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CD33抗原大量表达于急性髓细胞白血病(AML)细胞表面,可成为靶向免疫治疗的目标。美罗他格是人源化抗CD33单克隆抗体与强效抗肿瘤抗生素——乙酰棘孢霉素偶联物,与髓性白血病细胞表面CD33抗原结合,进入细胞后释放棘孢霉素,对髓细胞白血病细胞有明显杀灭作用,用于治疗复发、难治的CD33+AML,获得良好疗效,与其它化疗药物联合应用治疗AML的临床试验正在进行中。美罗他格的耐受性一般较好,但肝脏毒性及肝静脉阻塞综合征等毒副反应值得关注。美罗他格的耐药机制可能来自多方面,其中包括P-糖蛋白介导的药物排出等。
CD33 antigen is abundantly expressed on the surface of acute myeloid leukemia (AML) cells and can be the target of targeted immunotherapy. Meropetal is a humanized anti-CD33 monoclonal antibody conjugated with the potent antitumor antibiotic acetylchithosporin, which binds to the CD33 antigen on the surface of myeloid leukemia cells. Myeloid leukemia cells have a significant killing effect, for the treatment of relapsed and refractory CD33 + AML, to obtain good effect, combined with other chemotherapy drugs in the treatment of AML clinical trials are underway. Meropetal is generally well tolerated, but toxic side effects such as liver toxicity and hepatic veno-occlusive syndrome are of concern. Meropetal’s resistance mechanism may come from many aspects, including P-glycoprotein mediated drug discharge and so on.