Istradefylline

Istradefylline
Clinical data
Trade namesNouriast, Nourianz
Other namesKW-6002
AHFS/Drugs.comMonograph
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding98%
MetabolismMainly CYP1A1, CYP3A4, and CYP3A5
Elimination half-life64–69 hrs
Excretion68% faeces, 18% urine
Identifiers
  • 8-[(E)-2-(3,4-dimethoxyphenyl)vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione
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 mass384.436 g·mol−1
3D model (JSmol)
  • O=C2N(c1nc(n(c1C(=O)N2CC)C)\C=C\c3ccc(OC)c(OC)c3)CC
  • 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+ checkY
  • Key:IQVRBWUUXZMOPW-PKNBQFBNSA-N checkY
  (verify)

Istradefylline, sold under the brand name Nourianz, is a medication used as an add-on treatment to levodopa/carbidopa in adults with Parkinson's disease (PD) experiencing "off" episodes.[2][3][4] Istradefylline reduces "off" periods resulting from long-term treatment with the antiparkinson drug levodopa.[2] 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.[2]

Relatively common side effects include involuntary muscle movements (dyskinesia), constipation, hallucinations, dizziness and, much like its parent molecule caffeine, nausea and sleeplessness.[2]

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[5]

  1. ^ "Nourianz- istradefylline tablet, film coated". DailyMed. Retrieved 4 January 2021.
  2. ^ 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. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ^ "Drug Trials Snapshots: Nourianz". U.S. Food and Drug Administration (FDA). 23 September 2019. Archived from the original on 20 November 2019. Retrieved 19 November 2019. Public Domain This article incorporates text from this source, which is in the public domain.
  4. ^ 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. S2CID 85456263.
  5. ^ "New Drug Therapy Approvals 2019". U.S. Food and Drug Administration. 31 December 2019. Retrieved 15 September 2020. Public Domain This article incorporates text from this source, which is in the public domain.