Antineoplastic, hormonal and hormone antagonists

As antineoplastic agents in clinical practice, a number of hormonal drugs are used – agonists and antagonists of androgens, estrogens, gestagens and other hormones. These funds are indicated mainly for hormone-dependent tumors. Hormonal antitumor therapy is essential in the treatment of breast, endometrial, and prostate cancer. Hormonal agents are also used to treat kidney cancer, carcinoid, some pancreatic tumors, melanoma, etc.
The interaction between hormones and hormone-dependent tumors was first identified in 1896, when Glasgow surgeon J. Beatson published data on the successful treatment of three women with advanced breast cancer who underwent bilateral oophorectomy.
According to the mechanism of action, hormonal drugs differ from cytotoxic anticancer drugs. Their main role is to restore the disturbed humoral regulation of cell function. At the same time, a specific effect on tumor cells is not excluded: to a certain extent, they inhibit cell division and promote their differentiation.
GnRH analogs are available in various dosage forms – for s / c, i / m, intranasal use. Inside, these drugs are not assigned, tk. decapeptides are easily broken down and inactivated in the gastrointestinal tract. Considering the need for long-term treatment, GnRH analogues are also available in the form of prolonged-release medicinal forms, incl. microcapsules, microspheres.
The high rate of destruction of GnRH (2–8 min) does not allow its use in clinical practice for long-term use. For GnRH, the T1 / 2 value from the blood is 4 minutes, with s / c or intranasal administration of its analogs – about 3 hours. Biotransformation is carried out in the hypothalamus and pituitary gland. In renal or hepatic impairment, dosage adjustment is usually not required.
Aromatase inhibitors began to be used in oncological practice in the 70s and 80s. XX century Aromatase is a cytochrome P450-dependent enzyme responsible for the conversion of androgens synthesized in the adrenal cortex into estrogens. Aromatase is present in a variety of tissues and organs, including the ovaries, adipose tissue, skeletal muscle, liver, and breast tumor tissue. In premenopausal women, the ovaries are the main source of circulating estrogens, while in postmenopausal women estrogens are formed mainly outside the ovaries. Inhibition of aromatase leads to a decrease in the formation of estrogen in both premenopausal and postmenopausal women. However, in premenopausal women, a decrease in estrogen biosynthesis is compensated by an increase in the synthesis of gonadotropins according to the feedback principle – a decrease in estrogen synthesis in the ovaries stimulates the production of gonadotropins by the pituitary gland, which, in turn, increase the synthesis of androstenedione, and the level of estrogen rises again. As a result, aromatase inhibitors are ineffective in premenopausal women. In postmenopausal women, when the ovaries cease to function, the hypothalamus-pituitary-adrenal axis is ruptured, and inhibition of aromatase leads to a significant suppression of estrogen biosynthesis in peripheral tissues, as well as in breast tumor tissue.
The first and in fact the only representative of the 1st generation aromatase inhibitors is aminoglutethimide, a non-selective aromatase inhibitor. Since aminoglutethimide inhibits a number of enzymes involved in steroidogenesis (inhibits the secretion of glucocorticoids (cortisol) by the adrenal glands and is therefore used in Itsenko-Cushing’s disease, etc.), when using it, it is necessary to monitor the functional state of the adrenal cortex (its hypofunction may develop).
The search for new agents with greater selectivity, better tolerance and a more convenient dosing regimen led to the emergence of second and third generation aromatase inhibitors. To date, new non-steroidal (letrozole, anastrozole, etc.) and steroidal (exemestane) compounds of this group have been created.
The main indication for aromatase inhibitors is breast cancer in postmenopausal women, incl. with resistance to antiestrogen therapy.
The group of adrenal hormone biosynthesis inhibitors used in oncology includes mitotane and aminoglutethimide. They suppress the secretion of glucocorticoids and can cause destruction of normal and tumor tissue of the adrenal cortex.
Glucocorticoids – prednisolone, dexamethasone, due to their lymphocytic action and the ability to inhibit the mitosis of lymphocytes, are used in acute leukemia (mainly in children) and malignant lymphomas.
Some analogs of somatostatin are also used as antineoplastic agents. For example, octreotide and lanreotide are used for symptomatic therapy of endocrine tumors of the gastroenteropancreatic system.
Below is a list of hormonal anticancer agents and hormone antagonists:
AXASTROL® / Anastrozole (Anastrozolum)
Aminoglutethimide / Aminoglutethimide (Aminoglutethimidum)
Anabresis / Anastrozole (Anastrozolum)
Anamasten® / Anastrozole (Anastrozolum)
Anandron / Nilutamide (Nilutamidum)
Anastera / Anastrozole (Anastrozolum)
Anastrozole / Anastrozole (Anastrozolum)
Anastrozole Kabi / Anastrozole (Anastrozolum)
Anastrozole San / Anastrozole (Anastrozolum)
Anastrozole-Teva / Anastrozole (Anastrozolum)
Anastrozole-TL / Anastrozole (Anastrozolum)
Anastrex® / Anastrozole (Anastrozolum)
Andriol / Testosterone (Testosteronum)
Androblock® / Bicalutamide (Bicalutamidum)
Androkur® / Cyproterone (Cyproteronum)
Androkur® Depot / Cyproterone (Cyproteronum)
Arimidex® / Anastrozole (Anastrozolum)
Aromasin® / Exemestanum
Aromeston / Exemestanum
Balutar® / Bicalutamide (Bicalutamidum)
Bicalutamide / Bicalutamide (Bicalutamidum)
Bicalutamide Grindeks / Bicalutamide (Bicalutamidum)
Bicalutamide Kabi / Bicalutamide (Bicalutamidum)
Bicalutamide Canon / Bicalutamide (Bicalutamidum)
Bicalutamide Sandoz® / Bicalutamide (Bicalutamidum)
Bicalutamide-Teva / Bicalutamide (Bicalutamidum)
Bicalutera / Bicalutamide (Bicalutamidum)
Bikana® / Bicalutamide (Bicalutamidum)
Bikaprost® / Bicalutamide (Bicalutamidum)
Biehm / Tamoxifen (Tamoxifenum)
Bilumid / Bicalutamide (Bicalutamidum)
Buserelin / Buserelinum
Buserelin FSintez / Buserelin (Buserelinum)
Buserelin-depot / Buserelinum
Buserelin-long FS / Buserelinum
Buserelin Acetate / Buserelinum
Veraplex / Medroxyprogesterone (Medroxyprogesteronum)
Vero-Anastrozole / Anastrozole (Anastrozolum)
Vero-Tamoxifen / Tamoxifen (Tamoxifenum)
Vero-Flutamide / Flutamide (Flutamidum)
Genfastat® / Octreotidum
Hydroxyprogesterone Caproate / Hydroxyprogesterone caproate (Hydroxyprogesteroni caproas)
Hormoplex / Estrogens conjugatate
Decapeptyl / Triptorelin (Triptorelinum)
Decapeptyl depot / Triptorelin (Triptorelinum)
Depo-Provera® / Medroxyprogesterone (Medroxyprogesteronum)
Depostat® / Gestonoroni caproas
Dermestril® / Estradiol (Oestradiolum)
Divigel / Estradiol (Oestradiolum)
Dipherelin® / Triptorelin (Triptorelinum)
Zitazonium® / Tamoxifen (Tamoxifenum)
Zytiga® / Abirateron (Abirateronum)
Zoladex® / Goserelin (Goserelinum)
K.E.S. / Estrogens conjugatate
Calumid® / Bicalutamide (Bicalutamidum)
Casodex® / Bicalutamide (Bicalutamidum)
Klimara® / Estradiol (Oestradiolum)
Lestrodex / Letrozolum
Letroza / Letrozolum
Letrozole / Letrozolum
Letrozole-Acri® / Letrozolum
Letrozole-Teva / Letrozolum
Letrosan / Letrozolum
Letrotera / Letrozolum
Lukrin depot® / Leuprorelinum
Mamomite / Aminoglutethimide (Aminoglutethimidum)
Megeis® / Megestrol (Megestrolum)
Medroxyprogesterone-LENS / Medroxyprogesterone (Medroxyprogesteronum)
Methyltestosterone tablets 0.005 g / Methyltestosterone (Methyltestosteronum)
Nexazole / Letrozolum
Novofen / Tamoxifen (Tamoxifenum)
Nolvadex / Tamoxifen (Tamoxifenum)
Oxyprogesterone Capronate / Hydroxyprogesterone caproate (Hydroxyprogesteroni caproas)
Oxyprogesterone capronate solution for injection in oil / Hydroxyprogesterone caproate (Hydroxyprogesteroni caproas)
Oxyprogesterone capronate solution in oil 12.5% ​​in ampoules / Hydroxyprogesterone caproate (Hydroxyprogesteroni caproas)
Octreotide / Octreotidum
Octreotide San / Octreotidum
Octreotide Actavis / Octreotidum
Octreotide depot / Octreotidum
Octreotide-Long FS / Octreotidum
Octreotide® Psynthesis / Octreotidum
Octreotide Acetate / Octreotidum
Octretex® / Octreotidum
Octrid / Octreotidum
Omnadren® 250 / Testosterone (mix of esters) (Testosteronum (mixtio Aetherum))
Organometrile / Linestrenol (Lynoestrenolum)
Oreta / Letrozolum
Orimeten® / Aminoglutethimide (Aminoglutethimidum)
Prajisan / Progesterone (Progesteronum)
Premarin / Estrogens conjugatate
Provera® / Medroxyprogesterone (Medroxyprogesteronum)
Progesterone / Progesterone (Progesteronum)
Progestogel / Progesterone (Progesteronum)
Prostap / Leuprorelinum
Sandostatin / Octreotidum
Sandostatin Lar / Octreotidum
Selana® / Anastrozole (Anastrozolum)
SERAKSTAL / Octreotidum
Sinestrol / Hexestrol (Hexoestrolum)
Sinestrol tablets 0.001 g / Hexestrol (Hexoestrolum)
Suprefact / Buserelin (Buserelinum)
Suprefact depot / Buserelin (Buserelinum)
Sustanon-250 / Testosterone (mix of esters) (Testosteronum (mixtio Aetherum))
Tamoxen / Tamoxifen (Tamoxifenum)
Tamoxifen / Tamoxifen (Tamoxifenum)
Tamoxifen (Tamoplex) / Tamoxifen (Tamoxifenum)
Tamoxifen HEXAL / Tamoxifen (Tamoxifenum)
Tamoxifen Lahema / Tamoxifen (Tamoxifenum)
Tamoxifen-Ebeve / Tamoxifen (Tamoxifenum)
Tamoxifen Citrate / Tamoxifen (Tamoxifenum)
Tamoxifen citrate tablets 0.01 g / Tamoxifen (Tamoxifenum)
Testosterone Propionate / Testosterone (Testosteronum)
Testenate for injection 10% / Testosterone (mix of esters) (Testosteronum (mixtio Aetherum))
Triptorelin Acetate / Triptorelin (Triptorelinum)
Fazlodex® / Fulvestrant (Fulvestrantum)
Fareston / Toremifen (Toremifenum)
Femara / Letrozolum
Firmagon / Degarelixum
Flutacan / Flutamide (Flutamidum)
Flutamide / Flutamide (Flutamidum)
Flutamide Pliva / Flutamide (Flutamidum)
Flutamide Sandoz® / Flutamide (Flutamidum)
Flutamide STADA® / Flutamide (Flutamidum)
Flutaplex / Flutamide (Flutamidum)
Flucinom® / Flutamide (Flutamidum)
Fosfestrol solution 6% in ampoules / Phospestrol (Phosphoestrolum)
Fosfestrol tablets 0.1 g / Phospestrol (Phosphoestrolum)
Cyproterone-Teva / Cyproterone (Cyproteronum)
Egistrazole / Anastrozole (Anastrozolum)
Exemestan / Exemestanum
Exemestan-Teva / Exemestanum
Extraza / Letrozolum
Eligard / Leuprorelinum
Estradurin® / Polyestradiol phosphate (Polyoestradioli phosphas)
Estracite® / Estramustin (Estramustinum)
Estrimax / Estradiol (Oestradiolum)
Estrogel / Estradiol (Oestradiolum)
Estrolet® / Letrozolum
Ethinylestradiol Tablets / Ethinylestradiol (Aethinyloestradiolum)
ETRUZIL® / Letrozolum