Pitavastatin calcium

한글명:Pitavastatin calcium

카스 번호147526-32-7

상품명:Pitavastatin calcium

CBNumberCB6375308

분자식C25H26CaFNO4

포뮬러 무게463.56

MOL 파일147526-32-7.mol

화학적 성질

녹는점	>138oC (dec.)
알파	D20 +23.1° (c = 1.00 in acetonitrile/water)
저장 조건	2-8°C
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 황백색까지
안정성	흡습성
InChIKey	ADXNRJCYUMOXPZ-MNGIKBOWNA-N
SMILES	C(/C1C(C2CC2)=NC2C=CC=CC=2C=1C1C=CC(F)=CC=1)=C\[C@@H](O)C[C@@H](O)CC(=O)O.[Ca] \|&1:22,25,r\|
CAS 데이터베이스	147526-32-7(CAS DataBase Reference)

위험 및 안전 성명

안전지침서

24/25

HS 번호

29339900

독성

LDLo orl-rat: 500 mg/kg OYYAA2 56,67,1998

NFPA 704:

	0
2		0

그림문자(GHS)

Pitavastatin calcium 화학적 특성, 용도, 생산

개요
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.
화학적 성질
White to Off-White Powder
용도
Pitavastatin calcium (Livalo) is a novel member of the medication class of statins
정의
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.
위험도
A poison by ingestion.
Safety Profile
A poison by ingestion.Experimental reproductive effects. When heated todecomposition it emits toxic vapors of NOx and Fí.

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