Innovation of follow-on drugs in drug discovery
Zongru Guo · Zhongguo xin yao zazhi · 2009
Based upon the maturity of drug targets,drug discovery can be differentiated into pioneering and follow-on drug innovation.For realistic reasons,pioneering drugs are unlikely to be the most optimal molecule,which leaves an opportunity for follow-on drugs to exceed.The validated targets,definite SAR and pharmacophoric features make the follow-on approach straightforward and low risky.Drug molecules can be conceived as an assembly of scaffold and pharmacophore.To some extent,follow-on approaches involve molecular operation of altering or modifying the scaffold but maintaining the pharmacophore.By means of isosteric displacement,privileged structure substitution,and scaffold hopping,pharmacodynamic,pharmacokinetic,physico-chemical and safety properties can be optimized in the follow-on drug discovery and development.A new scaffold also endows a molecule novelty.