Pharmacokinetic Drug Interaction Study of Bazedoxifene and Ibuprofen

• Published in: Clinical pharmacology in drug development 2018-05, Vol.7 (4), p.358-364
• Main Authors: McKeand, William, Baird‐Bellaire, Susan, Ermer, James, Patat, Alain
• Format: Article
• Language: English
• Subjects: bazedoxifene; Bioequivalence; Hormone replacement therapy; ibuprofen; interaction; Nonsteroidal anti-inflammatory drugs; Pharmacokinetics; Pharmacology
• ISSN: 2160-763X; 2160-7648
• DOI: 10.1002/cpdd.433

The purpose of this article was to evaluate the potential for a pharmacokinetic interaction between bazedoxifene and ibuprofen. In a randomized crossover study, 12 healthy postmenopausal women (aged 45–65 years) received either a single oral dose of ibuprofen (600‐mg tablet), bazedoxifene (20‐mg capsule), or both ibuprofen and bazedoxifene during the 3 treatment periods. Serial blood samples were collected for pharmacokinetic analyses. There was no relationship between the UGT1A1 genotype and bazedoxifene clearance. The 90% log‐transformed confidence intervals (CIs) for bazedoxifene Cmax, 96% to 144%, and AUC, 85% to 134%, were slightly above the bioequivalence limits of 80% to 125%. The 90% log‐transformed CIs for ibuprofen pharmacokinetic parameters were within these limits (Cmax, 92%–122%; AUC, 94%–106%). The increase in bazedoxifene plasma concentrations when combined with ibuprofen versus bazedoxifene alone is unlikely to be clinically significant. The lack of interaction between bazedoxifene and ibuprofen suggests that they may be coadministered without dose adjustment.