Enerisant

Enerisant (TS-091) is an experimental small molecule drug developed by Taisho Pharmaceutical for the treatment of sleep-wake disorders, particularly narcolepsy and hypersomnia. It acts as a potent, highly selective antagonist/inverse agonist of the histamine H3 receptor. By blocking H3 receptors, enerisant increases histamine release from histaminergic neurons in the brain, thereby promoting wakefulness through stimulation of postsynaptic histamine H1 receptors. Enerisant demonstrates over 3,000-fold selectivity for the H3 receptor compared to other histamine receptor subtypes and does not bind to sigma-1 receptors. The drug is orally administered and exhibits minimal metabolism in humans; up to 90% is excreted unchanged via urine within 48 hours after administration. Clinical trials have evaluated its efficacy and safety in patients with narcolepsy[2][4][5][6].

Other names

enerisant