Steroidal anti androgen drugs

Neural injections of Bromodeoxyuridine (BrdU) were applied to males of both groups to test for neurogenesis . Analysis showed that testosterone and dihydrotestosterone regulated adult hippocampal neurogenesis (AHN). Adult hippocampal neurogenesis was regulated through the androgen receptor in the wild-type male rats, but not in the TMF male rats. To further test the role of activated androgen receptors on AHN, flutamide , an antiandrogen drug that competes with testosterone and dihydrotestosterone for androgen receptors , and dihydrotestosterone were administered to normal male rats. Dihydrotestosterone increased the number of BrdU cells, while flutamide inhibited these cells.

Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[ 18 F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp 741 to Cys). [1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. [2]

Hyperandrogenism is a condition in women in which androgen levels are excessively and abnormally high. [23] It is commonly seen in women with PCOS, and also occurs in women with intersex conditions like congenital adrenal hyperplasia . [23] Hyperandrogenism is associated with virilization – that is, the development of masculine secondary sexual characteristics like male-pattern facial and body hair growth (or hirsutism), voice deepening , increased muscle mass and strength , and broadening of the shoulders, among others. [23] Androgen-dependent skin and hair conditions like acne and androgenic alopecia may also occur in hyperandrogenism, and menstrual disturbances , like amenorrhea , are commonly seen. [23] Although antiandrogens do not treat the underlying cause of hyperandrogenism (., PCOS), they are able to prevent and reverse its manifestation and effects. [23] As with androgen-dependent skin and hair conditions, the most commonly used antiandrogens in the treatment of hyperandrogenism in women are cyproterone acetate and spironolactone. [23] Other antiandrogens, like bicalutamide, may be used alternatively. [23]

Steroidal anti androgen drugs

steroidal anti androgen drugs

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