New Trends in Drug Discovery
Gerd Schnorrenberg · 2018
This chapter highlights some trends in new chemical entities (NCEs), and new biological entities (NBEs) discovery, which should reflect the growing experience in both fields. At the beginning of every NCE drug discovery effort stands the question of how to identify a pharmacophoric model of interaction with a therapeutic target. The high proportion of NCEs in newly approved drugs in 2015 (61%) is clear evidence of a regain of efficiency and success rates in NCE discovery. The chapter focuses on mainly two aspects that contribute substantially to increased success rates: enhanced hit/lead generation strategies and enhanced characterization of development candidates reducing compound-related attrition rates. It gives a short overview on improvements in drug metabolism and pharmacokinetic (DMPK) characterization, tolerability assessment, and physicochemical characterization of compounds during lead optimization with the goal of generating high quality candidates for progression into preclinical and clinical phases.