Akeso, Inc. announced the publication of preclinical results of its anti-TIGIT monoclonal antibody (AK127) showing potent preclinical anti-tumor activities at the American Association for Cancer Research (AACR) Annual Meeting 2022. AK127 is a novel humanized immunoglobulin (Ig) G1 monoclonal antibody (mAb) targeting T cell immunoreceptor with immunoglobulin and immunoreceptor tyrosine-based inhibitory motif domain (TIGIT). AK127 specifically binds to TIGIT and blocks the interaction of TIGIT with its ligands, thus relieving immune suppression and promoting anti-tumor immune response.

Immune checkpoint blocking antibodies achieved great clinical success, yet a large fraction of cancer patients receive minimum benefit from current immunotherapies targeting PD-1 and CTLA-4. As a new multifunctional immune checkpoint molecule, TIGIT holds promise to become an important cancer immune therapy target. The observations in AK127's preclinical study support the development of AK127 as an anti-tumor agent in the clinic:AK127 blocked the immune inhibitory signal mediated by TIGIT, resulting in enhanced IL-2 secretion; AK127 exhibited binding to Fc?RIa, Fc?RIIIa and C1q, and eliciting ADCC, ADCP and CDC; In animal models, both AK104 (0.5 mg/kg) and AK127 (4 mg/kg) significantly inhibited tumor growth. The combination of AK127 and AK104 produced a significantly enhanced anti-tumor effect than either monotherapy, demonstrating the synergistic anti-tumor activity of AK127 combined with AK104.