Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Entacapone API Manufacturers & Suppliers
13 verified results
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Commercial-scale Suppliers
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Entacapone | CAS No: 130929-57-6 | GMP-certified suppliers
A medication that supports idiopathic Parkinson’s disease management by helping reduce end‑of‑dose wearing‑off symptoms in patients already receiving established dopaminergic therapy.
Therapeutic categories
Primary indications
- Used as an adjunct to levodopa / carbidopa in the symptomatic treatment of patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-dose "wearing-off"
Product Snapshot
- Oral small‑molecule product supplied as coated and film‑coated tablets
- Used as an adjunct agent to levodopa/carbidopa for management of end‑of‑dose motor fluctuations in idiopathic Parkinson’s disease
- Approved in the US, EU, and Canada, with additional investigational listings in some regions
Clinical Overview
Entacapone acts pharmacologically by inhibiting COMT in peripheral tissues. COMT is widely distributed, with highest activity in liver and kidney and measurable activity in multiple organ systems and glial cells. The enzyme catalyzes methylation of catechol-containing substrates, including catecholamines and L‑dopa. When a decarboxylase inhibitor is present, COMT becomes the predominant metabolic pathway for levodopa, converting it to 3‑O‑methyldopa. Inhibition of COMT reduces peripheral levodopa clearance, increasing levodopa exposure and producing more sustained plasma concentrations. This allows more continuous dopaminergic stimulation in the central nervous system.
The onset and duration of entacapone’s activity reflect its reversible peripheral inhibition, with no direct central pharmacodynamic effect. The compound is minimally active on its own and does not improve symptoms without concurrent levodopa therapy. It is structurally related to tolcapone but does not share the hepatotoxicity concerns associated with that agent.
Absorption is rapid, and entacapone undergoes extensive hepatic metabolism, primarily via glucuronidation pathways. It is highly protein bound and has a relatively short elimination half-life, supporting administration with each levodopa dose. Renal elimination of metabolites is the primary excretion route.
Safety considerations include dyskinesia potentiation due to enhanced levodopa exposure, gastrointestinal disturbances, urine discoloration, and orthostatic symptoms. No significant hepatotoxicity signal has been associated with entacapone, but routine clinical monitoring of the overall levodopa regimen remains essential.
Entacapone is widely available in combination levodopa/carbidopa products used in various regions. For API procurement, sourcing should emphasize validated manufacturing routes, control of nitrocatechol-related impurities, and compliance with regional pharmacopoeial specifications to support formulation and regulatory submissions.
Identification & chemistry
| Generic name | Entacapone |
|---|---|
| Molecule type | Small molecule |
| CAS | 130929-57-6 |
| UNII | 4975G9NM6T |
| DrugBank ID | DB00494 |
Pharmacology
| Summary | Entacapone is a selective, reversible inhibitor of catechol‑O‑methyltransferase (COMT), a major enzyme responsible for metabolizing levodopa when a decarboxylase inhibitor is present. By limiting peripheral COMT activity, it increases and prolongs circulating levodopa concentrations, supporting more consistent dopaminergic stimulation in the central nervous system. Its pharmacology is centered on modulating levodopa metabolism to address motor fluctuation patterns in Parkinson’s disease. |
|---|---|
| Mechanism of action | The mechanism of action of entacapone is believed to be through its ability to inhibit COMT in peripheral tissues, altering the plasma pharmacokinetics of levodopa. When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to a greater reduction in the manifestations of parkinsonian syndrome. |
| Pharmacodynamics | Entacapone is structurally and pharmacologically related to tolcapone, but unlike tolcapone, is not associated with hepatotoxicity. Entacapone is used in the treatment of Parkinson’s disease as an adjunct to levodopa/carbidopa therapy. Entacapone selectively and reversiblly inhibits catechol-O-methyltransferase (COMT). In mammals, COMT is distributed throughout various organs with the highest activities in the liver and kidney. COMT also occurs in the heart, lung, smooth and skeletal muscles, intestinal tract, reproductive organs, various glands, adipose tissue, skin, blood cells and neuronal tissues, especially in glial cells. COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include dopa, catecholamines (dopamine, norepinephrine, and epinephrine) and their hydroxylated metabolites. The function of COMT is the elimination of biologically active catechols and some other hydroxylated metabolites. COMT is responsible for the elimination of biologically active catechols and some other hydroxylated metabolites. In the presence of a decarboxylase inhibitor, COMT becomes the major metabolizing enzyme for levodopa, catalyzing the it to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD) in the brain and periphery. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Catechol O-methyltransferase | Humans | inhibitor |
ADME / PK
| Absorption | Entacapone is rapidly absorbed (approximately 1 hour). The absolute bioavailability following oral administration is 35%. |
|---|---|
| Half-life | 0.4-0.7 hour |
| Protein binding | 98% (bind to serum albumin) |
| Metabolism | Metabolized via isomerization to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer. |
| Route of elimination | Entacapone is almost completely metabolized prior to excretion, with only a very small amount (0.2% of dose) found unchanged in urine. As only about 10% of the entacapone dose is excreted in urine as parent compound and conjugated glucuronide, biliary excretion appears to be the major route of excretion of this drug. |
| Volume of distribution | * 20 L |
| Clearance | * 850 mL/min |
Formulation & handling
- Oral small‑molecule API with low aqueous solubility, typically formulated as film‑coated tablets to aid manufacturability and handling.
- Moderate LogP and poor solubility may require particle‑size control or solid‑state optimization to ensure consistent dissolution in oral formulations.
- Absorption is not food‑dependent, allowing flexible administration without specific food‑related formulation constraints.
Regulatory status
| Lifecycle | Most core U.S. and Canadian patents expired between 2010 and 2020, indicating the API is well past its primary exclusivity period. With products marketed in Canada, the US, and the EU, the API is in a mature, broadly generic market phase. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Entacapone is produced by a single originator manufacturer, with multiple third‑party packagers supporting downstream supply activities. Branded and combination products are available across the US, EU, and Canada, indicating established global market coverage. All listed patents have expired, suggesting that generic manufacturing is already present or readily feasible in most markets. |
|---|
Safety
| Toxicity | Side effect include increase the occurrence of orthostatic hypotension, severe rhabdomyolysis, dyskinesia, hallucinations, hyperkinesia, hypokinesia, dizziness, fatigu,e gastrointestinal effects including abdominal pain constipation diarrhea nausea |
|---|
- Handle with controls that account for CNS‑active effects
- Exposure may be associated with dyskinesia, hallucinations, hyper/hypokinesia, dizziness, and fatigue
- Implement measures to limit musculoskeletal and renal burden from accidental exposure, as severe rhabdomyolysis has been reported
Entacapone is a type of COMT inhibitors
COMT inhibitors, which stand for Catechol-O-methyltransferase inhibitors, are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various medical conditions. These inhibitors specifically target the enzyme catechol-O-methyltransferase, which plays a crucial role in the breakdown of certain neurotransmitters, such as dopamine, epinephrine, and norepinephrine.
The primary purpose of COMT inhibitors is to inhibit the activity of the COMT enzyme, thereby increasing the levels of these neurotransmitters in the brain and other parts of the body. By doing so, these inhibitors offer potential therapeutic benefits in the management of several disorders, including Parkinson's disease, psychiatric disorders, and pain syndromes.
The use of COMT inhibitors in the treatment of Parkinson's disease is particularly significant. These inhibitors, often used in combination with other medications like levodopa, help improve motor symptoms such as tremors, muscle rigidity, and bradykinesia. By prolonging the effects of levodopa, COMT inhibitors can enhance the therapeutic response and extend the "on" time for patients, reducing the fluctuations in motor control.
Furthermore, COMT inhibitors have shown promise in the field of psychiatry. By modulating the levels of neurotransmitters like dopamine, COMT inhibitors can help alleviate symptoms associated with mental health conditions, such as depression and schizophrenia. These inhibitors have also been explored for their potential analgesic effects in pain management, offering an alternative option for patients who do not respond well to conventional therapies.
In conclusion, COMT inhibitors are a vital subcategory of pharmaceutical APIs with significant therapeutic potential. Their ability to modulate neurotransmitter levels makes them valuable in the treatment of Parkinson's disease, psychiatric disorders, and pain syndromes. Ongoing research and development in this field aim to further enhance the efficacy and safety profile of these inhibitors, expanding their application in various medical domains.
Entacapone (COMT inhibitors), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Entacapone API manufacturers & distributors
Compare qualified Entacapone API suppliers worldwide. We currently have 13 companies offering Entacapone API, with manufacturing taking place in 8 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 |
|---|---|---|---|---|---|
| Divis Labs. | Producer | India | India | CoA, FDA, GMP, ISO9001, Other | 47 products |
| Erregierre | Producer | Italy | Italy | CoA, GMP, USDMF | 44 products |
| Fermion | Producer | Finland | Finland | CoA, USDMF | 29 products |
| HEC Pharm | Producer | Germany | Germany | CEP, CoA, FDA, GMP, USDMF | 31 products |
| Hetero Labs | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 90 products |
| Moehs | Producer | Spain | Spain | CoA, EDMF/ASMF, GMP, USDMF | 50 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF, WC | 44 products |
| Signa | Producer | Mexico | Mexico | CEP, CoA, FDA | 42 products |
| Standard C&P | Producer | Taiwan | Taiwan | CoA, USDMF | 4 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Suryakala Laboratories Pv... | Producer | India | India | CoA, ISO9001 | 6 products |
| USV | Producer | India | India | CoA, FDA, GMP, WC | 35 products |
When sending a request, specify which Entacapone 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 Entacapone 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 Entacapone API
Sourcing
What matters most when sourcing GMP-grade Entacapone?
Which documents are typically required when sourcing Entacapone API?
Which manufacturers are known to produce Entacapone API?
How can I request quotes for Entacapone API from GMP suppliers?
Is a GMP audit report available for Entacapone manufacturers?
How many suppliers offer Entacapone API on Pharmaoffer?
Which countries are known to manufacture Entacapone API?
Which certifications do suppliers of Entacapone usually hold?
Technical
What is Entacapone (CAS 130929-57-6) used for?
Which therapeutic class does Entacapone fall into?
What conditions is Entacapone mainly prescribed for?
How does Entacapone work?
What should someone know about the safety or toxicity profile of Entacapone?
What are important formulation and handling considerations for Entacapone as an API?
Is Entacapone a small molecule?
Are there special stability concerns for oral Entacapone?
Regulatory
Where is Entacapone approved or in use globally?
What’s the regulatory and patent landscape for Entacapone right now?
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Entacapone procurement?
Is Entacapone included in the PRO Data Insights coverage?
Where can I access the API market report for Entacapone?
