Drug intelligence / Profile preview

quiflapon

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-591 (quiflapon) is a potent, selective, and orally active small molecule inhibitor of 5-lipoxygenase-activating protein (FLAP). FLAP is a membrane-bound protein essential for the activation of 5-lipoxygenase (5-LO), the enzyme responsible for converting arachidonic acid into leukotrienes, which are potent inflammatory mediators. By binding to FLAP, MK-591 prevents the transfer of arachidonic acid to 5-LO, thereby blocking the production of leukotrienes such as LTB4 and LTC4. Originally developed by Merck for the treatment of asthma and ulcerative colitis, MK-591 demonstrated the ability to significantly reduce leukotriene levels in clinical trials but failed to show superior clinical efficacy over placebo in ulcerative colitis. More recent research has explored MK-591 for its potential neuroprotective effects in Alzheimer's disease, where it appears to modulate gamma-secretase activity and reduce tau phosphorylation, and as an antiviral agent against the Zika virus by inhibiting its NS2B-NS3 protease.

Other names
quiflapon sodium
02

Targets

FLAP (Arachidonate 5-lipoxygenase-activating protein)ZIKV NS2B-NS3pro (Zika virus NS2B-NS3 protease)

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