• ASHU RATHI Indian pharmacopoeia commission, Ghaziabad, UP
  • Dr. Shila Jain National Dope Testing Laboratory(NDTL), New Delhi
  • Dr. Alka Beotra National Dope Testing Laboratory(NDTL), New Delhi
  • Dr. Manisha Trivedi Indian pharmacopoeia commission, Ghaziabad, UP
  • Vandana Nimker National Dope Testing Laboratory(NDTL), New Delhi
  • Dr. Robin Kumar Indian pharmacopoeia commission, Ghaziabad, UP


Background; Tamoxifen, is a first-generation selective estrogen receptor modulator which  is widely used for adjuvant breast cancer therapy. Tamoxifen metabolite 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 1st day to 5th 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.


Keywords: Doping, WADA, Tamoxifen, GC-MS, Human Urine, Solid phase Extraction


Download data is not yet available.


1. Brito, Dayamin…et. all, Excretion study of clomiphene in human urine: evaluation of endogenous steroids profile after multiple oral doses, Journal of the Brazilian Chemical Society, 2010, 21 (12), 2220-2225.

2. Lu J….et al, Structural elucidation of new urinary tamoxifen metabolites by liquid chromatography quadrupole time-of-flight mass spectrometry, Journal of Mass Spectrometry, 2014, 47, (7), 570-78.

3. Jordan , V. C. and Jaspan, T., Tamoxifen as an anti-tumour agent: oestrogen binding as a predictive test for tumour response, Journal of Endocrinology, 1976, 68 (3) 453-460.

4. Rickert, EL….et all, Synthesis and Characterization of Bioactive Tamoxifen-Conjugated Polymers. Biomacromolecules, 2007,8 (11), 3608-3612.

5. Kisanga ER, Mellgren G, Lien EA., Excretion of hydroxylated metabolites of tamoxifen in human bile and urine, Anticancer Research . 2005 Nov-Dec;25(6C),4487-92.

6. Mihailescu R, Aboul‐Enein H Y. and Efstatide M.D., "Identification of Tamoxifen and Metabolites in Human Male Urine by GC/MS, Biomedical Chromatography,14, no. 3 (2000): 180-83.

7. Baez, H., C. Camargo, H. Osorio, and F. Umpierrez. "Detection of Tamoxifen Metabolites by GC-MSD." Journal of Chromatographic Science 42, no. 10 (2004): 551-53.

8. Beotra A. Drug Abuse in Sports. 7th ed. Inde, 2001.P.5-35.

9. Drug Today, Metabolism “Carcinoma chemotherapeutic Drug” Tamoxifen citrate.jan-mar:2010,
vol-2nd ,P.1109.

10. (n.d.). Retrieved January 11, 2016, from https://en.wikipedia.org/wiki/Anabolic_steroid
385 Views | 448 Downloads
How to Cite
RATHI A, Jain DS, Beotra DA, Trivedi DM, Nimker V, Kumar DR. URINE EXCRETION STUDY OF TAMOXIFEN METABOLITE, 3-HYDROXY-4-METHOHY TAMOXIFEN BY GC-MS. JDDT [Internet]. 15Jan.2016 [cited 3Mar.2021];6(1):19-4. Available from: http://jddtonline.info/index.php/jddt/article/view/1194