Is N1-Methylnicotinamide a Good Organic Cation Transporter 2 (OCT2) Biomarker?

ABSTRACT: Background/Objectives: The impact of potential precipitant drugs on plasma or urinary exposure of endogenous biomarkers is emerging as an alternative approach to evaluating drug-drug interaction (DDI) liability. N1-Methylnicotinamide (NMN) has been proposed as a potential biomarker for renal organic cation transporter 2 (OCT2). NMN is synthesized in the liver from nicotinamide by nicotinamide N-methyltransferase (NNMT) and is subsequently metabolized by aldehyde oxidase (AO). Multiple clinical studies have shown a reduction in NMN plasma concentration following the administration of OCT inhibitors such as cimetidine, trimethoprim, and pyrimethamine, which contrasts with their inhibition of NMN renal clearance by OCT2. We hypothesized that OCT1-mediated NMN release from hepato

SUBMITTER: Ailabouni AS 

PROVIDER: S-EPMC11857448 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature