博舒替尼治疗慢性粒细胞白血病现状

Current Situation of Bosutinib in the Treatment of Chronic Myeloid Leukemia

摘要: 慢性粒细胞白血病(Chronic myeloid leukemia, CML)是一种骨髓增生性肿瘤，每100,000名成人中有1~2例，且发病率随年龄增长而增加，男性略高于女性，比例约为1.3:1。自酪氨酸激酶抑制剂(Tyrosine kinase inhibitor, TKI)用于治疗CML以来，CML已从一种致命性疾病转变为可控慢性病。目前，有5种不同的TKI被许可用于治疗CML，即一代TKI：伊马替尼；二代TKI：尼洛替尼、达沙替尼和博舒替尼；以及三代TKI：普纳替尼，用于携带T315I突变的患者。博舒替尼为口服用药，建议起始剂量为每日500 mg，每天给药一次，随食物服用，其吸收随食物增加。到目前为止，博舒替尼已被批准用于慢性期(CP)、加速期(AP)和急变期(BC)的费城阳性CML患者，这些患者之前至少接受过1次TKI治疗，并且使用伊马替尼、达沙替尼或尼洛替尼似乎不是合适的选择。

Abstract: Chronic myelogenous leukemia (CML) is a kind of myeloproliferative tumor, with 1~2 cases in every 100,000 adults, and the incidence rate increases with age. The male is slightly higher than the fe-male, with a ratio of about 1.3:1. Since Tyrosine kinase inhibitor (TKI) was used to treat CML, CML has changed from a fatal disease to a controllable chronic disease. At present, there are five differ-ent TKIs licensed for the treatment of CML, namely, the first generation TKI: imatinib; Second gen-eration TKI: nilotinib, dasatinib and bosutinib; And the third generation TKI: Ponatinib, which is used for patients with T315I mutation. Shutinib is an oral drug. It is recommended that the starting dose be 500 mg per day, once a day. When taken with food, its absorption increases with food. So far, bosutinib has been approved for use in Philadelphia-positive CML patients in chronic phase (CP), accelerated phase (AP) and acute phase (BC). These patients have been treated with TKI at least once before, and it seems that the use of imatinib, dasatinib or nilotinib is not an appropriate choice.