Drug intelligence / Profile preview

alpha lipoic acid + metformin + rosiglitazone

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three agents—alpha lipoic acid, metformin, and rosiglitazone—used primarily in the management of type 2 diabetes mellitus and related metabolic disorders. - **Alpha lipoic acid** is an antioxidant that may help reduce oxidative stress and improve insulin sensitivity. It has been studied for its potential to alleviate diabetic neuropathy and other complications but does not directly lower blood glucose levels[8][3]. - **Metformin** is a biguanide antidiabetic agent that decreases hepatic glucose production, reduces intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral uptake and utilization of glucose[5][4]. - **Rosiglitazone** is a thiazolidinedione (TZD) class drug that acts as an agonist at peroxisome proliferator-activated receptor gamma (PPARγ), enhancing tissue sensitivity to insulin[6]. The rationale for combining these agents lies in their complementary mechanisms targeting different aspects of type 2 diabetes pathophysiology—insulin resistance, oxidative stress, and impaired β-cell function. While combinations such as metformin plus rosiglitazone are approved (e.g., Avandamet), the triple combination with alpha lipoic acid is less common but has been explored in clinical research settings for additive or synergistic effects on glycemic control and metabolic parameters[1][2].

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)RXRA (Retinoid X receptor alpha)PPARA (Peroxisome proliferator-activated receptor alpha)ND1 (Mitochondrial electron transport chain complex I)

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