All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

opicapone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
catechol-O-methyltransferase (COMT) inhibitors	5143	923287-50-7

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: opicapone ongentys BIA 9-1067

a peripheral, selective and reversible catechol-O-methyltransferase (COMT) inhibitor endowed with a high binding affinity (sub-picomolar) that translates into a slow complex dissociation rate constant and a long duration of action (>24 hours) in vivo Molecular weight: 413.17 Formula: C15H10Cl2N4O6 CLOGP: 2.31 LIPINSKI: 0 HAC: 10 HDO: 2 TPSA: 149.46 ALOGS: -3.97 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
50	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BMX,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK16,CDK19,CDK2,CDK4,CDK5,CDK9,CLK4,CSF1R,DDR1,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHB4,ERBB2,FGFR1,FLT3,FLT4,GRK2,GRK3,GSK3A,GSK3B,IGF1R,IKBKB,INSR,IRAK1,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K8,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MELK,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PRKCD,PRKCZ,PRKDC,PTK2,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,UHMK1,ULK1,ULK2,ZAP70	101
kinase-selectivity-class	AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,GRK2,MAP2K6,MAPK1,MAPK7,MET,PDK4,PRKDC,STK33,TEK,TTK,TYRO3	17
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
June 29, 2020	PMDA	Ono Pharmaceutical Co., Ltd
April 24, 2020	FDA	NEUROCRINE
June 24, 2016	EMA	Bial

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	112.84	60.06	33	536	65926	90561952
Dyskinesia	97.82	60.06	26	543	36508	90591370
Reduced facial expression	81.00	60.06	14	555	2539	90625339
Muscle rigidity	72.47	60.06	17	552	14292	90613586

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	119.42	39.23	53	1553	57454	42562275
On and off phenomenon	106.68	39.23	25	1581	3442	42616287
Dyskinesia	103.30	39.23	38	1568	25352	42594377
Akinesia	76.95	39.23	18	1588	2454	42617275
Bradykinesia	76.57	39.23	21	1585	5415	42614314
Hyperkinesia	74.47	39.23	17	1589	2081	42617648
Reduced facial expression	74.12	39.23	16	1590	1517	42618212
Freezing phenomenon	70.79	39.23	16	1590	1873	42617856
Muscle rigidity	60.09	39.23	21	1585	12038	42607691
Hallucination, visual	58.83	39.23	24	1582	20996	42598733
Therapeutic response shortened	53.98	39.23	20	1586	13534	42606195
Dystonia	47.74	39.23	18	1588	12772	42606957
Delusion	45.27	39.23	18	1588	14716	42605013

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hallucination	229.51	37.92	83	2104	101349	110485763
Dyskinesia	182.35	37.92	59	2128	51387	110535725
On and off phenomenon	145.42	37.92	30	2157	4394	110582718
Reduced facial expression	139.15	37.92	28	2159	3623	110583489
Muscle rigidity	129.30	37.92	38	2149	23993	110563119
Bradykinesia	128.79	37.92	32	2155	10756	110576356
Freezing phenomenon	111.38	37.92	22	2165	2587	110584525
Hyperkinesia	107.01	37.92	22	2165	3162	110583950
Dystonia	105.34	37.92	33	2154	25772	110561340
Therapeutic response shortened	96.87	37.92	32	2155	29551	110557561
Akinesia	92.56	37.92	20	2167	3647	110583465
Hallucination, visual	91.47	37.92	33	2154	39572	110547540
Delusion	63.20	37.92	22	2165	23733	110563379
Tremor	56.41	37.92	40	2147	202192	110384920
Hypokinesia	53.42	37.92	19	2168	21807	110565305
Saliva altered	44.72	37.92	8	2179	550	110586562
Psychotic disorder	43.88	37.92	21	2166	50916	110536196
Delirium	43.00	37.92	29	2158	134996	110452116
Infusion site abscess	40.64	37.92	7	2180	386	110586726
Jealous delusion	39.35	37.92	7	2180	466	110586646
Gait disturbance	39.25	37.92	37	2150	278171	110308941
Aggression	38.01	37.92	20	2167	59190	110527922

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N04BX04	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Other dopaminergic agents
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D065098	Catechol O-Methyltransferase Inhibitors
FDA MoA	N0000175756	Catechol O-Methyltransferase Inhibitors
FDA EPC	N0000175757	Catechol-O-Methyltransferase Inhibitor
CHEBI has role	CHEBI:48407	antiparkinson drug

Related Drugs by ATC class:

N04BX Other dopaminergic agents 3 drugs

budipineentacaponetolcapone

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Parkinson's disease	indication	49049000	DOID:14330

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.57	acidic
pKa2	10.45	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY INCREASING L-DOPA AMOUNTS THAT REACH THE BRAIN
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY INHIBITING COMT IN THE PERIPHERY
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY REDUCING O-METHYLATION OF L-DOPA
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY INCREASING L-DOPA AMOUNTS THAT REACH THE BRAIN
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY INHIBITING COMT IN THE PERIPHERY
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY REDUCING O-METHYLATION OF L-DOPA
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	8168793	Oct. 10, 2027	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9745290	Oct. 10, 2027	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	8168793	Oct. 10, 2027	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9745290	Oct. 10, 2027	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	8524746	July 14, 2029	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	8524746	July 14, 2029	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	10583130	March 31, 2030	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	10583130	March 31, 2030	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	12129247	Jan. 11, 2032	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY ADMINISTERING WITHOUT FOOD
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	12129247	Jan. 11, 2032	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES BY ADMINISTERING WITHOUT FOOD
25MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9630955	Dec. 12, 2032	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES
50MG	ONGENTYS	AMNEAL	N212489	April 24, 2020	RX	CAPSULE	ORAL	9630955	Dec. 12, 2032	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSON’S DISEASE EXPERIENCING OFF EPISODES

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Catechol O-methyltransferase	Enzyme	P21964	COMT_HUMAN	INHIBITOR	Ki	9		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Catechol O-methyltransferase	Enzyme		COMT_RAT	INHIBITOR	Ki	8.82		IUPHAR
Catechol O-methyltransferase	Enzyme		COMT_MOUSE	INHIBITOR	Ki	8.82		IUPHAR

External reference:

ID	Source
Y5929UIJ5N	UNII
4039693	VANDF
C2933912	UMLSCUI
CHEBI:134699	CHEBI
DNI	PDB_CHEM_ID
CHEMBL1089318	ChEMBL_ID
135565903	PUBCHEM_CID
DB11632	DRUGBANK_ID
9268	INN_ID
C549349	MESH_SUPPLEMENTAL_RECORD_UI
8988	IUPHAR_LIGAND_ID
2362167	RXNORM
253387	MMSL
32426	MMSL
d08530	MMSL
017858	NDDF
720356008	SNOMEDCT_US
763548009	SNOMEDCT_US
Y5929UIJ5N	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	64896-402	CAPSULE	25 mg	ORAL	NDA	27 sections
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	64896-402	CAPSULE	25 mg	ORAL	NDA	27 sections
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	64896-403	CAPSULE	50 mg	ORAL	NDA	27 sections
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	64896-403	CAPSULE	50 mg	ORAL	NDA	27 sections