Troglitazone

Troglitazone
Systematic (IUPAC) name
5-(4-((6-hydroxy-2,5,7,8- tetramethylchroman-2-yl-methoxy) benzyl)-2,4-thiazolidinedione)
Identifiers
CAS number	97322-87-7
ATC code	A10BG01
PubChem	5591
DrugBank	APRD00488
Chemical data
Formula	C24H27NO5S
Mol. mass	441.541 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	16-34 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

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Troglitazone (Rezulin®, Resulin® or Romozin®) is a member of the drug class of the thiazolidinediones. It was introduced in the late 1990s but turned out to be associated with an idiosyncratic reaction leading to drug-induced hepatitis. It was withdrawn from the USA market on 21 March 2000, and from other markets soon afterwards.

Troglitazone, like the other thiazolidinediones (pioglitazone and rosiglitazone), works by activating PPARs (peroxisome proliferator-activated receptors). Troglitazone is a ligand to both PPARα and - more strongly - PPARγ. Troglitazone also contains an α-tocopheroyl moiety, potentially giving it vitamin E-like activity in addition to its PPAR activation. It has been shown (Aljada et al) to reduce inflammation: troglitazone use was associated with a decrease of nuclear factor kappa-B (NFκB) and a concomitant increase in its inhibitor (IκB). NFκB is an important cellular transcription regulator for the immune response.

References

• Aljada A., Garg R., Ghanim H., Mohanty P., Hamouda W., Assian E., Dandona P.: Nuclear factor-κB suppressive and inhibitor-κB stimulatory effects of troglitazone in obese patients with type 2 diabetes: evidence of an antiinflammatory action? J. Clin. Endocrinol. Metab. 2001, 86, 3250-6. Fulltext. PMID 11443197.

See also

• Thiazolidinedione
• PPAR

External links

• Diabetes Monitor article on troglitazone
• RxList article on troglitazone
• FDA Recall FDA Recall Announcement