Peer-Reviewed Publication
Psychopharmacology (Berl)2026;243(3):565-580.March 1, 2026Journal Article
Ascending single-dose study of the safety, pharmacokinetics, and pharmacodynamics of CSTI-500, a novel monoamine triple reuptake inhibitor, first-in-human.
Lieuwe Appel1,2, Robert Risinger3, Anders Wall4,5, Harald Murck6,7, Shuang Liu8, Gunnar Antoni5,9, Roger Lane10
1Molecular Imaging and Medical Physics, Department of Surgical Sciences, Uppsala University, Uppsala, Sweden. lieuwe.appel@akademiska.se.
2PET Centre, Department of Medical Imaging, Uppsala University Hospital, 75185, Uppsala, Sweden. lieuwe.appel@akademiska.se.
3BioXcel Therapeutics Inc., 555 Long Wharf Drive, New Haven, CT, 06511, USA.
4Molecular Imaging and Medical Physics, Department of Surgical Sciences, Uppsala University, Uppsala, Sweden.
5PET Centre, Department of Medical Imaging, Uppsala University Hospital, 75185, Uppsala, Sweden.
6Philipps-University Marburg, Marburg, Germany.
7Murck-Neuroscience LLC Westfield, Westfield, NJ, USA.
8ConSynance Therapeutics, Inc., 11 University Place, Rensselaer, NY, 12144, USA.
9Department of Medical Chemistry, Uppsala University, Uppsala, Sweden.
10Ionis Pharmaceuticals, Inc., 2855 Gazelle Court, Carlsbad, CA, 92010, USA.
Abstract
RATIONALE: Monoamine triple reuptake inhibitors (TRIs) inhibit central dopamine, norepinephrine, and serotonin transporters, restoring functional monoamine neurotransmission.
OBJECTIVES: This clinical trial evaluated the safety, tolerability, and pharmacokinetics in healthy volunteers after single-ascending-doses (SAD) of the novel monoamine TRI CSTI-500. In addition, we estimated the peak and du…
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