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In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological...
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In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research: New Advances

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

Deadline for manuscript submissions: 25 April 2025 | Viewed by 3098

Special Issue Editors

Dr. Haitao Wu

E-Mail Website
Guest Editor
Chemistry and Synthesis Center (formerly Imaging Probe Development Center), National Heart, Lung, and Blood Institutes, National Institutes of Health. Rockville, MD 20850, USA
Interests: molecular imaging; imaging probe development; nanomedicine
Dr. Noriko Sato

E-Mail Website
Guest Editor
Molecular Imaging Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health. Bethesda, MD 20892, USA
Interests: molecular imaging; cell tracking; tumor microenvironment; tumor immunology

Special Issue Information

Dear Colleagues,

Nuclear medicine has played a crucial role in the rapid advancement of non-invasive molecular imaging in drug development and pharmacological research. Nuclear molecular imaging enables the visualization, characterization, and quantification of biological events at the molecular level in live subjects, and provides invaluable real-time insights into disease mechanisms and mechanisms of drug action. A quantitative assessment of drug delivery to the target as well as off-target organs or tissues is important for toxicity evaluation, and thus, nuclear molecular imaging has accelerated the advancement of more efficient therapies and personalized medicine. Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) have been the mainstream imaging modalities in recent years. The combination of computed tomography (CT) and magnetic resonance imaging (MRI) provides anatomical information for accurate diagnosis and has become a critical component of imaging for drug development. In addition to various efforts to facilitate this research, the discovery and development of more targeted radiotracers remain an increasingly complex task. This new Special Issue aims to cover recent and promising developments in nuclear molecular imaging for pharmacological studies in animal models and humans. This issue welcomes reviews and original research articles primarily covering the following topics:

  • Radiotracer development for imaging and diagnosis, including in vitro targeting validation;
  • Radiolabeling techniques, including radiosynthesis, automation, and formulation optimization;
  • Radiotracer in vivo biodistribution, targeting, and pharmacological and toxicity evaluation;
  • Bench-to-bedside translational research of radiotracers and imaging techniques, including clinical trials and disease mechanism investigation.

Dr. Haitao Wu
Dr. Noriko Sato
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

  • in vivo nuclear imaging
  • biomarker imaging
  • molecular imaging
  • PET
  • SPECT
  • pharmacokinetics
  • personalized medicine
  • drug development
  • molecular pathway

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Published Papers (3 papers)

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Research

19 pages, 8785 KiB  
Article
Novel 177Lu-Labeled [Thz14]Bombesin(6–14) Derivatives with Low Pancreas Accumulation for Targeting Gastrin-Releasing Peptide Receptor-Expressing Cancer
by Lei Wang, Devon E. Chapple, Hsiou-Ting Kuo, Sara Kurkowska, Ryan P. Wilson, Wing Sum Lau, Pauline Ng, Carlos Uribe, François Bénard and Kuo-Shyan Lin
Pharmaceuticals 2025, 18(4), 449; https://doi.org/10.3390/ph18040449 - 23 Mar 2025
Viewed by 237
Abstract
Background/Objectives: Gastrin-releasing peptide receptor is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake of reported GRPR-targeted radioligands limits their clinical applications. Our group previously reported one 68Ga-labeled GRPR antagonist, [68Ga]Ga-TacsBOMB5 (68Ga-DOTA-Pip-[D-Phe6,NMe-Gly [...] Read more.
Background/Objectives: Gastrin-releasing peptide receptor is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake of reported GRPR-targeted radioligands limits their clinical applications. Our group previously reported one 68Ga-labeled GRPR antagonist, [68Ga]Ga-TacsBOMB5 (68Ga-DOTA-Pip-[D-Phe6,NMe-Gly11,Leu13ψThz14]Bombesin(6–14)), and two agonists, [68Ga]Ga-LW01110 (68Ga-DOTA-Pip-[D-Phe6,Tle10,NMe-His12,Thz14]Bombesin(6–14)) and [68Ga]Ga-LW01142 (68Ga-DOTA-Pip-[D-Phe6,His7,Tle10,NMe-His12,Thz14]Bombesin(6–14)) showing minimal pancreas uptake. Thus, in this study, we prepared their 177Lu-labeled analogs, evaluated their therapeutic potentials, and compared them with the clinically evaluated [177Lu]Lu-AMBA. Methods: GRPR binding affinities were determined by in vitro competition binding assay using PC-3 prostate cancer cells. Longitudinal SPECT/CT imaging and ex vivo biodistribution studies were conducted in PC-3 tumor-bearing mice. Dosimetry data were calculated from the biodistribution results. Results: The Ki(GRPR) values of Lu-TacsBOMB5, Lu-LW01110, Lu-LW01142, and Lu-AMBA were 12.6 ± 1.02, 3.07 ± 0.15, 2.37 ± 0.28, and 0.33 ± 0.16 nM, respectively. SPECT/CT images and biodistribution results demonstrated good tumor accumulation of [177Lu]Lu-TacsBOMB5, [177Lu]Lu-LW01110, and [177Lu]Lu-LW01142 at early time points with rapid clearance over time. The pancreas uptake of all three [Thz14]Bombesin(6–14)-derived ligands was significantly lower than that of [177Lu]Lu-AMBA at all time points. The calculated absorbed doses of [177Lu]Lu-TacsBOMB5, [177Lu]Lu-LW01110, and [177Lu]Lu-LW01142 in PC-3 tumor xenografts were 87.1, 312, and 312 mGy/MBq, respectively, higher than that of [177Lu]Lu-AMBA (79.1 mGy/MBq), but lower than that of the previously reported [177Lu]Lu-RM2 (429 mGy/MBq). Conclusions: Our data suggest that [177Lu]Lu-TacsBOMB5 and [177Lu]Lu-LW01142 reduce radiation exposure to the pancreas. However, further optimizations are needed for both radioligands to prolong their tumor retention and enhance treatment efficacy. Full article
(This article belongs to the Special Issue In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research: New Advances)
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22 pages, 9584 KiB  
Article
Synthesis and Evaluation of 68Ga- and 177Lu-Labeled [diF-Pro14]Bombesin(6−14) Analogs for Detection and Radioligand Therapy of Gastrin-Releasing Peptide Receptor-Expressing Cancer
by Lei Wang, Chao-Cheng Chen, Devon Chapple, Antonio A. W. L. Wong, Sara Kurkowska, Wing Sum Lau, Carlos F. Uribe, François Bénard and Kuo-Shyan Lin
Pharmaceuticals 2025, 18(2), 234; https://doi.org/10.3390/ph18020234 - 8 Feb 2025
Viewed by 860
Abstract
Background/Objectives: Overexpressed in various solid tumors, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake of the current clinically evaluated GRPR-targeted radiopharmaceuticals limits their applications. In this study, we replaced the Pro14 [...] Read more.
Background/Objectives: Overexpressed in various solid tumors, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake of the current clinically evaluated GRPR-targeted radiopharmaceuticals limits their applications. In this study, we replaced the Pro14 residue in our previously reported GRPR-targeted LW02056 and ProBOMB5 with 4,4-difluoroproline (diF-Pro) to obtain an agonist LW02060 (DOTA-Pip-[D-Phe6,Tle10,NMe-His12,diF-Pro14]Bombesin(6–14)) and an antagonist LW02080 (DOTA-Pip-[D-Phe6,NMe-Gly11,Leu13(ψ)diF-Pro14]Bombesin(6–14)), respectively. Methods/Results: The binding affinities (Ki) of Ga-LW02060, Ga-LW02080, Lu-LW02060, and Lu-LW02080 were measured by in vitro competition binding assays using PC-3 cells and were found to be 5.57 ± 2.47, 21.7 ± 6.69, 8.00 ± 2.61, and 32.1 ± 8.14 nM, respectively. The 68Ga- and 177Lu-labeled ligands were obtained in 36–75% decay-corrected radiochemical yields with >95% radiochemical purity. PET imaging, SPECT imaging, and ex vivo biodistribution studies were conducted in PC-3 tumor-bearing mice. Both [68Ga]Ga-LW02060 and [68Ga]Ga-LW02080 enabled clear tumor visualization in PET images at 1 h post-injection (pi). Tumor uptake values of [68Ga]Ga-LW02060 and [68Ga]Ga-LW02080 at 1 h pi were 16.8 ± 2.70 and 7.36 ± 1.33 %ID/g, respectively, while their pancreas uptake values were 3.12 ± 0.89 and 0.38 ± 0.04 %ID/g, respectively. Compared to [177Lu]Lu-LW02080, [177Lu]Lu-LW02060 showed higher tumor uptake at all time points (1, 4, 24, 72, and 120 h pi). However, fast tumor clearance was observed for both [177Lu]Lu-LW02060 and [177Lu]Lu-LW02080. Conclusions: Our data demonstrate that [68Ga]Ga-LW02060 is promising for clinical translation for the detection of GRPR-expressing tumor lesions. However, further optimizations are needed for [177Lu]Lu-LW02060 and [177Lu]Lu-LW02080 to prolong tumor retention for therapeutic applications. Full article
(This article belongs to the Special Issue In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research: New Advances)
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14 pages, 1964 KiB  
Article
Assessment of Radiolabelled Derivatives of R954 for Detection of Bradykinin B1 Receptor in Cancer Cells: Studies on Glioblastoma Xenografts in Mice
by Miho Shukuri, Satoru Onoe, Tsubasa Karube, Risa Mokudai, Hayate Wakui, Haruka Asano, Shin Murai and Hiromichi Akizawa
Pharmaceuticals 2024, 17(7), 902; https://doi.org/10.3390/ph17070902 - 7 Jul 2024
Viewed by 1157
Abstract
Bradykinin B1 receptor (B1R) has garnered attention as a cancer therapeutic and diagnostic target. Several reports on radiolabelled derivatives of B1R antagonists have shown favourable properties as imaging agents in cells highly expressing hB1R following transfection. In the present study, we assessed whether [...] Read more.
Bradykinin B1 receptor (B1R) has garnered attention as a cancer therapeutic and diagnostic target. Several reports on radiolabelled derivatives of B1R antagonists have shown favourable properties as imaging agents in cells highly expressing hB1R following transfection. In the present study, we assessed whether radiolabelled probes can detect B1R endogenously expressed in cancer cells. To this end, we evaluated 111In-labelled derivatives of a B1R antagonist ([111In]In-DOTA-Ahx-R954) using glioblastoma cell lines (U87MG and U251MG) with different B1R expression levels. Cellular uptake studies showed that the specific accumulation of [111In]In-DOTA-Ahx-R954 in U87MG was higher than that in U251MG, which correlated with B1R expression levels. Tissue distribution in U87MG-bearing mice revealed approximately 2-fold higher radioactivity in tumours than in the muscle in the contralateral leg. The specific accumulation of [111In]In-DOTA-Ahx-R954 in the tumour was demonstrated by the reduction in the tumour-to-plasma ratios in nonlabelled R954-treated mice. Moreover, ex vivo autoradiographic images revealed that the intratumoural distribution of [111In]In-DOTA-Ahx-R954 correlated with the localisation of B1R-expressing glioblastoma cells. In conclusion, we demonstrated that [111In]In-DOTA-Ahx-R954 radioactivity correlated with B1R expression in glioblastoma cells, indicating that radiolabelled derivatives of the B1R antagonist could serve as promising tools for elucidating the involvement of B1R in cancer. Full article
(This article belongs to the Special Issue In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research: New Advances)
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