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BAY 3563254

Development stage
Phase 1
Lead developer
Bayer
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

BAY 3563254 (also known as 225Ac-PSMA-Trillium) is an investigational targeted alpha therapy developed by Bayer for the treatment of advanced metastatic castration-resistant prostate cancer (mCRPC). It consists of a novel small molecule that targets prostate-specific membrane antigen (PSMA), conjugated to the alpha-emitting radioisotope actinium-225. Upon intravenous administration, BAY 3563254 binds specifically to PSMA-expressing tumor cells, delivering cytotoxic alpha radiation directly to these cells and thereby inducing tumor cell death while aiming to minimize damage to normal tissues. The drug features a customized albumin-binding moiety designed to enhance therapeutic efficacy and reduce off-target toxicity, particularly in organs such as salivary glands. As of mid-2025, it is being evaluated in first-in-human Phase I clinical trials for safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with mCRPC[1][2][5][6].

Brand names
BAY3563254BAY-3563254BAY 3563254225Ac-PSMA-Trillium
Other names
actinium Ac 225-PSMA-trillium
02

Targets

PSMA (Prostate-specific membrane antigen)

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