抗乳腺癌新药——Akt激酶抑制剂capivasertib  

A new drug for treatment of breast cancer-Akt kinase inhibitor capivasertib

作　　者：张亚安 朱咏娟 曹楠 潘雅典 ZHANG Ya-an;ZHU Yong-juan;CAO Nan;PAN Ya-dian(Department of Pharmaceutical and Chemical Engineering,Southeast University Chengxian College,Nanjing JIANGSU 210088,China)

机构地区：[1]东南大学成贤学院制药与化学工程学院,江苏南京210088

出　　处：《中国新药与临床杂志》2024年第12期899-904,共6页Chinese Journal of New Drugs and Clinical Remedies

基　　金：江苏省高等学校大学生实践创新训练计划项目(HCX23013);江苏省青蓝工程优秀青年骨干教师培养资助(2023);江苏高校哲学社会科学研究一般项目(2023SJYB0659);东南大学成贤学院国家级科研项目培育基金(2022NCF001)。

摘　　要：capivasertib为口服蛋白激酶B,即Akt激酶抑制剂,靶向作用于磷脂酰肌醇3-激酶(PI3K)/Akt信号通路,抑制肿瘤细胞的增殖及转移而发挥治疗作用。2023年11月16日,美国食品和药物管理局批准capivasertib与氟维司群联合治疗具有一种或多种PIK3CA/AKT1/PTEN基因变异的激素受体阳性(HR+)、人表皮生长因子受体2阴性(HER2-)局部晚期或转移性乳腺癌患者。capivasertib为首款上市的口服Akt激酶抑制剂,Ⅲ期临床试验结果表明,对于耐药的HR+/HER2-晚期乳腺癌患者,capivasertib联合氟维司群比单独使用氟维司群可显著改善无进展生存期,且总体安全性良好,常见不良反应为腹泻、皮疹、高血糖、淋巴细胞减少等。Capivasertib,an orally available protein kinase B(Akt kinase)inhibitor,has targeted action on phosphatidylinositol 3-kinase(PI3K)/Akt signaling pathway,inhibiting tumor cell proliferation and metastasis.Capivasertib has been approved by U.S.Food and Drug Administration on November 16,2023 for the treatment of locally advanced or metastatic breast cancer patients with one or more PIK3CA/AKT1/PTEN-alterations who are hormone receptor-positive(HR+)or human epidermal growth factor receptor 2-negative(HER2-)in combination with fulvestrant.Capivasertib is the first marketed oral Akt kinase inhibitor.PhaseⅢclinical trial results showed that capivasertib combined with fulvestrant could significantly improve the progression free survival compared with fulvestrant alone in patients with drug-resistant HR+/HER2-advanced breast cancer,and the overall safety was good.The common adverse reactions were diarrhea,rash,hyperglycemia,lymphopenia and so on.

关 键 词：capivasertib 蛋白激酶B 乳腺肿瘤 激素受体 表皮生长因子受体 

分 类 号：R737.3[医药卫生—肿瘤]