Lexin Pharmaceuticals Inc., a privately held drugdiscovery company, is on the verge of securing its firstmajor pharmaceutical collaboration for development ofcompounds aimed at inhibiting serine proteases.

Astra Merck Inc., a joint venture between Sweden-basedAB Astra and New York-based Merck & Co., haspurchased an option to develop and market Lexin'sLEX032, a recombinant version of a human anti-chymotrypsin protein, for acute pancreatitis.

Financial terms of the deal were not disclosed.

Lexin's president and CEO, Jerry Hook, said the AstraMerck option agreement covers preclinical evaluation ofLEX032 in animal models for pancreatitis. Studies areexpected to take six months.

If the drug demonstrates effectiveness in the animal trials,Astra Merck, of Wayne, Pa., and Lexin will negotiateterms for a full-fledged drug development collaboration.

The alliance would be Lexin's first corporate partnership,launching the Horsham, Pa.-based company's proteaseinhibitor compounds into clinical development.

Lexin, founded in 1989 with technology developed at theUniversity of Pennsylvania in Philadelphia, makes serineprotease inhibitors based on derivations of alpha-1 anti-chymotrypsin, which is modified for selective therapeuticactivity.

In treating pancreatitis, the anti-chymotrypsin protein inLEX032 is altered to prevent the migration ofneutrophils, which in excessive amounts cause tissuedamage.

Lexin has conducted preclinical studies of LEX032 forother inflammatory diseases, such as acute pulmonaryinflammation. In those animal trials the compoundreduced neutrophil infiltration to the lungs.

The company also is developing protease inhibitors totreat coagulation disorders. Based on the modification ofthe anti-chymotrypsin protein, the compounds wouldeither inhibit plasmin or thrombin. Too much plasminprevents blood clotting while too much thrombin has theopposite effect.

In another modification of the anti-chymotrypsin protein,Lexin is developing a compound aimed at inhibitingchymase, which is involved allergies and asthma.

The Astra Merck agreement "is a big step forward forus," said Hook, who describes Lexin as a drug discoveryand preclinical development company. He added thatAstra Merck may be interested in developing other Lexinprotease inhibitors.

Lexin also is collaborating with Wichita State Universityin Wichita, Kan., on development of orally administeredsmall molecule drugs based on the protein-derivedprotease inhibitors. n

-- Charles Craig

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