NAV

Istradefylline

Identification

Summary

Istradefylline is a selective adenoside A2A receptor antagonist indicated in adjunct to levodopa and carbidopa for the treatment of Parkinson's Disease.

Brand Names
Nourianz
Generic Name
Istradefylline
DrugBank Accession Number
DB11757
Background

Istradefylline, or KW6002, was developed by Kyowa Hakko Kirin in Japan for the treatment of Parkinson's disease as an adjunct to standard therapy.2 Unlike standard dopaminergic therapies for Parkinson's, Istradefylline targets adenosine A2A receptors in the basal ganglia.2 This region of the brain is highly involved in motor control.2

Istradefylline is indicated as an adjunct treatment to levodopa and carbidopa for Parkinson's disease.8

This drug was first approved in Japan on 25 March 2013.2 Istradefylline was granted FDA approval on 27 August 2019.5

Type
Small Molecule
Groups
Approved, Investigational
Structure
3D
Similar Structures
Weight
Average: 384.436
Monoisotopic: 384.179755269
Chemical Formula
C20H24N4O4
Synonyms
  • Istradefylline
External IDs
  • Kw 6002
  • KW-6002
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Pharmacology

Indication

Istradefylline is indicated in adjunct to levodopa and carbidopa in the treatment of Parkinson's disease.8

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in treatment ofParkinson's disease••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Istradefylline is a selective adenosine A2A receptor inhibitor.1,2 It has a long duration of action as it is given once daily and has a half life of 64-69 hours.1,2,8 Patients taking this medication should be monitored for dyskinesia, hallucinations, and lack of impulse control.8 Consider dose reductions for these patients.8

Mechanism of action

Istradefylline is a selective adenosine A2A receptor inhibitor.1,2 These receptors are found in the basal ganglia, a region of the brain that suffers degeneration in Parkinson's disease, and is also significantly involved in motor control.2 A2A receptors are also expressed on GABAergic medium spiny neurons within the indirect striato-pallidal pathway.7 The GABAergic action of this pathway is thereby reduced.7 Istradefylline has 56 times the affinity for A2A receptors than A1 receptors.2

TargetActionsOrganism
AAdenosine receptor A2a
antagonist
Humans
NAdenosine receptor A1
antagonist
Humans
Absorption

Istradefylline reaches a Cmax of 181.1ng/mL with a Tmax of 2.0h and an AUC of 11,100ng*h/mL.1 M1, the primary active metabolite, reaches a Cmax of 4.34ng/mL with a Tmax of 3.5h.1 The M8 metabolite reaches a Cmax of 12.6ng/mL with a Tmax of 3.0h and an AUC of 610ng*h/mL.1

Volume of distribution

The apparent volume of distribution of istradefylline is 448-557L.1

Protein binding

Istradefylline is approximately 98% protein bound in plasma,1 mostly to serum albumin and alpha-1-acid glycoprotein.7

Metabolism

The primary metabolite found in urine is the active 4'-O-monodesmethyl istradefylline (M1).1 Istradefylline is metabolized mainly by CYP1A1, CYP3A4, and CYP3A5.1 CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C18, and CYP2D6 also partly contribute the the metabolism of istradefylline.1 Other identified metabolites are 1-β-hydroxylated-4’-O-demethyl istradefylline (M2), 3’,4’-O-didemethyl istradefylline (M3), M1 sulfate conjugate (M4), M1 glucuronide (M5), 1-β-hydroxylated istradefylline (M8) and hydrogenated M3 (M10).7

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Route of elimination

A 3mg/kg oral dose given to male rats was 17.6% elminated in the urine and 68.3% eliminated in the feces.7 In urine, 5.31% of the total dose was the M3 metabolite and 1.96% of the total dose was the M1 metabolite.7 In feces, 30.60% of the total dose was the M3 metabolite, 9.34% of the total dose was the M1 metabolite, 8.33% of the total dose was the M10 metabolite, and 1.62% of the total dose was unchanged istradefylline.7

Half-life

The terminal elimination half life of istradefylline was 64-69 hours.1,2

Clearance

The apparent clearance of istradefylline is 4.1-6.0L/h.1

Adverse Effects
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Toxicity

The oral LD50 in mice is >300mg/kg.6

Patients experiencing an overdose may present with hallucinations, agitation, and dyskinesia.8 Treat patients by discontinuing istradefylline and administering supportive treatment.8

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
Integrate drug-drug
interactions in your software
AbametapirThe serum concentration of Istradefylline can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Istradefylline can be increased when combined with Abatacept.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Istradefylline.
AbirateroneThe serum concentration of Istradefylline can be increased when it is combined with Abiraterone.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Istradefylline.
Food Interactions
  • Avoid St. John's Wort. St. John's Wort decreases istradefylline concentrations.
  • Take at the same time every day.
  • Take with or without food.

Products

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International/Other Brands
Nouriast
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
NourianzTablet, film coated40 mg/1OralKyowa Kirin, Inc.2019-08-27Not applicableUS flag
NourianzTablet, film coated20 mg/1OralKyowa Kirin, Inc.2019-08-27Not applicableUS flag

Categories

ATC Codes
N04CX01 — Istradefylline
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as xanthines. These are purine derivatives with a ketone group conjugated at carbons 2 and 6 of the purine moiety.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Imidazopyrimidines
Sub Class
Purines and purine derivatives
Direct Parent
Xanthines
Alternative Parents
6-oxopurines / Dimethoxybenzenes / Alkaloids and derivatives / Styrenes / Phenoxy compounds / Anisoles / Pyrimidones / Alkyl aryl ethers / N-substituted imidazoles / Heteroaromatic compounds
show 8 more
Substituents
6-oxopurine / Alkaloid or derivatives / Alkyl aryl ether / Anisole / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Dimethoxybenzene / Ether
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
2GZ0LIK7T4
CAS number
155270-99-8
InChI Key
IQVRBWUUXZMOPW-PKNBQFBNSA-N
InChI
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+
IUPAC Name
8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione
SMILES
[H]\C(=C(\[H])C1=CC(OC)=C(OC)C=C1)C1=NC2=C(N1C)C(=O)N(CC)C(=O)N2CC

References

Synthesis Reference

https://patents.google.com/patent/CN104974157A/en

General References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
  2. Dungo R, Deeks ED: Istradefylline: first global approval. Drugs. 2013 Jun;73(8):875-82. doi: 10.1007/s40265-013-0066-7. [Article]
  3. Takahashi M, Fujita M, Asai N, Saki M, Mori A: Safety and effectiveness of istradefylline in patients with Parkinson's disease: interim analysis of a post-marketing surveillance study in Japan. Expert Opin Pharmacother. 2018 Oct;19(15):1635-1642. doi: 10.1080/14656566.2018.1518433. Epub 2018 Oct 3. [Article]
  4. Kondo T, Mizuno Y: A long-term study of istradefylline safety and efficacy in patients with Parkinson disease. Clin Neuropharmacol. 2015 Mar-Apr;38(2):41-6. doi: 10.1097/WNF.0000000000000073. [Article]
  5. FDA News Release: Istradefylline Approval [Link]
  6. Cayman Chemicals: Istradefylline MSDS [Link]
  7. Pharmaceuticals and Medical Devices Agency Japan: Report on Istradefylline [Link]
  8. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
PubChem Compound
5311037
PubChem Substance
347828111
ChemSpider
4470574
BindingDB
50176050
RxNav
2199015
ChEBI
134726
ChEMBL
CHEMBL431770
ZINC
ZINC000003803921
PDBe Ligand
JQ9
Wikipedia
Istradefylline
PDB Entries
8gng

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentParkinson's Disease (PD) / Tremor1
3CompletedTreatmentIdiopathic Parkinson's Disease2
3CompletedTreatmentParkinson's Disease (PD)7
3TerminatedTreatmentParkinson's Disease (PD)1
2CompletedTreatmentMovement Disorder Syndrome / Parkinson's Disease (PD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral20 mg/1
Tablet, film coatedOral40 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US7727993No2010-06-012023-01-28US flag
US7727994No2010-06-012023-01-18US flag
US7541363No2009-06-022024-11-13US flag
US8318201No2012-11-272027-09-05US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)189-193Not Available
boiling point (°C)601Not Available
water solubility0.5µg/mLNot Available
pKa0.78FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.182 mg/mLALOGPS
logP2.82ALOGPS
logP2.42Chemaxon
logS-3.3ALOGPS
pKa (Strongest Basic)-1.4Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area76.9 Å2Chemaxon
Rotatable Bond Count6Chemaxon
Refractivity107.11 m3·mol-1Chemaxon
Polarizability42.28 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-0009000000-cfde16c35bf1fb1d4741
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0009000000-1cd23f9a23c06f37fd2b
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0009000000-cd6ccd5704add2cd3ab2
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0uec-1019000000-461e87b9328acc3cd8b7
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-02tl-0239000000-98c1b65355403ffb17b8
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0019-2179000000-e751892c6c490494e249
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-223.4704105
predicted
DarkChem Lite v0.1.0
[M-H]-186.94373
predicted
DeepCCS 1.0 (2019)
[M+H]+223.2778105
predicted
DarkChem Lite v0.1.0
[M+H]+189.3393
predicted
DeepCCS 1.0 (2019)
[M+Na]+195.25182
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Details1. Adenosine receptor A2a
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Identical protein binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
ADORA2A
Uniprot ID
P29274
Uniprot Name
Adenosine receptor A2a
Molecular Weight
44706.925 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
  2. Dungo R, Deeks ED: Istradefylline: first global approval. Drugs. 2013 Jun;73(8):875-82. doi: 10.1007/s40265-013-0066-7. [Article]
Details2. Adenosine receptor A1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Purine nucleoside binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
ADORA1
Uniprot ID
P30542
Uniprot Name
Adenosine receptor A1
Molecular Weight
36511.325 Da
References
  1. Dungo R, Deeks ED: Istradefylline: first global approval. Drugs. 2013 Jun;73(8):875-82. doi: 10.1007/s40265-013-0066-7. [Article]

Enzymes

Details1. Cytochrome P450 1A1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details2. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details3. Cytochrome P450 3A5
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details4. Cytochrome P450 3A Subfamily (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Components:
NameUniProt ID
Cytochrome P450 3A4P08684
Cytochrome P450 3A43Q9HB55
Cytochrome P450 3A5P20815
Cytochrome P450 3A7P24462
References
  1. Dungo R, Deeks ED: Istradefylline: first global approval. Drugs. 2013 Jun;73(8):875-82. doi: 10.1007/s40265-013-0066-7. [Article]
Details5. Cytochrome P450 1A2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details6. Cytochrome P450 2B6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details7. Cytochrome P450 2C8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details8. Cytochrome P450 2C9
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details9. Cytochrome P450 2C18
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C18
Uniprot ID
P33260
Uniprot Name
Cytochrome P450 2C18
Molecular Weight
55710.075 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]
Details10. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M: Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. [Article]

Carriers

Details1. Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Pharmaceuticals and Medical Devices Agency Japan: Report on Istradefylline [Link]
Details2. alpha1-acid glycoprotein (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
NameUniProt ID
Alpha-1-acid glycoprotein 1P02763
Alpha-1-acid glycoprotein 2P19652
References
  1. Pharmaceuticals and Medical Devices Agency Japan: Report on Istradefylline [Link]

Transporters

Details1. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Dungo R, Deeks ED: Istradefylline: first global approval. Drugs. 2013 Jun;73(8):875-82. doi: 10.1007/s40265-013-0066-7. [Article]
  2. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
Details2. ATP-binding cassette sub-family G member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
Details3. Solute carrier organic anion transporter family member 1B1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
  2. Pharmaceuticals and Medical Devices Agency Japan: Report on Istradefylline [Link]
Details4. Solute carrier organic anion transporter family member 1B3
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
Details5. Solute carrier family 22 member 6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
Details6. POU domain, class 2, transcription factor 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
Specific Function
Transcription factor that specifically binds to the octamer motif (5'-ATTTGCAT-3'). Regulates transcription in a number of tissues in addition to activating immunoglobulin gene expression. Modulate...
Gene Name
POU2F2
Uniprot ID
P09086
Uniprot Name
POU domain, class 2, transcription factor 2
Molecular Weight
51208.51 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
Details7. Multidrug and toxin extrusion protein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]
Details8. Multidrug and toxin extrusion protein 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. FDA Approved Drug Products: Istradefylline Oral Tablets [Link]

Drug created at October 20, 2016 20:45 / Updated at February 21, 2021 18:53