Overview
Pioglitazone is an antihyperglycemic used as an adjunct to diet, exercise, and other antidiabetic medications to manage type 2 diabetes mellitus. It is administered as a racemic mixture, though there is no pharmacologic difference between the enantiomers and they appear to interconvert in vivo with little consequence. The thiazolidinedione class of medications, which also includes rosiglitazone and troglitazone, exerts its pharmacological effect primarily by promoting insulin sensitivity and the improved uptake of blood glucose via agonism at the peroxisome proliferator-activated receptor-gamma (PPARγ). PPARs are ligand-activated transcription factors that are involved in the expression of more than 100 genes and affect numerous metabolic processes, most notably lipid and glucose homeostasis. Thiazolidinediones, including pioglitazone, have fallen out of favor in recent years due to the presence of multiple adverse effects and warnings regarding their use (e.g. congestive heart failure, bladder cancer) and the availability of safer and more effective alternatives for patients with type 2 diabetes mellitus.
Indication
Pioglitazone is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is also available in combination with metformin, glimepiride, or alogliptin for the same indication.
Associated Conditions
- Diabetes
- Diabetic Neuropathies
- Type 2 Diabetes Mellitus
Research Report
Pioglitazone: A Comprehensive Pharmacological and Clinical Review
1. Introduction to Pioglitazone
1.1 Overview and Classification
Pioglitazone (DrugBank ID: DB01132) is an oral antihyperglycemic agent belonging to the thiazolidinedione (TZD) class of medications.[1] Commonly marketed under brand names such as Actos® and Glustin™ [1], it is classified as a small molecule drug [1] with the Chemical Abstracts Service (CAS) number 111025-46-8. Pioglitazone is administered clinically as a racemic mixture; however, studies suggest that the enantiomers interconvert in vivo and possess minimal pharmacologic differences.[4]
1.2 Historical Context and Indication
Developed by Takeda Pharmaceuticals [1] and patented in 1985 [3], pioglitazone received initial regulatory approval from the U.S. Food and Drug Administration (FDA) in 1999 [1] and the European Medicines Agency (EMA) in 2000.[6] Its approved indication is as an adjunct to diet and exercise for the improvement of glycemic control in adult patients with type 2 diabetes mellitus (T2DM).[1] Pioglitazone addresses a fundamental pathophysiological defect in T2DM: insulin resistance.[2] Within the TZD class, it followed troglitazone, which was withdrawn due to hepatotoxicity, and was marketed alongside rosiglitazone.[2]
1.3 Initial Promise and Evolving Perceptions
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/04/10 | Phase 4 | Not yet recruiting | |||
2025/02/28 | Phase 4 | Not yet recruiting | Fundación para la Investigación del Hospital Clínico de Valencia | ||
2024/12/12 | Phase 2 | Recruiting | |||
2024/10/24 | Phase 4 | Not yet recruiting | |||
2024/09/13 | Phase 2 | Not yet recruiting | Affiliated Cancer Hospital & Institute of Guangzhou Medical University | ||
2024/06/06 | Phase 1 | Recruiting | |||
2024/05/06 | Phase 4 | Recruiting | |||
2024/03/29 | Phase 2 | Recruiting | |||
2024/02/07 | Phase 3 | Recruiting | |||
2023/12/11 | Phase 4 | Completed | United States Army Research Institute of Environmental Medicine |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Rebel Distributors Corp. | 21695-148 | ORAL | 30 mg in 1 1 | 9/1/2009 | |
| Rising Health, LLC | 57237-220 | ORAL | 30 mg in 1 1 | 2/19/2022 | |
| Rising Pharma Holdings, Inc. | 57237-220 | ORAL | 30 mg in 1 1 | 2/19/2022 | |
| A-S Medication Solutions | 50090-6874 | ORAL | 30 mg in 1 1 | 9/8/2022 | |
| Padagis Israel Pharmaceuticals Ltd | 45802-499 | ORAL | 45 mg in 1 1 | 3/31/2022 | |
| Macleods Pharmaceuticals Limited | 33342-056 | ORAL | 45 mg in 1 1 | 12/26/2022 | |
| Bryant Ranch Prepack | 71335-1333 | ORAL | 30 mg in 1 1 | 8/14/2021 | |
| Takeda Pharmaceuticals America, Inc. | 64764-123 | ORAL | 30 mg in 1 1 | 12/4/2023 | |
| Takeda Pharmaceuticals America, Inc. | 64764-158 | ORAL | 15 mg in 1 1 | 12/5/2023 | |
| Aurobindo Pharma Limited | 65862-514 | ORAL | 45 mg in 1 1 | 2/15/2022 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 7/28/2006 | ||
Authorised | 1/8/2007 | ||
Authorised | 9/19/2013 | ||
Authorised | 3/21/2012 | ||
Authorised | 3/15/2012 | ||
Authorised | 10/13/2000 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| ACTOS TABLET 30 mg | SIN12442P | TABLET | 30 mg | 10/10/2003 | |
| DECULIN TABLET 30MG | SIN16882P | TABLET | 30 MG | 10/11/2023 | |
| ACTOS TABLET 15 mg | SIN12441P | TABLET | 15 mg | 10/10/2003 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Pioglitazone Hydrochloride Orally Disintegrating | 国药准字H20080303 | 化学药品 | 片剂 | 11/8/2022 | |
| Pioglitazone Hydrochloride Orally Disintegrating | 国药准字H20051549 | 化学药品 | 片剂 | 6/23/2020 | |
| Pioglitazone Hydrochloride Capsules | 国药准字H20050030 | 化学药品 | 胶囊剂 | 2/11/2020 | |
| Pioglitazone Hydrochloride Capsules | 国药准字H20050838 | 化学药品 | 胶囊剂 | 6/19/2020 | |
| Pioglitazone Hydrochloride Capsules | 国药准字H20060621 | 化学药品 | 胶囊剂 | 11/18/2020 | |
| Pioglitazone Hydrochloride Capsules | 国药准字H20050136 | 化学药品 | 胶囊剂 | 5/15/2020 | |
| Pioglitazone Hydrochloride Capsules | 国药准字H20050137 | 化学药品 | 胶囊剂 | 5/15/2020 | |
| Pioglitazone Hydrochloride Dispersible Tablets | 国药准字H20060178 | 化学药品 | 片剂 | 8/13/2020 | |
| Pioglitazone Hydrochloride Dispersible Tablets | 国药准字H20050405 | 化学药品 | 片剂 | 6/19/2020 | |
| Pioglitazone Hydrochloride Dispersible Tablets | 国药准字H20080703 | 化学药品 | 片剂（分散片） | 2/27/2023 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
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