RCZY-690 / Rongchang Pharma - LARVOL DELTA

RCZY-690 and RCZY-680: Novel, highly potent, and orally bioavailable, tri-complex pan RAS-MULTI(ON) inhibitors with distinctive oral pharmacokinetic profiles, exhibiting broad anti-tumor activities in CDX models (AACR 2025) - "Although KRAS G12C inhibitors like sotorasib and adagrasib show promise for NSCLC, resistance develops rapidly, and effective therapies are still lacking for over 85% of RAS-driven or RAS-amplified cancers.Herein, we report RCZY-690 and RCZY-680 as novel and potent tri-complex RAS-MULTI(ON) inhibitors...This approach, exemplified by the lead compound RMC-6236, has shown promise in KRAS-mutant PDAC and NSCLC patients in phase 1 study...The superior anti-tumor efficacy may be attributed to their highly potent cellular cytotoxicity, long mouse half-lives (10.1 h and 4.8 h, respectively), and high oral exposure levels. In conclusion, RCZY-690 and RCZY-680 are tri-complex pan RAS-MULTI(ON) inhibitors with best-in-class clinical potential for treating RAS-driven solid tumors."

PK/PD data • Colorectal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • BRAF • DUSP6 • HRAS • KRAS • NRAS