Tyligand Bioscience Announces First Patient Dosed for the Phase 1 Trial of TSN222，the Global First Dual Action Tumor Immune Agonist

Shanghai, July 28^th, 2023 – Tyligand Bioscience, a clinical stage biotech company focused on the development of innovative drugs to treat drug-resistant tumors, is pleased to announce that the first patient has been dosed in the Phase 1 trial for TSN222 at Fudan University Shanghai Cancer Center in Shanghai.

TSN222 is a novel bifunctional small molecule designed with sequential release of immune agonism and cytotoxic function modulated by pharmacokinetics. It activates interferon production in the tumor microenvironment, then kills tumor cells to provide tumor antigens and DNAs to prime the adaptive immune system and further activate the STING pathway, synergistically.

Preclinical data of TSN222 has demonstrated good tolerability, excellent tumor suppression effect and sustainable immune memory. This first-in-human Phase 1 study is designed to evaluate the safety, tolerability, pharmacokinetic profile and preliminary efficacy of TSN222 in patients with advanced solid tumors or lymphoma. The study will be led by Professor Jian Zhang of Fudan University Shanghai Cancer Center.

“TSN222 is the first product from the DATIA^® (Dual Action Tumor Immune Agonist) platform that enters clinical stage”, said Tony Zhang, PhD., co-founder and CEO of Tyligand, “the achievement of this important milestone demonstrates the team's ability to produce quality clinical candidates by actualizing the "Tie + Ligand" concept with innovative molecular design capabilities. We have also established a differentiated antibody conjugates pipeline based on the DATIA^® platform and the preliminary data showed superior and long-lasting tumor inhibition efficacy. We are actively expanding external collaborations built from DATIA^® to accelerate the discovery and development of more effective and accessible therapeutic options for the patients.”

Professor Jian Zhang of the Fudan University Shanghai Cancer Center said: “Cancer treatment has now into the era of immunotherapy. However, only 15% ~20% of patients can benefit from immunotherapy, which involves using immune checkpoint inhibitors to "release the brakes". Additional approach uses immune agonist to "step on the engine" to activate immune response, making the anti-tumoral effects more sustained and effective, which is the current research of interest. Dosing the first patient is an important step toward understanding the potential role of TSN222 for patients with advanced tumors. We look forward to evaluating the results of this study and offering this innovative treatment option to patients.”