State-of-the-art boron clusters for boron neutron-capture therapy

Sep 28, 2026

Uploaded by Hazel

Boron neutron-capture therapy (BNCT) is a highly precise, cell-level radiotherapy that relies on neutron capture by boron-10, producing nuclear fission and high-energy particles to selectively damage cancer cells. It remains a leading approach for cancer treatment, yet current approved boron drugs, such as sodium mercaptoundecahydro-closo-dodecaborate and BPA, face limitations in targeting, intracellular concentration, residence time, and overall applicability. Boron clusters offer superior stability and three-dimensional architecture, enabling next-generation boron drug design by linking microstructure to macroscopic function. This review summarizes strategies for constructing boron clusters, including multi-level structures, functionalization for clinical translation, diverse applications of line-functionalized derivatives, and advances in BNCT visualization, anticancer mechanisms, and neutron accelerator devices.

LanguageEnglish

CategoryHealthcare

FormatPDF

Pages48

Reading Time2 h 1 min

AccessFree to download

Introduction

Boron neutron-capture therapy overview and historical development

Boron drugs and their limitations

Rationale for boron clusters in next-generation BNCT

Review scope and strategy overview

Construction strategies for boron clusters

Functionalization for clinical applications

Structure–function relationships and evaluation advances

Applications and mechanism

Line-functionalized derivative applications

BNCT anticancer mechanisms and accelerator devices

Theranostics 2026, Vol. 16, Issue 1 417 Ivyspring International Publisher Theranostics 2026; 16(1): 417-464. doi: 10.7150/thno.123376 Review State-of-the-art boron clusters for boron neutron-capture therapy Weiyao Wang1*, Enze Zhang1*, Jiaojiao Shan4*, Min Zhang1, Renwei Cai2, Runze Li3, Lulian Pang2, Baosheng Li2􀀍, Dejin Zang1􀀍 1. School of Pharmaceutical Sciences & Institute of Materia Medica, National Key Laboratory of Advanced Drug Delivery System, Key Laboratory for Biotechnology Drugs of National Health Commission (Shandong Academy of Medical Sciences), Key Lab for Rare & Uncommon Diseases of Shandong Province, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, Shandong, 250117, China. 2. Department of Radiation Oncology, Shandong Cancer Hospital and Institute, Shandong First Medical University and Shandong Academy of Medical Sciences, Jinan, Shandong, 250117, China. 3. Qingdao Medical College of Qingdao University, No. 1 Ningde Road, Haoyuan, Qingdao University, Qingdao, 266071, China. 4. The Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, 250114, China. * represents that they contribute equally to this work. 􀀍 Corresponding authors: E-[mail address: baoshli1963@163.com](mail address: baoshli1963@163.com) (B. Li) [zangdejin_lm@163.com](zangdejin_lm@163.com) (D. Zang) . © The author(s). This is an open access article distributed under the terms of the Creative Commons Attribution License ([https://creativecommons.org/licenses/by/4.0/](https://creativecommons.org/licenses/by/4.0/)). See [https://ivyspring.com/terms](https://ivyspring.com/terms) for full terms and conditions. Received: 2025.08.08; Accepted: 2025.09.24; Published: 2026.01.01 Abstract Boron neutron-capture therapy (BNCT) is a highly precise, cell-level cancer radiotherapy. It exploits the neutron-capture reaction that occurs when low-energy thermal neutrons are absorbed by a boron-10 atom, triggering a nuclear fission reaction that releases high-energy particles to selectively kill cancer cells. BNCT is at the forefront of cancer treatment. Presently, only sodium mercaptoundecahydro-closo-dodecaborate and boron borylphenylalanine (BPA) have been approved as boron drugs for clinical trials by the Food and Drug Administration. However, these drugs still suffer from shortcomings, such as poor targeting, low concentration in cancer cells, a short residence time, and low overall applicability. Conversely, boron clusters are three-dimensional polyhedral structures composed of carbon, boron, and hydrogen atoms. Owing to their excellent stability and unique three-dimensional shape, they are ideal candidates for next-generation boron drugs. These unique features make boron clusters an ideal model for correlating macroscopic properties with the microstructures of substances, providing a valuable framework for the rational design of next-generation boron drugs. Thus, from an interdisciplinary perspective, this review summarizes new strategies for constructing boron clusters, including multi-level structures. We describe key chemical strategies for their functionalization for clinical applications, reveal the multi-scenario applications of their line-functionalized derivatives, and highlight their cross-disciplinary value in precision synthesis, biomedicine, and advanced materials, all with a focus on elucidating the structure–function relationship in boron clusters. Additionally, we explored the latest advancements in the visual evaluation of BNCT, its anticancer mechanism, and exclusive neutron accelerator devices. In summary, the development of novel boron drugs based on functional boron clusters is a prerequisite to resolving the key technical issues in the research and development of new BNCT agents. This review provides insights into the design of new BNCT drugs, as well as related supporting equipment and treatment options, from the perspectives of medicinal chemist

FAQs

What is the core principle of boron neutron-capture therapy (BNCT)?

BNCT uses low-energy thermal neutrons absorbed by boron-10, triggering nuclear reactions that release high-energy particles to selectively kill cancer cells.

Why do current approved boron drugs limit BNCT performance?

Approved boron drugs have shortcomings including poor targeting, low concentration in cancer cells, short residence time, and limited overall applicability.

What makes boron clusters promising for next-generation BNCT agents?

Boron clusters are stable, three-dimensional polyhedral structures that support strong structure–function correlations and provide an ideal platform for rational functionalization and targeted clinical use.

Sep 28, 2026

Uploaded by Hazel