- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: KW-6002 | KW6002 | Nourianz®
istradefylline is an approved drug (Japan (2013), FDA (2019))
Compound class: Synthetic organic
Comment: Istradefylline is a high affinity, selective adenosine A2A receptor antagonist. Chemically it is a caffeine analogue. Istradefylline was developed to treat adult Parkinson's disease patients experiencing "OFF" episodes, as an adjunct to levodopa/carbidopa therapy.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.
|Summary of Clinical Use
|Istradefylline was approved for use in Japan for several years prior to its 2019 FDA approval . Istradefylline is indicated as an adjunct to levodopa/carbidopa therapy in adults who are experiencing Parkinson's disease "off" episodes.
|Mechanism Of Action and Pharmacodynamic Effects
|Istradefylline is an adenosine A2A receptor antagonist [1,3]. It is reported that in animal models istradefylline is able to reverse the motor impairments induced by dopamine depletion or antagonism, however this does not appear to translate to human Parkinson's patients with any significant improvement over placebo or levodopa in Phase 3 trial.