Istradefylline is a selective adenosine A2A receptor antagonist used as an adjunctive treatment for patients with Parkinson's disease experiencing "off" episodes while receiving levodopa/carbidopa therapy. It belongs to the xanthine derivative class and acts primarily by blocking adenosine A2A receptors in the basal ganglia.
Istradefylline is a non-dopaminergic antiparkinsonian agent. Unlike levodopa and dopamine agonists, it does not directly replace or stimulate dopamine. By antagonizing A2A receptors, Istradefylline modulates signaling pathways involved in motor control and may help reduce periods when Parkinson's disease symptoms return or worsen between levodopa doses.
Istradefylline is identified by CAS Number 155270-99-8. It has the molecular formula C10H10N4O2 and a molecular weight of 218.21 g/mol. It is a synthetic xanthine derivative containing a purine-2,6-dione core with a styryl substituent.
Istradefylline is generally described as a pale yellow to yellow crystalline powder. It is practically insoluble in water and has greater solubility in selected organic solvents. Its lipophilic character allows it to cross the blood-brain barrier and exert activity within the central nervous system.
Istradefylline selectively antagonizes adenosine A2A receptors. A2A receptors are highly expressed in the striatum and are functionally associated with dopamine D2 receptor signaling. Blocking these receptors modifies indirect-pathway signaling within the basal ganglia and can improve motor function in Parkinson's disease.
Istradefylline is used as an adjunctive treatment to levodopa/carbidopa in adults with Parkinson's disease who experience "off" episodes. It is administered orally and is intended to complement, rather than replace, dopaminergic therapy.
Pharmaceutical Istradefylline can be characterized using validated chromatographic and spectroscopic analytical methods. HPLC may be used for assay and related-substance determination, while appropriate spectroscopic and chromatographic procedures may be used for identity testing.
Quality control of Istradefylline API should include identity, assay, related substances, water content, residual solvents, elemental impurities and other applicable parameters according to the approved drug-substance specification.
Istradefylline should be stored in a tightly closed container under controlled pharmaceutical storage conditions. The material should be protected from excessive heat, moisture, light and contamination. Specific storage requirements should follow the applicable manufacturer specification and Certificate of Analysis.
Istradefylline API may be supplied for pharmaceutical manufacturing, formulation development, analytical testing and other qualified pharmaceutical applications. Product specifications, Certificate of Analysis, packaging configuration and regulatory documentation should be confirmed according to the intended application.
For Istradefylline API requirements, customers can request product specifications, analytical documentation, Certificate of Analysis, packaging information and commercial details. Quality parameters should be evaluated against the applicable pharmaceutical specification before procurement.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | Approximately 193–195°C |