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Summary of bioequivalence study for EFEZ, 25 mg eplerenone film-coated tablets; 50 mg eplerenone film-coated tablets

25 January 2023

Purpose. To prove the bioequivalence (BE) of the test investigational medicinal product (IMP) EFEZ, 50 mg eplerenone film-coated tablets, manufactured by PrJSC “Pharmaceutical Firm “Darnitsa” to the reference IMP INSPRA®, 50 mg eplerenone film-coated tablets, manufactured by Fareva Amboise, France (MAH: Pfizer Europe MA EEIG, Belgium) in a randomized, open-label, single-dose, two-sequence, two-period, crossover, comparative, oral bioequivalence study in 36 healthy male and female volunteers under fasting conditions.

Objects and methods of the study. Healthy male and female volunteers took a single oral dose of test or reference IMPs, i.e., 50 mg of eplerenone, in each period (i.e., 100 mg of eplerenone throughout the study) under fasting conditions. Data of 35 healthy volunteers fully completed the study according to the protocol and taken IMP in both periods were included in pharmacokinetic and statistical analysis.

Results. Pharmacokinetic analysis showed that eplerenone geometric least squares means ratios and corresponding 90% confidence intervals (CIs) of maximum plasma concentration (Cmax) and area under the plasma concentration curve from administration to last observed concentration at time (t) (AUC0-t) were 106.57% (101.86% to 111.50%) and 100.51% (95.08% to 106.25%), respectively. The criteria used to assess bioequivalence between the Test and Reference IMPs were all fulfilled since the Test to Reference ratio of geometric least squares means and corresponding 90% CI for Cmax and AUC0-t were all within the acceptance range of 80.00 to 125.00%.

A total of 10 adverse events (AEs) were reported by 9 subjects who received at least one dose of IMP. Five AEs had a “possible” relationship to the IMPs, two AEs were considered to be unlikely related, and another two AEs were not related to IMP administration.

In two cases of AEs, it was necessary to take 1000 mg of paracetamol (one case due to headache in 1 subject and one case due to pain in the epigastrium in 1 subject).

Overall, an oral single dose of eplerenone 50 mg (in a form of reference and test IMPs) administered to healthy volunteers in the fasted state was safe and well tolerated. No serious adverse events (SAEs) were reported for any of the subjects enrolled in the study. No subject was withdrawn for safety reasons.

Conclusions. The bioequivalence of the test IMP (EFEZ, 50 mg eplerenone film-coated tablets) to the reference IMP (INSPRA®, 50 mg eplerenone film-coated tablets) was demonstrated in this study. Both IMPs were characterized to have good tolerability with single (within each period) oral administration under fasting conditions.

The Sponsor of the study, PrJSC “Pharmaceutical Firm “Darnitsa”, expresses its gratitude to the employees of contract research organization (CRO) ACDIMA Center for Bioequivalence and Pharmaceutical Studies (Amman, Jordan) for conducting the research and processing its results.




Film-coated tablet
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