Echavarria Isabel, López-Tarruella Sara, Márquez-Rodas Iván, Jerez Yolanda, Martin Miguel
a Medical Oncology Department , Instituto de Investigación Sanitaria Gregorio Marañón (IiSGM) , Madrid , Spain.
b Medical Oncology Department , Instituto de Investigación Sanitaria Gregorio Marañón (IiSGM), CiberOnc , Madrid , Spain.
Expert Rev Anticancer Ther. 2017 Aug;17(8):669-679. doi: 10.1080/14737140.2017.1338954. Epub 2017 Jun 26.
Despite the advances in the treatment of HER2-positive breast cancer, resistance to actual chemotherapeutic regimens eventually occurs. Neratinib, an orally available pan-inhibitor of the ERBB family, represents an interesting new option for early-stage HER2-positive breast cancer. Areas covered: In this article, the development of neratinib, with a special focus on its potential value in the treatment of early-stage HER2-positive breast cancer, has been reviewed. For this purpose, a literature search was conducted, including preclinical studies, early-phase trials in advanced cancer with neratinib in monotherapy and in combination, and phase II and large phase III trials in the early setting. Management of neratinib-induced toxicity, future perspectives for the drug, and ongoing trials are also discussed in this review. Expert commentary: Neratinib is emerging as a promising oral drug for the treatment of HER2-positive breast cancer. Although FDA and EMA approval is derived from the extended adjuvant treatment, this setting may not be the ideal scenario to obtain the beneficial effects of neratinib. Confirmatory data in the neoadjuvant setting and subgroup analysis from the ExTENET trial might bring some light into the best setting for neratinib therapy. Data from confirmatory trials in the metastatic setting are also required.
尽管HER2阳性乳腺癌的治疗取得了进展，但最终仍会出现对现有化疗方案的耐药性。来那替尼是一种口服的ERBB家族泛抑制剂，是早期HER2阳性乳腺癌一个引人关注的新选择。涵盖领域：本文回顾了来那替尼的研发情况，特别关注其在早期HER2阳性乳腺癌治疗中的潜在价值。为此进行了文献检索，包括临床前研究、来那替尼单药及联合治疗晚期癌症的早期试验，以及早期阶段的II期和大型III期试验。本综述还讨论了来那替尼所致毒性的管理、该药物的未来前景以及正在进行的试验。专家评论：来那替尼正成为一种有前景的用于治疗HER2阳性乳腺癌的口服药物。尽管美国食品药品监督管理局（FDA）和欧洲药品管理局（EMA）的批准源于延长辅助治疗，但这种情况可能并非获得来那替尼有益效果的理想情形。新辅助治疗中的验证性数据以及ExTENET试验的亚组分析可能会为来那替尼治疗的最佳情形带来一些启示。转移性治疗中的验证性试验数据也是必要的。
