 |
|
 |
- May 17, 2008 |
|
|
Welcome to the #1 online source of information for Diabetes Specialists! An international online community of more than 10,000 Diabetes Specialists.
CME on Diabetes is a website built to transmit top-level CME conferences given by international experts in endocrinology, insulin resistance, prediabetes, metabolic syndrome and type 2 diabetes. More than 2.6 million slides have been viewed since the website launch. Thank you for your continued support and commitment!
|
|
|
| Presentation |
|
"Dual PPAR alpha/gamma Agonists - Promise and Problems"Prof. John Prins (biography)
English - 2005-12-07 - 29 minutes
|
 | (22 slides) |
Summary :
In this presentation Prof. Prins talks about a newer class of compounds, the dual PPAR α/γ agonists, collectively known as the glitazars.
The Peroxisome Proliferator-Activated Receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. PPAR α ligands include the fibrate drugs which are used in patients with hyperlipidemia and which reduce triglycerides, increase HDL cholesterol and reduce inflammation. Ligands of PPAR γ include the thiazolidinedione class of agents used in the treatment of type 2 diabetes. These drugs reduce circulating free fatty acid levels, improve insulin sensitivity and glycemic control, and have anti-inflammatory effects.
Since many patients with insulin resistance also have dyslipidemia it would be theoretically advantageous to have a dual PPAR α/γ agonist for the treatment of these individuals. Initial in vitro and animal studies found glitazar compounds to improve insulin sensitivity and lower blood glucose, improve lipid status, and reduce inflammation, all with a relatively modest weight gain. Human trials have since been initiated.
Muraglitazar and tesaglitazar are 2 compounds that gained FDA approval for longer-term and later phase clinical trials, and muraglitazar was recently reported from a 24-week study to have beneficial effects on glycemic control and lipid status in type 2 diabetic patients (1). Also published in 2005 was a composite analysis of all clinical results for muraglitazar raising concerns about an apparent increased cardiovascular risk associated with muraglitazar treatment in type 2 diabetic patients (2). Muraglitazar is currently being evaluated in further studies to address these concerns.
Copyright © 2006 E-MedHosting.com Inc.
Learning objectives :
After viewing this presentation the participant will be able to discuss:
- PPAR isoforms, their effects and ligands
- Dual PPAR α/γ agonists (glitazars): development and recent clinical data
- Safety issues related to glitazar treatment in type 2 diabetic patients
Bibliographic references :
1. Buse JB, Rubin CJ, Frederich R, Viraswami-Appanna K, Lin KC, Montoro R, Shockey G, Davidson JA.Muraglitazar, a dual (α/γ) PPAR activator: A randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with type 2 diabetes Clin Ther. 2005 Aug;27(8):1181-95.
2. Nissen SE, Wolski K, Topol EJ.Effect of muraglitazar on death and major adverse cardiovascular events in patients with type 2 diabetes mellitus. JAMA. 2005 Nov 23;294(20):2581-6.
|
|
|
|
|
|
| Search our website |
 |
| |
Would you like to know more about insulin resistance? Are you looking for information pertaining to Type 2 Diabetes? You can find what you are looking for in over 2000 references available on CMEonDiabetes. |
| |
|
|
| Social |
|
| |
Let others know about this presentation.
|
|
|
|
