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Pharmaceutics
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Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy
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Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Clinical Pharmaceutics".

Deadline for manuscript submissions: closed (20 March 2025) | Viewed by 17202

Special Issue Editors

Dr. Kuan Hu

E-Mail Website
Guest Editor
1. National Institutes for Quantum Science and Technology, Chiba, Japan
2. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Interests: radiopharmaceuticals; peptide; PET imaging; radiotheranostics; cancer management
Special Issues, Collections and Topics in MDPI journals
Dr. Volkan Tekin

E-Mail Website
Guest Editor
Department of Radiology, University of Alabama at Birmingham, Birmingham, AL 35294, USA
Interests: cancer research; radiopharmaceuticals; cell culture; nanoparticles
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Radiopharmaceutical therapy targets tumor- or nontumor-associated tissues to deliver a single or pair of radioactive atoms based on the location and/or the properties of the tissues. The variety of the ligands, such as protein, peptide, antibody, and nucleic acid, to be selected depending on the radioactive atom and the target tissue facilitates the targeting of many tissues, while the variety of radioactive atoms in terms of energy type, density, and the half-life ensures the destruction of the target tissues and effective treatment of many diseases with radiotherapy. Although the focus of radiopharmaceutical therapy is cancer treatment, it is known that it has a potential for use in the treatment of other diseases.

This Special Issue serves to highlight the potential of ligands and radioactive atoms to treat diseases by novel approaches or combining the current methods with a synergy of aspects. We invite authors to submit articles which focus on discovering the pathways of radiopharmaceuticals for disease therapy for this Special Issue.

Dr. Kuan Hu
Dr. Volkan Tekin
Guest Editors

Manuscript Submission Information

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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. Pharmaceutics 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

  • radiopharmaceutical
  • radionuclide therapy
  • radiotherapy
  • cancer treatment
  • imaging-guided therapy
  • radiotheranostics
  • nontumor diseases
  • alpha radiotherapy
  • disease treatment
  • therapy

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Published Papers (9 papers)

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26 pages, 7920 KiB  
Article
Polyacrylic Acid-Coated LaB6 Nanoparticles as Efficient Sensitizers for Binary Proton Therapy
by Mariya S. Ryabtseva, Marina V. Filimonova, Alexander S. Filimonov, Olga V. Soldatova, Anna A. Shitova, Vitaly A. Rybachuk, Irina K. Volkova, Kirill A. Nikolaev, Alexander O. Kosachenko, Sergei N. Koryakin, Dmitry S. Petrunya, Polina A. Kotelnikova, Alexander E. Shemyakov, Danil D. Kolmanovich, Anton L. Popov, Gleb V. Tikhonowski, Anton A. Popov, Anna A. Timakova, Andrey V. Kolobov, Sergey M. Deyev, Andrei V. Kabashin and Irina N. Zavestovskayaadd Show full author list remove Hide full author list
Pharmaceutics 2025, 17(4), 515; https://doi.org/10.3390/pharmaceutics17040515 - 15 Apr 2025
Viewed by 445
Abstract
Proton beam therapy (PBT) is a rapidly advancing modality of hadron therapy. The primary advantage of proton therapy lies in a unique depth-dose distribution characterized by the Bragg peak, which enables a highly targeted irradiation of the area limited to the tumor, while [...] Read more.
Proton beam therapy (PBT) is a rapidly advancing modality of hadron therapy. The primary advantage of proton therapy lies in a unique depth-dose distribution characterized by the Bragg peak, which enables a highly targeted irradiation of the area limited to the tumor, while minimizing the impact on healthy tissues. However, a broader clinical adoption of the ion beam therapy is limited by both economic and radiobiological constraints. One of the possible ways to increase the relative biological effectiveness (RBE) of proton therapy involves the use of radiosensitizers. Background/Objectives: In this work, we investigated the efficacy of using colloidal solutions of lanthanum hexaboride (LaB6) nanoparticles (NPs) coated with polyacrylic acid (PAA) as sensitizers to increase the antitumor biological effectiveness of proton irradiation. This material has not yet been studied extensively so far, despite its promising physical and chemical properties and several reports on its biocompatibility. Methods: LaB6 NPs were synthesized by femtosecond pulsed laser ablation, functionalized with PAA and characterized. The safety of NPs was evaluated in vitro using a Live/Dead assay on cell cultures: EMT6/P, BT-474, and in vivo in Balb/c mice after intravenous (i.v.) administration. The efficacy of binary proton therapy was evaluated in vitro on cell cultures: EMT6/P, BT-474, and in vivo in the model of human ductal carcinoma of the mammary gland BT-474 in female Nu/j mice after intratumoral (i.t.) administration at a dose of 2.0 mg/mouse and local proton irradiation (fractional exposure of 31 Gy + 15 Gy). The biodistribution of LaB6-PAA NPs in the animal body was also evaluated. Results: Significant enhancement in cancer cell death following proton beam irradiation was demonstrated in vitro on EMT6/P, BT-474 cell lines. Although the antitumor efficacy observed in vivo was comparatively lower—likely due to the high sensitivity of the BT-474 xenografts—both proton monotherapy and binary treatment were well tolerated. Conclusions: LaB6-PAA NPs show promise as efficient sensitizers capable of enhancing the biological efficacy of proton therapy, offering a potential path forward for improving therapeutic outcomes. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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18 pages, 2142 KiB  
Article
Towards DFO*12—Preliminary Results of a New Chelator for the Complexation of Actinium-225
by Irene V. J. Feiner, Dennis Svatunek, Martin Pressler, Tori Demuth, Xabier Guarrochena, Johannes H. Sterba, Susanne Dorudi, Clemens Pichler, Christoph Denk and Thomas L. Mindt
Pharmaceutics 2025, 17(3), 320; https://doi.org/10.3390/pharmaceutics17030320 - 1 Mar 2025
Viewed by 1025
Abstract
Background: Actinium-225 (225Ac) has gained interest in nuclear medicine for use in targeted alpha therapy (TAT) for the treatment of cancer. However, the number of suitable chelators for the stable complexation of 225Ac3+ is limited. The promising physical [...] Read more.
Background: Actinium-225 (225Ac) has gained interest in nuclear medicine for use in targeted alpha therapy (TAT) for the treatment of cancer. However, the number of suitable chelators for the stable complexation of 225Ac3+ is limited. The promising physical properties of 225Ac result in an increased demand for the radioisotope that is not matched by its current supply. To expand the possibilities for the development of 225Ac-based TAT therapeutics, a new hydroxamate-based chelator, DFO*12, is described. We report the DFT-guided design of dodecadentate DFO*12 and an efficient and convenient automated solid-phase synthesis for its preparation. To address the limited availability of 225Ac, a small-scale 229Th/225Ac generator was constructed in-house to provide [225Ac]AcCl3 for research. Methods: DFT calculations were performed in ORCA 5.0.1 using the BP86 functional with empirical dispersion correction D3 and Becke–Johnson damping (D3BJ). The monomer synthesis over three steps enabled the solid-phase synthesis of DFO*12. The small-scale 229Th/225Ac generator was realized by extracting 229Th from aged 233U material. Radiolabeling of DFO*12 with 225Ac was performed in 1 M TRIS pH 8.5 or 1.5 M NaOAc pH 4.5 for 30 min at 37 °C. Results: DFT calculations directed the design of a dodecadentate chelator. The automated synthesis of the chelator DFO*12 and the development of a small-scale 229Th/225Ac generator allowed for the radiolabeling of DFO*12 with 225Ac quantitatively at 37 °C within 30 min. The complex [225Ac]Ac-DFO*12 indicated good stability in different media for 20 h. Conclusions: The novel hydroxamate-based dodecadentate chelator DFO*12, together with the developed 229Th/225Ac generator, provide new opportunities for 225Ac research for future radiopharmaceutical development and applications in TAT. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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12 pages, 2735 KiB  
Article
PET Imaging of CD206 Macrophages in Bleomycin-Induced Lung Injury Mouse Model
by Volkan Tekin, Yujun Zhang, Clayton Yates, Jesse Jaynes, Henry Lopez, Charles Garvin, Benjamin M. Larimer and Suzanne E. Lapi
Pharmaceutics 2025, 17(2), 253; https://doi.org/10.3390/pharmaceutics17020253 - 14 Feb 2025
Viewed by 758
Abstract
Background/Objectives: The identification of inflammatory mediators and the involvement of CD206 macrophages in anti-inflammatory responses, along with the synthesis of fibrotic mediators, are crucial for the diagnosis and treatment of Idiopathic Pulmonary Fibrosis (IPF). Methods: In this study, the assessment of [...] Read more.
Background/Objectives: The identification of inflammatory mediators and the involvement of CD206 macrophages in anti-inflammatory responses, along with the synthesis of fibrotic mediators, are crucial for the diagnosis and treatment of Idiopathic Pulmonary Fibrosis (IPF). Methods: In this study, the assessment of 68Ga-labeled linear and cyclic forms of the RP832c peptide, which demonstrate a specific affinity for CD206 macrophages, was performed to evaluate efficacy for CD206 imaging through PET/CT, biodistribution studies, and CD206 staining in a bleomycin-induced lung injury mouse model (BLM). This model serves as a representative framework for inflammation and fibrosis. Results: The findings reveal significant peak PET/CT signals (SUV means), ID/gram values, and CD206 staining scores in lung tissues at one week post bleomycin instillation, likely due to the heightened expression of CD206 in the bleomycin-induced lung injury model. In contrast, the healthy mice exhibited no detectable CD206 staining, lower PET signals, and reduced radiopharmaceutical accumulation in lung tissues at the same timepoint. Conclusions: These findings suggest that both linear and cyclic [68Ga]Ga-RP832c may function as promising PET imaging agents for CD206 macrophages, and thereby a strategy to non-invasively explore the role of macrophages during fibrogenesis. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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15 pages, 5375 KiB  
Article
Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy
by Yunjie Xu, Pinghui Li, Shiran Sun, Yulin Chen, Lixia Feng, Dawei Jiang, Chidan Wan, Jianbo Li and Xiong Cai
Pharmaceutics 2025, 17(1), 90; https://doi.org/10.3390/pharmaceutics17010090 - 12 Jan 2025
Viewed by 1096
Abstract
Background: Acute liver injury (ALI) is a prevalent and potentially lethal condition globally, where pharmacotherapy plays a vital role. However, challenges such as rapid drug excretion and insufficient concentration at hepatic lesions often impede the treatment’s effectiveness. Methods: We successfully prepared glycyrrhizinate monoammonium [...] Read more.
Background: Acute liver injury (ALI) is a prevalent and potentially lethal condition globally, where pharmacotherapy plays a vital role. However, challenges such as rapid drug excretion and insufficient concentration at hepatic lesions often impede the treatment’s effectiveness. Methods: We successfully prepared glycyrrhizinate monoammonium cysteine (GMC)-loaded lipid nanoparticles (LNPs) using high-pressure homogenization. The characterization and safety of the LNPs were measured using electrophoretic light scattering (ELS), transmission electron microscopy (TEM), dynamic light scattering (DLS), cytotoxicity assays, and hemolysis tests. The distribution of LNPs in mice was explored using fluorescence labeling methods. The encapsulation efficiency of LNP-GMC was detected using High-Performance Liquid Chromatography (HPLC), and its slow-release effect on GMC was assessed through dialysis. The therapeutic effects of LNP-GMC and pure GMC on the ALI model were evaluated using fibroblast activation protein inhibitor (FAPI) PET imaging, blood biochemical indicators, and liver pathology slices. Results: The encapsulation of GMC in LNPs enhances drug stability and prolongs its hepatic retention, significantly improving its bioavailability and sustained release within the liver. This study also explores the expression of fibroblast activation protein (FAP) in ALI, employing 68Ga-FAPI PET/CT imaging for effective differentiation and assessment of liver injury. Conclusions: Our results suggest that LNPs offer an enhanced therapeutic approach for ALI treatment, reducing the required drug dosage, and 68Ga-FAPI PET/CT imaging provides a novel method for diagnosis and treatment assessment. This study contributes valuable insights into the utilization of LNPs in liver disease treatment, presenting a promising direction for future clinical applications. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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20 pages, 9041 KiB  
Article
Theranostic Potential of the iPSMA-Bombesin Radioligand in Patients with Metastatic Prostate Cancer: A Pilot Study
by Sofía González-Rueda, Osvaldo García-Pérez, Myrna Luna-Gutiérrez, Blanca Ocampo-García, Clara Santos-Cuevas, Gerardo Ramírez-Nava, Joel Vargas-Ahumada, Erika Azorín-Vega, Guillermina Ferro-Flores and Laura Meléndez-Alafort
Pharmaceutics 2024, 16(11), 1358; https://doi.org/10.3390/pharmaceutics16111358 - 24 Oct 2024
Cited by 1 | Viewed by 1994
Abstract
Background/Objectives: Prostate cancer (PC) represents the second most diagnosed form of cancer in men on a global scale. Despite the theranostic efficacy of prostate-specific membrane antigen (PSMA) radioligands, there is a spectrum of PC disease in which PSMA expression is low or absent. [...] Read more.
Background/Objectives: Prostate cancer (PC) represents the second most diagnosed form of cancer in men on a global scale. Despite the theranostic efficacy of prostate-specific membrane antigen (PSMA) radioligands, there is a spectrum of PC disease in which PSMA expression is low or absent. The gastrin-releasing peptide receptor (GRPR), also known as the bombesin type 2 receptor, has been identified as a target in both the early and advanced stages of PC. The objective of this study was to prepare and preclinically evaluate [99mTc]Tc-iPSMA-Bombesin ([99mTc]Tc-iPSMA-BN), estimate dosimetry in healthy subjects, and assess the diagnostic efficacy of the radiotracer in patients with metastatic PC, with the hypothesis of non-inferiority to one of the gold standards, [18F]-PSMA-1007. Moreover, the potential of [99mTc]Tc-iPSMA-BN as a theranostic pair with [177Lu]Lu-iPSMA-BN was investigated. Methods: [99mTc]Tc-iPSMA-BN was prepared under GMP conditions with radiochemical purities > 95%, showing specific recognition by PSMA and GRP receptors in prostate cancer cells and mice bearing PC tumors. Six healthy volunteers were enrolled, and [99mTc]Tc-iPSMA-BN SPECT/CT imaging (740 MBq) was performed to estimate the dosimetry. The pilot clinical study included seven mCRPC and four mCSPC patients with prior androgen deprivation therapy. All patients had a recent [18F]-PSMA-PET/CT scan and were enrolled in this prospective study on their own signed behalf. Volumetric lesion target-to-background ratios (TBRs) were obtained from PET/CT and SPECT/CT images. Results: [99mTc]Tc-iPSMA-BN effective radiation dose was 1.94 ± 0.39 mSv/740 MBq. A total of 178 lesions were detected via CT, 162 via [18F]-PSMA-1007 PET, and 155 via [99mTc]Tc-iPSMA-BN SPECT. Three patients with mCRPC had higher TBR values on SPECT than on PET. [99mTc]Tc-iPSMA-BN appears to have better lesion detection in patients with aggressive histologic transformation. Two-way ANOVA analysis revealed a significant difference in TBR values between patients with mCRPC and mCSPC (p < 0.05) but no difference between [18F]-PSMA-1007 and [99mTc]Tc-iPSMA-BN (p > 0.05). In one patient, [177Lu]Lu-iPSMA-BN showed a high correlation with [99mTc]Tc-iPSMA-BN for lesions that concentrated radioactivity. Conclusions: [99mTc]Tc-iPSMA-BN SPECT/CT is a promising alternative not only for diagnostic purposes but also for broadening the spectrum of PC patients who may benefit from radionuclide theranostics. The results justify the development of a clinical trial involving a significant number of patients with PC. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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11 pages, 922 KiB  
Article
Automated Production of [68Ga]Ga-Desferrioxamine B on Two Different Synthesis Platforms
by Martin Kraihammer, Miloš Petřík, Christine Rangger, Michael Gabriel, Hubertus Haas, Bernhard Nilica, Irene Virgolini and Clemens Decristoforo
Pharmaceutics 2024, 16(9), 1231; https://doi.org/10.3390/pharmaceutics16091231 - 21 Sep 2024
Viewed by 1054
Abstract
Background/Objectives: PET imaging of bacterial infection could potentially provide added benefits for patient care through non-invasive means. [68Ga]Ga-desferrioxamine B—a radiolabelled siderophore—shows specific uptake by human-pathogenic bacteria like Staphylococcus aureus or Pseudomonas aeruginosa and sufficient serum stability for clinical application. In this [...] Read more.
Background/Objectives: PET imaging of bacterial infection could potentially provide added benefits for patient care through non-invasive means. [68Ga]Ga-desferrioxamine B—a radiolabelled siderophore—shows specific uptake by human-pathogenic bacteria like Staphylococcus aureus or Pseudomonas aeruginosa and sufficient serum stability for clinical application. In this report, we present data for automated production of [68Ga]Ga-desferrioxamine B on two different cassette-based synthesis modules (Modular-Lab PharmTracer and GRP 3V) utilising commercially obtainable cassettes together with a licensed 68Ge/68Ga radionuclide generator. Methods: Quality control, including the determination of radiochemical purity, as well as a system suitability test, was set up via RP-HPLC on a C18 column. The two described production processes use an acetic acid/acetate buffer system with ascorbic acid as a radical scavenger for radiolabelling, yielding ready-to-use formulations with sufficient activity yield. Results: Batch data analysis demonstrated radiochemical purity of >95% by RP-HPLC combined with ITLC and excellent stability up to 2 h after synthesis. Specifications for routine production were set up and validated with four masterbatches for each synthesis module. Conclusions: Based on this study, an academic clinical trial for imaging of bacterial infection was initiated. Both described synthesis methods enable automated production of [68Ga]Ga-desferrioxamine B in-house with high reproducibility for clinical application. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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15 pages, 3425 KiB  
Article
In Vivo Evaluation of 68Ga-Labeled NOTA-EGFRvIII Aptamer in EGFRvIII-Positive Glioblastoma Xenografted Model
by Jun Young Park, Ye Lim Cho, Tae Sup Lee, Daekyun Lee, Ju-Hyung Kang, Soryong Lim, Yujin Lee, Jae Hyun Lim and Won Jun Kang
Pharmaceutics 2024, 16(6), 814; https://doi.org/10.3390/pharmaceutics16060814 - 16 Jun 2024
Viewed by 1862
Abstract
EGFRvIII is expressed only in tumor cells and strongly in glioblastoma and is considered a promising target in cancer diagnosis and therapy. Aptamers are synthetic single-stranded oligonucleotides that bind to biochemical target molecules with high binding affinity and specificity. This study examined the [...] Read more.
EGFRvIII is expressed only in tumor cells and strongly in glioblastoma and is considered a promising target in cancer diagnosis and therapy. Aptamers are synthetic single-stranded oligonucleotides that bind to biochemical target molecules with high binding affinity and specificity. This study examined the potential of the 68Ga-NOTA-EGFRvIII aptamer as a nuclear imaging probe for visualizing EGFRvIII-expressing glioblastoma by positron emission tomography (PET). EGFRvIII aptamer was selected using the SELEX technology, and flow cytometry and fluorescence microscopy verified the high binding affinity to EGFRvIII positive U87MG vIII 4.12 glioma cells but not to EGFRvIII negative U87MG cells. The EGFRvIII aptamer was conjugated with a chelator (1,4,7-triazanonane-1,4,7-triyl)triacetic acid (NOTA) for 68Ga-labeling. The 68Ga-NOTA-EGFRvIII aptamer was prepared using the preconcentration-based labeling method with a high radiolabeling yield at room temperature. Ex vivo biodistribution analyses confirmed the significantly higher tumor uptake of the 68Ga-NOTA-EGFRvIII aptamer in EGFRvIII-expressing xenograft tumors than that in EGFRvIII negative tumors, confirming the specific tumor uptake of the 68Ga-NOTA-EGFRvIII aptamer in vivo. PET imaging studies revealed a high retention rate of the 68Ga-NOTA-EGFRvIII aptamer in U87MG vIII 4.12 tumors but only low uptake levels in U87-MG tumors, suggesting that the 68Ga-NOTA-EGFRvIII aptamer may be used as a PET imaging agent for EGFRvIII-expressing glioblastoma. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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16 pages, 3519 KiB  
Article
GRPR-Antagonists Carrying DOTAGA-Chelator via Positively Charged Linkers: Perspectives for Prostate Cancer Theranostics
by Karim Obeid, Panagiotis Kanellopoulos, Ayman Abouzayed, Adam Mattsson, Vladimir Tolmachev, Berthold A. Nock, Theodosia Maina and Anna Orlova
Pharmaceutics 2024, 16(4), 513; https://doi.org/10.3390/pharmaceutics16040513 - 8 Apr 2024
Cited by 3 | Viewed by 2786
Abstract
Gastrin-releasing peptide receptor (GRPR)-antagonists have served as motifs in the development of theranostic radioligands for prostate cancer. Our efforts have been focused on the development of radiolabeled RM26 (H-DPhe6–Gln7–Trp8–Ala9–Val10–Gly11–His12–Sta [...] Read more.
Gastrin-releasing peptide receptor (GRPR)-antagonists have served as motifs in the development of theranostic radioligands for prostate cancer. Our efforts have been focused on the development of radiolabeled RM26 (H-DPhe6–Gln7–Trp8–Ala9–Val10–Gly11–His12–Sta13–Leu14–NH2) analogs, such as [111In]In-DOTAGA-PEG2-RM26. We recently showed that its Gly11/Sar11-substituted version, [111In]In-AU-RM26-M1, resisted degradation by neprilysin (NEP) while in circulation and achieved higher tumor uptake in mice. We herein introduce the following three new AU-RM26-M1 mimics labeled with In-111, with basic residues in the linker: (i) AU-RM26-M2 (PEG2-Pip), (ii) AU-RM26-M3 (PEG2-Arg), and (iii) AU-RM26-M4 (Arg-Arg-Pip). These analogs were compared in PC-3 cells and animal models vs. AU-RM26-M1 (reference). The new analogs showed high affinity and specificity for the GRPR, exhibiting an uptake and distribution pattern in PC-3 cells typical for a radiolabeled GRPR-antagonist. They showed high stability in peripheral mice blood, except for [111In]In-AU-RM26-M3. AU-RM26-M4 achieved the highest tumor uptake and promising background clearance, followed by [111In]In-RM26-M2, showing lower background levels. These findings were confirmed for [111In]In-AU-RM26-M2 and [111In]In-AU-RM26-M4 by micro-SPECT/CT at 4 and 24 h post-injection. Hence, the type of positively charged residues in the linker of AU-RM26-M1 mimics strongly influenced biological behavior. The analogs with Pip next to DPhe6 demonstrated the best overall characteristics and warrant further investigation. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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Review

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24 pages, 3843 KiB  
Review
Beyond Small Molecules: Antibodies and Peptides for Fibroblast Activation Protein Targeting Radiopharmaceuticals
by Xiaona Sun, Yuxuan Wu, Xingkai Wang, Xin Gao, Siqi Zhang, Zhicheng Sun, Ruping Liu and Kuan Hu
Pharmaceutics 2024, 16(3), 345; https://doi.org/10.3390/pharmaceutics16030345 - 29 Feb 2024
Cited by 7 | Viewed by 5090
Abstract
Fibroblast activation protein (FAP) is a serine protease characterized by its high expression in cancer-associated fibroblasts (CAFs) and near absence in adult normal tissues and benign lesions. This unique expression pattern positions FAP as a prospective biomarker for targeted tumor radiodiagnosis and therapy. [...] Read more.
Fibroblast activation protein (FAP) is a serine protease characterized by its high expression in cancer-associated fibroblasts (CAFs) and near absence in adult normal tissues and benign lesions. This unique expression pattern positions FAP as a prospective biomarker for targeted tumor radiodiagnosis and therapy. The advent of FAP-based radiotheranostics is anticipated to revolutionize cancer management. Among various types of FAP ligands, peptides and antibodies have shown advantages over small molecules, exemplifying prolonged tumor retention in human volunteers. Within its scope, this review summarizes the recent research progress of the FAP radiopharmaceuticals based on antibodies and peptides in tumor imaging and therapy. Additionally, it incorporates insights from recent studies, providing valuable perspectives on the clinical utility of FAP-targeted radiopharmaceuticals. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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