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ripretinib
- Development stage
- Approved
- Lead developer
- Deciphera Pharmaceuticals
- 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
Ripretinib is a novel small molecule tyrosine kinase inhibitor specifically designed to broadly inhibit both primary and secondary mutations in KIT and PDGFRA kinases, which are commonly implicated in gastrointestinal stromal tumors (GIST) and other cancers. It acts as a "switch-control" inhibitor, uniquely targeting the switch pocket and activation loop of these kinases, thereby overcoming resistance caused by various mutations. Ripretinib is approved for use in adults with advanced GIST who have received prior treatment with three or more kinase inhibitors, including imatinib. The drug has demonstrated significant clinical benefit in prolonging progression-free survival and overall survival for this patient population[1][3][5][7].
- Brand names
- Qinlock擎乐
- Other names
- 瑞派替尼
02
Targets
BRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)
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