Department of Hematology, Jagiellonian University Hospital, ul. Kopernika 17, 31-501 Kraków, Poland.
Division of Hematology & Internal Medicine, Department of Clinical & Biological Sciences of the University of Turin, 'San Luigi Gonzaga' University Hospital, 10043 Orbassano-Turin, Italy.
Future Oncol. 2019 Mar;15(9):953-965. doi: 10.2217/fon-2018-0468. Epub 2018 Dec 14.
Nilotinib, a second-generation tyrosine kinase inhibitor, was designed to overcome resistance of a wide range of BCR-ABL mutants to imatinib. When used in the first-line treatment in newly diagnosed chronic myeloid leukemia (CML), it induces faster and deeper molecular responses in higher than imatinib percentage of patients. Treatment-free remission after achievement of sustained deep molecular response represents an emerging treatment goal for a proportion of patients with CML in chronic phase. The pharmacologic properties, and the role of nilotinib in the current treatment of CML in the context of considered optimal end point of therapy including the discontinuation trial and durable treatment-free remission achievement is discussed in the article.
尼洛替尼是一种第二代酪氨酸激酶抑制剂,旨在克服广泛的 BCR-ABL 突变体对伊马替尼的耐药性。当用于新诊断的慢性髓性白血病(CML)的一线治疗时,它在高于伊马替尼的患者比例中诱导更快和更深的分子反应。在获得持续的深度分子反应后无治疗缓解代表了慢性期 CML 患者中一部分患者的新兴治疗目标。本文讨论了尼洛替尼的药理特性及其在当前 CML 治疗中的作用,包括停药试验和持久无治疗缓解的实现,这些都是考虑到治疗的最佳终点。