Bayer Initiates Phase I Clinical Trial of GPC3-Targeted Radiopharmaceutical BAY 3547926 for Hepatocellular Carcinoma

Apr 30, 2025 09:33 CST Updated 09:33

Bayer

Pharmaceutical Product R&D Developer

｜Edited by the Content Team of Zhong Peptide Biochemical

April 202529DayBayer announced the initiation of a Phase I clinical trial evaluating the targeted alpha radiopharmaceutical 225Ac-GPC3 (BAY 3547926) in tumors expressing Glypican-3 (GPC3) in patients with advanced hepatocellular carcinoma (HCC). The oncofetal protein GPC3 is a membrane-bound proteoglycan overexpressed in 70-75% of HCC lesions, making it an attractive target for targeted radionuclide therapy. This first-in-human, dose-escalation study (NCT06764316) will assess the safety, tolerability, and preliminary efficacy of BAY 3547926 as monotherapy and in combination therapy in patients with advanced HCC. The study plans to enroll 148 patients.

Targeted Alpha Therapy (TAT) has the potential to address highly unmet medical needs across various cancer types. Bayer's growing TAT portfolio combines alpha particle-emitting radionuclides with different targeting moieties. 225Ac-GPC3 is the third TAT project to enter clinical development and Bayer’s first investigational targeted radiopharmaceutical in the HCC space. This newly disclosed targeted alpha conjugate joins 225Ac-Pelgifatamab and 225Ac-PSMA-Trillium, both of which are currently in Phase I clinical trials in patients with advanced metastatic castration-resistant prostate cancer.

On April 28, 2025, Bayer presented 225Ac-GPC3 at the American Association for Cancer Research (AACR) Annual Meeting's "New Drugs on the Horizon" session, showcasing its preclinical profile, including low uptake and rapid clearance in normal organs, as well as tumor regression induction in in vivo models. The recognition at this special symposium underscores the company’s commitment to its precision oncology development portfolio.

BAY 3547926 is an investigational targeted alpha radiopharmaceutical being developed for the treatment of tumors expressing Glypican-3 (GPC3) in patients with advanced hepatocellular carcinoma (HCC). It consists of a high-affinity antibody targeting GPC3 conjugated with the radioactive isotope actinium-225 (225Ac). 225Ac-GPC3 delivers high-energy alpha particles to GPC3-expressing cancer cells, with the potential to induce DNA double-strand breaks, reduce cancer cell viability, and thereby potentially generate anti-tumor activity.

AboutBayer

Bayer is a life sciences company with over 150 years of history, possessing core competencies in healthcare and agriculture. Through innovative products, Bayer is always committed to finding solutions to address some of the major challenges facing the world today.

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1.Bayer