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devimistat + trifluridine + tipiracil + regorafenib
- Development stage
- Unknown
- Lead developer
- Cornerstone Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Devimistat + trifluridine + tipiracil + regorafenib is a combination therapy being investigated for the treatment of advanced or metastatic solid tumors, particularly metastatic colorectal cancer (mCRC). Devimistat (CPI-613), developed by Rafael Pharmaceuticals (formerly Cornerstone Pharmaceuticals), is a first-in-class small molecule lipoate analog that selectively targets the mitochondrial metabolism of cancer cells. It inhibits the pyruvate dehydrogenase (PDH) and alpha-ketoglutarate dehydrogenase (KGDH) complexes, thereby disrupting the tricarboxylic acid (TCA) cycle and inducing metabolic stress. Trifluridine/tipiracil (TAS-102) is a combination of a cytotoxic nucleoside analog and a thymidine phosphorylase inhibitor that prevents its degradation, while regorafenib is a multi-kinase inhibitor targeting pathways involved in angiogenesis (VEGFR1-3, TIE2), oncogenesis (KIT, RET, RAF), and the tumor microenvironment (PDGFR, FGFR). This combination aims to synergistically inhibit tumor growth and overcome resistance in patients who have failed standard treatment options.
- Brand names
- LonsurfStivarga
- Other names
- devimistattrifluridine/tipiracilregorafenibCPI-613 + TAS-102 + regorafenib
02
Targets
PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)TS (Thymidylate synthase)RAF1 (c-Raf-1 (Y340D/Y341D))PDH (Pyruvate dehydrogenase complex)BRAF V600EVEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)TYMP (Thymidine phosphorylase)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)α-KGDH (Alpha-ketoglutarate dehydrogenase complex)
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