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奈拉替尼治疗早期激素受体阳性、HER2 过表达乳腺癌。

Neratinib for the treatment of early-stage, hormone receptor-positive, HER2-overexpressed breast cancer.

机构信息

Medical Oncology Service, Hospital General Universitario Gregorio Marañón, Instituto de Investigación Sanitaria Gregorio Marañón (IiSGM), Departamento de Medicina, Universidad Complutense, CiberOnc, Madrid, Spain.

Medical Oncology Service, Hospital General Universitario Gregorio Marañón, Madrid, 28007, Spain.

出版信息

Future Oncol. 2020 Jun;16(17):1165-1177. doi: 10.2217/fon-2020-0046. Epub 2020 May 27.

Abstract

HER2-positive breast cancer accounts for 18-20% of all breast cancers. Despite significant advances and the currently available adjuvant treatments for management of the disease, approximately 25% of HER2-positive early-stage breast cancer patients show relapse and die. Neratinib is an irreversible tyrosine kinase inhibitor. Multiple studies have reported its significant antitumor activity in metastatic HER2-positive breast cancer. It is administered orally and has also been tested in the adjuvant setting. In this article, we present a comprehensive review of the pharmacokinetics and pharmacodynamics of neratinib as well as its clinical efficacy, with an emphasis on early HER2-positive breast cancer and suggestions for future directions for neratinib research.

摘要

人表皮生长因子受体 2 阳性乳腺癌占所有乳腺癌的 18%-20%。尽管在疾病的治疗方面取得了显著进展和目前可提供的辅助治疗方法,但仍有约 25%的人表皮生长因子受体 2 阳性早期乳腺癌患者出现复发和死亡。奈拉替尼是一种不可逆的酪氨酸激酶抑制剂。多项研究报道了其在转移性人表皮生长因子受体 2 阳性乳腺癌中的显著抗肿瘤活性。它通过口服给药,也已在辅助治疗环境中进行了测试。在本文中,我们全面回顾了奈拉替尼的药代动力学和药效学及其临床疗效,重点介绍了早期人表皮生长因子受体 2 阳性乳腺癌,并对奈拉替尼的研究方向提出了建议。

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