Drug intelligence / Profile preview

l-nmma + fluconazole

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous (for Experimental Use With L-nmma), Oral (fluconazole)
01

Overview

This is a combination of two agents: - **L-NMMA (N(G)-monomethyl-L-arginine)** is a non-selective inhibitor of nitric oxide synthase (NOS), used primarily in research to block the production of nitric oxide (NO) and study its physiological roles. By inhibiting NOS, L-NMMA reduces NO-mediated vasodilation and other NO-dependent processes. - **Fluconazole** is an antifungal agent belonging to the triazole class. It acts as a selective inhibitor of fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase, thereby blocking ergosterol synthesis and disrupting fungal cell membrane formation[2][6]. Fluconazole is widely used for treating systemic and superficial fungal infections. The combination has been studied experimentally to investigate vascular function in humans—specifically the interplay between endothelium-derived hyperpolarizing factor (EDHF) and nitric oxide in regulating arterial diameter. In such studies, L-NMMA inhibits NO production while fluconazole inhibits cytochrome epoxygenases involved in EDHF synthesis[1].

Other names
N(G)-monomethyl-L-arginineL-NMMANG-monomethyl-L-arginine2-(methylamino)-5-guanidinopentanoic acid
02

Targets

NOS1 (nNOS)CYP51A1 (Sterol 14α-demethylase)

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