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VS-7375 + carboplatin + pemetrexed + pembrolizumab
- Development stage
- Phase 2
- Lead developer
- GenFleet Therapeutics
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
VS-7375 + carboplatin + pemetrexed + pembrolizumab is an investigational combination regimen consisting of VS-7375 (GFH375), an oral, highly selective, non-covalent KRAS G12D dual ON/OFF inhibitor, combined with standard-of-care first-line chemo-immunotherapy (carboplatin, pemetrexed, and pembrolizumab). Developed by Verastem Oncology in collaboration with GenFleet Therapeutics, this combination is being evaluated for the first-line treatment of patients with advanced non-small cell lung cancer (NSCLC) harboring a KRAS G12D mutation. VS-7375 is designed to bind both the active (ON) and inactive (OFF) states of KRAS G12D, potentially providing more complete pathway inhibition than single-state inhibitors. The combination is being studied in the Phase 1/2 TARGET-D 101 trial (NCT07020221), where early clinical data demonstrated encouraging antitumor activity with a high objective response rate in patients with KRAS G12D-mutant lung adenocarcinoma.
- Other names
- GFH375 + carboplatin + pemetrexed + KeytrudaGFH375 + carboplatin + pemetrexed + pembrolizumabVS-7375 + carboplatin + pemetrexed + Keytruda
02
Targets
DNADHFR (Dihydrofolate reductase)KRAS (Kirsten rat sarcoma viral oncogene homolog)GART (GAR transformylase)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)
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