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Lopinavir

Lopinavir
Lopinavir structure
CAS No.
192725-17-0
Chemical Name:
Lopinavir
Synonyms
Koletr;Koletra;ABT 378;Aluviran;LOPINAVIR;A 157378.0;ABT-378 whatsapp;Lopinavir (350 mg);Lopinavir (ABT-378);Lopinavir for system suitability
CBNumber:
CB3663640
Molecular Formula:
C37H48N4O5
Formula Weight:
628.8
MOL File:
192725-17-0.mol

Lopinavir Properties

Melting point:
124-127°C
storage temp. 
Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility 
DMSO: soluble20mg/mL, clear
form 
powder
color 
white to beige
optical activity
[α]/D -20 to -27°, c = 0.4 in methanol
Stability:
Hygroscopic
CAS DataBase Reference
192725-17-0(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
RIDADR  3077
HS Code  29335990

Lopinavir price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1222 Lopinavir ≥98% (HPLC) 192725-17-0 10mg $22.7 2018-11-13 Buy
Sigma-Aldrich 1370101 Lopinavir United States Pharmacopeia (USP) Reference Standard 192725-17-0 350mg $1240 2018-11-13 Buy
Cayman Chemical 13854 Lopinavir ≥98% 192725-17-0 25mg $29 2018-11-13 Buy
Cayman Chemical 13854 Lopinavir ≥98% 192725-17-0 50mg $49 2018-11-13 Buy
Sigma-Aldrich SML1222 Lopinavir ≥98% (HPLC) 192725-17-0 50mg $57.7 2018-11-13 Buy

Lopinavir Chemical Properties,Uses,Production

Description

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.

Chemical Properties

White Crystalline Solid

Originator

Abbott (US)

Uses

A selective HIV protease inhibitor. An analogue of Ritonavir. Antiviral.

Uses

Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM

Definition

ChEBI: A dicarboxylic acid amide in which a parent structure of 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- ethyl-2-(2-oxotetrahydropyrimidin-1(2H)-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.

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.

brand name

Kaletra

Antimicrobial activity

Lopinavir is active against HIV-1 and HIV-2.

Acquired resistance

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.

General Description

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.

Pharmaceutical Applications

A synthetic compound, co-formulated with ritonavir for oral administration. In this formulation, ritonavir functions to inhibit the metabolic clearance of lopinavir, and does not contribute to the antiretroviral activity.

Pharmacokinetics

Oral absorption: Not known/available
Cmax 400 mg + ritonavir 100 mg twice daily: c. 9.6 mg/L
Cmin 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)

Side effects

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.

Side effects

Side effects, which are generally mild, include diarrhea, nausea, asthenia, and headache. Pancreatitis occurs rarely. Ritonavir is a potent inhibitor of CYP3A4 and also inhibits CYP2D6. In addition to the drugs contraindicated for all protease inhibitors, flecainide, propafenone, pimozide, and rifampin should not be given with lopinavir–ritonavir combination therapy.

Lopinavir Preparation Products And Raw materials

Raw materials

Preparation Products


Lopinavir Suppliers

Global( 204)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19918 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21676 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
alice@hbjkai.com CHINA 272 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32447 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2543 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30001 58
Shaanxi Yikanglong Biotechnology Co., Ltd.
17791478691
yklbiotech@163.com CHINA 297 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 969 58

View Lastest Price from Lopinavir manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-20 Lopinavir
192725-17-0
US $1.00 / KG 1G 98% 100KG career henan chemical co
2018-04-27 lopinavir;ABT-378 whatsapp;+8617197824028
192725-17-0
US $100.00 / G 1公斤 98 Wahtsapp;+8617197824028 150kg/day Hebei Jiangkai Trading Co., Ltd

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