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by | Mar 14, 2018 | Rosemary

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Estradiol mustard, also known as estradiol 3,17β-bis(4-(bis(2-chloroethyl)amino)phenyl)acetate, is a semisynthetic, steroidal estrogen and cytostatic antineoplastic agent and a phenylacetic acid nitrogen mustard-coupled estrogen ester that was never marketed.[1] It is selectively distributed into estrogen receptor (ER)-positive tissues such as ER-expressing tumors like those seen in breast and prostate cancers.[2] For this reason, estradiol mustard and other cytostatic-linked estrogens like estramustine phosphate have reduced toxicity relative to non-linked nitrogen mustard cytostatic antineoplastic agents.[2] However, they may stimulate breast tumor growth due to their inherent estrogenic activity and are said to be devoid of major therapeutic efficacy in breast cancer,[3] although estramustine phosphate has been approved for and is used (almost exclusively) in the treatment of prostate cancer.[4]

See also

References

  1. ^ Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 898–. ISBN 978-1-4757-2085-3.
  2. ^ a b Asai M, Takeuchi H, Okada H (January 1978). "In vivo interaction between steroidal alkylating agents and oestrogen receptors in rabbit uteri". Acta Endocrinologica. 87 (1): 173–180. doi:10.1530/acta.0.0870173. PMID 579532.
  3. ^ Leclercq G, Devleeschouwer N, Heuson JC (July 1983). James VH, Pasqualini JR (eds.). "Guide-lines in the design of new antiestrogens and cytotoxic-linked estrogens for the treatment of breast cancer". Journal of Steroid Biochemistry. 19 (1A). Elsevier Science: 75–85. doi:10.1016/S0022-4731(83)80009-0. ISBN 978-1-4831-9067-9. PMID 6887875.
  4. ^ Scullin P, O'Sullivan JM, Parker CC (5 September 2007). "Strategies for the Implementation of Chemotherapy". In Ablin RJ, Mason MD (eds.). Metastasis of Prostate Cancer. Springer Science & Business Media. pp. 311–. ISBN 978-1-4020-5847-9.
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