Introduction: The design of target-specific covalent inhibitors is conceptually attractive
because of increased biochemical efficiency through covalency and increased duration of …

Covalent drugs haveproved to be successful therapies for various indications, but largely
owing to safety concerns, they are rarely considered when initiating a target-directed drug …

In recent years, the number of drug candidates with a covalent mechanism of action
progressing through clinical trials or being approved by the FDA has increased significantly …

Highlights•High potencies and prolonged effects achievable with covalent drugs may result
in less frequent dosing and improved therapeutic margins for patients.•Covalent inhibition …

Covalent inhibitors are recognized as an important component in drug discovery and
therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the …

In the history of therapeutics, covalent drugs occupy a very distinct category. While
representing a significant fraction of the drugs on the market, very few have been …

Targeted covalent enzyme inhibition is experiencing resurgence as a medicinal chemistry
design strategy. Targeted covalent inhibitors exhibit slow target offset, increased binding …

In the first decade of targeted covalent inhibition, scientists have successfully reversed the
previous trend that had impeded the use of covalent inhibition in drug development …

Covalent drugs have a long history and such medicines are used for diverse therapeutic
indications. Prominent blockbuster drugs relying on covalent target engagement include …

Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …