Department of Rheumatology and Clinical Immunology, Peking University First Hospital, Beijing, China.
Drugs Today (Barc). 2022 Jan;58(1):23-32. doi: 10.1358/dot.2022.58.1.3352743.
Systemic lupus erythematosus (SLE) is a chronic autoimmune disease, in which aberrant immune cells and proinflammatory mediators act as key players in the pathogenesis of the disease. Telitacicept (RC-18) is a novel, recombinant fusion protein, consisting of transmembrane activator and calcium modulator and cyclophilin ligand interactor (TACI) and the Fc portion of human immunoglobulin G (IgG) (TACI-Fc). It was designed to inhibit the activity of two target cytokines, the B-cell lymphocyte stimulator (BLyS, also known as the B-cell activation factor [BAFF]) and a proliferation-inducing ligand (APRIL), both of which are involved in B cell-mediated autoimmune diseases. In Chinese patients with moderate to severe SLE, subcutaneous telitacicept (80, 160 and 240 mg) in combination with standard therapy was associated with clinical benefit and appeared to be well tolerated. On March 9, 2021, the Chinese National Medical Products Administration (NMPA) granted telitacicept conditional marketing approval for the treatment of adult patients with active, autoantibody-positive SLE. Additionally, on April 15, 2020, the U.S. Food and Drug Administration (FDA) granted fast track designation to telitacicept for the treatment of SLE. Here, we provide a comprehensive review of the preclinical and clinical activity of telitacicept in SLE.
系统性红斑狼疮（SLE）是一种慢性自身免疫性疾病，其中异常的免疫细胞和促炎介质是疾病发病机制中的关键因素。Telitacicept（RC-18）是一种新型的重组融合蛋白，由跨膜激活剂和钙调节剂及亲环素配体相互作用蛋白（TACI）和人免疫球蛋白 G（IgG）的 Fc 部分（TACI-Fc）组成。它被设计用于抑制两种靶向细胞因子的活性，即 B 细胞淋巴细胞刺激物（BLyS，也称为 B 细胞激活因子[BAFF]）和增殖诱导配体（APRIL），这两种细胞因子都参与 B 细胞介导的自身免疫性疾病。在中国中重度 SLE 患者中，皮下注射 telitacicept（80、160 和 240mg）联合标准治疗与临床获益相关，且似乎具有良好的耐受性。2021 年 3 月 9 日，中国国家药品监督管理局（NMPA）批准 telitacicept 有条件上市，用于治疗活动性、自身抗体阳性的成人 SLE 患者。此外，2020 年 4 月 15 日，美国食品和药物管理局（FDA）授予 telitacicept 快速通道指定，用于治疗 SLE。在这里，我们全面回顾了 telitacicept 在 SLE 中的临床前和临床活性。
