Biological Activity

• DescriptionCysteinyl leukotrienes (CysLTs, including LTC4, LTD4, and LTE4), mainly produced by eosinophils, mast cells, and macrophages in response to a variety of stimuli activating arachidonate 5-lipoxygenase pathway, are important inflammatory mediators. CysLT1 receptor (LTR1) expresses in human lung smooth muscle cells, lung macrophages, most peripheral blood eosinophils and pregranulocytic CD34+ cells, and in subsets of monocytes and B lymphocytes. Montelukast Sodium is a potent, selective and competitive LTR1 antagonist with IC₅₀ value < 5 nM and are currently used in the treatment of asthma. Nonsmoking patients with asthma treated with Montelukast Sodium(200mg, three times daily for 10 1/3 days) showed improvements in FEV₁, compared with placebo-treated patients^[5]. In C57BL/6 mice with asthma induced by chronic exposure to ovalbumin, Montelukast (6 mg/kg, once daily for 20 days) treatment significantly suppressed the increased eosinophils in bronchoalveolar lavage (BAL) fluid and lung tissue, and increased IL-5 level in BAL fluid in models^[6]. It was also proved that Montelukast inhibited the diabetes-induced capillary and neuronal degeneration in streptozotocin-induced diabetes mouse model^[7].
• MechanismMontelukast Sodium is a potent competing ligand for high affinity [³H]LTD4 specific binding.

• Animal Study
  Dose	Rat: 0.2 mg/kg - 20 mg/kg[3] (i.g.)
  Administration	i.g.
  Pharmacokinetics	Animal Mice[4] Rats[4] Monkeys[4] Dose 50 mg/kg 25 mg/kg 25 mg/kg Administration p.o. p.o. p.o. F 0.61 34.2 ± 13.8% 52.8 ± 25.2% T1/2 176 ± 122 min 457 ± 55.9 min AUC0→∞ 2411 μg·min/ml 580 ± 235 μg·min/ml 5360 ± 2557 μg·min/ml Cmax 14.4 μg/ml 2.82 ± 1.61 μg/ml 21.6 ± 4.32 μg/ml Tmax 60 min 37.5 ± 8.66 min 67.5 ± 35.7 min

• Clinical Study

• NCT Number	Condition or disease	Phase	Recruitment Status	Estimated Study Completion Date	Locations
  NCT02110654	Sinusitis Nas... more >>al Polyps Asthma Collapse <<	Phase 4	Unknown	June 2016	China, Guangdong ... more >> the first affiliated hospital, Sun Yat-sen University Not yet recruiting Guangzhou, Guangdong, China, 510080 Contact: Fenghong Chen, doctor    02086013560170816    chfhong@mail.sysu.edu.cn Principal Investigator: jianbo Shi, doctor Collapse <<
  NCT00504946	Asthma	Phase 3	Completed	-	Poland ... more >> Department of Pediatrics and Allergy, Medical University of Lodz Lodz, Poland Lodz, Poland, 93-513 Collapse <<
  NCT00398151	Asthma	Phase 3	Completed	-	-

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