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[11] [7] Peak levels of tamoxifen after a single 40 mg oral dose were 65 ng/mL and steady state levels at 20 mg/day were 310 ng/mL. [5] Levels of tamoxifen show clear dose dependency across a dosage range of 1 to 20 mg/day. [5] [93] Endoxifen levels are approximately 5 to 10 times higher than afimoxifene levels, with large interindividual ...
Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonists/antagonists (ERAAs), [1][2] are a class of drugs that act on estrogen receptors (ERs). [3] Compared to pure ER agonists – antagonists (e.g., full agonists and silent antagonists), SERMs are more tissue-specific, allowing them to selectively inhibit or ...
Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). [3] [4] [5] The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce endoxifen and afimoxifene (4-hydroxytamoxifen). [6]
The pharmacology of estradiol, an estrogen medication and naturally occurring steroid hormone, concerns its pharmacodynamics, pharmacokinetics, and various routes of administration. [1][2][3] Estradiol is a naturally occurring and bioidentical estrogen, or an agonist of the estrogen receptor, the biological target of estrogens like endogenous ...
The medication has been found to achieve 96.7% to 97.3% inhibition of aromatase at a dosage of 1 mg/day and 98.1% inhibition of aromatase at a dosage of 10 mg/day in humans. [ 3 ] [ 2 ] As such, 1 mg/day is considered to be the minimal dosage required to achieve maximal suppression of aromatase with anastrozole. [ 3 ]
The most common side effects (more than 10% of patients) are hot flashes and sweating, which are typical of estrogen deficiency as caused by exemestane, and also insomnia, headache, and joint pain. Nausea and fatigue are mainly observed in patients with advanced breast cancer.
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