Population pharmacokinetic modeling to assess the impact of CYP2D6 and CYP3A metabolic phenotypes on the pharmacokinetics of tamoxifen and endoxifen.

CONCLUSIONS: We have shown that not only CYP2D6, but also CYP3A enzyme activity influences the tamoxifen to endoxifen conversion in breast cancer patients. Our developed model may be used to separately assess the impact of CYP2D6 and CYP3A mediated drug-drug interactions with tamoxifen without the necessity of administering this anti-estrogenic drug and to support Bayesian guided therapeutic drug monitoring of tamoxifen in routine clinical practice.
PMID: 24697814 [PubMed - as supplied by publisher]

Source: Clinical Breast Cancer - April 2, 2014 Category: Cancer & Oncology Authors: Ter Heine R, Binkhorst L, de Graan AJ, de Bruijn P, Beijnen JH, Mathijssen RH, Huitema AD Tags: Br J Clin Pharmacol Source Type: research