Review of approaches and examples for monitoring biotransformation in protein and peptide therapeutics by MS.

Biotherapeutic drugs have emerged in quantity in pharmaceutical pipelines, and increasingly diverse biomolecules are progressed through preclinical and clinical development. As purification, separation, mass spectrometer detection and data processing capabilities improve, there is opportunity to monitor drug concentration by traditional ligand-binding assay or MS measurement and to monitor metabolism, catabolism or other biomolecular mass variants present in circulation. This review highlights approaches and examples of monitoring biotransformation of biotherapeutics by MS as these techniques are poised to add value to drug development in years to come. The increased use of such approaches, and the successful quantitation of biotherapeutic structural modifications, will provide insightful data for the benefit of both researchers and patients.