A pharmacokinetic evaluation of oral edivoxetine hydrochloride for the treatment of attention deficit-hyperactivity disorder

Abstract

Available data suggest edivoxetine is safe and well tolerated. Edivoxetine is readily absorbed with metabolism proceeding through the CYP hepatic enzyme pathway, with CYP2D6 and CYP3A4 playing the most prominent roles. The tmax is ∼ 2 h post-dose, and the plasma t1/2 is ∼ 4 - 6 h irrespective of the dose. Pharmacokinetic parameters are not substantially different between children and adults. Edivoxetine may be a promising non-stimulant therapeutic agent. However, at present, there is insufficient data available to permit a thorough analysis of its potential place in ADHD pharmacotherapy, or how its PK and pharmacodynamics may differ in clinically meaningful ways from existing agents.

Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas

“…Phase I studies indicate that edivoxetine is safe and well tolerated in healthy volunteers. 197 The absorption of edivoxetine was rapid with an average time to reach maximum plasma concentration (C max ) of 2 h. Edivoxetine is extensively metabolized, predominantly via the cytochrome P450 (CYP) enzyme CYP2D6 and CYP3A4. Following a single dose oral administration of edivoxetine, renal or hepatic impairment patients did not appear to influence overall subject tolerability.…”

“…In addition, edivoxetine dose-dependently displaced the NET-specific PET ligand in rhesus monkeys. Phase I studies indicate that edivoxetine is safe and well tolerated in healthy volunteers . The absorption of edivoxetine was rapid with an average time to reach maximum plasma concentration ( C max ) of 2 h. Edivoxetine is extensively metabolized, predominantly via the cytochrome P450 (CYP) enzyme CYP2D6 and CYP3A4.…”

Reflexiones nerviosas de huecos y de rellenos

“…Y a uno le da la impresión de que muchos prescriptores habrían aceptado sin la menor crí-tica ese viraje. El producto en cuestión, por cierto, se está empezando a estudiar como una alternativa en el TDAH (22), recuperando un camino ya recorrido por otra molécula del mismo propietario, que tras ser probado como un antidepresivo noradrenérgico en los 80 (23) pasó después a convertirse en uno de los medicamentos de referencia para esa indicación; en su viaje hacia una nueva indicación adquirió una "a" al comienzo del nombre con el que previamente era conocida.…”