Urelumab (BMS-663513 or anti-4-1BB antibody) is a fully human, non‐ligand binding, CD137 agonist immunoglobulin‐γ 4 (IgG4) monoclonal antibody. [1] It was developed utilizing Medarex's UltiMAb(R) technology by Bristol-Myers Squibb for the treatment of cancer and solid tumors. [ 2 ]

2023年3月2日 · 激动型4-1BB抗体的临床开发始于2005年的urelumab，这是一种人源化的抗4-1BB IgG4抗体。虽然最初的疗效还不错，但发生了两起由肝毒性引起的致命性不良事件。随后的研究表明，当urelumab在安全剂量(0.1mg/kg)下给药时，其效果非常有限。

2024年3月7日 · Urelumab is a monoclonal antibody agonist that binds to CD137 receptors expressed on T cells. Here, we report two studies that evaluated urelumab in combination with cetuximab or nivolumab in patients with select, advanced solid tumors.

Urelumab（BMS-663513）是一种IgG4 单克隆抗体，是第一个进入临床试验的靶向4-1BB治疗药物。 Urelumab不阻断4-1BB与其配体的相互作用，最初的临床结果发表于2008年。

经过多年探索，科学家认为，一种显著降低剂量的4-1BB抗体，在正确的时间给予患者治疗，很可能会获得理想的抗肿瘤效果，同时没有毒性作用。 4-1BB的配体是4-1BBL。 人4-1BBL位于染色体19p13.3，小鼠4-1BBL位于17号染色体，是含单个跨膜区段的II型糖蛋白。 其在专职APC上表达，包括DC和巨噬细胞以及B细胞。 T细胞活化. 在捕获抗原后，APC处理抗原并在其表面上提呈抗原肽。 APC上的B7-1，B7-2和抗原肽成为幼稚T细胞的初始激活信号。 作为激活的结果，T细 …

Agonistic mAbs are the leading therapeutic modality for harnessing the antitumour effects of CD137 signalling. Two anti-CD137 mAbs are currently in the clinic: urelumab (Bristol-Myers Squibb) is a fully humanised immunoglobulin G (IgG)4 mAb and PF-05082566 (Pfizer) is a fully human IgG2 mAb. The initial phase I study of urelumab was launched in ...

The first generation of 4–1BB agonistic antibodies entering the clinic, urelumab (BMS-663513) and utomilumab (PF-05082566), ... The clinical development of 4–1BB agonists for cancer immunotherapy has raised substantial interest during the past decade.

Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab . Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL ...

Utomilumab 是辉瑞开发的一款靶向4-1BB的人源化IgG2单克隆抗体，与Urelumab作用机制不同，Utomilumab既可激活4-1BB，又可阻断与4-1BBL的结合，因此对免疫细胞的激动能力相对较温和，安全性较高。但临床试验显示，作为单药治疗，Utomilumab抗肿瘤活性十分有限。

2017年4月15日 · Purpose: Urelumab is an agonist antibody to CD137 with potential application as an immuno-oncology therapeutic. Data were analyzed to assess safety, tolerability, and pharmacodynamic activity of urelumab, including the dose selected for ongoing development in patients with advanced solid tumo</span> …