Development of PSMA-targeted vectors containing an albumin binder and a cleavable linker

Erika Murce, Stephen Ahenkorah, Erik de Blois, Frederik Cleeren, Marion de Jong, Yann Seimbille

    Research outputpeer-review


    Peptide receptor radionuclide therapy (PRRT) is a promising strategy to treat several types of cancer. Particular attention was devoted to the development of vectors for the treatment of prostate cancer over the last two decades. The most successful candidates are currently being tested in clinical trials. Addition of an albuminbinder to the targeting vector can enhance the dose delivered to
    tumors, and substantially to some healthy organs. A common drawback
    of this therapy is off-target side-effects. Elevated renal uptake is
    commonly observed with compounds targeting the prostate specific
    membrane antigen (PSMA), limiting the dose of radiopharmaceutical
    administered. Hereby, we aimed to apply a cleavable linker strategy, where amino-acid sequences are specifically cleaved by renal brush border membrane (RBBM) enzymes to decrease the absorbed dose delivered to the kidneys. By employing both the albumin-binder and cleavable linker strategies, we advanced the development of optimized constructs with increased therapeutic efficacy and safety profile.
    Original languageEnglish
    Title of host publicationNuclear Medicine and Biology
    Subtitle of host publicationAbstract of the international symposium on radiopharmaceutical science iSRS 2022
    Number of pages2
    StatePublished - May 2022

    Publication series

    NameNuclear Medicine and Biology
    ISSN (Print)0969-8051
    ISSN (Electronic)1872-9614

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