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UPJOHN's CEPHALOSPORIN CS-807 IS IN PHASE II CLINICAL TRIALS

Executive Summary

UPJOHN's CEPHALOSPORIN CS-807 IS IN PHASE II CLINICAL TRIALS for respiratory infections, the company reported at the 27th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) in New York City. In an Oct. 5 presentation, Upjohn scientists discussed results of a number of preliminary investigations of CS-807, including Phase I human trials. "The spectrum and potency of [CS-807] was similar to that of [Lederle's NDA-pending] cefixime and significantly better than that of cefaclor and amoxicillin. In general, the activity of [CS-807] was comparable to cefixime for gram-negative bacteria, but more active than cefixime for gram-positive bacteria," an abstract of a study conducted by B. H. Yagi and G. E. Zurenko noted. Upjohn said that CS-807 is resistant to bacterial enzymes called beta-lactamases, which can break down antibiotics before they can take effect. The company licensed the orally active, third-generation antibiotic from the Japanese firm Sankyo in February, and has exclusive U.S. rights to the drug. In Japan, CS-807 is in Phase III trials. Upjohn has also licensed another third-generation cephalosporin, cefmetazole, from Sankyo. The injectable antibiotic is further along in the development cycle. Upjohn says that it expects to file an NDA for cefmetazole by year end. In addition, Upjohn scientists also reported on the company's progress with trospectomycin, an analog of Trobicin (spectinomycin). Developed in-house at Upjohn, trospectomycin is currently in Phase II clinicals for community-acquired pneumonia and sexually transmitted diseases. "Laboratory tests indicate that when injected, trospectomycin may distribute to the cerebrospinal fluid that bathes the brain (which many drugs do not), thus enabling it to combat the bacteria there that are known to cause meningitis," the company said in an Oct. 5 press release. Upjohn added that it has conducted "initial studies in healthy human volunteers." The Phase I studies have "revealed no clinically significant changes or irritation of surrounding tissue following intravenous and intramuscular administration."
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