Lopinavir , 95% , 192725-17-0

Synonym(s):
(αS)-N-[(1S,3S,4S)-4-[[(2,6-Dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-α-(1-methylethyl)-2-oxo-1(2H)-;Lopinavir

CAS NO.：192725-17-0

Empirical Formula: C37H48N4O5

Molecular Weight: 628.81

MDL number: MFCD04973616

EINECS: 200-001-8

PRODUCT Properties

• Melting point: 255.2-260.6 °F (124—127°C)
• Boiling point: 924.1±65.0 °C(Predicted)
• Density: 1.163±0.06 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO: soluble20mg/mL, clear
• form: powder
• pka: 13.89±0.46(Predicted)
• color: white to beige
• optical activity: [α]/D -20 to -27°, c = 0.4 in methanol
• Stability: Hygroscopic

Description and Uses

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.

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

Safety

• Symbol(GHS): GHS07,GHS08
• Signal word: Warning
• Hazard statements: H315-H373-H319-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P-P260-P314-P501
• RIDADR: 3077
• HS Code: 29335990