Influence of probenecid on endoxifen systemic exposure in breast cancer patients on adjuvant tamoxifen treatment
| Autor: | Stefan A. J. Buck, C. Louwrens Braal, Maaike M. Hofman, Esther Oomen-de Hoop, Peter de Bruijn, Inge M. Ghobadi Moghaddam-Helmantel, Koen G. A. M. Hussaarts, Mijntje B. Vastbinder, Quirine C. van Rossum-Schornagel, Ron H. N. van Schaik, Agnes Jager, Stijn L. W. Koolen, Ron H. J. Mathijssen |
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| Jazyk: | angličtina |
| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | Therapeutic Advances in Medical Oncology, Vol 14 (2022) |
| Druh dokumentu: | article |
| ISSN: | 1758-8359 17588359 |
| DOI: | 10.1177/17588359221081075 |
| Popis: | Introduction: In breast cancer patients treated with the anti-estrogen tamoxifen, low concentrations of the active metabolite endoxifen are associated with more disease recurrence. We hypothesized that we could increase endoxifen concentrations by induction of its formation and inhibition of its metabolism by co-administration of probenecid. Methods: We conducted a crossover study and measured endoxifen concentrations in patients on steady-state tamoxifen monotherapy and after 14 days of combination treatment with probenecid. Eleven evaluable patients were included. Results: Treatment with tamoxifen and probenecid resulted in a 26% increase of endoxifen area under the plasma concentration–time curve from 0 to 24 h (AUC 0–24h ) compared to tamoxifen monotherapy (95% confidence interval [CI]: 8–46%; p |
| Databáze: | Directory of Open Access Journals |
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