Drug intelligence / Profile preview

erdafitinib + itraconazole

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

Overview

**Erdafitinib + itraconazole** is a combination of **erdafitinib**, a selective pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, and **itraconazole**, a triazole antifungal agent and strong CYP3A4/P-glycoprotein inhibitor. Erdafitinib is indicated for locally advanced or metastatic urothelial carcinoma with FGFR2/FGFR3 mutations, while itraconazole is primarily used for various systemic fungal infections. When administered together, itraconazole increases the plasma exposure (AUC) of erdafitinib by inhibiting its metabolism through CYP3A4, necessitating dose adjustments due to the risk of increased adverse effects. This combination is not an approved combination product, but represents a clinically relevant drug-drug interaction scenario for pharmacokinetic management in oncology and infectious disease settings[1][2][5][4].

02

Targets

FGFR4 (Fibroblast growth factor receptor 4)PDGFRB (Platelet-derived growth factor receptor beta)ABCB1 (P-glycoprotein)VEGFR4 (Vascular endothelial growth factor Receptor-3)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)CYP3A4 (Cytochrome P450 3A4)FGFR3 (Fibroblast growth factor receptor 3)ORM1 (Alpha-1-acid glycoprotein 1)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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