By Mary Welch
In its first major U.S. collaboration and first sale of its set of compounds for screening, Molecumetics Ltd. signed a three-year, potential $45 million deal with Bristol-Myers Squibb Co. to develop drugs for inflammatory and immunological diseases.
Under the terms of the agreement, Bellevue, Wash.-based Molecumetics will supply its 150,000 MolecuSet compounds to Bristol-Myers for broad-based screening against a number of disease targets.
Edward Field, vice president of business development for Molecumetics, said the hit rate "is anticipated, based on internal efforts, to be significantly higher than the industry norm." Scaffolds on which the compounds are based, he said, mimic those in natural molecular recognition events.
"Nature has used it and it worked, and we're using it as well," Field said. "It's not just some molecule some chemist has come up with, and thrown at a target. There's some rationale. It seems to be working."
Bristol-Myers, of New York, will provide Molecumetics with research funding and milestone payments that could exceed $45 million over three years. Additional milestone and royalty payments are possible from Bristol-Myers' screening of MolecuSet compounds.
The collaborative research will focus on the identification of small-molecule transcription factor inhibitors that interact with novel molecular targets identified by Molecumetics.
A chemistry-based drug discovery company, Molecumetics has identified compounds for the treatment of cardiovascular, inflammatory and metastatic diseases. Its Smart Library technology involves the design and synthesis of proprietary small molecules for rapid lead identification and optimization.
The company has identified lead compounds for molecular targets including proteases, G-protein coupled receptors, protein kinases and protein-protein interactions. Smart Library mixes combinatorial chemistry with structural biology by focusing on molecular scaffolds that mimic nature's secondary structure motifs — extended strands, alpha-helices, and beta-turns.
"If you look at all proteases, for instance, all recognize their substrates in the extended-strand position," Field told BioWorld Today. Molecumetix's mimicking compounds, "when they go into the active site, all go into the extended strand position," he said.
The company also employs automated screening and molecular modeling capabilities in its internal discovery programs, which include tryptase inhibitors and urokinase inhibitors.
Partners Wanted For Blood Coagulation Inhibitors
A subsidiary of Tredegar Industries, of Richmond, Va., Molecumetics has partnerships with Asahi Chemical Industries Co. Ltd. and Teijin Ltd., both of Tokyo, aimed at identifying compounds to treat heart disease and blood coagulation disorders.
This fall, Molecumetics plans to seek partners interested in the U.S. and European rights to oral thrombin and Factor VIIa inhibitors retained from the Tokyo collaborations. Factor VIIa is a key protease in the blood-coagulation cascade.
Tredegar, a manufacturer of plastics and aluminum extrusions, has interests in drug discovery and other emerging technologies. *