Covalent inhibitor drugs

a reversible covalent inhibitor

Source: Nature Chemical Biology

Exceptions to a long-held rule against chemically bonding to biological targets are powering new cancer medicines, finds Andy Extance

Most drugs work by targeting an active site in an enzyme, but some do more than just target: they irreversibly covalently bond to it. For a long time, this was thought to be a serious problem, but now some companies are actively trying to design drugs that bind permanently to their targets. Drug companies Principia, Pfizer and Eli Lilly are working on this, often with academics at institutions such as The Scripps Research Institute and the University of California, San Francisco.