elisrasib

Elisrasib (D3S-001) is a next-generation, orally active small molecule inhibitor of the KRAS G12C mutation. Developed by D3 Bio, it is designed to target advanced solid tumors harboring the KRAS p.G12C mutation, including non-small cell lung cancer, colorectal cancer, and pancreatic cancer. The drug functions by covalently binding to the cysteine residue of the KRAS G12C protein, locking it in an inactive GDP-bound state and thereby inhibiting downstream oncogenic signaling. Elisrasib has demonstrated potent anti-tumor activity and complete target engagement at clinically relevant exposures. It has received Breakthrough Therapy and Orphan Drug designations from the FDA and is currently being evaluated in Phase 1/2 clinical trials as both a monotherapy and in combination with other agents like pembrolizumab or cetuximab.

Other names

2-PIPERAZINEACETONITRILE, 4-(7-(3-AMINO-2-FLUORO-5-METHYL-6-(TRIFLUOROMETHYL)PHENYL)-2-(((2R,7AS)-2-FLUOROTETRAHYDRO-1H-PYRROLIZIN-7A(5H)-YL)METHOXY)-7,8-DIHYDRO-5H-PYRANO(4,3-D)PYRIMIDIN-4-YL)-1-(2-FLUORO-1-OXO-2-PROPEN-1-YL)-, (2S)