Nature Reviews Drug Discovery 10, 243-245 (April 2011) | doi:10.1038/nrd3413
The US approval of Human Genome Sciences (HGS) and GlaxoSmithKline's belimumab (Benlysta) on 9 March ended a 50-year drought in the introduction of new lupus drugs. The two firms have blazed a path from mRNA to medicine in 15 years, and analysts are now predicting peak US sales of over US$2 billion annually for the monoclonal antibody (mAb).
Nature Reviews Drug Discovery 10, 307-317 (April 2011) | doi:10.1038/nrd3410
Juswinder Singh, Russell C. Petter, Thomas A. Baillie & Adrian Whitty
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 discovery project. There is a need to reassess this important class of drugs, and to reconcile the discordance between the historic success of covalent drugs and the reluctance of most drug discovery teams to include them in their armamentarium. This Review surveys the prevalence and pharmacological advantages of covalent drugs, discusses how potential risks and challenges may be addressed through innovative design, and presents the broad opportunities provided by targeted covalent inhibitors.
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