Istradefylline
Active Pharmaceutical Ingredients 2025-03-03
English Synonyms 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione
Catalog ID99715
CAS NO.155270-99-8
Purity 98%
MDL NumberMFCD00928421
EINEColecular FormulaC20H24N4O4
Molecular Weight 384.434
| Category | Content |
|---|---|
| Generic Name | Istradefylline |
| Brand Name | Nourianz |
| Drug Class | Adenosine A2A Receptor Antagonist |
| Mechanism of Action | Istradefylline is a selective antagonist of the adenosine A2A receptor (A2AR). It is believed to improve motor function in Parkinson’s disease by modulating the activity of these receptors in the basal ganglia. |
| Indications | Used as an adjunct to levodopa and carbidopa for the treatment of “off” episodes in adults with Parkinson’s disease. |
| Dosage Forms | Tablets (20 mg, 40 mg) |
| Administration | Oral, once daily, with or without food. Dose adjustments may be necessary for patients with moderate hepatic impairment or those who smoke. |
| Pharmacokinetics | – Bioavailability: High oral bioavailability.<br>- Elimination: Primarily hepatic metabolism.<br>- Half-life: Approximately 10 hours. |
| Side Effects | Common: Nausea, headache, insomnia, dizziness.<br> Serious: Worsening of dyskinesia or psychiatric symptoms. |
| Precautions | – Monitor for worsening of dyskinesia or psychiatric symptoms.<br>- Use with caution in patients with moderate hepatic impairment.<br>- Not recommended in severe hepatic impairment. |
| Storage | Store at room temperature, protect from moisture. |
| Developer | Kyowa Hakko Kirin Co., Ltd. |
| Approval Date | Approved by the FDA in August 2019 |
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