Drug intelligence / Profile preview

elironrasib + pembrolizumab

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

Overview

Elironrasib + pembrolizumab is an investigational combination regimen consisting of elironrasib (RMC-6291), an oral, covalent, tri-complex inhibitor of the active GTP-bound state of mutant KRAS G12C (RAS(ON) G12C), and pembrolizumab (Keytruda), an approved anti-PD-1 monoclonal antibody. Elironrasib works by binding to the abundant intracellular chaperone protein cyclophilin A (CypA) to form a binary complex that subsequently binds to and covalently inhibits active KRAS G12C, preventing downstream oncogenic signaling. Pembrolizumab blocks the interaction between PD-1 and its ligands, PD-L1 and PD-L2, thereby revitalizing T-cell-mediated antitumor immune responses. Developed by Revolution Medicines, this combination is being evaluated in Phase 1b/2 and Phase 3 clinical trials (such as RMC-LUNG-101 and RASolve 307) as a first-line treatment for patients with advanced or metastatic KRAS G12C-mutated non-small cell lung cancer (NSCLC) and other solid tumors.

Other names
RMC-6291 + pembrolizumabRMC-6291 plus pembrolizumabRMC6291 plus pembrolizumabRMC 6291 plus pembrolizumabelironrasib + pembrolizumabelironrasib plus pembrolizumab
02

Targets

KRAS (Kirsten rat sarcoma viral oncogene homolog)PPIA (Peptidyl-prolyl cis-trans isomerase A)PDCD1 (Programmed cell death protein 1 receptor)

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