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

Stem definitionDrug idCAS RN
catechol-O-methyltransferase (COMT) inhibitors 5143 923287-50-7

Description:

MoleculeDescription

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:

DoseUnitRoute
50 mg O

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
Parkinson's disease indication 49049000 DOID:14330




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.57 acidic
pKa2 10.45 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Catechol O-methyltransferase Enzyme INHIBITOR Ki 9 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Catechol O-methyltransferase Enzyme INHIBITOR Ki 8.82 IUPHAR
Catechol O-methyltransferase Enzyme INHIBITOR Ki 8.82 IUPHAR

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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