Lopinavir | HIV-1 protease inhibitor

Lopinavir chemical structure

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Lopinavir (192725-17-0) is a  potent and selective inhibitor of HIV-1 protease (IC50 = 6.5 nM, HIV cultured in peripheral blood mononuclear cells; Ki = 1.3 pM) which is highly selective over mammalian proteases.1 Lopinavir suffers from poor bioavailability due to extensive cytochrome P450-mediated metabolism. Thus, combination with ritonavir suppresses metabolism and is a preferred regimen for treatment of HIV infection.2 Inhibits replication of SARS CoV-2 virus in vitro, IC50 = 26.63 µM.3

References/Citations:

  1. Sham et al. (1998), ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease; Antimicrob. Agents Chemother. 42 3218
  2. Feng et al. (2012), CPY3A4-Mediated Lopinavir Bioactivation and Its Inhibition by Ritonavir; Drug Metab. Dispos. 40 18
  3. Choy et al. (2020), Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro; Antiviral Res. 178 104786
192725-17-0, ABT-378, ABT-378 supplier, HIV protease inhibitor, HIV-1 protease inhibitor, Lopinavir, Lopinavir supplier
Alternate Name:
ABT-378; A-157378

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N/A

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Lopinavir (192725-17-0) is a  potent and selective inhibitor of HIV-1 protease (IC50 = 6.5 nM, HIV cultured in peripheral blood mononuclear cells; Ki = 1.3 pM) which is highly selective over mammalian proteases.1 Lopinavir suffers from poor bioavailability due to extensive cytochrome P450-mediated metabolism. Thus, combination with ritonavir suppresses metabolism and is a preferred regimen for treatment of HIV infection.2 Inhibits replication of SARS CoV-2 virus in vitro, IC50 = 26.63 µM.3

References/Citations:

  1. Sham et al. (1998), ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease; Antimicrob. Agents Chemother. 42 3218
  2. Feng et al. (2012), CPY3A4-Mediated Lopinavir Bioactivation and Its Inhibition by Ritonavir; Drug Metab. Dispos. 40 18
  3. Choy et al. (2020), Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro; Antiviral Res. 178 104786