Avapritinib
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami-Ardakani
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Overview
Avapritinib is a Tyrosine Kinase Inhibitor that is FDA approved for the treatment of Gastrointestinal stromal tumor (GIST) with PDGFRA exon 18 mutations, Advanced systemic mastocytosis (AdvSM), and Indolent systemic mastocytosis (ISM). Common adverse reactions include Nausea, vomiting, diarrhea, constipation, abdominal pain, fatigue, edema, decreased appetite, cognitive impairment, dizziness, rash, and hair color changes..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
GIST with PDGFRA exon 18 mutations: 300 mg orally once daily on an empty stomach.
Advanced systemic mastocytosis (AdvSM): 200 mg orally once daily on an empty stomach.
Indolent systemic mastocytosis (ISM): 25 mg orally once daily on an empty stomach.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Avapritinib in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Avapritinib in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Avapritinib is not approved for use in pediatric patients.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Avapritinib in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Avapritinib in pediatric patients.
Contraindications
Hypersensitivity to avapritinib or any of its components.
Warnings
Intracranial hemorrhage: Monitor for signs and symptoms; discontinue if severe.
Cognitive effects: Includes memory impairment, confusion, and hallucinations; may require dose modification or discontinuation.
Embryo-fetal toxicity: Can cause fetal harm; advise effective contraception during treatment and for 6 weeks after the final dose.
Adverse Reactions
Clinical Trials Experience
Gastrointestinal: Nausea, vomiting, diarrhea, constipation, abdominal pain.
General: Fatigue/asthenia, edema, decreased appetite.
Neurological: Cognitive impairment, dizziness.
Dermatological: Rash, hair color changes.
Others: Increased lacrimation.
Postmarketing Experience
There is limited information regarding Avapritinib Postmarketing Experience in the drug label.
Drug Interactions
CYP3A inhibitors: Concomitant use may increase avapritinib plasma concentrations; avoid use.
CYP3A inducers: Concomitant use may decrease avapritinib plasma concentrations; avoid use.
Sensitive CYP3A substrates: Avapritinib may increase their plasma concentrations; monitor for adverse reactions.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Avapritinib in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Avapritinib in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Avapritinib during labor and delivery.
Nursing Mothers
Advise women not to breastfeed during treatment and for 2 weeks after the final dose.
Pediatric Use
There is no FDA guidance on the use of Avapritinib in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Avapritinib in geriatric settings.
Gender
There is no FDA guidance on the use of Avapritinib with respect to specific gender populations.
Race
There is no FDA guidance on the use of Avapritinib with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Avapritinib in patients with renal impairment.
Hepatic Impairment
For patients with severe hepatic impairment (Child-Pugh Class C), a lower starting dose is recommended due to increased avapritinib exposure.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Avapritinib in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Avapritinib in patients who are immunocompromised.
Administration and Monitoring
Administration
Administer avapritinib orally on an empty stomach, at least 1 hour before or 2 hours after a meal.
If a dose is missed, do not make up for the missed dose within 8 hours of the next scheduled dose.
If vomiting occurs after taking avapritinib, do not take an additional dose; continue with the next scheduled dose.
Monitoring
Prior to initiating treatment, obtain a complete blood count (CBC), including platelet count.
Monitor platelet counts every 2 weeks for the first 8 weeks of treatment, then as clinically indicated.
Monitor for signs and symptoms of intracranial hemorrhage, cognitive effects, and other adverse reactions.
IV Compatibility
Not applicable.
Overdosage
There is limited information regarding Avapritinib overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Avapritinib Pharmacology in the drug label.
Mechanism of Action
Avapritinib is a selective tyrosine kinase inhibitor that targets KIT and PDGFRA mutations, including PDGFRA D842V and KIT D816V mutations, which are associated with GIST and systemic mastocytosis.
Structure
There is limited information regarding Avapritinib Structure in the drug label.
Pharmacodynamics
Avapritinib inhibits the autophosphorylation of mutant KIT and PDGFRA kinases, leading to the inhibition of downstream signaling pathways involved in cell proliferation.
Pharmacokinetics
Absorption: Peak plasma concentration achieved approximately 2–4 hours after oral administration.
Distribution: Extensively distributed with a volume of distribution of approximately 15,000 L.
Metabolism: Primarily metabolized by CYP3A4.
Elimination: Eliminated mainly via feces; terminal half-life is approximately 32 hours.
Nonclinical Toxicology
There is limited information regarding Avapritinib Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Avapritinib Clinical Studies in the drug label.
How Supplied
Form: Film-coated tablets.
Strengths: 25 mg, 50 mg, 100 mg, 200 mg, and 300 mg.
Packaging: Available in bottles of 30 tablets.
Storage
Storage Conditions: Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F to 86°F).
Handling: Protect from moisture and keep in the original container.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
Advise patients to take avapritinib on an empty stomach, at least 1 hour before or 2 hours after a meal.
Inform patients about the potential for cognitive effects and to report symptoms such as memory impairment or confusion.
Advise women of reproductive potential to use effective contraception during treatment and for 6 weeks after the final dose.
Instruct patients to avoid grapefruit products during treatment.
Precautions with Alcohol
Alcohol-Avapritinib interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
Ayvakit Manufactured by Blueprint Medicines Corporation.
Look-Alike Drug Names
There is limited information regarding Avapritinib Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.