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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Optimizing uPAR-targeting radiopeptides for improved tissue distribution: progress towards radionuclide therapy.

Christian Vaccarin1, Darja Beyer1, Jerome V Schmid1

  • 1Center for Radiopharmaceutical Sciences, PSI Center for Life Sciences, Villigen-PSI, 5232, Switzerland.

European Journal of Nuclear Medicine and Molecular Imaging
|October 27, 2025
PubMed
Summary

New radiopeptides targeting urokinase-type plasminogen activator receptor (uPAR) were developed with enhanced albumin binding. [177Lu]Lu-uPAR-11 demonstrated superior tissue distribution and xenograft accumulation, making it a promising candidate for clinical translation.

Keywords:
p-tolyl entityAlbumin binderDOTA-AE105Lutetium-177SPECT imagingUrokinase-type plasminogen activator receptoruPAR

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Area of Science:

  • Nuclear medicine
  • Radiopharmaceutical chemistry
  • Molecular imaging

Background:

  • The urokinase-type plasminogen activator receptor (uPAR) is a promising target for cancer imaging and therapy.
  • Improving the pharmacokinetic profiles of targeting agents is crucial for effective delivery to tumor sites.
  • Albumin-binding moieties can enhance the circulation time and tissue distribution of radiopeptides.

Purpose of the Study:

  • To develop novel radiopeptides targeting uPAR, incorporating an albumin-binding moiety to optimize tissue distribution.
  • To synthesize and characterize a series of uPAR-targeting radiopeptides with varying linker and chelator designs.
  • To evaluate the in vitro and in vivo performance of these novel radiopeptides compared to a non-albumin-binding control.

Main Methods:

  • Synthesis of AE105 nonapeptide derivatives with p-tolyl-based albumin binders, variable linkers, and chelators.
  • Radiolabeling with Lutetium-177 ([177Lu]).
  • In vitro assessment of stability, albumin-binding affinity, and uPAR-binding affinity using HEK-uPAR cells.
  • In vivo evaluation through biodistribution and SPECT/CT imaging in HEK-uPAR xenografted nude mice.

Main Results:

  • Radiopeptides exhibited 11-155-fold higher albumin-binding affinity compared to [177Lu]Lu-DOTA-AE105.
  • uPAR-binding affinity was comparable to the control, with KD values in the range of 31–42 nM.
  • Xenograft accumulation was significantly higher (7-18 fold) for the novel radiopeptides (6.0-16% IA/g at 4 h p.i.).
  • PEG linkers enhanced xenograft accumulation, while alkane linkers resulted in high blood retention.
  • DOTAGA chelator led to unfavorable kidney retention.

Conclusions:

  • [177Lu]Lu-uPAR-11, featuring PEG spacers, demonstrated the most favorable profile for clinical translation.
  • This radiopeptide exhibited enhanced uPAR targeting and improved tissue distribution.
  • Future research will investigate the therapeutic potential of [177Lu]Lu-uPAR-11 in preclinical tumor models.