阿西米尼治疗慢性髓性白血病。

IF 1.8 4区 医学 Q2 Medicine Drugs of today Pub Date : 2022-10-01 DOI:10.1358/dot.2022.58.10.3441853
Giovanni Manfredi Assanto, Emilia Scalzulli, Massimo Breccia
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引用次数: 3

摘要

尽管在过去几年中,慢性髓性白血病(CML)患者的预期寿命已达到正常人群的预期寿命,但仍有相当比例的CML患者使用第一代或第二代酪氨酸激酶抑制剂(TKIs)治疗失败。一线治疗失败通常是由于分子耐药性或难以忍受的毒性。新的特异性化合物在这种情况下进行测试,以满足CML未满足的临床需求;其中,阿西米尼显示出基于变体抑制的疗效,这可以克服耐药性和脱靶毒性。本文旨在介绍阿西米尼将如何改变慢性粒细胞白血病的治疗方案,重点介绍其作用机制、药代动力学、疗效和毒性。对于携带耐药突变(如T315I)和/或不符合其他TKIs治疗条件的患者,阿西米尼将可能作为三线治疗的选择。
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Asciminib in chronic myeloid leukemia.

Despite the fact that, in the last years, life expectancy of chronic myeloid leukemia (CML) patients has reached that of the normal population, a significant proportion of CML patients is likely to fail treatment with first- or second-generation tyrosine kinase inhibitors (TKIs). Failure to first-line treatment is commonly due to molecular resistance or unbearable toxicity. New specific compounds are tested in this setting to fulfill this unmet clinical need in CML; of these, asciminib has shown efficacy based on allosteric inhibition which allows to overcome resistance and off-target toxicity. This review aims to cover how asciminib will change the therapeutic scenario of CML, highlighting its mechanism of action, pharmacokinetics, efficacy and toxicity. Asciminib will be a possible option as third-line therapy for patients carrying resistant mutations, such as T315I, and/or not eligible for treatment with other TKIs.

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来源期刊
Drugs of today
Drugs of today 医学-药学
CiteScore
3.90
自引率
0.00%
发文量
48
审稿时长
6-12 weeks
期刊介绍: An international, peer-reviewed journal publishing monographs on new products entering the market and review articles. Since its inception in 1965, Drugs of Today has established a reputation for excellence in providing physicians and other key healthcare professionals with practical, up-to-date monographs on recently approved and launched drugs.
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