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A radiohybrid molecule has two places to attach a radioactive atom. The same molecule can carry fluorine-18 for a PET scan or a metal such as lutetium-177 for treatment, so the scan shows exactly where the treatment version will go.
Radiohybrid ligands were introduced by Wurzer, Wester and colleagues at the Technical University of Munich (Journal of Nuclear Medicine 2020). Each molecule carries both a silicon-fluoride acceptor, labelled with fluorine-18 by isotopic exchange, and a metal chelator, so one scaffold can be made as an 18F PET tracer, a 68Ga PET tracer or a therapeutic radiometal conjugate with the same chemistry. Their rhPSMA inhibitors showed targeting equal to or better than the established 18F PSMA tracers in preclinical studies, with labelling completed in under 20 minutes at laboratory scale.
The first approved product is flotufolastat F-18 (rhPSMA-7.3, Posluma), a PSMA PET agent approved in the United States in 2023. On the treatment side, lutetium-177 rhPSMA-10.1 is in clinical trials in metastatic prostate cancer, developed by Blue Earth Therapeutics, which Bracco set up for radiohybrid therapy.
A targeting ligand carries a silicon-fluoride acceptor for 18F labelling and a chelator for a radiometal; the radiolabel sits on one site while the other is filled with the stable isotope or metal, so diagnostic and therapeutic versions are chemically identical.
Flotufolastat is a third PSMA PET tracer, with a radiohybrid chemistry designed to be reused for therapy.
Query for this technology: (TITLE:"Radiohybrid theranostics" OR ABSTRACT:"Radiohybrid theranostics" OR TITLE:"rhPSMA" OR ABSTRACT:"rhPSMA" OR TITLE:"radiohybrid ligands" OR ABSTRACT:"radiohybrid ligands" OR TITLE:"radiohybrid PSMA" OR ABSTRACT:"radiohybrid PSMA") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Radiohybrid theranostics (rhPSMA), not a curated reading list.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
Shares PSMA, PSMA PET, Radioligand therapy (beta emitters), Prostate cancer.
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