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methacholine

Trade name: provocholine

Small moleculeapproved

Approved

Oct 31, 1986

Methacholine (trade name Provocholine) is a synthetic choline ester that acts as a muscarinic receptor agonist. Methacholine is primarily used to diagnose bronchial hyperreactivity, which is the hallmark of asthma and also occurs in chronic obstructive pulmonary disease. This is accomplished through the bronchial challenge test, or methacholine challenge, in which a subject inhales aerosolized methacholine, leading to bronchoconstriction. — NCATS

Clinical trial activity

29 trials · 31 clinical orgs · 2 marketing orgs

Phase 1
2
Phase 2
6
Phase 3
6
Phase 4
5

Earliest trial started Aug 1, 2003 (NCT02263976)

Timeline

1980s

  1. Oct 31, 1986

    Earliest FDA Approval

  2. Oct 31, 1986

    Methapharm — NDA Secondary Org

2000s

  1. Jan 1, 2003

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2005

    Earliest Phase 3 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewOct 31, 1986

Chemistry & pharmacology

Loading structure…

SMILES

CC(=O)OC(C)C[N+](C)(C)C
Mol. weight
160.24 g/mol
Lipinski Ro5
Pass
Rule of 3
Yes
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Black box warning

Sources

Also known as

  • acetyl-beta-methylcholine
  • acetyl-beta-methylcholine
  • acetylmethylcholine
  • acetylmethylcholine
  • acetylmethylcholine
  • beta-methylacetylcholine
  • mch
  • mch
  • mecholin
  • mecholine
  • methachoine
  • methacholin
  • methacholine
  • methacholine
  • methacholine
  • methacholine
  • methacholine
  • methacholine
  • methacholine
  • methacholine chloride
  • methacholine chloride
  • methacholine chloride
  • methacholine chloride
  • methacholine chloride
  • methacholine chloride
  • methacholine chloride
  • provocholine
  • provocholine
  • provocholine

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06730620Phase 4Jan 29, 2024Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd, Peking University
NCT05634473N/ADec 31, 2022Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd
NCT05292976Phase 3Apr 30, 2022Aurobindo Pharma
NCT04912596N/ASep 30, 2021Intech Biopharm Ltd.
NCT03505489Phase 3May 1, 2018University of Saskatchewan
NCT03105843Phase 4Sep 1, 2017Queen's University, Belfast
NCT02822859N/AJun 1, 2016University of Saskatchewan
NCT02584257Phase 3Apr 1, 2016Lupin
NCT02630511N/ADec 1, 2015University of Alberta
NCT02502825N/AJul 31, 2015Firestone Institute for Respiratory Health, Guangzhou Medical University
NCT02574975Phase 4Apr 1, 2015Southern Medical University
NCT02100267Phase 3Apr 1, 2014Sanwa Kagaku Kenkyusho Co., Ltd.
NCT02097537Phase 3Feb 1, 2014Santen Inc.
NCT03062904N/AFeb 1, 2014University of Paris
NCT01907334Phase 4Aug 1, 2013Teva, University of Florida
NCT01847768N/AApr 1, 2013Asthma and Allergic Diseases Cooperative Research Centers, National Institute of Allergy and Infectious Diseases (NIAID), University of Calgary
NCT01699594N/AOct 1, 2012University of Saskatchewan
NCT01547286N/AMay 1, 2012Harvard University, National Heart, Lung, and Blood Institute (NHLBI)
NCT01642745Phase 4Nov 1, 2011University of Saskatchewan
NCT01919424N/AApr 1, 2011McMaster University
Showing 20 of 29 trials
Page 1 / 2

Organizations

Research & Development (31)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
University of SaskatchewanAcademic/Hospital5532009
Jiangsu Chia-tai Tianqing Pharmaceutical Co.,LtdFor profit2122022
National Heart, Lung, and Blood Institute (NHLBI)Government2012007
Queen's University, BelfastAcademic/Hospital2222010
SyntaraFor profit2122005
University of FloridaAcademic/Hospital2222005
Asthma and Allergic Diseases Cooperative Research CentersAcademic/Hospital1012013
Aurobindo PharmaFor profit1112022
Boehringer IngelheimFor profit1112003
Colorado Allergy and Asthma Centers, PCAcademic/Hospital1012005
Firestone Institute for Respiratory HealthAcademic/Hospital1012015
GlaxoSmithKlineFor profit1012005
Guangzhou Medical UniversityAcademic/Hospital1112015
Harvard UniversityAcademic/Hospital1112012
Intech Biopharm Ltd.For profit1112021
LupinFor profit1112016
MannKind CorpFor profit1112008
McMaster UniversityAcademic/Hospital1112011
National Institute of Allergy and Infectious Diseases (NIAID)Government1112013
NovartisFor profit1112007
31 organizations
Page 1 / 2

Marketing (2)

OrganizationOrg typeRelationshipDate
MethapharmFor profitNDA2Oct 31, 1986
RocheFor profitNDA—