Rituximab is a human/murine, chimeric anti-CD20 monoclonal antibody with established efficacy, and a favorable and well-defined safety profile in patients with various CD20-expressing lymphoid malignancies, including indolent and aggressive forms of B-cell non-Hodgkin lymphoma [1].
Intravenously administered rituximab was granted regulatory approval in 1997 by the US Food and Drug Administration and in 1998 by the European Medicines Agency for use in relapsed/refractory indolent non-Hodgkin lymphomas. Approvals for use in chronic lymphocytic leukemia followed in 2009 and 2010, respectively [1].
Rituximab binds with high affinity and specificity to the CD20 antigen, which is expressed on the vast majority of malignant B cells. The apparent affinity constant of rituximab for human CD20, as determined by Scatchard analysis using a human lymphoblastoid cell line, is approximately 5.2 nmol/L [2]. Rituximab provides significant, clinically meaningful benefits to patients with active rheumatoid arthritis also. In patients with active rheumatoid arthritis despite methotrexate treatment, a single course of two infusions of rituximab, alone or in combination with either cyclophosphamide or continued methotrexate, provided significant improvement in disease symptoms at both weeks 24 and 48 [3].
References:
[1]. Salles G, Barrett M, FoÀ R, et al. Rituximab in B-cell hematologic malignancies: a review of 20 years of clinical experience. Adv Ther. 2017;34(10):2232-2273.
[2]. Reff ME, Carner K, Chambers KS, et al. Depletion of B cells in vivo by a chimeric mouse human monoclonal antibody to CD20. Blood. 1994;83:435-45.
[3]. Edwards JC, Szczepanski L, Szechinski J, et al. Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis. N Engl J Med 2004;350:2572-2581
利妥昔单抗(Rituximab)是一种人/鼠嵌合型抗CD20单克隆抗体,已在表达各种CD20的淋巴样恶性肿瘤患者中展现出良好的疗效和安全性[1],包括慢性和侵袭性B细胞非何杰金淋巴瘤。静脉注射的利妥昔单抗于1997年获得美国食品和药物管理局的批准,并于1998年获得欧洲药品管理局的批准,用于复发/难治性慢性非何杰金淋巴瘤的治疗。随后,它们分别在2009年和2010年获得慢性淋巴细胞白血病的使用批准[1]。
利妥昔单抗与CD20抗原具有高亲和力和特异性结合,CD20抗原广泛表达于恶性B细胞的绝大多数。利妥昔单抗对人类CD20的表观亲和常数,通过使用人类淋巴母细胞系的Scatchard分析确定,约为5.2 nmol/L [2]。对于活动性类风湿性关节炎的患者,利妥昔单抗也提供了显著的、临床上有意义的益处。在接受甲氨蝶呤治疗但仍患有活动性类风湿性关节炎的患者中,两次利妥昔单抗输注的单独或与环磷酰胺或继续甲氨蝶呤联合使用,分别在24周和48周时提供了显著的疾病症状改善[3]。