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Antiprogestogen |
Drug class |
Mifepristone, an antiprogestogen that is used to induce medical abortions.
|
Class identifiers |
Synonyms |
Antiprogestins; Progesterone antagonists; Progesterone blockers |
Use |
Medical abortion, emergency contraception, uterine fibroids |
ATC code |
G03XB |
Biological target |
Progesterone receptor |
Chemical class |
Steroidal |
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. 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).
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.[4]
References
- ^ Judi Lindsley Nath (2006). Using Medical Terminology: A Practical Approach. Lippincott Williams & Wilkins. pp. 977–. ISBN 978-0-7817-4868-1.
- ^ Spitz, IM. (Oct 2006). "Progesterone receptor antagonists.". Curr Opin Investig Drugs. 7 (10): 882–90. PMID 17086932.
- ^ Tang, OS.; Ho, PC. (Dec 2006). "Clinical applications of mifepristone.". Gynecol Endocrinol. 22 (12): 655–9. PMID 17162706. doi:10.1080/09513590601005946.
- ^ Thomas H. Bourne; George Condous (17 October 2006). Handbook of Early Pregnancy Care. CRC Press. pp. 41–. ISBN 978-0-203-01621-3.
External links
- Antiprogestin entry in the public domain NCI Dictionary of Cancer Terms
This article incorporates public domain material from the U.S. National Cancer Institute document "Dictionary of Cancer Terms".
Progestogens and antiprogestogens
|
Progestogens
(and progestins) |
PR agonists |
- Progesterone derivatives: Progesterone
- Quingestrone
- Retroprogesterone derivatives: Dydrogesterone
- Trengestone
- 17α-Hydroxyprogesterone (and closely related) derivatives: Acetomepregenol (mepregenol diacetate)
- Algestone
- Algestone acetophenide (dihydroxyprogesterone acetophenide)
- Anagestone acetate
- Chlormadinone acetate
- Cyproterone acetate
- Delmadinone acetate
- Flugestone acetate (flurogestone acetate)
- Flumedroxone acetate
- Hydroxyprogesterone
- Hydroxyprogesterone acetate
- Hydroxyprogesterone caproate
- Hydroxyprogesterone heptanoate
- Medroxyprogesterone
- Medroxyprogesterone acetate#
- Megestrol acetate
- Melengestrol acetate
- Osaterone acetate
- Pentagestrone acetate
- Other 17α-substituted (besides hydroxylated) derivatives: Haloprogesterone
- Medrogestone
- Proligestone
- 19-Norprogesterone (including 17α-substituted) derivatives: Demegestone
- Gestonorone caproate (gestronol hexanoate)
- Nomegestrol acetate
- Norgestomet
- Promegestone
- Segesterone acetate (nestorone)
- Trimegestone
- 17α-Ethynyltestosterone derivatives:
- Danazol
- Dimethisterone
- Ethisterone
- 19-Nortestosterone (including 17α-substituted) derivatives: Estranes: Dienogest
- Etynodiol diacetate
- Gestrinone
- Lynestrenol
- Norethisterone (norethindrone)#
- Norethisterone acetate
- Norethisterone enanthate
- Noretynodrel
- Norgestrienone
- Quingestanol acetate
- Tibolone; Gonanes: Desogestrel
- Etonogestrel
- Gestodene
- Levonorgestrel#
- Norelgestromin
- Norgestimate
- Norgestrel; Others: Allylestrenol
- Altrenogest
- Norgesterone
- Normethandrone (methylestrenolone)
- Norvinisterone
- Oxendolone
- Spirolactone derivatives: Drospirenone
- Others: Anabolic–androgenic steroids (e.g., nandrolone and esters, trenbolone and esters, norethandrolone, normethandrone, others)
|
|
Antiprogestogens |
SPRMs |
- Asoprisnil†
- Telapristone§
- Ulipristal acetate
|
PR antagonists |
- Aglepristone
- Mifepristone
- Valproic acid
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
- See also
- Progesterone receptor modulators
- Androgens and antiandrogens
- Estrogens and antiestrogens
- List of progestogens
|
Progesterone receptor modulators
|
PR |
Agonists |
|
Mixed
(SPRMs) |
- Steroidal: Asoprisnil
- Asoprisnil ecamate
- Guggulsterone
- J1042
- LG-120838
- Mifepristone
- ORG-31710
- ORG-33628
- Telapristone
- Ulipristal acetate
- Vilaprisan
- ZK-137316
- Nonsteroidal: Apigenin
- Kaempferol
- LG-120920
- Naringenin
- PRA-910
- Syringic acid
|
Antagonists |
- Steroidal: Aglepristone
- Lilopristone
- Lonaprisan
- Onapristone
- RTI 3021–022
- Toripristone
- Zanoterone
- Nonsteroidal: LG001447
- LG-100127
- LG-100128
- LG-120830
- LG-121046
- Valproic acid
- ZM-150271
- ZM-172406
|
|
mPR
(PAQR) |
Agonists |
- 5α-Dihydroprogesterone
- 5β-Dihydroprogesterone
- 11-Deoxycortisone (21-hydroxyprogesterone)
- 11-Deoxycortisol (17α,21-dihydroxyprogesterone)
- 17α-Hydroxyprogesterone
- Allopregnanolone
- Mifepristone
- Pregnenolone
- Progesterone
|
Antagonists |
|
|
- See also
- Receptor/signaling modulators
- Progestogens and antiprogestogens
- Androgen receptor modulators
- Estrogen receptor modulators
- List of progestogens
|
UpToDate Contents
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English Journal
- Double-Blind Phase III Randomized Trial of the Antiprogestin Agent Mifepristone in the Treatment of Unresectable Meningioma: SWOG S9005.
- Ji Y1, Rankin C1, Grunberg S1, Sherrod AE1, Ahmadi J1, Townsend JJ1, Feun LG1, Fredericks RK1, Russell CA1, Kabbinavar FF1, Stelzer KJ1, Schott A1, Verschraegen C2.
- Journal of clinical oncology : official journal of the American Society of Clinical Oncology.J Clin Oncol.2015 Dec 1;33(34):4093-8. doi: 10.1200/JCO.2015.61.6490. Epub 2015 Nov 2.
- PURPOSE: Progesterone receptors are expressed in approximately 70% of meningiomas. Mifepristone is an oral antiprogestational agent reported to have modest activity in a phase II study. This multicenter, prospective, randomized, placebo-controlled phase III trial conducted by SWOG was planned to def
- PMID 26527781
- Replication-Competent Controlled Herpes Simplex Virus.
- Bloom DC1, Feller J1, McAnany P1, Vilaboa N2, Voellmy R3.
- Journal of virology.J Virol.2015 Oct 15;89(20):10668-79. doi: 10.1128/JVI.01667-15. Epub 2015 Aug 12.
- We present the development and characterization of a replication-competent controlled herpes simplex virus 1 (HSV-1). Replication-essential ICP4 and ICP8 genes of HSV-1 wild-type strain 17syn+ were brought under the control of a dually responsive gene switch. The gene switch comprises (i) a transact
- PMID 26269179
- Progesterone Plays a Critical Role in Canine Oocyte Maturation and Fertilization.
- Reynaud K1, Saint-Dizier M2, Tahir MZ3, Havard T3, Harichaux G4, Labas V4, Thoumire S5, Fontbonne A5, Grimard B3, Chastant-Maillard S6.
- Biology of reproduction.Biol Reprod.2015 Oct;93(4):87. doi: 10.1095/biolreprod.115.130955. Epub 2015 Sep 2.
- Canine oocyte maturation and fertilization take place within the oviducts under increasing plasma levels of progesterone (P4). In order to investigate the role of P4 in these processes, 51 beagle bitches were treated with the P4 receptor antagonist aglepristone at the end of proestrus and 32 females
- PMID 26333993
Japanese Journal
- SHNマウス下垂体移植誘発子宮腺筋症に与えるミフェプリストン(RU486)の影響
- Progesterone Is a Sperm-Releasing Factor from the Sperm-Storage Tubules in Birds
- Ito Tomomi,Yoshizaki Norio,Tokumoto Toshinobu,Ono Hiroko,Yoshimura Takashi,Tsukada Akira,Kansaku Norio,Sasanami Tomohiro
- Endocrinology 152(10), 3952-3962, 2011-08-02
- … A binding assay using [(3)H]-progesterone indicated the presence of a high affinity, limited capacity, saturable and single binding site for [(3)H]-progesterone in the membrane fraction of the UVJ, and this receptor did not interact with the synthetic antiprogestin RU486. …
- NAID 120004442651
- Chronic treatment of cycling rhesus monkeys with low doses of the antiprogestin ZK 137 316 : morphometric assessment of the uterus and oviduct
Related Links
- MLA style: "antiprogestin". Encyclopædia Britannica. Encyclopædia Britannica Online. Encyclopædia Britannica Inc., 2015. Web. 27 Nov. 2015 < http://www.britannica.com/science/antiprogestin >. APA style: antiprogestin. (2015). In Encyclopædia Britannica
- antiprogestin [an″te-, an″ti-pro-jes´tin] a substance that inhibits the formation of progestational agents; the most common example is mifepristone. an·ti·pro·ges·tin (an'tē-prō-jes'tin), A substance that inhibits progesterone formation ...
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