Degarelix:管理促性腺激素释放激素拮抗剂前列腺癌。

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Degarelix:管理促性腺激素释放激素拮抗剂前列腺癌。

其他。2009;31 Pt 2:2312-31。doi: 10.1016 / j.clinthera.2009.11.009。

PubMed ID
20110043 (在PubMed
]
文摘

背景:前列腺癌是男性最常被诊断出癌症。治疗包括手术、放疗、化疗或激素的操纵。促性腺激素释放激素(GnRH)类似物用于管理前列腺癌的减感作用的合成和释放促性腺激素的刺激,如促黄体激素(LH),刺激雄性激素的合成和释放,进而刺激前列腺癌细胞的生长。虽然有效,但这些药物有局限性,比如癌症症状的冲突开始前2周内的药物。目的:本文综述了药理学、药代动力学和药效学特征,新批准的药物和临床数据degarelix用于治疗前列腺癌。方法:搜索的医学文献进必威国际app行了2009年1月的MEDLINE和EMBASE数据库(1950年至今),国际制药抽象(1970 - 2008年11月)使用术语degarelix和FE200486;后续的搜索使用相同的必威国际app策略进行了2009年5月和2009年8月。额外的来源被确定通过扫描可用的引用和在线杂志和教科书。结果:GnRH拮抗剂,如degarelix,给临床医生提供另一个方法来减少循环雄激素水平和限制这种增长刺激针对恶性前列腺组织。Degarelix在动物实验中已被证明能够对抗垂体促性腺激素受体,导致显著减少循环LH和随后的减少睾酮的合成。 Pharmacokinetic analysis suggests that upon subcutaneous administration, degarelix forms a gel depot, from which the drug then distributes to the rest of the body in a first-order manner. A Phase II study of the effect of degarelix in 187 men with prostate cancer found a loading dose of 240 mg to be not significantly better than 200 mg in reducing serum testosterone concentrations to < or =0.5 ng/mL within 3 days of dosing (200 mg, 88%; 240 mg, 92%). This difference in percentage of patients with testosterone suppression became statistically significant when measured again 1 month into the study (200 mg, 86%; 240 mg, 95%; P = 0.048). Evaluation of 80-, 120-, and 160-mg maintenance doses found all doses effective in maintaining suppression of testosterone, LH, and prostate-specific antigen (PSA); only minor differences were observed during the study period. In a Phase III study of 610 patients with prostate cancer, a loading dose of degarelix 240 mg SC followed by monthly maintenance doses of either 80 or 160 mg was compared with monthly doses of leuprolide 7.5 mg IM. Degarelix was found to be at least as effective as leuprolide in the ability to suppress serum testosterone to < or =0.5 ng/mL for up to 1 year (degarelix response rate, 80 mg, 97.2%; 95% CI, 93.5%-98.8%; degarelix 160 mg, 98.3%; 95% CI, 94.8%-99.4%; leuprolide response rate, 96.4%; 95% CI, 92.5%-98.2%). Other studies investigating various doses and schedules of degarelix have also been conducted. Adverse effects of degarelix in clinical trials were mild and relatively uncommon and included flushing reactions, injection-site pain, weight gain, and increases in serum transaminase levels. CONCLUSIONS: Degarelix offers another option for chemical castration to reduce the androgenic growth stimulus on prostate cancer cells. The manufacturer of degarelix recommends a loading dose of 240 mg SC followed by the first monthly maintenance dose of 80 mg 28 days later. Serum testosterone and PSA concentrations must be obtained to monitor the response during treatment with degarelix.

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药物
药物靶点
药物 目标 类 生物 药理作用 行动
Degarelix 促性腺激素释放激素受体 蛋白质 人类
是的
拮抗剂
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