The role of noncovalent BTK inhibitors in the era of covalent BTK inhibitors.

IF 1.1 Q4 ONCOLOGY
Fateeha Furqan, Nirav N Shah
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引用次数: 0

Abstract

Despite significantly improving outcomes in patients with B-cell malignancies, covalent Bruton tyrosine kinase (BTK) inhibitors are limited by toxicities and the development of resistance. Some toxicities can be life-threatening, such as cardiotoxicity. These toxicities result from off-target effects of covalent BTK inhibitors and frequently lead to dose reductions and discontinuations of the drug. Noncovalent BTK inhibitors bind BTK in a unique fashion and, to date, have demonstrated an excellent safety profile as well as efficacy against a variety of B-cell malignancies. In addition, noncovalent BTK inhibitors have, for the first time, demonstrated efficacy in patients who progressed on other BTK inhibitors. Long-term data and comparative studies are needed to further investigate their efficacy and role in the landscape covalent BTK Inhibitors.

非共价 BTK 抑制剂在共价 BTK 抑制剂时代的作用。
尽管共价布鲁顿酪氨酸激酶(BTK)抑制剂大大改善了 B 细胞恶性肿瘤患者的治疗效果,但其毒性和耐药性的产生却限制了这种抑制剂的使用。有些毒性可危及生命,如心脏毒性。这些毒性是由共价 BTK 抑制剂的脱靶效应引起的,经常导致剂量减少和停药。非共价 BTK 抑制剂以一种独特的方式与 BTK 结合,迄今为止已显示出极佳的安全性以及对各种 B 细胞恶性肿瘤的疗效。此外,非共价 BTK 抑制剂还首次证明了对使用其他 BTK 抑制剂后病情恶化的患者的疗效。我们需要长期的数据和比较研究来进一步研究它们的疗效和在共价 BTK 抑制剂中的作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
1.10
自引率
0.00%
发文量
99
期刊介绍: Clinical Advances in Hematology & Oncology (CAH&O) is a monthly peer-reviewed journal reaching more than 27,000 hematology and oncology clinicians. CAH&O provides editorial content encompassing a wide array of topics relevant and useful to the fields of oncology and hematology, both separately and together. Content is directed by the strong input of today’s top thought leaders in hematology & oncology, including feature-length review articles, monthly columns consisting of engaging interviews with experts on current issues in solid tumor oncology, hematologic malignancies, hematologic disorders, drug development, and clinical case studies with expert commentary. CAH&O also publishes industry-supported meeting highlights, clinical roundtable monographs, and clinical review supplements.
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