On October 23, 2026 BioLineRx Ltd. (NASDAQ/TASE: BLRX), a clinical-stage biopharmaceutical company pursuing life-changing therapies in oncology and rare diseases, and Hemispherian AS, a clinical-stage oncology company developing novel small molecule therapeutics, reported that the companies presented data at the 2026 European Society for Medical Oncology Annual Congress (ESMO 2026) demonstrating synergy between GLIX1 and multiple PARP inhibitors (PARPi) in homologous recombination (HR)-proficient ovarian cancer cell lines and in an in vivo patient-derived xenograft (PDX) model.

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"These preclinical findings extend the rationale for GLIX1 beyond glioblastoma, where we have already enrolled three dose-level patient cohorts in our Phase 1/2a clinical trial," said Philip Serlin, Chief Executive Officer of BioLineRx. "Importantly, the in vivo results further strengthen the rationale for combining GLIX1 with PARP inhibitors, demonstrating meaningful anti-tumor activity in an HR-proficient ovarian cancer model even at reduced doses of both agents. We are very encouraged by these findings and look forward to further exploring GLIX1/PARP inhibitor combinations, including the planned addition of an ovarian cancer arm in the expansion phase of our ongoing clinical trial."

"GLIX1 is designed to restore TET2 activity and drive tumor-selective DNA damage," said Dr. Adam Robertson, Ph.D., Chief Scientific Officer of Hemispherian AS and presenting author of the abstract. "These findings suggest GLIX1 could remove the HR-deficiency requirement for PARPi activity, thereby both improving and broadening the use of PARP inhibitors in ovarian cancers, and we look forward to building on this work."

Presentation Details:

Title: GLIX1, a TET2 Activator Targeting the DNA Damage Response, Synergizes with PARP Inhibitors in Ovarian Cancer Cell Lines

Category: Gynecological Cancers

Presentation #: 1435eP

Presentation type: e-Poster

Location: e-Poster Area, Hall 25

Summary:

Ovarian cancer remains difficult to treat, particularly in HR-proficient tumors, where PARP inhibitors have shown limited activity. GLIX1 is a first-in-class small molecule that activates TET2, an enzyme that is suppressed in cancer and normally drives DNA demethylation. By restoring TET2 activity, GLIX1 is designed to induce tumor-selective single-stranded DNA breaks through base excision repair, which could overcome the PARP inhibitor requirement for HR deficiency.

GLIX1 was combined with three PARP inhibitors (olaparib, veliparib and niraparib) across a panel of HR-proficient ovarian cancer cell lines, supporting a mechanism-driven class effect. The combination produced reproducible synergy with all three agents, with ZIP synergy scores ranging from 10.9 to 43.2 (olaparib: 15.4–43.0; veliparib: 10.9–43.2; niraparib: 12.2–39.8). Cells treated with the combination also showed upregulation of p21, consistent with activation of the DNA damage response.

The poster also presents results from a 28-day study in an HR-proficient ovarian cancer patient-derived xenograft (PDX) model (OV0250). The low-dose combination of GLIX1 (50 mg/kg daily) and olaparib (10 mg/kg daily) demonstrated statistically significant tumor growth inhibition versus vehicle control, and greater antitumor activity than either GLIX1 (250 mg/kg daily) or olaparib (50 mg/kg daily) administered alone at their respective optimal doses. The combination also demonstrated tumor growth inhibition comparable to cisplatin.

Additional tumor-exposure measurements demonstrated GLIX1 penetration into ovarian tumor tissue following oral administration, with tumor-to-plasma concentration ratios of approximately 50%. Plasma and tumor GLIX1 concentrations were measured one hour after dosing in a representative animal from each of the two GLIX1 monotherapy groups.

These data support synthetic lethality between GLIX1 and PARP inhibition and indicate that GLIX1 may remove the HR-deficiency requirement for PARP inhibitor activity. Such a combination, when applied clinically, may improve and broaden the use of PARPi in ovarian cancers. GLIX1 is currently being evaluated in a Phase 1/2a clinical trial in glioblastoma, with plans to include an ovarian cancer arm in the expansion phase (NCT07464925).

About GLIX1

GLIX1 is a first-in-class, orally administered, brain-penetrant small molecule activator of the Ten-Eleven Translocation 2 (TET2) pathway, which is commonly suppressed in cancer. Activating TET2 with GLIX1 is designed to overwhelm the DNA repair capacity of cancer cells, resulting in tumor-selective cell death. GLIX1 is being developed by BioLineRx and Hemispherian AS for the treatment of glioblastoma and other solid tumors.

About Ovarian Cancer

Ovarian cancer is the deadliest gynecologic malignancy in the United States, with an estimated 21,000 new cases and over 12,000 deaths projected in 2026. Standard first-line treatment consists of cytoreductive surgery and platinum-based chemotherapy, with PARP inhibitors used as maintenance therapy in selected patients, particularly those with BRCA-mutated or homologous recombination (HR)-deficient disease. However, PARP inhibitors are markedly less effective in patients with HR-proficient tumors, which account for approximately 50% of high-grade serous ovarian cancers and are associated with primary platinum resistance and shorter survival. This leaves a substantial and currently underserved patient population in need of new treatment strategies capable of extending the benefits of PARP inhibitors.

(Press release, BioLineRx, OCT 23, 2026, View Source [SID1234673702])