Drug intelligence / Profile preview

cisplatin + pemetrexed + sunitinib

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three drugs: - **Cisplatin** is a platinum-based chemotherapy agent that forms DNA crosslinks, leading to apoptosis in rapidly dividing cells. - **Pemetrexed** is an antifolate antineoplastic agent that inhibits multiple folate-dependent enzymes involved in the synthesis of thymidine and purine nucleotides, thereby disrupting DNA and RNA synthesis essential for cell replication[4][5]. - **Sunitinib** is an oral small molecule multi-targeted tyrosine kinase inhibitor (TKI) that blocks several receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), KIT, FLT3, RET, and CSF1R. This inhibition disrupts tumor angiogenesis and cell proliferation[6][8][10]. This specific triple combination does not have a unique brand or code name; it represents the concurrent use of these three agents. While cisplatin plus pemetrexed is approved for non-squamous non-small cell lung cancer (NSCLC) and mesothelioma[1][5], sunitinib is approved as monotherapy for renal cell carcinoma, gastrointestinal stromal tumors (GIST), and pancreatic neuroendocrine tumors[6][8][10]. The triple combination may be explored in clinical trials or investigational settings but does not represent an established standard-of-care regimen.

02

Targets

GART (GAR transformylase)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)DHFR (Dihydrofolate reductase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)MAP4K1 (Hematopoietic progenitor kinase 1)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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