II. Indications
- Indications vary with specific SERM effects
-
Hormone Replacement in postmenopausal women
- Beyond hot flash stage
- Estrogen Replacement contraindicated (Breast Cancer)
- Raloxifene
- Breast Cancer Prevention in post-menopausal women
- Breast Cancer risk >1.66% in 5 years
- Raloxifene
- Tamoxifen
- Breast Cancer Prevention in pre-Menopause
- Breast Cancer risk >1.66% in 5 years and age over 35 years old
- Tamoxifen
- Refractory Atrophic Vaginitis with severe Dyspareunia
- Ospemifene (Osphena)
-
Osteoporosis Prevention in postmenopausal women
- HRT is now only recommended for menopausal symptom management
- Raloxifene
III. Contraindications
- Venous Thromboembolism
- Perioperative period
- Prolonged immobilization
- History of Cerebrovascular Accident (CVA) or Transient Ischemic Attack (TIA)
IV. Mechanism
- Selective Estrogen Receptor Modulator (SERM)
- Diverse group of agents that bind Estrogen receptors with variable activity depending on their target tissue
- Most SERMs in use are estrogen Antagonists at Breast and endometrial tissue
V. Medications
-
Raloxifene
- Indicated for breast Cancer Prevention in post-menopausal women and Hormone replacment therapy
- Historically used for Osteoporosis Prevention
- HRT is now only recommended for menopausal symptom management
-
Tamoxifen
- Indicated for Breast Cancer Prevention in pre-Menopauseal and post-menopausal women
- Ospemifene (Osphena)
- Indicated for refractory Atrophic Vaginitis with severe Dyspareunia
- Avoid in Estrogen-dependent cancer, Venous Thromboembolism, Cardiovascular Risk, pregnancy
- Dosing: 60 mg orally daily with food
-
Bazedoxifene
- Combined with Estrogen in Duavee, a Tissue-selective Estrogen Complex (TSEC)
- Indicared for Estrogen Replacement Therapy in patients with an intact Uterus
- Alternative to combination Estrogen with Progesterone
- Fulvestrant
- Synthetic Estrogen receptor Antagonist
- Competitively binds Estrogen receptors in Breast Cancer cells, decreasing Estrogen receptor binding
- May be effective in Tamoxifen-resistant, Estrogen-sensitive, Breast Cancer
- Other agents
- Droloxifene
- Idoxifene
- Toremifene
VI. Adverse Effects
- Hot Flashes
- Leg Cramps
- Increased Deep Vein Thrombosis and Thromboembolism risk
- DVT, PE and Cardiovascular Risk is an FDA black box warning
- More likely to occur in first 4 months of treatment
- Similar to risk with Estrogen Replacement
VII. Resources
VIII. References
Images: Related links to external sites (from Bing)
Related Studies
| osphena (on 12/20/2023 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| OSPHENA 60 MG TABLET | $7.75 each | |
Ontology: droloxifene (C0047498)
| Definition (NCI) | A phenolic analogue of tamoxifen, a nonsteroidal selective estrogen receptor modulator (SERM). Droloxifene competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. (NCI) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C038345 |
| English | meta-hydroxytamoxifen, Phenol, 3-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-butenyl)-, (E)-, 3-Hydroxytamoxifen, (E)--1-[4'-(2-dimethylaminoethyoxy)phenyl]-1(3-hydroxyphenyl)-2-phenyl-but-1-ene, (E)-3-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]phenol, (E)-alpha[p-[2-(dimethylamino)ethoxy]phenyl]-alpha'-ethyl-3-stilbenol, droloxifene, 3-hydroxytamoxifen, DROLOXIFENE, Droloxifene |
Ontology: Toremifene (C0076836)
| Definition (NCI) | A nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which are manifested according to tissue type or species. (NCI04) |
| Definition (NCI_NCI-GLOSS) | An anticancer drug that belongs to the family of drugs called antiestrogens. Toremifene blocks the effect of the hormone estrogen in the body. It may help control some cancers from growing, and it may delay or reduce the risk of cancer recurrence. |
| Definition (MSH) | A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. |
| Definition (PDQ) | A nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which are manifested according to tissue type or species. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41103&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41103&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1256" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D017312 |
| SnomedCT | 387588002, 96378009 |
| English | Ethanamine, 2-(4-(4-chloro-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, (Z)-, (Z)-2-[4-(4-Chloro-1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine, (Z)-4-Chloro-1,2-diphenyl-1[4-[2-(N,N-dimethylamino)ethoxy]phenyl]-1-butene, toremifene citrate, toremifene citrate (medication), toremifene citrate (Fareston), Toremifene [Chemical/Ingredient], toremifene, TOREMIFENE, Toremifene (product), Toremifene (substance), TOR, Toremifene |
| Swedish | Toremifen |
| Czech | toremifen |
| Finnish | Toremifeeni |
| Russian | TOREMIFEN, ТОРЕМИФЕН |
| Japanese | トレミフェン |
| Polish | Toremifen |
| Spanish | toremifeno (producto), toremifeno (sustancia), toremifeno, Toremifeno |
| French | Torémifène |
| German | Toremifen |
| Italian | Toremifene |
| Portuguese | Toremifeno |
Ontology: idoxifene (C0139560)
| Definition (NCI_NCI-GLOSS) | A drug that blocks the effects of estrogen. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C071362 |
| English | 1-(4-iodophenyl)-1-(4-(2-pyrrolidinoethoxy)phenyl)-2-phenyl-1-butene, 4-iodopyrrolidinotamoxifen, Pyr-I-Tam, Pyrrolidino-4-iodotamoxifen, 1-[2-[4-[(1E)-1-(4-Iodophenyl)-2-phenyl-1-butenyl]phenoxy]ethyl]pyrrolidine, idoxifene, pyrrolidino-4-iodotamoxifen, IDOXIFENE, Idoxifene |
| Japanese | イドキシフェン |
Ontology: Selective Estrogen Receptor Modulators (C0732611)
| Definition (NCI_NCI-GLOSS) | A drug that acts like estrogen on some tissues but blocks the effect of estrogen on other tissues. Tamoxifen and raloxifene are selective estrogen receptor modulators. |
| Definition (CSP) | structurally diverse group of compounds distinguished from estrogen by their ability to bind and activate the estrogen receptor, but act as either an estrogen agonist or antagonist depending on the tissue type and hormonal milieu; classified as either first generation because they demonstrate estrogen agonist properties in the endometrium or second generation based on their patterns of tissue specificity. |
| Definition (MSH) | A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63) |
| Concepts | Pharmacologic Substance (T121) , Hormone (T125) |
| MSH | D020845 |
| SnomedCT | 109030001, 415515000 |
| French | Modulateurs sélectifs des récepteurs estrogéniques, Modulateurs sélectifs des récepteurs oestrogéniques, Modulateurs spécifiques des récepteurs aux oestrogènes, Modulateurs spécifiques des récepteurs aux estrogènes, SERM (Selective Estrogen Receptor Modulators), Modulateurs sélectifs des récepteurs des oestrogènes, Modulateurs sélectifs du récepteur aux oestrogènes, Modulateurs sélectifs du récepteur des oestrogènes |
| Swedish | Selektiva estrogenreceptormodulatorer |
| English | ESTROGEN RECEPT MODULATORS SELECTIVE, SELECTIVE ESTROGEN RECEPT MODULATORS, Select estrogen recpt modultor, Estrogen Receptor Modulator, Selective, Estrogen Receptor Modulators, Selective, Selective Estrogen Receptor Modulator, SERM, SERMs, Selective Estrogen Receptor Modulators, serms, selective estrogen receptor modulator (SERM), serm, Selective estrogen receptor modulators, selective estrogen receptor modulator, Selective estrogen receptor modulator, Selective oestrogen receptor modulator, Selective estrogen receptor modulator (product), Selective estrogen receptor modulator (substance), SERM - Selective estrogen receptor modulator, SERM - Selective oestrogen receptor modulator, Selective Estrogen Receptor Modifying Agents |
| Czech | receptory estrogenů - selektivní modulátory, SERMs |
| Finnish | Selektiiviset estrogeenireseptorin modulaattorit |
| Russian | ESTROGENNYKH RETSEPTOROV MODULIATORY IZBIRATEL'NYE, ЭСТРОГЕННЫХ РЕЦЕПТОРОВ МОДУЛЯТОРЫ ИЗБИРАТЕЛЬНЫЕ |
| Japanese | エストロゲン受容体モジュレーター-選択的, 選択的エストロゲン受容体モジュレーター, 選択的エストロゲン受容体修飾薬, 選択的エストロゲン受容体調節薬 |
| Spanish | Moduladores Selectivos de los Receptores de Estrógeno, Moduladores Selectivos de Receptores de Estrógeno, modulador selectivo del receptor estrógénico (producto), modulador selectivo del receptor estrógénico, modulador selectivo del receptor estrogénico (producto), Moduladores Selectivos de los Receptores Estrogénicos, Moduladores Selectivos del Receptor Estrogénico, Moduladores Selectivos de los Receptores de Estrógenos, modulador selectivo del receptor de estrógeno (producto), modulador selectivo del receptor de estrógeno (sustancia), modulador selectivo del receptor de estrógeno, modulador selectivo del receptor estrogénico, modulador selectivo de receptor de estrógeno (sustancia), modulador selectivo de receptor de estrógeno, Mress |
| Italian | Modulatori selettivi dei recettori estrogenici, Modulatori selettivi degli estrogeno-recettori, SERM, Modulatori selettivi dei recettori degli estrogeni |
| Polish | Modulatory receptora estrogenowego selektywne |
| Norwegian | Selektive østrogenreseptormodulerende stoffer, Østrogenreseptormodulerende stoffer, selektive, SERM, SERMs |
| Portuguese | Moduladores Seletivos dos Receptores de Estrógenos, Moduladores Seletivos dos Receptores Estrogênicos, Moduladores Seletivos de Receptor de Estrógeno, Moduladores Seletivos de Receptores Estrogênicos, Moduladores Seletivos de Receptor Estrogênico, SERMs, Moduladores Seletivos de Receptor de Estrogênio |
| German | SERMs, Östrogen-Rezeptor-Modulatoren, selektive, Selektive Östrogen-Rezeptor-Modulatoren |
Ontology: fulvestrant (C0935916)
| Definition (NCI_NCI-GLOSS) | A drug used to treat certain types of breast cancer in postmenopausal women. It is also being studied in the treatment of other types of cancer. Faslodex blocks estrogen activity in the body and is a type of antiestrogen. |
| Definition (NCI) | A synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines. (NCI04) |
| Definition (PDQ) | A synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43053&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43053&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1379" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Steroid (T110) |
| MSH | C070081 |
| SnomedCT | 385519002, 404845006 |
| English | 7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)estra-1,3,5(10)-triene-3,17-diol, 7a-[9-[(4,4,5,5,5,-Pentafluoropentyl)sulphinyl]nonyl]-estra-1,3,5(10)-triene-3,17b-diol, fulvestrant (medication), FULVESTRANT, fulvestrant [Chemical/Ingredient], fulvestrant, Fulvestrant, Fulvestrant (substance), Fulvestrant (product) |
| Spanish | fulvestrant (sustancia), fulvestrant, fulvestrant (producto) |
Ontology: Ospemifene (C1313616)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C119141 |
| Japanese | オスペミフェン |
| English | OSPEMIFENE, ospemifene, Ospemifene, Z-2-(4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol |
