Pitavastatin Calcium Basic information
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Product Name: |
Pitavastatin calcium |
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Synonyms: |
Pitavasttin Calcium;Pitavastatin Calcium /NK-104;(+)-Monocalciunbis{(3r,5s,6e)-7-[2-cyclopropyl-4-(4-fluorophenyl-3-quinolyl]-3,5-dihydroxy-6-heptenotate};Pitavastatin calciuM(Livalo);Calcium (3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl)-3,5-dihydroxyhept-6-enoate;(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-6-heptenoic acid,calcium salt (2:1);NK-104 Calcium;Pitavastatin CalciuM DISCONTINUED |
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CAS: |
147526-32-7 |
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MF: |
C50H46CaF2N2O8 |
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MW: |
463.56 |
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EINECS: |
807-641-2 |
Pitavastatin Calcium Chemical Properties
| Melting point | >138oC (dec.) |
| alpha | D20 +23.1° (c = 1.00 in acetonitrile/water) |
| storage temp. | 2-8°C |
| solubility | DMSO (Slightly), Methanol (Slightly) |
| form | Solid |
| color | White to Off-White |
| Stability: | Hygroscopic |
Pitavastatin Calcium Usage And Synthesis
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Statin lipid-lowering drugs |
Pitavastatin calcium is jointly developed by two companies Nissan Chemical and Kowa Co.it is the first total synthesis HMG-CoA reductase inhibitor, it belongs to statin drugs ,it reduces the ability of the liver to manufacture cholesterol mainly through inhibition of some liver enzymes called HMGCo-A reductase , thus it improves the elevated blood cholesterol levels, it is primarily used for the treatment of hypercholesterolemia and familial hypercholesterolemia patients,its lipid-lowering effect is very good, it is the most potent lipid-lowering drug so far. |
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Description |
Pitavastatin, launched for the treatment of hypercholesterolemia, belongs to the family of second-generation statins, also referred to as superstatins due to their improved efficacy as cholesterol lowering agents. Like other statins, pitavastatin reduces plasma cholesterol levels by competitively inhibiting HMG-CoA reductase, the rate-limiting enzyme of cholesterol biosynthesis in the liver. It is a more potent inhibitor of HMG-CoA reductase than the previously marketed statins and has the potential benefit of not undergoing significant metabolism by CYP3A4. Pitavastatin is synthesized in a multi-step sequence, including the key step of introducing the dihydroxyheptenoate side chain by cross-coupling of a 3-iodoquinoline intermediate with an alkenylborane reagent. Unlike rosuvastatin, pitavastatin has a high oral bioavailability (～80%). Plasma protein binding is also high for pitavastatin (＞95%), and regardless of the dosing, the highest tissue levels are found in the liver, its target organ. After oral administration, the peak plasma concentration is reached at ,0.8 h and the mean elimination half-life is ～11 h. Pitavastatin is only minimally metabolized, mainly by CYP2C8 and CYP2C9, and the predominant route of elimination of the parent drug and its metabolites is by means of bile excretion followed by elimination in the feces. In clinical studies, oral doses of 2–4 mg/day of pitavastatin produced dose-dependent reduction in LDL-cholesterol levels by 40–48% from baseline in patients with heterozygous familial hypercholesterolemia. In a 12-week double-blind comparative study, pitavastatin (2 mg/day) was more effective than pravastatin (10 mg/day) in reducing LDL-cholesterol levels (38 and 18%, respectively); however, both agents produced similar increases in HDL-cholesterol (～9%). The drug was well tolerated and the adverse reactions were mild and transient. |
| Appearance | White to Off-White Powder |
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Use |
A potent inhibitor of HMG-CoA reductase |
Pharmacological effects
1. Inhibition of HMG-CoA reductase: Pitavastatin calcium has strong antagonistic inhibitory effect on HMG-CoA enzyme, IC50 value is 6.8nmol/L, its action intensity is 24 times that of simvastatin, 68 times that of fluvastatin.
2. Block the synthesis of cholesterol: It can effectively inhibit the process of cholesterol production in human hepatocytes HepG2, IC50 value is 5.8nmol/L, its action intensity is 29 times that of simvastatin, Chemicalbook is 57 times that of vastatin. However, the inhibitory effect of pitavastatin calcium on the enzymes in the process of cholesterol production after mevalonate production is very weak.
3. Increase LDL receptor density: Pitavastatin can induce the synthesis of LDS receptor mRNA at an ultra-low concentration of 1μmol/L, which increases the number of LDS receptor mrna and leads to the increase of LDL receptor density, thereby promoting LDL clearance and reducing plasma LDL-cholesterol concentration and plasma total triglyceride concentration.
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