Drug intelligence / Profile preview

RMC-6291 + RMC-6236

Development stage
Unknown
Lead developer
REVOLUTION Medicines
Modality
Small Molecules
Administration
Oral
01

Overview

**RMC-6291 + RMC-6236** is a combination of two investigational small molecule inhibitors targeting RAS proteins in cancer. RMC-6291 is a G12C-selective RAS(ON) inhibitor, while RMC-6236 is a multi-selective RAS(ON) inhibitor. Together, they are designed to inhibit RAS signaling in cancers harboring KRAS G12C mutations, with RMC-6291 offering specificity for KRAS G12C and RMC-6236 providing broader RAS pathway inhibition. Preclinical studies show that the combination leads to more durable RAS pathway suppression, greater induction of apoptosis, and improved anti-tumor responses compared to single agents, particularly in xenograft models of non-small cell lung cancer (NSCLC) that are resistant to other KRAS G12C inhibitors. The combination is currently being evaluated in a Phase 1b clinical trial for patients with advanced KRASG12C-mutated solid tumors, including NSCLC, colorectal cancer, and pancreatic ductal adenocarcinoma. Both drugs are investigational and not yet approved by regulatory authorities[1][2][3][5][6][7][9].

02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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