Cancer Biotherapy and Radiopharmaceuticals最新文献

{"title":"Development of a Freeze-Dried Bevacizumab Kit for ^99mTc Radiolabeling and Preclinical Evaluation <i>In Vitro</i> and in Normal Mice.","authors":"Thi Khanh Giang Nguyen, Thi Ngoc Nguyen, Thanh Binh Nguyen, Ho Hong Quang Dang, Thu Minh Chau Nguyen, Dang Khoa Nguyen, Thanh Nhan Nguyen, Tran Quang Thai Vo, Trung Tin Dang, Ngoc Bao Nam Dinh, Thanh Minh Pham, Thi Thu Nguyen","doi":"10.1177/10849785261461405","DOIUrl":"10.1177/10849785261461405","url":null,"abstract":"<p><strong>Background: </strong>Bevacizumab, a humanized monoclonal antibody targeting vascular endothelial growth factor (VEGF), was lyophilized and radiolabeled with ^99mTc for tumor-targeted imaging. In this study, a freeze-dried kit was developed, the formulation was optimized, and the radiolabeled bevacizumab was evaluated <i>in vitro</i> and <i>in vivo</i> for preclinical evaluation.</p><p><strong>Methods: </strong>The preparation process was optimized by investigating pH, temperature, time, and stabilizers. The radiochemical purity (RCP) and immunoreactivity of the lyophilized antibody were determined and confirmed by specific binding to VEGF immobilized on Ni-NTA agarose. Preclinical evaluations included binding assays on three human cancer cell lines (A-549, MCF-7, and HT-29), in which binding affinity (K_d) and maximum binding capacity (B_max) were calculated. Biodistribution studies were performed in normal mice.</p><p><strong>Results: </strong>The optimized kit contained 2.0 mg bevacizumab per vial in phosphate buffer at pH 7.5, ensuring reproducible reconstitution and high labeling efficiency. Quality control demonstrated RCP >97% and <i>in vitro</i> stability of ^99mTc-bevacizumab for at least 6 h post-labeling, with the freeze-dried form stable for 12 months. The ^99mTc-bevacizumab retained >90% immunoreactivity. Binding assays revealed approximately 80% specific binding, with a K_d of 2.8-9.9 nM and a B_max of 1.6-2.0 amol/cell, corresponding to about one million molecules per cell. Biodistribution revealed high initial blood retention, which was moderate in the liver, with a blood clearance half-life of 76.97 min, primarily via renal excretion.</p><p><strong>Conclusions: </strong>The freeze-dried bevacizumab enables convenient ^99mTc radiolabeling, providing a preclinical proof-of-concept supporting further development as a tumor imaging-agent.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"811-823"},"PeriodicalIF":1.7,"publicationDate":"2026-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148310419","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"PWidFHNet: Parallel Wider Forward Harmonic Net to Classify Breast Cancer Using Histopathological Images.","authors":"Rajesh Prasad, Jayashree Prasad, Nihar Ranjan, Amol Dhumane, Mubin Tamboli","doi":"10.1177/10849785261471259","DOIUrl":"10.1177/10849785261471259","url":null,"abstract":"<p><p><i>Background/Purpose:</i> Breast cancer poses a significant health risk to women worldwide. The timely diagnosis of breast cancer is essential to increase the survival rate and to control premature mortality. However, existing classification techniques may not account for all the variations of breast cancer, leading to potential misclassification, which adversely affects treatment decisions. This article, therefore, puts forward the PWidFHNet model to enable accurate classification of breast cancer from histopathological images.<i><b>Methods:</b></i>Initially, the acquired histopathological image is subjected to image preprocessing using a Gaussian filter. Subsequently, blood cell segmentation is performed using the Tversky-parallel reverse attention network. Moreover, feature extraction is performed, where shape features and learned invariant feature transform are extracted. Finally, the proposed PWidFHNet is used to perform the breast cancer classification. Here, PWidFHNet is established by incorporating the parallel convolutional neural network with the wide residual network, in which the network layers are enhanced through harmonic analysis.<i>Results:</i> The performance of PWidFHNet is evaluated using metrics such as specificity, accuracy, and sensitivity, all of which achieved their maximum values of 92.76%, 91.60%, and 90.86%, respectively.<i><b>Conclusion:</b></i>The proposed PWidFHNet model provides a reliable and efficient framework for breast cancer classification by integrating advanced image pre-processing, segmentation, feature extraction, and deep learning techniques. The achieved performance highlights its potential as a diagnostic support tool to assist pathologists in breast cancer assessment and clinical decision-making.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"832-850"},"PeriodicalIF":1.7,"publicationDate":"2026-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148622704","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Review of Glypican-3-Targeted Imaging Agents for Hepatocellular Carcinoma.","authors":"Wenye Li, Liqin Liu","doi":"10.1177/10849785261458595","DOIUrl":"10.1177/10849785261458595","url":null,"abstract":"<p><strong>Background: </strong>Hepatocellular carcinoma (HCC) is a highly prevalent malignant tumor globally, with low survival rates in advanced stages. Therefore, early diagnosis and precision therapy are pivotal to improving patient prognosis. Glypican-3 (GPC3) acts as a specific molecular target for HCC, which is highly expressed in 70%-85% of HCC tissues but undetectable in normal liver tissues, hepatitis, liver cirrhosis, and other pathological conditions. This stringent expression regulation renders it an ideal tumor-specific target.</p><p><strong>Main content: </strong>Based on the biological properties of GPC3, various specific tumor imaging agents have been developed, covering multiple biomolecular types, including antibodies, peptides, and aptamers. This review systematically summarizes the research advances, application advantages, and existing challenges of three types of molecular imaging probes in the precise diagnosis and treatment of HCC. It focuses on the development strategies of these probes and evaluates their current limitations in light of key characterization parameters.</p><p><strong>Conclusion: </strong>This review aims to provide new research ideas for the precision diagnosis of HCC and promote the translation of clinical applications.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"773-781"},"PeriodicalIF":1.7,"publicationDate":"2026-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148370684","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Analysis and Outlook on the Use of ^99mTc-FAPI SPECT/CT in the Diagnosis of Primary and Metastatic Lesions of Cholangiocarcinoma.","authors":"Xue Cai, Qingfan Hao","doi":"10.1177/10849785261431301","DOIUrl":"10.1177/10849785261431301","url":null,"abstract":"<p><strong>Introduction: </strong>Cholangiocarcinoma (CCA) is an aggressive malignancy characterized by a poor prognosis, where timely diagnosis and accurate staging are critical yet challenging. Conventional imaging techniques often fail to effectively differentiate primary lesions from micrometastases or to distinguish benign from malignant findings. Fibroblast activation protein (FAP), highly expressed in cancer-associated fibroblasts, presents a promising molecular target for improving diagnostic precision.</p><p><strong>Materials and methods: </strong>This review synthesizes current clinical evidence regarding the application of technetium-99m-labeled FAP inhibitors (^99mTc-FAPI) in single-photon emission computed tomography/computed tomography (SPECT/CT) for the detection of primary and metastatic cholangiocarcinoma. The analysis focuses on the diagnostic performance, sensitivity, and clinical utility of ^99mTc-FAPI SPECT/CT compared to standard imaging modalities such as contrast-enhanced CT and ¹⁸F-FDG PET/CT.</p><p><strong>Results: </strong>Literature indicates that FAP is expressed in over 93% of cholangiocarcinoma stroma, providing a strong rationale for FAPI imaging. Clinical studies demonstrate that ^99mTc-FAPI SPECT/CT effectively detects primary lesions with performance comparable to ¹⁸F-FDG PET/CT. Notably, it exhibits superior sensitivity for identifying lymph node and peritoneal metastases compared to contrast-enhanced CT, detecting a higher number of lesions.</p><p><strong>Conclusions: </strong>^99mTc-FAPI SPECT/CT holds significant potential as a valuable tool for the diagnosis and staging of cholangiocarcinoma, serving as an effective complement to existing imaging methods. Despite challenges such as lower spatial resolution and the need for standardized protocols, the modality offers economic and logistical advantages. Further well-designed, large-scale studies are required to validate these findings and support broader clinical adoption.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"759-772"},"PeriodicalIF":1.7,"publicationDate":"2026-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147576584","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Personalized Radionuclide Therapy via Avidin-Biotin Pretargeting: Biodistribution and Dosimetry of ¹⁷⁷Lu-DOTA-biotin with AvidinOX^TM in Solid Tumors.","authors":"Freddy Gonzalez, Vivek Subbiah, S Cheenu Kappadath, Lucia Martiniova, Gera Santiago, Ravi Murthy, Rita De Santis, Gregory C Ravizzini","doi":"10.1177/10849785261465837","DOIUrl":"10.1177/10849785261465837","url":null,"abstract":"<p><strong>Purpose: </strong>AvidinOX^™ forms a long-lasting artificial receptor that supports effective <i>in vivo</i> binding of circulating biotinylated therapeutic ¹⁷⁷Lu-DOTA-biotin. We investigated the biodistribution and radiation dosimetry of ¹⁷⁷Lu-DOTA-biotin in patients with solid tumors following image-guided intratumoral AvidinOX administration.</p><p><strong>Methods: </strong>Three patients received intratumoral injections of AvidinOX and two cycles of intravenous administration of ¹⁷⁷Lu-DOTA-biotin over a period of 2 weeks. Multi-time-point whole-body planar and SPECT/CT imaging was performed post infusion. Blood and urine samples were collected over 7 days, and organ radiation doses were estimated using the Medical Internal Radiation Dose methodology.</p><p><strong>Results: </strong>Sequential imaging demonstrated favorable tumor-to-background ratios and sustained uptake of ¹⁷⁷Lu-DOTA-biotin within the pretargeted lesions, confirming effective localization and prolonged retention. Most of the administered activity was excreted via urine within 4 h post infusion. The absorbed tumor radiation dose ranged from 3.96 to 50.37 Gy, while bone marrow (0.15-0.22 Gy) and kidney (0.66-1.84 Gy) doses remained below established safety thresholds. There were no serious adverse events.</p><p><strong>Conclusions: </strong>Intratumoral AvidinOX achieved effective and durable localization of ¹⁷⁷Lu-DOTA-biotin without exceeding the maximum allowable radiation absorbed dose to critical organs. These first-in-human dosimetric data provide quantitative insight into tumor retention, off-target exposure, and therapeutic potential across solid tumors, supporting the rational design of future radionuclide therapy trials.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"782-793"},"PeriodicalIF":1.7,"publicationDate":"2026-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148426548","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Hierarchical Framework for Autonomous Macrophage Migration Based on Exploration and Exploitation.","authors":"Muyu Ji, Chenyang Wang, Haiying Wan, Hamid Reza Karimi, Xiaoli Luan, Fei Liu","doi":"10.1177/10849785261497227","DOIUrl":"https://doi.org/10.1177/10849785261497227","url":null,"abstract":"<p><strong>Background: </strong>Macrophage migration is vital in cancer therapy, as it contributes to the elimination of cancer cells and enables targeted drug delivery. However, the natural migratory ability of macrophage is limited, and the location of cancer cells are dynamic and uncertain.</p><p><strong>Methods: </strong>To address this issue, we propose a hierarchical framework based on exploration and exploitation to enable autonomous macrophage migration. Specifically, the upper layer employs a particle filter to explore cancer cell location by sensing signaling molecule concentrations. This information is then passed to the middle layer, which applies the maximum Shannon entropy sampling principle to determine the optimal movement position. Finally, the lower layer utilizes optogenetics to guide migration toward targets, which constitutes exploitation. The interaction among the layers enables autonomous macrophage migration.</p><p><strong>Results: </strong>Simulation results verify the effectiveness of the proposed framework, demonstrating that the macrophage successfully eliminates the cancer cell even when the target location is unknown. Furthermore, the results reveal that the proposed framework achieves higher targeting precision compared to both greedy and nonlayered strategies, thereby enhancing the accuracy of cancer cell elimination and targeted drug delivery.</p><p><strong>Conclusions: </strong>This study highlights the potential translational value for improving targeted cancer therapy.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"10849785261497227"},"PeriodicalIF":1.7,"publicationDate":"2026-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149225490","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Focused Ultrasound-Enhanced Delivery of ED5, a CK1α-Targeting Oleanolic Acid Analogue, Suppresses Glioma Growth via MAPK-ROS-ERS Pathway Modulation.","authors":"Yongqi Liu, Lulu Zou, Chengpeng Zhan, Jinli Zhang, Meiying Li, Xinjiang Yan, Xiaoqing Chen, Jing Zhang, Guofeng Yu","doi":"10.1177/10849785261476936","DOIUrl":"https://doi.org/10.1177/10849785261476936","url":null,"abstract":"<p><strong>Aim: </strong>The objective of this study was to assess the anticancer efficacy of ED5, a new oleanolic acid (OA) analogue and selective casein kinase 1α (CK1α) inhibitor, and to ascertain if focused ultrasound (FUS) can improve its delivery and therapeutic effect against glioma. The authors carried out <i>in vitro</i>, <i>in vivo</i>, and mechanistic studies incorporating ultrasound-mediated drug delivery, building on the chemical synthesis of ED5 with OA as the main ingredient.</p><p><strong>Methods: </strong>The intratumoral penetration of ED5 in glioma cells and xenograft-bearing mice was enhanced by focused ultrasonic exposure. Cell counting kit-8 assays were used to measure cell viability to calculate IC₂₀ values and proliferative capability. Clonogenic survival was evaluated using crystal violet staining. Kinase activity was assessed by kinome profiling. Molecular docking, isothermal titration calorimetry, and surface plasmon resonance were used to confirm the binding between ED5 and CK1α. Changes in molecular expression brought on by ED5 with or without FUS were measured using quantitative polymerase chain reaction and immunohistochemistry.</p><p><strong>Results: </strong>When compared with OA, ED5 dramatically reduced the ability of human glioma cell lines U118MG and LN229 to proliferate and form colonies. The antiproliferative effects of ED5 were further amplified by FUS, which increased its absorption in glioma cells. Without causing any discernible systemic toxicity, the combination of ED5 and FUS <i>in vivo</i> resulted in a greater suppression of tumor growth than ED5 alone. According to mechanistic research, ED5 selectively binds CK1α and inhibits its kinase activity. Endoplasmic reticulum stress (ERS), reactive oxygen species (ROS) buildup, and activation of the JNK/c-Jun branch of the Mitogen-activated protein kinase (MAPK) signaling pathway were all brought on by this suppression. By increasing the effectiveness of ED5 administration, FUS further enhanced these molecular effects.</p><p><strong>Conclusions: </strong>ED5 targets CK1α and modulates the <i>MAPK-ROS-ERS</i> signaling pathway to demonstrate strong anticancer efficacy against glioblastoma. A novel ultrasound-enhanced biotherapy approach for glioma care is highlighted by FUS, which dramatically increases ED5 intratumoral delivery and therapeutic efficacy.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"10849785261476936"},"PeriodicalIF":1.7,"publicationDate":"2026-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149169103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Radioimmunotherapy: Mechanisms, Strategies, and Advances in Therapeutic Enhancement.","authors":"Syed Ali Raza Naqvi, Syeda Minahal Fatima, Syed Muhammad Waji-Ul-Hassan, Shakaib Arslan Gursal, Shazia Fatima, Muhammad Babar Imran, Mohammad Wasim, Mohamed Fawzy Ramadan, Nadeem Ahmed Lodhi","doi":"10.1177/10849785261486288","DOIUrl":"https://doi.org/10.1177/10849785261486288","url":null,"abstract":"<p><p>Radioimmunotherapy (RIT) represents a paradigm shift in precision cancer therapy by integrating the molecular specificity of monoclonal antibodies with the cytotoxic potential of therapeutic radionuclides. However, the therapeutic success of RIT is not merely associated with targeted radiation delivery but also depends on complex interplay of radiobiology, tumor immunology, antibody pharmacology, and patient-specific dosimetry. This review explores the molecular and cellular mechanisms, including DNA damage response, immunogenic cell death, tumor microenvironment remodeling, cytokine signaling, and bystander/abscopal effects of RIT. The role of key pharmacological determinants such as target antigen selection, antibody engineering, radionuclide chemistry, radiolabeling strategies, pharmacokinetics, biodistribution, and personalized dosimetry will also be evaluated for therapeutic effectiveness of RIT. Furthermore, translational challenges such as heterogeneous antigen expression, limited tumor penetration, dosimetric uncertainty, and immune-mediated therapeutic resistance in addition to logistical barriers have also been discussed.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"10849785261486288"},"PeriodicalIF":1.7,"publicationDate":"2026-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149170127","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Research Progress of Cyclooxygenase-2 in Colorectal Adenomas.","authors":"Zhongsen Dou, Zhiwei Wang, Fanglai Zhu","doi":"10.1177/10849785261415777","DOIUrl":"10.1177/10849785261415777","url":null,"abstract":"<p><strong>Background: </strong>Cyclooxygenase-2 (COX-2) serves as a pivotal molecule bridging inflammation and tumor development, playing a central role in the initiation, progression, and malignant transformation of colorectal adenomas.</p><p><strong>Methods: </strong>This review systematically examines COX-2 expression patterns, molecular regulatory networks, and its potential applications in clinical diagnosis, prognosis assessment, and chemoprevention.</p><p><strong>Results: </strong>Evidence indicates that COX-2 exhibits significantly elevated expression in adenoma tissues (e.g., 54.8% positive rate in polyps vs. 18.5% in adjacent tissue), driving pathological progression through multiple mechanisms including cell proliferation induction, apoptosis inhibition, angiogenesis promotion, and tumor immune microenvironment remodeling. Nonsteroidal anti-inflammatory drugs and selective COX-2 inhibitors have demonstrated clear promise in adenoma chemoprevention (with agents such as celecoxib reducing advanced adenoma recurrence risk by 33%-45%).</p><p><strong>Conclusions: </strong>COX-2 is a critical early-event biomarker and therapeutic target in colorectal adenomas. Targeting the COX-2 pathway represents a viable strategy for prevention, although challenges regarding safety and personalized application remain.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"655-663"},"PeriodicalIF":1.7,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146031756","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Validation of Manual In-House Synthesis, Imaging, Biodistribution, and Dosimetry of Tb-161 PSMA-617 for mCRPC Patients in a Tertiary Health Care Center: A Proof-of-Concept Study.","authors":"Parul Thakral, Nishant Rana, Abhishek Uppal, Mrinalini Koley, Darshan Thakrani, Jatin Gupta, Vikas Kumar, Dharmender Malik, Ishita Sen","doi":"10.1177/10849785261454146","DOIUrl":"10.1177/10849785261454146","url":null,"abstract":"<p><strong>Background: </strong>Metastatic castration-resistant prostate cancer (mCRPC) remains a therapeutic challenge, particularly in patients with suboptimal response to ¹⁷⁷Lu-PSMA-617. Terbium-161 (Tb-161), with its emission of β-particles and high-LET Auger/conversion electrons, offers potential advantages in targeting micrometastases. However, clinical validation, especially in resource-limited settings, remains limited.</p><p><strong>Materials and methods: </strong>This single-center, proof-of-concept study was conducted at the Department of Nuclear Medicine, FMRI, Gurgaon. Manual in-house radiolabeling of PSMA-617 with Tb-161 was performed. The samples were withdrawn for quality control analyses. Five mCRPC patients were administered Tb-161 PSMA-617. Post-therapy planar and single-photon emission computed tomography/computed tomography (SPECT/CT) imaging was conducted to assess biodistribution and dosimetric analysis.</p><p><strong>Results: </strong>Radiolabeling PSMA-617 with Tb-161 was more than 95% efficient with 55 min of heating at 95°C. The radiochemical purity was >98% for all the runs (<i>n</i> = 5). The sample was found to be sterile with no gel formation seen after 15 d for all the batches. Post-therapy imaging demonstrated favorable biodistribution and high tumor uptake. Dosimetric analysis revealed absorbed doses comparable or superior to historical ¹⁷⁷Lu-PSMA-617 data. No acute adverse events or safety concerns were observed post administration.</p><p><strong>Conclusions: </strong>This study successfully demonstrates the feasibility of manual in-house synthesis and clinical application of Tb-161 PSMA-617 in an Indian tertiary care setting. The favorable synthesis, imaging, biodistribution, and dosimetric profile support its potential as a next-generation theranostic agent for mCRPC. These findings warrant further validation through larger, controlled clinical trials.</p>","PeriodicalId":55277,"journal":{"name":"Cancer Biotherapy and Radiopharmaceuticals","volume":" ","pages":"721-732"},"PeriodicalIF":1.7,"publicationDate":"2026-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148037871","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}