Istradefylline

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.[1][2][3] 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.[1]

Istradefylline
Clinical data
Trade namesNourianz
Other namesKW-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
Chemical and physical data
FormulaC20H24N4O4
Molar mass384.429 g/mol g·mol−1
3D model (JSmol)
  (verify)

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.

History

It was first approved in Japan in 2013.[4]

The effectiveness of Nourianz in treating "off" episodes in patients with Parkinson's disease who are already being treated with levodopa/carbidopa was shown in four 12-week placebo-controlled clinical studies that included a total of 1,143 participants. In all four studies, people treated with Nourianz experienced a statistically significant decrease from baseline in daily "off" time compared to patients receiving a placebo.[1][2]

It was approved for medical use in the United States in 2019.[1][2] and approval was granted to Kyowa Kirin, Inc.[1]

References
  1. "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. This article incorporates text from this source, which is in the public domain.
  2. "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. This article incorporates text from this source, which is in the public domain.
  3. 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.
  4. 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.


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