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Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
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Bioavailability is a crucial pharmacokinetic parameter that quantifies the proportion of an administered drug that reaches the systemic circulation and is available for therapeutic action. Regulatory agencies mandate the assessment of bioavailability, typically measured as the area under the drug plasma concentration-versus-time curve (AUC), to ensure the efficacy and safety of pharmaceutical products. These evaluations are categorized as absolute and relative bioavailability studies.Absolute...
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Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
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Absolute Bioavailability of Tasimelteon.

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|February 7, 2015
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Tasimelteon, a treatment for Non-24-Hour Sleep-Wake Disorder, showed 38% absolute bioavailability. This dual melatonin receptor agonist was well-tolerated in healthy volunteers across oral and IV administration routes.

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Area of Science:

  • Pharmacology
  • Clinical Pharmacology
  • Sleep Medicine

Background:

  • Tasimelteon is the first FDA-approved treatment for Non-24-Hour Sleep-Wake Disorder.
  • It functions as a dual melatonin receptor agonist.

Purpose of the Study:

  • To assess the absolute bioavailability of tasimelteon.
  • To evaluate single-dose pharmacokinetics, safety, and tolerability of oral and intravenous (IV) tasimelteon.

Main Methods:

  • An open-label, randomized, crossover study involving 14 healthy volunteers.
  • Subjects received single oral (20-mg capsule) and IV (2-mg infusion) doses of tasimelteon.
  • A washout period of 5 ± 2 days separated the treatments.

Main Results:

  • Absolute bioavailability of tasimelteon was 38% (90% CI: 27%-54%).
  • Total clearance was 505 mL/min and volume of distribution was 42.7 L for IV administration.
  • Oral-to-IV exposure ratios for metabolites suggest first-pass metabolism. Elimination half-life was consistent between routes.
  • Mild, treatment-emergent adverse events occurred in 21.4% of subjects, with no serious events or discontinuations.

Conclusions:

  • Tasimelteon demonstrates moderate absolute bioavailability.
  • The drug is well-tolerated via both oral and IV routes in healthy individuals.
  • Evidence of presystemic metabolism was observed.