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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors
avapritinib
L01EX18
Forms & Strengths
- Oral tablets: 25 mg
- Oral tablets: 50 mg
- Oral tablets: 100 mg
- Oral tablets: 200 mg
- Oral tablets: 300 mg
Adult Dosing
- Advanced systemic mastocytosis: 300 mg orally once daily on an empty stomach
- Indolent systemic mastocytosis: 25 mg orally once daily on an empty stomach
- PDGFRA D842V mutant GIST: 300 mg orally once daily on an empty stomach
- Modify dose for severe adverse reactions or hepatotoxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of advanced systemic mastocytosis (AdvSM)
- Treatment of indolent systemic mastocytosis (ISM)
- Treatment of unresectable or metastatic gastrointestinal stromal tumors (GIST) harboring the PDGFRA D842V mutation
Mechanism of Action
- Potent, selective inhibitor of KIT and PDGFRA mutant kinases
- Targets KIT D816V and PDGFRA D842V activating mutations associated with mastocytosis and GIST pathogenesis
Adverse Reactions
- Edema (periorbital, peripheral, facial)
- Cognitive effects (memory impairment, cognitive disorder, confusional state)
- Fatigue and asthenia
- Nausea, diarrhea, and vomiting
- Anemia and thrombocytopenia
- Increased blood bilirubin and transaminases
Drug Interactions
- Strong CYP3A inhibitors: Avoid coadministration; if unavoidable, reduce avapritinib dose
- Moderate CYP3A inhibitors: Use with caution and monitor for toxicity
- Strong and moderate CYP3A inducers: Avoid coadministration
- CYP3A substrates: Avapritinib may alter concentrations of sensitive CYP3A substrates
Curated Content: Needs Vetting Before Put to Clinical Use