The anti-CD20 antibody rituximab (RTX; Rituxan®, MabThera®) was the first anti-cancer antibody approved by the US Food and Drug Administration in 1997 and it is now the most-studied unconjugated therapeutic antibody. The knowledge gained over the past 15 y on the pharmacodynamics (PD) of this antibody has led to the development of a new generation of anti-CD20 antibodies with enhanced efficacy in vitro. Studies on the pharmacokinetics (PK) properties and the effect of factors such as tumor load and localization, antibody concentration in the circulation and gender on both PK and clinical response has allowed the design of optimized schedules and novel routes of RTX administration. Although clinical results using newer anti-CD20 antibodies, such as ofatumumab and obinutuzumab, and novel administration schedules for RTX are still being evaluated, the knowledge gained so far on RTX PK and PD should also be relevant for other unconjugated monoclonal antibody therapeutics, and will be critically reviewed here.

抗CD20抗体利妥昔单抗（RTX；Rituxan®，MabThera®）是美国食品和药物管理局于1997年批准的第一种抗癌抗体，现在是研究最多的非偶联治疗性抗体。在过去 15 年中获得的关于该抗体药效学 (PD) 的知识已导致开发出具有增强体外功效的新一代抗 CD20 抗体。对药代动力学 (PK) 特性以及肿瘤负荷和定位、循环中的抗体浓度和性别等因素对 PK 和临床反应的影响的研究允许设计优化的时间表和新的 RTX 给药途径。尽管使用较新的抗 CD20 抗体（例如 ofatumumab 和 obinutuzumab）的临床结果以及 RTX 的新给药方案仍在评估中，