Pitavastatin
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| Trade names | Livalo, Livazo |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a610018 |
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| Routes of administration |
By mouth (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | 60% |
| Protein binding | 96% |
| Metabolism | Liver (CYP2C9, minimally) |
| Biological half-life | 11 hours |
| Excretion | Faeces |
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| ECHA InfoCard | 100.171.153 |
| Chemical and physical data | |
| Formula | C25H24FNO4 |
| Molar mass | 421.461 |
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Pitavastatin (usually as a calcium salt) is a member of the blood cholesterol lowering medication class of statins, marketed in the United States under the trade name Livalo, and in European Union and Russia under the trade name Livazo. Like other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis.
It has been available in Japan since 2003, and is being marketed in South Korea and in India. It is expected that pitavastatin will be approved outside Southeast Asia as well. In the US, it received FDA approval in 2009.Kowa Pharmaceuticals is the owner of the American patent to pitavastatin.
Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease.
A 2009 study of the 104 week LIVES trial found pitavastatin increased HDL cholesterol, especially in patients with HDL lower than 40 mg/dL, who had a 24.6% rise, in addition to greatly reducing LDL cholesterol 31.3%. HDL improved in patients who switched from other statins and rose over time. In the 70-month CIRCLE observational study, pitavastatin increased HDL more than atorvastatin.
It has neutral or possibly beneficial effects on glucose control. As a consequence, pitavastatin is likely to be appropriate for patients with metabolic syndrome plus high LDL, low HDL and diabetes mellitus.
Common statin-related side effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins. However, pitavastatin seems to lead to fewer muscle side effects than certain statins that are lipid-soluble, as a result of the fact that pitavastatin is water-soluble (as is pravastatin, for example). One study found that coenzyme Q10 was not reduced as much as with certain other statins (though this is unlikely given the inherent chemistry of the HMG-CoA reductase pathway that all statin drugs inhibit).
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