Home › NDC Lookup › Ingredients › Pralsetinib › 71332-0006-12

Gavreto Pralsetinib 100 mg Capsule, 120-count

by Rigel Pharmaceuticals, Inc. · 120 CAPSULE in 1 BOTTLE (71332-006-12)

NDC 71332-0006-12

🏷️ FDA NDC (as labeled) 71332-006-12 billing pads the product segment with a zero

This package

Contains120-count Pack sizes3 compare ↓

Also priced by: Part D plans $206.94/unit — full pricing hub ↓

Also comes in: 60 capsules 71332-0006-60 90 capsules 71332-0006-90

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 Dr. Brian Staiger, PharmD

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

🆔 Identity & classification

FDA NDC (as labeled) 71332-006-12

Product NDC 71332-006

11-digit billing NDC 71332000612

RxCUI 2394941, 2394947

UNII 1WPE73O1WV

Application # NDA213721

SPL Set ID 16edd46e-28b8-f06d-e063-6394a90ae31b

Established class (EPC) Kinase Inhibitor

Mechanism of action Rearranged during Transfection (RET) Inhibitors

DEA schedule Non-controlled

Marketing category NDA

Marketing status On market

FDA listing status Listed (active directory)

Marketing start 2024-06-24

Route ORAL

Dosage form CAPSULE

Substance PRALSETINIB

GPI-14 21535750000120

GCN Seq No 081450

GCN 48566

HICL code 046818

Ingredient (HICL) Pralsetinib

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 GAVRETO 100 MG CAPSULE

FDB brand name Gavreto

Legend status F — Federal legend — prescription drug or device

Why two NDCs? The FDA registers this code as 71332-006-12 — 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 → 71332-0006-12. 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 Rearranged during Transfection (RET) 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

LabelerRigel Pharmaceuticals, Inc.

Application holderRIGEL PHARMACEUTICALS INC

FDA applicationNDA213721 (NDA)

Labeler code71332

First marketedJun 2024

Product typeHuman Prescription Drug

Portfolio6 products on file

🔎 All NDCs from Rigel Pharmaceuticals, Inc.

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 GAVRETO 100 MG CAPSULE Ingredient Pralsetinib

📖 What it is MedlinePlus · NLM

Pralsetinib is used to treat a certain type of non small-cell lung cancer (NSCLC) in adults that has spread to other parts of the body. It is also used to treat a certain type of thyroid cancer in adults and children 12 years of age and older that is getting worse or that has spread to other parts of the body. Pralsetinib is used to treat a certain type of thyroid cancer in adults and children 12 years of age and older that is getting worse or that has spread to other parts of the body and cannot be treated with radioactive iodine. Pralsetinib is in a class of medications called kinase inhibit...

Read the full MedlinePlus article ↗

📗 Our plain-language guide HelloPharmacist

Gavreto only works against cancers that have a specific genetic change called a RET gene fusion. Without that change, the drug has no target to block. Your doctor uses an FDA-appro...
Why does my tumor need to be tested before I can start this medication?
Yes, it matters a lot. You need to take Gavreto on a completely empty stomach — that means no food for at least 2 hours before and at least 1 hour after your dose. Studies showed t...
Does it matter if I eat before taking my capsule?

📖 Read our full Pralsetinib guide →

Patient education

📘 MedlinePlus patient leaflet ↗

Supplement & herbal interactions

Some supplements/herbs that may interact with Pralsetinib — tap one for details:

Activated CharcoalMajor Coffee CharcoalModerate European MandrakeModerate GlucomannanModerate Guar GumModerate Gum ArabicModerate Slippery ElmModerate TragacanthModerate

🌿 Every supplement checked against Pralsetinib (181 interactions) — ranked by severity →

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

ShapeCapsule

ImprintBLU667

Size23 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 XF417D3PSL
Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
UNII 9XZ8H6N6OH
A plant-based cellulose derivative used as a binder to hold tablet ingredients together, a thickener in liquids, and a coating agent to control how fast the medicine dissolves.
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 8MDF5V39QO
A white powder form of baking soda that acts as a buffer and pH regulator in medicines. It helps maintain the right acid-base balance and may aid tablet disintegration.

4 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 system	Per each	Per 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	$206.94	$24,832.30 / 120 capsules

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

Product	Labeler	Pack	NADAC/unit	TE	Status	Price vs. this
Gavreto 100 mg 50242-0210-60	Genentech,	60 capsules	—	—	FDA listed	—
Gavreto 100 mgthis 71332-0006-12	Rigel	120 capsules	—	—	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

Sep 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 Jul 2042. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.

📅 FDA approved Sep 4, 2020 RLD RS ⏳ ~15.8 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 10030005 — drug substance (U-2952)

US 10030005 — drug substance (U-3002)

US 11273160 — method of use (U-2952)

US 12539303 — method of use (U-2828)

US 11872192 — method of use (U-2952)

US 11963958 — method of use (U-2828)

US 12655128 — drug substance

US 12448366 — drug substance

Exclusivity ODE-318

Exclusivity ODE-340

Exclusivity ODE-341

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 (8)

Patent	Type	Use code	Expires
US 10030005 ↗	Drug substance	U-2952	Nov 1, 2036
US 10030005 ↗	Drug substance	U-3002	Nov 1, 2036
US 11273160 ↗	Method of use	U-2952	Apr 3, 2039
US 12539303 ↗	Method of use	U-2828	Apr 3, 2039
US 11872192 ↗	Method of use	U-2952	Apr 3, 2039
US 11963958 ↗	Method of use	U-2828	Apr 3, 2039
US 12655128 ↗	Drug substance	—	Nov 1, 2036
US 12448366 ↗	Drug substance	—	Jul 7, 2042

FDA exclusivity

Code	What it grants	Expires
ODE-318	Orphan Drug Exclusivity (7-year)	Sep 4, 2027
ODE-340	Orphan Drug Exclusivity (7-year)	Dec 1, 2027
ODE-341	Orphan Drug Exclusivity (7-year)	Dec 1, 2027

Common questions

Is there a generic version of GAVRETO 100 MG CAPSULE?

No FDA-approved generic equivalent is currently listed in the FDA Orange Book for GAVRETO 100 MG CAPSULE. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Jul 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 Gavreto — 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 Gavreto. 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

$6.32M

Claims incl. refills

419

Beneficiaries

173

Spend / beneficiary

$36,541.83

Spend / claim

$15,087.68

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 Pralsetinib — the ingredient across all brands.

Top reported reactions

Product Prescribing Issue181

Death148

Fatigue126

Asthenia116

Anaemia98

Hypertension96

Diarrhoea93

Reporter sex

Serious outcomes

Death252

Life-threatening20

Disabling10

Reports over time (by year) — tap or hover for the count & year

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 NDC	Description	Marketing start	Status
71332-0006-12 You're viewing this	120 CAPSULE in 1 BOTTLE (71332-006-12)	2024-06-24	Active
71332-0006-60	60 CAPSULE in 1 BOTTLE (71332-006-60)	2024-06-24	Active
71332-0006-90	90 CAPSULE in 1 BOTTLE (71332-006-90)	2024-06-24	Active

You're viewing the largest of 3 pack sizes for this product.

Pack size FAQ

What quantity is in NDC 71332-0006-12?

NDC 71332-0006-12 is a 120-count package — 120 capsule in 1 bottle.

What is the difference between NDC 71332-0006-12 and NDC 71332-0006-60?

Both are Gavreto Pralsetinib 100 mg Capsule — the drug itself is identical. NDC 71332-0006-12 is the 120-count package, while NDC 71332-0006-60 is the 60 capsules package.

What NDC number is used to bill for this package of Gavreto Pralsetinib 100 mg Capsule?

Bill NDC 71332-0006-12 — the 11-digit billing format is 71332000612. 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 71332-006-12, 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: 71332-0006-12, written without dashes as 71332000612. 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 71332-0006-12, the first segment (71332) is the labeler code FDA assigned to Rigel Pharmaceuticals, Inc.; the middle segment (0006) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (12) 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 Rigel Pharmaceuticals, Inc.. 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 2 other package presentations of this same product, including 60 capsules (71332-0006-60), 90 capsules (71332-0006-90). 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?

Rigel Pharmaceuticals, Inc. 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.

🚨 Boxed Warning 🎯 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 💬 Medication Guide

🚨 Boxed Warning 103 words ▾

WARNING: SERIOUS INFECTIONS, INCLUDING OPPORTUNISTIC INFECTIONS GAVRETO may increase the risk for serious infections, including bacterial, fungal, viral and opportunistic infections, which can lead to hospitalization or death. Withhold, reduce the dose or permanently discontinue GAVRETO based on severity [see Dosage and Administration (2.3) , Warnings and Precautions (5.1) ] . WARNING: SERIOUS INFECTIONS, INCLUDING OPPORTUNISTIC INFECTIONS See full prescribing information for complete boxed warning.

GAVRETO may increase the risk for serious infections, including bacterial, fungal, viral and opportunistic infections, which can lead to hospitalization or death. Withhold, reduce the dose or permanently discontinue GAVRETO based on severity. ( 2.3 , 5.1 )

🎯 Indications and Usage ~1 min read ▾

1 INDICATIONS AND USAGE GAVRETO is a kinase inhibitor indicated for treatment of: Adult patients with metastatic rearranged during transfection (RET ) fusion-positive non-small cell lung cancer as detected by an FDA approved test (NSCLC). ( 1.1 ) Adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate). This indication is approved under accelerated approval based on overall response rate and duration of response.

Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s). ( 1.2 )

1.1Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer GAVRETO is indicated for the treatment of adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA approved test.

1.2RET Fusion-Positive Thyroid Cancer GAVRETO is indicated for the treatment of adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate). This indication is approved under accelerated approval based on overall response rate and duration of response [see Clinical Studies (14.2) ] . Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s).

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Select patients for treatment with GAVRETO based on the presence of a RET gene fusion. ( 2.1 , 14 ) The recommended dosage in adults and pediatric patients 12 years and older is 400 mg orally once daily on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after taking GAVRETO). ( 2.2 )

2.1Patient Selection Select patients for treatment with GAVRETO based on the presence of a RET gene fusion (NSCLC or thyroid cancer) [see Clinical Studies (14) ] . Information on FDA-approved tests for RET gene fusion (NSCLC) is available at http://www.fda.gov/CompanionDiagnostics. An FDA-approved test for the detection of RET gene fusion (thyroid cancer) is not currently available.

2.2Recommended Dosage The recommended dosage of GAVRETO is 400 mg orally once daily on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after taking GAVRETO ) [see Clinical Pharmacology (12.3) ] . Continue treatment until disease progression or until unacceptable toxicity. If a dose of GAVRETO is missed, it can be taken as soon as possible on the same day.

Resume the regular daily dose schedule for GAVRETO the next day. Do not take an additional dose if vomiting occurs after GAVRETO but continue with the next dose as scheduled.

2.3Dosage Modifications for Adverse Reactions The recommended dose reductions and dosage modifications for adverse reactions are provided in Table 1 and Table 2 . Table 1: Recommended Dose Reductions for GAVRETO for Adverse Reactions Dose Reduction Recommended Dosage First 300 mg once daily Second 200 mg once daily Third 100 mg once daily Permanently discontinue GAVRETO in patients who are unable to tolerate 100 mg taken orally once daily. The recommended dosage modifications for adverse reactions are provided in Table 2 .

Table 2: Recommended Dosage Modifications for GAVRETO for Adverse Reactions Adverse Reactions Severity Adverse reactions graded by the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version

4.03Dosage Modification Serious Infections, Including Opportunistic Infections [see Warnings and Precautions (5.1) ] Grade 2 or 3 Withhold GAVRETO until resolution. Resume at a reduced dose ( Table 1 ). Grade 4 Permanently discontinue GAVRETO.

ILD/Pneumonitis [see Warnings and Precautions (5.2) ] Grade 1 or 2 Withhold GAVRETO until resolution. Resume by reducing the dose as shown in Table 1 . Permanently discontinue GAVRETO for recurrent ILD/pneumonitis.

Grade 4 Permanently discontinue GAVRETO. Hypertension [see Warnings and Precautions (5.3) ] Grade 3 Withhold GAVRETO for Grade 3 hypertension that persists despite optimal antihypertensive therapy. Resume at a reduced dose when hypertension is controlled.

Grade 4 Discontinue GAVRETO. Hepatotoxicity [see Warnings and Precautions (5.4) ] Grade 3 or 4 Withhold GAVRETO and monitor AST/ALT once weekly until resolution to Grade 1 or baseline. Resume at reduced dose ( Table 1 ).

For recurrent events at Grade 3 or higher, discontinue GAVRETO. Hemorrhagic Events [see Warnings and Precautions (5.5) ] Grade 3 or 4 Withhold GAVRETO until recovery to baseline or Grade 0 or 1. Discontinue GAVRETO for severe or life-threatening hemorrhagic events.

Other Adverse Reactions [see Adverse Reactions (6.1) ] Grade 3 or 4 Withhold GAVRETO until improvement to ≤ Grade 2. Resume at reduced dose ( Table 1 ). Permanently discontinue for recurrent Grade 4 adverse reactions.

2.4Dose Modification for Use with CYP3A and/or P-glycoprotein (P-gp) Inhibitors Avoid coadministration of GAVRETO with any of the following: Strong CYP3A inhibitors Moderate CYP3A inhibitors P-gp inhibitors Combined P-gp and strong CYP3A inhibitors Combined P-gp and moderate CYP3A inhibitors If coadministration with any of the above inhibitors cannot be avoided, reduce the current dose of GAVRETO as recommended in Table 3 . After the inhibitor has been discontinued for 3 to 5 elimination half-lives, resume GAVRETO…

💊 Dosage Forms and Strengths 38 words ▾

3 DOSAGE FORMS AND STRENGTHS Capsules: 100 mg, light blue, opaque, hard hydroxypropyl methylcellulose (HPMC) capsule printed with "BLU-667" on the capsule shell body and "100 mg" on the capsule shell cap. Capsules: 100 mg. ( 3 )

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Serious Infections, Including Opportunistic Infections: Monitor for signs and symptoms of infection and treat appropriately. Withhold, reduce the dose, or permanently discontinue GAVRETO based on severity. ( 2.3 , 5.1 ) Interstitial Lung Disease (ILD)/Pneumonitis: Withhold GAVRETO for Grade 1 or 2 reactions until resolution and then resume at a reduced dose.

Permanently discontinue for recurrent ILD/pneumonitis. Permanently discontinue for Grade 3 or 4 reactions. ( 2.3 , 5.2 ) Hypertension : Do not initiate GAVRETO in patients with uncontrolled hypertension.

Optimize blood pressure (BP) prior to initiating GAVRETO. Monitor BP after 1 week, at least monthly thereafter and as clinically indicated. Withhold, reduce dose, or permanently discontinue GAVRETO based on severity.

( 2.3 , 5.3 ) Hepatotoxicity : Monitor ALT and AST prior to initiating GAVRETO, every 2 weeks during the first 3 months, then monthly thereafter and as clinically indicated. Withhold, reduce dose, or permanently discontinue GAVRETO based on severity. ( 2.3 , 5.4 ) Hemorrhagic Events : Permanently discontinue GAVRETO in patients with severe or life-threatening hemorrhage.

( 2.3 , 5.5 ) Tumor Lysis Syndrome: Closely monitor patients at risk and treat as clinically indicated. ( 2.3 , 5.6 ) Risk of Impaired Wound Healing: Withhold GAVRETO for at least 5 days prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing.

The safety of resumption of GAVRETO after resolution of wound healing complications has not been established. ( 5.7 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective non-hormonal contraception.

( 5.8 , 8.1 , 8.3 )

5.1Serious Infections, Including Opportunistic Infections GAVRETO may increase the risk for serious infections, including fatal and opportunistic infections. In the AcceleRET-Lung trial [see Adverse Reactions (6.1) ] , infections occurred in 72% of patients who received GAVRETO, including 18% with Grade 3, 3.7% with Grade 4, and 7% with fatal outcomes. Among the patients who received chemotherapy/immunotherapy, infections occurred in 52%, including 10% with Grade 3.

Infections in the GAVRETO arm included pneumonia, urinary tract infection, opportunistic infections (such as pneumocystis jirovecii pneumonia, and fungal infections) and others. Monitor patients for signs and symptoms of infection and treat appropriately. Withhold, reduce the dose, or permanently discontinue GAVRETO based on severity [see Dosage and Administration (2.3) ] .

5.2Interstitial Lung Disease/Pneumonitis Severe, life-threatening, and fatal interstitial lung disease (ILD) / pneumonitis can occur in patients treated with GAVRETO. Pneumonitis occurred in 12% of patients who received GAVRETO, including 3.3% with Grade 3-4, and 0.2% with fatal reactions. Monitor for pulmonary symptoms indicative of ILD/pneumonitis.

Withhold GAVRETO and promptly investigate for ILD in any patient who presents with acute or worsening of respiratory symptoms which may be indicative of ILD (e.g., dyspnea, cough, and fever). Withhold, reduce dose or permanently discontinue GAVRETO based on severity of confirmed ILD [see Dosage and Administration (2.3) ] .

5.3Hypertension Hypertension occurred in 35% of patients, including Grade 3 hypertension in 18% of patients [see Adverse Reactions (6.1) ] . Overall, 8% had their dose interrupted and 4.8% had their dose reduced for hypertension. Treatment-emergent hypertension was most commonly managed with anti-hypertension medications.

Do not initiate GAVRETO in patients with uncontrolled hypertension. Optimize blood pressure prior to initiating GAVRETO. Monitor blood pressure after 1 week, at least monthly thereafter and as clinically indicated.

Initiate or adjust anti-hypertensive therapy as appropriate. Withhold, reduce dose, or permanently discontinue GAVRETO based on the…

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Serious Infections, Including Opportunistic Infections [see Warnings and Precautions (5.1) ] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.2) ] Hypertension [see Warnings and Precautions (5.3) ] Hepatotoxicity [see Warnings and Precautions (5.4) ] Hemorrhagic Events [see Warnings and Precautions (5.5) ] Tumor Lysis Syndrome [see Warnings and Precautions (5.6) ] Risk of Impaired Wound Healing [see Warnings and Precautions (5.7) ] Embryo-Fetal Toxicity [see Warnings and Precautions (5.8) ] The most common adverse reactions (≥ 25%) were musculoskeletal pain, constipation, hypertension, diarrhea, fatigue, edema, pyrexia and cough.

The most common Grade 3-4 laboratory abnormalities (≥ 2%) were decreased lymphocytes, decreased neutrophils, decreased hemoglobin, decreased phosphate, decreased leukocytes, decreased sodium, increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), decreased calcium (corrected), decreased platelets, increased alkaline phosphatase, increased potassium, decreased potassium and increased bilirubin. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Rigel Pharmaceuticals, Inc. at 1-800-983-1329 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 pooled safety population in the WARNINGS AND PRECAUTIONS reflect exposure to GAVRETO as a single agent at 400 mg orally once daily in 540 patients in ARROW [see Clinical Studies (14) ]. Among 540 patients who received GAVRETO, 71% were exposed for 6 months or longer and 57% were exposed for greater than one year.

The most common adverse reactions (≥ 25%) were musculoskeletal pain, constipation, hypertension, diarrhea, fatigue, edema, pyrexia, and cough. The most common Grade 3-4 laboratory abnormalities (≥ 2%) were decreased lymphocytes, decreased neutrophils, decreased hemoglobin, decreased phosphate, decreased leukocytes, decreased sodium, increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), decreased calcium (corrected), decreased platelets, increased alkaline phosphatase, increased potassium, decreased potassium and increased bilirubin.

In addition to the 540 patients, certain subsections in the WARNINGS AND PRECAUTIONS describe adverse reactions observed with exposure to GAVRETO as a single agent in a randomized, open-label study, AcceleRET-Lung (NCT04222972), which enrolled 223 patients with RET-fusion positive locally advanced unresectable or metastatic NSCLC. RET Fusion-Positive Non-Small Cell Lung Cancer The safety of GAVRETO was evaluated as a single agent at 400 mg orally once daily in 281 patients with metastatic rearranged during transfection ( RET fusion-positive) non-small cell lung cancer (NSCLC) in ARROW [see Clinical Studies (14.1) ].

Among the 281 patients who received GAVRETO, 72% were exposed for 6 months or longer and 56% were exposed for ≥1 year. The median age was 60 years (range: 26 to 87 years); 54% were female, 46% were White, 46% were Asian, and 4% were Hispanic/Latino. Serious adverse reactions occurred in 65% of patients who received GAVRETO.

The most frequent serious adverse reactions (in ≥ 2% of patients) were pneumonia, anemia, pneumonitis, pyrexia, sepsis, urinary tract infection, coronavirus infection, pleural effusion, dyspnea, musculoskeletal pain, pulmonary embolism, and seizure. Fatal adverse reactions occurred in 7% of patients; fatal adverse reactions which occurred in > 1 patient included pneumonia (n=8), sepsis (n=3) and COVID (n=3). Permanent discontinuation due to an adverse reaction occurred in 20% of patients who received GAVRE…

🔄 Drug Interactions 197 words ▾

7 DRUG INTERACTIONS Strong or moderate CYP3A inhibitors and/or P-gp inhibitors : Avoid coadministration. If coadministration cannot be avoided, reduce the dose of GAVRETO. ( 2.4 , 7.1 , 12.3 ) Strong or moderate CYP3A inducers : Avoid coadministration. If coadministration cannot be avoided, increase the dose of GAVRETO. ( 2.5 , 7.1 , 12.3 )

7.1Effects of Other Drugs on GAVRETO Strong or Moderate CYP3A and/or P-gp Inhibitors Concomitant use with a strong or moderate CYP3A inhibitor and/or a P-gp inhibitor increases pralsetinib exposure [ Clinical Pharmacology (12.3) ] , which may increase the risk of adverse reactions related to GAVRETO. Avoid coadministration of GAVRETO with a strong or moderate CYP3A and/or P-gp inhibitor. If coadministration with any of the above inhibitors cannot be avoided, reduce the GAVRETO dose [see Dosage and Administration (2.4) ].

Strong or Moderate CYP3A Inducers Concomitant use with a strong CYP3A inducer decreases pralsetinib exposure [see Clinical Pharmacology (12.3) ], which may decrease efficacy of GAVRETO. Avoid concomitant use of GAVRETO with strong or moderate CYP3A inducers. If coadministration of GAVRETO with strong or moderate CYP3A inducers cannot be avoided, increase the GAVRETO dose [see Dosage and Administration (2.5) ]

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 ) Pediatric Use : Monitor open growth plates in adolescent patients. Consider interrupting or discontinuing GAVRETO if abnormalities occur. ( 8.4 )

8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, GAVRETO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ]. There are no available data on GAVRETO use in pregnant women to inform drug-associated risk. Oral administration of pralsetinib to pregnant rats during the period of organogenesis resulted in malformations and embryolethality at maternal exposures below the human exposure at the clinical dose of 400 mg once daily (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 an embryo-fetal development study, once daily oral administration of pralsetinib to pregnant rats during the period of organogenesis resulted in 100% post-implantation loss at dose levels ≥ 20 mg/kg (approximately 1.8 times the human exposure based on area under the curve [AUC] at the clinical dose of 400 mg).

Post-implantation loss also occurred at the 10 mg/kg dose level (approximately 0.6 times the human exposure based on AUC at the clinical dose of 400 mg). Once daily oral administration of pralsetinib at dose levels ≥ 5 mg/kg (approximately 0.2 times the human AUC at the clinical dose of 400 mg) resulted in an increase in visceral malformations and variations (absent or small kidney and ureter, absent uterine horn, malpositioned kidney or testis, retroesophageal aortic arch) and skeletal malformations and variations (vertebral and rib anomalies and reduced ossification).

8.2Lactation Risk Summary There are no data on the presence of pralsetinib or its metabolites in human milk or their effects on either the breastfed child or on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with GAVRETO and for 1 week after the last dose.

8.3Females and Males of Reproductive Potential Based on animal data, GAVRETO can cause embryolethality and malformations at doses resulting in exposures below the human exposure at the clinical dose of 400 mg daily [see Use in Specific Populations (8.1) ]. Pregnancy Testing Verify pregnancy status of females of reproductive potential prior to initiating GAVRETO [see Use in Specific Populations (8.1) ]. Contraception GAVRETO 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 non-hormonal contraception during treatment with GAVRETO and for 2 weeks after the last dose. GAVRETO may render hormonal contraceptives ineffective. Males Advise males with female partners of reproductive potential to use effective contraception during treatment with GAVRETO and for 1 week after the last dose.

Infertility Based on histopathological findings in the reproductive tissues of male and female rats and a dedicated fertility study in which animals of both sexes were treated and mated to each other, GAVRETO may impair fertility [see Nonclinical Toxicology (13.1) ].

🤰 Pregnancy ~1 min read ▾

🧒 Pediatric Use ~1 min read ▾

8.4Pediatric Use The safety and effectiveness of GAVRETO have been established in pediatric patients aged 12 years and older for RET fusion-positive thyroid cancer. Use of GAVRETO in this age group is supported by evidence from an adequate and well-controlled study of GAVRETO in adults with additional population pharmacokinetic data demonstrating that age and body weight had no clinically meaningful effect on the pharmacokinetics of pralsetinib, that the exposure of pralsetinib is expected to be similar between adults and pediatric patients age 12 years and older, and that the course of RET fusion-positive thyroid cancer is sufficiently similar in adults and pediatric patients to allow extrapolation of data in adults to pediatric patients [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14.2) ].

The safety and effectiveness of GAVRETO have not been established in pediatric patients with RET fusion-positive NSCLC or in pediatric patients younger than 12 years old with RET fusion-positive thyroid cancer. Animal Toxicity Data In a 4-week repeat-dose toxicology study in non-human primates, physeal dysplasia in the femur occurred at doses resulting in exposures similar to the human exposure (AUC) at the clinical dose of 400 mg. In rats there were findings of increased physeal thickness in the femur and sternum as well as tooth (incisor) abnormalities (fractures, dentin matrix alteration, ameloblast/odontoblast degeneration, necrosis) in both 4- and 13-week studies at doses resulting in exposures similar to the human exposure (AUC) at the clinical dose of 400 mg.

Recovery was not assessed in the 13-week toxicology study, but increased physeal thickness in the femur and incisor degeneration did not show evidence of complete recovery in the 28-day rat study. Monitor growth plates in adolescent patients with open growth plates. Consider interrupting or discontinuing therapy based on the severity of any growth plate abnormalities and based on an individual risk-benefit assessment.

🧓 Geriatric Use 56 words ▾

8.5Geriatric Use Of the 540 patients in ARROW who received the recommended dose of GAVRETO at 400 mg once daily, 31% were 65 years or and over, while 7% were 75 years and over. No overall differences in pharmacokinetics (PK), safety or effectiveness were observed between patients aged 65 years or older and younger patients.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Pralsetinib is a kinase inhibitor of wild-type RET and oncogenic RET fusions (CCDC6- RET ) and mutations ( RET V804L, RET V804M and RET M918T) with half maximal inhibitory concentrations (IC 50s ) less than 0.5 nM. In purified enzyme assays, pralsetinib inhibited DDR1, TRKC, FLT3, JAK1-2, TRKA, VEGFR2, PDGFRB, and FGFR1 at higher concentrations that were still clinically achievable at C max . In cellular assays, pralsetinib inhibited RET at approximately 14-, 40-, and 12-fold lower concentrations than VEGFR2, FGFR2, and JAK2, respectively.

Certain RET fusion proteins and activating point mutations can drive tumorigenic potential through hyperactivation of downstream signaling pathways leading to uncontrolled cell proliferation. Pralsetinib exhibited anti-tumor activity in cultured cells and animal tumor implantation models harboring oncogenic RET fusions or mutations including KIF5B- RET , CCDC6- RET , RET M918T, RET C634W, RET V804E, RET V804L and RET V804M. In addition, pralsetinib prolonged survival in mice implanted intracranially with tumor models expressing KIF5B- RET or CCDC6- RET .

12.2Pharmacodynamics Pralsetinib exposure-response relationships and the time course of pharmacodynamics response have not been fully characterized. Cardiac Electrophysiology The QT interval prolongation potential of pralsetinib was assessed in 34 patients with RET -altered solid tumors administered GAVRETO at the recommended dosage. No large mean increase in QTc (> 20 ms) was detected in the study.

12.3Pharmacokinetics At 400 mg GAVRETO once daily under fasting conditions, the steady state mean [% coefficient of variation (CV%)] of maximum observed plasma concentration (C max ) and area under the concentration-time curve (AUC 0-24h ) of pralsetinib was 2,470 (55%) ng/mL and 36,700 (66%) h•ng/mL, respectively. Pralsetinib C max and AUC increased inconsistently over the dose range of 60 mg to 600 mg once daily (0.15 to 1.5 times the recommended dose). Pralsetinib plasma concentrations reached steady state by 3 to 5 days.

The mean accumulation ratio was approximately 2-fold after once-daily oral administration. Absorption The median time to peak concentration (T max ) ranged from 2 to 4 hours following single doses of pralsetinib 60 mg to 600 mg. Food Effect Following administration of a single dose of 200 mg with a high-fat meal, (approximately 800 to 1000 calories with 50 to 60% of calories from fat), the mean C max of pralsetinib was increased by 2.0-fold, the mean AUC 0-INF was increased by 2.2-fold, and the median T max was delayed from 4 to 8.5 hours, compared to the fasted state.

Distribution The mean (CV%) apparent volume of distribution (Vd/F) of pralsetinib is 303 L (68%). Protein binding of pralsetinib is 97% and is independent of concentration. The blood-to-plasma ratio is 0.6 to 0.7.

Elimination The mean (±standard deviation) plasma elimination half-life (T ½ ) of pralsetinib is 16 hours (10) following single doses and 20 hours (12) following multiple doses of pralsetinib. The mean (CV%) apparent oral clearance (CL/F) of pralsetinib is 11 L/h (66%) at steady state. Metabolism Pralsetinib is primarily metabolized by CYP3A4 and to a lesser extent by CYP2D6 and CYP1A2, in vitro.

Following a single oral dose of 310 mg of radiolabeled pralsetinib, pralsetinib metabolites from oxidation and glucuronidation were detected as 5% or less. Excretion Approximately 73% (66% as unchanged) of the total administered radioactive dose [ 14 C] pralsetinib was recovered in feces and 6% (4.8% as unchanged) was recovered in urine. Specific Populations No clinically significant differences in the PK of pralsetinib were observed based on age (19 to 87 years), sex, race (White, Black, or Asian), and body weight (32 to 128 kg).

Mild and moderate renal impairment (CLcr 30 - 89 mL/min) had no effect on the exposure of pralsetinib. Pralsetinib has not been studied in patients with severe renal impairment (CL…

🧬 Mechanism of Action 166 words ▾

📦 How Supplied / Storage and Handling 84 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING GAVRETO (pralsetinib) 100 mg, light blue, opaque, immediate release, hydroxypropyl methylcellulose (HPMC) hard capsule printed with "BLU-667" on the capsule shell body and "100 mg" on the capsule shell cap are supplied as follows: Bottles of 60 capsules (NDC 71332-006-60). Bottles of 90 capsules (NDC 71332-006-90). Bottles of 120 capsules (NDC 71332-006-12).

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] . Protect from moisture.

📦 Storage and Handling 27 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] . Protect from moisture.

📋 Description 166 words ▾

11 DESCRIPTION Pralsetinib is an oral receptor tyrosine kinase inhibitor. The chemical name for pralsetinib is ( cis )- N -(( S )-1-(6-(4-fluoro-1 H -pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-(5-methyl-1 H -pyrazol-3-ylamino)pyrimidin-2-yl)cyclohexanecarboxamide. The molecular formula for pralsetinib is C 27 H 32 FN 9 O 2 , and the molecular weight is 533.61 g/mol.

Pralsetinib has the following structure: The solubility of pralsetinib in aqueous media decreases over the range pH 1.99 to pH 7.64 from 0.880 mg/mL to < 0.001 mg/mL, indicating a decrease in solubility with increasing pH. GAVRETO (pralsetinib) is supplied for oral use as immediate release hydroxypropyl methylcellulose (HPMC) hard capsules containing 100 mg pralsetinib. The capsules also contain inactive ingredients: citric acid, hydroxypropyl methylcellulose (HPMC), magnesium stearate, microcrystalline cellulose (MCC), pregelatinized starch and sodium bicarbonate.

The capsule shell consists of FD&C Blue #1 (Brilliant Blue FCF), hypromellose and titanium dioxide. The white printing ink contains butyl alcohol, dehydrated alcohol, isopropyl alcohol, potassium hydroxide, propylene glycol, purified water, shellac, strong ammonia solution 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 (Medication Guide). Serious Infections, Including Opportunistic Infections Advise patients that GAVRETO may increase the risk of serious infections and to contact their healthcare provider if they experience symptoms of infections [see Warnings and Precautions (5.1) ] . ILD/Pneumonitis Advise patients to contact their healthcare provider if they experience new or worsening respiratory symptoms [see Warnings and Precautions (5.2) ].

Hypertension Advise patients that they will require regular blood pressure monitoring and to contact their healthcare provider if they experience symptoms of increased blood pressure or elevated readings [see Warnings and Precautions (5.3) ]. Hepatotoxicity Advise patients that hepatotoxicity can occur and to immediately contact their healthcare provider for signs or symptoms of hepatotoxicity [see Warnings and Precautions (5.4) ]. Hemorrhagic Events Advise patients that GAVRETO may increase the risk for bleeding and to contact their healthcare provider if they experience any signs or symptoms of bleeding [see Warnings and Precautions (5.5) ].

Tumor Lysis Syndrome Advise patients to contact their healthcare provider promptly to report any signs and symptoms of TLS [see Warnings and Precautions (5.6) ]. Risk of Impaired Wound Healing Advise patients that GAVRETO may impair wound healing. Advise patients that temporary interruption of GAVRETO is recommended prior to any elective surgery [see Warnings and Precautions (5.7) ].

Embryo-Fetal Toxicity Advise 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 (5.8) , Use in Specific Populations (8.1) ]. Advise females of reproductive potential to use effective non-hormonal contraception during the treatment with GAVRETO and for 2 weeks after the last dose [see Use in Specific Populations (8.3) ].

Advise males with female partners of reproductive potential to use effective contraception during treatment with GAVRETO and for 1 week after the last dose [see Use in Specific Populations (8.3) ]. Lactation Advise women not to breastfeed during treatment with GAVRETO and for 1 week after the last dose [see Use in Specific Populations (8.2) ]. Infertility Advise males and females of reproductive potential that GAVRETO may impair fertility [See Use in Specific Populations (8.3) ].

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 GAVRETO on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after taking GAVRETO) [see Dosage and Administration (2.2) ].

💬 Medication Guide ~3 min read ▾

This Medication Guide has been approved by the U.S. Food and Drug Administration. Revised: 12/2025 MEDICATION GUIDE GAVRETO (gav-REH-toh) (pralsetinib) capsules, for oral use What is the most important information I should know about GAVRETO?

GAVRETO may cause serious side effects, including: Serious infections. GAVRETO may increase your risk for serious infections, including infections caused by bacteria, fungi, or viruses, or infections that can happen when your immune system is weak (opportunistic infections). These serious infections can lead to hospitalization or death.

Tell your healthcare provider right away if you get symptoms of an infection, including: chills body aches fever confusion nausea vomiting stomach pain weakness diarrhea cough or shortness of breath burning or pain when you urinate skin rash See "What are the possible side effects of GAVRETO?" for more information about side effects. What is GAVRETO? GAVRETO is a prescription medicine used to treat certain cancers caused by abnormal rearranged during transfection (RET) genes in: adults with non-small cell lung cancer (NSCLC) that has spread. adults and children 12 years of age and older with advanced thyroid cancer or thyroid cancer that has spread who require a medicine by mouth or injection (systemic therapy) and who have received radioactive iodine and it did not work or is no longer working.

Your healthcare provider will perform a test to make sure that GAVRETO is right for you. It is not known if GAVRETO is safe and effective when used to treat cancers caused by abnormal RET genes: in children for the treatment of NSCLC or in children younger than 12 years of age for the treatment of thyroid cancer. Before taking GAVRETO, tell your healthcare provider about all of your medical conditions, including if you: have an infection.

See "What is the most important information I should know about GAVRETO?" have lung or breathing problems other than lung cancer have high blood pressure have bleeding problems have liver problems plan to have surgery. You should stop taking GAVRETO at least 5 days before your planned surgery. See "What are the possible side effects of GAVRETO?" are pregnant or plan to become pregnant.

GAVRETO can harm your unborn baby. Females who are able to become pregnant: Your healthcare provider will do a pregnancy test before you start treatment with GAVRETO. You should use an effective form of non-hormonal birth control (contraception) during treatment and for 2 weeks after your last dose of GAVRETO.

Birth control methods that contain hormones (such as birth control pills, injections or transdermal system patches) may not work as well during treatment with GAVRETO. Talk to your healthcare provider about birth control methods that may be right for you during this time. Tell your healthcare provider right away if you become pregnant or think you might be pregnant during treatment with GAVRETO.

Males with female partners who are able to become pregnant: You should use effective birth control (contraception) during treatment and for 1 week after your last dose of GAVRETO. are breastfeeding or plan to breastfeed. It is not known if GAVRETO passes into your breast milk. Do not breastfeed during treatment and for 1 week after your last dose of GAVRETO.

Tell your healthcare provider about all the medicines you take , including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking GAVRETO with other medicines may affect how GAVRETO works. How should I take GAVRETO?

Take GAVRETO exactly as your healthcare provider tells you to take it. Take your prescribed dose of GAVRETO 1 time each day. Take GAVRETO on an empty stomach.

Do not eat for at least 2 hours before and at least 1 hour after taking GAVRETO. Do not change your dose or stop taking GAVRETO unless your healthcare provider tells you to. Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with GAVRETO if you develop side…

Glossary — plain-language definitions of medical terms used in this label:

in vitro: In a laboratory dish or test tube rather than in a living person or animal; results may not carry over to people.

Absorption: How a medicine moves from where it is taken, such as the stomach or gut, into the bloodstream.

accumulation: A buildup of a medicine in the body when new doses are taken before earlier ones are fully removed.

adverse reaction: An unwanted or harmful effect that a medicine causes in the body.

Adverse Reactions: Unwanted or harmful effects that people experienced while taking a medicine, listed on its official label.

alkaline phosphatase: An enzyme measured in a blood test; higher levels can point to problems with the liver, bile ducts, or bones.

ALT: A liver enzyme (alanine aminotransferase) checked by a blood test; raised levels can signal that the liver is irritated or damaged.

anemia: A low level of red blood cells or the oxygen-carrying protein inside them, which can cause tiredness, weakness, and paleness.

AST: A liver enzyme (aspartate aminotransferase) measured in a blood test; higher levels may point to liver or sometimes muscle injury.

AUC: A measure of total drug exposure over time, showing how much medicine the blood is exposed to overall.

baseline: A person's starting condition, measured before treatment begins, used to see how much they change later on.

bilirubin: A yellow substance the liver normally clears from the blood; high levels can turn the skin or the whites of the eyes yellow.

Boxed Warning: The strongest safety warning the FDA can require, set inside a bold black border because the risk it describes can be very serious.

clearance: How quickly the body removes a medicine from the blood, usually through the liver and kidneys.

Clinical Pharmacology: The label section explaining how a medicine works in the body and how the body processes it.

Clinical Studies: The label section summarizing the research trials used to show that a medicine works and is acceptably safe.

constipation: Having bowel movements less often than usual, or passing stools that are hard, dry, and difficult to move.

contraception: Methods used to prevent pregnancy, such as birth control pills, condoms, or an intrauterine device.

Contraindications: A list of situations or health conditions in which a medicine should not be used because the chance of harm is too high.

CYP1A2: A liver enzyme that breaks down certain medicines and whose activity can be changed by cigarette smoke.

CYP2D6: A liver enzyme that breaks down many medicines; people inherit different versions, so it works faster in some and slower in others.

CYP3A4: One of the most important liver and gut enzymes, responsible for breaking down a large share of all medicines.

diarrhea: Loose, watery bowel movements that happen more often than normal.

Distribution: How a medicine spreads from the blood into the body's tissues and organs after it is absorbed.

Dosage and Administration: The label section explaining how much of a medicine to use and how to take or give it.

dose reduction: Lowering the amount of a medicine, often to ease side effects or fit a person's needs.

Drug Interactions: The label section listing other medicines, foods, or substances that can change how a medicine works or raise the chance of side effects.

dyspnea: The medical word for shortness of breath, or the feeling that you cannot get enough air.

edema: Swelling caused by extra fluid trapped in the body's tissues.

efficacy: How well a treatment works under the controlled conditions of a clinical study.

Elimination: The overall removal of a medicine from the body by breaking it down and passing it out.

embolism: A blockage of a blood vessel by a clot or other material that has traveled from elsewhere in the body.

embryo-fetal toxicity: Harm to a developing baby in the womb, such as birth defects, slowed growth, or loss of the pregnancy.

estimated background risk: The normal chance that any pregnancy will have a birth defect or problem, even without taking any medicine.

Excretion: How the body removes a medicine or its leftover pieces, mainly through the urine or stool.

fertility: The natural ability to become pregnant or to father a child.

fetal harm: Injury or damage to a developing baby while it is growing inside the womb.

food effect: A change in how much or how fast a medicine is absorbed when it is taken with food.

Full Prescribing Information: The complete, detailed label for a prescription medicine that follows the summary highlights.

glucuronidation: The process where enzymes attach a sugar-like molecule to a drug so it dissolves in water and leaves the body.

Half-life: The time it takes for the amount of medicine in the blood to drop by half.

hemoglobin: The iron-containing protein inside red blood cells that carries oxygen throughout the body.

hemorrhage: Bleeding, especially heavy or uncontrolled bleeding, either inside the body or from an outside wound.

hepatotoxicity: Damage to the liver caused by a medicine or other substance.

How Supplied/Storage and Handling: The label section describing the forms and strengths a medicine comes in and how to store it properly.

hypertension: Blood pressure that stays higher than normal, commonly called high blood pressure.

Indications and Usage: The label section stating which medical conditions the FDA has officially approved the medicine to treat, prevent, or manage.

inducer: A substance that speeds up an enzyme, which can lower the levels of drugs that enzyme breaks down.

inhibitor: A substance that blocks an enzyme or transporter, which can raise the levels of drugs it normally handles.

interstitial lung disease: A group of conditions in which the tissue around the lungs' air sacs becomes scarred or inflamed, making breathing harder.

lactation: The making and release of milk from a mother's breasts after giving birth.

Mechanism of Action: How a medicine produces its effect in the body, described at the level of cells or body chemistry.

Medication Guide: An FDA-approved handout written for patients that explains important safety information about certain medicines in plain language.

Metabolism: How the body chemically changes a medicine, usually in the liver, into other substances.

NDC: A unique number that identifies a specific medicine, its maker, strength, and package size.

Nonclinical Toxicology: The label section summarizing safety findings from laboratory and animal studies, rather than from studies in people.

open-label: A study in which both the patients and their doctors know which treatment each person is receiving.

organogenesis: The early stage of pregnancy when the developing baby's organs are first forming.

P-glycoprotein: A tiny pump in cells that pushes certain medicines back out, affecting how much of a medicine is absorbed or stays in the body.

P-gp: A protein pump in cells that pushes certain drugs back out, limiting how much is absorbed or reaches tissues.

Patient Counseling Information: The label section telling health professionals what to explain to patients about using a medicine safely.

Pharmacokinetics: The study of how the body takes in a medicine, spreads it around, breaks it down, and removes it over time.

plasma concentration: The amount of medicine measured in the liquid part of the blood at a given time.

pleural effusion: A buildup of fluid in the space between the lungs and the chest wall.

pneumonitis: Inflammation of the lung tissue that is not caused by an infection and can lead to cough and breathlessness.

Prescribing Information: The official, detailed document approved by the FDA that tells health professionals how to use a prescription medicine.

protein binding: How much of a medicine sticks to proteins in the blood instead of moving freely through the body.

pulmonary embolism: A blood clot that has traveled to the lungs and blocks blood flow there, which can make breathing hard.

pyrexia: A raised body temperature; a fever.

QTc: A number from a heart tracing (ECG) that measures the heart's electrical recovery time, adjusted for the heart rate.

randomized: Assigned to a treatment group purely by chance, like a coin flip, so the groups being compared start out fair and similar.

receptor: A special docking spot on a cell that a medicine or natural body chemical attaches to in order to trigger an effect.

refractory: Describing a disease that does not respond to, or improve with, treatment.

renal impairment: Reduced kidney function, meaning the kidneys do not filter waste and fluid from the blood as well as normal.

reproductive potential: The ability to have children, meaning a person who could become pregnant or could father a child.

seizure: A sudden burst of abnormal electrical activity in the brain that can cause shaking, staring, confusion, or loss of awareness.

sepsis: A serious, body-wide reaction to an infection in which the body's own response can start to injure its tissues and organs.

steady state: The point where the amount of medicine going in equals the amount leaving, so blood levels stay fairly even.

transdermal: Delivered through the skin, usually from a patch, into the bloodstream over time.

treatment-emergent: Describes a side effect that first appears, or gets worse, after a person starts taking a treatment.

tumor lysis syndrome: A serious condition where many cancer cells break apart quickly, releasing their contents and upsetting the body's balance of salts and waste products.

Use in Specific Populations: The label section describing how a medicine affects particular groups, such as pregnant people, children, or older adults.

volume of distribution: A calculated value showing how widely a medicine spreads into body tissues versus staying in the blood.

Warnings and Precautions: The label section describing serious risks to know about and safety steps to follow while using a medicine.

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

← 71332-0005-01 · Rigel 71332-0007-30 · Rigel →

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.

Gavreto Pralsetinib 100 mg Capsule, 120-count

🆔 Identity & classification

🏷️ RxNorm drug class

🏭 Manufacturer & labeler

🩺 Clinical

Patient education

Supplement & herbal interactions

💊 What it looks like

🧪 Inactive Ingredients / Excipients

Inactive ingredient FAQ

💲 Pricing

🔁 Therapeutic equivalents

⏳ Availability & generic status

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

🔬 Reported adverse events (FAERS)

Top reported reactions

Reporter sex

Serious outcomes

📦 Packaging — all sizes for this product

Pack size FAQ

🧭 About this NDC listing & data coverage

Questions about this listing

📄 Full prescribing information FDA SPL

12 CLINICAL PHARMACOLOGY

🔗 Related NDC lookups

💊 Related drugs in this class