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Comtan (ENTACAPONE)
Comtan works by blocking the enzyme catechol-O-methyltransferase, which breaks down dopamine in the brain.
Comtan (Entacapone) is a small molecule catechol-O-methyltransferase inhibitor developed by Orion Pharma, currently owned by the same company. It was FDA approved in 1999 for the treatment of Parkinson's disease. As an off-patent medication, Comtan is available as a generic from multiple manufacturers. Key safety considerations include its short half-life of 2.4 hours and moderate bioavailability of 42%. Comtan is used in combination with levodopa and carbidopa to manage symptoms of Parkinson's disease.
At a glance
| Generic name | ENTACAPONE |
|---|---|
| Sponsor | Orion Pharma |
| Drug class | Catechol-O-Methyltransferase Inhibitor [EPC] |
| Target | Catechol O-methyltransferase |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 1999 |
Mechanism of action
Mechanism of Action. Entacapone is selective and reversible inhibitor of 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 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. In the presence of decarboxylase inhibitor, COMT becomes the major metabolizing enzyme for levodopa, catalyzing the metabolism to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD) i
Approved indications
- Parkinson's disease
Common side effects
- Dyskinesia
- Nausea
- Diarrhea
- Hyperkinesia
- Abdominal pain
- Constipation
- Vomiting
- Dyspnea
- Purpura
- Back pain
- Fatigue
- Asthenia
Key clinical trials
- [18F]F-DOPA Imaging in Patients With Autonomic Failure (PHASE1)
- Intestinal Levodopa + Entacapone Therapy (Lecigon®) to Counteract Dopaminergic Desensitization and Neuropsychiatric Complications in Parkinson's Disease (PHASE3)
- Long Term Effectiveness of Levodopa-Entacapone-Carbidopa Intestinal Gel in Participants With Advanced Parkinson's Disease
- Long-Term Observational Study on Effectiveness and Safety of Lecigon in Patients With Advanced Parkinson's Disease
- Evaluation of 611(Recombinant Humanized Anti-interleukin-4 Receptor Alpha IgG4 Monoclonal Antibody) in Chinese Adults With Moderate to Severe Atopic Dermatitis (PHASE3)
- Evaluation of 611 in Chinese Children and Adolescents With Moderate to Severe Atopic Dermatitis (PHASE1,PHASE2)
- A Study to Evaluate 611 in Patients With Chronic Rhinosinusitis With Nasal Polyps (PHASE3)
- Evaluation of 611 in Chinese Adults With Moderate to Severe Chronic Obstructive Pulmonary Disease (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |