Actos

Pioglitazone

Clinical data
Trade names	Actos
AHFS/Drugs.com	Monograph
MedlinePlus	a699016
License data	EU EMA: Glustin US FDA: Actos
Pregnancy category	C
Routes of administration	Oral
ATC code	A10BG03 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Protein binding	>99%
Metabolism	liver (CYP2C8)
Biological half-life	3–7 hours
Excretion	in bile
Identifiers
IUPAC name (RS)-5-(4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl)thiazolidine-2,4-dione
CAS Number	111025-46-8 Y
PubChem CID	4829
IUPHAR/BPS	2694
DrugBank	DB01132 Y
ChemSpider	4663 Y
UNII	X4OV71U42S
KEGG	D08378 Y
ChEBI	CHEBI:8228 Y
ChEMBL	CHEMBL595 Y
ECHA InfoCard	100.114.441
Chemical and physical data
Formula	C19H20N2O3S
Molar mass	356.44 g/mol
3D model (Jmol)	Interactive image
Chirality	Racemic mixture
SMILES O=C1NC(=O)SC1Cc3ccc(OCCc2ncc(cc2)CC)cc3
InChI InChI=1S/C19H20N2O3S/c1-2-13-3-6-15(20-12-13)9-10-24-16-7-4-14(5-8-16)11-17-18(22)21-19(23)25-17/h3-8,12,17H,2,9-11H2,1H3,(H,21,22,23) Y Key:HYAFETHFCAUJAY-UHFFFAOYSA-N Y

Pioglitazone (brand name Actos) is a prescription drug of the thiazolidinedione (TZD) class with hypoglycemic (antihyperglycemic, antidiabetic) action to treat diabetes. While pioglitazone does decrease blood sugar levels, studies on the main cardiovascular outcomes have not yielded statistically significant results.

Its cardiovascular safety profile compares favorably with that of rosiglitazone, which was withdrawn from some markets after concerns about an increased risk of cardiac events. Pioglitazone has been found to be associated with bladder tumors. It has been withdrawn in some countries.

Actos was the tenth-best selling drug in the U.S. in 2008, with sales exceeding $2.4 billion.

Pioglitazone is used to lower blood glucose levels in the treatment of diabetes mellitus type 2 (T2DM) either alone or in combination with a sulfonylurea, metformin, or insulin. The main study that looked at the medication, however, found no statistically significant difference in the main cardiovascular outcomes that were looked at. The secondary outcome of death from all causes, myocardial infarction, and stroke were lower.

Pioglitazone has also been used to treat non-alcoholic steatohepatitis (fatty liver), but this use is presently considered experimental.

Pioglitazone cannot be used in patients with a known hypersensitivity to pioglitazone, other thiazolidinediones or any of components of its pharmaceutical forms. It is ineffective and possibly harmful in diabetes mellitus type 1 and diabetic ketoacidosis. Its safety in pregnancy, lactation (breastfeeding) and people under 18 is not established.

Given previous experiences with the related drug troglitazone, acute diseases of the liver are regarded as a contraindication for pioglitazone.