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tipelukast
- Development stage
- Phase 2
- Lead developer
- MediciNova
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tipelukast (also known as MN-001 and KCA-757) is a novel, orally bioavailable small molecule compound with anti-fibrotic and anti-inflammatory properties. Its mechanism of action includes antagonism of leukotriene receptors, inhibition of phosphodiesterases (mainly types 3 and 4), and inhibition of 5-lipoxygenase. Tipelukast also down-regulates genes that promote fibrosis (such as LOXL2, collagen type I, TIMP-1) and inflammation (such as CCR2 and MCP-1). It has been investigated for the treatment of idiopathic pulmonary fibrosis (IPF), non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hypertriglyceridemia in patients with NAFLD/NASH, scleroderma/systemic sclerosis, interstitial cystitis, asthma, and other chronic inflammatory or fibrotic diseases. The drug was originally developed by Kyorin Pharmaceutical and is currently being developed by MediciNova[1][3][5][6][7].
- Other names
- tipelukast
02
Targets
PDE4 (Phosphodiesterase 4A1)CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)ALOX5 (Arachidonate 5-lipoxygenase)PDE3
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