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Montelukast is a leukotriene receptor antagonist used as part of an asthma therapy regimen, to prevent exercise induced bronchoconstriction, and to treat seasonal allergic rhinitis. Montelukast was first approved for clinical use by the US FDA in 1998 as Merck's brand name Singulair.
- Mechanism
- Curator reviewed · 35 references
Cysteinyl leukotrienes (CysLT) like LTC4, LTD4, and LTE4, among others, are eicosanoids released by a variety of cells like mast cells and eosinophils. When such CysLT bind to corresponding CysLT receptors like CysLT type-1 receptors located on respiratory airway smooth muscle cells, airway macrophages, and on various pro-inflammatory cells like eosinophils and some specific myeloid stem cells activities that facilitate the pathophysiology of asthma and allergic rhinitis are stimulated.
In particular, CysLT-mediated airway bronchoconstriction, occluding mucous secretion, vascular permeability, and eosinophil recruitment are all types of effects that facilitate asthma. Alternatively, in allergic rhinitis, CysLTs are released by the nasal mucosa when exposed to allergens during both early and late phase reactions and participate in eliciting symptoms of allergic rhinitis like a congested nose and airway.
Subsequently, montelukast is a leukotriene receptor antagonist that binds with high affinity and selectivity to the CysLT type 1 receptor, which consequently assists in inhibiting any physiological actions of CysLTs like LTC4, LTD4, and LTE4 at the receptor that may facilitate asthma or allergic rhinitis.
- Primary indication
- Montelukast is indicated for: (a) the prophylaxis and chronic treatment of asthma in adults and pediatric patients who are 12 months of age and older, although other regional health authorities specifically note this indication for...Curator reviewed · 5 structured indications
- Formula / weight
- C35H36ClNO3S · 586.183 g/mol (avg)
- First approval
- Canada, 2011 · United States, 1998
- Code names
- L 706631 · MK 0476 · MK 476
- Brand names
- Singulair
Resolves to
UCHDWCPVSPXUMX-TZIWLTJVSA-NSMILESOC(=O)CC1(CC1)CS[C@H](CCC1=CC=CC=C1C(O)(C)C)C1=CC=CC(\C=C\C2=NC3=C(C=CC(Cl)=C3)C=C2)=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Montelukast, and which of those have an active Phase 3 trial?