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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Bortolini, Michele Wright, Matthew B. Bopst, Martin Balas, Bogdana |
| Description | Country affiliation: Switzerland Author Affiliation: Bortolini M ( Cardiometabolic Franchise Safety Science Leader, F. Hoffmann-La Roche, Ltd, PDS-Safety Risk Management, 663/2028, CH4070 Basel, Switzerland. michele.bortolini@roche.com) |
| Abstract | INTRODUCTION: The peroxisome proliferator-activated receptor (PPAR)- and -γ agonists, fibrates and glitazones, are effective treatments for dyslipidemia and type 2 diabetes mellitus, respectively, but exhibit class-related, as well as compound-specific safety characteristics. AREAS COVERED: This article reviews the profiles of PPAR- , PPAR-γ, and dual PPAR- /γ agonists with regard to class-related and compound-specific efficacy and adverse effects. We explore how learnings from first-generation drugs are being applied to develop safer PPAR-targeted therapies. EXPERT OPINION: The finding that rosiglitazone may increase risk for cardiovascular events has led to regulatory guidelines requiring demonstration of cardiovascular safety in appropriate outcome trials for new type 2 diabetes mellitus drugs. The emerging data on the possibly increased risk of bladder cancer with pioglitazone may prompt the need for post-approval safety studies for new drugs. Since PPAR- and -γ affect key cardiometabolic risk factors (diabetic dyslipidemia, insulin resistance, hyperglycemia, and inflammation) in a complementary fashion, combining their benefits has emerged as a particularly attractive option. New PPAR-targeted therapies that balance the relative potency and/or activity toward PPAR- and -γ have shown promise in retaining efficacy while reducing potential side effects. |
| File Format | HTM / HTML |
| ISSN | 14740338 |
| Issue Number | 1 |
| Volume Number | 12 |
| e-ISSN | 1744764X |
| Journal | Expert Opinion on Drug Safety |
| Language | English |
| Publisher | Taylor & Francis |
| Publisher Date | 2013-01-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Diabetes Mellitus, Type 2 Drug Therapy Dyslipidemias Hypoglycemic Agents Therapeutic Use Hypolipidemic Agents Ppar Alpha Agonists Ppar Gamma Animals Cardiovascular Diseases Chemically Induced Metabolism Drug Design Humans Adverse Effects Chemistry Risk Assessment Risk Factors Treatment Outcome Urinary Bladder Neoplasms Journal Article Research Support, Non-u.s. Gov't Review |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology (medical) |
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