Development and validation of an LC–MS/MS method for the quantitative analysis of the adenosine A2a receptor antagonist NIR178 and its monohydroxy metabolite in human plasma: Application to clinical pharmacokinetics

2020 ◽  
Vol 34 (10) ◽  
Author(s):  
Olivier Heudi ◽  
Nathalie Plaud ◽  
Celine Aumonier ◽  
Shari Wu ◽  
Panos Hatsis ◽  
...  
Keyword(s):  
Quantitative Analysis ◽  
Receptor Antagonist ◽  
Human Plasma ◽  
Adenosine A2a Receptor ◽  
Clinical Pharmacokinetics ◽  
A2a Receptor ◽  
Adenosine A2a Receptor Antagonist ◽  
Adenosine A2a ◽  
Development And Validation

scholarly journals PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders

2018 ◽  
Vol 9 ◽  
Author(s):  
Fabiana Núñez ◽  
Jaume Taura ◽  
Juan Camacho ◽  
Marc López-Cano ◽  
Víctor Fernández-Dueñas ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Movement Disorders ◽  
Adenosine A2a Receptor ◽  
Rodent Models ◽  
A2a Receptor ◽  
Adenosine A2a Receptor Antagonist ◽  
Adenosine A2a

scholarly journals Efficacy of Istradefylline, an Adenosine A2A Receptor Antagonist, as Adjunctive Therapy to Levodopa in Parkinson’s Disease: A Pooled Analysis of 8 Phase 2b/3 Trials

2021 ◽  
pp. 1-13
Author(s):  
Robert A. Hauser ◽  
Nobutaka Hattori ◽  
Hubert Fernandez ◽  
Stuart H. Isaacson ◽  
Hideki Mochizuki ◽  
...  
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Receptor Antagonist ◽  
Repeated Measures ◽  
Pooled Analysis ◽  
Adenosine A2a Receptor ◽  
A2a Receptor ◽  
Adenosine A2a Receptor Antagonist ◽  
Adenosine A2a ◽  
Off Time

Background: Istradefylline is a selective adenosine A2A receptor antagonist for the treatment of patients with Parkinson’s disease (PD) experiencing OFF episodes while on levodopa/decarboxylase inhibitor. Objective: This pooled analysis of eight randomized, placebo-controlled, double-blind phase 2b/3 studies evaluated the efficacy and safety of istradefylline. Methods: Istradefylline was evaluated in PD patients receiving levodopa with carbidopa/benserazide and experiencing motor fluctuations. Eight 12- or 16-week trials were conducted (n = 3,245); four of these studies were the basis for istradefylline’s FDA approval. Change in OFF time as assessed in patient-completed 24-h PD diaries at Week 12 was the primary endpoint. All studies were designed with common methodology, thereby permitting pooling of data. Pooled analysis results from once-daily oral istradefylline (20 and 40 mg/day) and placebo were evaluated using a mixed-model repeated-measures approach including study as a factor. Results: Among 2,719 patients (placebo, n = 992; 20 mg/day, n = 848; 40 mg/day, n = 879), OFF hours/day were reduced at Week 12 at istradefylline dosages of 20 mg/day (least-squares mean difference [LSMD] from placebo in reduction from baseline [95%CI], –0.38 h [–0.61, –0.15]) and 40 mg/day (–0.45 h [–0.68, –0.22], p <  0.0001); ON time without troublesome dyskinesia (ON-WoTD) significantly increased. Similar results were found in the four-study pool (OFF hours/day, 20 mg/day, –0.75 h [–1.10, –0.40]; 40 mg/day, –0.82 h [–1.17, –0.47]). Istradefylline was generally well-tolerated; the average study completion rate among istradefylline-treated patients across all studies was 89.2%. Dyskinesia was the most frequent adverse event (placebo, 9.6%; 20 mg/day, 16.1%; 40 mg/day, 17.7%). Conclusion: In this pooled analysis, istradefylline significantly improved OFF time and ON-WoTD relative to placebo and was well-tolerated.

CSC, an adenosine A2A receptor antagonist and MAO B inhibitor, reverses behavior, monoamine neurotransmission, and amino acid alterations in the 6-OHDA-lesioned rats

2008 ◽  
Vol 1191 ◽  
pp. 192-199 ◽  
Author(s):  
Lissiana M.V. Aguiar ◽  
Danielle S. Macêdo ◽  
Silvania M.M. Vasconcelos ◽  
Aline A. Oliveira ◽  
F. Cléa F. de Sousa ◽  
...  
Keyword(s):  
Amino Acid ◽  
Receptor Antagonist ◽  
Adenosine A2a Receptor ◽  
Mao B ◽  
A2a Receptor ◽  
Adenosine A2a Receptor Antagonist ◽  
Adenosine A2a
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