Pitavastatin
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| Systematic (IUPAC) name | |
| (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid | |
| Identifiers | |
| CAS number | 147511-69-1 |
| ATC code | C10AA08 |
| PubChem | CID 6366718 |
| Chemical data | |
| Formula | C25H24FNO4 |
| Mol. mass | 421.461 |
| Pharmacokinetic data | |
| Bioavailability | 60% |
| Protein binding | 96% |
| Metabolism | hepatic |
| Half-life | 11 hours |
| Excretion | biliary |
| Therapeutic considerations | |
| Pregnancy cat. | X |
| Legal status | prescription |
| Routes | oral tablets 1, 2, & 4 mg |
Pitavastatin (usually as a calcium salt) is a novel member of the medication class of statins.1 Like the 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 under licence in South Korea and in India.2 It is likely that pitavastatin will be approved for use in hypercholesterolaemia (elevated levels of cholesterol in the blood) and for the prevention of cardiovascular disease outside South and Southeast Asia as well.3
Contents
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Uses
Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease.
Side-effects
Common statin-related side-effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins.3
Metabolism and interactions
Most statins are metabolised in part by one or more hepatic cytochrome P450 enzymes, leading to an increased potential for drug interactions and problems with certain foods (such as grapefruit juice). Pitavastatin appears to be a substrate of CYP2C9, and not CYP3A4 (which is a common source of interactions in other statins).3
History
Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) was discovered in Japan by Nissan Chemical Industries, Ltd. and developed further by Kowa Pharmaceuticals, Tokyo.3 Pitavastatin was recently approved for use in the United States by the FDA on 08/03/2009 under the trade name Livalo.
References
- ^ Kajinami K, Takekoshi N, Saito Y. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev 2003;21:199-215. PMID 12931254.
- ^ Zydus Cadila launches pitavastatin in India
- ^ a b c d Mukhtar RY, Reid J, Reckless JP. Pitavastatin. Int J Clin Pract 2005;59:239-52. PMID 15854203.
External links
- FDA approval history
External links
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