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binimetinib + carboplatin + pemetrexed
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a combination regimen consisting of three drugs: binimetinib, carboplatin, and pemetrexed. Binimetinib is a selective inhibitor of MEK1/2, part of the MAPK/ERK pathway involved in cell proliferation and survival. Carboplatin is a platinum-based chemotherapeutic agent that causes DNA crosslinking and apoptosis in rapidly dividing cells. Pemetrexed is an antifolate chemotherapy that inhibits multiple enzymes involved in folate metabolism and DNA synthesis, including thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase. This combination has been investigated primarily for advanced non-squamous non-small cell lung cancer (NSCLC), particularly as first-line therapy or for patients with specific mutations such as MAP2K1 or KRAS[1][2][4]. The regimen aims to combine targeted inhibition of the MAPK pathway with cytotoxic chemotherapy to improve antitumor efficacy.
- Other names
- binimetinib + carboplatin + pemetrexed
02
Targets
DHFR (Dihydrofolate reductase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)TS (Thymidylate synthase)Pt-DNA adduct (DNA-oxaliplatin adduct)GART (GAR transformylase)
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