VRAYLAR mechanism of action

VRAYLAR is the first and only dopamine and serotonin partial agonist approved for depressive and manic or mixed episodes associated with bipolar I disorder.1

The MOA of VRAYLAR is unknown. The efficacy of VRAYLAR is thought to occur through activity at the following receptors1:

Partial agonism: an adaptive response mechanism23

As a partial agonist, VRAYLAR theoretically acts as either an agonist or antagonist depending on the current concentration of central dopamine D2 and serotonin 5-HT1A neurotransmitters in the brain.1,23

Theoretical role of partial agonist23

During high dopamine or serotonin concentration

Helps inhibit receptors by acting as a functional antagonist

During low dopamine or serotonin concentration

Helps activate receptors by acting as a functional agonist

MOA=mechanism of action.

Pharmacodynamics

VRAYLAR is shown to have a higher dopamine D3 binding affinity than that of endogenous dopamine24

VRAYLAR receptor-binding affinity1

Cariprazine demonstrated up to ~8-fold greater in vitro affinity for dopamine D3 vs D2 receptors.1

The clinical significance of these in vitro data is unknown.

Cariprazine demonstrated up to ~8-fold greater in vitro affinity for dopamine D3 vs D2 receptors.1

The clinical significance of these in vitro data is unknown.

VRAYLAR has no appreciable affinity for cholinergic muscarinic receptors (IC50 >1000 nM).1

Ki (inhibitory constant) value represents the binding strength between a medication and a specific receptor. The smaller the Ki value, the greater the binding affinity to that receptor.

nM=nanomolar.