selumetinib + itraconazole

Selumetinib + itraconazole is a combination of two pharmaceutical agents: selumetinib, a selective small molecule inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), and itraconazole, a triazole antifungal that is a potent inhibitor of cytochrome P450 3A4 (CYP3A4). Selumetinib is primarily used for the treatment of neurofibromatosis type 1 (NF1)-related plexiform neurofibromas and other malignancies due to its targeted action against the MAPK/ERK pathway. Itraconazole is used in fungal infections and, in this context, acts as a pharmacokinetic booster for selumetinib by inhibiting CYP3A4-mediated metabolism, thereby increasing selumetinib plasma concentrations by approximately 49% in area under the curve (AUC) and 19% in maximum plasma concentration (Cmax). The combination is not marketed as a fixed formulation but may occur clinically due to co-administration. When used together, dosage adjustments of selumetinib are recommended to account for the increased systemic exposure, and their interaction highlights the significance of CYP3A4 inhibition in drug metabolism[1][2][3].

Other names

selumetinibAZD6244AZD-6244AZD 6244itraconazoleSporanox