Tamoxifen and Raloxifene emerge as frontrunners, each with a legacy of efficacy and FDA approval for specific ailments
Tamoxifen has been the most important therapeutic agent for the treatment of estrogen receptor (ER)-positive breast cancer for the past three decades
In breast cancer, resistance to endocrine therapies that target estrogen receptor α (ERα), such as tamoxifen and fulvestrant, remains a
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FDA-approved Indications include treatment of breast cancer in both females and males, adjuvant treatment of breast
The human
The administration of 1 μ g tamoxifen per gm body weight at zero time or 6 hr after the operation resulted in a significant inhibition both of DNA synthesis and of the number of cells in mitosis
Basic structural feature of the new compounds is the introduction of carbonyl group either in the form of carboxylate esters or as acid and amidic derivatives
Some breast cancers grow in response to hormones like estrogen
Structural studies of tamoxifen have led to the synthesis of more than 20 novel tamoxifen analogs as receptor
We previously reported the design and synthesis of a selective estrogen receptor down-regulator (SERD), (E/Z)-4-(1-{4-[2-(dodecylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl)phenol (C12), which is a tamoxifen derivative having a long alkyl chain on the amine moiety
Although the tamoxifen receptor complex is transported in the nucleus in the same way as estrogen receptor complex, it fails to activate synthesis of mRNA
For example, tamoxifen blocks the effects of estrogen in breast tissue but acts like estrogen in the uterus and bone
Tamoxifen is a drug commonly used in the treatment of breast cancer, especially for postmenopausal patients
A 3 H-thymidine assay was used to measure DNA synthesis in wounded dermal fibroblasts (n = 3) in the presence of 100 nM tamoxifen (black bar) and 100 nM raloxifene (white bar) and vehicle control (0