Drug intelligence / Profile preview

divarasib + pembrolizumab + carboplatin + pemetrexed

Development stage
Phase 2
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination regimen** of four active agents used in investigational and early-phase clinical trials for advanced or metastatic non-squamous non-small cell lung cancer (NSCLC) with KRAS G12C mutation[3][5][7]. The regimen consists of: - **Divarasib**: an orally active small molecule inhibitor targeting KRAS G12C mutant protein, blocking oncogenic signaling. - **Pembrolizumab**: a monoclonal antibody immune checkpoint inhibitor (anti-PD-1), enhancing antitumor immune response. - **Carboplatin**: a platinum-based chemotherapy agent causing DNA crosslinking and apoptosis. - **Pemetrexed**: a folate antimetabolite chemotherapy which inhibits multiple enzymes involved in purine and pyrimidine synthesis. This combination seeks to leverage KRAS-mutant targeted therapy, immunotherapy, and chemotherapy synergistically. Trials are ongoing to evaluate efficacy, safety, and dosing in newly diagnosed, previously untreated advanced NSCLC patients[3][7].

Other names
divarasib + pembrolizumab + carboplatin + pemetrexed
02

Targets

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

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