Bispecific antibodies (bsAbs) enable novel mechanisms of action and/or therapeutic applications that cannot be achieved using conventional IgG-based antibodies. Consequently, development of these molecules has garnered substantial interest in the past decade and, as of the end of 2023, 14 bsAbs have been approved: 11 for the treatment of cancer and 3 for non-oncology indications. bsAbs are available in different formats, address different targets and mediate anticancer function via different molecular mechanisms. Here, we provide an overview of recent developments in the field of bsAbs for cancer therapy. We focus on bsAbs that are approved or in clinical development, including bsAb-mediated dual modulators of signalling pathways, tumour-targeted receptor agonists, bsAb–drug conjugates, bispecific T cell, natural killer cell and innate immune cell engagers, and bispecific checkpoint inhibitors and co-stimulators. Finally, we provide an outlook into next-generation bsAbs in earlier stages of development, including trispecifics, bsAb prodrugs, bsAbs that induce degradation of tumour targets and bsAbs acting as cytokine mimetics.

双特异性抗体 (bsAb) 可实现使用传统 IgG 抗体无法实现的新作用机制和/或治疗应用。因此，这些分子的开发在过去十年中引起了人们的极大兴趣，截至 2023 年底，已有 14 种双特异性抗体获得批准：11 种用于治疗癌症，3 种用于非肿瘤适应症。双特异性抗体有不同的形式，针对不同的靶点并通过不同的分子机制介导抗癌功能。在这里，我们概述了用于癌症治疗的双特异性抗体领域的最新进展。我们专注于已批准或处于临床开发中的双特异性抗体，包括双特异性抗体介导的信号通路双重调节剂、肿瘤靶向受体激动剂、双特异性抗体-药物偶联物、双特异性 T 细胞、自然杀伤细胞和先天免疫细胞接合剂以及双特异性检查点抑制剂和共刺激器。最后，我们对处于早期开发阶段的下一代双特异性抗体进行了展望，包括三特异性抗体、双特异性抗体前药、诱导肿瘤靶标降解的双特异性抗体以及充当细胞因子模拟物的双特异性抗体。