Pitavastatin

Pitavastatin
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 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 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

  • 1 Uses
  • 2 Side-effects
  • 3 Metabolism and interactions
  • 4 History
  • 5 References
  • 6 External links
  • 7 External links

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

  1. ^ 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.
  2. ^ Zydus Cadila launches pitavastatin in India
  3. ^ 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

v • d • e
Lipid modifying agents (C10)
GI tract
Cholesterol absorption inhibitor, NPC1L1
Ezetimibe • SCH-48461
Bile acid sequestrants/resins (LDL)
Cholestyramine • Colestipol • Colestilan • Colextran • Colesevelam
Liver
Statins (HMG-CoA reductase, LDL)
Simvastatin# • Atorvastatin • Fluvastatin • Lovastatin • Mevastatin • Pitavastatin • Pravastatin • Rosuvastatin • Cerivastatin‡
Niacin and derivatives (HDL and LDL)
Niceritrol • Niacin • Nicofuranose • Aluminium nicotinate • Nicotinyl alcohol • Acipimox
Blood vessels
Fibrates (PPAR)
Clofibrate‡ • Bezafibrate • Aluminium clofibrate • Gemfibrozil • Fenofibrate • Simfibrate • Ronifibrate • Ciprofibrate • Etofibrate • Clofibride • Clinofibrate
CETP inhibitors (HDL)
Anacetrapib† • Torcetrapib§ • JTT-705
Combinations
Niacin/lovastatin • Niacin/simvastatin • Ezetimibe/simvastatin • Niacin/laropiprant
Other
Dextrothyroxine • Probucol • Tiadenol • Benfluorex • Meglutol • Omega-3-triglycerides • Magnesium pyridoxal 5-phosphate glutamate • Policosanol • Lapaquistat§ • Alipogene tiparvovec
#WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III

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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article http://en.wikipedia.org/wiki/Pitavastatin. Additionally, in some cases elements from this article might be licensed under a different license. Please refer to the original article to check the license status http://en.wikipedia.org/wiki/Pitavastatin.