Entacapone API

Name	Entacapone
Chinese name	恩他卡朋
Cas Number	130929-57-6
Source	Europe
Qualifications	USDMF/-/-/-/-

Entacapone was created by the Finnish company Orion and listed in the EU in 1998. It is a catechol-O-methyltransferase (COMT) inhibitor and is a reversible, specific, and peripheral COMT inhibitor Agent. Entacapone reduces the metabolism of levodopa by inhibiting the COMT enzyme, which increases the bioavailability of levodopa and increases the total amount of levodopa available in the brain. Entacapone is used as an adjuvant for levodopa/carbidopa therapy for the treatment of Parkinson's disease, which can prolong the elimination half-life of levodopa by 33% and increase its bioavailability by 35%, thereby prolonging the maintenance of drug efficacy Time, but does not affect the peak time and concentration, is an important adjuvant drug when there are complications such as reduced efficacy and switching phenomenon after long-term levodopa treatment. Compared with tocapone, entacapone brings fewer side effects, such as diarrhea, liver enzyme elevation is not obvious, and it has better safety. It will not occur rare but serious fatal acute fulminant liver failure. Reduce the deterioration of dyskinesia. Compared with piribedil in the treatment of Parkinson's disease complicated with dyskinesia, entacapone is more effective in the treatment of the disease, and can effectively improve the patient's clinical symptoms and improve their ability of daily living. Entacapone had global sales of 140 million U.S. dollars in 2016, and it is expected that the overall Parkinson's disease drug market will exceed 3.2 billion U.S. dollars by 2021.

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