Pitavastatin calcium

Pitavastatin calcium is a novel member of the medication class of statins. The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis. Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM) . It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions. Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure. (In Vitro) :Pitavastatin Calcium inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50 = 0.4-5 μM) or as spheroids (IC50=0.6-4 μM) .Pitavastatin Calcium (1 μM; 48 hours) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells.Pitavastatin (1 μM, 48 hours) causes PARP cleavage in Ovcar-8 cells. (In Vivo) :Pitavastatin Calcium (59 mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression.