Date: 2012-12-12
Type of information:
phase: Receptor Occupancy study
Announcement: results
Company: Vernalis (UK)
Product: V81444 (adenosine A2A receptor antagonist)
Action
mechanism: A2A receptor antagonists are believed to have advantages over conventional dopaminergic strategies, in that they may be able to help restore motor function in patients with Parkinson’s Disease (PD), without the side effects commonly associated with today’s treatments.
Disease: Parkinson’s Disease
other CNS indications
Therapeutic area: Neurodegenerative diseases - CNS diseases
Country:
Trial
details: The RO study examined the relationship between dose, plasma concentration and blockade of the A2A receptor using positron emission tomography (PET) scanning and included a preliminary evaluation, using functional MRI (fMRI), of the effects of V81444 on cognitive function.
Latest
news: * On December 12, 2012,Vernalis has announced successful results from a Receptor Occupancy (RO) study with V81444, its A2A antagonist which has potential applications in Parkinson’s disease and other CNS indications. The RO study demonstrated that full A2A blockade could be achieved with single doses that were within the range of doses previously shown to be well tolerated with no safety concerns. The RO study has provided confirmation of the appropriate dose to be used in the forthcoming clinical proof-of-concept trial.
Vernalis now plans to initiate, in the first half of next year, a Phase IIa proof-of-concept study to further evaluate the pharmacokinetics, safety and tolerability of V81444 in patients, together with an evaluation of efficacy in a target patient population.
* On August 22, 2012,Vernalis plc has announced it has dosed the first subject in a Receptor Occupancy study with V81444 which aims to demonstrate A2A activity in man. Following the successful outcome of the Phase I single and multiple ascending dose study announced on 2 May which showed a good safety and tolerability profile in healthy volunteers, the Receptor Occupancy study will examine the relationship between dose, plasma concentration and blockade of the A2A receptor using positron emission tomography (PET) scanning. The trial will also include a preliminary evaluation, using functional MRI (fMRI), of the effects of V81444 on cognitive function. The results are expected by the end of 2012.
