Drug intelligence / Profile preview

rosiglitazone + glimepiride

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

Overview

**Rosiglitazone + glimepiride** is an oral fixed-dose antidiabetic combination containing rosiglitazone, a thiazolidinedione insulin sensitizer, and glimepiride, a sulfonylurea insulin secretagogue. Rosiglitazone activates peroxisome proliferator-activated receptor gamma to improve insulin sensitivity in adipose tissue, skeletal muscle, and liver, while glimepiride stimulates pancreatic beta-cell insulin release through inhibition of ATP-sensitive potassium channels. The combination was developed by GSK for glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet and exercise and was marketed as Avandaryl in the United States and Avaglim in Europe. It carries clinically important risks associated with its components, including hypoglycemia from glimepiride and fluid retention and heart-failure risk from rosiglitazone. ([accessdata.fda.gov](https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021700s008lbl.pdf))

Brand names
Avaglim
Other names
glimepiride + rosiglitazoneglimepiride/rosiglitazonerosiglitazone + glimepiriderosiglitazone maleate + glimepiriderosiglitazone/glimepiride
02

Targets

SUR1 (Sulfonylurea receptor 1)PPARG (Peroxisome proliferator-activated receptor gamma)

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