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{{Short description|Class of compounds}}
An '''antiprogestogen''', also called an '''antiprogesterone agent''', or in the case of a [[Organic compound#Synthetic compounds|synthetic]] compound, an '''antiprogestin''', is a type of [[hormone antagonist]] in which that antagonizes or suppresses the actions of [[progesterone]] in the body, a [[sex hormone]] that plays a [[role]] in the [[menstrual cycle]] and [[pregnancy]]. Antiprogestogens may stop some [[cancer cells]] from [[Cell growth|growing]] and they are being studied in the treatment of [[breast cancer]].
{{Infobox drug class
| Image = Mifepristone_structure.svg
| Alt =
| Caption = [[Mifepristone]], an antiprogestogen that is used to induce [[medical abortion]]s.
| Width = 250px
| Synonyms = Antiprogestins; Progesterone antagonists; Progesterone blockers
<!-- Class identifiers -->
| Use = [[Medical abortion]], [[emergency contraception]], [[uterine fibroid]]s
| ATC_prefix = G03XB
| Biological_target = [[Progesterone receptor]]
| Chemical_class = [[Steroid]]al
<!-- Clinical data -->
| Drugs.com =
| Consumer_Reports =
| medicinenet =
| rxlist =
<!-- External links -->
| MeshID =
}}


'''Antiprogestogens''', or '''antiprogestins''', also known as '''progesterone antagonists''' or '''progesterone blockers''', are a class of [[drug]]s which prevent [[progestogen]]s like [[progesterone]] from mediating their [[biological effect]]s in the body. These drugs competitively inhibit progestin at progesterone receptors. They act by [[receptor antagonist|blocking]] the [[progesterone receptor]] (PR)and/or [[steroidogenesis inhibitor|inhibiting]] or [[antigonadotropin|suppressing]] progestogen [[biosynthesis|production]]. Antiprogestogens are one of three types of [[sex-hormonal agent|sex hormone antagonist]]s, the others being [[antiestrogen]]s and [[antiandrogen]]s.<ref name="Nath2006">{{cite book|author=Judi Lindsley Nath|title=Using Medical Terminology: A Practical Approach|url=https://books.google.com/books?id=UEvTZg_5FBIC&pg=PA977|year=2006|publisher=Lippincott Williams & Wilkins|isbn=978-0-7817-4868-1|pages=977–}}</ref>
An example of an antiprogestogen is [[mifepristone]].<ref name="Spitz-2006">{{Cite journal | last1 = Spitz | first1 = IM. | title = Progesterone receptor antagonists. | journal = Curr Opin Investig Drugs | volume = 7 | issue = 10 | pages = 882–90 | month = Oct | year = 2006 | doi = | PMID = 17086932 }}</ref><ref name="Tang-2006">{{Cite journal | last1 = Tang | first1 = OS. | last2 = Ho | first2 = PC. | title = Clinical applications of mifepristone. | journal = Gynecol Endocrinol | volume = 22 | issue = 12 | pages = 655–9 | month = Dec | year = 2006 | doi = 10.1080/09513590601005946 | PMID = 17162706 }}</ref>


Antiprogestogens are used as [[abortifacient]]s and [[emergency contraception|emergency contraceptive]]s and in the treatment of [[uterine fibroid]]s. They are also being studied in the treatment of [[breast cancer]]. Examples of antiprogestogens include the [[progesterone receptor]] weak [[partial agonist]] [[mifepristone]], the [[selective progesterone receptor modulator]] (SPRM) [[ulipristal acetate]], and the [[silent antagonist]] [[aglepristone]].<ref name="Spitz-2006">{{Cite journal | last1 = Spitz | first1 = IM. | title = Progesterone receptor antagonists. | journal = Curr Opin Investig Drugs | volume = 7 | issue = 10 | pages = 882–90 |date=Oct 2006 | pmid = 17086932 }}</ref><ref name="Tang-2006">{{Cite journal | last1 = Tang | first1 = OS. | last2 = Ho | first2 = PC. | title = Clinical applications of mifepristone. | journal = Gynecol Endocrinol | volume = 22 | issue = 12 | pages = 655–9 |date=Dec 2006 | doi = 10.1080/09513590601005946 | pmid = 17162706 | s2cid = 23295715 }}</ref> For [[medical abortion]], mifepristone is combined with a [[prostaglandin]] (e.g., [[gemeprost]]). Ulipristal is used as a form of emergency contraception. <ref>{{cite book |last1=Le |first1=Tao |last2=Bhushan |first2=Vikas |last3=Qiu |first3=Connie |last4=Chalise |first4=Anup |last5=Kaparaliotis |first5=Panagiotis |title=First Aid |date=2023 |publisher=McGraw Hill}}</ref>
Medical termination of pregnancy: mifepristone (partial agonist) combine with prostaglandin (e.g., gemeprost).

Several hundred antiprogestogens have been developed, but only three, [[mifepristone]], [[lilopristone]], and [[onapristone]], have been given to humans, and of these, only mifepristone has been approved and introduced for clinical use.<ref name="BourneCondous2006">{{cite book|author1=Thomas H. Bourne|author2=George Condous|title=Handbook of Early Pregnancy Care|url=https://books.google.com/books?id=_Y3PyNvc6dcC&pg=PA41|date=17 October 2006|publisher=CRC Press|isbn=978-0-203-01621-3|pages=41–}}</ref>

Progestins, including progesterone are important for the body to prepare the uterus for implantation of fertilized egg during the luteal phase of the menstrual cycle and, if fertilization, implantation, and other events necessary for pregnancy occur, increased progestin (i.e. progesterone) levels are heavily involved in maintaining the pregnancy. Blocking the effects of progestins, such as progesterone, is associated with anti-gestational events. <ref>{{cite book |last1=Le |first1=Tao |last2=Bhushan |first2=Vikas |last3=Qiu |first3=Connie |last4=Chalise |first4=Anup |last5=Kaparaliotis |first5=Panagiotis |title=First Aid |date=2023 |publisher=McGraw Hill}}</ref>


==See also==
==See also==
* [[Progesterone]]
*[[Antiestrogen]]
* [[Progestogen]]
*[[Antiandrogen]]
* [[Progestin]]
* [[Selective progesterone receptor modulator|SPRM]]
* [[Antiestrogen]]
* [[Antiandrogen]]


==References==
==References==
{{Reflist}}
{{Reflist|2}}


==External links==
==External links==
⚫
*{{Commonscatinline|Antiprogestogens}}
* [http://www.cancer.gov/dictionary?CdrID=561317 Antiprogestin] entry in the public domain NCI Dictionary of Cancer Terms
*[http://www.cancer.gov/dictionary?CdrID=561317 Antiprogestin] entry in the public domain NCI Dictionary of Cancer Terms
{{NCI-cancer-dict}}
{{NCI-cancer-dict}}




{{Progestogens}}
{{Progestogens and antiprogestogens}}
{{Progesterone receptor modulators}}
{{Progestogenics}}


[[Category:Antineoplastic drugs]]
[[Category:Antiprogestogens| ]]
⚫
[[Category:Antiprogestogens]]




Latest revision as of 16:20, 2 November 2023

Antiprogestogen
Drug class
Mifepristone, an antiprogestogen that is used to induce medical abortions.
Class identifiers
SynonymsAntiprogestins; Progesterone antagonists; Progesterone blockers
UseMedical abortion, emergency contraception, uterine fibroids
ATC codeG03XB
Biological targetProgesterone receptor
Chemical classSteroidal
Legal status
In Wikidata

Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. These drugs competitively inhibit progestin at progesterone receptors. They act by blocking the progesterone receptor (PR)and/or inhibiting or suppressing progestogen production. Antiprogestogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiandrogens.[1]

Antiprogestogens are used as abortifacients and emergency contraceptives and in the treatment of uterine fibroids. They are also being studied in the treatment of breast cancer. Examples of antiprogestogens include the progesterone receptor weak partial agonist mifepristone, the selective progesterone receptor modulator (SPRM) ulipristal acetate, and the silent antagonist aglepristone.[2][3] For medical abortion, mifepristone is combined with a prostaglandin (e.g., gemeprost). Ulipristal is used as a form of emergency contraception. [4]

Several hundred antiprogestogens have been developed, but only three, mifepristone, lilopristone, and onapristone, have been given to humans, and of these, only mifepristone has been approved and introduced for clinical use.[5]

Progestins, including progesterone are important for the body to prepare the uterus for implantation of fertilized egg during the luteal phase of the menstrual cycle and, if fertilization, implantation, and other events necessary for pregnancy occur, increased progestin (i.e. progesterone) levels are heavily involved in maintaining the pregnancy. Blocking the effects of progestins, such as progesterone, is associated with anti-gestational events. [6]

See also[edit]

References[edit]

  1. ^ Judi Lindsley Nath (2006). Using Medical Terminology: A Practical Approach. Lippincott Williams & Wilkins. pp. 977–. ISBN 978-0-7817-4868-1.
  2. ^ Spitz, IM. (Oct 2006). "Progesterone receptor antagonists". Curr Opin Investig Drugs. 7 (10): 882–90. PMID 17086932.
  3. ^ Tang, OS.; Ho, PC. (Dec 2006). "Clinical applications of mifepristone". Gynecol Endocrinol. 22 (12): 655–9. doi:10.1080/09513590601005946. PMID 17162706. S2CID 23295715.
  4. ^ Le, Tao; Bhushan, Vikas; Qiu, Connie; Chalise, Anup; Kaparaliotis, Panagiotis (2023). First Aid. McGraw Hill.
  5. ^ Thomas H. Bourne; George Condous (17 October 2006). Handbook of Early Pregnancy Care. CRC Press. pp. 41–. ISBN 978-0-203-01621-3.
  6. ^ Le, Tao; Bhushan, Vikas; Qiu, Connie; Chalise, Anup; Kaparaliotis, Panagiotis (2023). First Aid. McGraw Hill.

External links[edit]

Public Domain This article incorporates public domain material from Dictionary of Cancer Terms. U.S. National Cancer Institute.



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