前列腺癌中Akt抑制剂的研发与应用概述
Overview of the Development and Use of Akt Inhibitors in Prostate Cancer.
作者信息
Gasmi Anis, Roubaud Guilhem, Dariane Charles, Barret Eric, Beauval Jean-Baptiste, Brureau Laurent, Créhange Gilles, Fiard Gaëlle, Fromont Gaëlle, Gauthé Mathieu, Ruffion Alain, Renard-Penna Raphaële, Sargos Paul, Rouprêt Morgan, Ploussard Guillaume, Mathieu Romain
机构信息
Department of Urology, University of Rennes, 35000 Rennes, France.
Department of Medical Oncology, Institut Bergonié, 33000 Bordeaux, France.
出版信息
J Clin Med. 2021 Dec 29;11(1):160. doi: 10.3390/jcm11010160.
Deregulation of the PI3K-Akt-mTOR pathway plays a critical role in the development and progression of many cancers. In prostate cancer, evidence suggests that it is mainly driven by PTEN loss of function. For many years, the development of selective Akt inhibitors has been challenging. In recent phase II and III clinical trials, Ipatasertib and Capivasertib associated with androgen deprivation therapies showed promising outcomes in patients with metastatic castration-resistant prostate cancer and PTEN-loss. Ongoing trials are currently assessing several Akt inhibitors in prostate cancer with different combinations, at different stages of the disease.
PI3K-Akt-mTOR信号通路的失调在许多癌症的发生和发展中起着关键作用。在前列腺癌中，有证据表明其主要由PTEN功能丧失驱动。多年来，选择性Akt抑制剂的研发一直具有挑战性。在最近的II期和III期临床试验中，与雄激素剥夺疗法联合使用的Ipatasertib和Capivasertib在转移性去势抵抗性前列腺癌和PTEN缺失患者中显示出了有前景的结果。目前正在进行的试验正在评估几种Akt抑制剂在前列腺癌不同疾病阶段的不同联合应用情况。
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