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Ayvakit avapritinib 100 mg Tablet, Film Coated, 30-count — NDC 72064-0110-30 package photo

Ayvakit avapritinib 100 mg Tablet, Film Coated, 30-count

by Blueprint Medicines Corporation · 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72064-110-30)
NDC 72064-0110-30
🏷️ FDA NDC (as labeled) 72064-110-30 billing pads the product segment with a zero
Rx only Brand On market Non-controlled
🗂️ Data synced Sep 17, 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) 72064-110-30
Product NDC 72064-110
11-digit billing NDC 72064011030
NCPDP billing unit EA — each (per item)
RxCUI 2272112, 2272118, 2272120, 2272122, 2272124, 2272126, 2559723, 2559725,
UNII 513P80B4YJ
UPC 0372064125303, 0372064150305, 0372064110309, 0372064130307
Application # NDA212608
SPL Set ID 645c887c-8cd4-4623-8da9-ac223d71a8b9
Established class (EPC) Kinase Inhibitor
Mechanism of action Tyrosine Kinase Inhibitors; Cytochrome P450 2C9 Inhibitors; P-Glycoprotein Inhibitors; Breast Cancer Resistance Protein Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Multidrug and Toxin Extrusion Transporter 2 K Inhibitors; Bile Salt Export Pump Inhibitors
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2020-01-09
Route ORAL
Dosage form TABLET, FILM COATED
Substance AVAPRITINIB
GCN Seq No 080619
GCN 47516
HICL code 046291
Ingredient (HICL) Avapritinib
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 AYVAKIT 100 MG TABLET
FDB brand name Ayvakit
Legend status F — Federal legend — prescription drug or device
Why two NDCs? The FDA registers this code as 72064-110-30 — a 5-3-2 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 product segment → 72064-0110-30. 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) Other protein kinase inhibitors
How it works Tyrosine Kinase Inhibitors, P-Glycoprotein Inhibitors, Cytochrome P450 2C9 Inhibitors, Breast Cancer Resistance Protein 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

LabelerBlueprint Medicines Corporation
Application holderBLUEPRINT MEDICINES CORP
FDA applicationNDA212608 (NDA)
Labeler code72064
First marketedJan 2020
Product typeHuman Prescription Drug
Portfolio5 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 AYVAKIT 100 MG TABLET Ingredient Avapritinib
📖 What it is MedlinePlus · NLM

Avapritinib is used to treat a certain type of gastrointestinal stromal tumor (GIST; a type of tumor that grows in the wall of the stomach, intestine [bowel], or esophagus [tube that connects the throat with the stomach]) in adults that has spread to other parts of the body or that cannot be removed by surgery. It is also used to treat certain types of mastocytosis (a blood disorder in which there are too many mast cells [a certain kind of white blood cell]). Avapritinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals...

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • Ayvakit is not traditional chemotherapy. It's what's called a targeted therapy — a drug designed to zero in on specific mutant proteins (KIT and PDGFRA) that are driving your tumor...
  • What exactly is Ayvakit treating — is it chemotherapy?
  • Yes, timing really matters here. You need to take Ayvakit on an empty stomach — at least 1 hour before eating or 2 hours after your last meal. A high-fat meal can raise the amount...
  • Does it matter when I take it — can I take it with breakfast?
📖 Read our full Avapritinib 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 White / white
ShapeRound
ImprintBLU;50
Size6 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 5138Q19F1X
    Ammonia is a colorless gas made from nitrogen and hydrogen. It's used in medicines as a pH buffer to maintain the correct acidity level and help keep the product stable.
  • UNII 8PJ61P6TS3
    Butyl alcohol is a clear liquid organic solvent derived from petroleum or natural sources. In medicines, it helps dissolve active ingredients and serves as a solvent in liquid formulations and some topical products.
  • UNII D9C330MD8B
    Copovidone is a synthetic polymer made by combining two types of plastic-like molecules. It acts as a binder and film-former to help hold tablet ingredients together and improve how the medicine dissolves in your body.
  • 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 H3R47K3TBD
    FD&C Blue No. 1 is a synthetic blue dye approved for use in foods and medicines. It serves as a colorant to give the medication its distinctive appearance and help with product identification.
  • UNII XM0M87F357
    A dark iron oxide compound that gives medicines their black or dark color. It's used as a colorant in tablets and capsules to help identify the product and make it visually distinctive.
  • UNII ND2M416302
    Isopropyl alcohol is a clear liquid solvent derived from petroleum. In medicines, it dissolves active ingredients and other components, helps the product flow smoothly, and aids in sterilization during manufacturing.
  • 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 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 7T9FYH5QMK
    A plant-derived powder that serves as a binder and filler in tablets and capsules. It helps hold ingredients together, adds bulk, and aids in smooth tablet disintegration when swallowed.
  • UNII 4R4HFI6D95
    Polyethylene glycol 4000 is a synthetic polymer derived from petroleum. It serves as a binder, filler, and lubricant in solid dosage forms, and helps control how quickly the medicine dissolves.
  • UNII 660SZ0AKDA
    Polyvinyl alcohol is a synthetic polymer made by chemically treating polyvinyl acetate. It serves as a binder and film-forming agent in tablets and capsules, helping hold ingredients together and create protective coatings.
  • UNII 6DC9Q167V3
    Propylene glycol is a clear liquid derived from petroleum or vegetable sources. It acts as a solvent, humectant, and preservative in medicines, helping dissolve active ingredients and maintain product stability.
  • UNII 46N107B71O
    Shellac is a natural resin secreted by the lac beetle. It's used as a coating on tablets and capsules to control how quickly the medicine dissolves and to improve appearance and stability.
  • 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.

16 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 $1,432.96 $42,988.82 / 30 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
Ayvakit 100 mgthis 72064-0110-30 Blueprint 30 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

🏛️
2020
First FDA approval
Jan 2020
📍
2026
Currently FDA-listed
6 years listed
🛡️
2042
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 Mar 2042. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Jan 9, 2020 RLD RS ⏳ ~15.5 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 9944651 — drug substance (U-2726)
US 9994575 — drug substance (U-2726)
US 9200002 — drug substance (U-2726)
US 9994575 — drug substance (U-2726)
US 9200002 — drug substance (U-2726)
US 9944651 — drug substance (U-2726)
US 9944651 — drug substance (U-2726)
US 9994575 — drug substance (U-2726)
US 9200002 — drug substance (U-2726)
US 11999744 — method of use (U-3168)
US 11999744 — method of use (U-3168)
US 11999744 — method of use (U-3168)
US 11999744 — method of use (U-3168)
US 11999744 — method of use (U-3506)
US 9200002 — drug substance (U-3168)
US 9200002 — drug substance (U-3168)
US 9200002 — drug substance (U-3168)
US 9200002 — drug substance (U-3168)
US 12060354 — method of use (U-2726)
US 12060354 — method of use (U-2726)
US 12060354 — method of use (U-2726)
US 12252494 — method of use (U-3506)
US 9944651 — drug substance (U-3168)
US 9944651 — drug substance (U-3168)
US 9944651 — drug substance (U-3168)
US 9944651 — drug substance (U-3168)
US 9994575 — drug substance (U-3168)
US 9994575 — drug substance (U-3168)
US 9994575 — drug substance (U-3168)
US 9994575 — drug substance (U-3168)
US 9944651 — drug substance (U-3506)
US 9994575 — drug substance (U-3506)
US 9200002 — drug substance (U-3506)
US 11827642 — drug substance (U-3506)
US 11964980 — drug substance
US 11964980 — drug substance
US 11964980 — drug substance
US 11964980 — drug substance
US 11964980 — drug substance
Exclusivity ODE-356
Exclusivity ODE-366
Exclusivity ODE-434
Exclusivity ODE-356
Exclusivity ODE-366
Exclusivity ODE-434
Exclusivity ODE-356
Exclusivity ODE-366
Exclusivity ODE-434
Exclusivity I-912
Exclusivity ODE-356
Exclusivity ODE-366
Exclusivity ODE-434
Exclusivity ODE-356
Exclusivity ODE-366
Exclusivity ODE-434
2020 2022 2024 2026 2028 2030 2032 2034 2036 2038 2040 2042
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 (39)
PatentTypeUse codeExpires
US 9944651 ↗ Drug substance U-2726 Oct 15, 2034
US 9994575 ↗ Drug substance U-2726 Oct 15, 2034
US 9200002 ↗ Drug substance U-2726 Oct 15, 2034
US 9994575 ↗ Drug substance U-2726 Oct 15, 2034
US 9200002 ↗ Drug substance U-2726 Oct 15, 2034
US 9944651 ↗ Drug substance U-2726 Oct 15, 2034
US 9944651 ↗ Drug substance U-2726 Oct 15, 2034
US 9994575 ↗ Drug substance U-2726 Oct 15, 2034
US 9200002 ↗ Drug substance U-2726 Oct 15, 2034
US 11999744 ↗ Method of use U-3168 Apr 10, 2040
US 11999744 ↗ Method of use U-3168 Apr 10, 2040
US 11999744 ↗ Method of use U-3168 Apr 10, 2040
US 11999744 ↗ Method of use U-3168 Apr 10, 2040
US 11999744 ↗ Method of use U-3506 Apr 10, 2040
US 9200002 ↗ Drug substance U-3168 Oct 15, 2034
US 9200002 ↗ Drug substance U-3168 Oct 15, 2034
US 9200002 ↗ Drug substance U-3168 Oct 15, 2034
US 9200002 ↗ Drug substance U-3168 Oct 15, 2034
US 12060354 ↗ Method of use U-2726 Mar 8, 2042
US 12060354 ↗ Method of use U-2726 Mar 8, 2042
US 12060354 ↗ Method of use U-2726 Mar 8, 2042
US 12252494 ↗ Method of use U-3506 Apr 10, 2040
US 9944651 ↗ Drug substance U-3168 Oct 15, 2034
US 9944651 ↗ Drug substance U-3168 Oct 15, 2034
US 9944651 ↗ Drug substance U-3168 Oct 15, 2034
US 9944651 ↗ Drug substance U-3168 Oct 15, 2034
US 9994575 ↗ Drug substance U-3168 Oct 15, 2034
US 9994575 ↗ Drug substance U-3168 Oct 15, 2034
US 9994575 ↗ Drug substance U-3168 Oct 15, 2034
US 9994575 ↗ Drug substance U-3168 Oct 15, 2034
US 9944651 ↗ Drug substance U-3506 Oct 15, 2034
US 9994575 ↗ Drug substance U-3506 Oct 15, 2034
US 9200002 ↗ Drug substance U-3506 Oct 15, 2034
US 11827642 ↗ Drug substance U-3506 Oct 15, 2034
US 11964980 ↗ Drug substance — Apr 10, 2040
US 11964980 ↗ Drug substance — Apr 10, 2040
US 11964980 ↗ Drug substance — Apr 10, 2040
US 11964980 ↗ Drug substance — Apr 10, 2040
US 11964980 ↗ Drug substance — Apr 10, 2040
FDA exclusivity
CodeWhat it grantsExpires
ODE-356Orphan Drug Exclusivity (7-year)Jun 16, 2028
ODE-366Orphan Drug Exclusivity (7-year)Jan 9, 2027
ODE-434Orphan Drug Exclusivity (7-year)May 22, 2030
ODE-356Orphan Drug Exclusivity (7-year)Jun 16, 2028
ODE-366Orphan Drug Exclusivity (7-year)Jan 9, 2027
ODE-434Orphan Drug Exclusivity (7-year)May 22, 2030
ODE-356Orphan Drug Exclusivity (7-year)Jun 16, 2028
ODE-366Orphan Drug Exclusivity (7-year)Jan 9, 2027
ODE-434Orphan Drug Exclusivity (7-year)May 22, 2030
I-912New indication (3-year)May 22, 2026
ODE-356Orphan Drug Exclusivity (7-year)Jun 16, 2028
ODE-366Orphan Drug Exclusivity (7-year)Jan 9, 2027
ODE-434Orphan Drug Exclusivity (7-year)May 22, 2030
ODE-356Orphan Drug Exclusivity (7-year)Jun 16, 2028
ODE-366Orphan Drug Exclusivity (7-year)Jan 9, 2027
ODE-434Orphan Drug Exclusivity (7-year)May 22, 2030
Common questions
Is there a generic version of AYVAKIT 100 MG TABLET?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for AYVAKIT 100 MG TABLET. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Mar 2042 — 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 Ayvakit — 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 Ayvakit. 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
$76.68M
Claims incl. refills
1.8K
Beneficiaries
680
Spend / beneficiary
$112,768.65
Spend / claim
$42,507.03
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.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Ayvakit (this brand).

Top reported reactions

Fatigue1,735
Nausea1,218
Diarrhoea1,007
Headache568
Dizziness537
Swelling Face528
Vomiting518

Age at onset

Infant1
Child87
Adolescent58
Adult3,893
Elderly3,863

Reporter sex

12,039 reports
Male · 42%
Female · 58%

Serious outcomes

Hospitalization1,146
Life-threatening33
Reports over time (by year) — tap or hover for the count & year
2022 2023 2024 2026 2,496 1,207
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
72064-0110-30 You're viewing this 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72064-110-30) 2020-01-09 Active

🧭 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?
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📄 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 📦 Storage and Handling 📋 Description 💬 Information for Patients
🎯 Indications and Usage ~1 min read ▾

1 INDICATIONS AND USAGE AYVAKIT is a kinase inhibitor indicated for: Gastrointestinal Stromal Tumor (GIST) the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations. ( 1.1 , 2.2 ) Advanced Systemic Mastocytosis (AdvSM) the treatment of adult patients with AdvSM. AdvSM includes patients with aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia (MCL).

( 1.2 ) Limitations of Use: AYVAKIT is not recommended for the treatment of patients with AdvSM with platelet counts of less than 50 × 10 9 /L ( 1.2 ) Indolent Systemic Mastocytosis (ISM) the treatment of adult patients with ISM. ( 1.3 ) Limitations of Use: AYVAKIT is not recommended for the treatment of patients with ISM with platelet counts of less than 50 × 10 9 /L ( 1.2 )

1.1PDGFRA Exon 18 Mutation-Positive Unresectable or Metastatic Gastrointestinal Stromal Tumor (GIST) AYVAKIT ® is indicated for the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations [see Dosage and Administration (2.2) ] .

1.2Advanced Systemic Mastocytosis (AdvSM) AYVAKIT is indicated for the treatment of adult patients with advanced systemic mastocytosis (AdvSM). AdvSM includes patients with aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia (MCL). Limitations of Use : AYVAKIT is not recommended for the treatment of patients with AdvSM with platelet counts of less than 50 × 10 9 /L [see Warnings and Precautions (5.1) ] .

1.3Indolent Systemic Mastocytosis (ISM) AYVAKIT is indicated for the treatment of adult patients with indolent systemic mastocytosis (ISM). Limitations of Use : AYVAKIT is not recommended for the treatment of patients with ISM with platelet counts of less than 50 × 10 9 /L [see Warnings and Precautions (5.1) ] .

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION GIST: Select patients for treatment with AYVAKIT based on the presence of a PDGFRA exon 18 mutation. ( 2.2 ) GIST: The recommended dosage is 300 mg orally once daily. ( 2.2 ) AdvSM: The recommended dosage is 200 mg orally once daily. ( 2.3 ) ISM: The recommended dosage is 25 mg orally once daily. ( 2.4 ) Patients with severe hepatic impairment (Child-Pugh Class C): reduce dose of AYVAKIT. ( 2.7 )

2.1Recommended Administration Administer AYVAKIT orally on an empty stomach, at least 1 hour before or 2 hours after a meal [see Clinical Pharmacology (12.3) ] . Do not make up for a missed dose within 8 hours of the next scheduled dose. Do not repeat dose if vomiting occurs after AYVAKIT but continue with the next scheduled dose.

2.2GIST Harboring PDGFRA Exon 18 Mutations Select patients for treatment with AYVAKIT based on the presence of a PDGFRA exon 18 mutation [see Clinical Studies (14.1) ] . An FDA-approved test for the detection of exon 18 mutations is not currently available. The recommended dosage of AYVAKIT is 300 mg orally once daily in patients with GIST . Continue treatment until disease progression or unacceptable toxicity.

2.3Advanced Systemic Mastocytosis The recommended dosage of AYVAKIT is 200 mg orally once daily in patients with AdvSM. Continue treatment until disease progression or unacceptable toxicity.

2.4Indolent Systemic Mastocytosis The recommended dosage of AYVAKIT is 25 mg orally once daily in patients with ISM.

2.5Dosage Modifications for Adverse Reactions The recommended dosage reductions and modifications for adverse reactions are provided in Tables 1 and 2. Table 1: Recommended Dosage Reductions for AYVAKIT for Adverse Reactions Dose Reduction Level Dosage in patients with GIST Permanently discontinue AYVAKIT in patients with GIST who are unable to tolerate a dose of 100 mg once daily. Dosage in patients with AdvSM Permanently discontinue AYVAKIT in patients with AdvSM who are unable to tolerate a dose of 25 mg once daily.

First dose reduction 200 mg once daily 100 mg once daily Second dose reduction 100 mg once daily 50 mg once daily Third dose reduction - 25 mg once daily Table 2: Recommended Dosage Modifications for AYVAKIT for Adverse Reactions Adverse Reaction Severity Severity as defined by the National Cancer Institute Common Terminology Criteria for Adverse Events version

5.0Dosage Modification Patients with GIST or AdvSM Intracranial Hemorrhage [see Warnings and Precautions (5.1) ] Any grade Permanently discontinue AYVAKIT. Cognitive Effects [see Warnings and Precautions (5.2) ] Grade 1 Continue AYVAKIT at same dose or reduced dose or withhold until improvement to baseline or resolution. Resume at same dose or reduced dose.

Grade 2 or Grade 3 Withhold AYVAKIT until improvement to baseline, Grade 1, or resolution. Resume at same dose or reduced dose. Grade 4 Permanently discontinue AYVAKIT.

Other [see Adverse Reactions (6.1) ] Grade 3 or Grade 4 Withhold AYVAKIT until improvement to less than or equal to Grade 2. Resume at same dose or reduced dose, as clinically appropriate. Patients with AdvSM Thrombocytopenia [see Warnings and Precautions (5.1) ] <50 × 10 9 /L Interrupt AYVAKIT until platelet count is ≥ 50 × 10 9 /L, then resume at reduced dose (per Table 1).

If platelet counts do not recover above 50 × 10 9 /L, consider platelet support.

2.6Concomitant Use of Strong and Moderate CYP3A Inhibitors Avoid concomitant use of AYVAKIT with strong or moderate CYP3A inhibitors. If concomitant use with a moderate CYP3A inhibitor cannot be avoided, the starting dosage of AYVAKIT is as follows [see Drug Interactions (7.1) ] : GIST: 100 mg orally once daily AdvSM: 50 mg orally once daily For ISM, avoid concomitant use of AYVAKIT with strong or moderate CYP3A inhibitors.

2.7Dosage Modifications for Severe Hepatic Impairment A modified starting dosage of AYVAKIT is recommended for patients with severe hepatic impairment (Child-Pugh Class C) [see Use in Specific Populatio…

💊 Dosage Forms and Strengths 118 words ▾

3 DOSAGE FORMS AND STRENGTHS Tablets: 25 mg, round, white film-coated tablet with debossed text. One side reads "BLU" and the other side reads "25". 50 mg, round, white film-coated tablet with debossed text.

One side reads "BLU" and the other side reads "50". 100 mg, round, white film-coated, printed with blue ink "BLU" on one side and "100" on the other side. 200 mg, capsule shaped, white film-coated, printed with blue ink "BLU" on one side and "200" on the other side.

300 mg, capsule shaped, white film-coated, printed with blue ink "BLU" on one side and "300" on the other side. Tablets: 25 mg, 50 mg, 100 mg, 200 mg and 300 mg. ( 3 )

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Intracranial Hemorrhage : Permanently discontinue for any occurrence of any grade. ( 2.5 , 5.1 ) Cognitive Effects : A broad spectrum of cognitive adverse reactions can occur in patients receiving AYVAKIT. In patients with GIST, AdvSM, or ISM depending on the severity, continue AYVAKIT at same dose, withhold and then resume at same or reduced dose upon improvement, or permanently discontinue.

( 2.5 , 5.2 ) Photosensitivity: May cause photosensitivity reactions. Advise patients to limit direct ultraviolet exposure. ( 5.3 ) Embryo-Fetal Toxicity : Can cause fetal harm.

Advise females and males of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.4 , 8.1 , 8.3 )

5.1Intracranial Hemorrhage Serious intracranial hemorrhage may occur with AYVAKIT treatment; fatal events occurred in less than 1% of patients. Overall, intracranial hemorrhage (e.g., subdural hematoma, intracranial hemorrhage, and cerebral hemorrhage) occurred in 2.9% of the 749 patients with GIST or AdvSM who received AYVAKIT in clinical trials. No events of intracranial hemorrhage occurred in the 246 patients with ISM who received any dose of AYVAKIT in the PIONEER study .

Monitor patients closely for risk factors of intracranial hemorrhage which may include history of vascular aneurysm, intracranial hemorrhage or cerebrovascular accident within the prior year, concomitant use of anticoagulant drugs, or thrombocytopenia. Symptoms of intracranial hemorrhage may include headache, nausea, vomiting, vision changes, or altered mental status. Advise patients to seek immediate medical attention for signs or symptoms of intracranial hemorrhage.

Permanently discontinue AYVAKIT if intracranial hemorrhage of any grade occurs [see Dosage and Administration (2.5) ] . Gastrointestinal Stromal Tumors Intracranial hemorrhage occurred in 3 of 267 patients (1.1%). Two (0.7%) of the events were Grade ≥ 3 and resulted in discontinuation of study drug.

Events of intracranial hemorrhage occurred in a range from 1.7 months to 19.3 months after initiating AYVAKIT. Advanced Systemic Mastocytosis In patients with AdvSM who received AYVAKIT at 200 mg daily, intracranial hemorrhage occurred in 2 of 75 patients (2.7%) who had platelet counts ≥ 50 × 10 9 /L prior to initiation of therapy and in 3 of 80 patients (3.8%) regardless of platelet counts. In patients with AdvSM, a platelet count must be performed prior to initiating therapy; AYVAKIT is not recommended in patients with AdvSM with platelet counts < 50 × 10 9 /L.

Following treatment initiation, platelet counts must be performed every 2 weeks for the first 8 weeks regardless of baseline platelet count. After 8 weeks of treatment, monitor platelet counts every 2 weeks (or more frequently as clinically indicated) if values are less than 75 × 10 9 /L, every 4 weeks if values are between 75 and 100 × 10 9 /L, and as clinically indicated if values are greater than 100 × 10 9 /L. Manage platelet counts of < 50 × 10 9 /L by treatment interruption or dose-reduction of AYVAKIT.

Platelet support may be necessary [see Dosage and Administration (2.5) ] . Dose-interruptions and dose-reductions for thrombocytopenia occurred in 20% and 22% of AYVAKIT-treated patients, respectively. Thrombocytopenia was generally reversible by reducing or interrupting AYVAKIT.

5.2Cognitive Effects Cognitive adverse reactions can occur in patients receiving AYVAKIT. These cognitive adverse reactions occurred in 33% of the 995 patients with GIST, AdvSM or ISM who received AYVAKIT in clinical trials. These adverse reactions were managed with dose interruption and/or reduction when needed.

Overall, 10% led to dose interruptions, 7% led to dose reductions and 2.2% led to permanent discontinuation of AYVAKIT treatment in patients with GIST, AdvSM or ISM. Depending on the severity and indication, withhold AYVAKIT and then resume at the same dose or at a reduced dose upon improvement, or permanently discontin…

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Intracranial hemorrhage [see Warnings and Precautions (5.1) ] Cognitive effects [see Warnings and Precautions (5.2) ] Photosensitivity [see Warnings and Precautions (5.3) ] The most common adverse reactions are: GIST (≥20% incidence): edema, nausea, fatigue/asthenia, cognitive impairment, vomiting, decreased appetite, diarrhea, increased lacrimation, abdominal pain, constipation, rash, dizziness, and hair color changes.

( 6.1 ) AdvSM (≥20% incidence): edema, diarrhea, nausea, and fatigue/asthenia. ( 6.1 ) ISM (≥10% incidence): eye edema, dizziness, peripheral edema and flushing. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Blueprint Medicines Corporation at 1-888-258-7768 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 reflect exposure to AYVAKIT at 25 mg to 600 mg orally once daily in 995 patients enrolled in one of five clinicals trials conducted in patients with advanced malignancies and systemic mastocytosis, including NAVIGATOR, EXPLORER, PATHFINDER and PIONEER [see Clinical Studies (14.1 , 14.2 , 14.3) ].

These patients included 601 patients with GIST, 148 patients with AdvSM and 246 patients with ISM. Among the 995 patients receiving AYVAKIT, 54% were exposed for 6 months or longer and 26% were exposed for greater than 1 year. Gastrointestinal Stromal Tumors Unresectable or Metastatic GIST The safety of AYVAKIT in patients with unresectable or metastatic GIST was evaluated in NAVIGATOR [see Clinical Studies (14.1) ] .

The trial excluded patients with history of cerebrovascular accident or transient ischemic attacks, known risk of intracranial bleeding, and metastases to the brain. Patients received AYVAKIT 300 mg or 400 mg orally once daily (n = 204). Among patients receiving AYVAKIT, 56% were exposed for 6 months or longer and 44% were exposed for greater than one year.

The median age of patients who received AYVAKIT was 62 years (range: 29 to 90 years), 60% were <65 years, 62% were male, and 69% were White. Patients had received a median of 3 prior kinase inhibitors (range: 0 to 7). Serious adverse reactions occurred in 52% of patients receiving AYVAKIT.

Serious adverse reactions occurring in ≥1% of patients who received AYVAKIT were anemia (9%), abdominal pain (3%), pleural effusion (3%), sepsis (3%), gastrointestinal hemorrhage (2%), vomiting (2%), acute kidney injury (2%), pneumonia (1%), and tumor hemorrhage (1%). Fatal adverse reactions occurred in 3.4% of patients. Fatal adverse reactions that occurred in more than one patient were sepsis and tumor hemorrhage (1% each).

Permanent discontinuation due to adverse reactions occurred in 16% of patients who received AYVAKIT. Adverse reactions requiring permanent discontinuation in more than one patient were fatigue, abdominal pain, vomiting, sepsis, anemia, acute kidney injury, and encephalopathy. Dosage interruptions due to an adverse reaction occurred in 57% of patients who received AYVAKIT.

Adverse reactions requiring dosage interruption in >2% of patients who received AYVAKIT were anemia, fatigue, nausea, vomiting, hyperbilirubinemia, memory impairment, diarrhea, cognitive disorder, and abdominal pain. Dose reduction due to an adverse reaction occurred in 49% of patients who received AYVAKIT. Median time to dose reduction was 9 weeks.

Adverse reactions requiring dosage reduction in more than 2% of patients who received AYVAKIT were fatigue, anemia, hyperbilirubinemia, memory impairment, nausea, and periorbital edema. The most common adverse reactions (≥ 20%) were edema, nausea, fatigue/asthenia, cognitive im…

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Strong and Moderate CYP3A Inhibitors : Avoid coadministration of AYVAKIT with strong and moderate CYP3A inhibitors. If coadministration of AYVAKIT with a moderate inhibitor cannot be avoided, reduce dose of AYVAKIT in patients with GIST or AdvSM. ( 2.6 , 7.1 ) Strong and Moderate CYP3A Inducers : Avoid coadministration of AYVAKIT with strong and moderate CYP3A inducers.

( 7.1 ) Hormonal contraceptives containing ethinyl estradiol : See full prescribing information for dose-specific recommendations for concomitant use ( 7.2 )

7.1Effects of Other Drugs on AYVAKIT Strong and Moderate CYP3A Inhibitors Coadministration of AYVAKIT with a strong or moderate CYP3A inhibitor increases avapritinib plasma concentrations [see Clinical Pharmacology (12.3) ], which may increase the incidence and severity of adverse reactions of AYVAKIT. Avoid coadministration of AYVAKIT with strong or moderate CYP3A inhibitors. If coadministration of AYVAKIT with a moderate CYP3A inhibitor cannot be avoided, reduce the dose of AYVAKIT [see Dosage and Administration (2.6) ].

Strong and Moderate CYP3A Inducers Coadministration of AYVAKIT with a strong or moderate CYP3A inducer decreases avapritinib plasma concentrations [see Clinical Pharmacology (12.3) ] , which may decrease efficacy of AYVAKIT. Avoid coadministration of AYVAKIT with strong or moderate CYP3A inducers.

7.2Effects of AYVAKIT on Other Drugs Coadministration of AYVAKIT with ethinyl estradiol-containing contraceptives may increase the exposure of ethinyl estradiol, which may lead to increased risk of ethinyl estradiol-associated adverse reactions [see Clinical Pharmacology (12.3) ] . If the patient is unable to use or tolerate an effective nonhormonal contraceptive or an effective hormonal contraceptive without estrogen, use a formulation of ethinyl estradiol containing 20 mcg or less unless a higher dose is necessary.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 )

8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , AYVAKIT can cause fetal harm when administered to a pregnant woman. There are no available data on AYVAKIT use in pregnant women. Oral administration of avapritinib to pregnant rats during the period of organogenesis was teratogenic and embryotoxic at exposure levels approximately 31.4, 6.3 and 2.7 times the human exposure based on AUC at the 25 mg, 200 mg and 300 mg dose, respectively (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 2-4% and 15-20%, respectively. Data Animal Data In a reproductive toxicity study, administration of avapritinib to rats during the period of organogenesis resulted in decreased fetal body weights, post-implantation loss, and increases in visceral (hydrocephaly, septal defect, and stenosis of the pulmonary trunk) and skeletal (sternum) malformations at doses greater than or equal to 10 mg/kg/day (approximately 31.4, 6.3 and 2.7 times the human exposure based on AUC at the 25 mg, 200 mg and 300 mg dose, respectively).

8.2Lactation Risk Summary There are no data on the presence of avapritinib or its metabolites in human milk or the effects of avapritinib on the breastfed child or milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with AYVAKIT and for 2 weeks following the final dose.

8.3Females and Males of Reproductive Potential Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to initiating AYVAKIT [see Use in Specific Populations (8.1) ] . Contraception AYVAKIT can cause fetal harm when administered to pregnant women [see Use in Specific Populations (8.1) ]. Females Advise females of reproductive potential to use effective contraception during treatment with AYVAKIT and for 6 weeks after the final dose [see Drug Interactions (7.2) ].

Males Advise males with female partners of reproductive potential to use effective contraception during treatment with AYVAKIT and for 6 weeks after the final dose. Infertility Females Based on findings from animal studies, AYVAKIT may impair female fertility. These findings were not reversible within a two month recovery period [see Nonclinical Toxicology (13.1) ].

Males Based on findings from animal studies, AYVAKIT may impair male fertility. These findings were not reversible within a two month recovery period [see Nonclinical Toxicology (13.1) ] .

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

8.5Geriatric Use Of the 204 patients with unresectable or metastatic GIST who received AYVAKIT in NAVIGATOR, 40% were 65 years or older, while 6% were 75 years and older. Of the 131 patients with AdvSM who received AYVAKIT in EXPLORER and in PATHFINDER, 62% were 65 years or older, while 21% were 75 years and older. Of the 141 patients with ISM who received AYVAKIT in PIONEER, 6% were 65 years or older, while <1% were 75 years and older.

No overall differences in safety or efficacy were observed between these patients and younger adult patients.

8.6Renal Impairment No dose adjustment is recommended for patients with mild or moderate renal impairment [creatinine clearance (CLcr) 30 to 89 mL/min estimated by Cockcroft-Gault]. The recommended dose of AYVAKIT has not been established for patients with severe renal impairment (CLcr 15 to 29 mL/min) or end-stage renal disease (CLcr <15 mL/min) [see Clinical Pharmacology (12.3) ] .

8.7Hepatic Impairment No dose adjustment is recommended for patients with mild [total bilirubin ≤ upper limit of normal (ULN) and aspartate aminotransferase (AST) > ULN or total bilirubin > 1 to 1.5 t…

🤰 Pregnancy 198 words ▾

8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , AYVAKIT can cause fetal harm when administered to a pregnant woman. There are no available data on AYVAKIT use in pregnant women. Oral administration of avapritinib to pregnant rats during the period of organogenesis was teratogenic and embryotoxic at exposure levels approximately 31.4, 6.3 and 2.7 times the human exposure based on AUC at the 25 mg, 200 mg and 300 mg dose, respectively (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 2-4% and 15-20%, respectively. Data Animal Data In a reproductive toxicity study, administration of avapritinib to rats during the period of organogenesis resulted in decreased fetal body weights, post-implantation loss, and increases in visceral (hydrocephaly, septal defect, and stenosis of the pulmonary trunk) and skeletal (sternum) malformations at doses greater than or equal to 10 mg/kg/day (approximately 31.4, 6.3 and 2.7 times the human exposure based on AUC at the 25 mg, 200 mg and 300 mg dose, respectively).

🧒 Pediatric Use 16 words ▾

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

🧓 Geriatric Use 97 words ▾

8.5Geriatric Use Of the 204 patients with unresectable or metastatic GIST who received AYVAKIT in NAVIGATOR, 40% were 65 years or older, while 6% were 75 years and older. Of the 131 patients with AdvSM who received AYVAKIT in EXPLORER and in PATHFINDER, 62% were 65 years or older, while 21% were 75 years and older. Of the 141 patients with ISM who received AYVAKIT in PIONEER, 6% were 65 years or older, while <1% were 75 years and older.

No overall differences in safety or efficacy were observed between these patients and younger adult patients.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Avapritinib is a tyrosine kinase inhibitor that targets KIT D816V, PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC 50s ) less than 25 nM in biochemical assays. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor and mast cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1.

In cellular assays, avapritinib inhibited the autophosphorylation of KIT D816V with an IC 50 of 4 nM, approximately 48-fold lower concentration than wild-type KIT. In cellular assays, avapritinib inhibited the proliferation in KIT mutant cell lines, including a murine mastocytoma cell line and a human mast cell leukemia cell line. Avapritinib also showed growth inhibitory activity in a xenograft model of murine mastocytoma with KIT exon 17 mutation.

Avapritinib inhibited the autophosphorylation of PDGFRA D842V, a mutation associated with resistance to approved kinase inhibitors, with an IC 50 of 30 nM. Avapritinib also had anti-tumor activity in mice implanted with an imatinib-resistant patient-derived xenograft model of human GIST with activating KIT exon 11/17 mutations.

12.2Pharmacodynamics Exposure-Response Relationships Gastrointestinal Stromal Tumors or Advanced Systemic Mastocytosis Based on the data from four clinicals trials conducted in patients with advanced malignancies and AdvSM, including NAVIGATOR, EXPLORER, and PATHFINDER, higher exposure was associated with increased risk of Grade ≥ 3 related adverse effects, any Grade pooled cognitive adverse effects, Grade ≥ 2 pooled cognitive adverse effects, and Grade ≥ 2 pooled edema adverse effects over the dose range of 30 mg to 400 mg (0.1 to 1.33 times the recommended dose for GIST and 0.15 to 2 times the recommended dose for AdvSM) once daily.

Based on exposure and efficacy data from EXPLORER and PATHFINDER (n=84), higher avapritinib exposure was associated with faster time to response over the dose range of 30 mg to 400 mg (0.15 to 2 times the recommended dose for AdvSM) once daily. Cardiac Electrophysiology The effect of AYVAKIT on the QTc interval was evaluated in an open-label, single-arm study in 27 patients administered doses of 300 mg or 400 mg (12 to 16 times the lowest recommended 25 mg dose, 1.33 times the highest recommended 300 mg dose) once daily.

No large mean increase in QTc (i.e.> 20 ms) was detected at the mean steady state maximum concentration (C max ) of 899 ng/mL.

12.3Pharmacokinetics Avapritinib C max and AUC increased approximately proportionally over the dose range of 25 mg to 400 mg once daily. Steady state concentrations of avapritinib were reached prior to day 15 following daily dosing. Steady state pharmacokinetic parameters per recommended dosing regimen are described in Table 10.

Table 10. Steady State Pharmacokinetic Parameters of AYVAKIT Following Different Dosing Regimen Pharmacokinetic Parameters 25 mg once daily (ISM) 200 mg once daily (AdvSM) 300 mg once daily (GIST) Abbreviations: CV%=coefficient of variation C max (ng/mL) Geometric Mean (CV%) 70.2 (47.8 %, n=9) 377 (62%, n=18) 813 (52%, n=110) AUC 0-24h (h∙ng/mL) Geometric Mean (CV%) 1330 (49.5 %, n = 9) 6600 (54%, n=16) 15400 (48%, n=110) Mean accumulation ratio of AUC 0-24h 4.06 (n=9) 6.41 (n=9) 3.82 (n=34) Absorption The median time to peak concentration (T max ) ranged from 2 to 4 hours following single doses of avapritinib.

Effect of Food The C max of avapritinib was increased by 59% and the AUC 0-INF was increased by 29% when AYVAKIT was taken with a high-calorie, high-fat meal (approximately 909 calories, 58 grams carbohydrate, 56 grams fat and 43 grams protein) compared to those in the fasted state. Distribution The mean (CV %) apparent volume of distribution of avapritinib is 1310 L (51.5%) at 300 mg in patients with GIST,…

🧬 Mechanism of Action 197 words ▾

12.1Mechanism of Action Avapritinib is a tyrosine kinase inhibitor that targets KIT D816V, PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC 50s ) less than 25 nM in biochemical assays. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor and mast cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1.

In cellular assays, avapritinib inhibited the autophosphorylation of KIT D816V with an IC 50 of 4 nM, approximately 48-fold lower concentration than wild-type KIT. In cellular assays, avapritinib inhibited the proliferation in KIT mutant cell lines, including a murine mastocytoma cell line and a human mast cell leukemia cell line. Avapritinib also showed growth inhibitory activity in a xenograft model of murine mastocytoma with KIT exon 17 mutation.

Avapritinib inhibited the autophosphorylation of PDGFRA D842V, a mutation associated with resistance to approved kinase inhibitors, with an IC 50 of 30 nM. Avapritinib also had anti-tumor activity in mice implanted with an imatinib-resistant patient-derived xenograft model of human GIST with activating KIT exon 11/17 mutations.

📦 How Supplied / Storage and Handling 175 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING AYVAKIT (avapritinib) tablets are supplied as follows: 25 mg, round, white film-coated tablet with debossed text. One side reads "BLU" and the other side reads "25"; available in bottles of 30 tablets (NDC 72064-125-30). 50 mg, round, white film-coated tablet with debossed text.

One side reads "BLU" and the other side reads "50"; available in bottles of 30 tablets (NDC 72064-150-30). 100 mg, round, white film-coated tablet, printed with blue ink "BLU" on one side and "100" on the other side; available in bottles of 30 tablets (NDC 72064-110-30). 200 mg, capsule shaped, white film-coated tablet, printed with blue ink "BLU" on one side and "200" on the other side; available in bottles of 30 tablets (NDC 72064-120-30).

300 mg, capsule shaped, white film-coated tablet, printed with blue ink "BLU" on one side and "300" on the other side; available in bottles of 30 tablets (NDC 72064-130-30). Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

📦 Storage and Handling 23 words ▾

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

📋 Description 174 words ▾

11 DESCRIPTION Avapritinib is a kinase inhibitor with the chemical name ( S )-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1 H -pyrazol-4-yl)pyrrolo[2,1- f ][1,2,4]triazin-4-yl)piperazin-yl)pyrimidin-5-yl)ethan-1-amine. The molecular formula is C 26 H 27 FN 10 , and the molecular weight is 498.57 g/mol. Avapritinib has the following chemical structure: The solubility of avapritinib in 0.1N HCl (pH 1.0) and buffer solutions at pH 2.5, 4.0, and 7.0 (at 25°C) is 3.6 mg/mL, 0.14 mg/mL, 0.07 mg/mL and <0.001 mg/mL respectively, indicating a decrease in solubility with increasing pH.

AYVAKIT (avapritinib) film-coated tablets for oral use are supplied with five strengths that contain 25 mg, 50 mg, 100 mg, 200 mg or 300 mg of avapritinib. The tablets also contain inactive ingredients: copovidone, croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. The tablet coating consists of polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

The blue printing ink, used only for avapritinib 100 mg, 200 mg and 300 mg strength tablets, contains ammonium hydroxide, black iron oxide, esterified shellac, FD&C blue 1, isopropyl alcohol, n-butyl alcohol, propylene glycol, and titanium dioxide. Chemical Structure

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Intracranial Hemorrhage Advise patients to contact their healthcare provider immediately if experiencing neurological signs and symptoms that may be associated with intracranial hemorrhage (i.e., severe headache, vomiting, drowsiness, dizziness, confusion, slurred speech, or paralysis) [see Warnings and Precautions (5.1) ] . Inform patients with AdvSM of the need to monitor platelet counts before and during treatment [see Warnings and Precautions (5.1) ] .

Cognitive Effects Advise patients and caretakers to notify their healthcare provider if they experience new or worsening cognitive symptoms. Advise patients not to drive or operate hazardous machinery if they are experiencing cognitive adverse reactions [see Warnings and Precautions (5.2) ] . Photosensitivity Inform patients that there is a potential risk of photosensitivity reactions with AYVAKIT.

Advise patients to limit direct ultraviolet exposure by using sunscreen and protective clothing during treatment with AYVAKIT [see Warnings and Precautions (5.3) ]. Embryo-Fetal Toxicity Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions (5.4) , Use in Specific Populations (8.1) ] .

Advise females of reproductive potential to use effective contraception during treatment with AYVAKIT and for 6 weeks after the final dose [see Drug Interactions (7.2) , Use in Specific Populations (8.3) ] . Advise males with female partners of reproductive potential to use effective contraception during treatment with AYVAKIT and for 6 weeks after the final dose [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ] . Lactation Advise women not to breastfeed during treatment with AYVAKIT and for 2 weeks following the final dose [see Use in Specific Populations (8.2) ] .

Infertility Advise females of reproductive potential that AYVAKIT may impair fertility at 200 mg or 300 mg [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ]. Advise males of reproductive potential that AYVAKIT may decrease sperm production at 200 mg or 300 mg [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ]. Drug Interactions Advise patients and caregivers to inform their healthcare provider of all concomitant medications, including prescription medicines, over-the-counter drugs, vitamins, and herbal products [see Drug Interactions (7.1) ] .

Administration Advise patients to take AYVAKIT on an empty stomach, at least 1 hour before or at least 2 hours after a meal [see Dosage and Administration (2.1) ] .

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