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博舒替尼:一种用于治疗慢性粒细胞白血病的SRC-ABL酪氨酸激酶抑制剂。

Bosutinib: a SRC-ABL tyrosine kinase inhibitor for treatment of chronic myeloid leukemia.

作者信息

Rassi Fuad El, Khoury Hanna Jean

机构信息

Division of Hematology, Department of Hematology and Medical Oncology, the Winship Cancer Institute at Emory University, Atlanta, Georgia, USA.

出版信息

Pharmgenomics Pers Med. 2013 Aug 5;6:57-62. doi: 10.2147/PGPM.S32145.

DOI:10.2147/PGPM.S32145
PMID:24019749
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3760444/
Abstract

Bosutinib is one of five tyrosine kinase inhibitors commercially available in the United States for the treatment of chronic myeloid leukemia. This review of bosutinib summarizes the mode of action, pharmacokinetics, efficacy and safety data, as well as the patient-focused perspective through quality-of-life data. Bosutinib has shown considerable and sustained efficacy in chronic myeloid leukemia, especially in the chronic phase, with resistance or intolerance to prior tyrosine kinase inhibitors. Bosutinib has distinct but manageable adverse events. In the absence of T315I and V299L mutations, there are no absolute contraindications for the use of bosutinib in this patient population.

摘要

博舒替尼是美国市面上可用于治疗慢性髓性白血病的五种酪氨酸激酶抑制剂之一。本博舒替尼综述总结了其作用方式、药代动力学、疗效和安全性数据,以及通过生活质量数据体现的以患者为中心的观点。博舒替尼在慢性髓性白血病中显示出相当显著且持续的疗效,尤其是在慢性期,对于先前的酪氨酸激酶抑制剂耐药或不耐受的患者。博舒替尼有独特但可控的不良事件。在不存在T315I和V299L突变的情况下,在该患者群体中使用博舒替尼没有绝对禁忌证。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98d8/3760444/69fd70725511/pgpm-6-057Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98d8/3760444/1944615447f5/pgpm-6-057Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98d8/3760444/69fd70725511/pgpm-6-057Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98d8/3760444/1944615447f5/pgpm-6-057Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98d8/3760444/69fd70725511/pgpm-6-057Fig2.jpg

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Bosutinib reduces the efficacy of Dasatinib in triple-negative breast cancer cell lines.博舒替尼降低三阴性乳腺癌细胞系中达沙替尼的疗效。
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