Phase II trials of A2a receptor antagonists
 

Companies present Phase II data for emerging class of Parkinson's drugs at the AAN
16 April 2010
Asher Mullard
Data from two promising adenosine A2a receptor antagonists – Vernalis/ Biogen Idec's vipadenant (formerly known as BIIB014) and Synosia's SYN115 – was presented this week at the American Academy of Neurology (AAN) meeting in Toronto.

Clin Neuropharmacol. 2010 Mar-Apr;33(2):55-60.
An open-label, positron emission tomography study to assess adenosine A2A brain receptor occupancy of vipadenant (BIIB014) at steady-state levels in healthy male volunteers.
Brooks DJ, Papapetropoulos S, Vandenhende F, Tomic D, He P, Coppell A, O'Neill G.

Division of Neuroscience and Mental Health, Faculty of Medicine, Imperial College London, London, UK.

Abstract
OBJECTIVE: Adenosine A2A receptor antagonists are potential new treatments for Parkinson disease. We used positron emission tomography (PET) of the A2A receptor radiotracer, [C]SCH442416, to assess binding of the novel A2A antagonist, vipadenant (previously known as BIIB014), to human brain A2A receptors and to investigate the relationship among dose, steady-state plasma levels, and receptor occupancy. .. CONCLUSIONS: This study provides the first evidence that vipadenant occupies A2A receptors in the human brain. Receptor occupancy was related to both dose and plasma levels of vipadenant. These results, coupled with previous efficacy results in animals, justify continued development of vipadenant as a potential treatment for Parkinson disease.

PMID: 20375654 [PubMed - in process]
http://www.ncbi.nlm.nih.gov/pubmed/20375654

http://www.medicalnewstoday.com/articles/185600.php
Synosia Therapeutics' SYN-115 Improves Motor And Non-Motor Function In Patients With Mild- To-Moderate Parkinson's Disease


Synosia Therapeutics today announced the presentation of data from a phase 2a clinical study of the company's adenosine 2a (A2a) receptor antagonist (SYN-115) in Parkinson's disease. The data demonstrate that SYN-115 significantly improves measures of motor and non-motor function in patients with Parkinson's disease (PD) either alone or in combination with levodopa. The results also clearly illustrate the value of perfusion magnetic resonance imaging (MRI) as a tool to rapidly evaluate the pharmacodynamic effects of new drugs in the brain..