Drug intelligence / Profile preview

F901318 + fluconazole

Development stage
Unknown
Lead developer
F2G
Modality
Small Molecules
Administration
Oral
01

Overview

F901318 + fluconazole is a combination of two antifungal agents under investigation for the treatment and prophylaxis of invasive fungal infections, particularly those caused by resistant or difficult-to-treat fungi. - **F901318** (also known as olorofim) is a novel small molecule antifungal from the orotomide class that inhibits dihydroorotate dehydrogenase, an enzyme essential for fungal pyrimidine biosynthesis. It has shown activity against molds such as Aspergillus spp., Scedosporium spp., and Lomentospora prolificans, including strains resistant to other antifungals. - **Fluconazole** is a well-established triazole antifungal that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase, disrupting ergosterol synthesis in the cell membrane. It is widely used for candidiasis and cryptococcal infections[4][6][9]. The combination aims to broaden spectrum and address resistance by targeting different pathways in fungal cells. Clinical studies have evaluated safety, pharmacokinetics, and potential drug-drug interactions between these agents[1][2][3][7].

Brand names
Diflucan
Other names
olorofim + fluconazole
02

Targets

CYP51A1 (Sterol 14α-demethylase)DHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)

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