Estradiol/raloxifene - Misplaced Pages

Combination drug

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Pharmaceutical compound

Estradiol/raloxifene
Combination of
Estradiol	Estrogen
Raloxifene	Selective estrogen receptor modulator
Clinical data
Other names	E2/RLX; Raloxifene/estradiol; RLX/E2
Routes of administration	By mouth; Transdermal administration; Vaginal administration
Legal status
Legal status	US: ℞-only

Estradiol/raloxifene (E2/RLX) is a tissue-selective estrogen complex (TSEC) which was studied for potential use in menopausal hormone therapy but was never marketed. Today, E2/RLX is not generally used due to concerns of endometrial hyperplasia.

References

^ Pickar JH, Boucher M, Morgenstern D (September 2018). "Tissue selective estrogen complex (TSEC): a review". Menopause. 25 (9): 1033–1045. doi:10.1097/GME.0000000000001095. PMC 6110370. PMID 29533367.
Komm BS (December 2008). "A new approach to menopausal therapy: the tissue selective estrogen complex". Reprod Sci. 15 (10): 984–92. doi:10.1177/1933719108325759. PMID 19088368. S2CID 11875637.
Komm BS, Mirkin S, Jenkins SN (November 2014). "Development of conjugated estrogens/bazedoxifene, the first tissue selective estrogen complex (TSEC) for management of menopausal hot flashes and postmenopausal bone loss". Steroids. 90: 71–81. doi:10.1016/j.steroids.2014.06.004. PMID 24929044. S2CID 6342960.
Archer DF (July 2010). "Tissue-selective estrogen complexes: a promising option for the comprehensive management of menopausal symptoms". Drugs Aging. 27 (7): 533–44. doi:10.2165/11316000-000000000-00000. PMID 20583848. S2CID 23784261.
Pinkerton JV, Conner EA (April 2019). "Beyond estrogen: advances in tissue selective estrogen complexes and selective estrogen receptor modulators". Climacteric. 22 (2): 140–147. doi:10.1080/13697137.2019.1568403. PMID 30895900. S2CID 84842485.

Estrogen receptor modulators

ERTooltip Estrogen receptor

Agonists

Unknown/unsorted: ERB-26
ERA-45
ERB-79
ZK-283197

Xenoestrogens: Anise-related (e.g., anethole, anol, dianethole, dianol, photoanethole)
Chalconoids (e.g., isoliquiritigenin, phloretin, phlorizin (phloridzin), wedelolactone)
Coumestans (e.g., coumestrol, psoralidin)
Flavonoids (incl. 7,8-DHF, 8-prenylnaringenin, apigenin, baicalein, baicalin, biochanin A, calycosin, catechin, daidzein, daidzin, ECG, EGCG, epicatechin, equol, formononetin, glabrene, glabridin, genistein, genistin, glycitein, kaempferol, liquiritigenin, mirificin, myricetin, naringenin, penduletin, pinocembrin, prunetin, puerarin, quercetin, tectoridin, tectorigenin)
Lavender oil
Lignans (e.g., enterodiol, enterolactone, nyasol (cis-hinokiresinol))
Metalloestrogens (e.g., cadmium)
Pesticides (e.g., alternariol, dieldrin, endosulfan, fenarimol, HPTE, methiocarb, methoxychlor, triclocarban, triclosan)
Phytosteroids (e.g., digitoxin (digitalis), diosgenin, guggulsterone)
Phytosterols (e.g., β-sitosterol, campesterol, stigmasterol)
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol (teranol, β-zearalanol))
Steroid-like (e.g., deoxymiroestrol, miroestrol)
Stilbenoids (e.g., resveratrol, rhaponticin)
Synthetic xenoestrogens (e.g., alkylphenols, bisphenols (e.g., BPA, BPF, BPS), DDT, parabens, PBBs, PHBA, phthalates, PCBs)
Others (e.g., agnuside, rotundifuran)

Mixed
(SERMsTooltip Selective estrogen receptor modulators)

Antagonists

Coregulator-binding modulators: ERX-11

Noncompetitive inhibitors: Trilostane

GPERTooltip G protein-coupled estrogen receptor

Agonists	2-Methoxyestradiol 7β-Hydroxyepiandrosterone Afimoxifene (4-hydroxytamoxifen) Aldosterone Atrazine Bisphenol A Daidzein DDT (p,p'-DDT, o',p'-DDE) Diarylpropionitrile Equol Estradiol Ethinylestradiol Fulvestrant (ICI-182780) G-1 Genistein GPER-L1 GPER-L2 Hydroxytyrosol Kepone Nicotinic acid Nicotinamide Nonylphenol Oleuropein PCBs (2,2',5'-PCB-4-OH) Propylpyrazoletriol Quercetin Raloxifene Resveratrol STX Tamoxifen Tectoridin
Antagonists	CCL18 Estriol G-15 G-36 MIBE
Unknown	Diethylstilbestrol Zearalenone

See also: Receptor/signaling modulators; Estrogens and antiestrogens; Androgen receptor modulators; Progesterone receptor modulators; List of estrogens

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See also

References