Krug Lee M, Milton Daniel T, Jungbluth Achim A, Chen Lin-Chi, Quaia Emilio, Pandit-Taskar Neeta, Nagel Andrew, Jones Jessica, Kris Mark G, Finn Ronald, Smith-Jones Peter, Scott Andrew M, Old Lloyd, Divgi Chaitanya
Thoracic Oncology Service, Department of Medicine, Memorial Sloan-Kettering Cancer Center and Weill Medical College at Cornell University, New York, NY 10021, USA.
J Thorac Oncol. 2007 Oct;2(10):947-52. doi: 10.1097/JTO.0b013e3181560dcc.
Lewis Y (Le(y)) is a blood group antigen with robust expression on the surface of epithelial tumors, including small cell lung cancer (SCLC), making it a potential target for antibody-based immunotherapy. 3S193, an immunoglobulin G3 monoclonal antibody, has demonstrated superior specificity, affinity, and cytotoxicity over other anti-Le(y) antibodies. A phase I trial of humanized 3S193 (hu3S193) with dosing up to 40 mg/m2 demonstrated tumor targeting without serious toxicities or the development of human anti-human antibodies.
We tested the targeting and pharmacokinetics of hu3S193 in patients with SCLC. Eligibility required progressive SCLC treated with up to three previous chemotherapy regimens, measurable disease not previously irradiated, and tumor samples positive for 3S193 by immunohistochemistry. Patients received four weekly injections of hu3S193, five patients at 10 mg/m2 and five patients at 20 mg/m2. The first and fourth injections were radiolabeled with indium-111 for gamma camera imaging.
Of 40 patients screened, 25 of 34 (74%) assessable SCLC tumor samples were 3S193 positive by immunohistochemistry. Ten patients were treated with hu3S193; nine completed all four injections. All fluorodeoxyglucose (FDG)-avid lesions >2 cm were visualized on antibody single-photon emission computed tomography. Some lesions overlying vascular structures could not be visualized. No difference was noted in imaging or pharmacokinetics between the first and fourth injections. Toxicities included grade 2 urticaria (n = 1), grade 1 vomiting (n = 2), and grade 2 hypertension (n = 1) transiently after infusion at the higher dose.
Given the strong tumor targeting, particularly at the higher dose, the favorable toxicity profile, and the potential for immunomodulatory effects, hu3S193 warrants further investigation in SCLC.
Lewis Y(Le(y))是一种血型抗原,在上皮肿瘤表面有强烈表达,包括小细胞肺癌(SCLC),这使其成为基于抗体的免疫疗法的潜在靶点。3S193是一种免疫球蛋白G3单克隆抗体,已证明其在特异性、亲和力和细胞毒性方面优于其他抗Le(y)抗体。一项人源化3S193(hu3S193)的I期试验,给药剂量高达40mg/m²,显示出肿瘤靶向性,且无严重毒性或人抗人抗体的产生。
我们测试了hu3S193在SCLC患者中的靶向性和药代动力学。入选标准要求SCLC病情进展,之前接受过最多三种化疗方案治疗,有可测量的未接受过放疗的病灶,且肿瘤样本经免疫组化检测3S193呈阳性。患者每周接受一次hu3S193注射,共四次,五名患者剂量为10mg/m²五名患者剂量为20mg/m²。第一次和第四次注射用铟-111进行放射性标记,用于γ相机成像。
在40名筛选的患者中,34名可评估的SCLC肿瘤样本中有25名(74%)经免疫组化检测3S193呈阳性。10名患者接受了hu3S193治疗;9名完成了全部四次注射。所有直径>2cm的氟脱氧葡萄糖(FDG)摄取阳性病灶在抗体单光子发射计算机断层扫描中均可见。一些覆盖血管结构的病灶无法显影。第一次和第四次注射在成像或药代动力学方面未发现差异。毒性反应包括高剂量输注后短暂出现的2级荨麻疹(n = 1)、1级呕吐(n = 2)和2级高血压(n = 1)。
鉴于其强大的肿瘤靶向性,尤其是高剂量时,良好的毒性特征以及免疫调节作用的潜力,hu3S193值得在SCLC中进一步研究。