阿伐替尼 (Ayvakit, Ayvakyt)

概览

Avapritinib is a selective tyrosine kinase inhibitor being investigated for the treatment of multidrug resistant gastrointestinal tumors.

作用机制

Avapritinib has a negative modulating effect on the transporters ABCB1 and ABCG2, which mediate the multidrug resistance phenotype of some cancers. This modulation may be due to interactions of avapritinib with the drug binding pocket of these transporters. Negative modulation of these transporters, resensitizes cancerous cells to treatment with chemotherapeutic agents like paclitaxel.

适应症

Avapritinib is indicated for the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations. It is also used to treat adult patients with advanced systemic mastocytosis (AdvSM). AdvSM includes patients with aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia. However, it is not recommended for the treatment of patients with AdvSM with platelet counts of less than 50 X 10 L.

• Advanced Systemic Mastocytosis (AdvSM)
• Aggressive Systemic Mastocytosis
• Indolent Systemic Mastocytosis
• Mast Cell Leukemia (MCL)
• Metastatic Gastrointestinal Stromal Tumor (GIST)
• Systemic Mastocytosis With an Associated Hematological Neoplasm
• Unresectable Gastrointestinal stromal tumor