Solid dispersion of BIBR1532: A potent therapeutic for oesophageal squamous cancer

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.