Evaluation of Olaparib Tablet Safety and Pharmacokinetics in Healthy Chinese Male Subjects.

PURPOSE

To evaluate the safety and pharmacokinetics of olaparib tablet test formulation (T) and reference formulation (R) in healthy Chinese male subjects.

SUBJECTS AND METHODS

This was a single-dose, randomized-sequence, two-way crossover study including three parts: part A: a safety exploration design in lower dose (n = 14, 100 mg), part B: a pivotal comparative pharmacokinetic (PK) trial under fast condition (n = 44, 150 mg) and part C: a pivotal comparative PK trial under food condition (n = 44, 150 mg). Blood samples were collected for 72 hours and the PK parameters of C, AUC and AUC were used to evaluate PK differences.

RESULTS

PK analysis of the two olaparib formulations showed that the Geometric Least Squares Mean (GLSM) ratio 90% confidence intervals for pivotal fasting C, AUC and AUC were 94.82-108.97%, 92.94-104.28%, and 92.81-103.85%, respectively, and pivotal fed C, AUC, and AUC were 82.78-100.97%, 91.59-104.67%, and 92.17-104.76%, respectively. The 90% confidence interval of the two preparations, C, AUC, and AUC, all fall within the equivalent range of 80-125%. Both olaparib tablet formulations were well tolerated, with no serious adverse events (SAE) or adverse events (AE) causing withdrawal occurred.

CONCLUSION

Two types of olaparib tablets were bioequivalent under both fasting and fed condition, and were generally well tolerated in healthy Chinese male subjects.