GLIX1 / Tetragon Biosciences - LARVOL DELTA

GLIX1, a TET2 activator targeting the DNA damage response: Potent anti-tumor activity across multiple orthotopic glioblastoma models (EANO 2026) - P1 | "Temozolomide (TMZ) was included in the two models as positive control. GLIX1 showed robust efficacy across multiple orthotopic GBM models in a dose dependent manner, with strong antitumor activity observed already at the lowest dose tested. Based on these data, a first-in-human, dose escalating, Phase I/2a clinical trial with GLIX1 monotherapy for adults with recurrent or progressive HGG has been initiated (NCT07464925)."

First-in-human • Brain Cancer • Glioblastoma • Oncology • Solid Tumor • TET2

Phase 1 2a study of GLIX1, an oral TET2 activator, for the treatment of recurrent or progressive high-grade gliomas (EANO 2026) - P1 | "Breakthrough innovations are desperately needed for patients with high-grade gliomas. We present a FIH study with GLIX1, a novel, first-in-class, TET2 activator, targeting DNA damage response with a strong rationale for treatment of gliomas."

First-in-human • P1/2 data • Brain Cancer • Glioblastoma • Glioma • High Grade Glioma • Oncology • Solid Tumor • CDKN1A • TET2

GLIX1, a TET2 activator targeting DNA damage response: potent anti-tumor activity across multiple glioblastoma models; orthotopic CDX models and a subcutaneous TMZ-resistant PDX model (SNO 2026) - No abstract available

Brain Cancer • Glioblastoma • Oncology • Solid Tumor • TET2

Phase 1/2a study of GLIX1, a novel first-in-class oral TET2 activator, for the treatment of recurrent or progressive high-grade glioma (SNO 2026) - No abstract available

P1/2 data • Brain Cancer • Glioma • High Grade Glioma • Solid Tumor • TET2

Development Updates: GLIX1 in GBM (PRNewswire) - "In July, dosing commenced in the second of five planned cohorts in the Phase 1 dose escalation part of the Phase 1/2a study. Three leading cancer centers are enrolling patients in the Phase 1 part of the study: NYU Langone Health, led by Dr. Alexandra Miller; Northwestern University, led by Dr. Roger Stupp and Dr. Ditte Primdahl; and Moffit Cancer Center, led by Dr. Patrick Grogan. The Phase 1 part of the trial is expected to recruit up to 30 patients with recurrent and progressive GBM and other high-grade gliomas....The Phase 2a expansion part of the trial is planned to include various population cohorts, including GBM (newly diagnosed and/or recurrent), as well as additional cancers with/without standard of care (e.g., PARP inhibitors), including an ovarian cancer arm."

Trial status • Glioblastoma • Ovarian Cancer

BioLineRx…and Hemispherian AS…announced that an abstract featuring pre-clinical data demonstrating strong synergy between GLIX1 and various PARP inhibitors in HR-proficient ovarian cancer cell lines has been accepted as an e-Poster at the 2026 European Society for Medical Oncology Annual Congress (ESMO 2026) (PRNewswire)

Preclinical • Ovarian Cancer

BioLineRx and Hemispherian Announce New Preclinical Data Demonstrating Strong Synergistic Effect between GLIX1 and PARP Inhibitor in a Patient-Derived Ovarian Cancer Xenograft Model (PRNewswire) - "GLIX1 in combination with PARPi is expected to result in synthetic lethality, a mechanism in which GLIX1-induced single-stranded DNA breaks overcome PARP inhibitors' requirement for HR-deficiency, enabling synergistic activity in HR-proficient cancers. This effect was first observed in vitro, where GLIX1 showed reproducible synergy across different PARP inhibitors and multiple HR-proficient ovarian cancer cell lines, with very high ZIP synergy scores...'Based on these highly encouraging data, we plan to include an ovarian cancer arm in the expansion part of our ongoing Phase 1/2a study.'...Results show substantially better efficacy in the combination arm versus the control arm and versus the monotherapy arms, despite using lower doses in the combination arm....BioLineRx and Hemispherian plan to present the data from this study at one or more future medical conferences."

Preclinical • Trial status • Ovarian Cancer

Synergistic antitumor activity of GLIX1, a small molecule TET2 activator, in combination with PARP inhibition across multiple cancers. (ASCO 2026) - "These data demonstrate broad in vitro synergy between GLIX1 and PARP inhibition across diverse cancers. The complementary mechanisms of GLIX1-mediated DNA modification and PARP-dependent DNA repair provide a strong mechanistic rationale for combination therapy and support further translational and clinical evaluation."

Combination therapy • Oncology • HRD • TET2

GLIX1: A first-in-class oral molecule targeting the DNA damage response by restoring TET2 activity. (ASCO 2026) - "GLIX1 targets the DNA damage response by enhancing TET2 activity. Its unique mechanism is applicable to a broad range of cancers. GLIX1 crosses the blood brain barrier and has shown significant activity in various in vitro and in vivo GBM and glioma tumor models."

First-in-human • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • High Grade Glioma • Oncology • TET2

BioLineRx Reports First Quarter 2026 Financial Results and Provides Corporate Update (PRNewswire) - "Announced two abstracts on GLIX1 that were selected for publication during the American Society of Clinical Oncology (ASCO) Annual Meeting, which is scheduled for May 29-June 2, in Chicago, IL...Enrollment is continuing in the CheMo4METPANC Phase 2b clinical trial....A prespecified interim/futility analysis is planned when 40% of progression-free survival (PFS) events are observed, which the Company continues to anticipate will occur in 2026."

P2 data • Preclinical • Trial status • Glioblastoma • Pancreatic Ductal Adenocarcinoma

GLIX1: A first-in-class oral molecule targeting the DNA damage response by restoring TET2 activity (Morningstar.com) - "Preclinical studies have shown that GLIX1 effectively increases TET2 activity and downstream 5hmC production in biochemical assays, cell models, and in vivo animal systems. The high potency of GLIX1 was observed in vitro in a broad range of cancer cell lines. The drug demonstrated strong antitumor activity in multiple glioblastoma xenograft models (including U87-MG and SNB-19) and was able to penetrate the brain efficiently after oral dosing, with brain exposure corresponding to 68-85% of plasma levels in mice. Safety studies in animals indicated that GLIX1 is well-tolerated even at the highest feasible doses tested: 2000mg/kg in rats and 1000mg/kg in dogs."

Preclinical • Glioblastoma

Synergistic antitumor activity of GLIX1, a small molecule TET2 activator, in combination with PARP inhibition across multiple cancers (Morningstar.com) - "In preclinical in vitro studies across a wide range of cancer cell lines, the combination of GLIX1 with multiple PARP inhibitors produced strong and consistent cytotoxic effects, including in tumor types typically less responsive to PARP inhibition. This synergy was observed across different PARP inhibitors with varying properties, suggesting a class-wide effect rather than dependence on a specific agent. Overall, the findings provide a compelling mechanistic rationale for combining GLIX1 with PARP inhibitors and warrant further investigation of this strategy across diverse cancers."

Preclinical • Solid Tumor

BioLineRx and Hemispherian Announce New GLIX1 Data Demonstrating Potent Anti-Tumor Effect in Glioblastoma (GBM) Across Multiple In-Vivo Studies, Including a Temozolomide (TMZ)-Resistant Model with Patient-Derived Xenografts (PRNewswire) - "In a comprehensive pre-clinical program, orally administered GLIX1 demonstrated robust anti-tumor activity in orthotopic cell-derived xenograft (CDX) GBM models, as well as in a newly completed subcutaneous TMZ-resistant patient-derived xenograft (PDX) GBM model. In the three orthotopic CDX studies, significant tumor growth inhibition and survival benefit were observed following treatment with GLIX1 across all doses tested, with greater benefit at higher dose levels....BioLineRx and Hemispherian plan to present the data from these studies at one or more future medical conferences."

Preclinical • Glioblastoma

A Phase 1 Safety and Dose Finding Study of GLIX1 in Adults With Recurrent or Progressive High-grade Glioma (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: Tetragon Biosciences Ltd | Not yet recruiting ➔ Recruiting

Enrollment open • Brain Cancer • Glioblastoma • Glioma • High Grade Glioma • Oncology • Solid Tumor

BioLineRx…and Hemispherian AS…announced that the first patient has been dosed in the first-in-human, Phase 1/2a study of GLIX1 for the treatment of recurrent and progressive glioblastoma (GBM) and other high-grade gliomas (PRNewswire) - "The patient was dosed at NYU Langone Health under the supervision of Dr. Alexandra Miller, Chief of Neuro-Oncology & Co-Director of Brain and Spine Tumor Center, Perlmutter Cancer Center....The Phase 1 part of the trial is a dose escalation part where patients receive GLIX1 daily as monotherapy. This part is expected to recruit up to 30 patients with recurrent and progressive GBM and other high-grade gliomas....Data from the Phase 1 part of the trial are anticipated in H1 2027."

First-in-human • P1 data • Trial status • Glioblastoma • High Grade Glioma

BioLineRx Announces Initiation of Phase 1/2a Study of GLIX1 for the Treatment of Glioblastoma (GBM) (PRNewswire) - "The first center ready to start enrolling patients is NYU Langone Health, led by Dr. Alexandra Miller. This will be followed by Northwestern University, led by Dr. Roger Stupp and Dr. Ditte Primdahl, and by Moffit Cancer Center, led by Dr. Patrick Grogan...The Phase 1 part of the trial is expected to recruit up to 30 patients with recurrent and progressive GBM and other high-grade glioma...Data from the Phase 1 part of the trial are anticipated in H1 2027...The Phase 2a expansion part of the trial is planned to include various population cohorts, including GBM (newly diagnosed and/or recurrent), as well as additional cancers with/without standard of care (e.g., PARP inhibitors)."

P1 data • Trial status • Glioblastoma • Glioma • High Grade Glioma

Clinical Updates (PRNewswire) - "Continued to advance preparations for initiation of a Phase 1/2a clinical trial of GLIX1 in recurrent and newly diagnosed glioblastoma in the first quarter of 2026....Enrollment continues in the CheMo4METPANC Phase 2b clinical trial, which is being led by Columbia University, and supported by both Regeneron and BioLineRx. The CheMo4METPANC trial is evaluating motixafortide in combination with the PD-1 inhibitor cemiplimab and standard chemotherapy (gemcitabine and nab-paclitaxel)."

Enrollment status • New P1/2 trial • Glioblastoma • Pancreatic Ductal Adenocarcinoma

BioLineRx Announces Receipt of USPTO Notice of Allowance for Key Patent Covering GLIX1 for Treating a Broad Range of Cancer Types (PRNewswire) - "Patent covers the use of GLIX1 for treating cancers in which cytidine deaminase (CDA) is not over-expressed (representing over 90% of cancers). Patent further broadens and strengthens GLIX1 patent protection until 2040, with a possible patent-term extension of up to five years."

Patent • Solid Tumor

BioLineRx Ltd. and Hemispherian AS Establish Joint Venture to Develop GLIX1, a First-in-Class, Oral, Small Molecule Targeting DNA Damage Response in Glioblastoma and Other Cancers (StockTitan.net) - "The FDA has cleared the IND application for GLIX1, with a Phase 1/2a study set to begin in Q1 2026...Under the agreement, Hemispherian contributes GLIX1's global rights and will initially hold 60% of the JV, while BioLineRx will manage and fund development activities with a 40% initial stake, potentially increasing to 70%...With data expected in H1 2027, this represents a mid-term catalyst for BioLineRx..."

Commercial • P1/2 data • Glioblastoma

Hemispherian Receives FDA IND Clearance for First-in-Class Glioblastoma Therapeutic, GLIX1 (PRNewswire) - "Hemispherian AS...announced that the U.S. Food and Drug Administration (FDA) has cleared the company's Investigational New Drug (IND) application for GLIX1, a first-in-class small molecule targeting DNA repair vulnerabilities in glioblastoma and other solid tumors. The IND clearance allows Hemispherian to proceed with a first-in-human Phase 1 clinical trial to evaluate the safety, tolerability, pharmacokinetics, and preliminary efficacy of GLIX1 in patients with recurrent glioblastoma....The Phase 1 study will be conducted at leading neuro-oncology centers across the United States, starting at Northwestern University in Chicago."

IND • New P1 trial • Glioblastoma

Hemispherian Receives U.S. FDA Orphan Drug Designation for GLIX1 for the Treatment of Malignant Glioma (PRNewswire) - "Hemispherian AS...announced today that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) for GLIX1 for the treatment of malignant glioma, a category of devastating brain cancers that includes glioblastoma....The designation marks a major regulatory milestone for Hemispherian, recognizing both the urgent unmet medical need in glioma and the potential of GLIX1 to offer significant clinical benefit beyond current therapies....The designation is based on GLIX1's potential to treat a rare and life-threatening disease affecting fewer than 200,000 people in the United States. GLIX1 demonstrated substantial preclinical efficacy, including tumor regression and survival benefit in validated models of glioma."

Orphan drug • Glioblastoma • Glioma

Hemispherian receives positive opinion for Orphan Medicinal Product Designation in the EU for GLIX1 in glioma (Yahoo Finance) - "Hemispherian AS...announced today that the European Medicines Agency's (EMA) Committee for Orphan Medicinal Products (COMP) has issued a positive opinion recommending Orphan Drug Designation (ODD) for GLIX1, the company's lead molecule, for the treatment of glioma, one of the most devastating and lethal brain cancers."

Orphan drug • Glioma

Hemispherian awarded NOK 16M grant from the Research Council of Norway (PRNewswire) - "Hemispherian AS...has been granted NOK 16 million by the Research Council of Norway. Hemispherian's proprietary GLIX compounds target a novel mechanism that is common to all cancers. The company's lead drug candidate, GLIX1, is in late-stage preclinical development for the treatment of glioblastoma, a highly aggressive and most common primary brain cancer, which continues to be one of the highest unmet needs in oncology. The funding awarded is earmarked for the development of Hemispherian's promising drug candidates aimed at treating platinum-resistant ovarian cancers, one of the most challenging gynecological malignancies."

Financing • Brain Cancer • CNS Tumor • Glioblastoma • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

First-in-class cancer therapeutics targeting the DNA Damage Response (SNO 2023) - "Hemispherian’s lead GLIX molecules, GLIX1 and GLIX5, show excellent efficacy in vivo in xenograft models, have a superior safety profile, are orally bioavailable and are blood brain barrier penetrant. GLIX efficacy against a panel of patient-derived cell lines representing a broad spectrum of pediatric and adult brain tumor diagnoses will be discussed. Taken together, these molecules have an exceptional profile for treating a broad range of cancers including cancers of the brain."

Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Pediatrics • Solid Tumor • TET2

Hemispherian raises the first tranche of a Series A to fund the development of its novel cancer therapeutics (PRNewswire) - "Hemispherian AS...is delighted to announce the closure of the first tranche of its series A1 financing round. The round raised NOK 30M (USD 2.9M). The proceeds will support the company's drug development activities, expand its preclinical pipeline and advance its lead therapeutic compounds towards clinical development.'This funding will support preclinical development of GLIX1 and GLIX5, the company's lead assets'."

Financing • Oncology