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nintedanib + pemetrexed
- Development stage
- Phase 1
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Nintedanib + pemetrexed is a combination therapy used primarily in the treatment of advanced non-small cell lung cancer (NSCLC) and has been investigated for malignant pleural mesothelioma (MPM). Nintedanib is an oral small-molecule tyrosine kinase inhibitor that targets multiple angiogenesis-related receptors including vascular endothelial growth factor receptors (VEGFR 1–3), platelet-derived growth factor receptors (PDGFR α/β), and fibroblast growth factor receptors (FGFR 1–3), as well as Src family kinases. By inhibiting these pathways, nintedanib disrupts tumor angiogenesis and proliferation. Pemetrexed is an antifolate chemotherapy agent that inhibits several folate-dependent enzymes involved in nucleotide synthesis, thereby preventing DNA replication in rapidly dividing cells. The combination aims to enhance anti-tumor efficacy by simultaneously targeting tumor vasculature and cell division pathways[3][5][8].
- Brand names
- Vargatef
- Other names
- BIBF 1120 + pemetrexednintedanib + pemetrexed
02
Targets
ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)FLT3 (Fms related receptor tyrosine kinase 3)GART (GAR transformylase)LCK (Proto-oncogene tyrosine-protein kinase Lck)LYN (LYN proto-oncogene, Src family tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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