Drug intelligence / Profile preview

dapagliflozin + metformin

Development stage
Approved
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Dapagliflozin + metformin is an oral fixed-dose antidiabetic combination used for type 2 diabetes mellitus that pairs **dapagliflozin**, a selective sodium-glucose cotransporter 2 inhibitor that lowers plasma glucose by reducing renal glucose reabsorption and increasing urinary glucose excretion, with **metformin**, a biguanide that decreases hepatic glucose production and improves insulin sensitivity primarily through effects linked to AMP-activated protein kinase signaling and mitochondrial complex I inhibition. The combination has been developed and commercialized by AstraZeneca as an immediate-release and extended-release tablet formulation, including the once-daily extended-release product Xigduo XR. Across randomized trials, postmarketing studies, and multiple bioequivalence programs, the combination has shown improved HbA1c, fasting plasma glucose, body-weight reduction, and low intrinsic hypoglycemia risk relative to some comparator regimens, with known class-related adverse effects including genital and urinary tract infections from dapagliflozin and gastrointestinal intolerance and rare lactic acidosis risk from metformin.

Brand names
Xigduo XRXigduoEbymect
Other names
dapagliflozin + metformin XRdapagliflozin + metformin extended releasedapagliflozin + metformin modified releasedapagliflozin-metformin XRdapagliflozin + metformin ER
02

Targets

ND1 (Mitochondrial electron transport chain complex I)SGLT2 (Sodium-glucose cotransporter protein subunit 2)SLC5A1 (Sodium Glucose Cotransporter 1)

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