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rhPSMA-targeted agents

Development stage: Unknown
Lead developer: Blue Earth Therapeutics
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Intravenous

Overview

Radiohybrid PSMA-targeted agents (rhPSMA) represent a novel class of theranostic radiopharmaceuticals designed for the detection and treatment of prostate cancer. Developed by Blue Earth Diagnostics (a Bracco company) in collaboration with Scintomics GmbH and the Technical University of Munich, the rhPSMA platform utilizes a unique chemical structure that incorporates both a silicon-fluoride acceptor for fluorine-18 (18F) labeling and a chelator for radiometal complexation (such as lutetium-177 or actinium-225). This radiohybrid technology allows the same molecule to be used for both diagnostic PET imaging and targeted radioligand therapy. The lead diagnostic agent, flotufolastat F 18 (brand name POSLUMA), was FDA-approved in 2023 for PET imaging to detect and localize prostate cancer. Therapeutic variants, including 177Lu-rhPSMA-10.1 and 177Lu-rhPSMA-10.2, are currently in clinical development for the treatment of metastatic prostate cancer, targeting the prostate-specific membrane antigen (PSMA) expressed on the surface of cancer cells.

Brand names: POSLUMA
Other names: Radiohybrid PSMA-targeted agentsrhPSMAflotufolastat F 18

Targets

PSMA (Prostate-specific membrane antigen)

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