Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive difference among these drugs (i.e., the key difference) is their endometrial safety. Compared to bisphosphonate drug formulations for osteoporosis, SERMs are to be used primarily in postmenopausal women of younger age and are particularly recommended if there is a family history of invasive breast cancer, as their use greatly reduces the incidence of this type of cancer in women. Among the above mentioned SERMs, raloxifene has been widely used in prevention and treatment of postmenopausal osteoporosis and vertebral compression fractures, and clinical studies are now underway to test the comparative advantages of raloxifene with those of bazedoxifene, a more recently developed SERM. Research on a number of adverse side effects of SERM agents is being performed to determine the long-term safety of this class of compouds for treatment of osteoporosis.
Breast Neoplasms ; Chemistry, Pharmaceutical ; Estrogens ; Female ; Fractures, Compression ; Humans ; Incidence ; Osteoporosis ; Osteoporosis, Postmenopausal ; Raloxifene Hydrochloride ; Selective Estrogen Receptor Modulators* ; Tamoxifen

OBJECTIVE: Our purpose was to evaluate potential efficacy of selective estrogen receptor modulators (raloxifene and tamoxifen) to human uterine leiomyoma cells. METHODS: The samples were collected from ten hysterectomized specimen. we evaluated the estrogen-responsive growth of human uterine leiomyoma and normal myometrial cells. The potential efficacy of Selective Estrogen Receptor Modulators (SERMs: raloxifene and tamoxifen) to human uterine leiomyoma cells were conducted by MTS, cell count assay and Western-blot. RESULTS: Human uterine leiomyoma and normal myometrial cells that expressed estrogen receptor (ER) showed increases the cell number in the presence of estrogen compared with ER negative uterine leiomyoma cells. Raloxifene and tamoxifen inhibited estrogen-stimulated proliferation of ER-containing human uterine leiomyoma and normal myometrial cells. Raloxifene was more effective in inhibiting estrogen-induced increases of cell number compared with tamoxifen. CONCLUSION: The effect of SERMs on leiomyoma was inhibited the cell proliferation without apoptosis or cell cycle arrest. These data suggest that SERM should be examined as candidate of nonsurgical therapeutic agents for uterine leiomyoma.
Apoptosis ; Cell Count ; Cell Cycle Checkpoints ; Cell Proliferation ; Estrogens ; Humans* ; Leiomyoma* ; Raloxifene Hydrochloride ; Selective Estrogen Receptor Modulators* ; Tamoxifen

No abstract available.
Breast Neoplasms* ; Tamoxifen*

No abstract available.
Humans* ; Ovarian Neoplasms* ; Tamoxifen*

Breast cancer is the second most common cancer in Korean women and its mortality rate has increased steadily. Although breast cancer is heterogeneous tumor, hormone receptor-positive tumors comprise about 75 percent of all breast cancers. Therefore endocrine therapy that works by targeting estrogen receptor is a pivotal treatment for breast cancers. There are selective estrogen receptor modulators, such as tamoxifen and raloxifene, aromatase inhibitors, such as anastrozole, letrozole and exemestane, fulvestrant and luteinizing hormone-releasing hormone agonists used in endocrine therapy. Endocrine therapy is effective in treating early breast cancer as an adjuvant therapy and metastatic breast cancer as a palliative therapy. Also in women who are at high risk for breast cancer, tamoxifen or raloxifene can prevent breast cancer. Studies for neoadjuvant endocrine therapy are emerging. Considering side effects of each drug and overcoming drug resistance are needed to maximize effectiveness of treatment and advance endocrine therapy.
Antineoplastic Agents, Hormonal ; Aromatase Inhibitors ; Breast ; Breast Neoplasms* ; Drug Resistance ; Drug Therapy ; Estrogens ; Female ; Gonadotropin-Releasing Hormone ; Humans ; Mortality ; Palliative Care ; Raloxifene Hydrochloride ; Selective Estrogen Receptor Modulators ; Tamoxifen

Adenosarcoma of the uterus is a rare biphasic tumor containing benign glandular epithelial and malignant mesenchymal components. The tumor has been reported to be associated with antiestrogen therapy, particularly tamoxifen, but there have been a few case reports with MRI. We present two cases of MRI findings of uterine adenosarcoma after antiestrogen therapy, tamoxifen and toremifene in breast cancer patients. The tumor presents as a large polypoid mass occupying the endometrial cavity, and may protrude into the vagina. On MRI, the tumor typically shows solid components with scattered small cysts and heterogeneous enhancement. These findings are not significantly different from conventional adenosarcoma.
Adenosarcoma* ; Breast Neoplasms ; Estrogen Receptor Modulators ; Humans ; Magnetic Resonance Imaging* ; Tamoxifen ; Toremifene ; Uterus ; Vagina

Antiestrogens have been widely used in the treatment of breast cancer patients. Although tamoxifen is one of the most prevalent antiestrogens, some reported its hepatocarcinogenic effects and the long-term treatment may increase the risk of endometrial and gastrointestinal cancer. Toremifene is an interesting new antiestrogen and have a similar antitumor efficacy as tamoxifen, with less side-effect including less uterotrophic effect compared to tamoxifen, in mice. we report a case of endometrial polyp which were associated with toremifene use, in postmenopausal woman with breast cancer, with a brief review of literature.
Animals ; Breast Neoplasms ; Estrogen Receptor Modulators ; Female ; Gastrointestinal Neoplasms ; Humans ; Mice ; Polyps* ; Tamoxifen ; Toremifene

Toremifene is an anti-estrogen which has been shown to be effective in the treatment of breast cancer, and is thought to be a less uterotrophic agent than tamoxifen. The risk assessment concerning endometrial cancer has been inconclusive because of its rare use up to the mid-1990s. We report a case of an adenosarcoma, which is a very rare type of uterine malignancy, after toremifene treatment for 5 years in a breast cancer patient. After 1 year of toremifene use, the patient had a benign Mullerian adenofibroma. After an additional 4 years of toremifene treatment, the endometrial polypoid lesion was transformed into a Mullerian adenosarcoma. Although toremifene is a promising anti-estrogenic agent in the treatment of breast cancer patients, clinicians should not neglect the possibility of a uterine malignancy.
Adenofibroma ; Adenosarcoma ; Breast ; Breast Neoplasms ; Endometrial Neoplasms ; Female ; Humans ; Risk Assessment ; Tamoxifen ; Toremifene

PURPOSE: This study was conducted to evaluate the use of toremifene as an adjuvant hormonal therapy for estrogen recepter (ER) positive early breast cancer patients in terms of therapeutic efficacy and effect on endometrium as compared with tamoxifen. METHODS: Between January 2001 and December 2003, 451 patients with stage 0, I and II breast cancer, received adjuvant hormone therapy that consisted of either tamoxifen (N=387) or toremifene (N=64). The recurrence rate and survival rate were compared between two groups and the incidence of of endometrial event was evaluated in 273 of the patients. RESULTS: The median follow up period was 57 months and the median hormonal therapy period was 51 months. During the follow up period, there were 3 (2.0%) recurrence in the stage I tamoxifen group, 19 recurrences (8.7%) and 3 deaths (1.4%) in the stage II tamoxifen group (n=219), however there were no instances of recurrence or death in all of the toremifene group. In addition, endometrial cancer developed in 2 patients in the tamoxifen group, but in no patients in toremifene group during the follow up period. Further 21 of the patients who began treatment using tamoxifen changed to toremifene due to adverse side effects. The toremifene was well tolerated by 15 of the patients that changed treatment regimes. CONCLUSION: Toremifene was found to be as effective and safe as tamoxifen, when used as an adjuvant hormonal therapeutic agent in ER-positive early breast cancer, therefore toremifene may be a good option in place of tamoxifen for patients who are experiencing adverse effects as a result of tamoxifen treatment.
Breast Neoplasms* ; Breast* ; Endometrial Neoplasms ; Endometrium* ; Estrogens* ; Female ; Follow-Up Studies ; Humans ; Incidence ; Recurrence ; Survival Rate ; Tamoxifen ; Toremifene*

PURPOSE: To evaluate the differences in therapeutic efficacy and toxicity profiles between adjuvant toremifene and tamoxifene in postmenopausal breast cancer patients. METHODS: Toremifene 40 mg (n=115) and tamoxifen 20 mg (n =116) were administered daily for more than 2 years after curative surgery for lymph node-negative breast cancer. Toxicity profiles were compared between the two groups and the patient survival rate was also analyzed. RESULTS: Sweating and hot flashes were the most common symptoms in the two groups (toremifene vs. tamoxifen= 47.8% vs. 49.1%). Increase of vaginal discharge (39.1% vs. 36.2%) and weight gain (21.7% vs. 24.1%) were the next following adverse effects. There was no significant difference in adverse effect between the two groups. During the median follow-up period of 25 months (range: 9~38 months), five (4.3%) and four (3.3%) patients treated by toremifene and tamoxifen, respectively, had recurrent disease. CONCLUSION: The clinical outcome and adverse effect profiles of toremifene were similar to those of tamoxifen. Toremifene at 40 mg/day seems to be as safe and effective as tamoxifen at 20 mg/day in the treatment of postmenopausal, node-negative, breast cancer. However, a longer follow-up study is needed to verify this.
Breast Neoplasms* ; Breast* ; Follow-Up Studies ; Hot Flashes ; Humans ; Survival Rate ; Sweat ; Sweating ; Tamoxifen* ; Toremifene* ; Vaginal Discharge ; Weight Gain