Development of radioligands with an albumin-binding moiety of 4-(P-Iodophenyl) butyric acid for theranostic applications.

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Citation abstract

The rapid clearance of imaging probes from blood circulation is beneficial for receptor imaging, as it minimizes non-target tissue exposure and improves tumor-to-background contrast. However, this rapid clearance can hinder radioligand therapy by limiting tumor uptake of radiolabeled compounds. An optimal blood half-life is crucial, as it enhances the uptake of radiolabeled compounds in targets, improving tumor uptake and retention of small molecule drugs, and thus therapeutic outcomes. To address this, strategies to extend blood half-life have been developed, with the addition of an albumin-binding moiety (ABM) being particularly effective. Among these, 4-(p-iodophenyl)butyric acid (IPBA) has emerged as a versatile ABM for radiopharmaceutical design. IPBA conjugation has successfully enhanced tissue distribution profiles across various cancer types. This review highlights recent progress in the design, radiosynthesis, and application of IPBA-based small molecular radioligands, providing insights for future clinical development of IPBA-based radiopharmaceuticals.