A first-in-class dual antagonist of adenosine receptors for motor and non-motor symptoms treatment in Parkinson’s disease.
CVXL-0069 is a dual A2A/A1 receptor antagonist. It has demonstrated efficacy in increasing the efficacy of levodopa activity in a well recognized preclinical model of Parkinson’s Disease. Its dual A2A and A1 antagonism, addressing both motor and non-motor symptoms of Parkinson’s Disease, makes CVXL-0069 a major advance in patients’ lives.
Adenosine is a neuromodulator involved in a large array of cerebral activities. It engages four receptors of the adenosine receptors family. A specific inhibition of A2A and A1 receptors is expected to improve multiple symptoms of Parkinson’s Disease :
A2A and A1 receptor antagonism synergizes with dopamine signaling in the striatum, and therefore improve motor symptoms
A1 receptors antagonists enhance cognitive function
A2A and A1 antagonists, such as the non-selective antagonist caffeine, decrease risk of treatment- or disease-related somnolence by eliciting active waking
A2A and A1 antagonists have potential to increase dopamine release by the substantia nigra, therefore reducing exogenous dopamine needs in early-stage Parkinson’s Disease
CVXL-0069 is now in preclinical development.
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