Opicapone
- Generic Name
- Opicapone
- Brand Names
- Ongentys, Ontilyv
- Drug Type
- Small Molecule
- Chemical Formula
- C15H10Cl2N4O6
- CAS Number
- 923287-50-7
- Unique Ingredient Identifier
- Y5929UIJ5N
Overview
Opicapone is a potent, reversible, and peripherally-acting third-generation inhibitor of catechol-o-methyltransferase (COMT), an enzyme involved in the breakdown of various catecholamines including dopamine. Many patients with Parkinson’s disease treated with levodopa plus a dopa decarboxylase (DDC) inhibitor (eg carbidopa) experience motor complications over time, which calls for the management of these symptoms through the use of a dopamine agonist, a monoamine oxidase B inhibitor (selegiline, rasagiline), a catechol-O-methyl transferase (COMT) inhibitor, or amantadine, or using a modified-release formulation of levodopa. Opicapone is used for adjunct therapy to levodopa and carbidopa in adult patients with Parkinson's disease and end-of-dose motor fluctuations. Opicapone was approved for use by the European Commission in June 2016 and the FDA in April 2020. It is marketed under the brand name Ongentys as once-daily oral capsules. Exhibiting a long duration of action that exceeds 24 hours, opicapone can be administered once-daily and demonstrates the lowest risk for cytotoxicity compared to other catechol-O-methyltransferase inhibitors.
Background
Opicapone is a potent, reversible, and peripherally-acting third-generation inhibitor of catechol-o-methyltransferase (COMT), an enzyme involved in the breakdown of various catecholamines including dopamine. Many patients with Parkinson’s disease treated with levodopa plus a dopa decarboxylase (DDC) inhibitor (eg carbidopa) experience motor complications over time, which calls for the management of these symptoms through the use of a dopamine agonist, a monoamine oxidase B inhibitor (selegiline, rasagiline), a catechol-O-methyl transferase (COMT) inhibitor, or amantadine, or using a modified-release formulation of levodopa. Opicapone is used for adjunct therapy to levodopa and carbidopa in adult patients with Parkinson's disease and end-of-dose motor fluctuations. Opicapone was approved for use by the European Commission in June 2016 and the FDA in April 2020. It is marketed under the brand name Ongentys as once-daily oral capsules. Exhibiting a long duration of action that exceeds 24 hours, opicapone can be administered once-daily and demonstrates the lowest risk for cytotoxicity compared to other catechol-O-methyltransferase inhibitors.
Indication
Opicapone is indicated as adjunctive therapy in adults with Parkinson’s disease and end-of-dose motor fluctuations or “off” episodes whose symptoms cannot be stabilized on the combination therapy of levodopa and DOPA decarboxylase inhibitor (e.g., carbidopa).
Associated Conditions
- Parkinson's Disease (PD)
Research Report
Opicapone: A Pharmacological and Clinical Review for the Management of Parkinson's Disease
I. Introduction to Opicapone and its Therapeutic Context in Parkinson's Disease
A. Overview of Parkinson's Disease (PD) and "OFF" Episodes
Parkinson's disease (PD) is a progressive neurodegenerative disorder primarily characterized by the loss of dopaminergic neurons in the substantia nigra, leading to a deficiency of dopamine in the brain.[1] This dopamine deficit manifests clinically as a constellation of motor symptoms, including bradykinesia (slowness of movement), rigidity, resting tremor, and postural instability. Levodopa, a dopamine precursor, remains the cornerstone of symptomatic therapy for PD.[2] However, long-term levodopa treatment is often complicated by the development of motor fluctuations, particularly "OFF" episodes.[3] These "OFF" episodes represent periods when the therapeutic effects of levodopa wear off, leading to the re-emergence or worsening of Parkinsonian motor symptoms such as shaking, stiffness, and slowed movement before the next scheduled dose.[4] Such fluctuations significantly impair patients' quality of life and functional independence, necessitating adjunctive therapeutic strategies to provide more continuous dopaminergic stimulation.[3]
B. Role of Catechol-O-Methyltransferase (COMT) Inhibition in Levodopa Therapy
Clinical Trials
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