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 30 Target ID: CHEMBL251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23812646 \| https://www.ncbi.nlm.nih.gov/pubmed/16250647	Antagonist 2778		12.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Parkinson's disease 226 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26630457 https://www.ncbi.nlm.nih.gov/pubmed/23700273	Primary		Approved 8429	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 unknown	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 unknown	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 unknown	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) n = 124 Health Status: unhealthy Age Group: 65 years (range: 33 - 84 years) Sex: M+F Population Size: 124 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 Page: p. 53	unhealthy n = 142 Health Status: unhealthy Population Size: 142 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 53	Other AEs: Chest pain... Other AEs: Chest pain (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 53
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 Page: p. 16	unhealthy Health Status: unhealthy Condition: Parkinson’s disease Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 16	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 16
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 n = 1 Health Status: unhealthy Population Size: 1 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 Page: p. 38	unhealthy n = 378 Health Status: unhealthy Population Size: 378 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 38	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 Page: p. 38

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) n = 124 Health Status: unhealthy Age Group: 65 years (range: 33 - 84 years) Sex: M+F Population Size: 124 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 Page: p. 53	unhealthy n = 142 Health Status: unhealthy Population Size: 142 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 53
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 n = 1 Health Status: unhealthy Population Size: 1 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 n = 1 Health Status: unhealthy Population Size: 1 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 n = 1 Health Status: unhealthy Population Size: 1 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 Page: p. 38	unhealthy n = 378 Health Status: unhealthy Population Size: 378 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 38
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 Page: p. 38	unhealthy n = 378 Health Status: unhealthy Population Size: 378 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 38
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 Page: p. 38	unhealthy n = 378 Health Status: unhealthy Population Size: 378 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 38
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 Page: p. 38	unhealthy n = 378 Health Status: unhealthy Population Size: 378 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000MedR.pdf Page: p. 38

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587 inducer 781	substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1461 BCRP 699 OATP1B1 788 OATP1B3 706 OAT1 599 OCT2 647 MATE1 306 MATE2 263 OAT3 642 CYP1A2 1524 CYP2C19 1478	UGT 192 sulfotransferases 38 BCRP 561 OATP1B1 406 OATP1B3 350 CYP1A 22 CYP2C8 693 CYP2C18 138	CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	likely
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=145 Page: 145.0	not significant [IC50 >100 uM]
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	unlikely
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	unlikely
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	unlikely
P-gp 1650	inhibitor 3277 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 1925	inhibitor 3277 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 1737	substrate 3367 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 22	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2C18 138	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	minor
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=22 Page: 22.0	no
UGT 192	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=10 Page: 100;102	yes
sulfotransferases 38	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/022075Orig1s000ClinPharmR.pdf#page=10 Page: 100;102	yes

Sourcing

Vendor/Aggregator	ID	URL
AK Scientific, Inc. (AKSCI)	Z4210	http://www.aksci.com/item_detail.php?cat=Z4210
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
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
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
OChem	24599	http://www.ocheminc.com/index.php?act=psearch&pid=270I998
Oakwood	237499	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=118498&ExtHyperLink=1
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/
abcr GmbH	AB426255	http://www.abcr.com/shop/en/AB426255
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

PubMed

Title	Date	PubMed
		252160133
Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP.	1999 Nov	10591873
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 Apr	10739638
Adenosine A(2a) receptor antagonists: potential therapeutic and neuroprotective effects in Parkinson's disease.	2001 Nov	15111244
Cellular and behavioural effects of the adenosine A2a receptor antagonist KW-6002 in a rat model of l-DOPA-induced dyskinesia.	2003 Mar	12614340
A2A antagonist prevents dopamine agonist-induced motor complications in animal models of Parkinson's disease.	2003 Nov	14637099
Pharmacological validation of a mouse model of l-DOPA-induced dyskinesia.	2005 Jul	15899244
Forebrain adenosine A2A receptors contribute to L-3,4-dihydroxyphenylalanine-induced dyskinesia in hemiparkinsonian mice.	2006 Dec 27	17192438
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.	2007 Feb 22	17300165
Tremorolytic effects of adenosine A2A antagonists: implications for parkinsonism.	2008 May 1	18508458
The effects of adenosine A2A receptor antagonists on haloperidol-induced movement disorders in primates.	2008 Oct	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 Sep 15	18723354
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 Sep 29	19467297
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 Feb 10	21210664
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.	2011 Mar	21303899

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 `Sat Dec 16 17:52:37 GMT 2023` Edited by `admin` on `Sat Dec 16 17:52:37 GMT 2023`
Record UNII	2GZ0LIK7T4
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ISTRADEFYLLINE

Official 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

NOURIANZ

Brand Name

English

ISTRADEFYLLINE [ORANGE BOOK]

Common Name

English

NOURIAST

Brand Name

English

Classification Tree Code System Code

NCI_THESAURUS

C38149