Using nanobiotechnology to find new drugs discoveryAuthor(s): Peter Lucas
Although the "rule-of-five" (also known as "Lipinski's rule of drug-likeness") is a very helpful guideline for designing orally accessible small-molecule drugs, it has in some ways been overemphasised. First off, only 51% of all small-molecule medications that have received FDA approval are taken orally and adhere to the "rule-of-five." This doesn't even take into account the growing number of biologicals, some of which have become "blockbuster" hits. Secondly, it does not encompass natural product and semisynthetic natural product medications, which constitute roughly one-third of all marketed small-molecule pharmaceuticals. Instead of relying too heavily on 'rule-of-five' compliance, a more balanced and systematic approach to drug discovery ought to be more fruitful. These are especially important when attempting to combat "best-in-class" and/or extremely difficult targets, such proteases and those involving protein-protein interactions. Additionally, greater work should go into studying natural products. Synthetic biology, which involves genetically altering living things to make small-molecule medicines, may be able to address some of the difficult problems associated with natural product-based drug development, such as synthetic feasibility and ligand efficiency.