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This review systematically summarizes advances in targeted radiopharmaceutical development, emphasizing modern probe design strategies and click chemistry to accelerate synthesis and enhance targeting efficiency. It consolidates literature from January 2014 to April 2025 across diagnostic imaging with PET and SPECT and therapeutic use of alpha and beta emitters such as 225Ac and 177Lu, including clinically approved agents like 177Lu-DOTATATE and 177Lu-PSMA-617.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":35,"@type":76,"position":81},"https://docshare.wps.com/document/healthcare/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/advancements-in-targeted-radiopharmaceuticals-innovations-in-diagnosis-and-therapy-for-enhanced-cancer-management/371093/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/advancements-in-targeted-radiopharmaceuticals-innovations-in-diagnosis-and-therapy-for-enhanced-cancer-management/371093.png","ImageObject",300,407,{"name":92,"@type":93},"hdkawk","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-10-31","2026-09-23",true,{"@type":102,"interactionType":103,"userInteractionCount":39},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"What role do radiopharmaceuticals play in cancer management?","Question",{"text":112,"@type":113},"Radiopharmaceuticals support nuclear medicine by enabling precise diagnosis and targeted therapy for cancer through radioactive isotopes delivered to specific tissues or organs.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"Which techniques does the review highlight for improving radiopharmaceutical synthesis and targeting?",{"text":117,"@type":113},"The review focuses on state-of-the-art probe design strategies and click chemistry approaches that accelerate radiopharmaceutical synthesis and improve targeting efficiency.",{"name":119,"@type":110,"acceptedAnswer":120},"What imaging and treatment modalities are covered?",{"text":121,"@type":113},"Diagnostic coverage includes PET and SPECT imaging, while therapy includes alpha and beta emitters such as 225Ac and 177Lu, including clinically approved agents for specific cancer types.","https://schema.org",{"og:url":83,"og:type":124,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":126,"canonical":83},"index,follow",{"doc_id":128,"site_id":62},371093,1790880201,{"code":4,"msg":5,"data":131},{"doc_id":128,"user_id":132,"nickname":92,"user_avatar":133,"doc_module":4,"category_id":34,"category_name":35,"doc_title":65,"doc_description":67,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":39,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":36,"language":139,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":140,"faqs":141,"seo_title":142,"seo_description":67,"update_tm":143,"read_time":144},3985747859855,"https://ap-avatar.wpscdn.com/davatar_276721f389ce27ea32af1340a28f341c","ChemBioChem  \nReview  \n[doi.org/10.1002/cbic.202500676](doi.org/10.1002/cbic.202500676)  \n[www.chembiochem.org](www.chembiochem.org)  \nAdvancements in Targeted Radiopharmaceuticals: Innovations in Diagnosis and Therapy for Enhanced Cancer Management  \nMohd Sayeed Shaikh, Rupesh R. Kurhade, Abrar A. M. Siddiqui,  \nShaikh Shahbaz A. Majeed, Thomas J. Webster, Mohammad Intakhab Alam, Abdul Wasy Zia,* and Md. Faiyazuddin*  \nRadiopharmaceuticals (RPhs) represent a breakthrough in nuclear medicine due to their ability to provide precise diagnosis and targeted therapy for cancer by incorporating radioactive isotopes into carrier molecules. This review systematically discusses the recent advances in the development of RPhs, focusing on state-of-the-art probe design strategies and click chemistry applications that accelerate RPh syntheses and improve targeting efficiency. The manuscript synthesizes literature from multiple databases spanning January 2014 to April 2025, encompassing diagnostic modalities including positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging, and therapeutic applications utilizing alpha and beta emitters such as 225Ac and 177 Lu. Clinically approved agents, such as 177 Lu-DOTATATE and 177 Lu-PSMA-617, are used for neuroendocrine tumors and metastatic castration-resistant prostate cancer, respectively, with significant therapeutic efficacy. The review focuses on new  \ntargets, such as fibroblast activation protein, CXCR4 chemokine receptors, and gastrin-releasing peptide receptors, and new delivery systems using nanotechnology to improve biodistribution and tumor accumulation. Challenges regarding productionscalability, regulatory frameworks, and integrating artificial intelligence for personalized dosimetry and treatment planning remain crucial. Combination therapeutic approaches using targeted radionuclide therapy (TRT) in synergy with chemotherapy and immunotherapy and external beam radiation are showing promising results in refractory cancers. The potential avenues include theranostics, predictive modeling for patient selection, and new molecular targeting strategies. This review highlights the transformative potential of RPhsin precision oncology, providing an overview of the current clinical applications and future research trajectories toward improved cancer management.  \n\n| M. S. Shaikh |  | T. J. Webster |\n| --- | --- | --- |\n| Department of Pharmaceutical Chemistry |  | Division of Pre-college and Undergraduate Studies |\n| Y. B. Chavan College of Pharmacy |  | Brown University |\n| Dr. Rafiq Zakaria Campus, Aurangabad 431001, Maharashtra, India |  | Providence, Rhode Island 02912, USA |\n| R. R. Kurhade |  | M. I. Alam |\n| Department of Pharmaceutics |  | Department of Pharmaceutics |\n| Government College of Pharmacy, Osmanpura |  | College of Pharmacy |\n| Aurangabad 431001, Maharashtra, India |  | Jazan University |\n| A. A. M. Siddiqui |  | Jazan 45142, Saudi Arabia |\n| Formulation R & D (DPI) |  | A. W. Zia |\n| Global Respiratory |  | Institute of Mechanical Process and Energy Engineering (IMPEE) |\n| Cipla Ltd. |  | School of Engineering and Physical Sciences |\n| LBS Marg, Vikhroli (West), Mumbai, Maharashtra 400083, India |  | Heriot-Watt University |\n| S. S. A. Majeed Quality Assurance |  | Edinburgh EH14 4AS, UK\u003Cbr>E-mail: [a.zia@hw.ac.uk](a.zia@hw.ac.uk) |\n| Hetero Labs Limited |  | M. Faiyazuddin |\n| Hll Unit VI, Jadcherla, Hyderabad, Telangana 509301, India |  | Centre for Global Health Research |\n| T. J. Webster |  | Saveetha Institute of Medical & Technical Sciences |\n| School of Health Sciences and Biomedical Engineering\u003Cbr>Hebei University of Technology\u003Cbr>Tianjin 300132, China\u003Cbr>T. J. Webster | | Chennai, Tamil Nadu 600077, India\u003Cbr>E-mail: [faiyazuddin.smc@saveetha.com](faiyazuddin.smc@saveetha.com)\u003Cbr>© 2025 The Author(s). ChemBioChem published by Wiley-VCH GmbH. This isan open access article under the terms of the Creative Commons Attribution |","cbCaiiRi7YtOoldu","https://ap.wps.com/l/cbCaiiRi7YtOoldu","pdf",6243004,"English","# 1. Introduction to Targeted Radiopharmaceuticals (RPhs)\n## Components and design overview\n## Therapeutic and diagnostic applications","[{\"question\":\"What role do radiopharmaceuticals play in cancer management?\",\"answer\":\"Radiopharmaceuticals support nuclear medicine by enabling precise diagnosis and targeted therapy for cancer through radioactive isotopes delivered to specific tissues or organs.\"},{\"question\":\"Which techniques does the review highlight for improving radiopharmaceutical synthesis and targeting?\",\"answer\":\"The review focuses on state-of-the-art probe design strategies and click chemistry approaches that accelerate radiopharmaceutical synthesis and improve targeting efficiency.\"},{\"question\":\"What imaging and treatment modalities are covered?\",\"answer\":\"Diagnostic coverage includes PET and SPECT imaging, while therapy includes alpha and beta emitters such as 225Ac and 177Lu, including clinically approved agents for specific cancer types.\"}]","Advancements in Targeted Radiopharmaceuticals: Innovations in Diagnosis and Therapy for Enhanced Cancer Management | PDF",1790191225,101]