Drug intelligence / Profile preview

olomorasib + pembrolizumab + pemetrexed + platinum chemotherapy

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen used for the treatment of **advanced or metastatic non–small cell lung cancer (NSCLC) with KRAS G12C mutations**. It consists of: - **Olomorasib:** A second-generation, highly selective small molecule inhibitor of GDP-bound KRAS G12C, targeting a driver mutation in NSCLC. - **Pembrolizumab:** A monoclonal antibody immune checkpoint inhibitor, targeting PD-1, used to promote anti-tumor immunity. - **Pemetrexed:** An antimetabolite chemotherapy agent that inhibits folate-dependent enzymes essential for DNA synthesis. - **Platinum chemotherapy (usually cisplatin or carboplatin):** Alkylating agents that induce DNA crosslinking and apoptosis in rapidly dividing cells. The regimen is being evaluated as first-line treatment in patients with unresectable advanced or metastatic NSCLC, especially those with **PD-L1 expression ≥50%**, as part of global phase 3 trials (SUNRAY-01, NCT06119581). Olomorasib and pembrolizumab have received FDA breakthrough therapy designation for this indication[1][4][8].

Other names
olomorasib + pembrolizumab + pemetrexed + platinum chemotherapy
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)DNAKRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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