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Pitavastatin calcium

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Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-55531817
Products Intro: Product Name:Pitavastatin calcium
Purity:99% Package:100g,500g,1kg,5kg,10kg
Company Name: Beijing Cooperate Pharmaceutical Co.,Ltd
Tel: 010-60279497
Products Intro: Product Name:Pitavastatin Calcium
Purity:98% Package:100G;1KG;5KG;10KG;25KG;50KG;100KG
Company Name: Henan Tianfu Chemical Co.,Ltd.
Tel: 0371-55170693
Products Intro: Product Name:Pitavastatin calcium
Purity:0.99 Package:25KG,5KG;1KG;500G
Company Name: Shanghai Yingrui Biopharma Co., Ltd.
Tel: +86-21-33585366
Products Intro: Product Name:Pitavastatin calcium
Purity:99% Package:100g;500g;1kg;25kg...
Company Name: Hubei XinRunde Chemical Co., Ltd.
Tel: +8615102730682; +8618874586545
Products Intro: Product Name:147526-32-7 Pitavastatin Calcium
Purity:99% Package:1KG;10USD

Lastest Price from Pitavastatin calcium manufacturers

  • pitavastatin calcium
  • US $2.60 / KG
  • 2020-09-28
  • CAS:147526-32-7
  • Min. Order: 1g
  • Purity: 99%
  • Supply Ability: 9999KGs
  • Pitavastatin calcium
  • US $0.00-0.00 / KG
  • 2020-05-12
  • CAS:147526-32-7
  • Min. Order: 1KG
  • Purity: 99.0%
  • Supply Ability: 500 MT
  • Pitavastatin calcium
  • US $1.00 / KG
  • 2020-01-01
  • CAS:147526-32-7
  • Min. Order: 1KG
  • Purity: 95-99%
  • Supply Ability: 1ton
Pitavastatin calcium Basic information
Statin lipid-lowering drugs Pharmacological effects Pharmacokinetics Toxicity Clinical Study
Product Name:Pitavastatin calcium
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
Product Categories:Livalo;API;chemical;Pharmaceuticals;Cardiovascular Series;Active Pharmaceutical Ingredients;Inhibitors;Intermediates & Fine Chemicals
Mol File:147526-32-7.mol
Pitavastatin calcium Structure
Pitavastatin calcium Chemical Properties
alpha D20 +23.1° (c = 1.00 in acetonitrile/water)
CAS DataBase Reference147526-32-7(CAS DataBase Reference)
Safety Information
Safety Statements 24/25
HS Code 29339900
ToxicityLDLo orl-rat: 500 mg/kg OYYAA2 56,67,1998
MSDS Information
Pitavastatin calcium Usage And Synthesis
Statin lipid-lowering drugsPitavastatin calcium is jointly developed by two companies Nissan Chemical and Kowa 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.
Pharmacological effectsInhibition of HMG-CoA reductase: pitavastatin calcium has a strongly antagonistic inhibition effect on HMG-CoA enzyme , IC50 value is 6.8 nmol/L, and its intensity is 24 times of simvastatin, while it is 68 times of fluvastatin.
It Hinders the synthesis of cholesterol: the ability to effectively inhibit the process of generating cholesterol in human hepatocytes HepG2 , IC50 value is 5.8nmol/L, and its intensity is 29 times of simvastatin, it is 57 times that of atorvastatin. But pitavastatin calcium inhibition effect on each enzyme in cholesterol generation after generation of mevalonate is very weak.
It Increases LDL receptor density: pitavastatin induces the synthesis of LDS receptor mRNA in the ultra-low concentration of 1μmol/L, it can increase the number of LDS receptor mRNA , it results in the increasing of LDL receptor density , thereby it promotes clearance of LDL , so that plasma LDL-plasma total cholesterol concentration and triglyceride concentration decrease.
The above information is edited by the Chemicalbook of Tian Ye.
Pharmacokinetics The main parts of its absorption after oral administration are the duodenum and colon,its rate of binding plasma protein in the body is 96%and it is more selectively distributed in the liver after absorption , the drug concentration in body tissues is lower than that in the plasma or the same as that in the plasma . Pitavastatin calcium is mainly metabolized in the liver, kidney, lung, heart, muscle , metabolite concentrations are lower than the concentration of drug prototype, it is excreted through feces,there is also a small amount of drug excretion through urine , total excretion rate is almost 100%.
A healthy male adult oral pitavastatin is 0.5~8mg, t1/2 is about 10h,the cmax and AUC of the prototype drug in plasma increase with increasing dose , repeatedly taking does not result in medication savings.
ToxicityAcute toxicity: rats and dogs oral,study its acute toxicity. Pitavastatin calcium median lethal dose on the rats are about male 500~1000mg/kg, female 250~500 mg/kg, dogs lethal dose is about 50~100mg/kg.
Long term toxicity: respectively, rats, dogs and monkeys are administered a long-term experiment. From the experimental results, the safe dose of pitavastatin calcium are rats 1 mg/kg · d-1 (6 months), canine 0.3mg/kg · d-1 (12 months), monkey 3mg/kg · d-1 (6 months). No central nervous system, reproductive system, and myocardial dysfunction is observed which is common while taking other statins during administration.
Carcinogenicity, mutagenicity: mouse oral 1,12,30, 75mg/kg dose, the incidence of cancer has no significant increase than in the control group .in Chromosome abnormality tests, at the highest concentration of 625μg/ml,the result is positive, but at the same concentration, gene mutation recovery tests, micronucleus test s(in vivo) and UDS test s(in vivo) are negative.
Clinical StudyIn the therapeutic effect, statins is the first In the lipid-lowering drugs in which pitavastatin effect is very obvious, pitavastatin calcium is a third generation statins anti-hyperlipidemia drug, and Russell atorvastatin (rosuvastatin ) while being called "super statin", is one of the better statins which are current international clinical application of the treatment of hypercholesterolemia, familial hypercholesterolemia , because its clinically effective dose is 1-2mg/day, significantly lower than other marketed statins, with high efficiency, and security features, it has a good tolerability. clinical trail phase I results show that pitavastatin calcium in 1,2,4 mg dose has clinical significance in patients with high blood cholesterol.
Results of clinical trail phase Ⅱ determine that the best dosage of the pitavastatin calcium for the treatment of hyperlipidemia is 2mg/d.
clinical trail phaseⅢ comparison of experimental results show that the efficacy of pitavastatin calcium on reducing Tc and LDL-c is better than the effect of fluvastatin, and there is no significant difference in safety. Multi-center long-term administration tests carried out in Japan show that the dosage in 1~4mg/d range can effectively control blood lipid levels. The above test results demonstrate the effectiveness of pitavastatin calcium in treatment of hyperlipidemia on clinic.
DescriptionPitavastatin, 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.
Chemical PropertiesWhite to Off-White Powder
OriginatorNissan (Japan)
UsesA competitive inhibitor of HMG-CoA reductase.
UsesPitavastatin calcium (Livalo) is a novel member of the medication class of statins
DefinitionChEBI: The calcium salt of pitavastatin. Used for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.
Brand nameLivalo
HazardA poison by ingestion.
Safety ProfileA poison by ingestion.Experimental reproductive effects. When heated todecomposition it emits toxic vapors of NOx and Fí.
Pitavastatin calcium Preparation Products And Raw materials
Tag:Pitavastatin calcium(147526-32-7) Related Product Information
(E)-3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl-2-propenal (3S,5S,6E)-7-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-6-heptenoic Acid CalciuM Salt (3S,5R,6E)-7-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-6-heptenoic acid (3S,5R,6E)-7-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-6-heptenoic Acid CalciuM Salt 3-(Bromomethyl)-2-cyclopropyl-4-(4'-fluorophenyl)quinoline Calcium dobesilate Lapatinib Bortezomib VINBLASTINE Selumetinib Fluvastatin sodium salt Rosuvastatin calcium (4R,6S)-6-[(1E)-2-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]ethenyl]-2,2-dimethyl-1,3-dioxane-4-acetic acid tert-butyl ester Calcium Quinoline Pitavastatin 3-HEPTENOIC ACID INTERMEDIATES OF PITAVASTATIN CALCIUM