Applications

Rufinamide, developed by Eisai, gained FDA approval in November 2008 for Lennox-Gastaut syndrome seizures. Its 1,2,3-triazole improves metabolic stability and target binding, enhancing oral bioavailability and reducing drug metabolism liabilities.

Originally from Eli Lilly and approved by Vanda in Dec 2025, tradipitant prevents motion-induced vomiting as an NK1 antagonist. The triazole ring reinforces receptor interactions, optimizing potency while lowering off-target toxicity for better druggability.

Developed by Cempra, this ketolide treats community-acquired bacterial pneumonia. The triazole-phenylamine group strengthens ribosomal binding, overcomes macrolide resistance and improves aqueous solubility to elevate antibacterial druggability.

Trodelvy (Sacituzumab govitecan), initially developed by Immunomedics (acquired by Gilead), obtained FDA accelerated approval in April 2020 for metastatic triple-negative breast cancer.

Spatially selective surface crosslinking of superabsorbent polymer (SAP) particles can be realized by virtue of CuAAC click chemistry.

The novel anti-tuberculosis agent CMX4103 features a SuFEx warhead that forms a covalent bond with the Pks13 enzyme of Mycobacterium tuberculosis, leading to irreversible inhibition of its enzymatic function. This mechanism underpins its potent activity against a broad spectrum of Mycobacterium tuberculosis strains, including those resistant to currently available drugs.

Through the SuFEx reaction, highly efficient and selective covalent ligation between biomacromolecules can be achieved in living systems, including protein–protein, protein–polysaccharide, and nucleic acid–protein conjugation.

Polysulfate materials are efficiently constructed via SuFEx click chemistry, a versatile sulfur–fluorine exchange reaction enabling modular polymer assembly.