Ledasorexton

Ledasorexton
Clinical data
Other names	E-2086; E2086
Routes of; administration	Oral
Drug class	Orexin OX2 receptor agonist; Wakefulness-promoting agent
Identifiers
	IUPAC name (2R)-2-cyclopropyl-2-[(1S,5R)-3-[(3S,4R)-1-(5-fluoropyrimidin-2-yl)-3-methoxypiperidin-4-yl]-8-azabicyclo[3.2.1]octan-8-yl]acetamide;
CAS Number	2758363-88-9;
PubChem CID	162702128;
ChemSpider	133324961;
UNII	YF7U7E62EL;
ChEMBL	ChEMBL5795221;
Chemical and physical data
Formula	C22H32FN5O2
Molar mass	417.529 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CO[C@@H]1CN(CC[C@@H]1C2C[C@H]3CC[C@@H](C2)N3[C@H](C4CC4)C(=O)N)C5=NC=C(C=N5)F;
	InChI InChI=1S/C22H32FN5O2/c1-30-19-12-27(22-25-10-15(23)11-26-22)7-6-18(19)14-8-16-4-5-17(9-14)28(16)20(21(24)29)13-2-3-13/h10-11,13-14,16-20H,2-9,12H2,1H3,(H2,24,29)/t14?,16-,17+,18-,19-,20-/m1/s1; Key:AXOUSJFGEOVDQT-GFVFYWETSA-N;

Ledasorexton (INNTooltip International Nonproprietary Name; developmental code name E-2086) is a selective orexin OX₂ receptor agonist which is under development for the treatment of narcolepsy.^[1]^[2] It is taken orally.^[1] The drug is under development by Eisai.^[1]^[2] As of May 2026, it is in phase 2 clinical trials for narcolepsy.^[1]^[2]

References

^ ^a ^b ^c ^d ^e "Ledasorexton". AdisInsight. 27 May 2026. Retrieved 5 June 2026.
^ ^a ^b ^c "Delving into the Latest Updates on Ledasorexton with Synapse". Synapse. 23 May 2026. Retrieved 5 June 2026.

[AdisInsight-1] "Ledasorexton". AdisInsight. 27 May 2026. Retrieved 5 June 2026.

[Synapse-2] "Delving into the Latest Updates on Ledasorexton with Synapse". Synapse. 23 May 2026. Retrieved 5 June 2026.

[1]

[2]

Wakefulness-promoting agents
Catecholaminergic agents	Dopamine reuptake inhibitors (DRIs): Adrafinil^‡ Armodafinil Esmodafinil Mesocarb^‡ Modafinil Phenylpiracetam (fonturacetam) Norepinephrine reuptake inhibitors (NRIs): Atomoxetine Desipramine Reboxetine Viloxazine Norepinephrine–dopamine reuptake inhibitors (NDRIs): Amineptine^‡ Bupropion Dexmethylphenidate Methylphenidate Nomifensine^‡ Serdexmethylphenidate Solriamfetol Serotonin–norepinephrine–dopamine reuptake inhibitors (SNDRIs): Mazindol Norepinephrine releasing agents (NRAs): Ephedrine Pseudoephedrine Selegiline (via metabolites) Norepinephrine–dopamine releasing agents (NDRAs): Amphetamine Dextroamphetamine Levoamphetamine^‡ Lisdexamfetamine Methamphetamine Mixed amphetamine salts Pemoline^‡
Orexin receptor agonists	Alixorexton^§ Balumorexton^§ Cleminorexton^§ Danavorexton^§ Firazorexton^§ Ledasorexton^§ Oveporexton^†
Histamine H₃ receptor antagonists	Pitolisant Samelisant^§
Adenosine receptor antagonists	Caffeine Istradefylline Paraxanthine
Others	GABA_A receptor antagonists and negative allosteric modulators (e.g., clarithromycin, flumazenil, pentylenetetrazol (pentetrazol)) GABA_B receptor agonists (e.g., sodium oxybate/γ-hydroxybutyrate (GHB)) (via improved nightly sleep) Nicotinic acetylcholine receptor agonists (e.g., nicotine)
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III
See also: Stimulants List of investigational narcolepsy and hypersomnia drugs

See also

References