Author Archives: mcs1001

Drug discovery approaches to minimise drug induced liver injury in man


The recent literature has seen a flurry of papers describing the issue of, and potential approaches to minimising the incidence of, drug-induced liver injury (DILI) in the clinic.   It is well recognised that attrition throughout the development pipeline is often … Continue reading

Posted in Med Chem Strategy, Toxicology | Tagged , , , , , , , , , , , , , , , , | 3 Comments

More physicochemical musings & ChEMBL


Following on from his earlier papers (e.g. ADMET rules of thumb for candidate drug design), Gleeson’s most recent publication in Nature Reviews|Drug Discovery details a now familiar tale of physicochemical woe associated with the failure of many medicinal chemistry programmes to … Continue reading

Posted in Med Chem Strategy, Reviews, Software | Tagged , , , , , , | 1 Comment

Discovery of MK-1220 (Hepatitis C NS3/4A protease inhibitor)


A recent letter in ACS Med.Chem.Lett. details the optimisation of a series of inhibitors of the Hepatitis C virus (HCV) NS3/4A protease, and is interesting in that it provides detailed pharmacokinetic data for a series of macrocyclic lactones, a class of therapeutic … Continue reading

Posted in Clinical Candidates, Enzyme Inhibitors, Med Chem Strategy | Tagged , , , , , , , , , , , , , , , , , , , , , , , , | 1 Comment