Enerisant
chemical compound

Enerisant (INNTooltip International Nonproprietary Name; developmental code name TS-091) is an experimental drug under investigation as a potential treatment for narcolepsy. It is a member of the histamine H3 receptor antagonist/inverse agonist class of medications.
Pharmacology
Pharmacodynamics
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. 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
Pharmacokinetics
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. Within 48 hours, 64.5-89.9% of the administered dose is recovered unchanged in urine. Plasma protein binding is approximately 31.0–31.7% in humans.
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Datasets, specimens, observations and peer-reviewed methods provide the appropriate test for the technical claims summarized here. The source revision retrieved here is dated Dec 21, 2025. The linked authority identifier is Q27276798. None of the 0 selected statements returned an explicit reference.
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This entry incorporates text from “Enerisant” on English Wikipedia. Contributors are listed in the page history. Text is available under the Creative Commons Attribution-ShareAlike 4.0 License. Selected authority identifiers and statements are retrieved from Wikidata under CC0; their references and qualifiers remain part of the verification path.