Drug intelligence / Profile preview

metformin + nizatidine

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Metformin + nizatidine is a combination of two small molecule drugs, metformin and nizatidine, administered together. Metformin is an oral antihyperglycemic agent primarily used to manage type 2 diabetes mellitus by decreasing hepatic glucose production, reducing intestinal absorption of glucose, and increasing insulin sensitivity through activation of AMP-activated protein kinase (AMPK) and inhibition of mitochondrial complex I. Nizatidine is a histamine H2 receptor antagonist typically used for gastric acid-related disorders but also acts as a selective inhibitor of the renal transporter MATE2K (multidrug and toxin extrusion protein 2-K). When co-administered, nizatidine selectively inhibits MATE2K-mediated transport in the kidney, which can increase the apparent volume of distribution, half-life, and hypoglycemic activity of metformin without significantly affecting its renal clearance or systemic concentrations. This combination has been studied for potential drug-drug interactions but does not represent an approved fixed-dose pharmaceutical product[1][2].

02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)HRH2 (Histamine H2 Receptor)ND1 (Mitochondrial electron transport chain complex I)MATE2-K (Multidrug and toxin extrusion protein 2)

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