Name: | Lopinavir |
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PubChem Compound ID: | 11979606 |
Description: | An antiretroviral drug of the protease inhibitor class used as a fixed-dose combination with RITONAVIR. |
Molecular formula: | C74H96N10O10S2 |
Molecular weight: | 1349.75 g/mol |
Synonyms: |
LPV/r; 2,4,7,12-Tetraazatridecan-13-oic acid, 10-hydroxy-2-methyl-5-(1-methylethyl)-1-(2-(1-methylethyl)-4-thiazolyl)-3,6-dioxo-8,11-bis(phenylmethyl)-, 5-thiazolylmethyl ester, (5S,8S,10S,11S)-, mixt. with (aS)-N-((1S,3S,4S)-4-(((2,6-dimethylphenoxy)acetyl)amin; D02498; ABT-378 & ABT-538; Kaletra (TN); Kaletra; Lopinavir & Ritonavir; Lopinavir & Norvir; AIDS-003688; AIDS003688.
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Name: | Lopinavir |
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Name (isomeric): | DB01601 |
Drug Type: | small molecule |
Description: | An antiretroviral drug of the protease inhibitor class used as a fixed-dose combination with RITONAVIR. |
Synonyms: |
ABT-378; LPV
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Brand: | Koletra, Aluviran |
Brand name mixture: | Kaletra(Lopinavir + Ritonavir) |
Category: | HIV Protease Inhibitors, Anti-HIV Agents |
CAS number: | 192725-17-0 |
Indication: | Indicated in combination with other antiretroviral agents for the treatment of HIV-infection. |
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Pharmacology: | Lopinavir is an antiretroviral of the protease inhibitor class. Inhibiting HIV-1 protease (responsible for protein cleavage), results in selectively inhibiting the cleavage of HIV gag and gag-pol polyproteins, thereby preventing viral maturation. |
Mechanism of Action: | Lopinavir inhibits the HIV viral protease enzyme. This prevents cleavage of the gag-pol polyprotein and, therefore, improper viral assembly results. This subsequently results in non-infectious, immature viral particles. |
Absorption: | Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4. |
Protein binding: | Lopinavir is highly bound to plasma proteins (98-99%). |
Biotransformation: | Hepatic. Lopinavir is extensively metabolized by the hepatic cytochrome P450 system, almost exclusively by the CYP3A isozyme. |
Toxicity: | Although human experience of acute overdosage with lopinavir is limited, accidental ingestion of the product by a young child could result in significant alcohol-related toxicity and could approach the potential lethal dose of alcohol. |
Affected organisms: | Human Immunodeficiency Virus |
Food interaction: |
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