First-line treatment for chronic myeloid leukemia: dasatinib, nilotinib, or imatinib.
First-line treatment for chronic myeloid leukemia: dasatinib, nilotinib, or imatinib.
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DOI：
10.1186/1756-8722-3-47
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发表时间：
2010-11-26
影响因子：
28.5
通讯作者：
Liu D
中科院分区：
文献类型：
--
作者：
Wei G;Rafiyath S;Liu D
伊马替尼是一种BCR-ABL酪氨酸激酶抑制剂（TKI），作为慢性粒细胞白血病（CML）的标准一线治疗已有近10年。达沙替尼和尼洛替尼是两种较新的药物，对BCR-ABL的效力高于伊马替尼，对大多数伊马替尼耐药的BCR-ABL突变具有活性，在随机III期试验中，与伊马替尼相比，达沙替尼和尼洛替尼作为慢性期CML的一线治疗均显示出上级疗效。随访14个月，现有数据表明达沙替尼和尼洛替尼之间的疗效无明显差异。与伊马替尼相比，达沙替尼的胸腔积液和血小板减少发生率较高，但水肿、胃肠道AE、肌肉骨骼AE和皮疹发生率较低。与伊马替尼相比，尼洛替尼与皮肤毒性、头痛和与肝脏和胰腺毒性相关的生化异常的发生率较高相关，但水肿、胃肠道AE、肌肉痉挛和中性粒细胞减少的发生率较低。几项研究表明，伊马替尼依从性差会对缓解产生不良影响，在缓解欠佳的患者中应予以考虑。达沙替尼（每日一次，伴或不伴食物）和尼洛替尼（每日两次，空腹）的不同给药要求可能是选择一线药物的额外因素。本综述比较和对比了三种FDA批准的一线TKI药物。
Imatinib, a tyrosine kinase inhibitor (TKI) of BCR-ABL, was the standard first-line therapy for chronic myeloid leukemia (CML) for almost 10 years. Dasatinib and nilotinib, two newer drugs with higher potency than imatinib against BCR-ABL and activity against most imatinib-resistant BCR-ABL mutations, have each shown superior efficacy compared with imatinib for first-line treatment of chronic-phase CML in randomized phase 3 trials. With 14 months follow-up time, available data suggest no obvious differences in efficacy between dasatinib and nilotinib. Compared with imatinib, dasatinib is associated with higher rates of pleural effusion and thrombocytopenia, but lower rates of edema, gastrointestinal AEs, musculoskeletal AEs, and rash. Nilotinib is associated with higher rates of dermatologic toxicity, headache, and biochemical abnormalities associated with hepatic and pancreatic toxicity compared with imatinib, but lower rates of edema, gastrointestinal AEs, muscle spasm, and neutropenia. Several studies have shown that poor adherence to imatinib detrimentally affects responses and should be considered in patients with a suboptimal response. The different dosing requirements of dasatinib (once daily with or without food) and nilotinib (twice daily with fasting) may be an additional factor in selecting frontline agents. This review compares and contrasts the three FDA approved first line TKI agents.
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影响因子：
20.3
作者：
Gontarewicz, Artur;Balabanov, Stefan;Bruemmendorf, Tim H.
通讯作者：
Bruemmendorf, Tim H.
影响因子：
20.3
作者：
Giles, Francis J.;Cortes, Jorge;Freedman, Steven J.
通讯作者：
Freedman, Steven J.
影响因子：
158.5
作者：
Kantarjian, Hagop;Giles, Francis;Ottmann, Oliver G.
通讯作者：
Ottmann, Oliver G.
影响因子：
45.3
作者：
Cortes, Jorge E.;Jones, Dan;Kantarjian, Hagop
通讯作者：
Kantarjian, Hagop
DOI：
10.1007/978-3-642-01222-8_14
发表时间：
2010-01-01
期刊：
SMALL MOLECULES IN ONCOLOGY
影响因子：
--
作者：
Gontarewicz, Artur;Bruemmendorf, Tim H.
通讯作者：
Bruemmendorf, Tim H.