Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance
Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance
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DOI：
10.1182/blood-2007-03-080689
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发表时间：
2007-11-15
期刊：
影响因子：
20.3
通讯作者：
le Coutre, Philipp
中科院分区：
文献类型：
--
作者：
Kantarjian, Hagop M.;Giles, Francis;le Coutre, Philipp
尼洛替尼是一种口服生物可利用的选择性Ber-Abl酪氨酸激酶抑制剂，在临床前模型中的效力是伊马替尼的30倍，并克服了大多数伊马替尼耐药的BCR-ABL突变。在这项II期开放标签研究中，280例伊马替尼治疗失败或不耐受后的费城染色体阳性（Ph+）慢性髓性白血病慢性期（CML-CP）患者口服尼洛替尼400 mg，每日两次。患者至少有6个月的随访，并评估血液学和细胞遗传学反应，以及安全性和总生存期。6个月时，主要细胞遗传学缓解率（Ph
Nilotinib, an orally bioavailable, selective Ber-Abl tyrosine kinase inhibitor, is 30-fold more potent than imatinib in preclinical models, and overcomes most imatinib resistant BCR-ABL mutations. In this phase 2 open-label study, 400 mg nilotinib was administered orally twice daily to 280 patients with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia in chronic phase (CML-CP) after imatinib failure or intolerance. Patients had at least 6 months of followup and were evaluated for hematologic and cytogenetic responses, as well as for safety and overall survival. At 6 months, the rate of major cytogenetic response (Ph