Drug intelligence / Profile preview

nintedanib + pemetrexed

Development stage
Unknown
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

VEGFR2 (Vascular endothelial growth factor receptor 2)LCK (Proto-oncogene tyrosine-protein kinase Lck)TS (Thymidylate synthase)LYN (LYN proto-oncogene, Src family tyrosine kinase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)FGFR4 (Fibroblast growth factor receptor 4)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)GART (GAR transformylase)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)FGFR1 (Fibroblast growth factor receptor 1)

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