Mifepristone

Mifepristone 속성

Mifepristone MSDS

11b-[p-(Dimethylamino)phenyl]-17b-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one

Mifepristone C화학적 특성, 용도, 생산

개요

Mifepristone is an orally-active progesterone and glucocorticoid receptor antagonist indicated for use as a post-coital contraceptive. In addition to being an abortifacient, mifepristone is reported to be effective in the treatment of ocular hypertension; its potential therapeutic effect in hormone-dependent tumors is currently under investigation.

화학적 성질

Pale Yellow Solid

용도

Mifepristone is a progesterone receptor antagonist with partial agonist activity. Abortifacient.

Indications

Mifepristone is a progesterone receptor antagonist that has a high affinity for glucocorticoid receptors and little agonist effect.This drug has recently been approved for use in the United States for the treatment of hypercortisolism. At high doses, mifepristone blocks negative feedback of the hypothalamic–pituitary axis, thereby increasing endogenous corticotrophin and cortisol levels. Because mifepristone exerts its effects at the receptor level and not by altering glucocorticoid production, elevated serum cortisol and corticotrophin levels may not accurately reflect the effectiveness of the therapeutic regimen. Mifepristone does not inhibit cortisol binding to the mineralocorticoid receptor, so that the resulting corticotrophin disinhibition may cause potassium depletion. Thus, administration of a mineralocorticoid receptor antagonist such as spironolactone may be indicated with mifepristone. Hypoadrenalism, nausea, and drowsiness have been reported during prolonged administration of mifepristone.

World Health Organization (WHO)

Mifepristone, an antiprogesterone used in combination with a prostaglandin for the termination of early pregnancy, was introduced in 1990. Use of the combination has been associated with episodes of coronary spasm that are attributed to administration of the prostaglandin and which have resulted in several cases of cardiac infarction and ventricular fibrillation. At least one of these incidents has been fatal.

생물학적 활성

Selective antagonist at progesterone (PR) and glucocorticoid (GR) receptors in vitro and in vivo . Is a silent antagonist at PR and has a higher affinity than progesterone. Has higher affinity for GR than dexamethasone.

Pharmacokinetics

Following oral administration, mifepristone is rapidly absorbed, with a peak plasmaconcentration in approximately 90 minutes , an oral bioavailability of approximately 70%, and a term inal elimination half-life of 18 hours. It is 98% protein bound, primarily to album in and α1-acid glycoprotein. Mifepristone is metabolized primarily via CYP3A4 pathways involving mono- and di-N-demethylation and terminal hydroxylation of the 17-propynyl chain. The fact that approximately 83% of the drug is recovered in the feces and 9% in the urine suggests a biliary route of elimination. Mifepristone also demonstrates antiglucocorticoid activity.

Clinical Use

An antiprogestin is a substance that competes with progesterone for its receptor and, ultimately, prevents progesterone from binding to and activating its receptor. Because progesterone is integral to the continuation of an early pregnancy, it is expected that antipro-gestins will interfere with pregnancy maintenance. In 1982, the first antiproges tin, mifepristone (RU 486), was reported. Mifepristone was shown to interrupt early stages of implantation and pregnancy in humans.

참고 문헌

https://pubchem.ncbi.nlm.nih.gov/compound/mifepristone#section=Top
https://www.drugbank.ca/drugs/DB00834
https://www.drugs.com/cdi/mifepristone-tablets.html

Mifepristone 준비 용품 및 원자재

원자재

준비 용품

Mifepristone 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei Bonster Technology Co.,Limited	+8613315996897	bsterltd.wendy@gmail.com	China	796	58
Hebei Kangcang new material Technology Co., LTD	+8619133911216	Jany1001@kangcang.com.cn	China	338	58
Hong Kong Excellence Biotechnology Co., Ltd.	+86-86-18838029171 +8618126314766	ada@sh-teruiop.com	China	892	58
Henan Tengmao Chemical Technology Co. LTD	+8615238638457	salesvip2@hntmhg.com	China	415	58
Wuhan Haorong Biotechnology Co.,ltd	+8618565342920	sales@chembj.net	China	269	58
Nantong Guangyuan Chemicl Co,Ltd	+undefined17712220823	admin@guyunchem.com	China	616	58
Henan Senhaibao Pharmaceutical Technology Co., Ltd	+86-85246382586 +86-15118143473	anlenone888@gmail.com	China	9	58
Shaanxi Franta Biotechnology Co., Ltd	+86-13082019107 +86-13082019107	admin@flanderff.com	China	229	58
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	524	58
Shanghai Aosiris new Material Technology Co., LTD	+8615139564871	wrjmoon2000@163.com	China	354	58

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