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Tolterodine | CAS No: 124937-51-5 | GMP-certified suppliers
A medication that treats overactive bladder by reducing symptoms of urinary frequency, urgency, and urge incontinence to improve patients’ bladder control.
Therapeutic categories
Primary indications
- For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence)
Product Snapshot
- Tolterodine is available as oral tablets and capsules, including extended-release and film-coated formulations
- It is primarily indicated for the treatment of overactive bladder symptoms such as urinary frequency, urgency, and urge incontinence
- The product is approved in key regulatory markets including the United States and Canada
Clinical Overview
Pharmacodynamically, tolterodine functions as a competitive antagonist at muscarinic receptors, specifically targeting the M2 and M3 subtypes that are predominantly involved in mediating bladder contraction and salivation. The inhibition of these receptors reduces detrusor muscle overactivity, leading to decreased bladder contractions and detrusor pressure, as well as an increase in residual urine volume due to incomplete bladder emptying.
After oral administration, tolterodine undergoes extensive hepatic metabolism primarily via cytochrome P450 enzymes, resulting in the formation of the active 5-hydroxymethyl metabolite. This metabolite exhibits antimuscarinic activity comparable to the parent compound and significantly contributes to the overall therapeutic effect. Both tolterodine and its metabolite demonstrate high specificity for muscarinic receptors, with minimal off-target interactions, reducing the potential for unintended pharmacological effects.
Key pharmacokinetic considerations include metabolism through multiple CYP enzymes, including CYP2D6 and CYP3A4 isoforms, which may affect drug-drug interaction profiles and interindividual variability in exposure. Excretion occurs mainly via the renal route. Due to its anticholinergic mechanism, tolterodine may exhibit safety considerations such as dry mouth, constipation, blurred vision, and potential cardiovascular effects including tachycardia and QT interval prolongation, warranting cautious use in patients with relevant preexisting conditions.
Tolterodine is marketed under several brand names globally and is widely utilized in urological practice for symptom management in overactive bladder. When sourcing tolterodine API, attention should be given to stringent quality standards including purity, enantiomeric composition, and compliance with regulatory guidelines. Suppliers should provide full characterization data and demonstrate control over potential impurities and residual solvents consistent with pharmacopeial and ICH standards to ensure suitability for pharmaceutical formulation.
Identification & chemistry
| Generic name | Tolterodine |
|---|---|
| Molecule type | Small molecule |
| CAS | 124937-51-5 |
| UNII | WHE7A56U7K |
| DrugBank ID | DB01036 |
Pharmacology
| Summary | Tolterodine and its active metabolite act as competitive antagonists at muscarinic acetylcholine receptors (M1–M5), primarily targeting receptors involved in bladder contraction. This antagonism reduces detrusor muscle pressure and bladder contractility, leading to decreased urinary urgency and frequency. The pharmacodynamic effects are mediated through high receptor specificity, with minimal off-target activity. |
|---|---|
| Mechanism of action | Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder. |
| Pharmacodynamics | Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Muscarinic acetylcholine receptor M3 | Humans | antagonist |
| Muscarinic acetylcholine receptor M2 | Humans | antagonist |
| Muscarinic acetylcholine receptor M5 | Humans | antagonist |
ADME / PK
| Half-life | 1.9-3.7 hours |
|---|---|
| Protein binding | Approximately 96.3%. |
| Route of elimination | Following administration of a 5-mg oral dose of 14C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in urine and 17% was recovered in feces in 7 days. |
| Volume of distribution | * 113 ± 26.7 L |
Formulation & handling
- Tolterodine is a small molecule with oral administration typically formulated as immediate or extended-release tablets and capsules.
- Due to its low water solubility and high LogP, formulation strategies should address dissolution and bioavailability challenges.
- Administration with food is recommended to optimize absorption and minimize gastrointestinal side effects.
Regulatory status
| Lifecycle | The API is approaching full market maturity in the United States and Canada following the expiration of key patents between 2012 and 2020, allowing for broader generic competition in these markets. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Tolterodine is supplied by multiple packagers serving primarily the US and Canadian markets, with branded products such as Detrol present in these regions. The originator companies have established a global presence mainly in North America. Several US and Canadian patents have recently expired or will expire shortly, indicating the presence of existing or imminent generic competition. |
|---|
Tolterodine is a type of Urological spasmolytics
Urological spasmolytics belong to the pharmaceutical API subcategory designed to address conditions related to urinary system spasms and discomfort. These medications work by relaxing the smooth muscles in the urinary tract, helping to alleviate symptoms such as bladder spasms and urinary urgency.
Urological spasmolytics are commonly prescribed for various urological disorders, including urinary incontinence, interstitial cystitis, and overactive bladder. The active ingredients in these APIs target specific receptors in the urinary system, blocking the signaling pathways that trigger muscle contractions.
By reducing muscle spasms and promoting relaxation, urological spasmolytics help relieve symptoms associated with these conditions. This includes reducing the frequency of urination, decreasing urinary urgency, and alleviating the discomfort caused by bladder spasms.
It is important to note that urological spasmolytics are typically available in different formulations, including oral tablets, extended-release capsules, and transdermal patches. The choice of formulation depends on the specific needs and preferences of the patient, as well as the severity of the condition being treated.
Before starting any urological spasmolytic medication, it is crucial to consult a healthcare professional. They will evaluate the individual's medical history, perform a thorough examination, and recommend the appropriate dosage and duration of treatment.
Overall, urological spasmolytics play a significant role in managing urological disorders characterized by muscle spasms in the urinary tract. These pharmaceutical APIs offer relief from symptoms and enhance the quality of life for individuals suffering from such conditions.
Tolterodine (Urological spasmolytics), classified under Genitourinary Agents
Genitourinary agents are a category of pharmaceutical active ingredients (APIs) that are specifically designed to target and treat disorders related to the genitourinary system. The genitourinary system encompasses the organs and structures involved in the production, storage, and elimination of urine, as well as the reproductive organs.
These APIs play a crucial role in the treatment of various genitourinary conditions, including urinary tract infections (UTIs), erectile dysfunction, urinary incontinence, benign prostatic hyperplasia (BPH), and other related disorders. They exert their therapeutic effects by interacting with specific receptors or enzymes in the genitourinary system, regulating physiological processes, and restoring normal function.
Some commonly used genitourinary agents include alpha-blockers, which relax the smooth muscles in the prostate and bladder neck, improving urine flow in patients with BPH. Additionally, phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are widely prescribed for erectile dysfunction, as they enhance blood flow to the penile tissues, facilitating erection.
These APIs are typically formulated into various dosage forms, such as tablets, capsules, creams, gels, or injections, allowing for convenient administration to patients. The development and production of genitourinary agents involve stringent quality control measures and compliance with regulatory guidelines to ensure safety, efficacy, and consistent product performance.
In summary, genitourinary agents form a crucial category of pharmaceutical APIs used to treat a range of disorders affecting the genitourinary system. Their targeted mechanisms of action and diverse dosage forms make them valuable tools in improving genitourinary health and enhancing patients' quality of life.
Tolterodine API manufacturers & distributors
Compare qualified Tolterodine API suppliers worldwide. We currently have 11 companies offering Tolterodine 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 |
|---|---|---|---|---|---|
| Alkem Labs. | Producer | India | India | CoA, USDMF | 22 products |
| Amino Chemicals | Producer | Malta | Malta | CoA, USDMF | 20 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Erregierre | Producer | Italy | Italy | CoA, USDMF | 44 products |
| Harman Finochem | Producer | India | India | CoA, GMP, WC | 34 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| Lupin | Producer | India | India | CoA, GMP, USDMF, WC | 155 products |
| Natco Pharma | Producer | India | India | CoA, FDA, GMP, USDMF, WC | 40 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CEP, CoA, FDA, GMP, MSDS | 64 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
When sending a request, specify which Tolterodine 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 Tolterodine 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.
