Clinton Timothy N, Woldu Solomon L, Raj Ganesh V
a Department of Urology , University of Texas Southwestern Medical Center , Dallas , TX , USA.
Expert Opin Pharmacother. 2017 Jun;18(8):825-832. doi: 10.1080/14656566.2017.1328056. Epub 2017 May 19.
Androgen deprivation therapy (ADT) is the mainstay for advanced, hormone-sensitive prostate cancer, and options include surgical castration, luteinizing hormone-releasing hormone (LHRH) agonist, and more recently, gonadotropin releasing hormone (GnRH) antagonist therapy. Our understanding of the mechanisms and adverse effects of ADT has increased substantially, including the class-specific adverse effects of ADT. Areas covered: This review will summarize the pharmacodynamic and pharmacokinetic properties of the GnRH antagonist degarelix and its role in the management of advanced prostate cancer, the clinical evidence supporting its regulatory approval, as well as potential benefits and disadvantages over traditional LHRH agonist therapy. Expert opinion: Degarelix represents a newer class of ADT that results in a rapid and reliable decline in serum testosterone, a quality that makes it particularly advantageous in men presenting with symptomatic, hormone-sensitive prostate cancer. Due to differences in mechanism of action, there is observational data suggesting a potential cardiovascular and even oncologic benefit over traditional LHRH agonist therapy. Further research is ongoing to more clearly define this potential benefit.
雄激素剥夺疗法(ADT)是晚期激素敏感性前列腺癌的主要治疗方法,其选择包括手术去势、促黄体生成素释放激素(LHRH)激动剂,以及最近出现的促性腺激素释放激素(GnRH)拮抗剂疗法。我们对ADT的作用机制和不良反应的认识有了显著提高,包括ADT的类别特异性不良反应。涵盖领域:本综述将总结GnRH拮抗剂地加瑞克的药效学和药代动力学特性及其在晚期前列腺癌治疗中的作用、支持其获批的临床证据,以及与传统LHRH激动剂疗法相比的潜在优缺点。专家观点:地加瑞克代表了一类新型的ADT,它能使血清睾酮迅速且可靠地下降,这一特性使其在患有症状性激素敏感性前列腺癌的男性中具有特别的优势。由于作用机制不同,有观察数据表明,与传统LHRH激动剂疗法相比,它可能具有心血管甚至肿瘤学方面的益处。正在进行进一步研究以更明确地界定这种潜在益处。