Drug intelligence / Profile preview

nintedanib + rifampicin

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

Overview

The co-administration of nintedanib and rifampicin is primarily studied in the context of clinical drug-drug interaction (DDI) trials. Nintedanib is a small molecule multi-target tyrosine kinase inhibitor developed by Boehringer Ingelheim, primarily indicated for idiopathic pulmonary fibrosis (IPF), systemic sclerosis-associated interstitial lung disease (SSc-ILD), and certain non-small cell lung cancers. Rifampicin is a potent rifamycin antibiotic used for tuberculosis. The combination is clinically significant because rifampicin is a powerful inducer of P-glycoprotein (P-gp) and, to a lesser extent, CYP3A4. Since nintedanib is a substrate for P-gp, co-administration with rifampicin leads to a significant reduction in nintedanib's systemic exposure (AUC and Cmax), typically by approximately 50-60%, which can compromise its therapeutic efficacy. Consequently, the use of potent P-gp inducers is generally avoided during nintedanib therapy.

Brand names
Vargatef
Other names
nintedanib and rifampicin
02

Targets

FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)RNAP (Bacterial dna-dependent RNA polymerase)

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