De Surya K
Department of Chemistry, Conju-Probe, San Diego, California, USA.
Anticancer Agents Med Chem. 2025;25(6):371-377. doi: 10.2174/0118715206360571241126080725.
Breast cancer frequently occurs in women. Among the several types of breast cancers, almost 50% of breast cancers are caused by one or more gene mutations of the PI3K/mTOR/AKT pathway. Capivasertib, the first AKT inhibitor, was authorized by the US FDA on November 16, 2023. It is used for the treatment of adult patients with hormone receptor-positive, human epidermal growth factor receptor 2 negative metastatic breast cancer with at least one alteration on . In this short perspective, Capivasertib's physicochemical properties, synthesis, mechanism of action, binding mode, pharmacokinetics, drug interaction studies, and treatment-emergent adverse events are discussed.
乳腺癌在女性中频繁发生。在几种类型的乳腺癌中,近50%的乳腺癌是由PI3K/mTOR/AKT通路的一种或多种基因突变引起的。首个AKT抑制剂卡匹西利(Capivasertib)于2023年11月16日获得美国食品药品监督管理局(FDA)批准。它用于治疗激素受体阳性、人表皮生长因子受体2阴性的转移性乳腺癌成年患者,且这些患者的[此处原文缺失部分信息]至少有一处改变。在这篇简短的综述中,讨论了卡匹西利的物理化学性质、合成、作用机制、结合模式、药代动力学、药物相互作用研究以及治疗中出现的不良事件。