Ociperlimab (BGB-A1217): A Comprehensive Clinical and Scientific Monograph on a Discontinued Anti-TIGIT Immunotherapy

Executive Summary

Ociperlimab, also known as BGB-A1217, was an investigational humanized monoclonal antibody developed by BeiGene targeting the T-cell immunoreceptor with immunoglobulin and ITIM domains (TIGIT), a novel immune checkpoint. The scientific rationale for ociperlimab was rooted in the hypothesis that blocking the inhibitory TIGIT pathway, particularly in combination with PD-1 blockade, could restore and amplify anti-tumor immune responses. A key differentiating feature of ociperlimab was its design as an Fc-competent immunoglobulin G1 (IgG1) antibody, intended to mediate additional anti-tumor effects such as antibody-dependent cellular cytotoxicity (ADCC) against immunosuppressive regulatory T-cells.

The drug's development trajectory was initially marked by promising preclinical data and encouraging early-phase clinical results. The Phase 1/1b AdvanTIG-105 study established a manageable safety profile and demonstrated notable antitumor activity in expansion cohorts for non-small cell lung cancer (NSCLC), gastric cancer, and esophageal cancer, particularly when combined with chemotherapy. This early promise culminated in a landmark option and collaboration agreement with Novartis in December 2021, featuring a $300 million upfront payment, which served as a significant external validation of the program and the broader TIGIT therapeutic class.