Editing Selective estrogen receptor modulator (section)

==Examples==

[[Tamoxifen]] is a first-line [[Hormone therapy|hormonal treatment]] for ER-positive metastatic [[breast cancer]]. It is used for breast cancer risk reduction in women at high risk, and as [[Adjuvant therapy|adjuvant treatment]] for [[axillary node]]-negative and node-positive [[ductal carcinoma]] ''[[in situ]]''.<ref name="Pickar_2015" /><ref name="Mirkin_2015" /> Tamoxifen treatment is also used for the treatment of [[osteoporosis]] and [[blood lipids]] in postmenopausal women. Adverse effects of tamoxifen include [[hot flash]]es and an increase in the risk of developing [[endometrial cancer]] compared to women of similar age.<ref name="Mirkin_2015" /><ref name="Maximov_2013" />

[[Toremifene]], a [[chlorinated]] tamoxifen derivative developed to avoid [[Hepatocellular carcinoma|hepatic carcinomas]], was associated with fewer [[DNA adducts]] in the liver than tamoxifen in [[preclinical studies]]. It is used as [[Endocrine system|endocrine]] therapy for women with estrogen or [[progesterone receptor]]-positive, stage 4 or recurrent metastatic breast cancer<ref name="Miller_2002" /> and has demonstrated similar efficacy compared to tamoxifen as adjuvant treatment of breast cancer and in the treatment of metastatic breast cancer.<ref name="Mirkin_2015" />

[[Raloxifene]] is used for the prevention and treatment of [[Menopause|postmenopausal]] osteoporosis and breast cancer prevention in high-risk postmenopausal women with osteoporosis.<ref name=Pickar_2015 /> Preclinical and clinical reports suggest that it is considerably less potent than estrogen for the treatment of osteoporosis. It is associated with an acceptable endometrial profile and has not demonstrated tamoxifen-like effects on the uterus, but has been associated with adverse effects such as [[venous thromboembolism]] and vasomotor symptoms, including hot flushes.<ref name="Maximov_2013"/>

[[Ospemifene]] is an analogous [[metabolite]] of toremifene. Unlike tamoxifen, toremifene is not a rat [[hepatocarcinogen]], and therefore ospemifene would also be a safer SERM than tamoxifen.<ref name="Maximov_2013"/> It is used for the treatment of moderate to severe dyspareunia, a symptom of [[vulva]]r and [[Atrophic vaginitis|vaginal atrophy]] associated with menopause. Clinical data on breast cancer are not available, but both ''in vitro'' and ''in vivo'' data suggest that ospemifene may have [[chemopreventive]] activity in breast tissue.<ref name="Mirkin_2015" />

[[Bazedoxifene]] is used for treatment of osteoporosis in postmenopausal women at increased risk of [[Bone fracture|fracture]]. It has been shown to be relatively safe and well-tolerated. It shows no breast or endometrial stimulation and in the first two years the small increase is better in venous thromboembolism, and similar in the long term to other SERMs. The advantage of bazedoxifene over raloxifene is that it increases [[endothelial nitric oxide synthase]] activity and does not antagonize the effect of [[17β-estradiol]] on vasomotor symptoms.<ref name=Pickar_2015 />

The first [[tissue-selective estrogen complex]] (TSEC) combines [[conjugated estrogens]] and the SERM bazedoxifene to blend their activities. The combination therapy is used in the treatment of moderate to severe vasomotor symptoms associated with menopause, prevention of postmenopausal osteoporosis as well as treatment of [[Hypoestrogenism|estrogen deficiency]] symptoms in non-[[Hysterectomy|hysterectomized]] postmenopausal women. The combination allows for the benefits of estrogen with regard to relief of vasomotor symptoms without estrogenic stimulation of the [[endometrium]].<ref name=Pickar_2015 /><ref name="Mirkin_2015" />

SERMs have also been used in [[hormone replacement therapy]] by some [[transgender]] people.<ref>{{cite journal |last1=Xu |first1=Jane Y. |last2=O'Connell |first2=Michele A. |last3=Notini |first3=Lauren |last4=Cheung |first4=Ada S. |author4-link=Ada Cheung |last5=Zwickl |first5=Sav |last6=Pang |first6=Ken C. |title=Selective Estrogen Receptor Modulators: A Potential Option For Non-Binary Gender-Affirming Hormonal Care? |journal=Frontiers in Endocrinology |date=18 June 2021 |volume=12 |pages=701364 |doi=10.3389/fendo.2021.701364 |pmid=34226826 |pmc=8253879 |issn=1664-2392 |doi-access=free }}</ref>

[[10β,17β-Dihydroxyestra-1,4-dien-3-one|DHED]] is a '''centrally selective''', orally active prodrug of estradiol. 

=== Available forms ===
{| class="wikitable sortable mw-collapsible <!--mw-collapsed-->" style="margin-left: auto; margin-right: auto; border: none;"
|+ class="nowrap" | SERMs marketed for clinical or veterinary use
|-
! Name !! Brand&nbsp;name !! Approved uses !! Launch !! Notes
|-
| [[Anordrin]] || Zi Yun || [[Emergency contraception]] || 1970s || Only in [[China]], combined with [[mifepristone]]
|-
| [[Bazedoxifene]] || Duavee || [[Osteoporosis]] prevention || 2013 || Combined with [[conjugated estrogens]]
|-
| [[Broparestrol]] || Acnestrol || [[Dermatology]]; [[Breast cancer]] treatment || 1970s || Discontinued
|-
| [[Clomifene]] || Clomid || [[Female infertility]] || 1967 ||
|-
| [[Cyclofenil]] || Sexovid || Female infertility; [[Menopausal symptoms]] || 1970 || Mostly discontinued
|-
| [[Lasofoxifene]] || Fablyn || Osteoporosis prevention, treatment; [[Vaginal atrophy]] || 2009 || Only in [[Lithuania]] and [[Portugal]]
|-
| [[Ormeloxifene]] || Saheli || [[Hormonal contraception]] || 1991 || Only in [[India]]
|-
| [[Ospemifene]] || Osphena || [[Dyspareunia]] due to vaginal atrophy || 2013 ||
|-
| [[Raloxifene]] || Evista || Osteoporosis prevention, treatment; Breast cancer prevention || 1997 ||
|-
| [[Tamoxifen]] || Nolvadex || Breast cancer treatment || 1978 ||
|-
| [[Toremifene]] || Fareston || Breast cancer treatment || 1997 ||
|- class="sortbottom"
| colspan="5" style="width: 1px; background-color:#eaecf0; text-align: center;" | '''Sources:''' See individual articles.
|}