Subjective and objective effects of the novel triple reuptake inhibitor tesofensine in recreational stimulant users.
Tesofensine is a (triple) reuptake inhibitor of noradrenaline, dopamine, and serotonin that is in development for the treatment of obesity. The abuse potential of triple reuptake inhibitors is not yet known, and so this study was undertaken to evaluate the potential abuse-related effects of tesofensine in humans. It was designed as a single-dose, randomized, double-blind, crossover study involving tesofensine vs. placebo, D-amphetamine (positive control for dopaminergic/stimulant effects), bupropion, and atomoxetine (negative/unscheduled controls) in recreational stimulant users (N = 52). Subjective and objective measures were assessed for 48 h after drug administration. The study results show that the effects of D-amphetamine were significantly greater than those of placebo on all primary and secondary subjective measures. The effects of tesofensine were not significantly different from those of placebo and were lower than those of D-amphetamine 30 mg on all primary and most secondary measures. The effects of tesofensine were either lower than or not different from those of bupropion or atomoxetine. These results demonstrate that the abuse potential for tesofensine is no greater than that of bupropion or atomoxetine, and tesofensine is therefore unlikely to be recreationally abused.
Schoedel
K A
KA
Kendle Early Stage-Toronto, Ontario, Canada. schoedel.kerri@kendle.com
Meier
D
D
Chakraborty
B
B
Manniche
P M
PM
Sellers
E M
EM
D000293:Adolescent; D000328:Adult; D019969:Amphetamine-Related Disorders / Q000523:psychology; D000069445:Atomoxetine Hydrochloride; D001288:Attention / Q000187:drug effects; D015306:Biogenic Monoamines / Q000037:antagonists & inhibitors*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000009:adverse effects / Q000494:pharmacology*; D016642:Bupropion / Q000494:pharmacology; D000697:Central Nervous System Stimulants; D018592:Cross-Over Studies; D003913:Dextroamphetamine; D018765:Dopamine Uptake Inhibitors / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D023381:Endpoint Determination; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D008297:Male; D008875:Middle Aged; D011437:Propylamines / Q000494:pharmacology; D011597:Psychomotor Performance / Q000187:drug effects; D012959:Socioeconomic Factors; D019966:Substance-Related Disorders / Q000453:epidemiology / Q000523:psychology*; D016896:Treatment Outcome; D055815:Young Adult
D015306:Biogenic Monoamines; D019086:Bridged Bicyclo Compounds, Heterocyclic; D000697:Central Nervous System Stimulants; D018765:Dopamine Uptake Inhibitors; D011437:Propylamines; D016642:Bupropion; D000069445:Atomoxetine Hydrochloride; C518479:Tesofensine; D003913:Dextroamphetamine