Drug intelligence / Profile preview

1-methylnicotinamide

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

1-Methylnicotinamide is a small molecule metabolite of nicotinamide (vitamin B3) produced primarily in the liver via the action of nicotinamide N-methyltransferase. It was historically considered biologically inactive but has since been shown to possess anti-thrombotic, anti-inflammatory, vascular protective, and neuroprotective properties. Mechanistically, it acts as an endogenous activator of prostacyclin synthesis and enhances nitric oxide bioavailability by regulating endothelial nitric oxide synthase (eNOS), contributing to vasodilation and vascular health. It also inhibits platelet-dependent thrombosis through cyclooxygenase 2-mediated prostacyclin production. Its potential therapeutic indications include cardiovascular diseases, metabolic disorders, and inflammatory conditions[5][3][8]. Currently, it is under investigation as a hypolipidemic agent in clinical trials[1].

Brand names
TRIA-662TRIA662TRIA 662
Other names
N(1)-methylnicotinamide bromideN(1)-methylnicotinamide chlorideN(1)-methylnicotinamide cyanideN(1)-methylnicotinamide fluorideN(1)-methylnicotinamide iodidetrigonellamide chloride
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NOS3 (eNOS)SLC47A1 (Multidrug and toxin extrusion transporter 1)NNMT (Nicotinamide N-methyltransferase)OCT1 (Organic cation transporter 1)OCT2 (Organic cation transporter 2)

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