tiotropium

Trade name: spiriva

Small moleculeapproved

Approved

Jan 30, 2004

Tiotropium is a long–acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3–receptors at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies prevention of methacholine–induced bronchoconstriction effects were dose–dependent and lasted longer than 24 hours. The bronchodilation following inhalation of tiotropium is predominantly a site–specific effect. Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, on topical application it acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect. Tiotropium is used in the management of chronic obstructive pulmonary disease (COPD).Tiotropium bromide capsules for inhalation are co-promoted by Boehringer-Ingelheim and Pfizer under the trade name Spiriva. It is also manufactured and marketed by Cipla under trade name Tiova. — NCATS

Clinical trial activity

322 trials · 125 clinical orgs · 2 marketing orgs

Phase 1
46
Phase 2
173
Phase 3
119
Phase 4
92

Earliest trial started Feb 1, 1998 (NCT02172326)

Timeline

1990s

  1. Jan 1, 1998

    Boehringer Ingelheim — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1998

    Boehringer Ingelheim — Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 1998

    Boehringer Ingelheim — Earliest Phase 3 Sponsor(trial)

2000s

  1. Jan 30, 2004

    Boehringer Ingelheim — Earliest FDA Approval

  2. Jan 30, 2004

    Boehringer Ingelheim — NDA Secondary Org

  3. Jan 30, 2004

    Boehringer Ingelheim — NDA Organization

2020s

  1. Jun 20, 2023

    Lupin — Marketing Organization

Indications

Mechanism of action

Combination products

  • stiolto respimat

    with olodaterol

    Also known as spiolto respimat

Approval history

  • approvedJan 30, 2004

Chemistry & pharmacology

Loading structure…

SMILES

C[N+]1(C)[C@@H]2C[C@@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@H]1[C@@H]1O[C@@H]12
Mol. weight
392.52 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Sources

Also known as

  • (8r)-6 beta,7 beta-epoxy-8-ethyl-3 alpha((-)-tropoyl)-1 alpha h, 5 alpha h-tropanium bromide
  • ba 253
  • ba-253
  • ba 253br
  • ba-253br
  • ba 679 br
  • ba 679 br
  • ba-679-br
  • ba-679-br
  • bea 2180 br
  • braltus
  • oxitropium
  • oxitropium
  • oxitropium
  • oxitropium
  • oxitropium
  • oxitropium
  • oxitropium
  • oxitropium bromide
  • oxitropium bromide
  • oxitropium bromide
  • oxitropium bromide
  • oxitropium bromide
  • oxitropium iodide
  • oxitropium iodide
  • oxitropium iodide
  • oxitropium iodide
  • oxitropium iodide, (r)-isomer
  • oxitropium iodide, (s)-isomer
  • oxivent
  • oxivent
  • oxivent
  • oxytropium bromide
  • oxytropium bromide
  • pur0200
  • qat370
  • respimat
  • spiriva
  • spiriva
  • spiriva
  • spiriva
  • spiriva
  • spiriva respimat
  • spiriva respimat
  • tersigat
  • tiopropium
  • tiopropium
  • tiotropium
  • tiotropium
  • tiotropium
  • tiotropium
  • tiotropium
  • tiotropium
  • tiotropium
  • tiotropiumbromide
  • tiotropium bromide
  • tiotropium bromide
  • tiotropium bromide
  • tiotropium bromide
  • tiotropium bromide
  • tiotropium bromide
  • tiotropium bromide hydrate
  • tiotropium bromide hydrate
  • tiotropium bromide hydrate
  • tiotropium bromide hydrate
  • tiotropium bromide hydrate
  • tiotropium bromide monohydrate
  • tiotropium bromide monohydrate
  • tiotropium bromide monohydrate
  • ventilat

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07267130Phase 1Nov 25, 2025Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd
NCT06487416Phase 1Jun 10, 2024Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd
NCT06326671Phase 1Feb 28, 2024Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd
NCT05838703Phase 2May 1, 2023Duke University
NCT06254664Phase 1Oct 3, 2022Exeltis, Iberica Co. Ltd.
NCT05986591Phase 3Aug 17, 2022Exeltis, Iberica Co. Ltd.
NCT05246046Phase 1Feb 16, 2022Orion Corporation
NCT05165485Phase 4Dec 31, 2021Mylan, Theravance
NCT05161156Phase 3Dec 18, 2021Phargentis SA
NCT05113615Phase 4Nov 30, 2021University of Saskatchewan
NCT04994574N/AAug 31, 2021Yonsei University
NCT04990167Phase 2Aug 1, 2021Nemours Foundation, Thomas Jefferson University
NCT04850144Phase 1Apr 26, 2021Orion Corporation
NCT05295355N/AJan 25, 2021Boehringer Ingelheim, Guangzhou Medical University
NCT04648813Phase 4Nov 13, 2020University of Saskatchewan
NCT04780984Phase 2Nov 1, 2020Nephron Pharmaceuticals Corporation, Rho, Inc.
NCT04231214Phase 4Feb 1, 2020Boehringer Ingelheim, Fraunhofer
NCT04223843Phase 4Jan 10, 2020Boehringer Ingelheim
NCT04147572N/ANov 1, 2019Orion Corporation
NCT03964207Phase 4Aug 30, 2019Boehringer Ingelheim
Showing 20 of 322 trials
Page 1 / 17

Organizations

Research & Development (125)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Boehringer IngelheimFor profit15413951998
NovartisFor profit343252007
GlaxoSmithKlineFor profit242332003
PfizerFor profit23032006
AstraZenecaFor profit121142007
Pearl TherapeuticsFor profit8822009
ChiesiFor profit6532010
University of DundeeAcademic/Hospital6612006
3MFor profit5512015
Orion CorporationFor profit5522018
ParexelFor profit4022015
SunovionFor profit4432006
University of SaskatchewanAcademic/Hospital4312007
Fudan UniversityAcademic/Hospital3322010
Guangzhou Medical UniversityAcademic/Hospital3322011
Harvard UniversityAcademic/Hospital3222008
Henan University of Traditional Chinese MedicineAcademic/Hospital3312017
Jiangsu Chia-tai Tianqing Pharmaceutical Co.,LtdFor profit3312024
NeuTec PharmaFor profit3312014
QuotientFor profit3012013
125 organizations
Page 1 / 7

Marketing (3)

OrganizationOrg typeRelationshipDate
Boehringer IngelheimFor profitNDA2Jan 30, 2004
Boehringer IngelheimFor profitNDAJan 30, 2004
LupinFor profitMKTGJun 20, 2023