Drug intelligence / Profile preview

metformin + rabeprazole

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

Overview

Metformin + rabeprazole is a non-branded combination of two small molecule drugs, metformin and rabeprazole, used concomitantly rather than as a fixed-dose combination. Metformin is an oral biguanide antihyperglycemic agent primarily indicated for glycemic control in type 2 diabetes mellitus. It works by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. Rabeprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by inhibiting the H+/K+ ATPase enzyme system at the secretory surface of gastric parietal cells; it is indicated for conditions such as gastroesophageal reflux disease (GERD), duodenal ulcers, and other acid-related disorders. When co-administered, rabeprazole can modestly increase plasma concentrations of metformin due to inhibition of renal transporters involved in metformin elimination (notably OCT2 and MATE1). However, clinical studies indicate that this pharmacokinetic interaction does not significantly alter the glucose-lowering efficacy of metformin[1][5]. The combination may be prescribed when both glycemic control (metformin) and acid suppression (rabeprazole) are needed in patients with comorbidities such as type 2 diabetes mellitus with gastritis or peptic ulcer disease[5].

02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)OCT2 (Organic cation transporter 2)OCT3 (Organic cation transporter 3)OCTN1 (Solute carrier family 22 member 4)ND1 (Mitochondrial electron transport chain complex I)OCT1 (Organic cation transporter 1)ATP4A (Potassium–transporting ATPase alpha chain 1)

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