Drug intelligence / Profile preview

olomorasib + pembrolizumab + pemetrexed

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

Overview

olomorasib + Keytruda + pemetrexed is an investigational combination regimen being evaluated for the first-line treatment of advanced or metastatic non-small cell lung cancer (NSCLC) harboring a KRAS G12C mutation. The regimen combines olomorasib (LY3537982), a potent and highly selective oral small-molecule inhibitor of GDP-bound KRAS G12C developed by Eli Lilly; pembrolizumab (Keytruda), a PD-1-blocking monoclonal antibody developed by Merck & Co.; and pemetrexed, an antifolate chemotherapy agent. In the global Phase 3 SUNRAY-01 trial (NCT06119581), this combination is being evaluated with or without platinum chemotherapy (cisplatin or carboplatin) to compare its efficacy against standard-of-care chemoimmunotherapy. The FDA has granted breakthrough therapy designation to the doublet of olomorasib and pembrolizumab for first-line KRAS G12C-mutant NSCLC with PD-L1 expression of 50% or higher.

Brand names
Armisarte
Other names
LY3537982 + Keytruda + pemetrexedLY3537982 + pembrolizumab + pemetrexedolomorasib + Keytruda + pemetrexedolomorasib + pembrolizumab + pemetrexedolomorasib plus Keytruda and pemetrexedolomorasib plus pembrolizumab and pemetrexed
02

Targets

ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)CD274 (Programmed cell death protein 1 ligand 1)RAF1 (c-Raf-1 (Y340D/Y341D))DHFR (Dihydrofolate reductase)GART (GAR transformylase)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)PDCD1 (Programmed cell death protein 1 receptor)PDCD1LG2 (Programmed cell death 1 ligand 2)TS (Thymidylate synthase)

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