Istradefylline

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Istradefylline
Istradefylline.svg
Clinical data
Trade namesNourianz
SynonymsKW-6002
AHFS/Drugs.comMonograph
License data
Routes of
administration
By mouth
ATC code
  • none
Legal status
Legal status
Pharmacokinetic data
Protein binding98%
MetabolismMainly CYP1A1, CYP3A4, and CYP3A5
Elimination half-life64–69 hrs
Excretion68% faeces, 18% urine
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.230.117 Edit this at Wikidata
Chemical and physical data
FormulaC20H24N4O4
Molar mass384.429 g/mol g·mol−1
3D model (JSmol)
  (verify)

Istradefylline, sold under the brand name Nourianz, is a medication used to treat Parkinson's disease (PD).[1][2] Istradefylline reduces "off" periods resulting from long-term treatment with the antiparkinson drug levodopa.[1] An "off" episode is a time when a patient's medications are not working well, causing an increase in PD symptoms, such as tremor and difficulty walking.

Relatively common side effects include involuntary muscle movements (dyskinesia), constipation, hallucinations, dizziness and, much like its parent molecule caffeine, nausea and sleeplessness.[1] It is a selective antagonist at the A2A receptor. It was first approved in Japan in 2013.[3] It was approved by the Food and Drug Administration (FDA) in the United States in 2019.[1]

References[edit]

  1. ^ a b c d "FDA approves new add-on drug to treat off episodes in adults with Parkinson's disease". U.S. Food and Drug Administration (FDA) (Press release). 27 August 2019. Archived from the original on 4 September 2019. Retrieved 29 August 2019.
  2. ^ Cabreira V, Soares-da-Silva P, Massano J (April 2019). "Contemporary Options for the Management of Motor Complications in Parkinson's Disease: Updated Clinical Review". Drugs. 79 (6): 593–608. doi:10.1007/s40265-019-01098-w. PMID 30905034.
  3. ^ Dungo R, Deeks ED (June 2013). "Istradefylline: first global approval". Drugs. 73 (8): 875–82. doi:10.1007/s40265-013-0066-7. ISSN 1179-1950. PMID 23700273.