新药创制刍议

On the drug innovation

研发小分子药物可分为两类:首创性药物和模拟创新药物,虽然涵盖的内容相同,但涉及的生物学深度不同。首创性药物靶标有发现和确证的可药性过程,贯穿于研发过程的始终;模拟创新药物则无需确证靶标,而且可以有许多参考和借鉴。模拟创新药物的研发和市场空间日渐缩小,风险加大。以天然产物为先导物的新药创制,应重视有机合成技术的提高和药物化学理念的加强。超小分子药物的复兴是新药研发的一个新动向。

The innovation of newmolecular entities( NME) can be differentiated into two categories: pioneering drugs and follow-on drugs. In spite of having the same contents in drug discovery course,both approaches involve the biological fields to a different extent. Targets for pioneering drugs need a process of target discovery and validation,which always run through the innovation. The discovery of follow-on drugs is not necessary to validate the target,and possesses some information for reference. Nowadays the spaces of innovation and market of follow-on drugs have ever shrunk,and the risk has increased. Based upon natural pro-duct drug discovery the art of total organic syntheses and the conception of medicinal chemistry have to be highly emphasized. The renaissance of ultra-small molecule drugs is one of the NME discoveries.