• Positive biomarker analysis results and PK data from a Phase 1a clinical trial of TU2218 in patients with advanced solid tumor cancers

• In the Phase 1a, TU2218 demonstrated significant changes in key biomarkers, including CTGF and TGF-beta, suggesting that TU2218 has the potential to be an effective combination therapy with immune checkpoint inhibitors for cancer

TiumBio Co., Ltd. (KOSDAQ: 321550), a clinical-stage biopharmaceutical company focusing on discovering and developing innovative therapeutics for patients with incurable diseases, announces that it presented clinical data and biomarker analysis results from the Phase 1a clinical trial of TU2218 in patients with advanced solid tumors at the 38^th Society for Immunotherapy of Cancer (SITC) Annual Meeting on November 3, 2023.

In addition to the safety and tolerability results of TU2218 presented at ESMO 2023, the poster for TU2218 monotherapy in Phase 1a clinical trial (NCT05204862) contains major biomarker* analysis results.

*Biomarker: A biomarker, a measurable indicator of some biological state or condition, is used to objectively measure the degree of biological response to a drug.

In the study, significant reductions in biomarkers such as connective tissue growth factor (CTGF) and transforming growth factor-β (TGF-ß), which are known to be controlled by TGF-ß signaling, were observed at Day 7 after administered TU2218. In particular, the plasma concentration of CTGF decreased by an average of 27% compared to baseline in the lowest-dose group (15 mg BID) after 7 days of administration, and it decreased by an average of 47.8% in the highest-dose group (135 mg BID).

Furthermore, in groups that received 52.5mg BID* or higher, which is the starting dose of the next Phase 1b trial of TU2218 in combination with pembrolizumab, more greater reductions in CTGF and TGF-ß 1 were observed.

*BID : Twice a day

“We are encouraged to see key biomarker results, including CTGF and TGF-ß, from the study of TU2218 in patients,” said Hun-taek Kim, Ph.D., MBA, Founder and CEO of TiumBio. “These results suggest that TU2218 could effectively work for cancer with immune checkpoint inhibitors, and we expect that the combination of TU2218 and pembrolizumab could show great efficacy in following clinical trials,” he added.

TU2218 is a first-in-class oral dual kinase inhibitor targeting transforming growth factor beta receptor type 1 (TGFβRI) and vascular endothelial growth factor receptor-2 (VEGFR2). The investigational drug is expected to significantly improve the response rates of cancer patients who are unresponsive or have limited therapeutic effects with immune checkpoint inhibitors by simultaneously blocking TGF-β, which interferes with the activity of immune-oncology drugs in the tumor microenvironment, and VEGFR2, which is a factor a factor associated with blood vessel formation around tumor cells.

* Attached file : SITC_ePoster_TU2218 Phase 1a