蛋白酶体抑制剂卡非佐米的药理作用与临床评价

摘要

Carfilzomib is a second-generation proteasome inhibitor administered intravenously with welldocumented anticancer activities.Carfilzomib is approved by FDA on July 20,2012.It is indicated for the treatment of patients with multiple myeloma who have received at least two prior therapies including bortezomib and an immunomodulatory agent,and have demonstrated disease progression on or within 60 days of completion of the last therapy.The most common adverse reactions include fatigue,anemia,nausea,thrombocytopenia,dyspnea and fever.A literature search was conducted using Medline with the key words carfilzomib.Its pharmacology,pharmacodynamics,pharmacokinetics,the treatment of clinical,dosage,drug interactions and safety were reviewed in this paper.%卡非佐米是经静脉给药的第二代蛋白酶体抑制剂,具有良好的抗肿瘤活性,用于治疗预先接受过至少2种药物治疗(包括第一代蛋白酶体抑制剂硼替佐米和一种免疫调节剂),并有证据显示在完成末次治疗后60 d内疾病恶化的难治性多发性骨髓瘤,于2012年7月20日由美国食品和药物管理局(FDA)批准上市.其最为常见的不良反应为疲乏、贫血、恶心、血小板减少、呼吸困难、腹泻以及发热等.本文通过Medline对卡非佐米进行文献检索,并对其药理作用、药效学、药动学、临床评价、用法用量、药物相互作用和安全性进行了综述.