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avapritinib
- Development stage
- Approved
- Lead developer
- Blueprint Medicines
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Avapritinib is a selective small molecule tyrosine kinase inhibitor developed for the treatment of certain cancers and blood disorders. It is primarily indicated for adults with unresectable or metastatic gastrointestinal stromal tumors (GIST) harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations, as well as for advanced systemic mastocytosis (AdvSM), which includes aggressive systemic mastocytosis, systemic mastocytosis with associated hematological neoplasm, and mast cell leukemia. Avapritinib works by inhibiting mutant forms of PDGFRA and KIT kinases that drive tumor proliferation and are often resistant to other therapies. It also inhibits wild-type KIT, PDGFRB, and Colony stimulating factor 1 receptor (CSF1R). Additionally, avapritinib can modulate ABC transporter proteins such as ABCB1 and ABCG2 to help overcome multidrug resistance in cancer cells[1][2][3][5][6][8].
- Brand names
- Ayvakit
- Other names
- avapritinibBLU-285BLU285BLU 285AyvakitAyvakyt
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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