Raloxifene

EVISTA ® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer.

Raloxifene is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM). 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 blockade of estrogenic pathways in others (antagonism). The agonistic or antagonistic action of raloxifene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promoters. Raloxifene appears to act as an estrogen agonist in bone. It decreases bone resorption and bone turnover, increases bone mineral density (BMD) and decreases fracture incidence. Preclinical data demonstrate that raloxifene is an estrogen antagonist in uterine and breast tissues.

60 mg tablet orally once daily. Recommended Dosing The recommended dosage is one 60 mg EVISTA (raloxifene hydrochloride tablets) tablet daily, which may be administered any time of day without regard to meals. For the indications in risk of invasive breast cancer the optimum duration of treatment is not known.

Active or past history of venous thromboembolism, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Pregnancy.

Boxed warning (increased risk of venous thromboembolism and death from stroke): Increased risk of deep vein thrombosis and pulmonary embolism have been reported with EVISTA. Women with active or past history of venous thromboembolism should not take EVISTA. Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events. Venous Thromboembolism: Increased risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Discontinue use 72 hours prior to and during prolonged immobilization. Death Due to Stroke: Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events. No increased risk of stroke was seen in this trial.

Adverse reactions (>2% and more common than with placebo) include: hot flashes, leg cramps, peripheral edema, flu syndrome, arthralgia, sweating.

Cholestyramine: Use with EVISTA is not recommended. Reduces the absorption and enterohepatic cycling of raloxifene. Warfarin: Monitor prothrombin time when starting or stopping EVISTA. Highly Protein-Bound Drugs: Use with EVISTA with caution. Highly protein-bound drugs include diazepam, diazoxide, and lidocaine. EVISTA is more than 95% bound to plasma proteins.

Store at controlled room temperature, 20° to 25°C (68° to 77°F). The USP defines controlled room temperature as a temperature maintained thermostatically that encompasses the usual and customary working environment of 20° to 25°C (68° to 77°F), that results in a mean kinetic temperature calculated to be not more than 25°C, and that allows for excursions between 15° and 30°C (59° and 86°F) that are experienced in pharmacies, hospitals, and warehouses.