COMT inhibitor

COMT inhibitor

Catechol-o-methyltransferase inhibitor Neurology A drug that enhances the effectiveness of levodopa by blocking COMT, an enzyme that metabolizes levodopa before it reaches the brain; ↑ levodopa bioavailability in the brain results in steady and continuous dopaminergic stimulation, and more consistent and effective symptom relief in Parkinson's disease
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BIPARK-1 was a Phase III, randomised, double-blind placebo- and active-controlled study of opicapone as an adjunct to levodopa therapy in which 600 patients with Parkinson's disease and motor fluctuations received once-daily opicapone (5 mg, 25 mg, or 50 mg), placebo, or 200 mg doses of the COMT inhibitor entacapone for 14 to 15 weeks.
(20) As noted above, enta-capone is a COMT inhibitor; it increases the plasma half-life of levodopa and decreases variations in peak-trough levels.
Responsiveness was obtained from two clinical trials for WOQ-19 comparing add-on therapy with entacapone (a COMT inhibitor).
For example, the COMT inhibitor, tolcapone (Tasmar[R]), has been withdrawn from use in several countries (excluding the US) because it can increase liver problems by as much as 100%.
While the studies carried out in Europe have proved the effectiveness of this COMT inhibitor in L-dopa-induced hyperhomocysteinemia, no correlation has been demonstrated in studies conducted in the USA (2,22,24).
(1,11) The plasma half-life of levodopa increases approximately 50% when administered with a COMT inhibitor, consequently allowing lower levodopa doses to achieve desired effects.
When the other available COMT inhibitor, entacapone (Comtan), is given as 200 mg with each dose of Sinemet, it reduces L-dopa peaks.
A new COMT inhibitor, entacapone (Comtess[R]), has recently received approval in the United States.
BIPARK-1 was a Phase III, randomized, double-blind placebo- and active-controlled study of opicapone as an adjunct to levodopa therapy in which approximately 600 patients with Parkinson's disease and motor fluctuations received once-daily opicapone (5 mg, 25 mg, or 50 mg), placebo, or 200 mg doses of the COMT inhibitor entacapone for 14 to 15 weeks.
According to BIAL, ONGENTYS (opicapone) is a novel, once-daily, peripherally-acting, highly-selective COMT inhibitor proposed for use as adjunct therapy to levodopa in Parkinson's patients.
Adding a dopamine agonist or a COMT inhibitor to the regimen of a patient who is already on levodopa can cause dyskinesia and hallucinations, particularly in advanced patients.
In advanced disease, motor complications can also be managed by augmenting levodopa therapy with a dopamine agonist, MAO-B inhibitor, or COMT inhibitor (7,8) (SOR: A).