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List Of Selective Estrogen Receptor Modulators
This is a list of selective estrogen receptor modulators (SERMs). Approved SERMs that have been approved for medical use include anordrin (+mifepristone (Zi Yun)), bazedoxifene ( +conjugated estrogens (Duavee)), broparestrol (Acnestrol), clomifene (Clomid), cyclofenil (Sexovid), lasofoxifene (Fablyn), ormeloxifene (Centron, Novex, Novex-DS, Sevista), ospemifene (Osphena; deaminohydroxytoremifene), raloxifene (Evista), tamoxifen (Nolvadex), and toremifene (Fareston; 4-chlorotamoxifen). Clinical trials SERMs that are currently under development and in clinical trials include acolbifene, afimoxifene (4-hydroxytamoxifen; metabolite of tamoxifen), elacestrant, enclomifene ((''E'')-clomifene), endoxifen (4-hydroxy-''N''-desmethyltamoxifen; metabolite of tamoxifen), and zuclomifene ((''Z'')-clomifene).http://adisinsight.springer.com/ Non-approved SERMs that have not been approved for medical use include arzoxifene, brilanestrant, clomifenoxide (clomiphene N-oxide; metabolite of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tamoxifen2DACS
Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and treat breast cancer in women and men. It is also being studied for other types of cancer. It has been used for Albright syndrome. Tamoxifen is typically taken daily by mouth for five years for breast cancer. Serious side effects include a small increased risk of uterine cancer, stroke, vision problems, and pulmonary embolism. Common side effects include irregular periods, weight loss, and hot flashes. It may cause harm to the baby if taken during pregnancy or breastfeeding. It is a selective estrogen-receptor modulator (SERM) and works by decreasing the growth of breast cancer cells. It is a member of the triphenylethylene group of compounds. Tamoxifen was initially made in 1962, by chemist Dora Richardson. It is on the World Health Organization's List of Essential Medicines. Tamoxifen is available as a generic medication. In ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elacestrant
Elacestrant (INN) (developmental code names RAD-1901, ER-306323) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) (described as a "SERM/SERD hybrid (SSH)") that was discovered by Eisai and is under development by Radius Health and Takeda for the treatment estrogen receptor (ER)-positive advanced breast cancer. Elacestrant has dose-dependent, tissue-selective estrogenic and antiestrogenic activities, with biphasic weak partial agonist activity at the ER at low doses and antagonist activity at higher doses. It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues. Unlike the SERD fulvestrant, elacestrant is able to readily cross the blood-brain-barrier into the central nervous system, where it can target breast cancer metastases in the brain, and is orally bioavailable and does not require intramuscular injection. Menarini Group and Radius Health Announce Global License Agre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Miproxifene
Miproxifene ( INN) (former developmental code name DP-TAT-59) is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was never marketed. It is a derivative of afimoxifene (4-hydroxytamoxifen) in which an additional 4-isopropyl group is present in the β-phenyl ring. The drug has been found to be 3- to 10-fold more potent than tamoxifen in inhibiting breast cancer cell growth in ''in vitro'' models. Miproxifene is the active metabolite of miproxifene phosphate (TAT-59), a phosphate ester and prodrug of miproxifene that was developed to improve its water solubility. Miproxifene phosphate was under development for the treatment of breast cancer and reached phase III clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...s for this ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Levormeloxifene
Levormeloxifene (; developmental code names 6720-CDRI, NNC-460020) is a selective estrogen receptor modulator (SERM) which was being developed as an alternative to estrogen replacement therapy for the treatment and prevention of postmenopausal bone loss but did not complete development and hence was never marketed. The development was stopped because of a high incidence of gynecological side effects during clinical trials. Levormeloxifene is the levorotatory enantiomer of ormeloxifene, which, in contrast, has been marketed, though rather as a hormonal contraceptive Hormonal contraception refers to birth control methods that act on the endocrine system. Almost all methods are composed of steroid hormones, although in India one selective estrogen receptor modulator is marketed as a contraceptive. The origi .... See also * List of selective estrogen receptor modulators References External links Levormeloxifene - AdisInsight Abandoned drugs Benzopyrans Ethers Pyrroli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Idoxifene
Idoxifene (INN, USAN, BAN) (former developmental code names CB-7432, SB-223030), also known as pyrrolidino-4-iodotamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group which was under development for the treatment of breast cancer and postmenopausal osteoporosis but was never marketed.https://adisinsight.springer.com/drugs/800003448 It reached phase III clinical trials for postmenopausal osteoporosis and phase II clinical trials for breast cancer before development was discontinued in 1999 due to insufficient effectiveness in both cases. Chemistry Synthesis A large-scale chemical synthesis As a topic of chemistry, chemical synthesis (or combination) is the artificial execution of chemical reactions to obtain one or several products. This occurs by physical and chemical manipulations usually involving one or more reactions. In mod ... of idoxifene has been devised. References External links Idoxifene - AdisInsight ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fispemifene
Fispemifene (INN, USAN) (developmental code name HM-101) is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was developed for the treatment of male hypogonadism but was abandoned and never marketed. It reached phase II clinical trials for this indication before development was terminated in March 2016. The drug failed to achieve statistical significance on key effectiveness endpoint An endpoint, end-point or end point may refer to: * Endpoint (band), a hardcore punk band from Louisville, Kentucky * Endpoint (chemistry), the conclusion of a chemical reaction, particularly for titration * Outcome measure, a measure used as an e ...s in clinical trials and was discontinued by its developer for strategic reasons. See also * Ospemifene References External links Fispemifene - AdisInsight Primary alcohols Organochlorides Progonadotropins Selective estrogen receptor modulators Triphenylethylenes {{genito-urinary-drug-s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etacstil
Etacstil (developmental code names GW-5638, DPC974) is an orally active, nonsteroidal, combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was developed for the treatment of estrogen receptor-positive breast cancer. It was shown to overcome antiestrogen (tamoxifen, aromatase inhibitor, fulvestrant) resistance in breast cancer by altering the shape of the estrogen receptor, thus exhibiting SERD properties. Etacstil is a tamoxifen derivative and one of the first drugs to overcome tamoxifen-resistance. It is the predecessor of GW-7604, of which etacstil is a prodrug (GW-7604 being the 4-hydroxy metabolite of etacstil). This is analogous to the case of tamoxifen being a prodrug of afimoxifene (4-hydroxytamoxifen). Etacstil was developed in the early 1990s by Duke University, Glaxo Wellcome, and later, Dupont. In 2001, Bristol Myers-Squibb (BMS) acquired Dupont, and for non-scientific, corporate reasons, closed the trial and aba ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Droloxifene
Droloxifene ( INN, USAN) (former developmental code names FK-435, ICI-79280, K-060, K-21060E, RP-60850), also known as 3-hydroxytamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was developed originally in Germany and later in Japan for the treatment of breast cancer, osteoporosis in men and postmenopausal women, and cardiovascular disorders but was abandoned and never marketed. It reached phase II and phase III clinical trials for these indications before development was discontinued in 2000. The drug was found to be significantly less effective than tamoxifen in the treatment of breast cancer in two phase III clinical trials. Droloxifene is an analogue of tamoxifen, specifically 3-hydroxytamoxifen, but has been said to have 10- to 60-fold increased affinity for the estrogen receptor and reduced partial estrogen agonistic activity. The affinity of droloxifene for the estrogen receptor ranges from 0.2 to 15.2% relat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clomifenoxide
Clomifenoxide (INN), also known as clomifene ''N''-oxide, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that is described as an antiestrogen and " gonad stimulant" and was never marketed. It is an active metabolite of clomifene. See also * Afimoxifene * Endoxifen Endoxifen, also known as 4-hydroxy-''N''-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein kinase C (PKC) inhibitor. It is under development for the treatment ... References Human drug metabolites Organochlorides Progonadotropins Selective estrogen receptor modulators Triphenylethylenes Amine oxides {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brilanestrant
Brilanestrant ( INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceuticals and was under development by Genentech for the treatment of locally advanced or metastatic estrogen receptor (ER)-positive breast cancer. Development of brilanestrant was discontinued by Roche in April 2017. It reached phase II clinical trials for the treatment of breast cancer prior to the discontinuation of its development. Mechanism of action Similarly to tamoxifen, a SERM, brilanestrant shows some capacity to activate the ER in certain contexts and possesses weak estrogenic activity in the rat uterus, and unlike fulvestrant, which is currently the only SERD to have been marketed, brilanestrant is not a steroid and is orally bioavailable and does not need to be administered by intramuscular injection. Brilanestrant has been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arzoxifene
Arzoxifene (; developmental code name LY-353381) is a selective estrogen receptor modulator (SERM) of the benzothiophene group which was never marketed. It is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. Arzoxifene is a highly effective agent for prevention of mammary cancer induced in the rat by the carcinogen nitrosomethylurea and is significantly more potent than raloxifene in this regard. Arzoxifene is devoid of the uterotrophic effects of tamoxifen, suggesting that, in contrast to tamoxifen, it is unlikely that the clinical use of arzoxifene will increase the risk of developing endometrial carcinoma. Pharmacology Arzoxifene is a selective estrogen receptor modulator (SERM), and hence is a mixed agonist and antagonist of the estrogen receptor with tissue-selective estrogenic and antiestrogenic activity. It has antiestrogenic effects in the breast, mixed estrogenic and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
