• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

卡匹西利:首个获批用于治疗乳腺癌患者的AKT抑制剂。

Capivasertib: First Approved AKT inhibitor for the Treatment of Patients with Breast Cancer.

作者信息

De Surya K

机构信息

Department of Chemistry, Conju-Probe, San Diego, California, USA.

出版信息

Anticancer Agents Med Chem. 2025;25(6):371-377. doi: 10.2174/0118715206360571241126080725.

DOI:10.2174/0118715206360571241126080725
PMID:39633517
Abstract

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.

摘要

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。

相似文献

1
Capivasertib: First Approved AKT inhibitor for the Treatment of Patients with Breast Cancer.卡匹西利:首个获批用于治疗乳腺癌患者的AKT抑制剂。
Anticancer Agents Med Chem. 2025;25(6):371-377. doi: 10.2174/0118715206360571241126080725.
2
Capivasertib: A Novel AKT Inhibitor Approved for Hormone-Receptor-Positive, HER-2-Negative Metastatic Breast Cancer.卡培他滨:一种新型 AKT 抑制剂,获批用于激素受体阳性、HER2 阴性转移性乳腺癌。
Ann Pharmacother. 2024 Dec;58(12):1229-1237. doi: 10.1177/10600280241241531. Epub 2024 Apr 2.
3
mTORC1-Driven Protein Translation Correlates with Clinical Benefit of Capivasertib within a Genetically Preselected Cohort of PIK3CA-Altered Tumors.mTORC1 驱动的蛋白翻译与卡培他滨在 PIK3CA 改变肿瘤的遗传预选队列中的临床获益相关。
Cancer Res Commun. 2024 Aug 1;4(8):2058-2074. doi: 10.1158/2767-9764.CRC-24-0113.
4
"The emerging role of capivasertib in breast cancer".卡培他滨在乳腺癌中的新作用。
Breast. 2022 Jun;63:157-167. doi: 10.1016/j.breast.2022.03.018. Epub 2022 Apr 1.
5
Proliferation and AKT Activity Biomarker Analyses after Capivasertib (AZD5363) Treatment of Patients with ER Invasive Breast Cancer (STAKT).卡培他滨(AZD5363)治疗 ER 浸润性乳腺癌(STAKT)患者后的增殖和 AKT 活性生物标志物分析。
Clin Cancer Res. 2020 Apr 1;26(7):1574-1585. doi: 10.1158/1078-0432.CCR-19-3053. Epub 2019 Dec 13.
6
Capivasertib and fulvestrant for patients with HR-positive/HER2-negative advanced breast cancer: analysis of the subgroup of patients from Japan in the phase 3 CAPItello-291 trial.卡匹西利与氟维司群用于激素受体阳性/人表皮生长因子受体2阴性晚期乳腺癌患者:3期CAPItello-291试验中日本患者亚组分析
Breast Cancer. 2025 Jan;32(1):132-143. doi: 10.1007/s12282-024-01640-z. Epub 2024 Oct 8.
7
Fulvestrant plus capivasertib versus placebo after relapse or progression on an aromatase inhibitor in metastatic, oestrogen receptor-positive, HER2-negative breast cancer (FAKTION): overall survival, updated progression-free survival, and expanded biomarker analysis from a randomised, phase 2 trial.氟维司群联合卡培他滨对比安慰剂治疗激素受体阳性、HER2 阴性转移性乳腺癌患者在芳香化酶抑制剂治疗复发或进展后的疗效(FAKTION):一项随机、2 期临床试验的总生存、更新的无进展生存和扩展的生物标志物分析。
Lancet Oncol. 2022 Jul;23(7):851-864. doi: 10.1016/S1470-2045(22)00284-4. Epub 2022 Jun 4.
8
US Food and Drug Administration Approval Summary: Capivasertib With Fulvestrant for Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Locally Advanced or Metastatic Breast Cancer With // Alterations.美国食品和药物管理局批准概要:卡培他滨联合氟维司群用于激素受体阳性、人表皮生长因子受体 2 阴性局部晚期或转移性乳腺癌伴//改变。
J Clin Oncol. 2024 Dec;42(34):4103-4113. doi: 10.1200/JCO.24.00427. Epub 2024 Aug 19.
9
BEECH: a dose-finding run-in followed by a randomised phase II study assessing the efficacy of AKT inhibitor capivasertib (AZD5363) combined with paclitaxel in patients with estrogen receptor-positive advanced or metastatic breast cancer, and in a PIK3CA mutant sub-population.比彻:一项剂量探索的导入期研究,随后是一项随机的 II 期研究,评估 AKT 抑制剂卡培他滨(AZD5363)联合紫杉醇在雌激素受体阳性的晚期或转移性乳腺癌患者中的疗效,以及在 PIK3CA 突变亚群中的疗效。
Ann Oncol. 2019 May 1;30(5):774-780. doi: 10.1093/annonc/mdz086.
10
Practical treatment strategies and novel therapies in the phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) pathway in hormone receptor-positive/human epidermal growth factor receptor 2 (HER2)-negative (HR+/HER2-) advanced breast cancer.激素受体阳性/人表皮生长因子受体2阴性(HR+/HER2-)晚期乳腺癌中磷酸肌醇3激酶(PI3K)/蛋白激酶B(AKT)/雷帕霉素哺乳动物靶点(mTOR)通路的实用治疗策略和新型疗法
ESMO Open. 2024 Dec;9(12):103997. doi: 10.1016/j.esmoop.2024.103997. Epub 2024 Dec 13.

引用本文的文献

1
Coexistence of low-grade pulmonary mucinous epithelioid carcinoma and metastatic adrenal sarcomatoid carcinoma: a rare case report with BRAF p.V600E-driven molecular insights and clinical challenges.低级别肺黏液性上皮样癌与转移性肾上腺肉瘤样癌并存:一例罕见病例报告及BRAF p.V600E驱动的分子见解与临床挑战
Front Oncol. 2025 Aug 15;15:1564472. doi: 10.3389/fonc.2025.1564472. eCollection 2025.

本文引用的文献

1
Population Pharmacokinetics of Capivasertib in Patients with Advanced or Metastatic Solid Tumours.卡培他滨在晚期或转移性实体瘤患者中的群体药代动力学。
Clin Pharmacokinet. 2024 Aug;63(8):1191-1204. doi: 10.1007/s40262-024-01407-x. Epub 2024 Aug 10.
2
Resistance to Targeted Inhibitors of the PI3K/AKT/mTOR Pathway in Advanced Oestrogen-Receptor-Positive Breast Cancer.晚期雌激素受体阳性乳腺癌对PI3K/AKT/mTOR通路靶向抑制剂的耐药性
Cancers (Basel). 2024 Jun 18;16(12):2259. doi: 10.3390/cancers16122259.
3
Combination Therapy Approach to Overcome the Resistance to PI3K Pathway Inhibitors in Gynecological Cancers.
联合治疗方法克服妇科癌症中对 PI3K 通路抑制剂的耐药性。
Cells. 2024 Jun 19;13(12):1064. doi: 10.3390/cells13121064.
4
Capivasertib in combination with enzalutamide for metastatic castration resistant prostate cancer after docetaxel and abiraterone: Results from the randomized phase II RE-AKT trial.卡比沙替联合恩扎卢胺治疗多西他赛和阿比特龙治疗后的转移性去势抵抗性前列腺癌:随机 II 期 RE-AKT 试验结果。
Eur J Cancer. 2024 Jul;205:114103. doi: 10.1016/j.ejca.2024.114103. Epub 2024 May 8.
5
PI3K/AKT/mTOR signaling pathway: an important driver and therapeutic target in triple-negative breast cancer.PI3K/AKT/mTOR 信号通路:三阴性乳腺癌的重要驱动因子和治疗靶点。
Breast Cancer. 2024 Jul;31(4):539-551. doi: 10.1007/s12282-024-01567-5. Epub 2024 Apr 17.
6
Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries.2022 年全球癌症统计数据:全球 185 个国家和地区 36 种癌症的发病率和死亡率全球估计数。
CA Cancer J Clin. 2024 May-Jun;74(3):229-263. doi: 10.3322/caac.21834. Epub 2024 Apr 4.
7
Capivasertib: A Novel AKT Inhibitor Approved for Hormone-Receptor-Positive, HER-2-Negative Metastatic Breast Cancer.卡培他滨:一种新型 AKT 抑制剂,获批用于激素受体阳性、HER2 阴性转移性乳腺癌。
Ann Pharmacother. 2024 Dec;58(12):1229-1237. doi: 10.1177/10600280241241531. Epub 2024 Apr 2.
8
Optimal targeting of PI3K-AKT and mTOR in advanced oestrogen receptor-positive breast cancer.晚期雌激素受体阳性乳腺癌中 PI3K-AKT 和 mTOR 的最佳靶向治疗。
Lancet Oncol. 2024 Apr;25(4):e139-e151. doi: 10.1016/S1470-2045(23)00676-9.
9
Leniolisib: a novel treatment for activated phosphoinositide-3 kinase delta syndrome.来尼利西布:一种治疗活化磷脂酰肌醇-3激酶δ综合征的新型疗法。
Front Pharmacol. 2024 Feb 12;15:1337436. doi: 10.3389/fphar.2024.1337436. eCollection 2024.
10
Capivasertib combines with docetaxel to enhance anti-tumour activity through inhibition of AKT-mediated survival mechanisms in prostate cancer.卡培他滨与多西他赛联合应用通过抑制 AKT 介导的前列腺癌细胞存活机制增强抗肿瘤活性。
Br J Cancer. 2024 May;130(8):1377-1387. doi: 10.1038/s41416-024-02614-w. Epub 2024 Feb 23.