier to identify.
  • UNII RFW2ET671P
    Hydroxypropyl cellulose is a plant-derived thickening agent made from cellulose. It acts as a binder to hold tablet ingredients together and as a film-former to coat tablets or control how fast the medicine releases.
  • UNII 3NXW29V3WO
    Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
  • UNII 70097M6I30
    Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
  • UNII 3WJQ0SDW1A
    Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
  • UNII U725QWY32X
    Povidone K30 is a synthetic polymer made from petroleum. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in the stomach so the medicine can be absorbed.
  • UNII ETJ7Z6XBU4
    Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
  • UNII 7SEV7J4R1U
    A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
  • UNII 15FIX9V2JP
    Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.

11 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.

💲 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 eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $180.97 $3,800.42 / 21 tablets
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.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Zykadia 150 mgthis 00078-0694-48 Novartis 21 tablets — — 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

🏛️
2019
First FDA approval
Mar 2019
📍
2026
Currently FDA-listed
7 years listed
🛡️
2037
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 Dec 2037. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Mar 18, 2019 RLD RS ⏳ ~11.3 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 8703787 — method of use (U-1179)
US 12357630 — method of use (U-3096)
US 8377921 — method of use (U-1179)
US 7893074 — drug substance
US 8039479 — drug substance
US 8399450 — drug substance
US 7964592 — drug substance
US 9309229 — drug substance
2019 2021 2023 2025 2027 2029 2031 2033 2035 2037
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 (8)
PatentTypeUse codeExpires
US 8703787 ↗ Method of use U-1179 Feb 2, 2032
US 12357630 ↗ Method of use U-3096 Dec 13, 2037
US 8377921 ↗ Method of use U-1179 Nov 20, 2027
US 7893074 ↗ Drug substance — Apr 25, 2026
US 8039479 ↗ Drug substance — Jun 29, 2030
US 8399450 ↗ Drug substance — Nov 20, 2027
US 7964592 ↗ Drug substance — Apr 29, 2028
US 9309229 ↗ Drug substance — Jan 18, 2032
Common questions
Is there a generic version of ZYKADIA 150 MG TABLET?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for ZYKADIA 150 MG TABLET. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Dec 2037 — 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.

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

Medicare Part D (outpatient prescription) spending for Zykadia — 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 Zykadia. 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
$1.09M
Claims incl. refills
90
Beneficiaries
32
Spend / beneficiary
$34,210.66
Spend / claim
$12,163.79
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.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
00078-0694-48 You're viewing this 21 TABLET, FILM COATED in 1 BOTTLE (0078-0694-48) 2019-03-18 Active
00078-0694-84 84 TABLET, FILM COATED in 1 BOTTLE (0078-0694-84) 2019-03-18 Active

You're viewing the smallest of 2 pack sizes for this product.

Pack size FAQ

What quantity is in NDC 00078-0694-48?
NDC 00078-0694-48 is a 21-count package — 21 tablet, film coated in 1 bottle.
What is the difference between NDC 00078-0694-48 and NDC 00078-0694-84?
Both are ZYKADIA ceritinib 150 mg Tablet, Film Coated — the drug itself is identical. NDC 00078-0694-48 is the 21-count package, while NDC 00078-0694-84 is the 84 tablets package.
What NDC number is used to bill for this package of ZYKADIA ceritinib 150 mg Tablet, Film Coated?
Bill NDC 00078-0694-48 — the 11-digit billing format is 00078069448. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

🧭 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) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“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 FDA registers it as 0078-0694-48, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 00078-0694-48, written without dashes as 00078069448. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 00078-0694-48, the first segment (00078) is the labeler code FDA assigned to Novartis Pharmaceuticals Corporation; the middle segment (0694) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (48) identifies this exact package size and type. Together they name one specific package of one specific product.
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.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 84 tablets (00078-0694-84). Each has its own NDC and its own page — see the package list near the top of this page.
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.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. 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 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients
🎯 Indications and Usage 76 words ▾

1 INDICATIONS AND USAGE ZYKADIA ® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test [see Dosage and Administration (2.1)] . ZYKADIA is a kinase inhibitor indicated for the treatment of adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Recommended Dosage: 450 mg orally once daily with food. ( 2.2 )

2.1Patient Selection Select patients for treatment of metastatic NSCLC with ZYKADIA based on the presence of ALK positivity in tumor specimens [see Clinical Studies (14.1)] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics. 2.

2 Recommended Dosage The recommended dosage of ZYKADIA is 450 mg orally once daily with food until disease progression or unacceptable toxicity [see Clinical Pharmacology (12.3)] . If a dose of ZYKADIA is missed, make up that dose unless the next dose is due within 12 hours. If vomiting occurs during the course of treatment, do not administer an additional dose and continue with the next scheduled dose of ZYKADIA.

2. 3 Dosage Modifications for Adverse Reactions Table 1: Recommended ZYKADIA Dose Reductions Dose Reduction Recommended Dosage First-dose reduction 300 mg taken orally once daily with food Second-dose reduction 150 mg taken orally once daily with food Discontinue ZYKADIA for patients unable to tolerate 150 mg taken orally once daily with food. Dosage modifications for selected adverse reactions of ZYKADIA are provided in Table 2.

If dose reduction is required due to an adverse reaction not listed in Table 2, then reduce the daily dose of ZYKADIA by 150 mg. Table 2: Recommended ZYKADIA Dosage Modifications for Adverse Reactions Adverse Reaction ZYKADIA Dose Modification Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] Severe or intolerable nausea, vomiting, or diarrhea despite optimal antiemetic or anti-diarrheal therapy Withhold until improved, then resume ZYKADIA at the next lower dosage. Hepatotoxicity [see Warnings and Precautions (5.2)] ALT or AST elevation greater than 5 times ULN with total bilirubin elevation less than or equal to 2 times ULN Withhold until recovery to baseline or less than or equal to 3 times ULN, then resume ZYKADIA at the next lower dosage.

ALT or AST elevation greater than 3 times ULN with total bilirubin elevation greater than 2 times ULN in the absence of cholestasis or hemolysis Permanently discontinue ZYKADIA. Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.3)] Any Grade treatment-related ILD/pneumonitis Permanently discontinue ZYKADIA. QT Interval Prolongation [see Warnings and Precautions (5.4)] QTc interval greater than 500 msec on at least 2 separate ECGs Withhold until QTc interval is less than 481 msec or recovery to baseline if baseline QTc is greater than or equal to 481 msec, then resume ZYKADIA at the next lower dosage.

QTc interval prolongation in combination with torsades de pointes or polymorphic ventricular tachycardia or signs/symptoms of serious arrhythmia Permanently discontinue ZYKADIA. Hyperglycemia [see Warnings and Precautions (5.5)] Persistent hyperglycemia greater than 250 mg/dL despite optimal anti-hyperglycemic therapy Withhold until hyperglycemia is adequately controlled, then resume ZYKADIA at the next lower dosage. If adequate hyperglycemic control cannot be achieved with optimal medical management, discontinue ZYKADIA.

Bradycardia [see Warnings and Precautions (5.6)] Symptomatic bradycardia that is not life-threatening Withhold until recovery to asymptomatic bradycardia or to a heart rate of 60 bpm or above, evaluate concomitant medications known to cause bradycardia. If bradycardia cannot be attributed to another drug, resume ZYKADIA at the next lower dosage. Clinically significant bradycardia requiring intervention or life-threatening bradycardia in patients taking a concomitant medication also known to cause bradycardia or a medication known to cause hypotension Withhold until recovery to asymptomatic bradycardia or to a heart rate of 60 bpm or above.

If the concomitant medication can be adjusted or discontinued, resume ZYKADIA at the next lower dosage with frequent monitoring. Life-threatening bradycardi…

💊 Dosage Forms and Strengths 87 words ▾

3 DOSAGE FORMS AND STRENGTHS Capsules: 150 mg hard gelatin capsule with opaque blue cap and opaque white body containing a white to off-white powder. The opaque blue cap is marked in black ink with “LDK 150MG” and the opaque white body is marked in black ink with “NVR”. Tablets: 150 mg film-coated tablet, light blue, round, biconvex with beveled edges, without score, debossed with “NVR” on one side and “ZY1” on the other side.

Capsules: 150 mg ( 3 ) Tablets: 150 mg ( 3 )

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Gastrointestinal Adverse Reactions : ZYKADIA can cause gastrointestinal adverse reactions. If severe or intolerable, withhold if not responsive to antiemetics or antidiarrheals; upon improvement, resume ZYKADIA at a reduced dose. ( 2.3 , 5.1 ) Hepatotoxicity : ZYKADIA can cause hepatotoxicity.

Monitor liver laboratory tests at least monthly. Withhold then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.2 ) Interstitial Lung Disease/Pneumonitis : Occurred in 2.4% of patients.

Permanently discontinue ZYKADIA in patients diagnosed with treatment-related interstitial lung disease (ILD)/pneumonitis. ( 2.3 , 5.3 ) QT Interval Prolongation : ZYKADIA can cause QTc interval prolongation. Monitor electrocardiograms and electrolytes in patients with congestive heart failure, bradyarrhythmias, electrolyte abnormalities, or those who are taking medications that are known to prolong the QTc interval.

Withhold then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.4 ) Hyperglycemia : ZYKADIA can cause hyperglycemia. Monitor fasting glucose prior to treatment and periodically thereafter.

Initiate or optimize anti-hyperglycemic medications as indicated. Withhold, then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.5 ) Bradycardia : ZYKADIA can cause bradycardia.

Monitor heart rate and blood pressure regularly. Withhold, then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.6 ) Pancreatitis : Elevations of lipase and/or amylase and pancreatitis can occur.

Monitor lipase and amylase prior to treatment and periodically thereafter as clinically indicated. Withhold, then dose reduce ZYKADIA. ( 2.3 , 5.7 ) Embryo-Fetal Toxicity : ZYKADIA can cause fetal harm.

Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.8 , 8.1 , 8.3 )

5.1Gastrointestinal Adverse Reactions Severe gastrointestinal adverse reactions occurred in patients treated with ZYKADIA 750 mg under fasted conditions [see Adverse Reactions (6.1)] . Diarrhea, nausea, vomiting, or abdominal pain occurred in 95% of 925 patients, including severe cases (Grade 3 or 4) in 14% of patients treated with ZYKADIA across clinical studies. Diarrhea, nausea, vomiting, or abdominal pain leading to dose interruptions or reductions occurred in 36% of patients and leading to treatment discontinuation occurred in 1.6% of patients.

The incidence and severity of gastrointestinal adverse reactions were reduced for patients treated with ZYKADIA 450 mg with food in a dose optimization study (ASCEND-8). Diarrhea, nausea, vomiting, or abdominal pain occurred in 79% of 108 patients treated with ZYKADIA at the recommended dose of 450 mg with food. Of these, 53% were Grade 1 events and 24% were Grade 2 events.

One patient (0.9%) experienced Grade 3 diarrhea, and one patient (0.9%) experienced Grade 3 vomiting. One patient (0.9%) required dose adjustment due to vomiting. Eleven (10%) patients had diarrhea, nausea, vomiting, or abdominal pain that required at least one dose interruption.

Monitor and manage patients using standard of care, including antidiarrheals, antiemetics, or fluid replacement, as indicated. Withhold ZYKADIA if gastrointestinal adverse reaction is severe or intolerable and is not responsive to antiemetics or antidiarrheals. Upon improvement, resume ZYKADIA at a reduced dose [see Dosage and Administration (2.3)] .

5.2Hepatotoxicity Drug-induced hepatotoxicity occurred in patients treated with ZYKADIA [see Adverse Reactions (6.1)] . Elevations in alanine aminotransferase (ALT) > 5 times the upper limit of normal (ULN) occurred in 28% and elevations in aspartate aminotransferase (AST) > 5 times ULN occurred in 16% of 925 patients across clinical studies. Concurrent elevations in ALT > 3 times the ULN and total bilirubin > 2 times the ULN, with alkaline phosphatase < 2 times the ULN occurred in 0.3% of patients across clinical studies.

Approximately 1% of patients required…

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings and Precautions (5.2)] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.3)] QT Interval Prolongation [see Warnings and Precautions (5.4)] Hyperglycemia [see Warnings and Precautions (5.5)] Bradycardia [see Warnings and Precautions (5.6)] Pancreatitis [see Warnings and Precautions (5.7)] The most common adverse reactions (incidence of ≥ 25%) in patients treated with ZYKADIA 450 mg with food are diarrhea, nausea, abdominal pain, vomiting, and fatigue; and with ZYKADIA 750 mg under fasted conditions are diarrhea, nausea, vomiting, fatigue, abdominal pain, decreased appetite, and weight loss.

( 6 ) 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. The data in the Warnings and Precautions section reflect exposure to ZYKADIA 750 mg once daily under fasted conditions in 925 patients with ALK-positive NSCLC across seven clinical studies, including ASCEND-4 and ASCEND-1, described below, a randomized active-controlled study, two single arm studies, and two dose-escalation studies.

The majority of patients enrolled in these studies had received prior treatment with chemotherapy and/or crizotinib for NSCLC. Among these 925 patients, the most common adverse reactions (≥ 25% incidence) were diarrhea, nausea, vomiting, fatigue, abdominal pain, decreased appetite, and weight loss. Approximately 45% of patients initiating treatment with ZYKADIA 750 mg under fasted conditions had an adverse reaction that required at least one dose reduction and 66% of patients had an adverse reaction that required at least one dose interruption.

The median time to first dose reduction due to any reason was 7 weeks. Dose Optimization Study: Dosing Regimen of 450 mg Daily With Food In ASCEND-8, a dose optimization study, ZYKADIA 450 mg daily with food (N = 108) was compared to 750 mg daily under fasted conditions (N = 110) in both previously treated and untreated patients with ALK-positive NSCLC. The overall safety profile of ZYKADIA 450 mg with food was consistent with ZYKADIA 750 mg fasted, except for a reduction in gastrointestinal adverse reactions, while achieving comparable steady-state exposure [see Clinical Pharmacology (12.3)] .

The most common adverse reactions (≥ 25% incidence) in the 450 mg with food arm were diarrhea, nausea, abdominal pain, vomiting, and fatigue. The incidence and severity of gastrointestinal adverse reactions (diarrhea 59%, nausea 43%, and vomiting 38%) were reduced for patients treated with ZYKADIA 450 mg with food; Grade ≥ 3 adverse reactions were reported in two patients (1.9%): Grade 3 diarrhea and Grade 3 vomiting in one patient each [see Warnings and Precautions (5.1)] . In patients treated with ZYKADIA 450 mg with food, 24% of patients had an adverse reaction that required at least one dose reduction and 56% of patients had an adverse reaction that required at least one dose interruption.

The median time to first dose reduction due to any reason was 8 weeks. Previously Untreated ALK-Positive Metastatic NSCLC The safety of ZYKADIA was evaluated in ASCEND-4, an open-label, randomized, active-controlled multicenter study of 376 previously untreated ALK-positive NSCLC patients [see Clinical Studies (14.1)] . Patients received ZYKADIA 750 mg daily (N = 189) under fasted conditions or chemotherapy and maintenance chemotherapy (N = 187).

Chemotherapy regimens were pemetrexed (500 mg/m 2 ) and investigator’s…

🔄 Drug Interactions ~2 min read ▾

7 DRUG INTERACTIONS CYP3A Inhibitors and Inducers : Avoid concurrent use of ZYKADIA with strong CYP3A inhibitors or inducers. If concurrent use of a strong CYP3A inhibitor is unavoidable, dose reduce ZYKADIA. ( 2.4 , 7.1 ) CYP3A Substrates : Avoid coadministration of ZYKADIA with sensitive CYP3A substrates.

( 7.2 ) CYP2C9 Substrates : Avoid coadministration of ZYKADIA with CYP2C9 substrates for which minimal concentration changes may lead to serious toxicities. ( 7.2 )

7.1Effect of Other Drugs on ZYKADIA Strong CYP3A Inhibitors A strong CYP3A4/P-gp inhibitor (ketoconazole) increased the systemic exposure of ceritinib [see Clinical Pharmacology (12.3)] , which may increase the incidence and severity of adverse reactions of ZYKADIA. Avoid concurrent use of strong CYP3A inhibitors during treatment with ZYKADIA. If concurrent use of strong CYP3A inhibitors is unavoidable, reduce the ZYKADIA dose [see Dosage and Administration (2.4)] .

Do not consume grapefruit and grapefruit juice as they may inhibit CYP3A. Strong CYP3A Inducers A strong CYP3A4/P-gp inducer (rifampin) decreased the systemic exposure of ceritinib [see Clinical Pharmacology (12.3)] , which may decrease the efficacy of ZYKADIA. Avoid concurrent use of strong CYP3A inducers during treatment with ZYKADIA.

7.2Effect of ZYKADIA on Other Drugs CYP3A Substrates Ceritinib increased the systemic exposure of a sensitive CYP3A substrate (midazolam) [see Clinical Pharmacology (12.3)] . Avoid coadministration of ZYKADIA with sensitive CYP3A substrates. If concomitant use is unavoidable, consider dose reduction of the sensitive CYP3A substrate(s).

If ZYKADIA is coadministered with other CYP3A substrates, refer to the CYP3A substrate labeling for dosage recommendation with strong CYP3A inhibitors. CYP2C9 Substrates Ceritinib increased the systemic exposure of a CYP2C9 substrate (warfarin) [see Clinical Pharmacology (12.3)] . Increase the frequency of INR monitoring if coadministration with warfarin is unavoidable as the anti-coagulant effect of warfarin may be enhanced.

Avoid coadministration of ZYKADIA with CYP2C9 substrates for which minimal concentration changes may lead to serious toxicities. If concomitant use of such CYP2C9 substrates is unavoidable, consider dose reduction for the coadministered CYP2C9 substrates.

7.3Drugs That Prolong QT Interval ZYKADIA causes concentration-dependent increases in the QTc interval. When possible, avoid coadministration of ZYKADIA with other products with a known potential to prolong the QTc interval [see Warnings and Precautions (5.4), Clinical Pharmacology (12.2)] .

7.4Drugs That Cause Bradycardia ZYKADIA can cause bradycardia. When possible, avoid coadministration of ZYKADIA with other products known to cause bradycardia [see Warnings and Precautions (5.6), Clinical Pharmacology (12.2)] .

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 ) Severe Hepatic Impairment : For patients with severe hepatic impairment (Child-Pugh C), dose reduce ZYKADIA. ( 8.6 )

8.1Pregnancy Risk Summary Based on animal studies and its mechanism of action [see Clinical Pharmacology (12.1)] , ZYKADIA can cause fetal harm when administered to a pregnant woman. The limited available data on the use of ZYKADIA in pregnant women are insufficient to inform a risk. Administration of ceritinib to rats and rabbits during the period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits ( see Data ).

Advise a pregnant woman 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 are 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study in which pregnant rats were administered daily doses of ceritinib during organogenesis, dose-related skeletal anomalies were observed at doses as low as 50 mg/kg (less than 0.5-fold the human exposure by AUC at the recommended dose).

Findings included delayed ossifications and skeletal variations. In pregnant rabbits administered ceritinib daily during organogenesis, dose-related skeletal anomalies, including incomplete ossification, were observed at doses equal to or > 2 mg/kg/day (approximately 0.015-fold the human exposure by AUC at the recommended dose). A low incidence of visceral anomalies, including absent or malpositioned gallbladder and retroesophageal subclavian cardiac artery, was observed at doses equal to or > 10 mg/kg/day (approximately 0.13-fold the human exposure by AUC at the recommended dose).

Maternal toxicity and abortion occurred in rabbits at doses of 35 mg/kg or greater. In addition, embryolethality was observed in rabbits at a dose of 50 mg/kg. 8.

2 Lactation Risk Summary There are no data regarding the presence of ceritinib or its metabolites in human milk, the effects of ceritinib on the breastfed child or its effects on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with ZYKADIA and for 2 weeks following completion of therapy.

8.3Females and Males of Reproductive Potential Pregnancy Testing Verify pregnancy status in females of reproductive potential prior to initiating ZYKADIA [see Use in Specific Populations (8.1)] . Contraception ZYKADIA can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1)] . Females Advise females of reproductive potential to use effective contraception during treatment with ZYKADIA and for 6 months following completion of therapy.

Males Based on the potential for genotoxicity, advise males with female partners of reproductive potential to use condoms during treatment with ZYKADIA and for 3 months following completion of therapy [see Nonclinical Toxicology (13.1)] .

8.4Pediatric Use The safety and effectiveness of ZYKADIA in pediatric patients have not been established.

8.5Geriatric Use Of the 925 patients in clinical studies of ZYKADIA, 18% were 65 years or older, while 5% were 75 years or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects.

8.6Hepatic Impairment For patients with severe hepatic impairment (Child-Pugh C), reduce the dose of ZYKADIA [see Dosage and Administration (2.5)] . No dose adjustment is recommended for patients with mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment.

🤰 Pregnancy ~1 min read ▾

8.1Pregnancy Risk Summary Based on animal studies and its mechanism of action [see Clinical Pharmacology (12.1)] , ZYKADIA can cause fetal harm when administered to a pregnant woman. The limited available data on the use of ZYKADIA in pregnant women are insufficient to inform a risk. Administration of ceritinib to rats and rabbits during the period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits ( see Data ).

Advise a pregnant woman 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 are 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study in which pregnant rats were administered daily doses of ceritinib during organogenesis, dose-related skeletal anomalies were observed at doses as low as 50 mg/kg (less than 0.5-fold the human exposure by AUC at the recommended dose).

Findings included delayed ossifications and skeletal variations. In pregnant rabbits administered ceritinib daily during organogenesis, dose-related skeletal anomalies, including incomplete ossification, were observed at doses equal to or > 2 mg/kg/day (approximately 0.015-fold the human exposure by AUC at the recommended dose). A low incidence of visceral anomalies, including absent or malpositioned gallbladder and retroesophageal subclavian cardiac artery, was observed at doses equal to or > 10 mg/kg/day (approximately 0.13-fold the human exposure by AUC at the recommended dose).

Maternal toxicity and abortion occurred in rabbits at doses of 35 mg/kg or greater. In addition, embryolethality was observed in rabbits at a dose of 50 mg/kg.

🧒 Pediatric Use 16 words ▾

8.4Pediatric Use The safety and effectiveness of ZYKADIA in pediatric patients have not been established.

🧓 Geriatric Use 40 words ▾

8.5Geriatric Use Of the 925 patients in clinical studies of ZYKADIA, 18% were 65 years or older, while 5% were 75 years or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK.

Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays. Ceritinib inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice and rats. Ceritinib exhibited dose-dependent anti-tumor activity in mice bearing EML4-ALK-positive NSCLC xenografts with demonstrated resistance to crizotinib, at concentrations within a clinically relevant range.

12.2Pharmacodynamics Cardiac Electrophysiology Twelve of 919 patients (1.3%) treated with ZYKADIA 750 mg once daily under fasted conditions with at least one post-baseline ECG assessment were found to have a QTc > 500 msec and 58 patients (6%) had an increase from baseline QTc > 60 msec. In ASCEND-4, a central tendency analysis of the QTc data at average steady-state concentrations demonstrated that the upper bound of the 2-sided 90% CI for QTc was 15.3 msec at ZYKADIA 750 mg once daily under fasted conditions. A pharmacokinetic/pharmacodynamic analysis suggested concentration-dependent QTc interval prolongation [see Warnings and Precautions (5.4)] .

Ten of 925 patients (1.1%) had bradycardia defined as < 50 beats per minute [see Warnings and Precautions (5.6)] .

12.3Pharmacokinetics After a single oral administration of ZYKADIA in patients, AUC and C max increased dose proportionally over 50 mg to 750 mg under fasted conditions. Following ZYKADIA 750 mg once daily under fasted conditions, steady state was reached by 15 days with a geometric mean accumulation ratio of 6.2 after 3 weeks. Systemic exposure increased in a greater than dose proportional manner after repeat doses of 50 mg to 750 mg once daily under fasted conditions.

Absorption After a single oral administration of ZYKADIA in patients, peak plasma levels (C max ) of ceritinib were achieved around 4 to 6 hours. Food Effect A food effect study conducted in healthy subjects with a single 500 mg dose of ZYKADIA capsules showed that a high-fat meal (containing approximately 1000 calories and 58 grams of fat) increased ceritinib AUC by 73% and C max by 41% and a low-fat meal (containing approximately 330 calories and 9 grams of fat) increased ceritinib AUC by 58% and C max by 43% as compared with the fasted conditions.

A food effect study conducted in healthy subjects with a single 750 mg dose of ZYKADIA tablets showed that a high-fat meal (containing approximately 1000 calories and 58 grams of fat) increased ceritinib AUC by 64% and C max by 58% and a low-fat meal (containing approximately 330 calories and 9 grams of fat) increased ceritinib AUC by 39% and C max by 42% as compared with the fasted conditions. Dose Optimization Study: Dosing Regimen of 450 mg Daily With Food In a dose optimization study (ASCEND-8) in patients receiving 450 mg dose of ZYKADIA capsules daily with food (approximately 100 to 500 calories and 1.5 to 15 grams of fat) or 750 mg daily under fasted conditions, there was no clinically meaningful difference in the systemic steady-state exposure of ceritinib (AUC) between the 450 mg with food arm and the 750 mg fasted arm.

Distribution Ceritinib is 97% bound to human plasma proteins, independent of drug concentration. The geometric mean apparent volume of distribution (V d /F) is 4230 L following a single 750 mg ZYKADIA dose under fasted conditions in patients. Ceritinib also has a slight preferential distribution to red blood cells, relative to plasma, with a mean in vitro blood-to-plasma ratio o…

🧬 Mechanism of Action 122 words ▾

12.1Mechanism of Action Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK.

Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays. Ceritinib inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice and rats. Ceritinib exhibited dose-dependent anti-tumor activity in mice bearing EML4-ALK-positive NSCLC xenografts with demonstrated resistance to crizotinib, at concentrations within a clinically relevant range.

📦 How Supplied / Storage and Handling 124 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING ZYKADIA 150 mg capsules Hard gelatin capsule with opaque blue cap and opaque white body; opaque blue cap marked in black ink with “LDK 150MG”, opaque white body marked in black ink with “NVR”. Available in: Bottles of 70 capsules…………………………………………………………………………………….NDC 0078-0640-70 Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. ZYKADIA 150 mg tablets Film-coated tablet, light blue, round, biconvex with beveled edges, without score, debossed with “NVR” on one side and “ZY1” on the other side.

Available in: Bottles of 84 tablets…………………………………………………………………………………NDC 0078-0694-84 Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

📋 Description 159 words ▾

11 DESCRIPTION Ceritinib is a kinase inhibitor for oral administration. The molecular formula for ceritinib is C 28 H 36 N 5 O 3 ClS. The molecular weight is 558.14 g/mol.

Ceritinib is described chemically as 5-Chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine. The chemical structure of ceritinib is shown below: Ceritinib is a white to almost white or light yellow powder. ZYKADIA is supplied as printed hard-gelatin capsules containing 150 mg of ceritinib and the following inactive ingredients: colloidal silicon dioxide, hard gelatin capsule shells, low substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate.

The capsule shell is composed of FD&C Blue # 2, gelatin, and titanium dioxide. ZYKADIA is supplied as film-coated tablets containing 150 mg of ceritinib and the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, low-substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose and povidone. The tablet coating contains FD&C Blue # 2 aluminum lake, hypromellose, polyethylene glycol 4000, talc, and titanium dioxide.

The chemical structure of ceritinib.

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information) . Gastrointestinal Adverse Reactions Inform patients that diarrhea, nausea, vomiting, and abdominal pain are the most commonly reported gastrointestinal adverse reactions. Inform patients of supportive care options, such as antiemetic and anti-diarrheal medications.

Advise patients to contact their healthcare provider for severe or intolerable gastrointestinal symptoms. Inform patients that if vomiting occurs during the course of treatment, they should not take an additional dose, but should continue with the next scheduled dose of ZYKADIA [see Warnings and Precautions (5.1)] . Hepatotoxicity Inform patients of the signs and symptoms of hepatotoxicity.

Advise patients to contact their healthcare provider immediately for signs or symptoms of hepatotoxicity [see Warnings and Precautions (5.2)] . Interstitial Lung Disease/Pneumonitis Inform patients of the risks of severe or fatal ILD/pneumonitis. Advise patients to contact their healthcare provider immediately to report new or worsening respiratory symptoms [see Warnings and Precautions (5.3)] .

Arrhythmias Inform patients of the risks of QTc interval prolongation and bradycardia. Advise patients to contact their healthcare provider immediately to report new chest pain or discomfort, changes in heartbeat, palpitations, dizziness, lightheadedness, fainting, and changes in or new use of heart or blood pressure medications [see Warnings and Precautions (5.4, 5.6)] . Hyperglycemia Inform patients of the signs and symptoms of hyperglycemia.

Advise patients to contact their healthcare provider immediately for signs or symptoms of hyperglycemia [see Warnings and Precautions (5.5)] . Pancreatitis Inform patients of the signs and symptoms of pancreatitis and the need to monitor lipase and amylase levels prior to the start of treatment and periodically thereafter as clinically indicated [see Warnings and Precautions (5.7)] . Photosensitivity Inform patients of the signs and symptoms of photosensitivity.

Advise patients to avoid prolonged sun exposure and to use sunscreen or protective clothing during treatment with ZYKADIA [see Adverse Reactions (6.1)] . Embryo-Fetal Toxicity Advise pregnant women and females of reproductive potential of the potential risk to a fetus and to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions (5.8), Use in Specific Populations (8.3)] . Advise females of reproductive potential to use effective contraception during treatment with ZYKADIA and for 6 months following completion of therapy [see Use in Specific Populations (8.3)] .

Advise males with female partners of reproductive potential to use condoms during treatment with ZYKADIA and for 3 months following completion of therapy [see Use in Specific Populations (8.3), Nonclinical Toxicology (13.1)] . Lactation Advise women not to breastfeed during treatment with ZYKADIA and for 2 weeks following completion of therapy [see Use in Specific Populations (8.2)]. Drug Interactions Inform patients not to consume grapefruit and grapefruit juice during treatment with ZYKADIA [see Drug Interactions (7.1)] .

Dosing Instructions Advise patients to take ZYKADIA with food [see Dosage and Administration (2.2)] . Advise patients to make up a missed dose of ZYKADIA unless the next dose is due within 12 hours [see Dosage and Administration (2.2)] . Distributed by: Novartis Pharmaceuticals Corporation East Hanover, New Jersey 07936 © Novartis T2021-132

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