Drug intelligence / Profile preview

dolutegravir + metformin

Development stage
Phase 1
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

Dolutegravir + metformin is a **combination of two oral small molecule drugs**: dolutegravir, an antiretroviral integrase strand transfer inhibitor (INSTI) primarily used for HIV-1 infection, and metformin, a biguanide antihyperglycemic agent used as first-line therapy for type 2 diabetes mellitus. When co-administered, dolutegravir inhibits the organic cation transporter 2 (OCT2), which results in significantly increased plasma exposure of metformin by reducing its renal clearance. This interaction can lead to higher risk of metformin-associated adverse events such as lactic acidosis, especially in patients with comorbidities or renal impairment. Dose adjustment of metformin is recommended to maintain optimal glycemic control and reduce toxicity when used alongside dolutegravir[1][2][3][5]. The combination is not marketed as a fixed-dose product but is often used concomitantly in clinical settings, especially for HIV-infected patients with diabetes. The combination has been shown to be generally well tolerated in healthy adults, but careful clinical monitoring is advised due to pharmacokinetic interactions and rare but serious potential side effects[1][3][2].

Brand names
dolutegravir + metformin
Other names
dolutegravir plus metforminDTG + metformin
02

Targets

Integrase allosteric pocket (HIV)SLC47A1 (Multidrug and toxin extrusion transporter 1)OCT2 (Organic cation transporter 2)

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