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Pioglitazone, Rosiglitazone

Korea University Anam Hospital · FDA-approved active Small molecule

Pioglitazone and rosiglitazone are thiazolidinediones that activate peroxisome proliferator-activated receptor gamma (PPAR-γ) to improve insulin sensitivity and reduce blood glucose in type 2 diabetes.

Pioglitazone and rosiglitazone are thiazolidinediones that activate peroxisome proliferator-activated receptor gamma (PPAR-γ) to improve insulin sensitivity and reduce blood glucose in type 2 diabetes. Used for Type 2 diabetes mellitus.

At a glance

Generic namePioglitazone, Rosiglitazone
SponsorKorea University Anam Hospital
Drug classThiazolidinedione (PPAR-γ agonist)
TargetPPAR-γ (Peroxisome proliferator-activated receptor gamma)
ModalitySmall molecule
Therapeutic areaDiabetes
PhaseFDA-approved

Mechanism of action

These drugs bind to PPAR-γ, a nuclear receptor involved in glucose and lipid metabolism, enhancing insulin sensitivity in muscle, adipose tissue, and liver. By reducing insulin resistance, they lower fasting and postprandial glucose levels without directly stimulating insulin secretion. This mechanism makes them effective for glycemic control in type 2 diabetes, though they carry metabolic side effects including weight gain and fluid retention.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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