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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/10/28 20:37:34」(JST)
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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
- Choline acetyltransferase and TrkA expression, as well as the improvement in cognition produced by E2 and P4 in ovariectomized rats, are blocked by ICI 182 780 and RU486.
- Espinosa-Raya J, Cruz-Raya U, López-Martínez M, Picazo O.
- Behavioural pharmacology. 2018 08;29(5)457-461.
- Treatment with 17-β estradiol and progesterone improves the performance of ovariectomized rats in an autoshaping learning task, representing cognitive improvement. To test whether this is attributable to genomic mechanisms, the antiestrogen ICI 182 780 or antiprogesterone RU486 was injected into
- PMID 29319543
- The Role of Endocrine and Dioxin-Like Activity of Extracts of Petroleum Substances in Developmental Toxicity as Detected in a Panel of CALUX Reporter Gene Assays.
- Kamelia L, Louisse J, de Haan L, Maslowska-Gornicz A, Ketelslegers HB, Brouwer A, Rietjens IMCM, Boogaard PJ.
- Toxicological sciences : an official journal of the Society of Toxicology. 2018 08;164(2)576-591.
- Recent evidence suggests that the interaction of polycyclic aromatic hydrocarbons (PAHs), present in some petroleum substances (PS), with particular nuclear-hormone-receptors and/or the dioxin (aryl hydrocarbon receptor [AhR]) receptor, may play a role in the prenatal developmental toxicity (PDT) in
- PMID 29726971
- Histopathologic Characterization of Mifepristone-induced Ovarian Toxicity in Cynomolgus Monkeys.
- Taketa Y, Horie K, Goto T, Ohta E, Nakano-Ito K, Hayakawa K, Seki Y, Goto A, Hosokawa S.
- Toxicologic pathology. 2018 04;46(3)283-289.
- Mifepristone, which is an orally active synthetic steroid with antiprogesterone activity, is known as an ovarian toxicant. Because the available data regarding the histopathologic characteristics of ovarian toxicity in nonhuman primates are limited, the present study was undertaken in order to inves
- PMID 29558845
Japanese Journal
- 症例報告 帝王切開瘢痕部妊娠に対してメトトレキサートと抗プロゲステロン製剤併用療法を行った1例
- ISP-5-5 The Effect of GnRH Agonist, Serm, Antiprogesterone in the Treatment of Uterine Myomas(Group 5 Women's Health 2,IS Poster,International Session) :
- シンポジウム１７‐２ 難治性末梢神経疾患の治療戦略 Ｃｈａｒｃｏｔ－Ｍａｒｉｅ－Ｔｏｏｔｈ病の治療戦略