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Last update 04 Dec 2025
APD-916
Last update 04 Dec 2025
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms APD 916, APD916 |
Target |
Action inverse agonists |
Mechanism H3 receptor inverse agonists(Histamine H3 receptor inverse agonists) |
Therapeutic Areas |
Active Indication- |
Inactive Indication |
Originator Organization |
Active Organization- |
Inactive Organization |
License Organization- |
Drug Highest PhasePendingPhase 1 |
First Approval Date- |
Regulation- |
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Structure/Sequence
Molecular FormulaC29H39NO10S |
InChIKeyVKBJTEGIYYKTCH-FSRHSHDFSA-N |
CAS Registry1021169-72-1 |
Related
1
Clinical Trials associated with APD-916NCT01093508
Phase 1, Randomized, Double-Blind, Placebo-Controlled, Single-Dose Escalation Study to Assess the Tolerability and Pharmacokinetics of APD916 Administered to Healthy Adult Subjects
100 Clinical Results associated with APD-916
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100 Translational Medicine associated with APD-916
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100 Patents (Medical) associated with APD-916
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1
Literatures (Medical) associated with APD-91601 Jan 2012Bioorganic & medicinal chemistry lettersQ4 · MEDICINE
Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)
Q4 · MEDICINE
Article
Author: Santora, Vincent J. ; Schultz, Jeffrey A. ; Hayashi, Rena ; Park, Douglas M. ; Semple, Graeme ; Lorea, Jodie ; Estrada, Scott A. ; Gallardo, Charlemagne ; Grottick, Andrew J. ; Ren, Albert ; Covel, Jonathan A. ; Smith, Brian M. ; Ibarra, Jason B. ; Frazer, John ; Smith, Jeffrey M. ; Hart, Ryan ; Suarez, Marissa ; Hofilena, Brian J. ; Hauser, Erin K. ; Edwards, Jeffrey E.
The design of a new clinical candidate histamine-H(3) receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by replacement of the sulfonamide linkage with a sulfone. One compound from this series, 2j (APD916) increased wakefulness in rodents as measured by polysomnography with a duration of effect consistent with its pharmacokinetic properties. The identification of a suitable salt form of 2j allowed it to be selected for further development.
100 Deals associated with APD-916
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R&D Status
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Narcolepsy | Phase 1 | United States | 01 Mar 2010 |
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