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177Lu-SibuDAB (also known as 177Lu-(S)-Ibu-DAB-PSMA) is an investigational, albumin-binding radioligand therapy developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Developed by the Paul Scherrer Institute (PSI) in collaboration with ITM Isotope Technologies Munich, the compound consists of a urea-based prostate-specific membrane antigen (PSMA)-targeting ligand conjugated to an (S)-ibuprofen moiety via a diaminobutyric acid (DAB) linker, radiolabeled with the beta-emitting isotope lutetium-177 (177Lu). The (S)-ibuprofen component acts as a weak-to-moderate albumin binder, which prolongs blood circulation and enhances tumor accumulation and retention compared to conventional radioligands like 177Lu-PSMA-617, while maintaining a favorable safety profile with reduced salivary gland uptake (preventing xerostomia) and manageable kidney clearance.
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