Hematology and Oncology Institute, Hospital Israelita Albert Einstein, São Paulo, SP, Brazil.
Expert Opin Pharmacother. 2012 Nov;13(16):2381-95. doi: 10.1517/14656566.2012.725722. Epub 2012 Sep 20.
Dasatinib is a dual Abl/Src tyrosine kinase inhibitor (TKI), which was developed to treat patients with chronic myelogenous leukemia (CML), who had failed or were intolerant to therapy with imatinib.
In this article, we review preclinical and clinical studies with dasatinib for the therapy of Philadelphia (Ph)-positive leukemias.
Dasatinib is very effective in the setting of CML resistance or intolerance to imatinib, particularly in patients in chronic phase (CP). Dasatinib is also effective against most BCR-ABL1 mutations that arise during therapy with imatinib. Further studies have confirmed activity of dasatinib as a single-agent, and combined with chemotherapy, for the treatment of patients with Philadelphia-positive acute lymphoblastic leukemia (Ph+-ALL). More recently, randomized trials have demonstrated that dasatinib is superior to imatinib in the initial therapy of patients with CML, and the drug was approved by the FDA for this indication in 2011.
达沙替尼是一种双重 Abl/Src 酪氨酸激酶抑制剂(TKI),旨在治疗对伊马替尼治疗失败或不耐受的慢性髓性白血病(CML)患者。
本文综述了达沙替尼治疗费城染色体阳性(Ph+)白血病的临床前和临床研究。
达沙替尼在治疗对伊马替尼耐药或不耐受的 CML 方面非常有效,特别是在慢性期(CP)的患者中。达沙替尼对伊马替尼治疗期间出现的大多数 BCR-ABL1 突变也有效。进一步的研究证实了达沙替尼作为单一药物,以及与化疗联合,用于治疗费城阳性急性淋巴细胞白血病(Ph+-ALL)患者的疗效。最近,随机试验表明,达沙替尼在 CML 患者的初始治疗中优于伊马替尼,该药物于 2011 年获得 FDA 批准用于该适应证。