A modified heparin molecule designed to preserve heparin'santi-restenotic property while eliminating its anti-coagulanttendencies, has shown the ability to block vascular restenosis.

Researchers reported the results of animal studies on GlycomedInc.'s (NASDAQ:GLYC) product Astenose this week at the 65thAnnual Heart Association Meeting in New Orleans.

Restenosis is the chronic reclosing of arteries followingangioplasty and open heart surgery. There are no drugscurrently available to treat this condition.

Gregory Dube, a researcher at Lilly Research Labs, a division ofEli Lilly and Co., presented results from rabbit models ofballoon angioplasty that confirmed earlier rodent experimentsdemonstrating Astenose's ability to block restenosis aftersubcutaneous injection.

And Ian Timms of the University of Pennsylvania didessentially the same experiments, with the same results, excepthis rabbits had experimentally elevated blood cholesterollevels. Glycomed claimed that "this animal model more closelymimics the condition of restenosis in humans because highcholesterol levels appear to be an important risk factor for thedevelopment of heart disease."

Brian Atwood, Glycomed's senior vice president of operations,added that Lilly has also studied the drug in a high-cholesterolrabbit model.

Also, "Lilly did a significant amount of work on dose responseand toxicity," Atwood told BioWorld. "At elevated doses theyobserved anorexia and weight loss, but these doses are two tothree times what we anticipate using in humans."

Additionally, researchers Michael Sobel and Robert Harris atthe Medical College of Virginia found that Astenose preventsplatelet aggregation in vitro. Glycomed is "following that up inguinea pigs now," Atwood said.

Astenose was discovered during a three-year collaborationbetween Glycomed and Lilly. Now the Alameda, Calif.,carbohydrate-drug firm is discussing with Lilly terms to regainmarketing rights to the product. "We believe that theopportunity to regain the rights ... is of singular importance toGlycomed," said Alan Timms, the company's president and chiefexecutive officer. "We intend filing an IND (investigational newdrug application) by the end of 1993."

Under the terms of its January 1990 agreement with Lilly,Glycomed licensed rights to compounds for preventingrestenosis and atherosclerosis, including Astenose, to Lilly forroyalty payments. The agreement expires at the end of theyear, when "the rights would come back to Glycomed anyway,"Atwood said.

Glycomed now wants to develop and commercialize Astenosefor its cardiovascular indications, while Lilly, which "discoveredanother biological effect of these compounds ... has asked forthe right to continue researching that activity," Atwoodexplained.

If a potential product results, Lilly would license Glycomed todevelop and commercialize the product, and Glycomed wouldpay Lilly a royalty, Atwood told BioWorld.

-- Jennifer Van Brunt Senior Editor

(c) 1997 American Health Consultants. All rights reserved.