Abirapro 250mg is used in the treatment of prostate cancer, which has spread to other parts of the body. Abirapro is used for patients in which the cancer is resistant to medical or surgical treatment. It can be used before chemotherapy or cancer, which has progressed or after chemotherapy containing docetaxel. Abiraterone is an in hibitor of androgen biosynthesis. In particular, abiraterone selectively inhibits the activity of the enzyme 17α-hydroxylase / C17,20-lyase (CYP17). This enzyme is necessary for the biosynthesis of androgens in the testes, adrenals, and cells of the tumor of the prostate.
Abiraterone is an inhibitor of androgen biosynthesis. In particular, abiraterone selectively inhibits the activity of the enzyme 17α-hydroxylase / C17,20-lyase (CYP17). This enzyme is necessary for the biosynthesis of androgens in the testes, adrenals, and cells of the tumor of the prostate. CYP17 catalyzes the conversion of pregnenolone and progesterone by 17α-hydroxylation and breaking of the C17,20 bond into testosterone precursors: dehydroepiandrosterone and androstenedione, respectively. The inhibition of CYP17 activity is also accompanied by increased synthesis of mineralocorticoids in the adrenal glands. Antiandrogenic therapy, such as the use of luliberin agonists or orchidectomy, weakens the synthesis of androgens in the testicles but does not affect the synthesis of androgens in the adrenal gland and tumor. The use of abiraterone together with lylyberyrin agonists (or orchidectomy) lowers serum testosterone concentrations to below the detection threshold. The concentration of prostate-specific antigen (PSA) serves as a biomarker in patients with prostate cancer.
For oral use, the prodrug of abiraterone acetate is converted to an active metabolite, abiraterone, which has anti-androgenic activity. Joint reception with food increases the absorption of the drug and, therefore, can increase and greatly alter the effect of the drug, so abiraterone should be taken on an empty stomach. The drug binds well to proteins (> 99%) and is metabolized in the liver with the participation of CYP3A4 and SULT2A1 in inactive metabolites. Abiraterone is excreted with feces (~ 88%) and urine (~ 5%). The final half-life is 12 ± 5 hours.
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