Estrogen synthesis inhibitor

An estrogen synthesis inhibitor is a type of drug which inhibits the enzymatic synthesis of estrogens, such as estradiol.[1][2][3] They include:

Types of estrogen synthesis inhibitors
Class Target Action
Aromatase inhibitors CYP19A1 inhibit the synthesis of estrogens from androgens
CYP17A1 inhibitors 17α-hydroxylase/17,20-lyase inhibit the synthesis of androgens and therefore estrogens
3β-Hydroxysteroid dehydrogenase inhibitors 3β-HSD inhibit the synthesis of progestogens and of more-potent androgens, thereby inhibiting the synthesis of estrogens
Cholesterol side-chain cleavage enzyme inhibitors P450SCC/CYP11A1 inhibit the synthesis of pregnenolone from cholesterol, thereby inhibiting the synthesis of most steroid hormones (which are derived from pregnenolone) including estrogens
17β-Hydroxysteroid dehydrogenase inhibitors 17β-HSD inhibit the interconversion of estrogens, including the synthesis of estradiol from the less-potent estrone
Steroid sulfatase inhibitors STS inhibit the conversion of inactive estrogen sulfates into active estrogens like estradiol

Inhibitors of cholesterol synthesis can also reduce estrogen production by inhibiting cholesterol production.

Estrogen synthesis inhibitors have medical applications in the treatment of breast cancer,[4][5] precocious puberty,[6] gynecomastia,[7] and hyperestrogenism,[8] among other estrogen-dependent conditions.

See also

References

  1. ↑ Bhatnagar, A. S.; Miller, W. R. (1999). "Pharmacology of Inhibitors of Estrogen Biosynthesis". Estrogens and Antiestrogens II. Vol. 135 / 2. Berlin, Heidelberg: Springer Berlin Heidelberg. pp. 223–230. doi:10.1007/978-3-642-60107-1_12. ISBN 978-3-642-64261-6. Retrieved 11 May 2026.
  2. ↑ Santen RJ (August 1993). "Estrogen synthesis inhibitors: from "off the rack" to haute couture". J Clin Endocrinol Metab. 77 (2): 316–318. doi:10.1210/jcem.77.2.8345033. PMID 8345033.
  3. ↑ Santen RJ (July 2002). "To block estrogen's synthesis or action: that is the question". J Clin Endocrinol Metab. 87 (7): 3007–3012. doi:10.1210/jcem.87.7.8589. PMID 12107191.
  4. ↑ Johnston SR, Dowsett M (November 2003). "Aromatase inhibitors for breast cancer: lessons from the laboratory". Nat Rev Cancer. 3 (11): 821–831. doi:10.1038/nrc1211. PMID 14668813.
  5. ↑ Chumsri S (2015). "Clinical utilities of aromatase inhibitors in breast cancer". Int J Womens Health. 7: 493–499. doi:10.2147/IJWH.S69907. PMC 4427607. PMID 26005359.
  6. ↑ Eugster EA (2004). "Aromatase inhibitors in precocious puberty: rationale and experience to date". Treat Endocrinol. 3 (3): 141–151. doi:10.2165/00024677-200403030-00002. PMID 16026110.
  7. ↑ Narula HS, Carlson HE (November 2014). "Gynaecomastia--pathophysiology, diagnosis and treatment". Nat Rev Endocrinol. 10 (11): 684–698. doi:10.1038/nrendo.2014.139. PMID 25112235.
  8. ↑ Karaer O, Oruç S, Koyuncu FM (August 2004). "Aromatase inhibitors: possible future applications". Acta Obstet Gynecol Scand. 83 (8): 699–706. doi:10.1111/j.0001-6349.2004.00562.x. PMID 15255840.


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