Novel Therapeutic Options for Diabetes: Unlocking the Door for CV Benefits

Corporate-sponsored symposium
Sunday, June 06, 2004
7:00 – 9:45 pm

Chair:
James Gavin III, MD, PhD

Faculty:
Ralph DeFronzo, MD, FACP
Peter Libby, MD
Simeon Taylor, MD, PhD

Reviewed by Joelle Escoffery, PhD

This program stressed the importance of more intensive risk factor management in patients with type 2 diabetes (T2D). The faculty discussed a new class of insulin sensitizers, PPAR agents, which have been shown to reduce hyperglycemia and dyslipidemia.

The current T2D agents have certainly done their job with regards to glucose lowering, however, we know now that T2D involves much more than just hyperglycemia.  PPAR agents are currently being developed to correct both hyperglycemia and dyslipidemia.

Through RXR binding, PPAR agents are able to lower glucose and insulin, thereby increasing insulin sensitivity, increase HDL-C, and lower LDL-C, triglycerides, and free fatty-acids (FFAs). PPARα receptor activation has an anti-inflammatory effect, while PPARγ receptor activation inhibits macrophages and monocyte-inhibitory cytokines.

Muraglitazar is a novel non-TZD, PPARα/γ dual agonist that is in development for the treatment of T2D and associated dyslipidemia. Its anticipated clinical dose range is 1.5 – 20 mg/day.