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Oestrogens receptor antagonists

Addo S, Yates RA, Laight A (2002) A phase I trial to assess the pharmacology of the new oestrogen receptor antagonist fulvestrant on the endometrium in healthy postmenopausal volunteers. Br J Cancer 87 1354-1359... [Pg.164]

Tamoxifen is on oestrogen-receptor antagonist. It is used in post-menopousol women with oestrogen-receptor-positive metastatic breast cancer at a dose of 20 mg doily. It con also be used in combination with chemotherapy. Severe side-effects ore infrequent however, it is associated with a small risk of endometrial cancer. Patients should be informed and reassured that the benefits of the treatment at this dose outweigh the risk. [Pg.38]

Tamoxifen is an oestrogen-receptor antagonist indicated as adjuvant hormonal treatment in oestrogen-receptor-positive breast cancer in postmenopausal women. Common side-effects include alopecia and uterine fibroids. [Pg.81]

Q79 Tamoxifen is an oestrogen-receptor antagonist that is only effective as adjuvant endocrine therapy of early breast cancer in postmenopausal v/omen. Tamoxifen is given by mouth and treatment should not exceed 1 year. [Pg.322]

Tamoxifen is an oestrogen-receptor antagonist effective in premenopausal, perimenopausal and postmenopausal women with early breast cancer. Aromatase inhibitors, such as anastrazole, may be used only in postmenopausal women. Tamoxifen is administered as tablets. Treatment with tamoxifen is usually given for at least 5 years. [Pg.339]

Fulvestrant is a competitive oestrogen receptor antagonist which binds to the receptor in a competitive manner with an affinity similar to that of estradiol. Fulvestrant downregulates the oestrogen receptor in human breast cancer cells. It is marketed for treatments of hormone-dependent breast cancer (Fig. 59) [145]. [Pg.600]

Oestrogen-receptor antagonists Fulvestrant, Tamoxifen, Toremifene... [Pg.609]

Pike ACW, Brzozowski AM, Hubbard RE et al. Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist. EM BO J. 18, 4608-4618, 1999. [Pg.392]

As previously mentioned, despite the benefits of tamoxifen in the treatment of breast cancer, it is known to increase the risk of endometrial cancer and the formation of blood clots in women. Raloxifen, Chart 3, is a benzothiophene selective oestrogen receptor modulator, which, like tamoxifen, acts as an oestrogen antagonist in the breast. Formally known as LY 156,758 or keoxifen, it was first developed in the early 1980s as a candidate for the treatment of breast cancer [76], However, it performed poorly against tamoxifen in laboratory models, and no further development followed until its ability to maintain bone density in postmenopausal women was recognised. It was approved under the new name of raloxifen for the treatment and prevention of osteoporosis (Evista ) [77, 78],... [Pg.90]

Selective antagonists of the oestrogen receptor are used either to induce gonadotrophin release in anovulatory infertility, or to block stimulation of oestrogen-receptor-positive carcinomas of the breast... [Pg.719]

Hormone receptor antagonist The hepatocytes possess oestrogen receptors and react to oestrogen with proliferation. Therefore, it seemed advisable to apply anti-oestrogens as part of the therapy. However, the efficacy of these substances, e.g. tamoxifen at 10(-20) mg twice daily, could not be confirmed. Toremifen appeared to be more successful. Cyproterone acetate proved inefficacious as an anti-androgenic agent. Flutamide likewise showed no effect. [Pg.786]

Mestinon pyridostigmine bromide, mestranol [ban, inn, usan] (CB 8027 EE3ME L 33355 RS 1044) is a synthetic steroid oestrogen, a constituent in many combined oral CONTRACEPTIVES, and also used in oral HRT. mesulergino [inn] is an ergoline amine derivative, a (S-HTsc) 5-HYDROXYTRYPtAMINE RECEPTOR ANTAGONIST and DOPAMINE RECEPTOR ANTAGONIST, mesulfen mesulphen. [Pg.177]

ANTIOESTROCENS include tamoxifen which binds to oestrogen receptors with little stimulation, so acts as an antagonist us to treat oestrogen-dependent breast cancer. [Pg.207]

Selective oestrogen receptor modulators (oestrogen antagonists and aromatase inhibitors)... [Pg.39]


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See also in sourсe #XX -- [ Pg.38 , Pg.59 , Pg.81 ]




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Oestrogen antagonists

Oestrogen receptor

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