Past, Present and Future Radiotracer Techniques: Radiopharmaceuticals in Cancer Theranostics

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: 16 September 2024 | Viewed by 801

Special Issue Editors


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Guest Editor
Service Unit Radiopharmaceuticals and Pre-Clinical Studies, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 223, 69120 Heidelberg, Germany.
Interests: radiopharmaceutical chemistry; GMP production; quality control; automated synthesis; positron emission tomography (PET); diagnostic tracers

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Guest Editor
Research Group Molecular Biology of Systemic Radiotherapy, Research Program Imaging and Radiooncology, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 223, 69120 Heidelberg, Germany
Interests: theranostic radioligands; targeted radionuclide therapies; targeted alpha therapies; combination therapies; molecular imaging; pharmaceutical radiochemistry; coordination and bioinorganic chemistry; radionuclide production and separation methods
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Special Issue Information

Dear Colleagues, 

Following its tradition of publishing Special Issues on selected and highly interesting topics, the journal “Pharmaceuticals” is planning to launch a new Special Issue on the topic “Past, Present and Future Radiotracer Techniques: Radiopharmaceuticals in Cancer Theranostics”. 

More than five years ago, [177Lu]Lu-DOTA-TATE (Lutathera®) was approved by both the EMA and the FDA as the first radiopharmaceutical for Peptide Receptor Radionuclide Therapy (PRRT) of neuroendocrine tumors (NET) while joining its diagnostic counter-partner [68Ga]Ga-DOTA-TOC (SomaKit TOC®, TOCscan®). A further success story was represented by the approval of [177Lu]Lu-PSMA-617 (Pluvicto®) to various diagnostic counter-partners like [68Ga]Ga-PSMA-11 (Locametz®/Illuccix®) or [18F]DCFPyL (PYLARIFY®)  for the treatment of prostate cancer. Both radiotherapeutics are prime examples for the successful application of targeted radionuclide therapy (TRNT) in modern cancer management. 

However, the aforementioned theranostic pairs can only supply a limited number of cancer patients and, therefore, the development of new radiotracers and/or radiopharmaceuticals for various targets and cancer types is further ongoing. Such a developmental chain usually takes a couple of years and involves a variety of different steps from synthesis of the labeling precursor and reference compounds, optimization of radiolabeling and pre-clinical evaluations to the development of automated GMP compliant synthesis and quality control, first-in-human studies and various clinical trials. All these essential steps can be covered in the Special Issue. Areas of interest include, but are not limited to: 

  • Development and pre-clinical evaluation of diagnostic tracers and radiotherapeutic pharmaceuticals·       
  • Establishment and validation of GMP compliant synthesis and quality control·       
  • Translation into clinics: first-in-human studies, clinical trials

Please refer also to the list of keywords.

We cordially invite you to submit research as well as review articles to this Special Issue and look forward to reading your articles.

Dr. Ute Hennrich
Dr. Martina Benešová-Schäfer
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • diagnostic radiotracers
  • therapeutic radiopharmaceuticals
  • theranostics
  • radiolabeling techniques
  • GMP compliance
  • automated synthesis and quality control
  • pre-clinical studies
  • translation into clinics and first-in-human studies
  • clinical trials
  • regulatory approval

Published Papers (1 paper)

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Research

14 pages, 4551 KiB  
Article
Human ABC and SLC Transporters: The Culprit Responsible for Unspecific PSMA-617 Uptake?
by Harun Taş, Gábor Bakos, Ulrike Bauder-Wüst, Martin Schäfer, Yvonne Remde, Mareike Roscher and Martina Benešová-Schäfer
Pharmaceuticals 2024, 17(4), 513; https://doi.org/10.3390/ph17040513 - 16 Apr 2024
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Abstract
[177Lu]Lu-PSMA-617 has recently been successfully approved by the FDA, the MHRA, Health Canada and the EMA as Pluvicto®. However, salivary gland (SG) and kidney toxicities account for its main dose-limiting side-effects, while its corresponding uptake and retention mechanisms still [...] Read more.
[177Lu]Lu-PSMA-617 has recently been successfully approved by the FDA, the MHRA, Health Canada and the EMA as Pluvicto®. However, salivary gland (SG) and kidney toxicities account for its main dose-limiting side-effects, while its corresponding uptake and retention mechanisms still remain elusive. Recently, the presence of different ATP-binding cassette (ABC) transporters, such as human breast cancer resistance proteins (BCRP), multidrug resistance proteins (MDR1), multidrug-resistance-related proteins (MRP1, MRP4) and solute cassette (SLC) transporters, such as multidrug and toxin extrusion proteins (MATE1, MATE2-K), organic anion transporters (OAT1, OAT2v1, OAT3, OAT4) and peptide transporters (PEPT2), has been verified at different abundances in human SGs and kidneys. Therefore, our aim was to assess whether [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 are substrates of these ABC and SLC transporters. For in vitro studies, the novel isotopologue ([α,β-3H]Nal)Lu-PSMA-617 was used in cell lines or vesicles expressing the aforementioned human ABC and SLC transporters for inhibition and uptake studies, respectively. The corresponding probe substrates and reference inhibitors were used as controls. Our results indicate that [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 are neither inhibitors nor substrates of the examined transporters. Therefore, our results show that human ABC and SLC transporters play no central role in the uptake and retention of [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 in the SGs and kidneys nor in the observed toxicities. Full article
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