selumetinib + fluconazole

This combination refers to concomitant administration of **selumetinib**, a small molecule, oral, selective inhibitor of mitogen-activated protein kinase kinase (MEK1/2), and **fluconazole**, an oral or intravenous antifungal triazole agent. Selumetinib blocks MEK1/2 activity in the MAPK/ERK pathway, inhibiting cell proliferation in tumors, and is approved for pediatric patients with neurofibromatosis type 1 with symptomatic, inoperable plexiform neurofibromas. Fluconazole inhibits fungal cytochrome P450-dependent enzyme lanosterol 14-α-demethylase, disrupting fungal cell membrane synthesis, and is widely used for fungal infections. Importantly, fluconazole is a moderate CYP3A4 and strong CYP2C19 inhibitor; co-administration with selumetinib increases selumetinib plasma concentrations and the risk of side effects, so dose adjustment of selumetinib is required in the presence of fluconazole.

Brand names

Koselugo (selumetinib)Diflucan (fluconazole)

Other names

selumetinib + fluconazole