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Peak plasma levels of raloxifene occur 0.5 to 6 hours after an oral dose. [3] [4] In healthy postmenopausal women treated with 60 mg/day raloxifene, peak circulating raloxifene levels normalized by dose and body weight were (i.e., divided by (mg/kg)), 0.50 ng/mL (500 pg/mL) after a single dose and 1.36 ng/mL (1,360 pg/mL after multiple doses).
One of the largest breast cancer prevention studies ever, [2] it included 22,000 women in 400 medical centers in the United States and Canada. [3] [4] [5]The study concluded that raloxifene caused fewer side-effects and less endometrial cancer than tamoxifen.
Raloxifene has a benzothiophene group (red) and is connected with a flexible carbonyl hinge to a phenyl 4-piperidinoethoxy side chain (green). Raloxifene belongs to the second-generation benzothiophene SERM drugs. It has a high affinity for the ER with potent antiestrogenic activity and tissue-specific effects distinct from estradiol. [19]
Average number of moderate-to-severe hot flashes per week with placebo and different doses of oral estradiol in menopausal women [40] [41]. Estradiol is used in menopausal hormone therapy to prevent and treat moderate to severe menopausal symptoms such as hot flashes, vaginal dryness and atrophy, and osteoporosis (bone loss). [11]
The antiestrogen withdrawal response is a paradoxical improvement in breast cancer caused by discontinuation of antiestrogen therapy for breast cancer. [1] [2] [3] [4 ...
Fulvestrant, sold under the brand name Faslodex among others, is an antiestrogenic medication used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with abemaciclib or palbociclib in women with disease progression after endocrine therapy. [2]
Estradiol/raloxifene (E2/RLX) is a tissue-selective estrogen complex (TSEC) which was studied for potential use in menopausal hormone therapy but was never marketed. [ 2 ] [ 1 ] [ 3 ] [ 4 ] [ 5 ] Today, E2/RLX is not generally used due to concerns of endometrial hyperplasia .
Short term drug side effects are most likely to occur at or near the C max, whereas the therapeutic effect of drug with sustained duration of action usually occurs at concentrations slightly above the C min. [citation needed] The C max is often measured in an effort to show bioequivalence (BE) between a generic and innovator drug product. [4]