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Tiotropium | CAS No: 186691-13-4 | GMP-certified suppliers
A medication that supports maintenance treatment of COPD by reducing bronchospasm and preventing exacerbations, while also providing long‑term control of asthma in eligible patients.
Therapeutic categories
Primary indications
- Tiotropium powder for inhalation is indicated for the maintenance of bronchospasm in COPD and to prevent exacerbations of COPD
- A combination tiotropium and [olodaterol] metered inhalation spray is indicated for maintenance of COPD
- A tiotropium inhalation spray is indicated for the maintenance of bronchospasm in COPD, to prevent exacerbations of COPD, and to treat asthma in patients 12 or more years old
- A tiotropium metered inhalation spray is indicated for the maintenance of bronchospasm in COPD, to prevent exacerbations of COPD, and to treat asthma in patients 6 or more years old
Product Snapshot
- Tiotropium is an inhaled small-molecule anticholinergic supplied mainly as dry powder or metered-dose inhalation solutions
- It is used for maintenance management of bronchospasm in COPD, prevention of COPD exacerbations, and maintenance treatment of asthma
- It is approved in the US and Canada for these indications
Clinical Overview
Tiotropium is classified as a morpholine derivative and belongs to the broader group of anticholinergic and bronchodilator agents. It exhibits functional selectivity for muscarinic receptors located in the airways, particularly M3 receptors on airway smooth muscle. Antagonism of M1 to M5 receptors reduces cholinergic tone, with inhibition of M3 driving sustained smooth muscle relaxation and bronchodilation. Compared with shorter‑acting antimuscarinics, its kinetic profile supports once‑daily dosing.
Pharmacodynamic activity persists for more than 24 hours due to slow dissociation from M3 receptors. The drug shows a wide therapeutic index, and clinically significant overdose is uncommon at exposures exceeding standard therapeutic levels. As an inhaled agent, systemic pharmacological effects are generally limited but may include anticholinergic responses consistent with its mechanism.
Absorption following inhalation is partial, with most of the dose deposited in the oropharynx and swallowed. Tiotropium undergoes minimal hepatic metabolism and is primarily excreted unchanged in the urine. Renal clearance is an important determinant of systemic exposure, and reduced renal function can increase plasma concentrations. The compound is a substrate of CYP2D6 and CYP3A isoenzymes, although these pathways contribute minimally to overall elimination.
Safety considerations include potential anticholinergic effects such as dry mouth and, less commonly, urinary retention or tachycardia, especially in susceptible populations. Long‑term tolerability in approved indications is well established.
For API procurement, sourcing should ensure control of stereochemistry, consistent particle‑size distribution for inhalation use, and compliance with pharmacopeial specifications and regional GMP requirements to support product quality and regulatory acceptance.
Identification & chemistry
| Generic name | Tiotropium |
|---|---|
| Molecule type | Small molecule |
| CAS | 186691-13-4 |
| UNII | 0EB439235F |
| DrugBank ID | DB01409 |
Pharmacology
| Summary | Tiotropium is a long‑acting antimuscarinic agent that binds muscarinic receptors M1 through M5, with therapeutic bronchodilation primarily driven by inhibition of M3 receptors in airway smooth muscle. This blockade reduces cholinergic tone, leading to sustained airway smooth muscle relaxation. Its pharmacodynamic profile features prolonged receptor dissociation and effects lasting more than 24 hours. |
|---|---|
| Mechanism of action | Tiotropium is an antagonist of muscarinic receptors M<sub>1</sub> to M<sub>5</sub>.Inhibition of the M<sub>3</sub> receptor in the smooth muscle of the lungs leads to relaxation of smooth muscle and bronchodilation. |
| Pharmacodynamics | Tiotropium is a long acting antimuscarinic that causes bronchodilation.The effects of tiotropium last over 24 hours and there is a wide therapeutic index as overdoses are uncommon even at doses well above the recommended maximum. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Muscarinic acetylcholine receptor M3 | Humans | antagonist |
| Muscarinic acetylcholine receptor M1 | Humans | antagonist |
| Muscarinic acetylcholine receptor M2 | Humans | antagonist |
ADME / PK
| Absorption | 33% of an inhaled solution reaches systemic circulation, while oral solutions have a bioavailability of 2-3%.A dry powder for inhalation is 19.5% bioavailable.Tiotropium metered spray for inhalation reaches a maximum concentration in 5-7 minutes. |
|---|---|
| Half-life | The terminal half life of tiotropium is 24 hours in patients with COPD and 44 hours in patients with asthma. |
| Protein binding | Tiotropium is 72% protein bound in plasma. |
| Metabolism | Tiotropium is not heavily metabolized in the body.74% of an intravenous dose is excreted in the urine as unchanged drug.Tiotropium is nonenzymatically cleaved to the inactive metabolites N-methylscopine and dithienylglycolic acid._In vitro_ experiments show cytochrome P-450 dependent oxidation and glutathione conjugation to further metabolites. |
| Route of elimination | 74% of intravenous tiotropium was excreted unchanged in urine.14% of a dry powder inhalation dose was excreted unchanged in the urine.24 hour urinary excretion after 21 days of 5µg once daily inhalation in patients with COPD is 18.6% and in patients with asthma is 12.8%. |
| Volume of distribution | The volume of distribution of tiotropium is 32L/kg. |
| Clearance | The total clearance of tiotropium is 880mL/min in healthy subjects receiving 5µg daily.The renal clearance of tiotropium was 669mL/min. Patients <65 years old demonstrated a clearance of 365mL/min while patients ≥65 demonstrated a clearance of 271mL/min.This decreased clearance is not associated with increased AUC or C<sub>max</sub>. |
Formulation & handling
- Primarily formulated for inhalation; solid-state API is incorporated into dry‑powder, capsule-inhaler, and solution/aerosol systems requiring tight control of particle size and aerodynamic performance.
- Highly hydrophilic (logP −1.8) small molecule suited to aqueous inhalation solutions, with attention to pH control to maintain solubility and chemical stability.
- Oral forms exist but absorption is limited; no significant food‑related constraints, and handling focuses mainly on moisture control for dry powders.
Regulatory status
| Lifecycle | Most key patent protections in Canada and the United States have expired, with the final U.S. patent extending coverage to 2026. The API is therefore approaching late‑lifecycle status, with both markets positioned for increasing generic competition as remaining exclusivities conclude. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Tiotropium is supplied primarily by the originator manufacturer, with additional distribution handled by several packagers in North America. Branded products such as Spiriva and related formulations are established in the US and Canadian markets. With key patents expiring between 2010 and 2026, portions of the product landscape already allow for generic competition, with broader entry expected as remaining protections lapse. |
|---|
Safety
| Toxicity | Symptoms of overdose include altered mental status, tremors, abdominal pain, and severe constipation.However, doses of up to 282µg did not lead to systemic anticholinergic effects in a trial of 6 patients. In case of overdose, stop tiotropium and being symptomatic and supportive therapy. |
|---|
- Overexposure may elicit central and peripheral anticholinergic manifestations, including altered mental status, tremors, abdominal discomfort, and severe constipation
- Clinical data indicate that single doses up to 282 µg did not produce systemic anticholinergic effects in a small cohort, suggesting limited systemic uptake at typical exposure levels
- Handling controls should account for the compound’s anticholinergic activity profile to minimize inadvertent high‑level exposure
Tiotropium is a type of Anticholinergics/Parasympathemimetics
Anticholinergics/Parasympathomimetics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These compounds exhibit specific pharmacological actions by targeting the cholinergic system in the body.
Anticholinergics are drugs that block the action of acetylcholine, a neurotransmitter that regulates various bodily functions. By inhibiting the activity of acetylcholine, anticholinergics can have diverse therapeutic effects, including reducing muscle spasms, decreasing gastrointestinal motility, and alleviating symptoms associated with certain respiratory conditions.
On the other hand, parasympathomimetics, also known as cholinomimetics, mimic the action of acetylcholine by stimulating cholinergic receptors. These compounds enhance the parasympathetic nervous system, which is responsible for the "rest and digest" functions of the body. Parasympathomimetics are commonly used to treat conditions such as glaucoma, urinary retention, and Alzheimer's disease.
The use of anticholinergics/parasympathomimetics requires careful consideration and medical supervision due to their potential side effects, which can include dry mouth, blurred vision, urinary retention, constipation, and cognitive impairment. These medications are available in various forms, including tablets, capsules, patches, and inhalers, and their dosage is determined by the specific medical condition being treated.
Overall, anticholinergics/parasympathomimetics play a vital role in modern medicine, providing targeted therapeutic effects by modulating the cholinergic system. Their usage has significantly improved patient outcomes in various medical conditions and continues to be an important category of pharmaceutical APIs.
Tiotropium (Anticholinergics/Parasympathemimetics), classified under Autonomic Nervous System Agents
Autonomic Nervous System Agents are a crucial category of pharmaceutical active ingredients (APIs) that target the autonomic nervous system (ANS). The ANS plays a vital role in regulating essential bodily functions such as heart rate, blood pressure, digestion, and respiratory rate. This category of pharmaceutical APIs encompasses a wide range of drugs designed to modulate the activity of the ANS.
One subcategory within Autonomic Nervous System Agents is the Sympathomimetic agents, which mimic the effects of the sympathetic nervous system. These drugs are often used to treat conditions such as asthma, nasal congestion, and hypotension by stimulating specific adrenergic receptors.
Conversely, Sympatholytic agents act to inhibit or block the sympathetic nervous system. They are employed to treat hypertension, anxiety, and certain cardiac conditions by reducing sympathetic activity.
Another subcategory is Parasympathomimetic agents, which mimic the effects of the parasympathetic nervous system. These drugs are commonly used to treat glaucoma, urinary retention, and certain gastrointestinal disorders by stimulating cholinergic receptors.
Parasympatholytic agents, on the other hand, act to block the parasympathetic nervous system. They find applications in the treatment of conditions such as overactive bladder and irritable bowel syndrome by inhibiting cholinergic receptors.
The Autonomic Nervous System Agents API category includes various drugs with distinct mechanisms of action that enable healthcare professionals to fine-tune the balance of the autonomic nervous system. By targeting specific receptors and pathways, these pharmaceutical APIs provide valuable therapeutic options for managing a wide range of medical conditions related to autonomic dysfunction.
Tiotropium API manufacturers & distributors
Compare qualified Tiotropium API suppliers worldwide. We currently have 9 companies offering Tiotropium API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Boehringer Ingelheim | Producer | Germany | Unknown | CEP, CoA, FDA, GMP, USDMF | 35 products |
| Cerbios-Pharma | Producer | Switzerland | Switzerland | CoA, USDMF | 9 products |
| Cipla | Producer | India | Unknown | CEP, CoA | 164 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 products |
| Industriale Chimica | Producer | Italy | Unknown | CoA, USDMF | 33 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA | 757 products |
| Vamsi Labs | Producer | India | India | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC, WHO-GMP | 29 products |
When sending a request, specify which Tiotropium API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Tiotropium API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Tiotropium API
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Regulatory
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