• - TiumBio will pursue three indications for the TU2218 combination clinical trial with pembrolizumab
• - TU2218 demonstrated a favorable safety and a synergetic effect with immuno-oncology drugs in preclinical studies

TiumBio Co., Ltd. (KOSDAQ: 321550), a clinical-stage biopharmaceutical company focused on discovering and developing innovative therapeutics for patients with rare and incurable diseases, announced that it has submitted Investigational New Drug (IND) application to the Korean Ministry of Food and Drug Safe (MFDS) for a Phase 2a study of TU2218, an oral immuno-oncology drug, in late February, 2024 and that preclinical results of TU2218 will be presented at the upcoming 2024 American Association for Cancer Research (AACR) Annual Meeting.

TU2218 is a novel oral dual inhibitor targeting transforming growth factor beta receptor 1 (TGFR1) and vascular endothelial growth factor receptor 2 (VEGFR2). TGF-ß and VEGF pathways are known to be factors that interfere with the activity of immuno-oncology drugs, so TU2218 is expected to maximize the efficacy of immuno-oncology drugs by blocking them. TiumBio is currently conducting a Phase 1b clinical trial of TU2218 in combination with Keytruda (pembrolizumab) in advanced solid tumors in the U.S.

For the Phase 2a trial, TiumBio has selected indications in biliary tract cancer (BTC), head and neck squamous cell carcinoma (HNSCC), and colorectal cancer (CRC). The study will enroll up to 116 evaluable participants across three cohorts (up to 40 participants for BTC, up to 36 participants for HNSCC, and up to 40 participants for CRC, respectively) and will evaluate the efficacy and safety of TU2218 administered in combination with pembrolizumab.

BTC, HNSCC, and CRC have historically shown low treatment response rates to existing therapies. TiumBio expects that the combination of TU2218 and Keytruda will improve response rates in these tumors.

Meanwhile, to test the feasibility of various combination options with TU2218, TiumBio conducted in vivo efficacy studies in 4T1, MC39, and CT26 syngeneic tumor models. Results will be presented at the 2024 AACR, taking place from April 5-10 in San Diego, California. 

The poster abstract highlights the improved efficacy and safety profile of TU2218 in combination with various immuno-oncology drugs. Specifically, the combination of lenvatinib, anti-PD-1 antibody, and TU2218 demonstrated a significant tumor growth inhibition (TGI) of 99% and a complete response (CR) rate of 67% in the CT 26 model, compared to a TGI of 76% and CR of 17% in the control group receiving only lenvatinib and anti-PD-1 antibody. The statistical difference in anti-tumor activity between the two groups was deemed significant (p<0.001).

"We believe that the results of this TU2218 triple combination regimen show substantial potential in enhancing anticancer efficacy. We will explore the commercial potential of the combination," said Hun-taek Kim, Ph.D., MBA, Founder and CEO, TiumBio. "The three indications we selected are diseases characterized by high expression of the target protein TGF-beta within the microenvironment, coupled with a significant unmet medical need attributed to low response rates to anti-PD-1 therapies. We will develop TU2218 as a safer and more effective novel drug to increase clinical benefits of the immune checkpoint inhibitors in this area," he added.