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olomorasib + pembrolizumab + pemetrexed + platinum chemotherapy
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
- 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
DNADHFR (Dihydrofolate reductase)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)
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