2015
DOI: 10.1097/mjt.0000000000000195
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Absolute Bioavailability of Tasimelteon

Abstract: Tasimelteon is a novel dual melatonin receptor agonist and is the first treatment approved by the US Food and Drug Administration for Non-24-Hour Sleep-Wake Disorder. This study was conducted to assess the absolute bioavailability of tasimelteon and to further assess the single-dose pharmacokinetics, safety, and tolerability of oral and intravenous (IV) routes of administration of the drug. This study was an open-label, single-dose, randomized, 2-period, 2-treatment, 2-sequence, crossover study in which 14 hea… Show more

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Cited by 8 publications
(9 citation statements)
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“…In both preclinical and human studies, timed pulsatile melatonin administration was more efficacious than prolonged administration for phase‐shifting the circadian clock . Because the response of the endogenous clock is time dependent, the timing of administration as well as the pharmacokinetic parameters (Table ) of a given melatonin agonist will likely play a key role in its overall effects on the circadian system.…”
Section: Treatment Of Crswdsmentioning
confidence: 99%
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“…In both preclinical and human studies, timed pulsatile melatonin administration was more efficacious than prolonged administration for phase‐shifting the circadian clock . Because the response of the endogenous clock is time dependent, the timing of administration as well as the pharmacokinetic parameters (Table ) of a given melatonin agonist will likely play a key role in its overall effects on the circadian system.…”
Section: Treatment Of Crswdsmentioning
confidence: 99%
“…One of the primary drawbacks of dietary supplement melatonin is its documented poor and highly variable bioavailability from person to person due to high first‐pass metabolism in the liver, poor gut absorption, or possibly a combination of both factors . The four approved melatonin receptor agonists exhibit a wide range of absolute bioavailability parameters, with an average of 3.3% for agomelatine, 15% for prolonged‐release melatonin, 1.8% for ramelteon, and 38.3% for tasimelteon . It is notable that, in the absence of bioavailability data for the approved prolonged‐release melatonin formulation, the estimate provided for the approved product is based on immediate‐release formulations .…”
Section: Treatment Of Crswdsmentioning
confidence: 99%
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“…Tasimelteon is rapidly and consistently absorbed, with a mean absolute bioavailability of 38% [2]. Tasimelteon is extensively metabolized with CYP1A2 and CYP3A4 being the major isozymes involved in the metabolism of tasimelteon [3].…”
Section: Introductionmentioning
confidence: 99%