ISTRADEFYLLINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H24N4O4
Molecular Weight	384.429
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN1C2=C(N(C)C(\C=C\C3=CC(OC)=C(OC)C=C3)=N2)C(=O)N(CC)C1=O

InChI

InChIKey=IQVRBWUUXZMOPW-PKNBQFBNSA-N

InChI=1S/C20H24N4O4/c1-6-23-18-17(19(25)24(7-2)20(23)26)22(3)16(21-18)11-9-13-8-10-14(27-4)15(12-13)28-5/h8-12H,6-7H2,1-5H3/b11-9+

HIDE SMILES / InChI

Molecular Formula	C20H24N4O4
Molecular Weight	384.429
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: http://www.e-search.ne.jp/~jpr/PDF/KYOWA13.PDF | https://www.ncbi.nlm.nih.gov/pubmed/23812646

Istradefylline is a first-in-class adenosine A2A receptor antagonist antiparkinsonian agent and has been marketed as the brand name NOURIAST® in Japan since May 30, 2013. NOURIAST is indicated for the improvement of wearing-off phenomena in patients with Parkinson’s disease on concomitant treatment with levodopa-containing products.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adenosine A2a receptor 31 Target ID: CHEMBL251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23812646 \| https://www.ncbi.nlm.nih.gov/pubmed/16250647	Antagonist 2849		12.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Parkinson's disease 232 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26630457 https://www.ncbi.nlm.nih.gov/pubmed/23700273	Primary		Approved 8583	NOURIAST Approved Use Improvement of wearing-off phenomena in patients with Parkinson’s disease on concomitant treatment with levodopa-containing products. Launch Date 2013

C_max

Value	Dose	Co-administered	Analyte	Population
230.9 ng/mL REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ISTRADEFYLLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
3249 ng × h/mL REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ISTRADEFYLLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
72.1 h REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ISTRADEFYLLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ISTRADEFYLLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	unhealthy, 65 years (range: 33 - 84 years) Health Status: unhealthy Age Group: 65 years (range: 33 - 84 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	Disc. AE: Dyskinesia... AEs leading to discontinuation/dose reduction: Dyskinesia (6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf
120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	Other AEs: Chest pain... Other AEs: Chest pain (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf
300 mg single, oral Highest studied dose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf
120 mg single, oral Overdose Dose: 120 mg Route: oral Route: single Dose: 120 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	Other AEs: Hallucinations, Agitation... Other AEs: Hallucinations Agitation Dyskinesia Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf
40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	Disc. AE: Visual hallucinations, Hallucination olfactory... Other AEs: Auditory hallucinations... AEs leading to discontinuation/dose reduction: Visual hallucinations (1%) Hallucination olfactory (1%) Somatic hallucination (1%) Other AEs: Auditory hallucinations (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf

AEs

AE	Significance	Dose	Population
Dyskinesia	6% Disc. AE	40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	unhealthy, 65 years (range: 33 - 84 years) Health Status: unhealthy Age Group: 65 years (range: 33 - 84 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf
Chest pain	0.7%	120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf
Agitation		120 mg single, oral Overdose Dose: 120 mg Route: oral Route: single Dose: 120 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf
Dyskinesia		120 mg single, oral Overdose Dose: 120 mg Route: oral Route: single Dose: 120 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf
Hallucinations		120 mg single, oral Overdose Dose: 120 mg Route: oral Route: single Dose: 120 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022075s000lbl.pdf
Auditory hallucinations	1%	40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf
Hallucination olfactory	1% Disc. AE	40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf
Somatic hallucination	1% Disc. AE	40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf
Visual hallucinations	1% Disc. AE	40 mg 1 times / day steady, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: steady Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	substrate 1193 inhibitor 2438	substrate 1388 inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 BCRP 910 OATP1B1 1079 OATP1B3 961 OAT1 725 OCT2 779 MATE1 415 MATE2 267 OAT3 747 CYP1A2 2153 CYP2C19 2057	UGT 219 sulfotransferases 39 BCRP 697 OATP1B1 503 OATP1B3 435 CYP1A 26 CYP2C8 810 CYP2C18 149	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
MATE2 267	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	unlikely
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	unlikely
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	unlikely
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=11 Page: 11;121	weak [IC50 1.74 uM]	weak (co-administration study) Comment: administered with digoxin (substrate); digoxin exposures increased by 33% (Cmax) and 21% (AUC0-inf) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=11 Page: 11;121
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=11 Page: 11;145	yes [IC50 2.9 uM]	yes (co-administration study) Comment: administered with midazolam (substrate): doses of 80 mg/day of istradefylline resulted in 1.6-fold (Cmax) and 2.4-fold (AUC0-inf) increase in midazolam exposures; administered with atorvastatin (substrate): doses of 40 mg/day of istradefylline resulted in 1.5-fold (Cmax and AUC0-inf) increase in atorvastatin exposures Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=11 Page: 11;145

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=11 Page: 11,22	major	yes (co-administration study) Comment: administered with ketoconazole (inhibitor); the exposures of istradefylline increased by 2.5-fold for AUC0-inf while Cmax was not affected; administered with rifampin: the exposures of istradefylline decreased by 45% and 81% for Cmax and AUC, respectively; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=11 Page: 11,22
CYP1A 26	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2C18 149	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
UGT 219	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=10 Page: 100;102	yes
sulfotransferases 39	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=10 Page: 100;102	yes

Sourcing

Vendor/Aggregator	ID	URL
abcr GmbH	AB426255	http://www.abcr.com/shop/en/AB426255
AbMole Bioscience	M3188	http://www.abmole.com/products/istradefylline.html
Achemtek	0102-011713	http://www.achemtek.com/155270-99-8
Acorn PharmaTech	ACN-048222	http://www.acornpharmatech.com/
Adooq BioScience	A11451	https://www.adooq.com/istradefylline-kw-6002.html
AK Scientific, Inc. (AKSCI)	Z4210	http://www.aksci.com/item_detail.php?cat=Z4210
Alfa Chemistry	AP155270998	https://reagents.alfa-chemistry.com/product/istradefylline-cas-155270-99-8-5680.html
Ambinter	Amb20247751	http://www.ambinter.com/reference/20247751
ApexBio Technology	A8454	http://www.apexbt.com/istradefylline-kw-6002.html
Ark Pharma Scientific Limited	H-006271	http://www.arkpharmtech.com/product/11326.html
AstaTech, Inc.	27839	http://www.astatechinc.com/CPSResult.php?CRNO=30689
Aurora Fine Chemicals LLC	A17.924.517	http://online.aurorafinechemicals.com/info?ID=A17.924.517
Aurum Pharmatech LLC	MP-2039	http://www.Aurumpharmatech.com/Product/ProductDetails/MP_2039
Axon MedChem	1423	https://www.axonmedchem.com/product/1423
BioChemPartner	BCP02194	http://www.biochempartner.com/155270-99-8-BCP02194
BioCrick	BCC3798	http://www.biocrick.com/Istradefylline-KW-6002-BCC3798.html
BioSynth	J-009183	https://www.biosynth.com/en/products/all-products/products/J-009183.html
BioSynth	J-519355	https://www.biosynth.com/en/products/all-products/products/J-519355.html
Chem Scene	CS-0737	http://www.chemscene.com/155270-99-8.html
ChemMol	49410320	http://www.chemmol.com/chemmol/49410320.html
ChemMol	97900060	http://www.chemmol.com/chemmol/97900060.html
Chemspace	CSSB00016988022	https://chem-space.com/CSSB00016988022
DC Chemicals	DCAPI1080	http://www.dcchemicals.com//product_show-Istradefylline_KW_6002_.html
eNovation Chemicals	D673395	https://www.enovationchem.com/ProductDetails.asp?ProductID=D673395
eNovation Chemicals	D763059	https://www.enovationchem.com/ProductDetails.asp?ProductID=D763059
eNovation Chemicals	Y0982235	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0982235
Hairui	HR110769	http://www.hairuichem.com/en/product/155270-99-8.html
Huateng Pharma	F99715	http://en.huatengsci.com/product/Istradefylline.html
Lab Network	LN00334150	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00334150
Matrix Scientific	144294	https://www.matrixscientific.com/144294.html
MedChem Express	HY-10888	https://www.medchemexpress.com/Istradefylline.html
MolPort	MolPort-035-395-095	https://www.molport.com/shop/molecule-link/MolPort-035-395-095
MuseChem	I001965	https://www.musechem.com/product/I001965.html
Oakwood	237499	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=118498&ExtHyperLink=1
OChem	24599	http://www.ocheminc.com/index.php?act=psearch&pid=270I998
Renno Tech	RL01993	http://www.rennotech.com/product_show.asp?id=2242
Selleck Chemicals	S2790	http://www.selleckchem.com/products/istradefylline-kw-6002.html
Sigma-Aldrich	SML0422_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/sml0422?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S531012	http://www.smolecule.com/products/s531012
Smolecule	S759435	https://www.smolecule.com/products/s759435
Synblock Inc	SB18985	http://www.synblock.com/product/155270-99-8.html
THE BioTek	bt-270136	https://www.thebiotek.com/product/inhibitors/bt-270136
Tocris	5147	https://www.tocris.com/products/istradefylline_5147
Vesino Industrial Co Ltd	VA11117	http://www.vsnchem.com/goto/product/22302/

PubMed

Title	Date	PubMed
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.	2011-03	21303899
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.	2011-02-10	21210664
Effects of the adenosine A 2A antagonist KW 6002 (istradefylline) on pimozide-induced oral tremor and striatal c-Fos expression: comparisons with the muscarinic antagonist tropicamide.	2009-09-29	19467297
The effects of adenosine A2A receptor antagonists on haloperidol-induced movement disorders in primates.	2008-10	18594798
Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.	2008-09-15	18723354
Tremorolytic effects of adenosine A2A antagonists: implications for parkinsonism.	2008-05-01	18508458
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.	2007-02-22	17300165
Forebrain adenosine A2A receptors contribute to L-3,4-dihydroxyphenylalanine-induced dyskinesia in hemiparkinsonian mice.	2006-12-27	17192438
Pharmacological validation of a mouse model of l-DOPA-induced dyskinesia.	2005-07	15899244
A2A antagonist prevents dopamine agonist-induced motor complications in animal models of Parkinson's disease.	2003-11	14637099
Cellular and behavioural effects of the adenosine A2a receptor antagonist KW-6002 in a rat model of l-DOPA-induced dyskinesia.	2003-03	12614340
Adenosine A(2a) receptor antagonists: potential therapeutic and neuroprotective effects in Parkinson's disease.	2001-11	15111244
Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys.	2000-04	10739638
Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP.	1999-11	10591873

Patents

Sample Use Guides

In Vivo Use Guide

To be administered concomitantly with levodopa-containing products. The usual adult dosage of istradefylline is 20 mg orally administered once daily. According to symptoms, 40 mg of istradefylline can be orally administered once daily.

Route of Administration: Oral

In Vitro Use Guide

The binding kinetics of istradefylline to the human A2A receptor were investigated using 1 nmol/L of [3H]-istradefylline binding to the human A2A receptor.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 09:43:12 GMT 2025` Edited by `admin` on `Wed Apr 02 09:43:12 GMT 2025`
Record UNII	2GZ0LIK7T4
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ISTRADEFYLLINE

Official Name

English

NOURIANZ

Preferred Name

English

KW-6002

Code

English

(E)-8-(3,4-DIMETHOXYSTYRYL)-1,3-DIETHYL-7-METHYL-3,7-DIHYDRO-1H-PURINE-2,6-DIONE

Systematic Name

English

Istradefylline [WHO-DD]

Common Name

English

8-[(1E)-2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione

Systematic Name

English

1H-PURINE-2,6-DIONE, 8-((1E)-2-(3,4-DIMETHOXYPHENYL)ETHENYL)-1,3-DIETHYL-3,7-DIHYDRO-7-METHYL-

Systematic Name

English

ISTRADEFYLLINE [USAN]

Common Name

English

ISTRADEFYLLINE [MI]

Common Name

English

ISTRADEFYLLINE [JAN]

Common Name

English

istradefylline [INN]

Common Name

English

ISTRADEFYLLINE [ORANGE BOOK]

Common Name

English

NOURIAST

Brand Name

English

Classification Tree Code System Code

NCI_THESAURUS

C38149