Drug intelligence / Profile preview

nintedanib + ketoconazole

Development stage
Phase 1
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**Nintedanib + ketoconazole** is a combination of nintedanib, a small molecule tyrosine kinase inhibitor (Ofev), and ketoconazole, an imidazole antifungal agent (Nizoral). Nintedanib targets receptor tyrosine kinases involved in angiogenesis—platelet-derived growth factor receptors (PDGFR), vascular endothelial growth factor receptors (VEGFR), and fibroblast growth factor receptors (FGFR)—and is primarily indicated for idiopathic pulmonary fibrosis and other fibrotic conditions. Ketoconazole, a potent P-glycoprotein (P-gp) and CYP3A4 inhibitor, is added in experimental settings to assess drug-drug interactions, affecting the bioavailability and serum concentration of nintedanib. Co-administration increases nintedanib exposure by inhibiting its P-gp-mediated efflux and CYP3A4 metabolism[1][2][3][4][5].

Other names
nintedanibketoconazole
02

Targets

FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FLT3 (Fms related receptor tyrosine kinase 3)CYP51A1 (Sterol 14α-demethylase)LCK (Proto-oncogene tyrosine-protein kinase Lck)ABCB1 (P-glycoprotein)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)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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