Drug intelligence / Profile preview

ketoconazole + GW642444M

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Oral, Topical, Inhalation
01

Overview

Ketoconazole is an imidazole-class broad-spectrum antifungal agent that inhibits fungal growth by blocking 14-α-sterol demethylase, a cytochrome P450 enzyme essential for ergosterol synthesis in fungal cell membranes. It is used to treat various systemic and topical fungal infections when other antifungals are not suitable[1][4][7]. GW642444M is a code name for vilanterol, a long-acting beta2-adrenoceptor agonist (LABA) developed as an inhaled bronchodilator. In clinical research and therapy, it is often combined with fluticasone furoate (a corticosteroid) for the treatment of asthma and chronic obstructive pulmonary disease (COPD). The combination of ketoconazole with GW642444M has been studied primarily to assess drug-drug interactions because ketoconazole can inhibit CYP3A4-mediated metabolism of LABAs like vilanterol, potentially increasing their systemic exposure[5]. This entry refers to the co-administration or study of both drugs together rather than a fixed-dose pharmaceutical product.

Brand names
Nizoral
Other names
fluticasone furoate + GW642444M
02

Targets

ADRB2 (β2)CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)

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