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Details

Stereochemistry ACHIRAL
Molecular Formula C15H10Cl2N4O6
Molecular Weight 413.1696
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OPICAPONE

SMILES

Cc1c(c(Cl)n(=O)c(C)c1Cl)-c2nc(-c3cc(c(c(c3)O)O)N(=O)=O)on2

InChI

InChIKey=ASOADIZOVZTJSR-UHFFFAOYSA-N
InChI=1S/C15H10Cl2N4O6/c1-5-10(13(17)20(24)6(2)11(5)16)14-18-15(27-19-14)7-3-8(21(25)26)12(23)9(22)4-7/h3-4,22-23H,1-2H3

HIDE SMILES / InChI
Opicapone (Ongentys®), a potent, oral, third-generation, long-acting, peripheral catechol-O-methyltransferase (COMT) inhibitor, is approved as the adjunctive treatment to levodopa (L-Dopa)/dopa-decarboxylase inhibitor (DDCI) therapy in adults with Parkinson's disease (PD) and end-of-dose motor fluctuations who cannot be stabilized on those combinations. Opicapone is a hydrophilic 1,2,4-oxadiazole analog with a pyridine N-oxide at position 3, with these modifications enhancing its potency and extending its duration of action, whilst avoiding cell toxicity. In preclinical animal studies, Opicapone-induced inhibition of peripheral (but not central) COMT activity was associated with a prolonged increase in systemic and central exposure to L-Dopa, with a corresponding reduction in 3-OMD exposure. Following single or multiple doses of Opicapone (5–1200 mg) in healthy adult volunteers or patients with PD, Opicapone inhibited COMT activity in ex vivo erythrocyte assays in a reversible dose-dependent manner, with the duration of Opicapone-induced COMT inhibition independent of dose. Adjunctive Opicapone was generally well tolerated during more than a year of treatment in BIPARK I and BIPARK II (double-blind plus extension phases). The recommended dosage is 50 mg once daily, which should be taken at bedtime at least 1 h before or after L-Dopa combinations.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
10.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Ongentys

Approved Use

Unknown

Launch Date

1.46776326E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
58 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
343 ng/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
301 ng/mL
30 mg 1 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
95 ng/mL
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
424.5 ng/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
756.2 ng/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
124 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1432 ng × h/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1441 ng × h/mL
30 mg 1 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
238 ng × h/mL
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1321 ng × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
2244 ng × h/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.4 h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.4 h
30 mg 1 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.1 h
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.97 h
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
0.92 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.1%
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
0.1%
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OPICAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
1200 mg 1 times / day single, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: single
Dose: 1200 mg, 1 times / day
Sources:
healthy, 18-45 years
n = 6
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 67.7 years
n = 495
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 67.7 years
Sex: M+F
Population Size: 495
Sources:
Disc. AE: Nausea, Constipation...
AEs leading to
discontinuation/dose reduction:
Nausea (2%)
Constipation (1.4%)
Hallucination (1%)
Dizziness (1%)
Dyskinesia (1%)
Sources:
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 115
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 115
Sources:
Other AEs: Nausea...
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Disc. AE: Dyskinesia...
Other AEs: Dyskinesia, Dizziness...
AEs leading to
discontinuation/dose reduction:
Dyskinesia (3%)
Other AEs:
Dyskinesia (20%)
Dizziness (3%)
Constipation (6%)
Dry mouth (3%)
Hallucination (3%)
Insomnia (3%)
Blood creatine increased (5%)
Weight decreased (4%)
Hypotension orthostatic (5%)
Hypertension (3%)
Sources:
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
DLT: Depression, Abnormal behaviour...
Disc. AE: Creatine kinase increased, Creatine kinase increased...
Dose limiting toxicities:
Depression (grade 1, 0.4%)
Abnormal behaviour (grade 3, 0.4%)
AEs leading to
discontinuation/dose reduction:
Creatine kinase increased
Creatine kinase increased
Pulmonary embolism (grade 3, 0.4%)
Cholecystitis acute (grade 3, 0.4%)
Delirium febrile (grade 2, 0.4%)
Head injury (grade 3, 0.4%)
Atrioventricular block complete (grade 1, 0.4%)
Hallucination, auditory (grade 3, 0.4%)
Sources:
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy, adults
n = 244
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 244
Sources:
Disc. AE: Osteoarthritis, Superficial spreading melanoma...
AEs leading to
discontinuation/dose reduction:
Osteoarthritis (grade 1, 0.4%)
Superficial spreading melanoma (grade 1, 0.4%)
Malignant melanoma (grade 3, 0.4%)
Jealous delusion (grade 3, 0.4%)
Sources:
5 mg 1 times / day steady, oral
Studied dose
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adults
n = 122
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 122
Sources:
Disc. AE: Hepatic enzyme increased...
AEs leading to
discontinuation/dose reduction:
Hepatic enzyme increased (grade 2, 0.2%)
Sources:
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
n = 356
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 356
Sources:
Disc. AE: Hallucinations, Visual hallucinations...
AEs leading to
discontinuation/dose reduction:
Hallucinations (1.7%)
Visual hallucinations (0.3%)
Sources:
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 265
Sources:
Disc. AE: Nausea and vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea and vomiting (2%)
Sources:
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: Parkinson's disease
Sources:
Disc. AE: Hallucinations...
AEs leading to
discontinuation/dose reduction:
Hallucinations (1.7%)
Sources:
5 mg 1 times / day steady, oral
Studied dose
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: Parkinson's disease
Sources:
Disc. AE: Hallucinations...
AEs leading to
discontinuation/dose reduction:
Hallucinations (0.8%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Dizziness 1%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 67.7 years
n = 495
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 67.7 years
Sex: M+F
Population Size: 495
Sources:
Dyskinesia 1%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 67.7 years
n = 495
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 67.7 years
Sex: M+F
Population Size: 495
Sources:
Hallucination 1%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 67.7 years
n = 495
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 67.7 years
Sex: M+F
Population Size: 495
Sources:
Constipation 1.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 67.7 years
n = 495
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 67.7 years
Sex: M+F
Population Size: 495
Sources:
Nausea 2%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 67.7 years
n = 495
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 67.7 years
Sex: M+F
Population Size: 495
Sources:
Nausea 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 115
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 115
Sources:
Dyskinesia 20%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Dizziness 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Dry mouth 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Hallucination 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Hypertension 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Insomnia 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Dyskinesia 3%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Weight decreased 4%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Blood creatine increased 5%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Hypotension orthostatic 5%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Constipation 6%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Creatine kinase increased Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Creatine kinase increased Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Depression grade 1, 0.4%
DLT
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Atrioventricular block complete grade 1, 0.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Delirium febrile grade 2, 0.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Abnormal behaviour grade 3, 0.4%
DLT
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Cholecystitis acute grade 3, 0.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Hallucination, auditory grade 3, 0.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Head injury grade 3, 0.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Pulmonary embolism grade 3, 0.4%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adults
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 265
Sources:
Osteoarthritis grade 1, 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy, adults
n = 244
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 244
Sources:
Superficial spreading melanoma grade 1, 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy, adults
n = 244
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 244
Sources:
Jealous delusion grade 3, 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy, adults
n = 244
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 244
Sources:
Malignant melanoma grade 3, 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy, adults
n = 244
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 244
Sources:
Hepatic enzyme increased grade 2, 0.2%
Disc. AE
5 mg 1 times / day steady, oral
Studied dose
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adults
n = 122
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adults
Sex: M+F
Population Size: 122
Sources:
Visual hallucinations 0.3%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
n = 356
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 356
Sources:
Hallucinations 1.7%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
n = 356
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 356
Sources:
Nausea and vomiting 2%
Disc. AE
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy
n = 265
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 265
Sources:
Hallucinations 1.7%
Disc. AE
25 mg 1 times / day steady, oral
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: Parkinson's disease
Sources:
Hallucinations 0.8%
Disc. AE
5 mg 1 times / day steady, oral
Studied dose
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: Parkinson's disease
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
no
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
no
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
yes [IC50 1.089 uM]
no (co-administration study)
Comment: 0.45 μg/mL. studies demonstrated no clinically relevant interaction with repaglinide (CYP2C8 and OATP1B1 substrate)
Page: 13.0
yes [IC50 10.55 uM]
yes [IC50 13.16 uM]
no (co-administration study)
Comment: 6.7 μg/mL, studies demonstrated no clinically relevant interaction with repaglinide (CYP2C8 and OATP1B1 substrate)
Page: 27.0
yes [IC50 14.75 uM]
yes [IC50 2.178 uM]
no (co-administration study)
Comment: 0.9 μg/mL, studies demonstrated no clinically relevant interaction with repaglinide (CYP2C8 and OATP1B1 substrate)
Page: 27.0
yes [IC50 22.22 uM]
yes [IC50 25.92 uM]
yes [IC50 3.388 uM]
yes [IC50 40.65 uM]
no (co-administration study)
Comment: 20.7 μg/mL, clinical studies demonstrated no clinically relevant interaction with warfarin (CYP2C9 substrate) or repaglinide (CYP2C8 and OATP1B1 substrate)
Page: 27.0
yes [IC50 43.57 uM]
no (co-administration study)
Comment: 18 μg/mL, clinical studies demonstrated no clinically relevant interaction with warfarin (CYP2C9 substrate) or repaglinide (CYP2C8 and OATP1B1 substrate)
Page: 27.0
yes [IC50 5 uM]
yes [IC50 5.5 uM]
no (co-administration study)
Comment: 2.80 ug/ml, studies demonstrated no clinically relevant interaction with repaglinide (CYP2C8 and OATP1B1 substrate)
Page: 13.0
yes [IC50 72.61 uM]
yes
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
yes
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
yes
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
yes
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
yes
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
yes
unlikely
Comment: CYP-mediated clinically relevant drug interactions perpetrated by OPC or its metabolite BIA 9-1103 are considered unlikely when taking into consideration the relevant free (unbound) Cmax following 50 mg dosing for OPC and its major metabolite.
Page: 13.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: Following administration of OPC 1 hour after 600 mg quinidine, median Tmax for OPC was approximately 1.5 hours later compared to when OPC was administered alone. OPC exposure (Cmax and AUC parameters) were approximately 30% to 37% lower when administered after quinidine compared to administration alone.
Page: 13.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Discovery of a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase.
2010 Apr 22
A fragment-based approach to identifying S-adenosyl-l-methionine -competitive inhibitors of catechol O-methyl transferase (COMT).
2014 Jun 26
Opicapone as an adjunct to levodopa in patients with Parkinson's disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial.
2016 Feb
Patents

Sample Use Guides

The recommended dosage is 50 mg once daily, which should be taken at bedtime at least 1 h before or after L-Dopa combinations
Route of Administration: Oral
COMT inhibition by Opicapone was evaluated in rat liver homogenates by measuring the formation of metanephrine (O-methylated adrenaline) Opicapone was under tight-binding conditions at a 10-fold lower concentration of 3 μM.The reactionmixture (total volume of 1 mL) contained homogenate (2 mg/mL), NCE (3 μM for nitrocatechols or 30 μM for non-nitrocatechols), 100 μM MgCl2 , 1 mM EGTA, 100 μM pargyline, and S-adenosyl-L-methionine (500 μM) in phosphate buffer (5 mM, pH 7.8). After a 20 min preincubation period at 37 C, the reaction was initiated with adrenaline (1000 μM when testing nitrocatechols or 25 μM when testing nonnitrocatechols) and proceeded for 5 min at 37 C. Reactions were terminated with the addition of 1/10 volume of 2 N perchloric acid. Samples were centrifuged (16000g for 3 min at 4 C) and filtered through 0.22 μm pore size Spin-X 200 filters. Metanephrine was then quantified by HPLC with electrochemical detection as previously detailed
Name Type Language
OPICAPONE
INN   WHO-DD  
INN  
Official Name English
5-(3-(2,5-DICHLORO-4,6-DIMETHYL-1-OXY-PYRIDIN-3-YL)-(1,2,4)OXADIAZOL-5-YL)-3-NITROBENZENE-1,2-DIOL
Systematic Name English
OPICAPONE [WHO-DD]
Common Name English
BIA 9-1067
Code English
OPICAPONE [MI]
Common Name English
OPICAPONE [USAN]
Common Name English
1,2-BENZENEDIOL, 5-(3-(2,5-DICHLORO-4,6-DIMETHYL-1-OXIDO-3-PYRIDINYL)-1,2,4-OXADIAZOL-5-YL)-3-NITRO-
Systematic Name English
BIA-9-1067
Code English
ONGENTYS
Brand Name English
OPICAPONE [INN]
Common Name English
2,5-DICHLORO-3-(5-(3,4-DIHYDROXY-5-NITROPHENYL)-1,2,4-OXADIAZOL-3-YL)-4,6-DIMETHYLPYRIDINE N-OXIDE
Systematic Name English
BIA-91067
Code English
Classification Tree Code System Code
WHO-ATC N04BX04
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
Code System Code Type Description
PUBCHEM
135565903
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
INN
9268
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
FDA UNII
Y5929UIJ5N
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
MESH
C549349
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
RXCUI
2362167
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
WIKIPEDIA
Opicapone
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
MERCK INDEX
M11976
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
CAS
923287-50-7
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
EVMPD
SUB130629
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
DRUG CENTRAL
5143
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
DRUG BANK
DB11632
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY
NCI_THESAURUS
C170258
Created by admin on Sat Jun 26 16:09:47 UTC 2021 , Edited by admin on Sat Jun 26 16:09:47 UTC 2021
PRIMARY