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Discovery and development of ML3000

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NSAID management of the inflammatory process has focused on reducing the production of inflammatory prostaglandins by inhibiting the cyclooxygenase (COX) enzyme. However, blocking COX also reduces gastroprotective prostaglandins, causing the well-known gastrointestinal side effects. Furthermore, a shunting of arachidonic acid to the 5-lipoxygenase (5-LOX) pathway may also occur, causing an increase in leukotrienes and further GI damage. Several compounds, designed to block both COX and 5-LOX, have failed in clinical trials due to liver toxicity, related to their redox potential. ML3000 is a new pyrrolizine compound resulting from a systematic approach to design a non-redox substrate analog of arachidonic acid that inhibited both COX and 5-LOX. Pharmacodynamic studies determined that ML3000 is a dual inhibitor of COX and 5-LOX, with analgesic, anti-inflammatory, antipyretic, antiplatelet, and anti-bronchoconstrictive activity, and minimal gastrointestinal side effects. Clinical studies show efficacy in osteoarthritis and excellent gastrointestinal safety. ML3000 is now in phase III development.

Affiliations: 1: Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, University of Tuebingen, Auf der Morgenstelle 8, D-72076 Tuebingen, Germany


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