Antengene Corporation Limited ("Antengene" SEHK: 6996.HK), a leading innovative, global biopharmaceutical company dedicated to discovering, developing and commercializing first-in-class and/or best-in-class medicines for cancer and other life-threatening diseases, announced today a clinical trial collaboration to evaluate the safety, pharmacokinetics and preliminary efficacy of ATG-017 in combination with Bristol Myers Squibb's PD-1 checkpoint inhibitor, Opdivo? (nivolumab). The open-label Phase 1/2 trial will evaluate the investigational combination as a potential treatment option for patients with advanced solid tumors.

"Our clinical collaboration with Bristol Myers Squibb underscores Antengene's commitment to explore combination regimens from our portfolio with other mechanisms of action that might transform cancer care", said Jay Mei, M.D., Ph.D., Founder and CEO of Antengene. "We are excited to enter this clinical collaboration with Bristol Myers Squibb and look forward to initiating enrollment in this exciting combination regimen in the first half of 2022."

ATG-017 is an oral and selective inhibitor of extracellular signal–regulated protein kinase 1 and 2 (ERK1/2). Opdivo? is a human programmed death receptor-1 (PD-1) blocking antibody that binds to the PD-1 receptor expressed on activated T-cells. This collaboration builds on Antengene's preclinical data set, some of which was presented at the Society for Immunotherapy in Cancer (SITC) 2021, which showed that the combination of an ERK1/2 inhibitor and an immune checkpoint inhibitor (CPI) worked synergistically to produce improved efficacy in preclinical immune CPI-resistant cancer models.

"Antengene believes that rational combination of targeted therapies and immuno-oncology drugs may offer the greatest chance of success in the next advances of cancer treatments," said Kevin Lynch, M.D., Antengene's Chief Medical Officer. "We believe ATG-017 could be useful in multiple combination regimens. In preclinical studies, the combination of ATG-017 and an immune CPI demonstrated promising synergy in resistant and refractory murine tumor models. With the initiation of our Phase 1/2 combination trial, we will be working to validate these promising findings in the clinic. We believe these data will inform the design of future studies and, if positive, demonstrate ATG-017's potential to synergize with immuno-oncology agents and turn "cold" tumors "hot". Potent inhibition of ERK has the potential to reverse an immune-suppressed tumor microenvironment, or block ERK-mediated disease progression that may characterize CPI-resistance and hyper-progressive disease. This represents a major unmet need in cancer therapy," continued Dr. Lynch.

ATG-017 is currently being investigated in a Phase 1/2 open-label, multicenter dose-finding study, the "ERASER" study, in patients with identified mutations in the RAS-MAPK pathway. The trial is being conducted in two parts, with dose-escalation and dose-expansion parts exploring both monotherapy and as a combination therapy, with a PD-1 checkpoint inhibitor as the first partner drug.

Under the terms of the Agreement, Antengene will sponsor and fund the study and Bristol-Myers Squibb will provide Opdivo? for the combination dose escalation and combination dose expansion portions of the trial. Antengene has global commercial and development rights to ATG-017. Opdivo? is a trademark of Bristol-Myers Squibb Company.

About ATG-017

ATG-017 is a potent and selective small molecule extracellular signal-regulated kinases 1 and 2 (ERK1/2) inhibitor. ERK1/2 are related protein-serine/threonine kinases that function as terminal kinases in the RAS-MAPK signal transduction cascade. This cascade regulates a large variety of cellular processes, including proliferation. The RAS-MAPK pathway is dysregulated in more than 30% of human cancers with the most frequent alterations being observed in RAS or BRAF genes across multiple tumor types. An ERK inhibitor enables the targeting of both RAS and BRAF mutant diseases.

Antengene recently presented data at the 2021 Society for Immune Therapy in Cancer meeting (SITC 2021) detailing compelling preclinical results showing the combination of ATG-017 and an anti-PD-L1 monoclonal antibody (atezolizumab) in an aggressive immune checkpoint resistant murine cancer model rendered "cold" tumors "hot."

About Antengene

Antengene Corporation Limited ("Antengene", SEHK: 6996.HK) is a leading clinical-stage R&D- driven global biopharmaceutical company focused on innovative first-in-class/best-in-class therapeutic medicines for oncology and other life-threatening diseases. Driven by its vision of "Treating Patients Beyond Borders", Antengene aims to provide the most advanced anti-cancer drugs to patients in the Asia Pacific Region and around the world. Since initiating operations in 2017, Antengene has obtained 20 investigational new drug (IND) approvals in Asia Pacific and the US, submitted 6 new drug applications (NDAs) in multiple Asia Pacific markets, with the NDA for selinexor/ATG-010 in South Korea already approved through a priority review process. Antengene has built a broad and expanding pipeline of 15 clinical and preclinical assets by leveraging partnerships as well as in-house drug discovery. The Company has global rights on 10 programs and Asia Pacific rights, including the Greater China region, on 5 programs.

Forward Looking Statement

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Source: Antengene Corporation Limited