ImmunoPharmaceutics Inc. has synthesized two newcompounds that it hopes to develop into a hypertension drugthat blocks the effects of endothelin, a naturally occurringprotein that raises blood pressure.
The San Diego company (IPI) synthesized the compounds usinga patent-pending rational drug design process that uses theshape of pharmacologically active antibodies and other proteinsto create new orally active drugs.
The process involves X-ray crystallography to determine thethree-dimensional coordinates of a protein. It also usessupercomputers to calculate 3-D structures of amino acids andto simulate the action of very small molecules, said Dr. EdwardMaggio, president and chief executive officer of IPI andSynbiotics Corp. (NASDAQ:SBIO), which owns 48 percent of IPI.
The process allows researchers to study how proteins interactwith a biological target. "It is a major breakthrough in theprotein area," said Maggio, because it requires no assumptionsabout the shape of a protein. The process allowed IPI tocompute the key shape of endothelin, and it predicted that theidentified compounds would demonstrate significant endothelinreceptor antagonist activity.
Laboratory tests have confirmed "precisely the activitypredicted by our drug design process," Maggio told BioWorld.
The endothelin antagonist candidate would be IPI's firstproduct, and the San Diego company plans to apply forinvestigational new drug status by the end of 1992, Maggiosaid.
IPI will begin synthesizing its second drug candidatecompound, an interleukin-1 receptor antagonist, within a fewmonths, he said, and is developing other compounds to treatcardiovascular disease and disorders stemming frominflammation and faulty immune regulation.
IPI uses two IBM RS/6000 workstations. Together, theyprovide up to 60 percent to 80 percent of the computing powerof the Cray Research supercomputers that the company hadbeen using through a time-sharing arrangement, "but at a verysmall fraction of the cost," Maggio said.
"It's a breakthrough in the drug area because now companiesof our size have the ability to do these drug calculations, whichnormally would be very expensive," he said.
-- Kris Herbst BioWorld Washington Bureau
(c) 1997 American Health Consultants. All rights reserved.