Akeso, Inc. Doses First Patient in a Clinical Study of Anti-TIGIT Monoclonal Antibody (AK127) in Combination with Cadonilimab (Anti-PD-1/CTLA-4) for Treatment of Advanced or Metastatic Solid Tumors

(HONG KONG, 22 Oct 2021) Akeso, Inc. (the Company, 9926.HK) announces that the first patient was dosed in a Phase I clinical study of Akeso’s independently developed anti-TIGIT monoclonal antibody (AK127) in combination with Akeso’s global first-in-class anti-PD-1/CTLA-4 bi-specific antibody, cadonilimab (AK104), for the treatment of advanced or metastatic solid tumors in Australia.


This open-label, multicenter Phase I study is designed to evaluate the safety, tolerability, pharmacokinetic (PK), immunogenicity, pharmacodynamics and anti-tumor activity of AK127 in combination with cadonilimab in subjects with advanced or metastatic solid tumors.


Clinical trials have demonstrated promising efficacy of TIGIT monoclonal antibody in combination with PD-1 monoclonal antibody in immuno-oncology therapy. Cadonilimab simultaneously targets the two well-established immune checkpoints, PD-1 and CTLA-4. Preclinical studies showed that the combination of AK127 and cadonilimab produced a significantly enhanced anti-tumor effect in mice model.


Based on the promising efficacy seen in both preclinical and clinical studies on TIGIT monoclonal antibody in combination with PD-1 monoclonal antibody therapy, AK127 in combination with cadonilimab has the potential to demonstrate significant anti-tumor activity in treating patients with solid tumors, further enhance the potential and outlook of combination therapy, and strengthen and enrich the Company’s multi-target portfolio in immuno-oncology therapy.


Lead Principal Investigator for Study AK127-101 and Medical Oncologist at Monash Health, Melbourne, Australia, Dr. Sophia Frentzas shared, “In early phase studies, AK104 has shown encouraging anti-tumor activity in several tumor types with an improved safety profile compared to the co-administration of anti-PD-1 plus anti-CTLA-4 antibodies. AK127 is a novel, anti-TIGIT monoclonal antibody demonstrating encouraging anti-tumor and safety data in preclinical studies. We are thrilled to see our first patient dosed with AK127 and look forward to the results of this combination study as we believe it has the potential to address unmet clinical needs in several tumor types, both from a treatment resistance and tolerance perspective.”


By developing a rich pipeline of therapeutic antibodies for the treatment of cancer, the Company seeks to transform the treatment paradigm in the immuno-oncology space with combination therapies against various immune targets; and realize the full commercial value of its bi-specific antibodies that are based on an anti-PD-1 antibody backbone. Currently, clinical trials such as cadonilimab in combination with anti-CD47 monoclonal antibody (AK117), anti-VEGFR-2 monoclonal antibody (AK109), anti-CD73 monoclonal antibody (AK119) and anti-PD-1/VEGF (AK112) in combination with AK117, have all been successfully initiated.


About AK127 (TIGIT Monoclonal Antibody)

AK127 is a novel humanized IgG1k monoclonal antibody drug independently developed by the Company targeting TIGIT. TIGIT, which belongs to a constantly expanding family of poliovirus receptor (PVR)-like proteins, is an immune checkpoint inhibitory receptor. It is primarily expressed on activated and ‘‘exhausted’’ T and natural killer (NK) cells. Anti-TIGIT agents prevent TIGIT from binding to its ligand, CD155, leading to the removal of the inhibitory signal that impedes T cells and NK cells from attacking cancers. AK127 binds to TIGIT specifically and blocks the interaction of TIGIT and its ligands, thus relieves immune suppression and promotes anti-tumor immune response. TIGIT expression strongly correlates with PD-1, especially in tumor infiltrating T cells, and these two targets are often co-expressed on the same cell, which provides a scientific rationale for developing anti-TIGIT antibody agents in combination with anti-PD-L1 antibodies.


About Cadonilimab (PD-1/CTLA-4 Bi-Specific Antibody)

Cadonilimab (AK104) is a novel, potential next-generation, first-in-class bi-specific PD-1/CTLA-4 immuno-oncology backbone drug independently developed by the Company, and its major indications include liver cancer, cervical cancer, lung cancer, gastric cancer, esophageal squamous cell cancer and nasopharyngeal carcinoma. The preliminary research data of cervical cancer, gastric cancer and other tumors shows that, as compared with the combination therapy of PD-1 and CTLA-4, cadonilimab has much lower toxicity and demonstrated promising safety profile and efficacy.


Information about Akeso, Inc.

Akeso, Inc. is a biopharmaceutical company dedicated to the research, development, manufacturing and commercialization of new innovative antibody drugs that are affordable   to patients worldwide. Since the Company’s establishment, the Company has established an end-to-end comprehensive drug development platform (ACE Platform) and system, encompassing fully integrated drug discovery and development functions, including target validation, antibody drug discovery and development, CMC production process development, and GMP compliant scale production. The Company has also successfully developed a bi-specific antibody drug development technology (Tetrabody technology). The Company currently has a pipeline of over 20 innovative drugs for the treatment of major diseases like tumors, autoimmune diseases, inflammation and metabolism diseases, 13 of which have entered clinical stage, including two first-in-class bi-specific antibody drugs (PD-1/CTLA-4 and PD-1/VEGF). In Aug 2021, the Company’s first in-house innovatively researched and developed differentiated PD-1 monoclonal antibody Penpulimab monoclonal antibody injection (安尼可®) was approved to the market. The Company’s vision is to become a global leading biopharmaceutical company through research and development of high efficacy and breakthrough new drugs that are first-in-class and best-in-class therapies.