Drug reference

ripretinib

kinase inhibitor (PDGFR, KIT, VEGFR2, TIE2) · Antineoplastic agent

kinase inhibitor (PDGFR, KIT, VEGFR2, TIE2)Antineoplastic agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AmprenavirSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter
BoceprevirSevereDatabaseDDInter

Mechanism

Ripretinib is an orally bioavailable kinase inhibitor of the PDGFR, wild-type and mutant KIT, and other kinases including VEGFR2 and tyrosine kinase with Ig and EGF domains (TIE) 2.

Indications

advanced GIST who have received prior treatment with three or more kinase inhibitors, including imatinib

Pharmacokinetics

Half-life

14.8 h

Metabolism

CYP3A

Side effects

Common

palmar-plantar erythrodysesthesia syndrome (PPES)nauseavomitingconstipationdiarrheaalopecia

Serious

hypertension
cardiac dysfunction

Pregnancy & lactation

Pregnancy

Drug interactions

Amprenavir

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Carbamazepine

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Ceritinib

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Clarithromycin

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Cobicistat

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Conivaptan

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Delavirdine

Severe

Database

Clinical effect not specified

Source: DDInter

Enzalutamide

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Fosamprenavir

Severe

Database

Clinical effect not specified

Source: DDInter

Related guidelines

Heart failure in diabetes

RSSDI · Cardiology · 2023

Hypertension in adults

ICMR · Cardiology · 2019

Chronic kidney disease — assessment and management

NICE · Nephrology · 2021

Hypertrophic cardiomyopathy

ESC · Cardiology · 2026

Type 2 diabetes in adults

NICE · Endocrinology · 2022

Ask House about ripretinib

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Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team