It has significant LDL-C lowering potential, minimal potential for CYP3A4 interactions, and low extrahepatic tissue penetration. A completely synthesized HMG-CoA reductase inhibitor is rosuvastatin. Other HMG-CoA reductase inhibitors are either synthetically made from heptanoic acid or naturally produced from mevalonic acid (lovastatin, simvastatin, and pravastatin) (atorvastatin, fluvastatin). A novel class of 3, 5-dihydroxy-heptanoate and N-methane sulfonyl pyrrole-substituted methane sulphonamide pyrimidines include rosuvastatin. Including stable polar methane-sulphonamide group results in low lipophilicity and improved ionic interaction with the HMG-CoA reductase enzyme, enhancing its binding affinity to this enzyme even if the characteristic statin pharmacophore is comparable to that of other statins.
References
Luvai, Ahai, et al. “Rosuvastatin: A Review of the Pharmacology and Clinical Effectiveness in Cardiovascular Disease.†Clinical Medicine Insights: Cardiology, vol. 6, Jan. 2012, p. CMC.S4324, https://doi.org/10.4137/cmc.s4324. ‌
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