Estradiol cyclooctyl acetate explained

Estradiol cyclooctyl acetate (E2COA), or estradiol 17β-cyclooctylacetate, also known as estra-1,3,5(10)-triene-3,17β-diol 17β-cyclooctylacetate, is an estrogen medication and an estrogen ester – specifically, the 17β-cyclooctylacetate ester of estradiol – which has been studied for use in hormone replacement therapy for ovariectomized women and as a hormonal contraceptive in combination with a progestin but was never marketed.[1] [2] [3] [4] It has greater oral bioavailability than does micronized estradiol due to absorption via the lymphatic system and hence partial bypassing of first-pass metabolism. It is approximately twice as potent as micronized estradiol orally and has a comparatively reduced impact on liver parameters such as changes in sex hormone-binding globulin production. It was investigated in combination with desogestrel as a birth control pill, but resulted in unacceptable menstrual bleeding patterns and was not further developed.

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Notes and References

  1. Bastianelli C, Farris M, Rosato E, Brosens I, Benagiano G . Pharmacodynamics of combined estrogen-progestin oral contraceptives 3. Inhibition of ovulation . Expert Review of Clinical Pharmacology . 11 . 11 . 1085–1098 . November 2018 . 30325245 . 10.1080/17512433.2018.1536544 . 53246678 .
  2. Dahlgren E, Crona N, Janson PO, Samsioe G . Oral replacement with estradiol-cyclooctyl acetate: a new estradiol analogue. Effects on serum lipids, proteins, gonadotrophins, estrogens and uterine endometrial morphology . Gynecologic and Obstetric Investigation . 20 . 2 . 84–90 . 1985 . 3932144 . 10.1159/000298978 .
  3. Schubert W, Cullberg G . Ovulation inhibition with 17 beta-estradiol cyclo-octyl acetate and desogestrel . Acta Obstetricia et Gynecologica Scandinavica . 66 . 6 . 543–547 . 1987 . 2962418 . 10.3109/00016348709015732 . 73200770 .
  4. Schubert W, Cullberg G . Fat-soluble 17 beta-estradiol: a way of reducing dosage in steroid hormonal substitution? . Acta Obstetricia et Gynecologica Scandinavica . 67 . 3 . 271–275 . 1988 . 2972162 . 10.3109/00016348809004218 . 39664429 .

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