 | |
| Clinical data | |
|---|---|
| Other names | TS-091 |
| Routes of administration | By mouth |
| Pharmacokinetic data | |
| Protein binding | 31.0–31.7%[1] |
| Eliminationhalf-life | 8 hours[1] |
| Excretion | Kidney (64.5–89.9%)[1] |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| IUPHAR/BPS | |
| ChemSpider | |
| UNII | |
| Chemical and physical data | |
| Formula | C22H30N4O3 |
| Molar mass | 398.507 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Enerisant is an experimental drug under investigation as a potential treatment fornarcolepsy. It is a member of thehistamine H3 receptor antagonist/inverse agonist class of medications.[1][2][3]
Enerisant functions as a potent and highly selective antagonist/inverse agonist of thehistamine H3 receptor. This mechanism of action is similar to that ofpitolisant, 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 postsynaptichistamine 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. 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.[1][5]