Discovery and development of statins trials showed very good inhibitory effect as in clinical trials, however in a long term toxicity study in dogs it resulted in toxic effects at higher doses and as a result was believed to be too toxic to be given to humans. In 1978, Alfred Alberts and colleagues at Merck Research Laboratories discovered a new natural product in a fermentation broth of "Aspergillus terreus", their product showed good HMGR inhibition and they named the product mevinolin, which later became known as lovastatin. The cholesterol controversy began in the early promotion of statins. Statins are a competitive antagonists of HMG CoA,
Discovery and development of statins electronegative sulfone group on rosuvastatin makes it the statin that has the greatest number of bonding interactions with HGMR. All statins have the same pharmacophore so the difference in their pharmacodynamic effect is mostly based on the substituents. The activity of each statin is dependent on the binding affinity of the compound for the substrate site and the length of time it binds to the site. Type 2 statins have unique fluorophenyl group that causes additional polar interaction between the enzyme and the statins, which results in a tighter binding to the enzyme. The newest statin, rosuvastatin has a unique