InteKrin Therapeutics Presents Positive Long Term INT131 Preclinical Cardiovascular Safety Data at the 45th Annual European Association for the Study of Diabetes Meeting
--2-Year Rodent Studies Also Show No Evidence of Carcinogenicity--
LOS ALTOS, Calif., Sept. 30 /PRNewswire/ -- InteKrin Therapeutics Inc. announced today positive results for INT131 in long term, high exposure preclinical safety studies. Data will be presented at the 45th Annual European Association for the Study of Diabetes Meeting in Vienna, Austria at 12:45 PM Thursday, October 1, 2009 by InteKrin Therapeutics' Chief Operating Officer, Linda Higgins, PhD, in a presentation "Chronic Cardiovascular Safety of INT131 Besylate, a Selective PPAR-gamma Modulator (SPPARM) in Rodents and Monkeys is Differentiated from TZD Full Agonists."
"Typical cardiovascular effects noted with PPAR-gamma full agonists in preclinical and clinical studies, such as weight gain, fluid retention, cardiac hypertrophy, and premature death were not observed in the 2-year studies in rats and mice, or in a 1-year study in cynomolgus monkeys even at the highest doses tested, which provided very high exposure multiples of the clinical exposure at efficacious doses," said Dr. Higgins. "Results are consistent with in vitro and in vivo studies and with clinical data demonstrating a SPPARM profile of INT131 having unique PPAR-gamma activating properties with minimal cardiovascular side effects."
"Chronic nonclinical safety studies of PPAR-gamma ligands have been highly predictive of clinical experience," noted Jeri El Hage, PhD, an expert in PPAR toxicology who served over 18 years in the Center for Drug Evaluation and Research (CDER) at the FDA. "INT131 displayed an unprecedented preclinical safety profile with no cardiac safety signals at exposure multiples far greater than other PPAR agonists tested to date."
The high cardiovascular safety margin validates the design of INT131 to minimize the safety and tolerability issues associated with full agonist PPAR-gamma agents while retaining the clinically proved anti-diabetic properties of PPAR-gamma. In addition, the 2-year rodent studies showed no evidence of carcinogenicity following lifetime exposure to INT131. These results are enabling for INT131 to initiate planned Phase 3 clinical studies.
INT131 is a next-generation insulin sensitizer that addresses insulin resistance, a key etiological feature in the onset and subsequent progression of type 2 diabetes. INT131 has been designed to provide a safer therapeutic tool for physicians and patients, which is complementary to available classes of medications, and allows for powerful glucose control and the opportunity for modification of the underlying disease. As a SPPARM, INT131 selectively modulates PPAR-gamma, and is ideally positioned to safely improve insulin resistance, addressing an important unmet medical need.
About InteKrin (www.InteKrin.com):
InteKrin Therapeutics is a privately-held clinical-stage drug development company focused on diabetes, obesity and metabolic disease. InteKrin's business strategy is to build a robust portfolio of high value products by in-licensing clinical-stage therapeutic candidates that address significant unmet medical needs and rapidly move them through critical development stages. InteKrin's team of world-class scientific and medical experts includes veterans from several successful BioPharma organizations, internationally recognized experts in nuclear receptors and metabolism, top scientists formerly with the Food and Drug Administration and key clinical and commercialization leaders.
Source: InteKrin Therapeutics Inc.
CONTACT: Heather Zimmerman of InteKrin Therapeutics Inc.,
Web Site: http://www.intekrin.com/
Posted: October 2009