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Pitavastatin calcium

Statin lipid-lowering drugs Pharmacological effects Pharmacokinetics Toxicity Clinical Study
Pitavastatin calcium
Pitavastatin calcium structure
CAS No.
147526-32-7
Chemical Name:
Pitavastatin calcium
Synonyms
nk104;D01862;nk104(acid);ITAVASTATIN CA;NK-104 Calcium;Pitavastatin Calciu;ITAVASTATIN CALCIUM;Pitavasttin Calcium;Pitavastatin Calcuim;PITAVASTATIN CALCIUM
CBNumber:
CB6375308
Molecular Formula:
C50H46CaF2N2O8
Formula Weight:
880.98
MOL File:
147526-32-7.mol

Pitavastatin calcium Properties

alpha 
D20 +23.1° (c = 1.00 in acetonitrile/water)
CAS DataBase Reference
147526-32-7(CAS DataBase Reference)
FDA UNII
IYD54XEG3W
SAFETY
  • Risk and Safety Statements
Safety Statements  24/25
HS Code  29339900
Toxicity LDLo orl-rat: 500 mg/kg OYYAA2 56,67,1998

Pitavastatin calcium price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 15414 Pitavastatin (calcium salt) ≥98% 147526-32-7 10mg $49 2020-06-24 Buy
Cayman Chemical 15414 Pitavastatin (calcium salt) ≥98% 147526-32-7 25mg $80 2020-06-24 Buy
Cayman Chemical 15414 Pitavastatin (calcium salt) ≥98% 147526-32-7 50mg $135 2020-06-24 Buy
Cayman Chemical 15414 Pitavastatin (calcium salt) ≥98% 147526-32-7 100mg $221 2020-06-24 Buy

Pitavastatin calcium Chemical Properties,Uses,Production

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.

Pharmacological effects

Inhibition 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.

Toxicity

Acute 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 Study

In 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.

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.

Chemical Properties

White to Off-White Powder

Originator

Nissan (Japan)

Uses

A competitive inhibitor of HMG-CoA reductase.

Uses

Pitavastatin calcium (Livalo) is a novel member of the medication class of statins

Definition

ChEBI: 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 name

Livalo

Hazard

A poison by ingestion.

Safety Profile

A poison by ingestion.Experimental reproductive effects. When heated todecomposition it emits toxic vapors of NOx and Fí.

Pitavastatin calcium Preparation Products And Raw materials

Raw materials

Preparation Products


Pitavastatin calcium Suppliers

Global( 285)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21821 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 568 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58
Jinan Chenghui-Shuangda Chemical Co.,Ltd
+86-531-58897082
+86-531-58897093 ericqiao@jnchsd.com CHINA 157 58
SHANDONG ZHI SHANG CHEMICAL CO.LTD
+86 18953170293
+86 0531-67809011 sales@sdzschem.com CHINA 2995 58
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23977 58

View Lastest Price from Pitavastatin calcium manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-05-11 Pitavastatin calcium
147526-32-7
US $0.00-0.00 / KG 1KG 99.0% 500 MT Shaanxi Dideu Medichem Co. Ltd
2019-12-31 Pitavastatin calcium
147526-32-7
US $1.00 / KG 1KG 95-99% 1ton Career Henan Chemical Co
2018-08-16 Pitavastatin calcium
147526-32-7
US $7.00 / KG 1KG 99% 1000KG career henan chemical co

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