The Institute for Diabetes Discovery,
LLC (IDD) has presented data on the most selective Aldose Reductase Inhibitors
(ARIs) ever developed for reducing the impact of diabetic peripheral neuropathy
(DPN), according to a recent report from The American Chemical Society's
national meeting.
As part of its aldose reductase inhibitor program, IDD produced several series
of inhibitors that led to the discovery of lidorestat, which has advanced to
phase 2 clinical trials. More recently, IDD focused its efforts on next
generation ARIs with an emphasis on enhanced efficacy, desirable
pharmacokinetic properties and greater selectivity. The result has been the
discovery and development of a novel series of potent compounds that are orally
active, (IC50 < 10 nM), and extremely selective (>25,000:1) for aldose
reductase versus aldehyde reductase, a closely related enzyme with a beneficial
physiological role. IDD's new compounds are all aimed at slowing the progress
of diabetic complications, particularly peripheral neuropathy. These new
compounds have significantly improved the motor nerve conduction velocity by
69% to 85% in an STZ-induced model. IDD compounds also lower sciatic nerve
sorbitol levels (ED50 = 0.6 - 2.5 mg/kg/d) and are highly bioavailable (79 -
97%).
While recent scientific evidence has confirmed the effectiveness of ARI therapy
in treating DPN, the development of this class of drugs has been hindered by
negative side effects, many of which are attributed to a lack of selectivity.
About 17 million people in the United States have been diagnosed with diabetes,
and it is estimated that 50% have some degree of peripheral neuropathy. The
total annual cost incurred by all payers in treating people with DPN and
associated complications is approximately $11 billion.
According to Professor Paul Zimmet, Chairman of the IDD Scientific Advisory
Board and Director of the International Diabetes Institute in Melbourne,
Australia, "What AIDS was in the last 20 years of the 20th Century, diabetes
and its complications will be in the first 20 years of this century. The
discovery of drugs to address the neuropathic complications of diabetes is a
very important initiative in attacking the devastation that diabetes causes to
both individuals and society."
IDD is a biopharmaceutical company specializing in the discovery and
preclinical development of small-molecule drugs for the prevention and
treatment of obesity and diabetes and its complications. IDD is a division of
The Institutes for Pharmaceutical Discovery, LLC, a privately held
pharmaceutical company located in Branford, Connecticut.
DATASOURCE: The Institute for Diabetes Discovery, LLC
CONTACT: Nils Bergenhem, Vice President of Research, The Institute for
Diabetes Discovery, LLC, +1-203-315-4000
Web site: http://www.idd-diabetes.com/