BioLineRx and Hemispherian Present GLIX1 Data

Tel Aviv, Israel, and Oslo, Norway, September 10, 2026

GLIX1 Shows Antitumor Activity in GBM Models

The oral presentation will focus on GLIX1’s activity in multiple preclinical glioblastoma models. GLIX1 is being developed as an oral TET2 activator designed to target the DNA damage response. According to the companies, the investigational compound demonstrated high potency across cancer cell lines and increased TET2-dependent 5-hydroxymethylcytosine (5hmC) generation in biochemical, cellular and xenograft studies. The preclinical program also provided evidence that GLIX1 can reach the central nervous system. In mouse studies, brain exposure reached 68% to 85% of plasma levels, supporting the compound’s ability to penetrate the brain and potentially reach tumors located within the central nervous system. In two orthotopic GBM xenograft models, including the slower-growing SNB19 model and the more aggressive U87-MG model, oral GLIX1 produced dose-dependent tumor growth inhibition and survival benefits across the tested dose range. Antitumor activity was observed even at the lowest dose evaluated, while greater effects were reported at higher doses. A temozolomide-resistant patient-derived xenograft model also contributed to the preclinical development rationale. Importantly, these findings are preclinical results from animal and laboratory models and do not establish that GLIX1 will demonstrate similar efficacy or safety in patients.

Phase 1/2a Trial Evaluates GLIX1 in Glioma

The second EANO presentation will outline the design of the ongoing Phase 1/2a study of GLIX1 in patients with recurrent or progressive high-grade glioma. The first-in-human, open-label, multicenter trial is actively enrolling patients and is designed to evaluate the investigational therapy in patients with WHO grade 3/4 glioma who have received no more than two prior lines of therapy. The study will use a Bayesian Optimal Interval (BOIN) design to guide dose escalation across up to five dose levels and is planned to enroll up to 30 patients. The primary objectives are to characterize safety and tolerability and determine the maximum tolerated dose and/or recommended Phase 2 dose. Secondary assessments will include pharmacokinetics and antitumor response, while exploratory analyses will examine pharmacodynamic biomarkers including P21, TMEM71, 5hmC, 5mC and γH2AX. Four leading U.S. academic institutions are expected to participate in patient enrollment. The trial represents an important transition for GLIX1 from laboratory development into human clinical evaluation. However, the program remains investigational, and clinical safety and efficacy have yet to be established.

Companies Advance TET2-Targeted Oncology Program

The development strategy for GLIX1 is based on the role of TET2 activity and DNA methylation in cancer biology. According to the companies, glioblastoma shows markedly reduced genomic 5hmC compared with healthy brain tissue, reflecting impaired TET2 activity. GLIX1 is designed to activate TET2 and promote DNA demethylation, ultimately generating DNA damage that could selectively affect tumor cells. The companies believe this mechanism could provide a differentiated approach to treating glioblastoma, one of the most aggressive forms of brain cancer. The program is also being investigated for potential application across a broader range of solid tumors. The EANO 2026 presentations will provide an opportunity for the scientific community to review both the preclinical efficacy evidence supporting GLIX1 and the clinical strategy being used to evaluate the therapy in humans. Results from the ongoing Phase 1/2a study will be important for determining whether the preclinical findings can translate into meaningful clinical activity.

Source: BioLineRx, Hemispherian press release