RALOXIFENE HYDROCHLORIDE

SERM

Brand names: Raloxifene Hydrochloride

Oral

Mechanism of Action

12.1 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. 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. These results are consistent with findings in clinical trials, which suggest that raloxifene hydrochloride lacks estrogen-like effects on the uterus and breast tissue.

Indications

reduction of the risk of recurrence of breast cancer

one or more first-degree relatives with breast cancer

or a 5-year predicted risk of breast cancer ≥1.66% (based on the modified Gail model). Among the factors included in the modified Gail model are the following: current age

number of first-degree relatives with breast cancer

number of breast biopsies

age at menarche

Contraindications

• 4 CONTRAINDICATIONS Active or past history of venous thromboembolism
• including deep vein thrombosis
• pulmonary embolism
• and retinal vein thrombosis. (4.1) Pregnancy (4.2
• 8.1) 4.1 Venous Thromboembolism Raloxifene hydrochloride tablets are contraindicated in women with active or past history of venous thromboembolism (VTE)

FDA Warnings

5 WARNINGS AND PRECAUTIONS Venous Thromboembolism : Increased risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis
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

Known Side Effects

12 documented side effects by frequency

Nausea

1-10%

Falls

1-10%

Drug Not Working

1-10%

Limb Pain

1-10%

Joint Pain

1-10%

Dizziness

1-10%

Fatigue

1-10%

Headache

1-10%

Diarrhea

1-10%

Back Pain

1-10%

Shortness of Breath

1-10%

Weakness

0.1-1%

Community Discussions

No community discussions found for RALOXIFENE HYDROCHLORIDE yet.

Compare With

3 available comparisons

Formulations

Dosage Forms

Tablet

Route

Oral