A novel throughput assay to assess molecular hydrophobicity during early biotherapeutic developability assessments

一种用于早期生物治疗药物开发评估中评估分子疏水性的新型高通量检测方法

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Abstract

Developability studies provide essential data to identify monoclonal antibodies (mAbs) with optimal drug-like properties, which are indicative of a molecule's suitability for large-scale manufacturing, long-term storage, and ease of administration. Hydrophobicity is a critical molecular attribute that affects solubility, aggregation, and stability at high protein concentrations and is routinely assessed in these studies. Although traditional analytical hydrophobic interaction chromatography (aHIC) is considered the benchmark for measuring hydrophobicity, its application in early developability studies is limited because the process requires serial sample injections, which is time-intensive and impractical for the evaluation of hundreds of molecules. To overcome this limitation, we developed an alternative aHIC method that uses a plate-based assay format, enabling rapid screening of large sample sets. Compatible with automation platforms, this surrogate aHIC method demonstrates excellent accuracy in distinguishing between low- and high-risk molecules, proving to be an efficient tool for preliminary developability assessments. This innovative assay provides a robust, timesaving, and sample-efficient means of evaluating hydrophobicity that readily supports early phase biotherapeutic antibody discovery through selection of mAbs with favorable drug-like properties. Furthermore, the potential for adaptation of this method to various molecular formats suggests its broad applicability in biotherapeutic discovery.

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