Safety and efficacy of TQB2102, a novel bispecific anti-HER2 antibody–drug conjugate, in patients with advanced solid tumors: Preliminary data from the first-in-human phase 1 trial.

作者：Rui‐Hua Xu, Shusen Wang, Dan‐Yun Ruan, Shaoyan Lin, Furong Liu, Hao‐Xiang Wu, Jia Huang, Qiufan Zheng, Kuikui Jiang, Xiaobo Du, Xiujuan Qu, Ning Li, Yongmei Yin, Yanqiao Zhang, Zhenyang Liu, Junjie Peng, Huihua Xiong, Aili Suo, Rongbo Lin, Shuang Zhang · 发表于：Journal of Clinical Oncology · 年份：2025 · DOI：10.1200/jco.2025.43.16_suppl.3003 · 被引用次数：7 · 研究领域：HER2/EGFR in Cancer Research、Monoclonal and Polyclonal Antibodies Research、Lung Cancer Treatments and Mutations

3003 Background: TQB2102 is an antibody-drug conjugate (ADC) comprised of a recombinant, humanized anti-human epidermal growth factor receptor 2 (HER2) bispecific antibody conjugated to a topoisomerase I inhibitor via an enzyme-cleavable linker. The bispecific antibody component can target both extra-cellular domains II (pertuzumab binding site) and IV (trastuzumab binding site) of HER2. We conducted a multicenter, dose escalation and expansion first-in human (FIH) phase 1 study of TQB2102 in advanced solid tumors. Methods: In the dose escalation phase, eligible patients (pts) with advanced solid tumors whose disease had progressed after standard systemic treatments, were enrolled in a 3+3 dose escalation study of TQB2102(1.5, 3, 4.5, 6, 7.5 or 9 mg/kg) IV, every 3wks (Q3W). In the dose expansion phase, pts with HER2 positive cancers and HER2 low (HER2 1+ or HER2 2+ and FISH negative) metastatic breast cancer (MBC) received the selected recommended phase 2 dose (RP2D). The primary objectives were to evaluate the safety and tolerability, dose limiting toxicities (DLTs) and maximum tolerated dose (MTD) of TQB2102. Results: As of October 1, 2024, 181pts (41 pts in dose escalation phase and 140 pts in dose expansion phase) were enrolled from 12 centers. Most common tumor types included MBC (N = 80), Colorectal cancer (N = 37) and Gastric cancer (N = 23).Twenty-five (31%) MBC received prior anti-HER2 ADCs, including 21 pts received T-DM1, 8 pts received DS-8201.The median duration...