Drug intelligence / Profile preview

vemurafenib + itraconazole

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

**Vemurafenib + itraconazole** refers to the combination of two individual pharmaceutical agents: **vemurafenib**, a small-molecule BRAF kinase inhibitor used for the treatment of BRAF V600 mutation-positive cancers such as metastatic melanoma, and **itraconazole**, a broad-spectrum triazole antifungal agent that acts primarily by inhibiting fungal 14α-demethylase. The combination is not an approved fixed-dose product but refers to concomitant administration of the two drugs, mainly explored due to their drug-drug interaction: itraconazole is a potent CYP3A4 inhibitor and can increase the plasma levels of vemurafenib by approximately 40% at steady-state exposure, as shown in a phase 1 clinical pharmacokinetic study[1][2][4].

02

Targets

BRAF V600ECYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)

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