This review offers a comprehensive overview of THF-containing pharmaceuticals, focusing on pharmacological activities, SAR ( structure-activity relationship), and clinical uses. It highlights THF's role in improving solubility, bioavailability, and target binding, and discusses challenges/opportunities in drug discovery.

Tetrahydrofuran (THF), a five-membered cyclic ether with a carbon-oxygen ring structure, is a common solvent and an important functional group in the field of organic synthesis methodology. In addition, THF also plays an important role in drug discovery. The US food and drug administration (FDA) has approved a total of 13 THF-containing drugs for a range of clinical diseases, such as Terazosin and Darunavir. These drugs exhibit superior pharmacological effects in multiple therapeutic fields. This review offers an extensive overview of FDA-approved drugs containing the THF nucleus, emphasizing their pharmacological activities and structure–activity relationships.