Drug intelligence / Profile preview

verlukast

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

Overview

Verlukast (MK-0679) is a potent and selective small molecule antagonist of the leukotriene D4 (LTD4) receptor, also known as the cysteinyl leukotriene receptor 1 (CYSLTR1). It was developed by Merck as an oral therapy for asthma, particularly targeting patients with aspirin-sensitive asthma. Verlukast demonstrated significant clinical efficacy in blocking airway obstruction induced by inhaled lysine-aspirin and produced bronchodilation lasting at least nine hours in clinical studies. Despite its specificity and oral bioavailability, development was discontinued during late-stage trials due to concerns about liver enzyme elevations and insufficient potency compared to desired standards[2][3][6][7].

Other names
verlukast
02

Targets

MRP (Multidrug resistance-associated protein family)CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)

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