Francis M Dijkstra, Rob G J A Zuiker, Pieter S Siebenga, Richard A Leigh-Pemberton, Lei Sun, Joan D Manthis, Marieke L de Kam, Richard Lin, Lisa L von Moltke, David Rezendes, Joop M A van Gerven
AIMS: ALKS 7119 is a novel compound with in vitro affinity highest for the SERT, and for μ receptor, α1A -adrenoceptor, α1B -adrenoceptor, NMDA receptor and sigma non-opioid intracellular receptor 1. This first-in-human study evaluated safety and PK/PD effects of single ascending doses (SAD) of ALKS 7119 in healthy males and compared effects with neurotransmitter modulators with partially overlapping targets. METHODS: In 10 cohorts (n = 10 subjects each), PK, safety and PD (NeuroCart tests, measuring neurophysiologic effects [pupillometry, pharmaco-EEG (pEEG)], visuomotor coordination, alertness, [sustained] attention [saccadic peak velocity, adaptive tracking], subjective drug effects [VAS Bowdle and VAS Bond and Lader] and postural stability [body sway]) were evaluated...
June 2022: British Journal of Clinical Pharmacology