<p>Lovastatin is given as a lactone prodrug and thus, in order to produce its mechanism of action, it is required to be converted to the active beta-hydroxy form. This drug activation process does not seem to be related to CYP isoenzyme activity<sup class="text-reference-group"><a class="reference-popover-link" data-content="Whirl-Carrillo M, McDonagh EM, Hebert JM, Gong L, Sangkuhl K, Thorn CF, Altman RB, Klein TE: Pharmacogenomics knowledge for personalized medicine. Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96. (PubMed ID 22992668)" href="#reference-A414">7</a></sup> but rather to be controlled by the activity of serum paraoxonase.<sup class="text-reference-group"><a class="reference-popover-link" data-content="Draganov DI, Stetson PL, Watson CE, Billecke SS, La Du BN: Rabbit serum paraoxonase 3 (PON3) is a high density lipoprotein-associated lactonase and protects low density lipoprotein against oxidation. J Biol Chem. 2000 Oct 27;275(43):33435-42. (PubMed ID 10931838)" href="#reference-A15320">11</a></sup></p><p>Lovastatin is metabolized by the microsomal hepatic enzyme system (Cytochrome P-450 isoform 3A4). The major active metabolites present in human plasma are the β-hydroxy acid of lovastatin, its 6'-hydroxy, 6'-hydroxymethyl, and 6'-exomethylene derivatives.<sup class="text-reference-group"><a class="reference-popover-link" data-content="Health Canada Monograph - Lovastatin" href="#reference-F4664">44</a></sup> The uptake of lovastatin by the liver is enhanced by the activity of OATP1B1.<sup class="text-reference-group"><a class="reference-popover-link" data-content="Neuvonen PJ, Backman JT, Niemi M: Pharmacokinetic comparison of the potential over-the-counter statins simvastatin, lovastatin, fluvastatin and pravastatin. Clin Pharmacokinet. 2008;47(7):463-74. doi: 10.2165/00003088-200847070-00003. (PubMed ID 18563955)" href="#reference-A35026">9</a></sup> </p><p class="d-none d-sm-block"><strong>Hover over products below to view reaction partners</strong></p>