治疗乳腺癌的首个PI3K抑制剂Alpelisib

Alpelisib:the First PI3K Inhibitor for the Treatment of Breast Cancer

Alpelisib是首个磷脂酰肌醇-3-激酶(PI3K)抑制剂,2019年5月美国FDA批准它与氟维司群(Fulvestrant)联用治疗绝经后女性及男性特定晚期或转移性乳腺癌患者,这些患者的激素受体(HR)阳性、人表皮生长因子受体阴性并携带PIK3CA突变。与该联合疗法相关的不良反应有高血糖、腹泻和恶心等。本文综述了Alpelisib的研究进展,包括其药效学、药动学、临床疗效、安全性和注意事项等信息,旨在向临床医生和患者提供有益的参考。

Alpelisib is the first phosphoinositide 3-kinase(PI3K)inhibitor,which received the approval from the U.S.FDA in May 2019 for the treatment of hormone receptor(HR)positive,human epidermal growth factor receptor 2(HER2)negative,PIK3CA-mutated,advanced or metastatic breast cancer in combination with fulvestrant for postmenopausal women and male patients.The adverse effects related to the combination therapy include hypeglycemia,diarrhea and nausea,and so on.The article describes the advancement of Alpelisib about its pharmacodynamics,pharmacokinetics,clinical efficacy,safety,and precautions to provide reference to clinicians and patients.