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avapritinib

Brand and Other Names: AYVAKIT
Mechanism of Action:

Avapritinib is a tyrosine kinase inhibitor that targets KIT D816V, PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC50s) less than 25 nM in biochemical assays. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor and mast cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1.

Indications:

Gastrointestinal Stromal Tumor (GIST):

  • For adults with unresectable or metastatic GIST harboring a PDGFRA exon 18 mutation, including PDGFRA D842V.

Advanced Systemic Mastocytosis (AdvSM):

  • Includes aggressive systemic mastocytosis (ASM), SM-AHN, and mast cell leukemia (MCL).

Indolent Systemic Mastocytosis (ISM)

Route: oral
Dose:

GIST: 300 mg once daily

AdvSM: 200 mg once daily

ISM: 25 mg once daily

Adverse Reactions:
  • Intracranial hemorrhage 
  • Cognitive effects 
  • Photosensitivity
Contraindication:

None

Warnings and Precautions:

Intracranial Hemorrhage: Occurred in 2.9% of GIST/AdvSM patients; permanently discontinue if it occurs.

Cognitive Effects: Includes memory issues, confusion, somnolence. May require dose reduction or discontinuation.

Photosensitivity: Use sun protection.

Embryo-Fetal Toxicity: Can cause fetal harm. Use contraception during and after therapy.

See package insert for full prescribing information.