Nicolaou on drug development

06 September 2014 - Pharma

It would be a disappointment if someone like K.C. Nicolaou would write an essay on the present and the future of drug development along the lines that everything that is being done is simply fantastic. The opening line of his essay on this very topic in the Angewandte then is not an encouragement: The recent successes of the pharmaceutical enterprise are undeniable and extraordinary (DOI). K.C. Nicolaou does not read blogs. Luckily the text is not devoid of quotable segments.

On strategies : It is particularly disappointing that the human genome project has not as yet had the expected impact on drug discovery, Disappointingly, other developments that started in the 1990s, such as the combinatorial chemistry and high throughput screening of random compound libraries, also failed to impact dramatically the drug discovery and development process.

On conservative and non-innovative organic chemists: it is surprising that so many of the essential experimental techniques employed in laboratories of organic synthesis today are very similar, if not the same, as those employed one or even two generations ago, in contrast to the rather dramatic increase of useful reactions for molecular construction and improvements in analytical instrumentation in the same period.

What does not always work: Several important and long-lasting drugs of natural origin such as Taxol, amphotericin B, and vancomycin, for example, lie outside the rule of five and, in that respect, they are inspiring

And what may work: Interestingly, the first drugs to be approved for use against new targets in recent times are those emerging from research directed toward orphan or rare diseases