Bio-orthogonal Chemistry

Bio-orthogonal Chemistry encompasses chemical reactions that proceed selectively in biological environments without interfering with or being interfered by native biochemistry, employing reaction pairs including azide-alkyne cycloadditions, tetrazine-transcyclooctene ligations, and Staudinger ligations that are absent from biology providing selectivity.

The biopharmaceutical industry leverages bio-orthogonal chemistry for in vivo imaging, site-specific bioconjugation, and selective modification of biomolecules in complex biological environments. Metabolic labelling incorporates bio-orthogonal handles into cellular biomolecules including glycans, lipids, nucleic acids, and proteins, enabling subsequent selective modification for imaging or capture. Pre-targeting strategies in oncology deliver bio-orthogonal reactive groups to tumour sites using targeting antibodies, followed by administration of bio-orthogonally reactive imaging or therapeutic agents concentrating at tumours. Antibody-drug conjugate manufacturing increasingly employs bio-orthogonal chemistry for site-specific conjugation producing homogeneous products. As reaction rates improve through catalyst development and selectivity expands, bio-orthogonal chemistry continues expanding pharmaceutical applications.