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

Stem definition	Drug id	CAS RN
N-methylated xanthine derivatives	4882	155270-99-8

Description:

Molecule	Description
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: 3.03 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

Molecule

Description

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: 3.03
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:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Aug. 27, 2019	FDA	KYOWA KIRIN
March 15, 2013	PMDA

FDA Adverse Event Reporting System (Female)

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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
Dyskinesia	78.21	56.70	19	218	31983	63456802
Hallucination	68.06	56.70	19	218	54798	63433987

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FDA Adverse Event Reporting System (Male)

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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	56.02	48.23	19	244	51479	34905189

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FDA Adverse Event Reporting System (Geriatric)

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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
Dyskinesia	101.53	43.69	29	565	44744	79699050
Hallucination	98.72	43.69	33	561	85712	79658082
Hallucination, visual	64.31	43.69	19	575	32710	79711084

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
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

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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	1.59	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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
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	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	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

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Adenosine receptor A2a	GPCR	P29274	AA2AR_HUMAN	ANTAGONIST	Ki	8.66	CHEMBL	SCIENTIFIC LITERATURE
Adenosine receptor A2b	GPCR	P29275	AA2BR_HUMAN		Ki	5.75	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.35	CHEMBL
Adenosine receptor A1	GPCR	P30542	AA1R_HUMAN		Ki	6.08	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme	P27338	AOFB_HUMAN		Ki	7.57	CHEMBL
Adenosine receptor A1	GPCR		AA1R_RAT		Ki	6.82	CHEMBL
Adenosine receptor A2a	GPCR		AA2AR_RAT		Ki	8.70	CHEMBL

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External reference:

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ID	Source
JQ9	PDB_CHEM_ID
018108	NDDF
2199015	RXNORM
2GZ0LIK7T4	UNII
322306	MMSL
37365	MMSL
4038742	VANDF
5311037	PUBCHEM_CID
5608	IUPHAR_LIGAND_ID
789546007	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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