Pitavastatin Calcium is the calcium salt formulation of Pitavastatin, a lipophilic statin that inhibits cholesterol synthesis and displays cardioprotective properties. Pitavastatin is often combined with zoledronic acid for oncology applications. It was discovered by Nissan Chemical Industries (Japan) and developed further by Kowa Pharmaceuticals (Tokyo) and patented in 1987 by Kowa Pharmaceuticals.
Pitavastin is soluble in DMSO and DMF but sparingly soluble in aqueous buffers.
| Mechanism of Action |
Pitavastatin is a competitive inhibitor of the enzyme that catalyzes the first step in cholesterol synthesis known as hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase. This enyzme catalyzes the conversion of HMG-CoA to mevalonic acid, the third step in a series of reactions that produce many compounds in lipid metabolism and transport including cholestrol, low-density lipoprotein (LDL), and very-low density lipoprotein (VLDL). Pitavastatin has pleiotropic effects including anti-inflammatory, antioxidant, immunomodulatory, anti-apoptotic, anti-cancer, and angiogenesis-regulating properties. It is an interesting molecule with many effects, and supports several research applications. |
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Cancer Applications |
Pitavastatin is superior to other statins for oncology research because it is the only statin that is both lipophilic and has a suitably long half-life. Pitavastatin was found to inhibit the growth of ovarian cancer cell cultures. Combinations with zoledronic acid displayed additive or synergistic effects in 10 of 11 cell lines tested (Abdullah et al, 2017). Interleukin 33 (IL-33) is a cytokine that plays a complex role in cancer development. In human pancreatic tissue samples, IL-33 was over-expressed in samples from patients with chronic pancreatitis and pancreatic cancer compared with normal pancreatic tissue. Pitavastin reduced the onset of pancreatitis in mice and human tissue via suppression of IL-33 expression (Park et al, 2024). |
| Molecular Formula |
C50H46F2N2O8 • Ca |
| References |
Abdullah, MI et al. (2017) Inhibition of the mevalonate pathway augments the activity of Pitavastatin against ovarian cancer cells. Scientific Rep. 8090 Isley WL (2001) Pitavastatin (NK-104), a new HMG-CoA reductase inhibitor. Drugs Today (Barc). 37(9):587-594 PMID 12743630 Park J et al (2024) Statin prevents cancer development in chronic inflammation by blocking interleukin 33 expression. Nature Comm. 15(1) Sahebkar A et al (2021) A comprehensive review on the lipid and pleiotropic effects of Pitavastatin. Prog. Lipid Res. 84:101127 PMID 34509516 Saka M et al. (2006) Pitavastatin improves cardiac function and survival in association with suppression of the myocardial endothelin system in a rat model of hypertensive heart failure. J. Cardiovasc. Pharmacol. 47:770-779 |
