Opicapone

Opicapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure.

• ONGENTYS is indicated as adjunctive treatment to levodopa/carbidopa in patients with Parkinson’s disease (PD) experiencing “off” episodes. ONGENTYS is a catechol-O-methyltransferase (COMT) inhibitor indicated as adjunctive treatment to levodopa/carbidopa in patients with Parkinson’s disease (PD) experiencing “off” episodes.

• ONGENTYS is contraindicated in patients with: Concomitant use of non-selective monoamine oxidase (MAO) inhibitors [ see Drug Interactions ( 7.1 ) ] . Pheochromocytoma, paraganglioma, or other catecholamine secreting neoplasms.contraindicated

The recommended dosage is 50 mg administered orally once daily at bedtime. ( 2.1 ) Patients should not eat food for 1 hour before and for at least 1 hour after intake of ONGENTYS. ( 2.1 ) The recommended dosage in patients with moderate hepatic impairment is 25 mg orally once daily at bedtime; avoid use in patients with severe hepatic impairment. ( 2.2 ) 2.1 Dosing and Administration Information The recommended dosage of ONGENTYS is 50 mg administered orally once daily at bedtime. Patients should not eat food for 1 hour before and for at least 1 hour after intake of ONGENTYS [see Clinical Pharmacology ( 12.3 )]. 2.2 Dosage Recommendations for Patients with Hepatic Impairment In patients with moderate hepatic impairment (Child-Pugh B), the recommended dose of ONGENTYS is 25 mg orally once daily at bedtime [see Use in Specific Populations ( 8.7 ), Clinical Pharmacology ( 12.3 )]. Avoid use of ONGENTYS in patients with severe (Child-Pugh C) hepatic impairment [ see Use in Specific Populations ( 8.7 ) , Clinical Pharmacology ( 12.3 ) ]. 2.3 D iscontinuation and Missed Dose When discontinuing ONGENTYS, monitor patients and consider adjustment of other dopaminergic therapies as needed. If a dose of ONGENTYS is missed, the next dose should be taken at the scheduled time the next day.

Cardiovascular Effects with Concomitant Use of Drugs Metabolized by Catechol-O-Methyltransferase (COMT): May cause arrhythmias, increased heart rate, and excessive changes in blood pressure. Monitor patients when treated concomitantly with products metabolized by COMT. ( 4 , 5.1 ) Falling Asleep During Activities of Daily Living: Advise patients prior to treatment. ( 5.2 ) Hypotension/Syncope: If occurs, consider discontinuing ONGENTYS or adjusting dosage of other medications that can lower blood pressure. ( 5.3 ) Dyskinesia: May cause or exacerbate dyskinesia; consider levodopa or dopaminergic medication dose reduction. ( 5.4 ) Hallucinations and Psychosis: Consider stopping ONGENTYS if occurs. ( 5.5 ) Impulse Control/Compulsive Disorders: Consider stopping ONGENTYS if occurs. ( 5.6 ) Withdrawal-Emergent Hyperpyrexia and Confusion: When discontinuing ONGENTYS, monitor patients and consider adjustment of other dopaminergic therapies as needed. ( 5.7 ) 5.1 Cardiovascular Effects with Concomitant Use of Drugs Metabol ized by Catechol-O-Methyltransferase (COMT) Possible arrhythmias, increased heart rate, and excessive changes in blood pressure may occur with concomitant use of ONGENTYS and drugs metabolized by COMT (e.g., isoproterenol, epinephrine, norepinephrine, dopamine, and dobutamine), regardless of the route of administration (including inhalation). Monitor patients treated concomitantly with ONGENTYS and drugs metabolized by COMT [see Contraindications ( 4 ), Drug Interactions ( 7.1 , 7.2 )] .

The following clinically significant adverse reactions are discussed in more detail in other sections of the labeling: Cardiovascular Effects with Concomitant Use of Drugs Metabolized by Catechol-O-Methyltransferase (COMT) [see Warnings and Precautions ( 5.1 )] Falling Asleep During Activities of Daily Living and Somnolence [see Warnings and Precautions ( 5.2 )] Hypotension/Syncope [see Warnings and Precautions ( 5.3 )] Dyskinesia [see Warnings and Precautions ( 5.4 )] Hallucinations and Psychosis [see Warnings and Precautions ( 5.5 )] Impulse Control/Compulsive Disorders [see Warnings and Precautions ( 5.6 )] Withdrawal-Emergent Hyperpyrexia and Confusion [see Warnings and Precautions ( 5.7 )] Most common adverse reactions (≥4% and > placebo): dyskinesia, constipation, blood creatine kinase increased, hypotension/syncope, and weight decreased. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of ONGENTYS was evaluated in 265 patients with Parkinson’s disease (PD) in two 14-15 week placebo- and active-controlled (Study 1) or placebo-controlled (Study 2) studies [see Clinical Studies ( 14 )] .

Pregnancy: Based on animal data, may cause fetal harm ( 8.1 ) Avoid use in patients with end-stage renal disease. ( 8.6 ) 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with use of ONGENTYS in pregnant women. In animal studies, oral administration of opicapone during pregnancy resulted in adverse effects on embryofetal development (increased incidence of fetal abnormalities) at clinically relevant plasma exposures in one of two species tested. In addition, opicapone is always given concomitantly with levodopa/carbidopa, which is known to cause developmental toxicity in rabbits ( s ee Data ). The background risk of major birth defects and miscarriage in the U.S. general population is 2-4% and 15-20% of clinically recognized pregnancies, respectively. The background risk for major birth defects and miscarriage in patients with Parkinson’s disease is unknown. Data Animal Data Oral administration of opicapone (0, 150, 375, or 1000 mg/kg/day) to pregnant rats throughout gestation resulted in no adverse effects on embryofetal development. Plasma exposure (AUC) at the highest dose tested (1000 mg/kg/day) was approximately 40 times that in humans at the recommended human dose (50 mg/day).

Metabolism

Opicapone demonstrates dose-proportional pharmacokinetics over a 25 mg (0.5 times the recommended dosage) to 50 mg dose range. The pharmacokinetics of opicapone are similar in both PD patients and healthy subjects.

No specific antidotes for ONGENTYS are known. As a general measure, removal of ONGENTYS by gastric lavage and/or inactivation by administering activated charcoal should be considered. In managing overdose, provide supportive care, including close medical supervision and monitoring, and consider the possibility of multiple drug involvement. If an over-exposure occurs, call your poison control center at 1-800-222-1222 or www.poison.org.

• Apr 24, 2020NDANDA212489Amneal

1. 1Hallucination29514%
2. 2Dyskinesia27713%
3. 3Fall23911%
4. 4Tremor1346.3%
5. 5Death1336.3%
6. 6Gait Disturbance1235.8%
7. 7Drug Ineffective1225.8%
8. 8On And Off Phenomenon1215.7%
9. 9Parkinson^s Disease1195.6%
10. 10Confusional State1175.5%
11. 11Constipation1055.0%
12. 12Anxiety974.6%
13. 13Fatigue974.6%
14. 14Dizziness944.4%
15. 15Hallucination, Visual904.3%

The 10 most recently updated of 49 ClinicalTrials.gov registrations naming Opicapone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• REal-life ON PARKinson's - ITaly (REONPARK-IT)
  Recruiting · Observational · 200 enrolled · Bial - Portela C S.A.
  NCT07403799updated 2026-05-05
• Fall Risk Assessment in Parkinson's Disease Using Kinetikos Health
  Not yet recruiting · Observational · 100 enrolled · Taipei Medical University Shuang Ho Hospital
  NCT07257393updated 2025-12-04
• OpiCapone Effect on Motor Fluctuations and pAiN
  Completed · Phase 4 · Interventional · 144 enrolled · Bial - Portela C S.A.
  NCT04986982updated 2025-03-28
• Early ParkinSon wIth L-DOPA/DDCI and OpicapoNe (EPSILON Study)
  Completed · Phase 3 · Interventional · 410 enrolled · Bial - Portela C S.A.
  NCT04978597updated 2025-03-12
• Relative Bioavailability and Bioequivalence Of Different Formulations of Opicapone in Healthy Volunteers
  Completed · Phase 1 · Interventional · 85 enrolled · Bial - Portela C S.A.
  NCT02305277updated 2025-03-12
• eArly levoDopa With Opicapone in Parkinson's paTients wIth motOr fluctuatioNs.
  Completed · Phase 4 · Interventional · 106 enrolled · Bial - Portela C S.A.
  NCT04990284updated 2025-03-12
• OpicApone Sleep dISorder
  Completed · Phase 4 · Interventional · 22 enrolled · Bial - Portela C S.A.
  NCT04986995updated 2025-03-12
• Opicapone as Adjunctive Therapy to Levodopa-Carbidopa Intestinal Gel in Parkinson's Disease
  Completed · Interventional · 22 enrolled · University Hospital of Ferrara
  NCT06432309updated 2025-03-03
• A Study to Evaluate the add-on Efficacy and Safety of Opicapone 50 mg or an Extra Dose of L-DOPA 100 mg for the Treatment of Wearing-off in Patients With PD
  Completed · Phase 4 · Interventional · 169 enrolled · SK Chemicals Co., Ltd.
  NCT04821687updated 2023-06-01
• Opicapone Treatment Initiation Open-Label Study
  Completed · Observational · 239 enrolled · Neurocrine Biosciences
  NCT04787965updated 2022-11-28

Frequently asked questions

How does Opicapone work?

Opicapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure.

What is Opicapone used for?

According to FDA labeling, Opicapone carries indications including: ONGENTYS is indicated as adjunctive treatment to levodopa/carbidopa in patients with Parkinson’s disease (PD) experiencing “off” episodes. ONGENTYS is a catechol-O-methyltransferase (COMT) inhibitor indicated as adjunctive treatment to levodopa/carbidopa in patients with Parkinson’s disease (PD) experiencing “off” episodes.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Opicapone?

Opicapone is classified as Other dopaminergic agents, Catechol-O-Methyltransferase Inhibitor, Catechol O-Methyltransferase Inhibitors, Monoamine Oxidase Inhibitors, Increased Central Nervous System Dopamine Activity.

What are the brand names for Opicapone?

Opicapone is marketed under brand names including Ongentys.

What are the contraindications for Opicapone?

Opicapone labeling lists contraindications including: ONGENTYS is contraindicated in patients with: Concomitant use of non-selective monoamine oxidase (MAO) inhibitors [ see Drug Interactions ( 7.1 ) ] . Pheochromocytoma, paraganglioma, or other catecholamine secreting neoplasms.. Always consult the full prescribing information and a clinician.