tiotropium
Trade name: spiriva
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
Earliest trial started Feb 1, 1998 (NCT02172326)
Timeline
1990s
- Jan 1, 1998
Boehringer Ingelheim — Earliest Phase 1 Sponsor(trial)
- Jan 1, 1998
Boehringer Ingelheim — Earliest Phase 2 Sponsor(trial)
- Jan 1, 1998
Boehringer Ingelheim — Earliest Phase 3 Sponsor(trial)
2000s
- Jan 30, 2004
Boehringer Ingelheim — Earliest FDA Approval
- Jan 30, 2004
Boehringer Ingelheim — NDA Secondary Org
- Jan 30, 2004
Boehringer Ingelheim — NDA Organization
2020s
- Jun 20, 2023
Lupin — Marketing Organization
Indications
Studied for
- Airway Management · Phase 4
- Airway Obstruction · Phase 4
- Asthma · Phase 4
- Bronchiectasis · Phase 4
- Bronchiolitis · Phase 4
- Bronchitis · Phase 4
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Cystic Fibrosis · Phase 3
- Dyspnea · Phase 2
- Emphysema · Phase 4
- Exercise · Phase 4
- Healthy Volunteers · Phase 4
- Lung Diseases, Obstructive · Phase 3
- Pulmonary Emphysema · Phase 4
- Renal Insufficiency · Phase 1
- Respiratory Sounds · Phase 4
- Spinal Cord Injuries · Phase 2
Mechanism of action
- Muscarinic acetylcholine receptor M3ANTAGONIST
CHRM3 antagonist
Indicated for COPD, M3 likely responsible
Combination products
stiolto respimat
with olodaterol
Also known as spiolto respimat
Approval history
- approvedJan 30, 2004
Chemistry & pharmacology
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
- ChEMBLCHEMBL1900528 ↗
- WikipediaTiotropium bromide ↗
- NCATS0EB439235F ↗
- ChEMBLCHEMBL4297109 ↗
- ChEMBLCHEMBL1182657 ↗
- ChEMBLCHEMBL1697846 ↗
- ChEMBLCHEMBL3545181 ↗
- ChEMBLCHEMBL1739767 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07267130 | Phase 1 | Nov 25, 2025 | Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd |
| NCT06487416 | Phase 1 | Jun 10, 2024 | Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd |
| NCT06326671 | Phase 1 | Feb 28, 2024 | Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd |
| NCT05838703 | Phase 2 | May 1, 2023 | Duke University |
| NCT06254664 | Phase 1 | Oct 3, 2022 | Exeltis, Iberica Co. Ltd. |
| NCT05986591 | Phase 3 | Aug 17, 2022 | Exeltis, Iberica Co. Ltd. |
| NCT05246046 | Phase 1 | Feb 16, 2022 | Orion Corporation |
| NCT05165485 | Phase 4 | Dec 31, 2021 | Mylan, Theravance |
| NCT05161156 | Phase 3 | Dec 18, 2021 | Phargentis SA |
| NCT05113615 | Phase 4 | Nov 30, 2021 | University of Saskatchewan |
| NCT04994574 | N/A | Aug 31, 2021 | Yonsei University |
| NCT04990167 | Phase 2 | Aug 1, 2021 | Nemours Foundation, Thomas Jefferson University |
| NCT04850144 | Phase 1 | Apr 26, 2021 | Orion Corporation |
| NCT05295355 | N/A | Jan 25, 2021 | Boehringer Ingelheim, Guangzhou Medical University |
| NCT04648813 | Phase 4 | Nov 13, 2020 | University of Saskatchewan |
| NCT04780984 | Phase 2 | Nov 1, 2020 | Nephron Pharmaceuticals Corporation, Rho, Inc. |
| NCT04231214 | Phase 4 | Feb 1, 2020 | Boehringer Ingelheim, Fraunhofer |
| NCT04223843 | Phase 4 | Jan 10, 2020 | Boehringer Ingelheim |
| NCT04147572 | N/A | Nov 1, 2019 | Orion Corporation |
| NCT03964207 | Phase 4 | Aug 30, 2019 | Boehringer Ingelheim |
Organizations
Research & Development (125)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Boehringer Ingelheim | For profit | 154 | 139 | 5 | 1998 |
| Novartis | For profit | 34 | 32 | 5 | 2007 |
| GlaxoSmithKline | For profit | 24 | 23 | 3 | 2003 |
| Pfizer | For profit | 23 | 0 | 3 | 2006 |
| AstraZeneca | For profit | 12 | 11 | 4 | 2007 |
| Pearl Therapeutics | For profit | 8 | 8 | 2 | 2009 |
| Chiesi | For profit | 6 | 5 | 3 | 2010 |
| University of Dundee | Academic/Hospital | 6 | 6 | 1 | 2006 |
| 3M | For profit | 5 | 5 | 1 | 2015 |
| Orion Corporation | For profit | 5 | 5 | 2 | 2018 |
| Parexel | For profit | 4 | 0 | 2 | 2015 |
| Sunovion | For profit | 4 | 4 | 3 | 2006 |
| University of Saskatchewan | Academic/Hospital | 4 | 3 | 1 | 2007 |
| Fudan University | Academic/Hospital | 3 | 3 | 2 | 2010 |
| Guangzhou Medical University | Academic/Hospital | 3 | 3 | 2 | 2011 |
| Harvard University | Academic/Hospital | 3 | 2 | 2 | 2008 |
| Henan University of Traditional Chinese Medicine | Academic/Hospital | 3 | 3 | 1 | 2017 |
| Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd | For profit | 3 | 3 | 1 | 2024 |
| NeuTec Pharma | For profit | 3 | 3 | 1 | 2014 |
| Quotient | For profit | 3 | 0 | 1 | 2013 |
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Boehringer Ingelheim | For profit | NDA2 | Jan 30, 2004 |
| Boehringer Ingelheim | For profit | NDA | Jan 30, 2004 |
| Lupin | For profit | MKTG | Jun 20, 2023 |