Rosiglitazone: profile and news

HEALTH BRIEFS 16 May 2006
...maker GlaxoSmithKline poised to open three Phase III clinical trials this summer to test whether the diabetes drug, also called rosiglitazone, might protect ... - Kalamazoo Gazette,

Pioglitazone Has Cholesterol Advantages Versus Rosiglitazone in ... May 2, 2006
CHICAGO, IL -- May 2, 2006 -- A new study shows that pioglitazone and rosiglitazone exert significantly different effects on lipid metabolism and potential ... - DG News

Drug May Reduce Risk of Diabetic Retinopathy: Presented at ARVO May 3, 2006
FT. LAUDERDALE, FL -- May 3, 2006 -- The insulin sensitizer rosiglitazone (Avandia) could offer some degree of protection for patients with diabetes who are at ... - DG News

Higher Risk Patients Benefit More After Conversion from ... May 3, 2006
CHICAGO, IL -- May 3, 2006 -- A new study shows that conversion from rosiglitazone to pioglitazone while maintaining statin therapy, improves the lipid ... - DG News

Health Highlights: May 2, 2006 May 2, 2006
Avandia (rosiglitazone) treats Type II diabetes by resensitizing the body to insulin. The Phase III studies will be conducted by Avandia maker GlaxoSmithKline. ... - Forbes

Diabetes drug set for Alzheimer's test May 3, 2006
...maker GlaxoSmithKline, poised to open three Phase III clinical trials this summer to test whether the diabetes drug, also called rosiglitazone, might protect ... - Economic Times,

Looking for Alzheimer's link May 4, 2006
Avandia (rosiglitazone) treats Type II diabetes by resensitising the body to insulin. The Phase III studies will be conducted by Avandia maker GlaxoSmithKline. ... - Health24.com,

Diabetes drug may help fight Alzheimer's May 7, 2006
Scientists at GlaxoSmithKline are testing the company's diabetes drug, Avandia, or rosiglitazone, for the treatment of Alzheimer's. ... - Indianapolis Star,

AXE THREAT PLANT WINS 100 JOBS May 12, 2006
Now Glaxo will recruit specialists from agencies over the next few months to help the plant's workers make rosiglitazone and carvedilol to cope with a sudden ... - Glasgow Daily Record,

Fresh from the Pipeline: Inhaled human insulin May 4, 2006
2 diabetes not optimally controlled with diet and exercise compared inhaled insulin before meals with the oral hypoglycaemic drug rosiglitazone twice daily 6 ... - Nature.com (subscription),

Diabetes link to Alzheimer’s under probe May 1, 2006
...this summer. to test whether the diabetes drug, also called rosiglitazone, might protect certain patients’ brains. Diabetes has ... - Pueblo Chieftain,

Latest Issue Of Alzheimer's & Dementia Explores New Ideas For ... Apr 23, 2006
The new hypothesis is supported by the results of 24-week randomized clinical trial of an unmarketed formulation of rosiglitazone maleate (Avandia ... - Medical News Today (press release),

Theory links diabetes to Alzheimer's May 2, 2006
...have Avandia maker GlaxoSmithKline poised to open three clinical trials to test whether the diabetes drug, also called rosiglitazone, protects certain patients ... - AZ Central.com,

ERRATUM: Higher Risk Patients Benefit More After Conversion from ... May 5, 2006
There was an error in the title of our DG Dispatch (May 4, 2006) based on a presentation at the American Association of Clinical Endocrinologists (AACE) annual ... - DG News

EASL CONGRESS VIENNA - BATTLE AGAINST VIRUSES AND FATTY May 1, 2006
...a placebo-controlled study it has been possible to prove that fatty liver hepatitis is ameliorated after a year's treatment with the diabetes drug rosiglitazone ... - ITNews,

Avandia May Help Alzheimer's Patients May 3, 2006
Avandia-maker GlaxoSmithKline poised to open three clinical trials in the summer to test whether the diabetes drug, also called rosiglitazone, might protect ... - DiabeticNews.com,

Women Gain More Weight Than Men When Taking Thiazolidinedione ... May 3, 2006
...the charts of 100 outpatients in an endocrinology practice who had received or were receiving the thiazolidinediones pioglitazone or rosiglitazone as either ... - DG News

Committee for Medicinal Products for Human Use Summary of Positive ... Apr 28, 2006
The active substances of Avaglim are rosiglitazone (as maleate) and glimepiride, a combination of oral blood glucose lowering drugs medicinal product, which ... - PharmaLive.com (press release),

Newer Diabetic Meds Cost More, But Users Have Fewer Hospital ... Apr 28, 2006
TZDs (pioglitazone and rosiglitazone, brand names Actos and Avandia, respectively), were approved by the Food and Drug Administration in the late 1990s. ... - eMaxHealth.com,

Zydus Cadila files IND application for NME - ZYH2 Apr 24, 2006
In recent times, glitazones (rosiglitazone and pioglitazone) have been launched to treat increasing prevalence of insulin resistance in Type - II diabetes. ... - Express Pharma,

Other information

Indication
For the treatment of Type II diabetes mellitus

Pharmacology
Rosiglitazone, a member of the drug group known as the thiazolidinediones or "insulin sensitizers", is not chemically or functionally related to the alpha-glucosidase inhibitors, the biguanides, or the sulfonylureas. Rosiglitazone targets insulin resistance and, hence, is used alone or with metformine or sulfonylurea to improve glycemic control in patients with type 2 diabetes mellitus.

Mechanism Of Action
Rosiglitazone acts as an agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, rosiglitazone enhances tissue sensitivity to insulin.

Drug Category
Vasodilator Agents; Hypoglycemic Agents; Fibrinolytic Agents; Thazolidinediones; ATC:A10BG02

Brand Names/Synonyms
Avandia; Rosigliazone Maleate; Rosiglitazone; Rosiglitazone Maleate; Rosiglitazone and Its Intermediates; Rosiglizole

Dosage Forms
Tablets

Absorption
The absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, AVANDIA may be administered with or without food.

Interactions
Interactions for Rosiglitazone:

An inhibitor of CYP2C8 (such as gemfibrozil) may increase the AUC of rosiglitazone and an inducer of CYP2C8 (such as rifampin) may decrease the AUC of rosiglitazone. Therefore, if an inhibitor or an inducer of CYP2C8 is started or stopped during treatment with rosiglitazone, changes in diabetes treatment may be needed based upon clinical response.

Chemical IUPAC Name
5-[[4-[2-(methyl-pyridin-2-yl-amino)ethoxy]phenyl]methyl]thiazolidine-2,4-dione

Chemical Formula
C18H19N3O3S

Half Life
3-4 hours

Drug Type
Approved Drug

# Accession No
APRD00403

CAS Registry Number
122320-73-4