Alias: Raloxifene HCL;
Appearance:light yellow powder
Usage :It is used in the prevention of osteoporosis in postmenopausal women.
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.
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.
Raloxifene appears to act as an estrogen agonist in bone.It decreases bone resorption and bone turnover, increases bone mineral density and decreases fracture incidence.