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selumetinib + fluconazole
- Development stage
- Phase 1
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral, Intravenous (fluconazole Only)
01
Overview
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
02
Targets
CYP51A1 (Sterol 14α-demethylase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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