• In Phase 1a, TU2218 demonstrated a favorable safety and tolerability profile in patients with advanced tumors with no TRAEs of Grade 3 or higher

• TiumBio plans to complete its ongoing Phase 1b trial of TU2218 in combination with Keytruda (pembrolizumab) and enter into a Phase 2a study in the first half of 2024

TiumBio Co., Ltd. (KOSDAQ: 321550), a clinical-stage biopharmaceutical company focusing on discovering and developing innovative therapeutics for patients with incurable diseases, announces that clinical results from its Phase 1a clinical trial of TU2218 were presented at the European Society of Medical Oncology (ESMO) 2023 Congress on Monday, October 23, 2023.

TU2218 is a first-in-class oral dual kinase inhibitor against transforming growth factor-beta (TGF-β) receptor type 1 and vascular endothelial growth factor receptor 2 (VEGFR2). It is expected to significantly improve the response rate in combination with immune checkpoint inhibitors such as anti-PD1 antibodies. Overexpressed TGF-β in the tumor microenvironment is reported as a major factor that hinders the efficacy of immune-oncology drugs and VEGF is known to be involved in angiogenesis around tumor cells.

“In the first-in-human study, TU2218 was administered daily in escalating doses from 30mg to 270mg, and dose limiting toxicity (DLT) and treatment-related adverse events of Grade 3 or higher were not observed, demonstrating a favorable safety and tolerability profile of TU2218,” said Do-Youn Oh. M.D., the principal investigator of the clinical trial and a presenting author, professor in the Division of Medical Oncology at Seoul National University College of Medicine.

“Following the successful results of TU2218 in combination with immunotherapies in preclinical studies, we are thrilled to see safety results from the Phase 1a trial in patients with advanced solid tumors,” said Hun-taek Kim, Ph.D., MBA, Founder and CEO of TiumBio. “Based on the findings from the clinical studies, we remain committed to delivering innovative anti-cancer treatment options to patients who do not respond to or are refractory to existing therapies,” he added.

In the TU2218 Phase 1a study (NCT05204862), 22 patients with advanced solid tumor in Korea and the United States were administered TU2218 with escalating doses, ranging from 30mg (15mg BID*) to 270mg (135mg BID) per day.

*BID: Twice a day

Meanwhile, TiumBio is currently conducting a Phase 1b clinical trial (NCT05784688) of the combination of TU2218 and Keytruda in the United States, and the clinical results of Phase 1b are expected in the first half of next year. Furthermore, it plans to initiate a TU2218 Phase 2a study in the first half of 2024.

*  Attached file : TU2218  Phase 1a Poster Presentation at ESMO