Description
Droloxifeneisananti-estrogentriphenylthyleneselectiveestrogenreceptormodulator(SERM);itisananalogoftamoxifen.DroloxifeneactsasanestrogenreceptoragoNISTinboneandasanestrogenreceptorantagonistinbreasttissue.Asaresultoftheseactions,thiscompoundexhibitsanticancerchemotherapeutic,chemopreventive,anti-osteoporotic,andanti-resorptivebenefits.Inbreastcancercells,droloxifenedecreasesproductionofNOandincreaseslevelsofpro-apoptoticTGF-β.Droloxifeneincreasesapoptosisinlutealcellsinvivo,increasinglevelsofc-mycandincreasingtheBax/Bcl-2ratio.Inovariectomizedratsthatactasapostmenopausalanimalmodel,droloxifeneinhibitsboneresorptionandturnoveraswellasestrogen-relatedboneloss.ThiscompoundalsodecreaseslevelsofE-selectinandincreaseslevelsifvascularcellularadhesionmolecule1(VCAM-1)inclinicalsettings.
References
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