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Evista
Aka: Evista, Raloxifene, Droloxifene, Idoxifene, Toremifene, Selective Estrogen Receptor Modulator, SERM- See Also
- Mechanism
- Indication
- Osteoporosis Prevention in postmenopausal women
- Hormone Replacement in postmenopausal women
- Beyond hot flash stage
- Estrogen Replacement contraindicated (Breast Cancer)
- 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
- No Uterine endometrial stimulation (unlike Estrogen)
- Precautions
- DVT, PE and cardiovascular risk is an FDA black box warning
- Disadvantages
- Expensive: $65/month (Premarin is $20/month)
- Anti-Estrogen effects (Hot Flashes)
- 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
- Dosing
- Raloxifene 60 mg PO qd
- Reference
| Medication Costs | ||
|---|---|---|
| Evista (on 2/9/2012 at DrugStore.com) | ||
| Evista 60mg Tablets | #30 for $149.99 | ($5.00/unit) |
| FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. | ||
droloxifene (C0047498) |
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|---|---|
| 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 | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C038345 |
| English | 3-hydroxytamoxifen, 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, droloxifene, Droloxifene |
| Sources |
Derived from the NIH UMLS (Unified Medical Language System) |
Raloxifene (C0244404) |
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|---|---|
| Definition (NCI) | 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 (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 (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 (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 | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | D020849 |
| SnomedCT | 109029006, 419530003 |
| 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, raloxifene (medication), Raloxifene, Raloxifene [Chemical/Ingredient], 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 |
| Sources |
Derived from the NIH UMLS (Unified Medical Language System) |
pyrrolidino-4-iodotamoxifen (C0139560) |
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|---|---|
| Definition (NCI) | A drug that blocks the effects of estrogen. |
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C071362 |
| English | 1-(4-iodophenyl)-1-(4-(2-pyrrolidinoethoxy)phenyl)-2-phenyl-1-butene, pyrrolidino-4-iodotamoxifen, 4-iodopyrrolidinotamoxifen, Pyr-I-Tam, idoxifene, Pyrrolidino-4-iodotamoxifen, 1-[2-[4-[(1E)-1-(4-Iodophenyl)-2-phenyl-1-butenyl]phenoxy]ethyl]pyrrolidine, IDOXIFENE, Idoxifene |
| Japanese | イドキシフェン |
| Sources |
Derived from the NIH UMLS (Unified Medical Language System) |
Evista (C0720318) |
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|---|---|
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | D020849 |
| English | ELi Lilly Brand of Raloxifene, Lilly Brand of Raloxifene, Raloxifene Lilly Brand, evista, Evista |
| Sources |
Derived from the NIH UMLS (Unified Medical Language System) |
Toremifene (C0076836) |
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|---|---|
| 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 (NCI) | 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 (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 (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 | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | D017312 |
| SnomedCT | 387588002, 96378009 |
| English | Ethanamine, 2-(4-(4-chloro-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, (Z)-, toremifene, (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, toremifene citrate, toremifene citrate (medication), toremifene citrate (Fareston), Toremifene [Chemical/Ingredient], 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 |
| Sources |
Derived from the NIH UMLS (Unified Medical Language System) |
Selective Estrogen Receptor Modulators (C0732611) |
|
|---|---|
| Definition (NCI) | 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) |
| MSH | D020845 |
| SnomedCT | 109030001, 415515000 |
| English | selective estrogen receptor modulator, 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, Estrogen Agonist/Antagonist [EPC], Estrogen Agonist/Antagonist, Mixed Estrogen Agonist and Antagonist, serms, selective estrogen receptor modulator (SERM), serm, 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 |
| 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 |
| 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 del Receptor Estrogénico, Moduladores Selectivos de Receptores de Estrogeno, Moduladores Selectivos de los Receptores de Estrógeno, Moduladores Selectivos de los Receptores Estrogénicos, Moduladores Selectivos de los Receptores de Estrógenos, Moduladores Selectivos de los Receptores de Estrogenos, Moduladores Selectivos de los Receptores de Estrogeno, Moduladores Selectivos de los Receptores Estrogenicos, Moduladores Selectivos de Receptores de Estrógeno, Moduladores Selectivos del Receptor Estrogenico, modulador selectivo del receptor estrógénico (producto), modulador selectivo del receptor estrógénico, modulador selectivo del receptor estrogénico (producto), 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 |
| Portuguese | Moduladores Seletivos de Receptores Estrogênicos, Moduladores Seletivos dos Receptores de Estrógenos, Moduladores Seletivos dos Receptores Estrogênicos, Moduladores Seletivos de Receptor de Estrógeno, Moduladores Seletivos de Receptor Estrogênico, SERMs, Moduladores Seletivos de Receptor de Estrogênio |
| Italian | Modulatori selettivi dei recettori estrogenici, Modulatori selettivi degli estrogeno-recettori, SERM, Modulatori selettivi dei recettori degli estrogeni |
| Polish | Modulatory receptora estrogenowego selektywne |
| German | SERMs, Östrogen-Rezeptor-Modulatoren, selektive, Selektive Östrogen-Rezeptor-Modulatoren |
| Sources |
Derived from the NIH UMLS (Unified Medical Language System) |