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Darifenacin | CAS No: 133099-04-4 | GMP-certified suppliers
A medication that treats overactive bladder by reducing urinary urgency, frequency, and urge incontinence, supplied as a GMP-compliant active pharmaceutical ingredient for formulation use.
Therapeutic categories
Primary indications
- For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency
Product Snapshot
- Darifenacin is available as an oral extended release film-coated tablet and standard tablet formulations
- It is primarily indicated for the treatment of overactive bladder symptoms including urge urinary incontinence, urgency, and frequency
- The product is approved for use in key regulatory markets including the US, Canada, and the European Union
Clinical Overview
Pharmacologically, darifenacin functions as a competitive antagonist at muscarinic acetylcholine receptors, exhibiting pronounced selectivity for the M3 receptor subtype. In vitro binding studies demonstrate darifenacin has a 9- to 12-fold higher affinity for M3 receptors compared to M1 and M5 receptors, and a 59-fold greater affinity relative to M2 and M4 receptors. The M3 receptor subtype mediates contraction of bladder smooth muscle, as well as salivary gland secretion and iris sphincter control. By selectively blocking M3 receptors, darifenacin reduces involuntary bladder contractions, thereby diminishing urinary urgency and frequency. However, the clinical significance of its M3 selectivity compared to non-selective antimuscarinics remains unclear.
The mechanism of action centers on antagonism of M3 muscarinic receptors in the bladder, modulating cholinergic signaling that drives detrusor muscle contraction. Common adverse effects attributable to peripheral M3 receptor blockade include dry mouth and constipation, with potential visual disturbances linked to iris sphincter involvement. Importantly, darifenacin is contraindicated in patients with urinary retention due to its mechanism reducing bladder contractility.
Darifenacin undergoes hepatic metabolism primarily via cytochrome P450 isoenzymes CYP2D6 and CYP3A4, serving as both a substrate and moderate inhibitor of CYP2D6. This pharmacokinetic profile necessitates consideration of potential drug-drug interactions when coadministered with other CYP2D6 and CYP3A4 substrates or inhibitors.
From a sourcing and quality perspective, procurement of darifenacin API demands adherence to stringent Good Manufacturing Practices (GMP) to ensure consistent purity, potency, and absence of isomeric impurities. Analytical methods must reliably characterize the diphenylmethane structure, and robust control of raw materials and intermediates is critical to maintaining product integrity for pharmaceutical formulation.
Identification & chemistry
| Generic name | Darifenacin |
|---|---|
| Molecule type | Small molecule |
| CAS | 133099-04-4 |
| UNII | APG9819VLM |
| DrugBank ID | DB00496 |
Pharmacology
| Summary | Darifenacin is a competitive antagonist with high selectivity for muscarinic M3 receptors, which mediate smooth muscle contraction in the bladder and gastrointestinal tract, as well as salivary secretion and iris sphincter function. By inhibiting M3 receptor activity, darifenacin reduces cholinergically induced bladder contractions associated with overactive bladder symptoms. The compound exhibits significantly lower affinity for other muscarinic receptor subtypes (M1, M2, M4, M5). |
|---|---|
| Mechanism of action | Darifenacin selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function. |
| Pharmacodynamics | Darifenacin is a competitive muscarinic receptor antagonist. <i>In vitro</i> studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs. |
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 | The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively. |
|---|---|
| Half-life | The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours. |
| Protein binding | Darifenacin is approximately 98% bound to plasma proteins (primarily to alpha-1-acid-glycoprotein). |
| Metabolism | Hepatic. Primarily mediated by the cytochrome P450 enzymes CYP2D6 and CYP3A4. |
| Volume of distribution | * 163 L |
| Clearance | * 40 L/h [extensive metabolizers] * 32 L/h [poor metabolizers] |
Formulation & handling
- Darifenacin is a small molecule drug formulated for oral administration primarily as extended-release film-coated tablets.
- Due to its low water solubility and high lipophilicity (LogP 4.54), formulation should ensure adequate bioavailability.
- Absorption is not affected by food, allowing flexible dosing relative to meals.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is in a mature market phase in the United States following patent expirations between 2015 and 2016, while in Canada patent protections concluded as recently as 2022. The product is marketed in Canada, the US, and the EU, where market dynamics may vary based on regional patent statuses. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Darifenacin is primarily manufactured by originator companies such as Novartis, with packaging handled by multiple firms including Novartis AG and Pfizer Inc. Branded products are available across the US, EU, and Canadian markets, reflecting a global presence. Patent expiration dates ranging from 2015 to 2022 indicate that the drug is subject to existing or imminent generic competition in key regions. |
|---|
Safety
| Toxicity | Overdosage can potentially result in severe central anticholinergic effects. |
|---|
- Potential for severe central anticholinergic toxicity in cases of overdosage
- Handle with appropriate protective equipment to avoid exposure due to systemic anticholinergic effects
- Store under recommended conditions to maintain compound stability and minimize degradation-related hazards
Darifenacin 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.
Darifenacin (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.
Darifenacin API manufacturers & distributors
Compare qualified Darifenacin API suppliers worldwide. We currently have 8 companies offering Darifenacin API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Dalian Wista Pharma Co Lt... | Producer | China | China | CoA | 16 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, WC | 98 products |
| MSN Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 31 products |
| Mylan | Producer | India | India | CoA, GMP, WC | 201 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
When sending a request, specify which Darifenacin 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 Darifenacin 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.
