Zhang XJ, Deng NX, Zhang HQ, Cen JZ, Zheng ZX, Guo MQ, Huang ZW. Solid dispersion of BIBR1532: A potent therapeutic for oesophageal squamous cancer. World J Gastrointest Oncol 2026; 18(1): 114924 [PMID: 41607744 DOI: 10.4251/wjgo.v18.i1.114924]
Corresponding Author of This Article
Zheng-Wei Huang, PhD, Associate Professor, College of Pharmacy, Jinan University, No. 855 East Xingye Dadao, Panyu District, Guangzhou 511443, Guangdong Province, China. huangzhengw@jnu.edu.cn
Research Domain of This Article
Gastroenterology & Hepatology
Article-Type of This Article
Letter to the Editor
Open-Access Policy of This Article
This article is an open-access article which was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: http://creativecommons.org/licenses/by-nc/4.0/
Xue-Juan Zhang, Nai-Xuan Deng, Huan-Qing Zhang, Jie-Zuan Cen, Zi-Xuan Zheng, Meng-Qin Guo, Zheng-Wei Huang, College of Pharmacy, Jinan University, Guangzhou 511443, Guangdong Province, China
Author contributions: Zhang XJ contributed to manuscript writing and file sorting; Deng NX contributed to core tip and conclusion writing; Zhang HQ contributed to abstract writing and Figure 1 making; Cen JZ contributed to introduction writing and Figures 2 and 3 making; Zheng ZX contributed to reference list inserting; Guo MQ revised and polished the manuscript; Huang ZW contributed to theoretical framework, supervision, proofreading, and submission; all of the authors read and approved the final version of the manuscript to be published.
Supported by “Continuation” Project of Excellent Doctors, Guangdong Basic and Applied Basic Research Foundation, No. 2025A04J5082; and Guangdong Basic and Applied Basic Research Foundation, No. 2024A1515011236.
Conflict-of-interest statement: All the authors report no relevant conflicts of interest for this article.
Open Access: This article is an open-access article that was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution NonCommercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: https://creativecommons.org/Licenses/by-nc/4.0/
Corresponding author: Zheng-Wei Huang, PhD, Associate Professor, College of Pharmacy, Jinan University, No. 855 East Xingye Dadao, Panyu District, Guangzhou 511443, Guangdong Province, China. huangzhengw@jnu.edu.cn
Received: October 10, 2025 Revised: November 5, 2025 Accepted: November 20, 2025 Published online: January 15, 2026 Processing time: 102 Days and 0.7 Hours
Abstract
This letter addresses challenges in the clinical translation of BIBR1532, a promising telomerase inhibitor, for the treatment of esophageal squamous cell carcinoma (ESCC). BIBR1532 exerts its anti-cancer effect by activating DNA damage response (ATR/CHK1 and ATM/CHK2) pathways and downregulating telomere-binding proteins. Although its therapeutic potential is limited by poor aqueous solubility, solid dispersion (SD) technology may overcome this obstacle. Systematic analysis using PubChem-derived simplified molecular input line entry system identifiers and artificial intelligence-driven FormulationDT platform evaluation (oral formulation feasibility index: 0.38) revealed that the SD technology, with superior scalability (32 approved products by 2021) and lower production risks, outperforms lipid-based formulations as an optimal dissolution strategy. Material analysis revealed hydroxypropyl methylcellulose (HPMC) as the optimal carrier with lower hygroscopicity, higher temperature and no intestinal targeting, thus enabling ESCC therapy. HPMC-based SD enhances BIBR1532 solubility and bioavailability for effective ESCC treatment. Future studies should focus on pilot tests for SD fabrication.
Core Tip: To overcome the poor aqueous solubility and low druggability of the anti-cancer agent BIBR1532, we proposed hydroxypropyl methylcellulose (HPMC)-based solid dispersion technology for solubilisation. This approach has lower costs and risks than lipid-based formulations for large-scale manufacturing. We selected an HPMC-based strategy because of its low hygroscopicity and high glass transition temperature. These properties ensure the release and absorption of the drug in the upper gastrointestinal tract, which is a key requirement for the treatment of esophageal squamous cell carcinoma.
