There are catalysis geniuses (looking at you, process chemists!) and then there are those of us just looking to put compounds in vials. Here are the simplest conditions that’ll get you what you want 90% of the time. Beyond that you’ll need to ask a guru like Nick White or Malcolm Huestis. Hope this helps. …
When interpreting compound pharmacokinetic (PK) data, it’s helpful to have reference values to compare experimental data to. A compound with a measured rat clearance value of 0.3 L/hr/kg, for example, is being removed at a slow rate relative to rat liver blood flow (3.3 L/hr/kg), indicating that the compound is not rapidly metabolized or excreted …
Of the record 59 FDA drug approvals from 2018, the majority were small molecules (64%). Keep at it, chemists! 🙂 Oncology and infectious diseases were the areas with most small molecule approvals, followed by genetic/rare diseases. Some more statistics below. Last year the FDA approved a record 59 novel drugs, which included 38 small molecule …
Modern hit-finding technologies are incredible. Dean Brown and Jonas Bostrom at AstraZeneca have a very nice review out summarizing the hit-finding strategies for 66 clinical candidates published from 2016-2017. Some highlights include a clinical candidate from DNA-encoded libraries at GSK, the discovery of an RNA-binding drug candidate by PTC/Roche, and fragment-based programs with candidates 100,000x …
Where Do Recent Small Molecule Clinical Candidates Come From? Read More »