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Tolcapone | CAS No: 134308-13-7 | GMP-certified suppliers
A medication that supports management of Parkinson’s disease by helping stabilize symptoms in patients experiencing fluctuations despite existing levodopa/carbidopa therapy.
Therapeutic categories
Primary indications
- Used as an adjunct to levodopa/carbidopa therapy for the symptomatic treatment of Parkinson's Disease
- This drug is generally reserved for patients with parkinsonian syndrome receiving levodopa/carbidopa who are experiencing symptom fluctuations and are not responding adequately to or are not candidates for other adjunctive therapies
Product Snapshot
- Oral small‑molecule drug supplied as coated or film‑coated tablets
- Used as an adjunct to levodopa/carbidopa for symptomatic control of Parkinson’s disease in patients with motor fluctuations
- Approved in the US, Canada, and EU, with historical withdrawals or restrictions in certain markets
Clinical Overview
Tolcapone modifies catecholamine metabolism by inhibiting COMT, an enzyme broadly distributed in peripheral tissues and the central nervous system. COMT normally catalyzes methylation of catechol substrates including dopamine, norepinephrine, epinephrine, and dopa. In the presence of a decarboxylase inhibitor such as carbidopa, COMT becomes a major pathway for levodopa conversion to 3‑O‑methyldopa. By inhibiting this route, tolcapone increases plasma levodopa exposure and reduces circulating 3‑O‑methyldopa, which decreases competition for CNS transport and supports more stable central dopaminergic stimulation.
Pharmacodynamic effects include more sustained levodopa levels and potential enhancement of both therapeutic response and levodopa‑related adverse events. Clinical use often requires dose adjustments of levodopa to maintain tolerability.
Tolcapone is orally administered and undergoes hepatic metabolism. It is known to inhibit CYP2C9, although the extent of this inhibition may vary. Renal excretion contributes to elimination. Key safety concerns center on hepatotoxicity, which has led to restricted or withdrawn status in some regions. Liver function monitoring is essential, and treatment is typically limited to patients who demonstrate clear clinical need and can adhere to required safety assessments.
Products containing tolcapone have been marketed under names such as Tasmar in certain jurisdictions, though availability varies due to regional regulatory decisions.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of impurity profiles, validated analytical methods for identity and potency, and robust evidence of compliance with current Good Manufacturing Practice and regional pharmacopoeial requirements.
Identification & chemistry
| Generic name | Tolcapone |
|---|---|
| Molecule type | Small molecule |
| CAS | 134308-13-7 |
| UNII | CIF6334OLY |
| DrugBank ID | DB00323 |
Pharmacology
| Summary | Tolcapone is a selective, reversible inhibitor of catechol‑O‑methyltransferase that reduces peripheral metabolism of levodopa and lowers formation of the competing metabolite 3‑O‑methyldopa. By sustaining plasma levodopa concentrations, it supports more consistent central dopaminergic signaling. Its therapeutic role is as an adjunct to levodopa/carbidopa in Parkinson’s disease to address motor fluctuations related to variable levodopa availability. |
|---|---|
| Mechanism of action | The precise mechanism of action of tolcapone is unknown, but it is believed to be related to its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa, resulting in an increase in plasma levodopa concentrations. The inhibition of COMT also causes a reduction in circulating 3-OMD as a result of decreased peripheral metabolism of levodopa. This may lead to an increase distribution of levodopa into the CNS through the reduction of its competitive substrate, 3-OMD, for transport mechanisms. Sustained levodopa concentrations presumably result in more consistent dopaminergic stimulation, resulting in greater reduction in the manifestations of parkinsonian syndrome. |
| Pharmacodynamics | Tolcapone is a potent, selective, and reversible inhibitor of catechol-O-methyltransferase (COMT). In humans, COMT is distributed throughout various organs. 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, 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 it to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD) in the brain and periphery. When tolcapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that these sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson's disease in patients as well as increased levodopa adverse effects, sometimes requiring a decrease in the dose of levodopa. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Catechol O-methyltransferase | Humans | inhibitor |
ADME / PK
| Absorption | Rapidly absorbed (absolute bioavailability is about 65%) |
|---|---|
| Half-life | 2-3.5 hours |
| Protein binding | > 99.9% (to serum albumin) |
| Metabolism | The main metabolic pathway of tolcapone is glucuronidation |
| Route of elimination | Tolcapone is almost completely metabolized prior to excretion, with only a very small amount (0.5% of dose) found unchanged in urine. The glucuronide conjugate of tolcapone is mainly excreted in the urine but is also excreted in the bile. |
| Volume of distribution | * 9 L |
| Clearance | * 7 L/h |
Formulation & handling
- Solid, lipophilic small molecule with low aqueous solubility, requiring conventional oral tablet technologies to manage dissolution and absorption.
- Absorption may be modestly reduced by proximate food intake, so formulation should not rely on food-dependent dissolution enhancement.
- Chemically stable benzophenone derivative suitable for standard solid‑dose handling, with no peptide- or biologic‑specific storage constraints.
Regulatory status
| Lifecycle | The API’s primary U.S. patents expired in 2012, indicating that it has been off‑patent for more than a decade. With availability across the US, Canada, and the EU, the product is in a mature stage of its lifecycle with established generic presence in these markets. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Tolcapone is supplied by a single originator manufacturer, with several third‑party packagers supporting distribution, indicating a relatively centralized production base. Branded products are present across the US, Canada, and the EU, reflecting established global market availability. All listed US patents have expired, suggesting that generic competition is already possible where regulatory and market conditions permit. |
|---|
Safety
| Toxicity | LD<sub>50</sub> = 1600 mg/kg (Orally in rats) |
|---|
- Oral LD50 of ~1600 mg/kg in rats indicates low acute toxicity, but bulk handling should still minimize ingestion and dust inhalation
- May cause dopaminergic‑related adverse effects (e
- G
Tolcapone 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.
Tolcapone (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.
Tolcapone API manufacturers & distributors
Compare qualified Tolcapone API suppliers worldwide. We currently have 3 companies offering Tolcapone API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Glochem | Producer | India | India | CoA, USDMF | 14 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | India | CoA, GMP, USDMF, WC | 44 products |
When sending a request, specify which Tolcapone 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.).
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