Abstract
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.
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 language | English |
---|---|
Title of host publication | Nuclear Medicine and Biology |
Subtitle of host publication | Abstract of the international symposium on radiopharmaceutical science iSRS 2022 |
Publisher | Elsevier |
Pages | S48-S49 |
Number of pages | 2 |
Volume | 108-109 |
Edition | May-June |
DOIs | |
State | Published - May 2022 |
Publication series
Name | Nuclear Medicine and Biology |
---|---|
Publisher | Elsevier |
Number | 3MT-7 |
Volume | 108-109 |
ISSN (Print) | 0969-8051 |
ISSN (Electronic) | 1872-9614 |