Microcide Pharmaceuticals Collaborates With Pharmaceutical On Antifungals

NAEJA's Azoles Combined With Microcide's Efflux Pump Inhibitor Technology MOUNTAIN VIEW, Calif. and EDMONTON, Alberta, July 12, 2001 /PRNewswire/ -- Microcide Pharmaceuticals, Inc. (Nasdaq: MCDE - news) today announced that it has entered into a collaborative research and license agreement with NAEJA Pharmaceutical Inc., a private Alberta-based company, to discover, develop and commercialize drugs based upon NAEJA's proprietary azole antifungals and Microcide's proprietary fungal efflux pump inhibitor leads, in order to overcome resistance mechanisms in clinically-important fungal pathogens.

The collaboration gives Microcide exclusive worldwide rights to develop and commercialize compounds based on NAEJA Pharmaceutical's proprietary azoles-both alone and in combination with a Microcide fungal efflux pump inhibitor. Microcide will make milestone payments to NAEJA upon the selection of an azole and its advancement through clinical trials, and will pay royalties on sales of products commercialized by Microcide.

The initial goal of the collaboration is to select a preclinical development candidate from NAEJA's lead series, which are broader in spectrum and have greater potency against Candida and Aspergillus than current azole antifungals. The combination of the candidate compound with a Microcide efflux pump inhibitor should lead to a substantial improvement in terms of activity against resistant fungal organisms.

"We are very pleased to be collaborating with NAEJA to combine their promising novel azoles with our own fungal efflux pump inhibitors," said Jim Rurka, President & CEO of Microcide. "There is a clear unmet clinical need for new antifungal agents due to the limited number available, growing resistance and the high mortality related to invasive infections in cancer and other diseases. The worldwide market for products to address severe systemic fungal infections is estimated at $750 million."

Rurka added, "The collaborative R & D program based upon these azoles and their pairing with Microcide's anti-resistance technology produces the second Microcide-owned potential product opportunity identified in the past six months. In addition, we have development activities underway for four other potential antimicrobial products, that are advancing toward the clinic with partners."

"This collaboration with Microcide enables NAEJA to cover a very important development in antifungal therapy and places Microcide and NAEJA in the forefront of antifungal resistance control. We expect this collaboration to produce a promising antifungal drug candidate in the near future," commented Dr. Ronald Micetich, Chairman of the Board and President and CEO of NAEJA.

Christopher Micetich, Vice President and Chief Operating Officer of NAEJA commented, "We have identified several compounds that have excellent potency against Candida and Aspergillus and are pleased to collaborate on their optimization with Microcide. With this new Microcide collaboration, we see the potential to add value by applying Microcide's expertise in overcoming resistance mechanisms in pathogenic fungi, which could ultimately give these compounds even greater efficacy and safety advantages over the competition."

"Our efflux research indicates that a number of existing antibiotics and antifungals can be substantially improved by adding an efflux pump inhibitor to overcome resistance mechanisms," said George H. Miller, Ph.D., Senior Vice President of Research and Development of Microcide. "Our team of scientists is eager to work with NAEJA on this attractive broad-spectrum azole series for both yeasts and moulds. This is the third application of our efflux pump technology to reach this advanced stage. We have successfully collaborated on inhibitors of levofloxacin efflux in Pseudomonas with Daiichi Pharmaceuticals, and are currently working with Schering-Plough Animal Health on veterinary antibacterials."

Microcide is a biopharmaceutical company committed to the discovery, development and commercialization of novel antimicrobials for the improved treatment of serious bacterial, fungal and viral infections. The Company's three discovery research platforms address the growing problems of antibiotic resistance and the need for improved antifungal and antiviral therapeutics. The Company's Cephalosporin Antibiotics and Efflux Pump Inhibition platforms focus on developing novel antibiotics and antibiotic potentiators (efflux inhibitors) to directly address existing bacterial and fungal resistance problems. Microcide's Microbial Genomics platform utilizes proprietary bacterial, fungal and viral genetics and genomics tools -- the VALID System -- to discover entirely new classes of antimicrobial agents.

NAEJA Pharmaceutical Inc. is a private Canadian company created from the acquisition of assets from SynPhar Laboratories Inc. SynPhar's staff were responsible for the discovery of two drugs -- tazobactam, a beta-lactamase inhibitor marketed worldwide in combination with piperacillin as Zosyn® or Tazosyn® by American Home Products; and Mofezolac®, a non steroidal anti-inflammatory agent particularly useful for arthritis, and marketed only in Japan by Yoshitomi Pharmaceutical Ltd. NAEJA is a pharmaceutical research company specializing in the areas of infectious diseases, cancer and cysteine protease inhibitors, the latter particularly useful for the treatment of osteoporosis, asthma and rheumatoid arthritis. In addition to the above internal research, NAEJA utilizes its expertise in carrying out specialized early stage contract research up to the IND stage.

The statements contained in this press release which are not historical facts may be deemed to contain forward-looking statements. Actual results may differ materially from those expressed or implied in any forward-looking statement as a result of certain risks and uncertainties including, without limitation, the following. There is no assurance that any antifungal compounds developed will successfully proceed through preclinical development and clinical trials, obtain requisite regulatory approvals for marketing or result in a commercially useful product. There is no assurance that the Company will successfully continue existing corporate collaborations or enter into further collaborations with respect to any of its internally funded research programs or that current collaborators will elect to proceed through the various stages of clinical development as currently anticipated or on the same schedule as we would proceed if we were conducting such trials independently. For a discussion of other risks and uncertainties affecting Microcide's business, see the Company's annual report on Form 10-K/A for the year ended December 31, 2000 and its quarterly report on Form 10-Q for the quarter ended March 31, 2001. Actual results and timing of certain events could differ materially from those indicated in the forward-looking statements as a result of these or other factors.