Estrogen ester

An estrogen ester is an ester of an endogenous, steroidal estrogen, generally estradiol but also estrone or estriol.[1] Esterification renders these drugs into metabolically-resistant prohormones of their respective parent estrogen, improving oral bioavailability, increasing lipophilicity, and extending half-life (which necessitates less frequent administration).[2] In addition, with intramuscular injection, they are absorbed more slowly into the body, further improving half-life.[1]

Estrogen esters are used in hormone replacement therapy and as hormonal contraceptives, among other indications.

The first estrogen ester to be marketed was estradiol benzoate in 1936,[3][4] which was quickly followed by many more.

List of estrogen esters

Many esters of estradiol have been marketed, including the following:[5][6]

As well as the following esters of other estrogens:[5][6]

A few other estrogen esters which are notable but have not been marketed include atrimustine (bestrabucil), estrapronicate, orestrate, which are estradiol esters.[6]

See also

References

  1. 1 2 R. S. Satoskar; S. D. Bhandarkar &nirmala N. Rege (1969). Pharmacology And Pharmacotherapeutics (New Revised 21 St Ed.). Popular Prakashan. p. 24. ISBN 978-81-7991-527-1. Retrieved 29 May 2012.
  2. Gordon L. Amidon; Ping I. Lee; Elizabeth M. Topp (2000). Transport Processes in Pharmaceutical Systems. CRC Press. p. 188-189. ISBN 978-0-8247-6610-8. Retrieved 29 May 2012.
  3. Enrique Raviña; Hugo Kubinyi (16 May 2011). The Evolution of Drug Discovery: From Traditional Medicines to Modern Drugs. John Wiley & Sons. p. 175. ISBN 978-3-527-32669-3. Retrieved 20 May 2012.
  4. Folley SJ (December 1936). "The effect of oestrogenic hormones on lactation and on the phosphatase of the blood and milk of the lactating cow" (PDF). The Biochemical Journal 30 (12): 2262–72. PMC 1263335. PMID 16746289.
  5. 1 2 Index Nominum 2000: International Drug Directory. Taylor & Francis US. 2000. p. 404. ISBN 978-3-88763-075-1. Retrieved 29 May 2012.
  6. 1 2 3 A. D. Roberts (1991). Dictionary of Steroids: Chemical Data, Structures, and Bibliographies. CRC Press. p. 415. ISBN 978-0-412-27060-4. Retrieved 20 May 2012.



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