This drug blocks the transformation of cholesterol into pregnenolone, and androgens into estrogens in the adrenal glands, thus completely suppressing the production of all steroid hormones. Aminoglutethimide is used for palliative treatment of prostate carcinomas and post-menopausal breast carcinomas. Synonyms of aminoglutethimide are orimeten, cita-dren and others.
Flutamide: Synthesis of flutamide (29.2.15) is described in Chapter 29.
o2n o2n o ch3
This drug blocks binding of androgens to tissue-muscle cells and prevents biological action of androgens, including in pancreatic tumor cells.
It is used in combination with leuprolide for prostate carcinomas. Synonyms of flu-tamide are chimax, drogenil and others.
Mitotane: Mitotane, 1,1-dichloro-2-(o-chlorophenyl)ethane (30.5.8), is made by alkylating chlorobenzene with 1-(2-chlorophenyl)-2,2-dichloroethane (30.5.7) in the presence of sulfuric acid. The necessary 1-(2-chlorophenyl)-2,2-dichloroethanol (30.5.7) is in turn made from reacting 2-chlorophenylmagnesiumbromide with dichloroacetic aldehyde .
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Mitotane, a derivative of the insecticide DDT, quickly lowers the level of corticosteroids, and is metabolized in the blood and urine and used on non-operable metastatic prostate carcinomas. Synonyms of this drug are lysodren and others.
Tamoxifen: Synthesis of tamoxifen (28.2.8) is described in Chapter 28.
This drug blocks estrogen receptors, stops the progression of cancerous diseases, and stimulates estrogens.
Leuprolide: Leuprolide, 5-oxo-L-prolyl-L-histadyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leu-cil-L-leucil-L-arginyl-N-ethyl-L-prolinamide (30.5.9), is made synthetically [136-139].
The nonapeptide leuprolide is a synthetic analog of the decapeptide, gonadotropin releasing hormone, and it exceeds the activity of the natural hormone and significantly elevates the level of testosterone and dihydrotestosterone in men, and estrogen in women. It also inhibits follicle-stimulating hormone and leutenizing hormone.
Leuprolide is used for prostate cancer, when orchiectomy or estrogen therapy is counterproductive to the patient. A synonym of this drug is lupron.
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