Identification
NameMontelukast
Accession NumberDB00471  (APRD00434)
TypeSmall Molecule
GroupsApproved
Description

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair®, produced by Indian company Cipla.

Structure
Thumb
Synonyms
(R-(e))-1-(((1-(3-(2-(7-Chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropaneacetic acid
1-[[[(1 R)-1-[3-[(1e)-2-(7-chloro-2-Quinolinyl)ethenyl] phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid
Montelukast
Montélukast
Montelukastum
External IDs L 706631 / MK 0476 / MK 476
Product Ingredients
IngredientUNIICASInChI KeyDetails
Montelukast sodiumU1O3J18SFL 151767-02-1LBFBRXGCXUHRJY-HKHDRNBDSA-MDetails
Product Images
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Accel-montelukast Sodium TabletsTablet10 mgOralAccel Pharma IncNot applicableNot applicableCanada
Ach-montelukastTablet, chewable5 mgOralAccord Healthcare Limited2014-06-09Not applicableCanada
Ach-montelukastTablet, chewable4 mgOralAccord Healthcare Limited2014-06-09Not applicableCanada
Auro-montelukastTablet10 mgOralAuro Pharma Inc2013-03-04Not applicableCanada
Auro-montelukast Chewable TabletTablet, chewable5 mgOralAuro Pharma Inc2014-03-26Not applicableCanada
Auro-montelukast Chewable TabletTablet, chewable4 mgOralAuro Pharma Inc2014-03-26Not applicableCanada
Bio-montelukastTablet10 mgOralBiomed PharmaNot applicableNot applicableCanada
Dom-montelukastTablet, chewable4 mgOralDominion Pharmacal2012-10-03Not applicableCanada
Dom-montelukastTablet, chewable5 mgOralDominion Pharmacal2012-10-03Not applicableCanada
Dom-montelukast FcTablet10 mgOralDominion Pharmacal2012-09-26Not applicableCanada
Ipg-montelukastTablet10 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-montelukastTablet, chewable4 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-montelukastTablet, chewable5 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-montelukastTablet, chewable4 mgOralJamp Pharma CorporationNot applicableNot applicableCanada
Jamp-montelukastTablet, chewable5 mgOralJamp Pharma CorporationNot applicableNot applicableCanada
Jamp-montelukastTablet10 mgOralJamp Pharma Corporation2012-09-21Not applicableCanada
Mar-montelukastTablet, chewable4 mgOralMarcan Pharmaceuticals Inc2013-12-30Not applicableCanada
Mar-montelukastTablet, chewable5 mgOralMarcan Pharmaceuticals Inc2013-12-30Not applicableCanada
Mar-montelukastTablet10 mgOralMarcan Pharmaceuticals Inc2013-12-30Not applicableCanada
Mint-montelukastTablet10 mgOralMint Pharmaceuticals Inc2013-10-17Not applicableCanada
Mint-montelukastTablet, chewable4 mgOralMint Pharmaceuticals Inc2013-10-17Not applicableCanada
Mint-montelukastTablet, chewable5 mgOralMint Pharmaceuticals Inc2013-10-17Not applicableCanada
MontelukastTablet10 mgOralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
MontelukastTablet, chewable5 mgOralSanis Health Inc2012-03-21Not applicableCanada
MontelukastTablet, chewable5 mgOralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
MontelukastTablet, chewable5 mgOralPro Doc Limitee2012-03-29Not applicableCanada
MontelukastTablet10 mgOralSanis Health Inc2012-03-21Not applicableCanada
MontelukastTablet, chewable4 mgOralSanis Health Inc2012-03-21Not applicableCanada
MontelukastTablet10 mgOralPro Doc Limitee2012-03-29Not applicableCanada
MontelukastTablet, chewable4 mgOralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
MontelukastTablet10 mgOralRanbaxy Inc.Not applicableNot applicableCanada
MontelukastTablet, chewable4 mgOralPro Doc Limitee2012-03-29Not applicableCanada
Montelukast SodiumGranule4 mg/1OralPrasco, Laboratories2013-07-26Not applicableUs
Montelukast Sodium TabletsTablet10 mgOralAccord Healthcare Limited2012-03-28Not applicableCanada
Mylan-montelukastTablet, chewable4 mgOralMylan Pharmaceuticals2012-02-27Not applicableCanada
Mylan-montelukastTablet10 mgOralMylan Pharmaceuticals2011-10-20Not applicableCanada
Mylan-montelukastTablet, chewable5 mgOralMylan Pharmaceuticals2012-02-27Not applicableCanada
Ntp-montelukastTablet, chewable5 mgOralTevaNot applicableNot applicableCanada
Ntp-montelukastTablet10 mgOralTevaNot applicableNot applicableCanada
Ntp-montelukastTablet, chewable4 mgOralTevaNot applicableNot applicableCanada
Pendo-montelukastTablet, chewable5 mgOralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
Pendo-montelukastTablet, chewable4 mgOralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
Pendo-montelukast FcTablet10 mgOralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
PMS-montelukastTablet, chewable4 mgOralPharmascience Inc2011-10-11Not applicableCanada
PMS-montelukastTablet, chewable5 mgOralPharmascience Inc2011-10-11Not applicableCanada
PMS-montelukast FcTablet10 mgOralPharmascience Inc2011-10-11Not applicableCanada
Priva-montelukast FcTablet10 mgOralPharmapar IncNot applicableNot applicableCanada
Q-montelukastTablet10 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Ran-montelukastTablet, chewable5 mgOralRanbaxy Inc.2013-07-08Not applicableCanada
Ran-montelukastTablet10 mgOralRanbaxy Inc.2013-01-17Not applicableCanada
Ran-montelukastTablet, chewable4 mgOralRanbaxy Inc.2013-07-08Not applicableCanada
Ratio-montelukastTablet10 mgOralTevaNot applicableNot applicableCanada
Ratio-montelukastTablet, chewable5 mgOralTevaNot applicableNot applicableCanada
Ratio-montelukastTablet, chewable4 mgOralTevaNot applicableNot applicableCanada
Riva-montelukastTablet, chewable4 mgOralLaboratoire Riva IncNot applicableNot applicableCanada
Riva-montelukastTablet, chewable5 mgOralLaboratoire Riva IncNot applicableNot applicableCanada
Riva-montelukast FcTablet10 mgOralLaboratoire Riva Inc2013-01-17Not applicableCanada
Sandoz MontelukastTablet, chewable4 mgOralSandoz Canada Incorporated2011-10-11Not applicableCanada
Sandoz MontelukastTablet, chewable5 mgOralSandoz Canada Incorporated2011-10-11Not applicableCanada
Sandoz Montelukast GranulesGranule4 mgOralSandoz Canada Incorporated2011-10-11Not applicableCanada
Sandoz Montelukast TabletTablet10 mgOralSandoz Canada Incorporated2011-10-11Not applicableCanada
SingulairTablet, chewable5 mg/1Oralbryant ranch prepack1998-02-20Not applicableUs
SingulairTablet, film coated10 mg/1OralRebel Distributors1998-02-20Not applicableUs
SingulairTablet, film coated10 mg/1OralA S Medication Solutions1998-08-122017-06-20Us
SingulairTablet10 mgOralMerck Ltd.1998-08-21Not applicableCanada
SingulairTablet, chewable4 mg/1OralPhysicians Total Care, Inc.2002-05-30Not applicableUs
SingulairGranule4 mg/1OralMerck Sharp & Dohme Limited2002-07-26Not applicableUs
SingulairTablet, film coated10 mg/1OralPhysicians Total Care, Inc.2000-12-05Not applicableUs
SingulairTablet, chewable5 mg/1OralCardinal Health1998-02-20Not applicableUs
SingulairTablet, chewable5 mgOralMerck Ltd.1998-08-21Not applicableCanada
SingulairTablet, film coated10 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-212017-04-14Us
SingulairGranule5 mg/1OralRemedy Repack2013-02-262016-10-13Us
SingulairTablet, film coated10 mg/1Oralbryant ranch prepack1998-02-20Not applicableUs
SingulairTablet, film coated10 mg/1OralMerck Sharp & Dohme Limited1998-02-20Not applicableUs00006 9117 54 nlmimage10 663f3329
SingulairTablet, chewable5 mg/1OralDispensing Solutions, Inc.2009-10-08Not applicableUs
SingulairTablet, chewable5 mg/1OralRebel Distributors1998-02-20Not applicableUs
SingulairTablet, chewable5 mg/1OralA S Medication Solutions2000-11-102017-06-20Us
SingulairTablet, chewable4 mgOralMerck Ltd.2001-04-09Not applicableCanada
SingulairTablet, chewable5 mg/1OralPhysicians Total Care, Inc.2003-07-03Not applicableUs
SingulairTablet, film coated10 mg/1OralPd Rx Pharmaceuticals, Inc.1998-02-202017-02-24Us
SingulairTablet, chewable5 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-212017-04-14Us
SingulairGranule10 mg/1OralRemedy Repack2013-03-012016-10-13Us
SingulairTablet, chewable4 mg/1OralMerck Sharp & Dohme Limited1998-02-20Not applicableUs
SingulairTablet, chewable4 mg/1Oralbryant ranch prepack1998-02-20Not applicableUs
SingulairTablet, film coated10 mg/1OralCardinal Health1998-02-20Not applicableUs
SingulairTablet, chewable5 mg/1OralMerck Sharp & Dohme Limited1998-02-20Not applicableUs
SingulairTablet, film coated10 mg/1OralDispensing Solutions, Inc.2009-10-08Not applicableUs
SingulairTablet, film coated10 mg/1OralRemedy Repack2013-03-282016-10-22Us
SingulairTablet, chewable4 mg/1OralA S Medication Solutions1999-04-232017-06-20Us
SingulairGranule4 mgOralMerck Ltd.2004-02-20Not applicableCanada
SingulairTablet, chewable4 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-212017-04-14Us
SingulairTablet, chewable4 mg/1OralPd Rx Pharmaceuticals, Inc.1998-02-202017-01-27Us
Teva-montelukastTablet, chewable4 mgOralTeva2011-10-11Not applicableCanada
Teva-montelukastTablet, chewable5 mgOralTeva2011-10-11Not applicableCanada
Teva-montelukastTablet10 mgOralTeva2011-10-11Not applicableCanada
Uni-montelukastTablet, chewable4 mgOralUnimark Remedies LimitedNot applicableNot applicableCanada
Uni-montelukastTablet, chewable5 mgOralUnimark Remedies LimitedNot applicableNot applicableCanada
Uni-montelukastTablet10 mgOralUnimark Remedies LimitedNot applicableNot applicableCanada
Van-montelukastTablet10 mgOralVanc Pharmaceuticals IncNot applicableNot applicableCanada
Van-montelukastTablet, chewable4 mgOralVanc Pharmaceuticals IncNot applicableNot applicableCanada
Van-montelukastTablet, chewable5 mgOralVanc Pharmaceuticals IncNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-montelukastTablet, chewable5 mgOralApotex Corporation2013-02-15Not applicableCanada
Apo-montelukastTablet10 mgOralApotex Corporation2012-01-20Not applicableCanada
Apo-montelukastTablet, chewable4 mgOralApotex Corporation2013-02-15Not applicableCanada
MontelukastTablet, chewable5 mg/1OralAse Direct, Inc.2014-12-012017-01-14Us
MontelukastTablet, chewable4 mg/1OralRecipharm Pharmaservices Private Limited2014-12-01Not applicableUs
MontelukastTablet, film coated10 mg/1OralSandoz2012-08-03Not applicableUs
MontelukastTablet, film coated10 mg/1OralWest Ward Pharmaceutical2014-12-01Not applicableUs
MontelukastTablet, film coated10 mg/1OralBionpharma Inc.2014-12-01Not applicableUs
MontelukastTablet10 mg/1OralNu Care Pharmaceuticals,inc.2012-02-28Not applicableUs
MontelukastTablet, film coated10 mg/1OralRecipharm Pharmaservices Private Limited2014-12-01Not applicableUs
MontelukastTablet, chewable5 mg/1OralSandoz2012-08-03Not applicableUs00781 5555 92 nlmimage10 d5496aab
MontelukastTablet10 mg/1OralMacleods Pharmaceuticals Limited2012-02-28Not applicableUs
MontelukastTablet, film coated10 mg/1OralLegacy Pharmaceutical Packaging2014-09-10Not applicableUs
MontelukastTablet, film coated10 mg/1OralClinical Solutions Wholsesale2012-08-032017-06-20Us
MontelukastTablet, film coated10 mg/1OralAse Direct, Inc.2014-12-012017-01-14Us
MontelukastTablet, chewable5 mg/1OralProficient Rx LP2014-12-01Not applicableUs
MontelukastTablet, chewable5 mg/1OralRecipharm Pharmaservices Private Limited2014-12-01Not applicableUs
MontelukastTablet, film coated10 mg/1Oralbryant ranch prepack2012-08-03Not applicableUs
MontelukastTablet, chewable5 mg/1OralWest Ward Pharmaceutical2014-12-01Not applicableUs
MontelukastTablet, chewable4 mg/1OralBionpharma Inc.2014-12-01Not applicableUs
MontelukastTablet, chewable5 mg/1OralPreferreed Pharmaceuticals Inc.2016-09-13Not applicableUs
MontelukastTablet, chewable4 mg/1OralAse Direct, Inc.2014-12-012017-01-14Us
MontelukastTablet, chewable4 mg/1OralWest Ward Pharmaceutical2014-12-01Not applicableUs
MontelukastTablet, chewable5 mg/1OralBionpharma Inc.2014-12-01Not applicableUs
MontelukastTablet, chewable4 mg/1OralSandoz2012-08-03Not applicableUs00781 5554 31 nlmimage10 d944ece7
MontelukastTablet, film coated10 mg/1OralInternational Laboratories, Llc2013-10-04Not applicableUs00093 7426 56 nlmimage10 dc27ee6f
MontelukastTablet, film coated10 mg/1OralCamber Pharmaceuticals2014-09-10Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralTeva2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralBlue Point Laboratories2014-03-13Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAidarex Pharmaceuticals LLC2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralPhysicians Total Care, Inc.2012-08-09Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralPreferreed Pharmaceuticals Inc.2014-05-05Not applicableUs
Montelukast SodiumGranule4 mg/1OralAjanta Pharma Limited2015-08-13Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralCardinal Health2012-08-29Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1Oralbryant ranch prepack2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAv Kare, Inc.2012-08-10Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralMed Vantx, Inc.2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralRemedy Repack2017-01-23Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralCarilion Materials Management2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralKremers Urban2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralAv Pak2014-11-11Not applicableUs
Montelukast SodiumTablet, coated10 mg/1OralProficient Rx LP2015-11-10Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralA S Medication Solutions2013-04-112017-06-20Us
Montelukast SodiumTablet, chewable5 mg/1OralAurobindo Pharma2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralMylan Pharmaceuticals2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralLucid Pharma Llc2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralReady Meds2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralLucid Pharma Llc2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralLegacy Pharmaceutical Packaging2012-08-032017-07-20Us
Montelukast SodiumTablet, film coated10 mg/1OralA S Medication Solutions2016-01-012017-06-20Us
Montelukast SodiumTablet, film coated10 mg/1OralA S Medication Solutions2012-08-032016-10-25Us
Montelukast SodiumTablet, coated10 mg/1OralRemedy Repack2015-05-212017-04-14Us
Montelukast SodiumTablet, chewable4 mg/1OralDr Reddy's Laboratories2012-08-06Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralPreferreed Pharmaceuticals Inc.2016-06-08Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralRemedy Repack2017-08-16Not applicableUs
Montelukast SodiumTablet, coated10 mg/1OralLegacy Pharmaceutical Packaging2012-08-06Not applicableUs55111 0725 30 nlmimage10 9f3a4fc2
Montelukast SodiumTablet, coated10 mg/1OralAmerincan Health Packaging2015-02-15Not applicableUs
Montelukast SodiumTablet10 mg/1OralAvera Mc Kennan Hospital2015-07-03Not applicableUs
Montelukast SodiumTablet10 mg/1OralHangzhou Minsheng Binjiang Pharm2016-05-30Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAphena Pharma Solutions Tennessee, Inc.2012-08-10Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast sodiumTablet, chewable5 mg/1OralMacleods Pharmaceuticals Limited2013-12-27Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralHangzhou Minsheng Binjiang Pharmaceutical Co., Ltd.2015-11-30Not applicableUs
Montelukast SodiumTablet, coated10 mg/1OralAjanta Pharma Limited2015-08-13Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralPar Pharmaceutical2012-08-032018-09-30Us
Montelukast SodiumTablet10 mg/1OralProficient Rx LP2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralCamber Pharmaceuticals2015-05-27Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralNu Care Pharmaceuticals,inc.2013-04-11Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralCitron Pharma LLC2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralMylan Pharmaceuticals2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast SodiumTablet, chewable5 mg/1OralWest Ward Pharmaceutical2012-08-03Not applicableUs
Montelukast SodiumGranule4 mg/1OralDr Reddy's Laboratories2012-09-20Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralTorrent Pharmaceuticals Limited2012-08-03Not applicableUs13668 0080 30 nlmimage10 9b3e4da2
Montelukast SodiumTablet, film coated10 mg/1OralPhysicians Total Care, Inc.2012-08-09Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralApotex Corporation2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAurobindo Pharma2012-08-03Not applicableUs
Montelukast SodiumGranule4 mg/500mgOralMylan Pharmaceuticals2013-09-182018-08-31Us
Montelukast SodiumTablet, chewable5 mg/1OralLucid Pharma Llc2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralTeva2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAccord Healthcare Limited2013-01-15Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralRebel Distributors2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralCardinal Health2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralProficient Rx LP2015-11-10Not applicableUs
Montelukast SodiumTablet10 mg/1OralPd Rx Pharmaceuticals, Inc.2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralAjanta Pharma Limited2015-08-13Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralProficient Rx LP2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralAv Kare, Inc.2013-01-02Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAmerincan Health Packaging2012-07-022016-02-29Us
Montelukast SodiumTablet, film coated10 mg/1OralUnichem Pharmaceuticals (USA), Inc.2016-01-01Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralCarilion Materials Management2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralKremers Urban2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralDirectrx2017-03-29Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralAv Pak2014-11-12Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralCarilion Materials Management2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralNu Care Pharmaceuticals,inc.2013-04-11Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast SodiumTablet, film coated10 mg/1OralGlenmark Pharmaceuticals Inc.,Usa2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralPar Pharmaceutical2012-08-032018-10-31Us
Montelukast SodiumTablet, chewable4 mg/1OralCitron Pharma LLC2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralAmerincan Health Packaging2012-07-022015-12-31Us
Montelukast SodiumTablet, chewable5 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast SodiumTablet10 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast SodiumTablet10 mg/1OralWest Ward Pharmaceutical2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralDr Reddy's Laboratories2012-08-06Not applicableUs
Montelukast SodiumTablet10 mg/1OralMajor2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralApotex Corporation2012-08-03Not applicableUs60505 3562 09 nlmimage10 a33a51d2
Montelukast SodiumTablet, film coated10 mg/1OralProficient Rx LP2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralProficient Rx LP2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralCamber Pharmaceuticals2015-05-27Not applicableUs
Montelukast SodiumTablet10 mg/1OralAmneal Pharmaceuticals2013-07-31Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralAurobindo Pharma2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralMylan Pharmaceuticals2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast SodiumTablet, chewable4 mg/1OralTeva2012-08-03Not applicableUs00093 7424 56 nlmimage10 0f280780
Montelukast SodiumTablet, chewable4 mg/1OralPreferreed Pharmaceuticals Inc.2017-04-17Not applicableUs
Montelukast SodiumTablet10 mg/1OralTorrent Pharmaceuticals Limited2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralPhysicians Total Care, Inc.2012-08-09Not applicableUs00093 7425 56 nlmimage10 d727ebff
Montelukast SodiumTablet, film coated10 mg/1OralProficient Rx LP2013-04-11Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralKremers Urban2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralRemedy Repack2017-03-17Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralAv Pak2014-10-02Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralLegacy Pharmaceutical Packaging2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralNu Care Pharmaceuticals,inc.2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralRemedy Repack2016-10-27Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralAmerincan Health Packaging2015-02-152016-11-30Us
Montelukast SodiumTablet, chewable5 mg/1OralPreferreed Pharmaceuticals Inc.2016-02-01Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralCardinal Health2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralMajor2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralPd Rx Pharmaceuticals, Inc.2013-04-11Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralPd Rx Pharmaceuticals, Inc.2012-08-03Not applicableUs13668 0079 30 nlmimage10 1b3c8d84
Montelukast SodiumTablet, film coated10 mg/1OralCardinal Health2013-05-23Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralDirectrx2014-01-01Not applicableUs
Montelukast sodiumTablet, chewable4 mg/1OralMacleods Pharmaceuticals Limited2014-04-01Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralHangzhou Minsheng Binjiang Pharmaceutical Co., Ltd.2015-11-30Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralAjanta Pharma Limited2015-08-13Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralPar Pharmaceutical2012-08-032018-08-31Us
Montelukast SodiumTablet, chewable5 mg/1Oralbryant ranch prepack2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralAv Kare, Inc.2013-01-02Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralCarilion Materials Management2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralMylan Institutional2012-08-28Not applicableUs
Montelukast SodiumTablet10 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralProficient Rx LP2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralCitron Pharma LLC2012-08-03Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralAmerincan Health Packaging2013-05-222015-12-31Us
Montelukast SodiumTablet, coated10 mg/1OralRemedy Repack2017-03-08Not applicableUs
Montelukast SodiumTablet, chewable5 mg/1OralA S Medication Solutions2012-08-032017-06-20Us
Montelukast SodiumTablet, chewable4 mg/1OralWest Ward Pharmaceutical2012-08-03Not applicableUs
Montelukast SodiumTablet, coated10 mg/1OralDr Reddy's Laboratories2012-08-06Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralTorrent Pharmaceuticals Limited2012-08-03Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralState of Florida DOH Central Pharmacy2014-11-01Not applicableUs
Montelukast SodiumTablet, film coated10 mg/1OralPreferreed Pharmaceuticals Inc.2016-06-17Not applicableUs
Montelukast SodiumTablet, chewable4 mg/1OralApotex Corporation2012-08-03Not applicableUs
Montelukast sodium chewableTablet, chewable4 mg/1OralJubilant Cadista Pharmaceuticals Inc.2015-02-28Not applicableUs
Montelukast sodium chewableTablet, chewable5 mg/1OralJubilant Cadista Pharmaceuticals Inc.2015-02-28Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LukotasNot Available
MollyAllenge
MonocastBeximco
MontefloNot Available
Montelo-10Not Available
MonteneSquare
RespaireSanta-Farma
SurfairSandoz
TelumantesActavis
VentekSearle
VentilarGutis
XalarUnimed
ZespiraBilim
Brand mixturesNot Available
Categories
UNIIMHM278SD3E
CAS number158966-92-8
WeightAverage: 586.183
Monoisotopic: 585.21044242
Chemical FormulaC35H36ClNO3S
InChI KeyUCHDWCPVSPXUMX-TZIWLTJVSA-N
InChI
InChI=1S/C35H36ClNO3S/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39)/b15-10+/t32-/m1/s1
IUPAC Name
2-[1-({[(1R)-1-{3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl}-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanyl}methyl)cyclopropyl]acetic acid
SMILES
OC(=O)CC1(CC1)CS[[email protected]](CCC1=CC=CC=C1C(O)(C)C)C1=CC=CC(\C=C\C2=NC3=C(C=CC(Cl)=C3)C=C2)=C1
Pharmacology
Indication

For the treatment of asthma

Structured Indications
Pharmacodynamics

Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.

Mechanism of action

Montelukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Montelukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.

TargetKindPharmacological actionActionsOrganismUniProt ID
Cysteinyl leukotriene receptor 1Proteinyes
antagonist
HumanQ9Y271 details
Arachidonate 5-lipoxygenaseProteinunknown
other/unknown
HumanP09917 details
Related Articles
Absorption

Rapidly absorbed following oral administration (bioavailability is 64%)

Volume of distribution
  • 8 to 11 L
Protein binding

99% (to plasma proteins)

Metabolism

Hepatic

SubstrateEnzymesProduct
Montelukast
Not Available
Montelukast metabolite M1Details
Montelukast
Montelukast metabolite M2aDetails
Montelukast
Montelukast metabolite M2bDetails
Montelukast
Montelukast metabolite M5aDetails
Montelukast
Montelukast metabolite M5bDetails
Montelukast
Montelukast metabolite M6aDetails
Montelukast
Montelukast metabolite M6bDetails
Route of elimination

Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

Half life

2.7-5.5 hours

Clearance
  • 45 mL/min [healthy adults]
Toxicity

Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe metabolism of Montelukast can be decreased when combined with Abiraterone.Approved
AmiodaroneThe metabolism of Montelukast can be decreased when combined with Amiodarone.Approved, Investigational
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Montelukast.Approved
AprepitantThe serum concentration of Montelukast can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe metabolism of Montelukast can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Montelukast can be decreased when combined with Atomoxetine.Approved
BexaroteneThe serum concentration of Montelukast can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Montelukast can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Montelukast can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Montelukast can be decreased when it is combined with Bosentan.Approved, Investigational
CapecitabineThe metabolism of Montelukast can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Montelukast can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Montelukast can be increased when it is combined with Ceritinib.Approved
CholecalciferolThe metabolism of Montelukast can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
ClarithromycinThe metabolism of Montelukast can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Montelukast can be decreased when combined with Clemastine.Approved
ClotrimazoleThe metabolism of Montelukast can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Montelukast can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Montelukast can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Montelukast can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Montelukast can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Montelukast can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Montelukast can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Montelukast can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Montelukast can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Montelukast can be decreased when combined with Delavirdine.Approved
DexamethasoneThe serum concentration of Montelukast can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DihydroergotamineThe metabolism of Montelukast can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Montelukast can be decreased when combined with Diltiazem.Approved
DoxycyclineThe metabolism of Montelukast can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Montelukast can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Montelukast can be decreased when it is combined with Efavirenz.Approved, Investigational
EnzalutamideThe serum concentration of Montelukast can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Montelukast can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Montelukast can be decreased when it is combined with Eslicarbazepine acetate.Approved
EtravirineThe serum concentration of Montelukast can be decreased when it is combined with Etravirine.Approved
FloxuridineThe metabolism of Montelukast can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Montelukast can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Montelukast can be decreased when combined with Fluorouracil.Approved
FluvastatinThe metabolism of Montelukast can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Montelukast can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Montelukast can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Montelukast can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Montelukast can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Montelukast can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe serum concentration of Montelukast can be increased when it is combined with Gemfibrozil.Approved
IdelalisibThe serum concentration of Montelukast can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Montelukast can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Montelukast can be decreased when combined with Indinavir.Approved
IrbesartanThe metabolism of Montelukast can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Montelukast can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Montelukast can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Montelukast can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Montelukast can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Montelukast can be decreased when combined with Ketoconazole.Approved, Investigational
LeflunomideThe metabolism of Montelukast can be decreased when combined with Leflunomide.Approved, Investigational
LopinavirThe metabolism of Montelukast can be decreased when combined with Lopinavir.Approved
LosartanThe metabolism of Montelukast can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Montelukast can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Montelukast is combined with Loxapine.Approved
LuliconazoleThe serum concentration of Montelukast can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Montelukast can be decreased when it is combined with Lumacaftor.Approved
MifepristoneThe serum concentration of Montelukast can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Montelukast can be decreased when it is combined with Mitotane.Approved
ModafinilThe serum concentration of Montelukast can be decreased when it is combined with Modafinil.Approved, Investigational
NafcillinThe serum concentration of Montelukast can be decreased when it is combined with Nafcillin.Approved
NefazodoneThe metabolism of Montelukast can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Montelukast can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Montelukast can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Montelukast can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Montelukast can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Montelukast can be decreased when combined with Nicotine.Approved
NilotinibThe metabolism of Montelukast can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Montelukast can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Montelukast can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Montelukast can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Montelukast can be increased when it is combined with Palbociclib.Approved
PentobarbitalThe metabolism of Montelukast can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Montelukast can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Montelukast can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Montelukast can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Montelukast can be increased when combined with Primidone.Approved, Vet Approved
PyrimethamineThe metabolism of Montelukast can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinineThe metabolism of Montelukast can be decreased when combined with Quinine.Approved
RanolazineThe metabolism of Montelukast can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Montelukast can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Montelukast can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Montelukast can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Montelukast can be decreased when combined with Ritonavir.Approved, Investigational
SaquinavirThe metabolism of Montelukast can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Montelukast can be increased when combined with Secobarbital.Approved, Vet Approved
SildenafilThe metabolism of Montelukast can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Montelukast can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Montelukast can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Montelukast can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Montelukast can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Montelukast can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Montelukast can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Montelukast can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Montelukast can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Montelukast can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Montelukast can be decreased when combined with Telithromycin.Approved
TicagrelorThe metabolism of Montelukast can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Montelukast can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Montelukast can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Montelukast can be decreased when combined with Tolbutamide.Approved
TrimethoprimThe metabolism of Montelukast can be decreased when combined with Trimethoprim.Approved, Vet Approved
Valproic AcidThe metabolism of Montelukast can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Montelukast can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe metabolism of Montelukast can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Montelukast can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Montelukast can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Montelukast can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Montelukast can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take without regard to meals.
References
Synthesis Reference

Evgeny Shapiro, Ronit Yahalomi, Valerie Niddam-Hildesheim, Greta Sterimbaum, Kobi Chen, "Processes for preparing montelukast sodium." U.S. Patent US20050256156, issued November 17, 2005.

US20050256156
General ReferencesNot Available
External Links
ATC CodesR03DC53 — Montelukast, combinationsR03DC03 — Montelukast
AHFS Codes
  • 48:10.24
PDB EntriesNot Available
FDA labelDownload (503 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentAsthma Bronchial4
1CompletedNot AvailableAsthma and Allergic Rhinitis1
1CompletedNot AvailableDrug-drug Interaction Study1
1CompletedNot AvailableHealthy Volunteers4
1CompletedBasic ScienceChronic Lung Disease of Prematurity1
1CompletedBasic ScienceRheumatoid Arthritis2
1CompletedDiagnosticAsthma Bronchial1
1CompletedDiagnosticAsthma, Exercise-Induced1
1CompletedOtherAsthma Bronchial2
1CompletedTreatmentAsthma Bronchial4
1CompletedTreatmentChronic Asthma1
1CompletedTreatmentHealthy Volunteers7
1CompletedTreatmentOesophagitis, Eosinophilic1
1CompletedTreatmentRhinitis1
1RecruitingTreatmentMultiple Myeloma (MM)1
1Unknown StatusBasic ScienceAsthma Bronchial1
1, 2RecruitingTreatmentDisseminated Sclerosis1
2Active Not RecruitingTreatmentChronic Graft Versus Host Disease / Hematopoietic Stem Cell Transplant (HSCT) / Leukotriene / Montelukast / Obliterative Bronchiolitis1
2Active Not RecruitingTreatmentPremature Labour1
2CompletedPreventionChronic Lung Disease of Prematurity / Premature Births / Very Low Birth Weight Infant1
2CompletedTreatmentAllergic Rhinitis (AR)1
2CompletedTreatmentAsthma Bronchial16
2CompletedTreatmentAsthma Bronchial / Rhinitis, Allergic, Seasonal1
2CompletedTreatmentBronchiolitis1
2CompletedTreatmentObliterative Bronchiolitis1
2Not Yet RecruitingTreatmentAsthma Acute / Asthma Bronchial / Asthma in Children1
2TerminatedPreventionCryptogenic Organizing Pneumonia / Lung Diseases, Interstitial / Obliterative Bronchiolitis / Respiratory Tract Infections (RTI)1
2TerminatedTreatmentAsthma Bronchial1
2TerminatedTreatmentSleep Apnea Syndrome1
2Unknown StatusTreatmentAsthma Bronchial1
2Unknown StatusTreatmentCoughing1
2WithdrawnTreatmentAsthma Bronchial1
2, 3CompletedPreventionAsthma Bronchial / Chronic Lung Diseases1
2, 3Unknown StatusTreatmentAsthma Bronchial1
2, 3Unknown StatusTreatmentAsthma Bronchial / Status Asthmaticus2
2, 3WithdrawnTreatmentAsthma Bronchial1
3Active Not RecruitingTreatmentOesophagitis, Eosinophilic / Swallowing Disorders1
3CompletedPreventionAsthma, Exercise-Induced3
3CompletedTreatmentAllergic Rhinitis (AR)1
3CompletedTreatmentAsthma Bronchial21
3CompletedTreatmentAsthma Bronchial / Chronic Obstructive Pulmonary Disease (COPD)1
3CompletedTreatmentAsthma Bronchial / Wheezing1
3CompletedTreatmentBronchial Asthma1
3CompletedTreatmentBronchiolitis1
3CompletedTreatmentExercised Induced Asthma1
3CompletedTreatmentPerennial Allergic Rhinitis (PAR)3
3CompletedTreatmentRhinitis, Allergic, Perennial1
3CompletedTreatmentRhinitis, Allergic, Seasonal2
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)7
3CompletedTreatmentWheezing1
3Not Yet RecruitingTreatmentPain1
3Unknown StatusPreventionUpper Respiratory Tract Infections1
3Unknown StatusTreatmentBronchial Asthma1
3WithdrawnTreatmentBronchial Asthma1
4Active Not RecruitingTreatmentAsthma Bronchial1
4Active Not RecruitingTreatmentDisseminated Sclerosis1
4CompletedNot AvailableAsthma Bronchial2
4CompletedBasic ScienceAsthma Bronchial1
4CompletedDiagnosticAsthmatic Smokers / Non-asthmatic Smokers1
4CompletedPreventionAcute Otitis Media / Ear Infection / Otitis Media (OM)1
4CompletedPreventionAirway Reactivity1
4CompletedPreventionExercise Induced Bronchospasm1
4CompletedPreventionUpper Respiratory Infections1
4CompletedSupportive CareAsthma Bronchial1
4CompletedTreatmentAcute Asthma Exacerbation1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentAllergic Rhinitis (AR) / Asthma Bronchial1
4CompletedTreatmentAsthma Bronchial17
4CompletedTreatmentAsthma Bronchial / Asthma, Exercise-Induced1
4CompletedTreatmentAsthma Bronchial / Conjunctivitis, Seasonal Allergic / Moderate, refractory Atopic dermatitis / Seasonal Allergic Rhinitis (SAR)1
4CompletedTreatmentAsthma Bronchial / Seasonal Allergic Rhinoconjunctivitis1
4CompletedTreatmentBronchial Asthma1
4CompletedTreatmentBronchial Hyperreactivity / Coughing1
4CompletedTreatmentChronic Periodontitis1
4CompletedTreatmentCoughing1
4CompletedTreatmentElderly / Persistent Asthma1
4CompletedTreatmentExercise-Induced Bronchoconstriction (EIB)1
4CompletedTreatmentLung Diseases, Obstructive / Signs and Symptoms, Respiratory1
4CompletedTreatmentObliterative Bronchiolitis / Rejection, Transplant / Transplantation, Lung1
4CompletedTreatmentObstructive Sleep Apnea Syndrome (OSAS)1
4CompletedTreatmentPerennial Allergic Rhinitis (PAR)1
4CompletedTreatmentModerate, refractory Atopic dermatitis1
4Not Yet RecruitingTreatmentModerate, refractory Atopic dermatitis1
4RecruitingDiagnosticCoughing1
4RecruitingTreatmentAsthma Bronchial2
4RecruitingTreatmentCoughing1
4RecruitingTreatmentHealthy Volunteers1
4TerminatedDiagnosticAsthma Bronchial1
4TerminatedTreatmentAcute Coronary Syndromes (ACS) / Coronary Artery Disease1
4TerminatedTreatmentAsthma Bronchial1
4TerminatedTreatmentObstructive Sleep Apnea (OSA)1
4TerminatedTreatmentRhinitis, Allergic, Perennial1
4Unknown StatusTreatmentAsthma Bronchial1
4Unknown StatusTreatmentAsthma Bronchial / Polyps, Nasal / Sinusitis1
4Unknown StatusTreatmentBronchial Asthma / Children / Food Allergy1
4Unknown StatusTreatmentNonasthmatic Eosinophilic Bronchitis1
4Unknown StatusTreatmentPersistent Cough / Whooping Cough1
4Unknown StatusTreatmentRhinitis1
4Unknown StatusTreatmentSeasonal Allergic Rhinitis (SAR)1
4Unknown StatusTreatmentSleep Disordered Breathing (SDB)1
4Unknown StatusTreatmentWheezing1
Not AvailableCompletedNot AvailableAsthma Bronchial3
Not AvailableCompletedBasic ScienceAirway Inflammation1
Not AvailableCompletedDiagnosticBronchial Asthma1
Not AvailableCompletedPreventionAsthma Bronchial1
Not AvailableCompletedPreventionRhinitis, Allergic, Perennial1
Not AvailableCompletedTreatmentAsthma Bronchial3
Not AvailableCompletedTreatmentAsthma Bronchial / BMI >30 kg/m2 / Inflammatory Reaction1
Not AvailableCompletedTreatmentAsthma Bronchial / Chronic Lung Diseases1
Not AvailableCompletedTreatmentAsthma, Allergic1
Not AvailableCompletedTreatmentBronchiolitis2
Not AvailableCompletedTreatmentBronchiolitis / Coughing / Wheezing1
Not AvailableCompletedTreatmentCoronary Heart Disease (CHD)1
Not AvailableCompletedTreatmentEosinophilic Gastroenteritis / Indigestion1
Not AvailableCompletedTreatmentRenal Insufficiency,Chronic1
Not AvailableCompletedTreatmentModerate, refractory Atopic dermatitis1
Not AvailableRecruitingNot AvailableAsthma Bronchial1
Not AvailableRecruitingNot AvailableBronchiolitis Obliterans Syndrome (BOS)1
Not AvailableRecruitingNot AvailablePortal Vein, Cavernous Transformation Of1
Not AvailableRecruitingBasic ScienceNasal Allergies1
Not AvailableTerminatedTreatmentAsthmatic Patients1
Not AvailableTerminatedTreatmentOesophagitis, Eosinophilic1
Not AvailableUnknown StatusBasic ScienceAsthma Bronchial1
Not AvailableUnknown StatusTreatmentChronic Otitis Media With Effusion / Conductive Hearing Loss1
Not AvailableUnknown StatusTreatmentCoughing1
Not AvailableUnknown StatusTreatmentStatus Asthmaticus1
Pharmacoeconomics
Manufacturers
  • Merck research laboratories div merck co inc
  • Merck and co inc
Packagers
Dosage forms
FormRouteStrength
Tablet, chewableOral4 mg/1
Tablet, chewableOral5 mg/1
Tablet, film coatedOral10 mg/1
GranuleOral4 mg/500mg
TabletOral10 mg/1
Tablet, coatedOral10 mg/1
GranuleOral10 mg/1
GranuleOral4 mg/1
GranuleOral4 mg
GranuleOral5 mg/1
TabletOral10 mg
Tablet, chewableOral4 mg
Tablet, chewableOral5 mg
Prices
Unit descriptionCostUnit
Singulair 30 4 mg Chew Tabs Bottle145.91USD bottle
Singulair 30 4 mg Packets Packet145.91USD packet
Singulair 30 5 mg Chew Tabs Bottle145.91USD bottle
Singulair 10 mg tablet4.77USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2179407 No2009-03-172014-12-22Canada
CA2053209 No1998-12-082011-10-10Canada
US8007830 No2002-10-242022-10-24Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP7.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility8.2e-06 mg/mLALOGPS
logP7.25ALOGPS
logP8.49ChemAxon
logS-7.8ALOGPS
pKa (Strongest Acidic)4.4ChemAxon
pKa (Strongest Basic)3.12ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area70.42 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity169.5 m3·mol-1ChemAxon
Polarizability66.36 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9947
Blood Brain Barrier+0.9311
Caco-2 permeable+0.5428
P-glycoprotein substrateSubstrate0.6839
P-glycoprotein inhibitor INon-inhibitor0.8863
P-glycoprotein inhibitor IINon-inhibitor0.9154
Renal organic cation transporterNon-inhibitor0.8395
CYP450 2C9 substrateNon-substrate0.6967
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7284
CYP450 1A2 substrateNon-inhibitor0.6266
CYP450 2C9 inhibitorNon-inhibitor0.7177
CYP450 2D6 inhibitorNon-inhibitor0.8436
CYP450 2C19 inhibitorNon-inhibitor0.5777
CYP450 3A4 inhibitorNon-inhibitor0.6759
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5515
Ames testNon AMES toxic0.7532
CarcinogenicityNon-carcinogens0.9126
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6488 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.985
hERG inhibition (predictor II)Non-inhibitor0.7932
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted GC-MSPredicted GC-MS Spectrum - GC-MSNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as linear 1,3-diarylpropanoids. These are organic compounds with a structure based on a C6-C3-C6 skeleton, where the two benzene rings are not linked together.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassLinear 1,3-diarylpropanoids
Sub ClassNot Available
Direct ParentLinear 1,3-diarylpropanoids
Alternative ParentsChloroquinolines / Phenylpropanes / Styrenes / Thia fatty acids / Hydroxy fatty acids / Pyridines and derivatives / Aryl chlorides / Tertiary alcohols / Heteroaromatic compounds / Sulfenyl compounds
SubstituentsLinear 1,3-diarylpropanoid / Haloquinoline / Chloroquinoline / Quinoline / Phenylpropane / Styrene / Hydroxy fatty acid / Thia fatty acid / Aryl chloride / Aryl halide
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptorsquinolines, monocarboxylic acid, aliphatic sulfide (CHEBI:50730 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Leukotriene receptor activity
Specific Function:
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affini...
Gene Name:
CYSLTR1
Uniprot ID:
Q9Y271
Uniprot Name:
Cysteinyl leukotriene receptor 1
Molecular Weight:
38540.55 Da
References
  1. Nayak A: A review of montelukast in the treatment of asthma and allergic rhinitis. Expert Opin Pharmacother. 2004 Mar;5(3):679-86. [PubMed:15013935 ]
  2. Zhang YJ, Zhang L, Wang SB, Shen HH, Wei EQ: Montelukast modulates lung CysLT(1) receptor expression and eosinophilic inflammation in asthmatic mice. Acta Pharmacol Sin. 2004 Oct;25(10):1341-6. [PubMed:15456537 ]
  3. Hamacher J, Eichert K, Braun C, Grebe T, Strub A, Lucas R, Eltze M, Wendel A: Montelukast exerts no acute direct effect on NO synthases. Pulm Pharmacol Ther. 2007;20(5):525-33. Epub 2006 May 19. [PubMed:16815057 ]
  4. Langlois A, Ferland C, Tremblay GM, Laviolette M: Montelukast regulates eosinophil protease activity through a leukotriene-independent mechanism. J Allergy Clin Immunol. 2006 Jul;118(1):113-9. Epub 2006 May 19. [PubMed:16815146 ]
  5. Alfieri AB, Tramontana M, Cialdai C, Lecci A, Giuliani S, Crea A, Manzini S, Maggi CA: Heterogeneous effect of leucotriene CysLT1 receptor antagonists on antigen-induced motor and inflammatory responses in guinea-pig airways. Auton Autacoid Pharmacol. 2007 Jan;27(1):39-46. [PubMed:17199874 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
General Function:
Iron ion binding
Specific Function:
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
Gene Name:
ALOX5
Uniprot ID:
P09917
Uniprot Name:
Arachidonate 5-lipoxygenase
Molecular Weight:
77982.595 Da
References
  1. Ramires R, Caiaffa MF, Tursi A, Haeggstrom JZ, Macchia L: Novel inhibitory effect on 5-lipoxygenase activity by the anti-asthma drug montelukast. Biochem Biophys Res Commun. 2004 Nov 12;324(2):815-21. [PubMed:15474500 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Uniprot Name:
Cytochrome P450 3A4
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Uniprot Name:
Cytochrome P450 2C9
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Uniprot Name:
Cytochrome P450 2C8
Molecular Weight:
55824.275 Da
References
  1. Schoch GA, Yano JK, Sansen S, Dansette PM, Stout CD, Johnson EF: Determinants of cytochrome P450 2C8 substrate binding: structures of complexes with montelukast, troglitazone, felodipine, and 9-cis-retinoic acid. J Biol Chem. 2008 Jun 20;283(25):17227-37. doi: 10.1074/jbc.M802180200. Epub 2008 Apr 15. [PubMed:18413310 ]
  2. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Uniprot Name:
Prostaglandin G/H synthase 1
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Uniprot Name:
Cytochrome P450 2A6
Molecular Weight:
56501.005 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Uniprot Name:
Solute carrier organic anion transporter family member 2B1
Molecular Weight:
76709.98 Da
References
  1. Mougey EB, Feng H, Castro M, Irvin CG, Lima JJ: Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet Genomics. 2009 Feb;19(2):129-38. doi: 10.1097/FPC.0b013e32831bd98c. [PubMed:19151602 ]
Drug created on June 13, 2005 07:24 / Updated on September 01, 2017 10:28