Lopinavir

한글명:Lopinavir

카스 번호192725-17-0

상품명:Lopinavir

CBNumberCB3663640

분자식C37H48N4O5

포뮬러 무게628.81

MOL 파일192725-17-0.mol

화학적 성질

녹는점	255.2-260.6 °F (124—127°C)
끓는 점	924.1±65.0 °C(Predicted)
밀도	1.163±0.06 g/cm3(Predicted)
저장 조건	2-8°C
용해도	DMSO: 용해성20mg/mL, 투명
산도 계수 (pKa)	13.89±0.46(Predicted)
물리적 상태	가루
색상	흰색에서 베이지색
optical activity	[α]/D -20 to -27°, c = 0.4 in methanol
안정성	흡습성
CAS 데이터베이스	192725-17-0(CAS DataBase Reference)

위험 및 안전 성명

유엔번호(UN No.)

3077

HS 번호

29335990

유해 물질 데이터

192725-17-0(Hazardous Substances Data)

NFPA 704:

	0
2		0

그림문자(GHS)

Lopinavir 화학적 특성, 용도, 생산

개요
Lopinavir, the sixth HIV protease inhibitor in the “navir” class, was launched in coformulation with ritonavir, another HIV protease inhibitor already marketed (Abbott, 1996); this original formulation was introduced as Kaletra for use in combination with either nucleoside or non-nucleoside reverse transcriptase inhibitors for the treatment of AIDS in adults and children. Lopinavir is a peptidomimetic compound with a structural core identical to that of ritonavir, on which terminal groups, particularly a modified valine, were introduced by peptide coupling procedures. Lopinavir is a potent competitive inhibitor of HIV-I protease exhibiting high potential against ritonavir-resistant mutations. In several animal species, pharmacokinetic studies with the lopinavirlritonavir association showed that the modest properties of lopinavir were significantly improved in presence of ritonavir, in terms of Cmax and duration of action. Ritonavir inhibits the P450 isoenzyme CYP3A4 and the human liver microsomal metabolism of lopinavir, so strongly amplifying plasma levels of this latter component. In AIDS patients, the plasma HIV RNA level was considerably reduced and the CD4+ T-cell counts increased after administration of lopinavir combined with relatively small doses of ritonavir. Kaletra is intended to be used jointly with other antiretroviral agents.
화학적 성질
Lopinavir is a white to light tan powder. It is freely soluble in methanol and ethanol, soluble in isopropanol and practically insoluble in water.
용도
Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM
정의
ChEBI: Lopinavir is a dicarboxylic acid diamide that is amphetamine is substituted on nitrogen by a (2,6-dimethylphenoxy)acetyl group and on the carbon alpha- to nitrogen by a (1S,3S)-1-hydroxy-3-{[(2S)-3-methyl-2-(2-oxotetrahydropyrimidin-1-yl)butanoyl]amino}-4-phenylbutyl group. An antiretroviral of the protease inhibitor class, it is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir. It has a role as an antiviral drug, a HIV protease inhibitor and an anticoronaviral agent. It is a member of amphetamines and a dicarboxylic acid diamide.
Indications
Lopinavir is available in the United States only as a fixed-dose combination with ritonavir (Kaletra). In this regimen, a low dose of ritonavir is used to inhibit the rapid inactivation of lopinavir by CYP3A4.
Antimicrobial activity
Lopinavir is active against HIV-1 and HIV-2.
원료
Significant resistance to the antiretroviral efficacy of ritonavirbooted lopinavir occurs as a result of amino acid substitutions at positions 32, 47 and 82 in the protease region. Protease inhibitor resistance is uncommon in patients identified with early failure of combination therapy with ritonavir boostedlopinavir and nucleotide reverse transcriptase inhibitors.
일반 설명
Lopinavir is a protease inhibitor that has been approved foruse in combination with ritonavir for patients with HIV whohave not responded to other treatment modalities. Lopinaviris used in excess over ritonavir. Ritonavir at amounts givenhas no antiretroviral activity, Ritonavir inhibits lopinavir’smetabolism by CYP3A4, causing a higher level of lopinavirin the system. The combination is the first protease inhibitorapproved for patients as young as 6 months of age.
Pharmacokinetics
Oral absorption: Not known/available
C_max 400 mg + ritonavir 100 mg twice daily: c. 9.6 mg/L
C_min 400 mg + ritonavir 100 mg twice daily: c. 5.5 mg/L
Plasma half-life: c. 5–6 h
Volume of distribution: Not known/available
Plasma protein binding: c. 98–99%
Absorption and distribution
The absorption of lopinavir–ritonavir in capsule or liquid form is favorably affected by the presence of food, particularly if high in fat. The CNS penetration is good. It has a semen:plasma ratio of 0.07. It is distributed into breast milk.
Metabolism
Lopinavir is extensively metabolized by the CYP3A4 system, but this is inhibited by ritonavir.
Excretion
Over an 8-day period after single dosing with the combined formulation, around 10% and 83% of the administered dose is recovered in urine and feces, respectively. Less than 3% of the dose is recovered as unchanged drug in urine and 20% in feces. In mild to moderate hepatic impairment, an increase in exposure of approximately 30% is observed, but is probably not clinically relevant. It should be avoided in severe hepatic impairment.
Clinical Use
Treatment of HIV infection (in combination with ritonavir and other antiretroviral agents)
부작용
The most common adverse events seen in trials of complex antiretroviral regimens were diarrhea, nausea, headache, fatigue, vomiting and rash. Ritonavir-boosted lopinavir is associated with a dyslipidemia profile characteristic of those treated with other protease inhibitors boosted with 200 mg of ritonavir.

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