Drug intelligence / Profile preview

exenatide + rosiglitazone

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Peptides, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

A combination of **exenatide** and **rosiglitazone** used experimentally in the management of type 2 diabetes mellitus, designed to target multiple aspects of diabetic pathophysiology. **Exenatide** is a glucagon-like peptide-1 (GLP-1) receptor agonist that enhances glucose-dependent insulin secretion and suppresses inappropriate glucagon secretion, thereby improving glycemic control and contributing to weight loss[1][2][3][4]. **Rosiglitazone** is a thiazolidinedione (TZD) that primarily improves insulin sensitivity by acting as a peroxisome proliferator-activated receptor gamma (PPARγ) agonist. When used together, this combination provides additive glycemic benefit, improving both insulin sensitivity and β-cell function, while offsetting the weight gain usually associated with rosiglitazone alone[1]. This combination is not marketed as a fixed-dose product and has only been studied in clinical trials.

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)GLP1R (GLP-1R)

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