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Dasotraline

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https://www.readbyqxmd.com/read/28596833/absorption-distribution-metabolism-and-excretion-of-14-c-dasotraline-in-humans
#1
Yu-Luan Chen, Estela Skende, Jing Lin, Yijun Yi, Peter L Wang, Sarah Wills, H Scott Wilkinson, Kenneth S Koblan, Seth C Hopkins
Dasotraline is a dopamine and norepinephrine reuptake inhibitor, and the early clinical trials show a slow absorption and long elimination half-life. To investigate the absorption, distribution, metabolism, and excretion of dasotraline in humans, a single dose of [(14)C]-dasotraline was administered to eight healthy male adult volunteers. At 35 days, 90.7% of the dosed radioactivity was recovered in the urine (68.3%) and feces (22.4%). The major metabolic pathways involved were: (1) amine oxidation to form oxime M41 and sequential sulfation to form M42 or glucuronidation to form M43; (2) N-hydroxylation and sequential glucuronidation to form M35; (3) oxidative deamination to form (S)-tetralone; (4) mono-oxidation of (S)-tetralone and sequential glucuronidation to form M31A and M32; and (5) N-acetylation to form (1R,4S)-acetamide M102...
February 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/26794682/assessment-of-human-abuse-potential-of-dasotraline-compared-to-methylphenidate-and-placebo-in-recreational-stimulant-users
#2
RANDOMIZED CONTROLLED TRIAL
K S Koblan, S C Hopkins, K Sarma, N Gallina, F Jin, N Levy-Cooperman, K A Schoedel, A Loebel
AIMS: The aim of this study was to evaluate the abuse potential of dasotraline, a novel dopamine and norepinephrine reuptake inhibitor with slow absorption (tmax, 10-12h) and elimination (t1/2=47-77 h) that is in development for the treatment of attention deficit hyperactivity disorder (ADHD). METHODS: Recreational stimulant users (N=48) who had specific experience with cocaine, and who were able to distinguish methylphenidate (60 mg) versus placebo in a qualification session, were randomized, in a 6-period, double-blind, crossover design, to receive single doses of dasotraline 8 mg, 16 mg, and 36 mg, methylphenidate (MPH) 40 mg and 80 mg, and placebo...
February 1, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/26597180/pharmacokinetics-and-exposure-response-relationships-of-dasotraline-in-the-treatment-of-attention-deficit-hyperactivity-disorder-in-adults
#3
Seth C Hopkins, Soujanya Sunkaraneni, Estela Skende, Jeremy Hing, Julie A Passarell, Antony Loebel, Kenneth S Koblan
BACKGROUND AND OBJECTIVES: Dasotraline is a novel inhibitor of dopamine and norepinephrine reuptake currently being investigated in clinical studies for the treatment of attention-deficit/hyperactivity disorder (ADHD). Uniquely, relative to current ADHD medications, dasotraline has a slow absorption and long elimination half-life. Here we relate the pharmacokinetics and pharmacodynamics of dasotraline to reduction in ADHD symptoms based on simulated clinical trial outcomes. METHODS: Dasotraline pharmacokinetics were analyzed by population pharmacokinetic methodologies using data collected from 395 subjects after single or multiple oral dose administrations ranging from 0...
February 2016: Clinical Drug Investigation
https://www.readbyqxmd.com/read/25948101/dasotraline-for-the-treatment-of-attention-deficit-hyperactivity-disorder-a-randomized-double-blind-placebo-controlled-proof-of-concept-trial-in-adults
#4
RANDOMIZED CONTROLLED TRIAL
Kenneth S Koblan, Seth C Hopkins, Kaushik Sarma, Fengbin Jin, Robert Goldman, Scott H Kollins, Antony Loebel
Attention-deficit/hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterized by symptoms of inattention, hyperactivity, and impulsivity associated with clinically significant impairment in functioning. ADHD has an early onset, but frequently persists, with a prevalence estimate of 4% in adults. Dasotraline is a novel compound that is a potent inhibitor of dopamine and norepinephrine transporters that achieves stable plasma concentrations with once-daily dosing. In this study, adult outpatients meeting DSM-IV-TR criteria for ADHD were randomized to 4 weeks of double-blind, once-daily treatment with dasotraline 4 and 8 mg/day or placebo...
November 2015: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
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