Towards Personalized Treatment of Prostate Cancer: PSMA I&T, a Promising Prostate-Specific Membrane Antigen-Targeted Theranostic Agent

@article{Chatalic2016TowardsPT,
  title={Towards Personalized Treatment of Prostate Cancer: PSMA I\&T, a Promising Prostate-Specific Membrane Antigen-Targeted Theranostic Agent},
  author={Kristell L.S. Chatalic and Sandra Heskamp and Mark W. Konijnenberg and Janneke D. M. Molkenboer-Kuenen and Gerben M. Franssen and Marian C. Clahsen‐van Groningen and Margret Schottelius and Hans-J{\"u}rgen Wester and Wytske M. van Weerden and Otto C Boerman and Marion de Jong},
  journal={Theranostics},
  year={2016},
  volume={6},
  pages={849 - 861}
}
Prostate-specific membrane antigen (PSMA) is a well-established target for nuclear imaging and therapy of prostate cancer (PCa. [...] Key Result (111)In-PSMA I&T showed dose-dependent uptake in PSMA-expressing tumors, kidneys, spleen, adrenals, lungs and salivary glands. Coadministration of 2-(phosphonomethyl)pentane-1,5-dioic acid (2-PMPA) efficiently reduced PSMA-mediated renal uptake of (111)In-PSMA I&T, with the highest tumor/kidney radioactivity ratios being obtained using a dose of 50 nmol 2-PMPA.Expand
Extensive preclinical evaluation of lutetium-177-labeled PSMA-specific tracers for prostate cancer radionuclide therapy
TLDR
Based on the preclinical evaluation, [177Lu]Lu-PSMA-617 is the best performing tracer to be taken further into clinical evaluation for PSMA-targeted radiotherapeutic development although with careful evaluation of the tracer binding to PSma-expressing organs.
Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer
TLDR
In this review, both the recent preclinical and clinical advances made in the development of PSMA-TAT are summarized, as well as the availability of therapeutic alpha-emitting radionuclides, theDevelopment of small molecules and antibodies targeting PSMA, and the potentials, limitations, and future perspectives.
213Bi-Labeled Prostate-Specific Membrane Antigen-Targeting Agents Induce DNA Double-Strand Breaks in Prostate Cancer Xenografts.
TLDR
213Bi-PSMA I&T and 213Bi-JVZ-008 showed efficient and rapid tumor targeting and produced DSBs in PSMA-expressing LNCaP cells and xenografts in PCa therapy.
Targeted α-therapy of prostate cancer using radiolabeled PSMA inhibitors: a game changer in nuclear medicine.
TLDR
An overview of the successes and challenges currently faced in TAT of mCRPCa using radiolabeled PSMA inhibitors is presented, and it is expected that this therapeutic modality will play a pivotal role in advanced stage PCa management in the foreseeable future.
The Future of PSMA-Targeted Radionuclide Therapy: An Overview of Recent Preclinical Research
TLDR
This review will give an overview of the recent preclinical research projects regarding PCa-TRT using PSMA-specific radiotracers to give an indication of where the PSMA -TRT research movement is going and what the authors can expect in future clinical trials.
Single Low-Dose Injection of Evans Blue Modified PSMA-617 Radioligand Therapy Eliminates Prostate-Specific Membrane Antigen Positive Tumors.
TLDR
The construct described here, EB-PSMA-617, may improve the radiotherapeutic efficacy for patients with PSMA-positive tumors by reducing both the amount of activity needed for therapy as well as the frequency of administration, as compared to PSma-617.
Photosensitizer-based multimodal PSMA-targeting ligands for intraoperative detection of prostate cancer
TLDR
A novel PSMA-targeting ligand, optimized for multimodal image-guided PCa surgery combined with targeted photodynamic therapy of PCa lesions is developed.
Dual-Target Binding Ligands with Modulated Pharmacokinetics for Endoradiotherapy of Prostate Cancer
TLDR
RPS-027 shows dual targeting to PSMA and albumin, resulting in a high tumor uptake, highly favorable tissue distribution, and promising therapeutic profile in a preclinical model of prostate cancer.
177 Lu-Labeled Phosphoramidate-Based PSMA Inhibitors : The Effect of an Albumin Binder on Biodistribution and Therapeutic Efficacy in Prostate Tumor-Bearing Mice
Prostate-specific membrane antigen (PSMA) continues to be an active biomarker for small-molecule PSMA-targeted imaging and therapeutic agents for prostate cancer and various non-prostatic tumors that
Image-Guided Surgery: Are We Getting the Most Out of Small-Molecule Prostate-Specific-Membrane-Antigen-Targeted Tracers?
TLDR
The focus is on the chemical aspects of PSMA, e.g., imaging label, spacer moiety, and targeting vector and their impact on in vitro and in vivo tracer characteristics (e.g, affinity, tumor uptake, and clearance pattern).
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