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opicapone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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

Approvals:

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

FDA Adverse Event Reporting System (Female)

None

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	80.47	58.72	32	650	51466	34904783
Akinesia	61.54	58.72	13	669	2171	34954078

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	145.31	54.77	49	856	85696	79657787
Therapeutic response shortened	84.17	54.77	22	883	15841	79727642
Bradykinesia	77.39	54.77	18	887	8025	79735458
Akinesia	69.03	54.77	14	891	3298	79740185
Dystonia	68.68	54.77	20	885	21379	79722104
Hallucination, visual	68.42	54.77	22	883	32707	79710776
Muscle rigidity	65.65	54.77	19	886	19863	79723620
Reduced facial expression	65.47	54.77	13	892	2752	79740731
Freezing phenomenon	63.87	54.77	12	893	1902	79741581
Dyskinesia	57.90	54.77	21	884	44752	79698731

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	D018726	Anti-Dyskinesia Agents
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D065098	Catechol O-Methyltransferase Inhibitors
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D004791	Enzyme Inhibitors
FDA MoA	N0000175756	Catechol O-Methyltransferase Inhibitors
FDA EPC	N0000175757	Catechol-O-Methyltransferase Inhibitor

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	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	METHOD OF INHIBITING COMT IN THE PERIPHERY
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	METHOD OF REDUCING O-METHYLATION OF L-DOPA
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	METHOD OF TREATING PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	METHOD OF INHIBITING COMT IN THE PERIPHERY
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	METHOD OF REDUCING O-METHYLATION OF L-DOPA
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9550759	July 26, 2026	METHOD OF TREATING PARKINSONS DISEASE
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9745290	Oct. 10, 2027	METHOD OF TREATING PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9745290	Oct. 10, 2027	METHOD OF TREATING PARKINSONS DISEASE
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	8168793	April 2, 2029	METHOD OF TREATING PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	8168793	April 2, 2029	METHOD OF TREATING PARKINSONS DISEASE
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	8524746	July 14, 2029	METHOD OF TREATING PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	8524746	July 14, 2029	METHOD OF TREATING PARKINSONS DISEASE
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	10583130	March 31, 2030	METHOD OF TREATING PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	10583130	March 31, 2030	METHOD OF TREATING PARKINSONS DISEASE
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9630955	Dec. 12, 2032	METHOD OF TREATING PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	9630955	Dec. 12, 2032	METHOD OF TREATING PARKINSONS DISEASE
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	10357468	May 27, 2035	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	10357468	May 27, 2035	ADJUNCTIVE TREATMENT TO LEVODOPA/CARBIDOPA IN PATIENTS WITH PARKINSONS DISEASE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
25MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	April 24, 2025	NEW CHEMICAL ENTITY
50MG	ONGENTYS	NEUROCRINE	N212489	April 24, 2020	RX	CAPSULE	ORAL	April 24, 2025	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	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
8988	IUPHAR_LIGAND_ID
2362167	RXNORM
253387	MMSL
32426	MMSL
d08530	MMSL
017858	NDDF
720356008	SNOMEDCT_US
763548009	SNOMEDCT_US
C549349	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	70370-3025	CAPSULE	25 mg	ORAL	NDA	28 sections
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	70370-3025	CAPSULE	25 mg	ORAL	NDA	28 sections
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	70370-3050	CAPSULE	50 mg	ORAL	NDA	28 sections
ONGENTYS	HUMAN PRESCRIPTION DRUG LABEL	1	70370-3050	CAPSULE	50 mg	ORAL	NDA	28 sections