II. Mechanism
III. Indication
- Osteoporosis Prevention in postmenopausal women
-
Hormone Replacement in postmenopausal women
- Beyond hot flash stage
- Estrogen Replacement contraindicated (Breast Cancer)
- Breast Cancer Prevention in post-menopausal women with Breast Cancer risk >1.66% in 5 years
- Lower efficacy than Tamoxifen for breast Cancer Prevention, but also lower Venous Thromboembolism and Endometrial Cancer Risks
IV. Contraindications
- Venous Thromboembolism
- Perioperative period
- Prolonged immobilization
- History of Cerebrovascular Accident (CVA) or Transient Ischemic Attack (TIA)
V. Advantages
- No Uterine endometrial stimulation (unlike Estrogen)
- Does not require concurrent Progestin use
- Does not stimulate Breast tissue (unlike Estrogen)
- No Breast swelling, tenderness, or pain
- No data yet on Breast Cancer
- Increases Bone Mineral Density
- Modest effect (1-2%) at hip, spine, and long bones
- Not as effective as Estrogen Replacement
- Positive lipid effects
- Lowers LDL 10-12%
- Lowers Total Cholesterol 6-7%
- Helps stabilize pelvic floor
- Protects against Uterine Prolapse
- Decreases Incidence of Urinary Incontinence
- Reduces pelvic surgery rate by 50%
- Goldstein (2001) Obstet Gynecol 98:91-6 [PubMed]
VI. Precautions
- DVT, PE and cardiovascular risk is an FDA black box warning
VII. Disadvantages
- Expensive: $65/month (Premarin is $20/month)
- Anti-Estrogen effects (Hot Flashes)
VIII. Adverse Effects
- Hot Flashes (24.6%)
- Leg Cramps (5.9%)
- Increased Deep Vein Thrombosis and Thromboembolism risk
- More likely to occur in first 4 months of treatment
- Similar to risk with Estrogen Replacement
IX. Dosing
- Raloxifene 60 mg PO daily
- Course of 5 years if used for breast Cancer Prevention
Images: Related links to external sites (from Bing)
Related Studies (from Trip Database) Open in New Window
| evista (on 4/19/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| EVISTA 60 MG TABLET | Generic | $1.24 each |
| raloxifene (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| RALOXIFENE HCL 60 MG TABLET | Generic | $1.24 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: Raloxifene (C0244404)
| Definition (NCI_NCI-GLOSS) | The active ingredient in a drug used to reduce the risk of invasive breast cancer in postmenopausal women who are at high risk of the disease or who have osteoporosis. It is also used to prevent and treat osteoporosis in postmenopausal women. It is also being studied in the prevention of breast cancer in certain premenopausal women and in the prevention and treatment of other conditions. Raloxifene blocks the effects of the hormone estrogen in the breast and increases the amount of calcium in bone. It is a type of selective estrogen receptor modulator (SERM). |
| Definition (NCI) | A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects. (NCI04) |
| Definition (CSP) | a selective estrogen receptor modulator; has both agonist and antagonist estrogen action. |
| Definition (MSH) | A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue. |
| Definition (PDQ) | A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43109&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43109&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1518" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D020849 |
| SnomedCT | 109029006, 419530003 |
| LNC | LP171633-3 |
| English | Methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-piperidinyl)ethoxy)phenyl)-, raloxifene, [6-Hydroxy-2-(4-hydroxyphenyl)-benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone, raloxifene (medication), Raloxifene, Raloxifene [Chemical/Ingredient], RALOXIFENE, Raloxifene (substance), RALOX, Keoxifene, Raloxifene (product) |
| Spanish | raloxifeno (producto), raloxifeno (sustancia), raloxifeno, Raloxifeno |
| Swedish | Raloxifen |
| Czech | raloxifen |
| Finnish | Raloksifeeni |
| Russian | RALOKSIFEN, РАЛОКСИФЕН |
| Italian | Keoxifene, Raloxifene |
| Polish | Raloksyfen |
| Japanese | ケオキシフェン, ラロキシフェン |
| French | Raloxifène |
| German | Raloxifen |
| Portuguese | Raloxifeno |
Ontology: Evista (C0720318)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D020849 |
| English | ELi Lilly Brand of Raloxifene, Lilly Brand of Raloxifene, Raloxifene Lilly Brand, evista, Evista |
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 |
