Drug intelligence / Profile preview

muraglitazar + glyburide

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Muraglitazar + glyburide is an oral combination therapy studied for the treatment of type 2 diabetes, particularly in patients not adequately controlled with sulfonylurea monotherapy. Muraglitazar is a small molecule dual peroxisome proliferator-activated receptor (PPAR) agonist that targets both the alpha (PPAR-α) and gamma (PPAR-γ) subtypes, leading to improvements in glycemic control and favorable effects on lipid profiles. Glyburide is a sulfonylurea that stimulates insulin secretion from pancreatic β-cells. Clinical trials demonstrated that the combination leads to a significant reduction in HbA1c and triglycerides compared to glyburide alone. However, use of muraglitazar, especially in combination therapy, has been associated with higher rates of congestive heart failure, cardiovascular events, weight gain, and edema. Development of muraglitazar was discontinued after phase 3 due to safety signals indicating increased cardiovascular risk[1][2][3][4][5][6].

02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)KATP channel (ATP-sensitive potassium channel)

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