[Research Advance of BCR-ABL Mutation and the Efficacy of Second and Third Generation TKI in Chronic Myeloid Leukemia--Review]

Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2023 Apr;31(2):585-588. doi: 10.19746/j.cnki.issn.1009-2137.2023.02.040.
[Article in Chinese]

Abstract

The treatment of chronic myeloid leukemia (CML) was revolutionized with the advent of the first-generation tyrosine kinase inhibitors (TKIs), but drug resistance developed during treatment, leading to the development of the second-generation (dasatinib, nilotinib, and bosutinib) and third-generation (ponatinib) TKI. Compared with previous treatment regimens, specific TKI can significantly improve the response rate, overall survival rate and prognosis of CML. Only a few patients with BCR-ABL mutation are insensitive to the second-generation TKIs, so it is suggested to select the second-generation TKIs for patients with specific mutations. For patients with other mutations and without mutations, the second-generation TKI should be selected according to the patient's medical history, while the third-generation TKIs should be selected for mutations that are insensitive to the second-generation TKIs, such as T315I mutation that is sensitive to ponatinib. Due to different BCR-ABL mutations in patients with different sensitivity to the second and third-generation TKIs, this paper will review the latest research progress of the efficacy of the second and third-generation TKIs in CML patients with BCR-ABL mutations.

题目: 慢性髓性白血病BCR-ABL 突变与二、三代TKI的疗效研究进展.

摘要: 随着第一代酪氨酸激酶抑制剂(TKI)的问世,慢性髓性白血病的治疗发生了革命性变化,但在治疗过程中出现了耐药性,由此研发了第二代(达沙替尼、尼洛替尼和博苏替尼)和第三代(普纳替尼)TKI。相比之前的治疗方案,选择特定的TKI能显著提高慢性髓性白血病的缓解率、总生存率,改善预后,仅少数BCR-ABL 突变患者对二代TKI不敏感,建议针对有特定突变的患者选择二代TKI,对于其他突变和没有突变的患者,应根据患者的病史选择二代TKI,对二代TKI不敏感的突变可选择三代TKI,如T315I突变对第三代TKI普纳替尼敏感。由于不同BCR-ABL 突变的患者对二、三代TKI的敏感性不同,本文将对二、三代TKI在BCR-ABL 突变的慢性髓性白血病患者中疗效的最新研究进展作一综述。.

Keywords: BCR-ABL ; chronic myeloid leukemia; mutation; tyrosine kinase inhibitor.

Publication types

  • English Abstract
  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Dasatinib / pharmacology
  • Drug Resistance, Neoplasm / genetics
  • Fusion Proteins, bcr-abl / genetics
  • Humans
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / drug therapy
  • Mutation
  • Protein Kinase Inhibitors / therapeutic use

Substances

  • Antineoplastic Agents
  • Dasatinib
  • Fusion Proteins, bcr-abl
  • Protein Kinase Inhibitors