Istradefylline is a selective adenoside A2A receptor antagonist indicated in adjunct to levodopa and carbidopa for the treatment of Parkinson's Disease. Istradefylline, or KW6002, was developed by Kyowa Hakko Kirin in Japan for the treatment of Parkinson's disease as an adjunct to standard therapy.
- Mechanism
- Curator reviewed · 6 references
Istradefylline is a selective adenosine A2A receptor inhibitor. These receptors are found in the basal ganglia, a region of the brain that suffers degeneration in Parkinson's disease, and is also significantly involved in motor control. A2A receptors are also expressed on GABAergic medium spiny neurons within the indirect striato-pallidal pathway. The GABAergic action of this pathway is thereby reduced. Istradefylline has 56 times the affinity for A2A receptors than A1 receptors.
- Primary indication
- Istradefylline is indicated in adjunct to levodopa and carbidopa in the treatment of Parkinson's disease.Curator reviewed · 1 structured indication
- Formula / weight
- C20H24N4O4 · 384.436 g/mol (avg)
- First approval
- United States, 2019
- Code names
- KW-6002
- Brand names
Resolves to
IQVRBWUUXZMOPW-PKNBQFBNSA-NSMILES[H]\C(=C(\[H])C1=CC(OC)=C(OC)C=C1)C1=NC2=C(N1C)C(=O)N(CC)C(=O)N2CCWhat you can answer from here — as of November 03, 2025
Which drugs share a target with Istradefylline, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account