Exploring Bispecific Antibodies for Multifaceted Cancer Targeting

Bispecific antibodies (BsAbs) represent an exciting approach to cancer therapy, potentially addressing the limitations of traditional treatments, including monoclonal antibodies. BsAbs simultaneously target more than one antigen or epitope of different types. The dual-targeting ability of BsAbs offers a compound mechanism of action that includes immune cell recruitment to tumour cells or the inhibition of signalling pathways associated with cancer proliferation. According to recent reports, hundreds of BsAbs are in the process of development at various stages. Nineteen BsAbs, mostly for oncology targets as well as a few for non-oncology applications, have been approved globally by regulators as of May 2025. This chapter examines the structural formats, mechanism of action, clinical applications, and prospects of BsAbs in oncology, highlighting their potential to transform cancer treatment standards. Depending on tumour type, target accessibility, and desired immune engagement, BsAbs deliver tailored therapeutic strategies by various structural formats. These formats of BsAbs are engineered differently, such as fragment-based and IgG-based. Additionally, BsAbs employ antitumour effects through diverse mechanisms such as T-cell redirection, checkpoint blockade, and dual antigen targeting. Several BsAbs have shown efficacy in haematological and solid tumours. BsAbs also have targeting advantages, as they can overcome tumour heterogeneity by targeting multiple antigens or pathways, potentially leading to more effective tumour management. As they target multiple pathways, BsAbs have the potential to minimize the possibility of treatment resistance. BsAbs mark a transformative advancement in cancer immunotherapy, with their multitarget precision and evolving design poised to fulfil their therapeutic promise.