istradefylline Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
N-methylated xanthine derivatives 4882 155270-99-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nourianz
  • istradefylline
  • nouriast
  • KW-6002
  • KW6002
selective antagonist at the A2A receptor, used in the treatment of Parkinson's disease
  • Molecular weight: 384.44
  • Formula: C20H24N4O4
  • CLOGP: 3.37
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 0
  • TPSA: 76.90
  • ALOGS: -3.33
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 27, 2019 FDA KYOWA KIRIN
March 15, 2013 PMDA

FDA Adverse Event Reporting System (Female)

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
Dyskinesia 77.50 56.55 19 190 31814 53317043

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 56.32 52.50 18 173 52601 32460734

Pharmacologic Action:

SourceCodeDescription
ATC N04CX01 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
OTHER ANTIPARKINSON DRUGS
Other antiparkinson drugs
MeSH PA D058917 Adenosine A2 Receptor Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D058914 Purinergic Antagonists
MeSH PA D058915 Purinergic P1 Receptor Antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Parkinson's disease indication 49049000 DOID:14330

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.59 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
20MG NOURIANZ KYOWA KIRIN N022075 Aug. 27, 2019 RX TABLET ORAL 7727994 Jan. 18, 2023 A METHOD OF REDUCING OFF TIME FROM L-DOPA THERAPY, COMPRISING ADMINISTERING, TO A HUMAN PATIENT WITH PARKINSONS DISEASE, AN EFFECTIVE AMOUNT OF ISTRADEFYLLINE, WHEREIN THE PATIENT CURRENTLY RECEIVES SAID L-DOPA THERAPY
40MG NOURIANZ KYOWA KIRIN N022075 Aug. 27, 2019 RX TABLET ORAL 7727994 Jan. 18, 2023 A METHOD OF REDUCING OFF TIME FROM L-DOPA THERAPY, COMPRISING ADMINISTERING, TO A HUMAN PATIENT WITH PARKINSONS DISEASE, AN EFFECTIVE AMOUNT OF ISTRADEFYLLINE, WHEREIN THE PATIENT CURRENTLY RECEIVES SAID L-DOPA THERAPY
20MG NOURIANZ KYOWA KIRIN N022075 Aug. 27, 2019 RX TABLET ORAL 7727993 Jan. 28, 2023 A METHOD OF REDUCING OFF TIME FROM L-DOPA THERAPY, COMPRISING ADMINISTERING, TO A HUMAN PATIENT WITH PARKINSONS DISEASE, AN EFFECTIVE AMOUNT OF ISTRADEFYLLINE, WHEREIN THE PATIENT CURRENTLY RECEIVES SAID L-DOPA THERAPY
40MG NOURIANZ KYOWA KIRIN N022075 Aug. 27, 2019 RX TABLET ORAL 7727993 Jan. 28, 2023 A METHOD OF REDUCING OFF TIME FROM L-DOPA THERAPY, COMPRISING ADMINISTERING, TO A HUMAN PATIENT WITH PARKINSONS DISEASE, AN EFFECTIVE AMOUNT OF ISTRADEFYLLINE, WHEREIN THE PATIENT CURRENTLY RECEIVES SAID L-DOPA THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
20MG NOURIANZ KYOWA KIRIN N022075 Aug. 27, 2019 RX TABLET ORAL Aug. 27, 2024 NEW CHEMICAL ENTITY
40MG NOURIANZ KYOWA KIRIN N022075 Aug. 27, 2019 RX TABLET ORAL Aug. 27, 2024 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Adenosine receptor A2a GPCR ANTAGONIST Ki 8.66 CHEMBL SCIENTIFIC LITERATURE
Adenosine receptor A2b GPCR Ki 5.75 CHEMBL
Adenosine receptor A3 GPCR Ki 5.35 CHEMBL
Adenosine receptor A1 GPCR Ki 6.08 CHEMBL
Amine oxidase [flavin-containing] B Enzyme Ki 7.57 CHEMBL
Adenosine receptor A1 GPCR Ki 6.82 CHEMBL
Adenosine receptor A2a GPCR Ki 8.70 CHEMBL

External reference:

IDSource
2GZ0LIK7T4 UNII
D04641 KEGG_DRUG
4038742 VANDF
C0673470 UMLSCUI
CHEBI:134726 CHEBI
CHEMBL431770 ChEMBL_ID
5311037 PUBCHEM_CID
DB11757 DRUGBANK_ID
C111599 MESH_SUPPLEMENTAL_RECORD_UI
5608 IUPHAR_LIGAND_ID
8387 INN_ID
2199015 RXNORM
322306 MMSL
37365 MMSL
d09365 MMSL
018108 NDDF
789546007 SNOMEDCT_US
789550000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NOURIANZ HUMAN PRESCRIPTION DRUG LABEL 1 42747-602 TABLET, FILM COATED 20 mg ORAL NDA 31 sections
NOURIANZ HUMAN PRESCRIPTION DRUG LABEL 1 42747-604 TABLET, FILM COATED 40 mg ORAL NDA 31 sections