Anna M Mc Laughlin, Thomas Helland, Fenja Klima, Stijn L W Koolen, Ron H N van Schaik, Ron H J Mathijssen, Patrick Neven, Jesse J Swen, Henk-Jan Guchelaar, Florence Dalenc, Melanie White-Koning, Robin Michelet, Gerd Mikus, Werner Schroth, Thomas Mürdter, Hiltrud Brauch, Matthias Schwab, Håvard Søiland, Gunnar Mellgren, Fabienne Thomas, Charlotte Kloft, Daniel L Hertz
Tamoxifen is widely used in patients with hormone receptor-positive breast cancer. The polymorphic enzyme CYP2D6 is primarily responsible for metabolic activation of tamoxifen, resulting in substantial interindividual variability of plasma concentrations of its most important metabolite, Z-endoxifen. The Z-endoxifen concentration thresholds below which tamoxifen treatment is less efficacious have been proposed but not validated, and prospective trials of individualized tamoxifen treatment to achieve Z-endoxifen concentration thresholds are considered infeasible...
March 18, 2024: Clinical Pharmacology and Therapeutics