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Istradefylline (KW-6002)
Istradefylline is an adenosine A2A receptor antagonist that blocks inhibitory signaling in the basal ganglia, thereby enhancing dopaminergic motor control.
Istradefylline is an adenosine A2A receptor antagonist that blocks inhibitory signaling in the basal ganglia, thereby enhancing dopaminergic motor control. Used for Parkinson's disease with motor fluctuations in patients on levodopa therapy.
At a glance
| Generic name | Istradefylline (KW-6002) |
|---|---|
| Sponsor | Kyowa Kirin, Inc. |
| Drug class | Adenosine A2A receptor antagonist |
| Target | Adenosine A2A receptor |
| Modality | Small molecule |
| Therapeutic area | Neurology |
| Phase | Phase 3 |
Mechanism of action
By selectively antagonizing adenosine A2A receptors on GABAergic neurons in the striatum, istradefylline reduces inhibitory tone on motor output pathways. This potentiates dopamine signaling and improves motor symptoms in Parkinson's disease, particularly in patients experiencing motor fluctuations and "off" periods despite levodopa therapy.
Approved indications
- Parkinson's disease with motor fluctuations in patients on levodopa therapy
Common side effects
- Dyskinesia
- Nausea
- Dizziness
- Headache
- Insomnia
Key clinical trials
- Adenosine 2A Receptor Antagonism and AIH in ALS (PHASE1, PHASE2)
- Combining Low Oxygen Therapy and an Adenosine A2a Receptor Antagonist to Improve Functional Mobility After Spinal Cord Injury (PHASE1, PHASE2)
- Effect of Istradefylline Treatment on Behavioral Measures of Apathy in Parkinson's Disease.
- Istradefylline for Parkinson Disease With Cognitive Impairment (PHASE2)
- Istradefylline Effect Protocol on Parkinson's Disease Tremor (PHASE4)
- An Extension of Istradefylline in North American Parkinson's Disease Patients Who Have Completed Study 6002-INT-001 (PHASE3)
- 12-Week, Double-Blind, Placebo-Controlled Study of 20 and 60 mg/Day Istradefylline in Parkinson's Disease Patients on Levodopa/Carbodopa (PHASE2)
- A Study of Istradefylline (KW-6002) in Treating Patients With Parkinson's Disease on Levodopa (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Istradefylline (KW-6002) CI brief — competitive landscape report
- Istradefylline (KW-6002) updates RSS · CI watch RSS
- Kyowa Kirin, Inc. portfolio CI