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MN-002 is a metabolite of tipelukast (MN-001), an orally bioavailable small molecule compound. MediciNova obtained an exclusive worldwide license (excluding Japan, China, South Korea, and Taiwan) from Kyorin Pharmaceuticals to develop and commercialize MN-002 for all indications except ophthalmic solutions. Tipelukast, and by extension its metabolite MN-002, exhibits anti-inflammatory and anti-fibrotic activities through multiple mechanisms, including leukotriene receptor antagonism, inhibition of phosphodiesterases (PDE) 3 and 4, and inhibition of 5-lipoxygenase (5-LO). It also leads to the down-regulation of genes that promote fibrosis, such as LOXL2, collagen type 1, and TIMP-1, and genes responsible for promoting inflammation, like CCR2 and MCP-1.
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