URINE EXCRETION STUDY OF TAMOXIFEN METABOLITE, 3-HYDROXY-4-METHOHY TAMOXIFEN BY GC-MS

Abstract

INTRODUCTION The Purpose of this study was to perform excretion study of Tamoxifen and to Detect its main active metabolite 3-hydroxy-4-methoxy by GC-MS. Tamoxifen (C 26 H 29 NO with mol mass-371.515,fig-1) works against the effect of estrogen on cell(an "anti-estrogen)slows the growth of cancer cell and prevent original breast cancer from returning. It also has beneficial effect of menopausal estrogen replacement therapy such as lowering of blood cholesterol and slowing of osteoporosis 1. In recent year, athletic competition has intensified to the point that increasing number of athletes are striving to upgrade their performance with the desire to be recognized as the best. Hence a sports person needs to keep himself vigorous, energetic, full of vitality and endurance. To achieve all this, some sports persons resort to pills and injections as shortcuts to success, as they don't understand that good genes, scientific coaching, proper nutrition and dedication to the task are what ultimately bring them success 1-2. The use of performance enhancing drugs is banned in sports 2-5. Figure 1: Tamoxifen Chemical structure 10. ABSTRACT Background; Tamoxifen, is a first-generation selective estrogen receptor modulator which is widely used for adjuvant breast cancer therapy. Tamoxifen metabolites completely bind to estrogen receptor on tumors as well as other tissues and target a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. But these Selective Estrogen Receptor Modulators (SERMs) are classified as Prohibited substances according to the list of forbidden substances in sports by the World Anti-Doping Agency (WADA) In sports male athletes use tamoxifen in fighting against increase of estrogen level in the body, breast swelling, gynecomastia and fat forming a pear-silhouette very successfully. Aim; In the present study Tamoxifen was investigated carefully by administering to a Healthy volunteer. Material and Method; Urine samples are collected at different hours from 1 st day to 5 th day and analyzed by GC-MS. Result; It was found that Tamoxifen is rapidly metabolized in to their metabolite 3-hydrohy-4-methoxy Tamoxifen. Urinary extracts were analyzed by Gas Chromatography-Mass spectrometric Detector by using Selective ion modulator (SIM) and targeted GC-MS techniques with accurate mass. By the GC-MS study it is observed that 3-hydroxy-4-methoxy Tamoxifen metabolite gives two neutral loss m/z value at 58 & 72, but m/z value 58 shows more abundance than 72m/z value, hence it was selected as the marker m/z value to check the presence of metabolite in urine. Conclusion; After oral administration, Tamoxifen metabolite can be detected in to their maximum period up to 5 days.