Drug intelligence / Profile preview

erdafitinib + fluconazole

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of erdafitinib, a selective oral inhibitor of fibroblast growth factor receptor kinases (FGFR1-4), and fluconazole, a moderate inhibitor of cytochrome P450 2C9 (CYP2C9) and 3A4 (CYP3A4)**. Erdafitinib is used in oncology, primarily for the treatment of advanced urothelial carcinoma with susceptible FGFR2 or FGFR3 alterations. Fluconazole is an antifungal agent but here acts pharmacologically as a CYP enzyme inhibitor, which increases exposure (plasma concentrations) of erdafitinib by inhibiting its main metabolic pathways. Coadministration results in higher erdafitinib exposure and may require dose adjustments to manage increased risk of adverse effects[1][3][6]. No combination product under this name is currently marketed; this is a drug-drug interaction scenario for clinical management and research purposes.

02

Targets

FGFR4 (Fibroblast growth factor receptor 4)VEGFR4 (Vascular endothelial growth factor Receptor-3)VEGFR2 (Vascular endothelial growth factor receptor 2)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)PDGFRA (Platelet-derived growth factor receptor alpha)CYP3A4 (Cytochrome P450 3A4)FGFR3 (Fibroblast growth factor receptor 3)CSF1R (Macrophage colony-stimulating factor receptor)FGFR2 (Keratinocyte growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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