Drug intelligence / Profile preview

daraxonrasib + elironrasib + zoldonrasib

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

Overview

Daraxonrasib (RMC-6236), elironrasib (RMC-6291), and zoldonrasib (RMC-9805) are investigational oral RAS(ON) inhibitors from Revolution Medicines targeting the active GTP-bound ("ON") state of mutant RAS proteins to suppress oncogenic signaling in RAS-driven cancers. Daraxonrasib is a pan-RAS(ON) multi-selective inhibitor active against mutant and wild-type K/N/H-RAS variants; elironrasib is KRAS G12C-selective; and zoldonrasib is KRAS G12D-selective. The combination is being explored preclinically and in early clinical trials to enhance RAS pathway suppression, overcome monotherapy resistance, and improve antitumor activity in models of KRAS-mutant colorectal cancer (CRC), non-small cell lung cancer (NSCLC), and pancreatic ductal adenocarcinoma (PDAC), often with deeper tumor regressions than single agents.[1][3][5]

02

Targets

HRAS (H-Ras protein)GTP-bound Kirsten rat sarcoma viral oncogene homolog G12DKRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)PPIA (Peptidyl-prolyl cis-trans isomerase A)

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