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MERCK LEUKOTRIENE ANTAGONIST MK-571 ASTHMA CLINICALS

Executive Summary

MERCK LEUKOTRIENE ANTAGONIST MK-571 ASTHMA CLINICALS should reach publication stage in 1990, Anthony Ford-Hutchinson of the Merck Frosst Centre for Therapeutic Research reported at a recent conference on allergic disease. MK-571 is one of the lead leukotriene compounds being studied by Merck at the Canadian research facility. The compound is a leukotriene D4 receptor antagonist. The allergy conference, sponsored by International Business Communications, took place in Boston Oct. 3-4. According to Dr. Hutchinson, "while several mediators have been suggested as possible factors in causing asthma, leukotriene D4 may play a major role, since it has been found to induce multiple pathologic airway responses in studies involving human tissue." In particular "leukotriene D4 induces smooth muscle contraction in human peripheral airways, . . . causes bronchoconstriction when inhaled, . . . increases the release of mucous in human airways, . . . and has been shown to induce bronchial hyperreactivity when administered by aerosol to asthmatic patients." According to Hutchinson, "MK-571 (formerly L-660, 711) is an example of a new class of potent leukotriene D4 receptor antagonists," and appears to inhibit the binding of leukotriene D4 to human lung homogenates selectively. The compound is believed to be in Phase II development. Having been shown to be "well-tolerated (when) administered intravenously in normal and asthmatic subjects in single doses of 15 to 1500 mg," and "shown to inhibit leukotriene D4-induced bronchoconstriction" in six healthy male volunteers, "MK-571 is currently being evaluated in asthmatics with and without bronchial provocation," Hutchinson reported. Intravenous, oral and aerosolized forms of the compound are all being examined, the Merck researcher observed. Another Merck leukotriene-related substance currently in clinical trials under the auspices of the Merck Frosst Centre is MK-886, an inhibitor of leukotriene biosynthesis rather than a receptor antagonist. In contrast to the receptor antagonists, MK-886 is believed to prevent the synthesis of leukotriene D4 within cells by preventing the activation of 5-lipoxygenase, an enzyme pathway through which the production of leukotrienes is catalyzed. Without discussing particulars of clinical trials, Hutchinson stated that "clinical studies in man with MK-886 will help define the role of leukotrienes in a variety of pathological processes including bronchial asthma, and comparative studies with MK-571 will provide information as to the relative importance of other leukotrienes than leukotriene D4, such as leukotriene B4."

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