Raloxifene Hydrochloride — Drug Monograph

Brand names: Evista

Drug class: Hormonal Agent

Mechanism of Action

Raloxifene is a second-generation selective estrogen receptor modulator (SERM) that binds the estrogen receptor and produces tissue-selective agonist or antagonist effects. In bone it acts as an estrogen agonist, decreasing bone resorption and increasing bone mineral density, while in breast and uterine tissue it acts as an estrogen antagonist, blocking estrogen-stimulated proliferation of estrogen-receptor-positive mammary epithelium without the endometrial-stimulating (agonist) activity of tamoxifen. Its antagonism of estrogen signaling in breast tissue underlies its ability to reduce the…

FDA Indications

• 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
• Treatment of osteoporosis in postmenopausal women
• Prevention of osteoporosis in postmenopausal women

Common Side Effects

• Hot flashes / vasomotor symptoms
• Leg cramps and muscle spasm
• Peripheral edema
• Arthralgia
• Flu-like syndrome
• Sweating

Clinical Pearl

In the STAR (Study of Tamoxifen and Raloxifene / NSABP P-2) trial, raloxifene was compared with tamoxifen for breast cancer risk reduction in postmenopausal women; raloxifene was associated with fewer thromboembolic events, cataracts, and uterine cancers than tamoxifen, though longer-term follow-up showed it was somewhat less effective than tamoxifen at preventing invasive disease. Unlike tamoxifen, raloxifene does not stimulate the endometrium, so it does not raise uterine cancer risk —…

Related Therapies & Mechanisms

• Anastrozole (Arimidex) — Hormonal Agent · Breast
• Exemestane (Aromasin) — Hormonal Agent · Breast
• Fulvestrant (Faslodex) — Hormonal Agent · Breast
• Goserelin (Zoladex) — Hormonal Agent · Breast