Drug intelligence / Profile preview

fruquintinib + sintilimab + pemetrexed + carboplatin

Development stage
Unknown
Lead developer
HUTCHMED
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a four-drug combination regimen consisting of fruquintinib, sintilimab, pemetrexed, and carboplatin. Fruquintinib is a highly selective small molecule inhibitor of vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR1/2/3), which inhibits tumor angiogenesis. Sintilimab is a monoclonal antibody targeting programmed death-1 (PD-1), functioning as an immune checkpoint inhibitor to enhance anti-tumor immune responses. Pemetrexed is an antimetabolite chemotherapy agent that inhibits multiple folate-dependent enzymes involved in nucleotide synthesis, leading to inhibition of DNA and RNA synthesis in rapidly dividing cells. Carboplatin is a platinum-based chemotherapeutic that causes DNA crosslinking and apoptosis in cancer cells. This combination leverages antiangiogenic therapy (fruquintinib), immunotherapy (sintilimab), and cytotoxic chemotherapy (pemetrexed plus carboplatin) for synergistic anti-tumor effects.

02

Targets

PDCD1 (Programmed cell death protein 1 receptor)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)GART (GAR transformylase)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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