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Selective progesterone receptor modulator : ウィキペディア英語版
Selective progesterone receptor modulator
A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor. A characteristic that distinguishes such substances from receptor full agonists (such as progesterone) and full antagonists (such as aglepristone) is that their action differs in different tissues (agonist in some while antagonist in others). This mixed agonist/antagonist profile of action leads to selective stimulation or inhibition progesterone-like action in different tissues and furthermore raises the possibility of dissociation of desirable therapeutic effects from undesirable side effects in synthetic progesterone receptor drug candidates.
== Drugs ==

Members include:
* Mifepristone ("Mifeprex")
* Ulipristal acetate ("Ella")
* Asoprisnil (J867; status uncertain)
* Telapristone (CDB-4124; Proellex, Progenta; under development)
SPRM activity is mainly mediated via the progesterone receptor, where the endometrium is the major target tissue. In contrast to pure progesterone antagonist (PA) , such as Mifepristone, the ability to terminate the pregnancy is eliminated or at least minimised, from the SPRMs due to their partial progesterone agonist activity. Since SPRMs have a low affinity for the estrogen receptor, they are not thought to induce post-menopausal associated bone loss.〔 SPRM have been suggested for multiple gynaecological applications, such as contraception and emergency contraception, treatment for endometriosis, uterine leiomyoma and as a hormone replacing therapy in post-menopausal women SPRMs use has been associated with endometrial metaplasia , which calls for the need for a long-term safety assessment.〔

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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