Hatzimichael Eleftheria, Tsolas Evangelos, Briasoulis Evangelos
Department of Haematology, University Hospital of Ioannina, Ioannina, Greece.
J Blood Med. 2014 Aug 19;5:143-52. doi: 10.2147/JBM.S51253. eCollection 2014.
Pacritinib (previously known as SB-1518) is an innovative selective inhibitor of Janus kinase 2 and FMS-related tyrosine kinase 3 providing potential in the treatment of hematological malignancies such as myeloproliferative neoplasias, acute myeloid leukemia, and various lymphomas. Pacritinib has potent antiproliferative activity in Janus kinase 2 and/or FMS-related tyrosine kinase 3 activity-dependent cell lines and an ability to promote apoptosis and inhibit the signal transducers and activators of transcription (STAT) pathway. Pharmacokinetic studies have indicated a good per os bioavailability and favorable kinetic parameters. To date, promising results have been produced in five completed early-phase clinical trials in which pacritinib has been studied. Pacritinib displayed interesting activity and an acceptable safety profile, with mild to moderate gastrointestinal disorders being its most common adverse effects.
帕西替尼（曾用名SB - 1518）是一种创新的Janus激酶2和FMS相关酪氨酸激酶3选择性抑制剂，在治疗血液系统恶性肿瘤如骨髓增殖性肿瘤、急性髓系白血病及各种淋巴瘤方面具有潜力。帕西替尼在Janus激酶2和/或FMS相关酪氨酸激酶3活性依赖的细胞系中具有强大的抗增殖活性，并有促进细胞凋亡和抑制信号转导及转录激活因子（STAT）通路的能力。药代动力学研究表明其口服生物利用度良好且动力学参数有利。迄今为止，在五项已完成的对帕西替尼进行研究的早期临床试验中取得了有前景的结果。帕西替尼显示出有趣的活性和可接受的安全性，轻度至中度胃肠道疾病是其最常见的不良反应。
