Oct. 3, 2000--Axys Pharmaceuticals, Inc. (Nasdaq:AXPH - news) announced today the achievement of an important research milestone in its collaboration with Aventis (NYSE:AVE - news) on Cathepsin S, an enzyme believed to play a critical role in asthma. Axys indicated that a discrete collaboration compound synthesized by Axys had successfully demonstrated in vivo efficacy in a model of asthma, qualifying the compound and its analogs as a lead compound series. This family of compounds has been advanced into lead optimization, including pharmacokinetic evaluation, safety pharmacology, chemical scale-up, and formulation studies. Upon the successful conclusion of these activities, the Company believes that Aventis will formally nominate a clinical development candidate for the treatment of asthma.
Cathepsin S is a member of a large family of cysteine proteases, enzymes that are responsible for the cleavage and breakdown of other natural proteins in normal biological processes. In disease conditions, cysteine proteases can often be misregulated, providing an entry point for drug intervention. Cathepsin S has been highly associated with the processing and activation of the antigen receptor called MHC-II, essential for the initiation of both normal and pathological immune responses mediated by T-cells. Drugs designed to inhibit this enzyme could provide a novel method for control of antigen-induced response in multiple inflammatory diseases such as asthma, COPD, atherosclerosis and a variety of autoimmune and inflammatory diseases.
Approximately 10 months ago, Axys announced achievement of a milestone from Aventis (then Rhone-Poulenc Rorer) following the successful conclusion of in vivo efficacy proof-of-concept studies that confirmed the biological connection of Cathepsin S to the inflammatory process. These studies also showed that inhibiting Cathepsin S could provide a directed way to regulate the pathological imbalances in autoimmunity and inflammation.
``The milestone that we achieved this summer represents another success for the Company's preclinical research group. Moving this novel compound family into final optimization studies reflects the confidence of our partner, Aventis, that a candidate compound for the treatment of asthma will ready for formal nomination as a clinical development candidate in the near term. In addition to the proof-of-concept studies established at the end of last year, the latest studies confirm the potential for the use of the specific candidate in controlling asthma by oral administration,'' commented Michael C. Venuti, Ph.D., senior vice president, research and preclinical development, and chief technical officer at Axys Pharmaceuticals, Inc.
In December 1998, Axys and Aventis entered into a collaboration to discover and develop small molecule therapeutics that inhibit Cathepsin S. Under the terms of the agreement with Aventis, Axys and Aventis are collaborating on research and development of, among other things, orally bioavailable Cathepsin S inhibitors for asthma, atherosclerosis and rheumatoid arthritis. In addition to the two milestones met less than 18 months from the initiation of the collaboration, Axys remains eligible for a number of additional preclinical and clinical milestone payments..... |
