Lopinavir
Active Pharmaceutical Ingredients 2025-03-03
CAS NO.: 192725-17-0
Molecular formula: C37H48N4O5
Molecular weight: 628.81
Standard: enterprise standard
Content: ≥98.0%
Packaging: 25KG/barrel
Introduction to Lopinavir
| Attribute | Details |
|---|---|
| Chemical Name | (2S)-N-amino]-4-hydroxy-1,6-diphenyl-hexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide |
| Brand Name | Kaletra (in combination with Ritonavir) |
| Mechanism of Action | Lopinavir is a potent inhibitor of HIV-1 protease, preventing the maturation of viral particles and thereby blocking viral replication. It also shows inhibitory activity against SARS-CoV-2 3CLpro, making it a potential antiviral agent for COVID-19. |
| Clinical Uses | – HIV Treatment: Used in combination with ritonavir to treat HIV-1 infection.<br>- COVID-19: Investigated for its potential antiviral activity against SARS-CoV-2.<br>- Hepatitis C: Used in combination with other drugs for treating HCV genotype 4. |
| Pharmacokinetics | – Bioavailability: Poor oral bioavailability when used alone; significantly enhanced when combined with ritonavir.<br>- Metabolism: Metabolized by CYP3A4 in the liver.<br>- Half-Life: Approximately 6–8 hours. |
| Adverse Effects | Common side effects include nausea, vomiting, diarrhea, and headache. Long-term use may lead to metabolic disorders, such as hyperlipidemia. |
| Drug Interactions | – CYP3A4 Inhibitors: May increase plasma levels of lopinavir.<br>- CYP3A4 Inducers: May decrease plasma levels of lopinavir. |
| Formulation | – Combination Therapy: Often combined with ritonavir (100 mg) to enhance its bioavailability and efficacy.<br>- Dosage Forms: Available as tablets and oral solution. |
Lopinavir is a potent HIV-1 protease inhibitor used primarily in combination with ritonavir to treat HIV infection. It has also been explored for its potential antiviral activity against SARS-CoV-2. Its efficacy is significantly enhanced when co-administered with ritonavir, which inhibits the metabolism of lopinavir.
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