Drug intelligence / Profile preview

MK-1084 + pembrolizumab + carboplatin + pemetrexed

Development stage
Phase 1
Lead developer
Merck
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
Oral, Intravenous
01

Overview

MK-1084 + pembrolizumab + carboplatin + pemetrexed is an investigational **four-drug combination regimen** under clinical development, primarily for first-line treatment of metastatic non-small cell lung cancer (NSCLC) in patients with KRAS G12C mutations and high PD-L1 expression. **MK-1084** is a selective oral KRAS G12C inhibitor that targets tumor cells harboring this mutation, disrupting KRAS-mediated oncogenic signaling. **Pembrolizumab** (KEYTRUDA) is a monoclonal antibody acting as a PD-1 immune checkpoint inhibitor, enhancing antitumor immune response. **Carboplatin** and **pemetrexed** are chemotherapeutics: carboplatin is a platinum agent causing DNA crosslinking and apoptosis, while pemetrexed is an antifolate that interferes with folate-dependent enzymes involved in DNA synthesis. The combination leverages targeted therapy, immunotherapy, and chemotherapy for synergistic antineoplastic effects[1][2][4][5][6][7].

Other names
pembrolizumabcarboplatinpemetrexed
02

Targets

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

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