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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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Rolapitant Absolute Bioavailability and PET Imaging Studies in Healthy Adult Volunteers.

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Area of Science:

  • Pharmacology
  • Neuroscience

Background:

  • Chemotherapy-induced nausea and vomiting (CINV) is a significant challenge.
  • Neurokinin-1 (NK-1) receptor antagonists offer a therapeutic approach.

Purpose of the Study:

  • To evaluate the absolute bioavailability of oral rolapitant.
  • To assess neurokinin-1 (NK-1) receptor occupancy following rolapitant administration.

Main Methods:

  • Two studies in healthy volunteers assessed rolapitant's pharmacokinetics and pharmacodynamics.
  • Absolute bioavailability was determined by comparing oral and intravenous doses.
  • Positron emission tomography (PET) was used to measure NK-1 receptor occupancy in the brain.

Main Results:

  • Oral rolapitant demonstrated approximately 100% absolute bioavailability.
  • A single 180-mg oral dose achieved near-saturable NK-1 receptor occupancy (94% ± 9%) at 120 hours postdose.
  • Pharmacokinetic-pharmacodynamic modeling predicted sustained receptor occupancy.

Conclusions:

  • A single 180-mg oral dose of rolapitant is well-absorbed and provides sustained NK-1 receptor blockade.
  • These findings support the use of rolapitant for effective CINV prevention.