0
慢性骨髓性白血病用药博舒替尼/伯舒替尼(BOSULIF)效果如何?

博舒替尼.jpg

     据印度正品代购了解,参与国际研究的研究人员报告说,一种新的酪氨酸激酶抑制剂博舒替尼似乎优于格列卫(伊马替尼)用于慢性骨髓性白血病(CML)患者的初始治疗。大多数CML病例的特征是染色体异常 - 费城染色体 - 其中遗传物质在染色体9和染色体22之间交换。这种交换汇集了两个基因:BCR和ABL。将这两种基因组合到单个BCR-ABL基因中导致产生有助于不受控制的细胞生长的蛋白质。认识到BCR-ABL蛋白在CML中的关键作用导致格列卫的发展,格列卫阻断了该蛋白的活性。 格列卫在慢性期CML患者中产生缓解率,并显著改变了该病的治疗。

Bosutinib, a new tyrosine kinase inhibitor, appears to be superior to gleevec (imatinib) for initial treatment in patients with chronic myeloid leukemia (CML), researchers involved in an international study report. Most cases of CML are characterized by chromosomal abnormalities - the Philadelphia chromosome - in which genetic material is exchanged between chromosomes 9 and 22. This exchange brings together two genes: BCR and ABL. Combining the two genes into a single BCR-ABL gene results in the production of proteins that facilitate uncontrolled cell growth. Recognition of the key role of the BCR-ABL protein in CML led to the development of Gleevec, which blocked the activity of the protein. Gleevec produced remission rates in patients with chronic CML and significantly changed the treatment of the disease.

 

  靶向BCR-ABL蛋白的较新药物包括尼罗替尼和达沙替尼。 尼罗替尼和达沙替尼似乎优于格列卫,用于CML患者的初始治疗,并被FDA批准用于此目的。博舒替尼是一种靶向Abl和Src激酶的第三代酪氨酸激酶抑制剂。据说博舒替尼的效果是格列卫的30倍,对格列卫和尼罗替尼或格列卫和达沙替尼失败的患者有效。博苏替尼也有效治疗CML的加速和爆发阶段,包括干细胞移植失败的患者。

Newer drugs targeting THE BCR-ABL protein include nilatinib and dasatinib. Nilatinib and dasatinib appear to be superior to Gleevec for the initial treatment of patients with CML and are approved by the FDA for this purpose. Bosutinib is a third generation tyrosine kinase inhibitor targeting Abl and Src kinases. Bosutinib is said to be 30 times more effective than Gleevec, and is effective in patients who have failed gleevec and niletinib or Gleevec and dasatinib. Bosutinib is also effective in the accelerated and explosive stages of CML, including in patients who have failed stem cell transplantation.

 

  博舒替尼靶向Src是重要的,因为Src激酶的过度表达已经与格列卫的抗性相关。一项临床研究随机分配502例新诊断的CML患者,用格列卫或博舒替尼进行治疗。博舒替尼一年中累积的完全细胞遗传学缓解率为79%,格列卫为75%。一年中累积的主要分子响应率为博舒替尼组47%,格列卫组32%。在博舒替尼组中,完成细胞遗传学缓解或主要分子反应的时间更快。

Bosutinib targeting Src is important because overexpression of Src kinase has been associated with gleevec resistance. A clinical study randomized 502 patients with newly diagnosed CML to gleevec or bosutinib. The cumulative full cytogenetic response rate for bosutinib over a year was 79% versus 75% for Gleevec. The cumulative response rates of major molecules during one year were 47% in the Bosutinib group and 32% in the Gleevec group. In the Bosutinib group, the time to complete the cytogenetic response, or major molecular response, was faster.


咨询客服
Top