Abiraterone acetate, whose active metabolite inhibits an enzyme necessary for the biosynthesis of testosterone, was approved April 28 by FDA for use in combination with prednisone to treat patients with metastatic advanced prostate cancer who have received docetaxel.The drug will be marketed as Zytiga,...
Agents that block the action (antiandrogens) of endogenous hormones (e.g., testosterone) are highly effective and routinely used for the treatment of prostate cancer (androgen ablation therapy). While initially effective at suppressing tumor growth, these androgen ablation therapies eventually fail in ...
This is comparable with known anti-androgens such as flutamide and cyproterone. The same compound gives an ED50 of 17 mg/kg (the dose required to inhibit testosterone propionate stimulated prostate weight gain by 50%). Chemistry: 2′-Methylsulphonyl-5α-pregn-2-en-20-yno[3,2-d]thiazol-...
(ADT). Treatments (for instance, through luteinizing hormone-releasing hormone agonists or surgical castration) that significantly reduce the level of testosterones and other anti-androgens in the circulation, generally the first type of hormone therapy used to treat advanced prostate cancer. Tumour mic...
Metastatic castrate-resistant prostate cancer (CRPC) is a disease state characterized by a testosterone level of less than 50 ng/dL, with 2 consecutive increases in prostate-specific antigen (PSA) with a PSA level of 2 ng/dL or more. ...
Testosterone can drive the growth of prostate cancer and anti-androgens are used to inhibit prostate cancer growth by preventing testosterone from binding to androgen receptors. But receptors in cells within the testes are also blocked and start to make more testosterone to compensate. Some of this...
Many patients with rising prostate-specific antigen (PSA) levels eventually progress to castration-resistant PC (CRPC), often associated with persistent androgen receptor (AR) signaling, despite maintaining castrate concentrations of serum testosterone, defined as <50 ng/dL [13, 14]. This review ...
Prior to the treatment initiation, the dosage of the total testosterone was not very often performed (4.8%). Associated comorbidities such as arterial hypertension (53.6%) and hypercholesterolemia (31.8%) did not constitute a barrier to the initiation of ADT, alone (60.5%) or combined with anti...
This research, encompassing an individual patient level analysis from two multinational randomizedclinical trials, showcases relugolix's ability to rapidly achieve and maintainlow testosterone levels, a necessary condition for some men's prostate cancer treatment, in both short-term (24 weeks) and longe...
The mechanisms of action of antiandrogens are different [177]: Inhibition of testosterone secretion; Inhibition of androgen action. 4.1.1. Inhibition of Testosterone Secretion The first mechanism is achieved indirectly, via the hypothalamus–pituitary–gonadal axis or by direct inhibition of testosterone...