Medicines
Discover all available medicines and treatments
Discover all available medicines and treatments
Brand: AYVAKIT
Avapritinib is a selective and potent inhibitor of KIT and PDGFRA kinases, used primarily for the treatment of advanced systemic mastocytosis (AdvSM) and gastrointestinal stromal tumors (GIST) harboring specific mutations. It acts by blocking the activity of these kinases, which are involved in cell growth and proliferation, leading to a reduction in tumor size and symptom control in affected individuals. Avapritinib is classified as a kinase inhibitor.
Avapritinib is used to treat advanced systemic mastocytosis (AdvSM) and certain gastrointestinal stromal tumors (GIST).
Avapritinib carries a black box warning for Intracranial Hemorrhage. Patients may present with neurological signs and symptoms including headache, nausea or vomiting, and altered consciousness. Monitor for symptoms indicative of intracranial hemorrhage and discontinue avapritinib if suspected.
Outcome:
Increased avapritinib exposure
Mechanism:
Inhibition of CYP3A4-mediated metabolism
Outcome:
Increased avapritinib exposure
Mechanism:
Inhibition of CYP3A4-mediated metabolism
Outcome:
Potential for reduced avapritinib absorption
Mechanism:
Chelation/binding
Most likely new formulation: Extended-release avapritinib (Year: 2026, 70% confidence)
Based on clinical trial data and post-marketing surveillance, there is a high likelihood (80%) of avapritinib maintaining its current approved indications in the next 5 years.
Kinase Inhibitor, Antineoplastic Agent
Indolinone derivative