MEDI 214 |
| In the late 1970's the cysteinyl leukotrienes (CysLTs) were identified as novel peptidolipid mediators that were the active principles in “Slow Reacting Substance of Anaphylaxis (SRS-A)” and their role in the etiology of asthma was postulated. In 1979 a project was initiated at Merck Frosst first to synthesize leukotrienes, and then to discover potent and orally active inhibitors of leukotriene biosynthesis or antagonists of CysLT1, (the receptor for leukotriene D4, the most potent of the CysLTs). Sustained and intensive efforts over almost 20 years identified a number of development candidates, which reached clinical trials but were not deemed acceptable, before the discovery and development of the CysLT1 receptor antagonist, SINGULAIR (montelukast, MK-0476). SINGULAIR was approved by the FDA in 1998 as a well-tolerated and effective therapy for the treatment of chronic asthma, and is now approved also for allergic rhinitis. The success of SINGULAIR is due to its efficacy with rapid onset, excellent safety profile, simple once-daily oral dosing (including formulations optimized for children) and lack of significant drug or food interactions. SINGULAIR is one of the few drugs approved at initial launch for use by adults and by children (initially as young as 6 years) and is now approved for marketing in at least 109 countries and for use in infants as young as age 6 months. As the only well-tolerated oral agent that is effective both for asthma and for allergic rhinitis, SINGULAIR has changed the management of respiratory disease all around the world. |
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Heroes of Chemistry
1:30 PM-5:00 PM, Monday, August 20, 2007 BCEC -- 210 B/C, Oral
Division of Medicinal Chemistry |