Drug intelligence / Profile preview

adagrasib + pembrolizumab + pemetrexed + cisplatin + carboplatin

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This regimen is a **combination therapy** consisting of the KRAS G12C inhibitor adagrasib, the PD-1 immune checkpoint inhibitor pembrolizumab, and the chemotherapeutic agents pemetrexed, cisplatin, and carboplatin. Adagrasib is a selective, covalent inhibitor of the KRAS G12C mutant protein, disrupting oncogenic signaling in tumors harboring this mutation. Pembrolizumab is a monoclonal antibody that blocks the interaction between PD-1 and its ligands, restoring T-cell mediated antitumor activity (immunotherapy). Pemetrexed is a multitargeted antifolate cytotoxic chemotherapy agent that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase, interfering with DNA and RNA synthesis. Cisplatin and carboplatin are platinum-based DNA crosslinking agents that inhibit DNA replication and transcription. This combination is under investigation for first-line treatment of advanced or metastatic non-small cell lung cancer (NSCLC) with KRAS G12C mutation, typically in non-squamous histology and in patients with various PD-L1 expression levels[1][3][5].

Brand names
KeytrudaAlimtaPlatinolParaplatin
Other names
adagrasib + pembrolizumab + pemetrexed + cisplatin + carboplatin
02

Targets

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

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