istradefylline

Ligand id: 5608

Name: istradefylline

Structure and Physico-chemical Properties

2D Structure
Click here for structure editor
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 0
Rotatable bonds 6
Topological polar surface area 80.28
Molecular weight 384.18
XLogP 4.05
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Istradefylline was approved for use in Japan for several years prior to its 2019 FDA approval [2]. 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.