2. Academic Validation
  3. The discovery of setileuton, a potent and selective 5-lipoxygenase inhibitor

The discovery of setileuton, a potent and selective 5-lipoxygenase inhibitor

  • ACS Med Chem Lett. 2010 Apr 13;1(4):170-4. doi: 10.1021/ml100029k.
Yves Ducharme 1,  Marc Blouin 1,  Christine Brideau 1,  Anne Châteauneuf 1,  Yves Gareau 1,  Erich L Grimm 1,  Hélène Juteau 1,  Sébastien Laliberté 1,  Bruce MacKay 1,  Frédéric Massé 1,  Marc Ouellet 1,  Myriam Salem 1,  Angela Styhler 1,  Richard W Friesen 1
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Quebec, Canada H9H 3L1.
PMID: 24900191 DOI: 10.1021/ml100029k
Abstract

The discovery of novel and selective inhibitors of human 5-lipoxygenase (5-LO) is described. These compounds are potent, orally bioavailable, and active at inhibiting leukotriene biosynthesis in vivo in a dog PK/PD model. A major focus of the optimization process was to reduce affinity for the human ether-a-go-go gene Potassium Channel while preserving inhibitory potency on 5-LO. These efforts led to the identification of inhibitor (S)-16 (MK-0633, setileuton), a compound selected for clinical development for the treatment of respiratory diseases.

Keywords

Human 5-lipoxygenase; MK-0633; leukotriene biosynthesis; respiratory diseases; setileuton.

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