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Synonyms:RALOXIFENE HCL;RALOXIFENE HYDROCHLORIDE;ly156758 ;methanone,(6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-piperidin ;KEOXIFENE;KEOXIFENE HYDROCHLORIDE;LY 139481;AKOS 92138
storage temp. -20°C Freezer
solubility DMSO: 28 mg/mL, soluble
Raloxifene hydrochloride is a second-generation Selective Estrogen Receptor Modulator (SERM) of the benzothiophene family. This drug is similar in effect to tamoxifen, exhibiting estrogen receptor antagonist (blocking) properties in some tissues while acting as an estrogen receptor agonist (activator) in others.
The main point of variation between these two agents is their tissue selectivity. While raloxifene hydrochloride is a strong anti-estrogen in breast and uterine tissues, it appears to be estrogenic in bone. This allows it to protect bone density, mimicking the beneficial effects of endogenous estradiol. This is quite different from tamoxifen, which is anti-estrogenic in both breast and bone.
In a role that was novel for an anti-estrogen, raloxifene hydrochloride was approved by the FDA for the prevention and treatment of osteoporosis in post-menopausal women. It is also being investigated for several other potential uses, including the treatment and prevention of cardiovascular disease, breast cancer, gynecomastia, prostate cancer, acromegaly, and uterine cancer.
Raloxifene Hydrochloride is used to help prevent and treat thinning of the bones (osteoporosis) only in postmenopausal women.
It works like an estrogen to stop the bone loss that can develop in women after menopause, but it does not increase the bone density as much as daily 0.625 mg doses of conjugated estrogens. Raloxifene Hydrochloride will not treat hot flashes of menopause and may cause hot flashes to occur. Also, Raloxifene Hydrochloride does not stimulate the breast or uterus as estrogen does.
Raloxifene Hydrochloride lowers the blood concentrations of total and low-density lipoprotein (LDL) cholesterol, the bad cholesterols, but it does not increase concentrations of high-density lipoprotein (HDL) cholesterol, the good cholesterol, in your blood.
Raloxifene Hydrochloride is also used to lower chances of having invasive breast cancer in postmenopausal women with osteoporosis or at high risk of having invasive breast cancer .
This medicine is available only with your doctor's prescription.
Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, Raloxifene Hydrochloride is used in certain patients with the following medical conditions:
Breast cancer prevention in high-risk women who have already gone through menopause.
May prevent or treat corticosteroid-induced bone loss. American College of Rheumatology states that raloxifene can be offered to selected postmenopausal corticosteroid-treated women who refuse hormone replacement therapy or other antiresorptive agents or in whom such therapies are contraindicated.
Reduction in the incidence of invasive breast cancer inpostmenopausal women at high risk for developing the disease. Effect comparable to that of tamoxifen in reducing the risk of invasive breast cancer (STAR trial). No effect on the risk of lobular carcinoma in situ or ductal carcinoma in situ (STAR trial).
Effect on breast cancer incidence in women with BRCA1 or BRCA2 genetic mutations not established. Not indicated for the treatment of breast cancer or to reduce the risk of recurrence of breast cancer. 1 Not indicated for reduction in the risk of noninvasive breast cancer.
1. Amino acid, nutrient
2. Labeled , intended for use as an internal standard for the quantification by GC- or LC-mass
3. A nonsteroidal, selective estrogen receptor modulator (SERM). Antiosteoporotic.
Mechanism of Action
Evista (raloxifene hydrochloride) is an estrogen agonist/antagonist, referred to as a selective estrogen receptor modulator (SERM) and belongs to the benzothiophene class of compounds. The biological actions of raloxifene are largely mediated through binding to estrogen receptors.
This binding results in activation of estrogenic pathways in some tissues (agonism) and and the blockade of estrogenic pathways in other tissues (antagonism). The agonistic or antagonistic activity of raloxiffene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promotors.
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