Drug intelligence / Profile preview

Istradefylline

Development stage
Approved
Lead developer
Kyowa Kirin
Modality
Small Molecules
Administration
Oral
01

Overview

Istradefylline is a selective adenosine A2A receptor antagonist used as an adjunct to levodopa and carbidopa for the treatment of "off" episodes in adults with Parkinson's disease. Unlike standard dopaminergic therapies, it works by blocking adenosine A2A receptors in the basal ganglia, a brain region involved in motor control. This mechanism helps regulate GABAergic neurotransmission without directly affecting dopamine pathways, thereby reducing excessive activation of the indirect striato-pallidal pathway associated with motor symptoms in Parkinson's disease. Istradefylline was developed by Kyowa Hakko Kirin and first approved in Japan in 2013 and later by the FDA in 2019[1][3][6].

Brand names
Nourianz
Other names
istradefyllineKW-6002KW6002KW 6002
02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)

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