Raloxifene Hydrochloride

What it is and how it works

Mechanism of Action 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.

Indications

Raloxifene hydrochloride tablets are 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: Raloxifene hydrochloride tablets are 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. Treatment and Prevention of Osteoporosis in Postmenopausal Women Raloxifene hydrochloride tablets are indicated for the treatment and prevention of osteoporosis in postmenopausal women [ see Clinical Studies ( 14.1 , 14.2 ) ]. Reduction in the Risk of Invasive Breast Cancer in Postmenopausal Women with Osteoporosis Raloxifene hydrochloride tablets are indicated for the reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis [ see Clinical Studies ].

Dosage and administration (summary)

60 mg tablet orally once daily. Recommended Dosing The recommended dosage is one 60 mg raloxifene hydrochloride tablet daily, which may be administered any time of day without regard to meals [ see Clinical Pharmacology ]. For the indications in risk of invasive breast cancer the optimum duration of treatment is not known [ see Clinical Studies ( 14.3 , 14.4 ) ]. Recommendations for Calcium and Vitamin D Supplementation For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Postmenopausal women require an average of 1500 mg/day of elemental calcium.

Contraindications

Active or past history of venous thromboembolism, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Pregnancy. ( 4.2 , 8.1 ) Venous Thromboembolism Raloxifene hydrochloride tablets are contraindicated in women with active or past history of venous thromboembolism (VTE), including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis [ see Warnings and Precautions ].

Warnings and precautions

Venous Thromboembolism : Increased risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Discontinue use 72 hours prior to and during prolonged immobilization. ( 5.1 , 6.1 ) 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. Consider risk-benefit balance in women at risk for stroke.

Pregnancy

Pregnancy Risk Summary Raloxifene hydrochloride is contraindicated for use in pregnant women, and is not indicated for use in females of reproductive potential. Based on mechanism of action, raloxifene hydrochloride may block the important functions that estrogen has during all stages of pregnancy [ see Clinical Pharmacology ].

Storage and supply

NDC: 71335-1715-1: 60 Tablets in a BOTTLE NDC: 71335-1715-2: 30 Tablets in a BOTTLE

Source: Raloxifene Hydrochloride (Raloxifene Hydrochloride) — US FDA prescribing information, 2023-10-23, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.