Enerisant is an experimental drug under investigation as a potential treatment for sleep-wake disorders, particularly narcolepsy.

[1][2][3] Enerisant functions as a potent and highly selective antagonist/inverse agonist of the histamine H3 receptor.

This mechanism of action is similar to that of pitolisant, a currently approved H3 receptor antagonist/inverse agonist for narcolepsy; however, enerisant has demonstrated greater affinity and selectivity for the H3 receptor in preclinical studies.

[1][2][3][4][5] By blocking H3 receptors, enerisant increases histamine release from histaminergic neurons, leading to stimulation of postsynaptic histamine H1 receptors, a key mechanism in promoting wakefulness[1][3][4] Enerisant exhibits minimal metabolism in humans and is primarily eliminated unchanged via renal excretion.

After oral administration, it rapidly absorbs and exhibits dose-dependent plasma concentrations.