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).[1]
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).[2]
Sivifene (A-007) was initially thought to be a SERM due to its structural similarity to tamoxifen but it was subsequently found not to bind to the estrogen receptor (ER).[8]Tesmilifene (DPPE; YMB-1002, BMS-217380-01) is also structurally related to tamoxifen but similarly does not bind to the ER and is not a SERM.[9][10]
Structure[]
SERMs can be variously classified structurally as triphenylethylenes (tamoxifen, clomifene, toremifene, droloxifene, idoxifene, ospemifene, fispemifene, afimoxifene, others), benzothiophenes (raloxifene, arzoxifene), indoles (bazedoxifene, zindoxifene, pipendoxifene), tetrahydronaphthalenes (lasofoxifene, nafoxidine), and benzopyrans (acolbifene, ormeloxifene, levormeloxifene).[11][12][13]
References[]
^ abPinkerton, JoAnn V.; Thomas, Semara (2014). "Use of SERMs for treatment in postmenopausal women". The Journal of Steroid Biochemistry and Molecular Biology. 142: 142–154. doi:10.1016/j.jsbmb.2013.12.011. ISSN0960-0760. PMID24373794. S2CID24196362.
^Eilender, David; LoRusso, Patricia; Thomas, Leonard; McCormick, Catherine; Rodgers, Andrew H.; Hooper, Catherine L.; Tornyos, Karl; Krementz, Edward T.; Parker, Steven; Morgan, Lee Roy (2005). "4,4′-Dihydroxybenzophenone-2,4-dinitrophenylhydrazone (A-007): a topical treatment for cutaneous metastases from malignant cancers". Cancer Chemotherapy and Pharmacology. 57 (6): 719–726. doi:10.1007/s00280-005-0124-2. ISSN0344-5704. PMID16184382. S2CID10830366.
^Brandes LJ (2008). "N,N-diethyl-2-[4-(phenylmethyl) phenoxy] ethanamine (DPPE; tesmilifene), a chemopotentiating agent with hormetic effects on DNA synthesis in vitro, may improve survival in patients with metastatic breast cancer". Hum Exp Toxicol. 27 (2): 143–7. doi:10.1177/0960327108090751. PMID18480139. S2CID20966915.
^Brandes LJ, Hermonat MW (1984). "A diphenylmethane derivative specific for the antiestrogen binding site found in rat liver microsomes". Biochem. Biophys. Res. Commun. 123 (2): 724–8. doi:10.1016/0006-291x(84)90289-4. PMID6548377.
^John P. Bilezikian; Lawrence G. Raisz; T. John Martin (29 September 2008). Principles of Bone Biology. Academic Press. pp. 891–. ISBN978-0-08-056875-1.
Anabolic steroids (e.g., testosterone and esters, methyltestosterone, metandienone (methandrostenolone), nandrolone and esters, many others; via estrogenic metabolites)