Evaluation of the Pharmacokinetics of Abiraterone Acetate and Abiraterone Following Single-Dose Administration of Abiraterone Acetate to Healthy Subjects

  • Mohammed Bouhajib
  • Zia TayabEmail author
Original Research Article


Background and Objective

Following oral administration of abiraterone acetate, the parent compound abiraterone acetate is rapidly metabolized to abiraterone. To our knowledge, bioanalytical methods to date have not been able to detect the parent compound in human plasma, and bioassay was only performed on the metabolite. A highly sensitive bioanalytical method was developed and validated to measure plasma concentrations of the parent compound. In this study, both analytes were assayed and used to evaluate the full pharmacokinetic profile of abiraterone acetate tablets.


This was an open-label, single-dose, one-period, one-treatment, pharmacokinetic study performed in 18 healthy subjects. Each subject was administered four tablets (corresponding to a total dose of 1000 mg) of abiraterone acetate. Blood samples for pharmacokinetic analysis were collected up to 60 h post-dose. Subjects’ plasma concentrations for abiraterone acetate were assayed using highly sensitive validated bioanalytical methods with a lower limit of quantitation (LLOQ) of 0.5 pg/ml for abiraterone acetate and 0.1 ng/ml for abiraterone. Safety assessments were performed throughout the study.


The pharmacokinetic results for abiraterone acetate showed a mean for the maximum plasma concentration (Cmax) of 54.67 ± 68.30 pg/ml, and a median time to maximum concentrations (tmax) of 5.53 h (range 2.67–35.00 h). The means for area under the concentration-time curve (AUC) from time 0 h to infinity (AUCinf) and AUC from time zero h to the time of the last measurable abiraterone acetate concentrations (AUCt) were 386.13 ± 266.80 pg·h/ml and 460.07 ± 378.78 pg·h/ml, respectively. The apparent elimination half-life (t1/2) showed a mean of 8.98 ± 3.92 h. None of the adverse events that affected three subjects (16.7%) were related to the study drug.


The ability to detect the low plasma abiraterone acetate concentrations, in addition to abiraterone, resulted in a complete characterization of the pharmacokinetics of abiraterone acetate that was not possible with other analytical methods that only measured the metabolite. The development of new bioanalytical methods such as these will allow for a more thorough understanding of the pharmacokinetics of abiraterone acetate, and this, in turn, can have an impact on both future examinations into abiraterone acetate pharmacokinetic behaviour and the evaluation of its generic formulations.



The authors acknowledge the assistance provided by Ashraf El Sheikh Ali in the preparation of the manuscript.

Compliance with Ethical Standards


This study was funded by Pharma Medica Research Inc.

Conflict of interest

Mohammed Bouhajib and Zia Tayab are employees of Pharma Medica Research Inc. They do not have any other conflicts of interest to declare.

Ethical approval

All procedures performed in studies involving human participants were in accordance with the ethical standards of the institutional and/or national research committee and with the 1964 Helsinki declaration and its later amendments or comparable ethical standards. The study protocol and informed consent form were approved by Salus Institutional Review Board (IRB), Texas, USA.

Informed consent

Informed consent was obtained from all individual participants included in the study, prior to any activity in the trial.


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Copyright information

© Springer Nature Switzerland AG 2019

Authors and Affiliations

  1. 1.Pharma Medica Research Inc.MississaugaCanada

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