Hormone dependent tumors

Noncontraceptive Uses of Progestins. Progestins have other therapeutic uses aside from contraception. Hormone-dependent tumors and cysts involving reproductive tissues respond to progestins. Megestrol acetate and MPA are the two most commonly used progestins to treat breast cancer... 

A stmcturally related series of phenyfiiydrazones resulted ia the selection of compound A-007 [2675-35-6] (DEKK-TEC)(37) for the treatment of hormone-dependent tumors. A-007 is an antiestrogen that, ia contrast to tamoxifen, demonstrated inhibitory activity both ia the presence and absence of estradiol ia ZR-75-1 estrogen-dependent human breast cancer cells, and afforded more protection than tamoxifen ia the 7,12-dimethylbenz[i7]anthracene... 

Toko T, Sugimoto Y, Matsuo K, Yamasaki R, Takeda S, Wierzba K, et al. (1990) TAT-59, a newtriphenylethylene derivative with antitumor activity against hormone-dependent tumors. Eur J Cancer 26 397-404... 

Hormones. Although not strictly cytotoxic, hormones have been used to control the environment of hormone-dependent tumors such as those of the prostate, breast, and endometrium, i.e., androgens are used to control the growth of estrogen-dependent breast tumors, whereas estrogens control androgen-dependent tumors of the prostate. Hormones that have anticancer activities are listed in Table 6. 

The relationship between hormones and hormone-dependent tumors was initially demonstrated in 1896 when Beatson showed that oophorectomy produced improvement in women with advanced breast cancer. Sex hormones and adrenocortical hormones are employed in the management of... 

Tumors that are steroid hormone-sensitive may be either (1) hormone-responsive, where the tumor regresses following treatment with a specific hormone (2) hormone-dependent, where removal of a hormonal stimulus causes tumor regression or (3) both. Hormone treatment of responsive tumors is usually only palliative, except in the case of the cytotoxic effect of glucocorticoids (for example, prednisone) on lymphomas. Removal of hormonal stimuli from hormone-dependent tumors can be accomplished by surgery, for example, in the case of orchiectomy for patients with advanced prostate cancer, or by drugs, for example in the case of breast cancer, treatment with the antiestrogen... 

This luteinizing hormone-releasing hormone has been used in the treatment of endometriosis and hormone-dependent tumors. Modes of administration have included injections, nasal sprays and subcutaneous implantations. One study, conducted in pigs, demonstrated the value of glycodeoxycholate (a penetration enhancer) in improving the bioavailability of buserelin by up to five-fold after buccal delivery. ... 

Unfortunately, a third of hormone-dependent tumors do not respond to tamoxifen and another third acquire resistance. In order to overcome these deficiencies, several platinum complexes derived from estradiol, estrone, or the synthetic estrogen hexestrol were prepared as estradiol receptors. These compounds proved to be similar in activity to... 

After 5 years of tamoxifen therapy, a significant number of patients experience a relapse, primarily because of tamoxifen resistance. What is observed clinically is that the weak estrogenic effects of tamoxifen begin to predominate and effectively feed the hormone-dependent tumor. 

The aim of this assay is to evaluate the expression of steroid receptors (receptor status) in hormone-dependent tumors, since these receptors (estrogen, progesterone and androgen receptors) are essential for the proliferation and differentiation of tumors derived from hormone-dependent tissues such as breast, ovarian and uterine tissue. 

However it is known that a third of hormone-dependent tumors will not respond to tamoxifen and that another third will become resistant after a longer or shorter period of time. There is thus a real need to find new SERMs, or compounds that reach other targets, in order to provide an appropriate therapeutic response for a greater percentage of patients. 

WITH SPECIFIC ACTIVITY AGAINST HORMONE DEPENDENT TUMORS, in... 

Steroids - Large doses of estrogen inhibit prolactin stimulation of mammary tumor growth as demonstrated by the effect of estradiol benzoate to DMBA-lnduced mammary adenocarcinomas in female rats. Estrogen may be involved in transport of RNA from nucleus to cytoplasm. Specific binding of estradiol within the nucleus is confined to hormone-dependent tumors... 

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