Drug intelligence / Profile preview

RMC-6236 + cetuximab

Development stage
Unknown
Lead developer
REVOLUTION Medicines
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

RMC-6236 + cetuximab is an investigational combination therapy comprising RMC-6236, a small molecule RAS(ON) multi-selective noncovalent inhibitor that targets the active, GTP-bound state of both mutant and wild-type RAS isoforms, and cetuximab, a monoclonal antibody that inhibits the epidermal growth factor receptor (EGFR). RMC-6236 (daraxonrasib) binds to a composite pocket on RAS formed with cyclophilin A, blocking downstream signaling through the MAPK pathway in RAS-driven cancers, including tumors with a broad range of KRAS mutations such as G12D, G12V, G12A, and G13D, as well as wild-type RAS[1][2][3]. Cetuximab binds to EGFR, preventing ligand-mediated receptor activation and downstream signaling. The combination is being explored in patients with advanced solid tumors, especially those harboring KRAS mutations, to address resistance mechanisms and enhance antitumor activity seen in preclinical and early clinical studies[1][2].

Other names
daraxonrasib + cetuximab
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)KRAS (Kirsten rat sarcoma viral oncogene homolog)PPIA (Peptidyl-prolyl cis-trans isomerase A)

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