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Lopinavir

Generic Name
Lopinavir
Brand Names
Kaletra
Drug Type
Small Molecule
Chemical Formula
C37H48N4O5
CAS Number
192725-17-0
Unique Ingredient Identifier
2494G1JF75

Overview

Lopinavir is an antiretroviral protease inhibitor used in combination with other antiretrovirals in the treatment of HIV-1 infection. Lopinavir is marketed and administered exclusively in combination with ritonavir - this combination, first marketed by Abbott under the brand name Kaletra in 2000, is necessary due to lopinavir's poor oral bioavailability and extensive biotransformation. Ritonavir is a potent inhibitor of the enzymes responsible for lopinavir metabolism, and its co-administration "boosts" lopinavir exposure and improves antiviral activity. Like many other protease inhibitors (e.g. saquinavir, nelfinavir), lopinavir is a peptidomimetic molecule - it contains a hydroxyethylene scaffold that mimics the peptide linkage typically targeted by the HIV-1 protease enzyme but which itself cannot be cleaved, thus preventing the activity of the HIV-1 protease. Lopinavir was previously under investigation in combination with ritonavir for the treatment of COVID-19 caused by SARS-CoV-2.

Background

Lopinavir is an antiretroviral protease inhibitor used in combination with other antiretrovirals in the treatment of HIV-1 infection. Lopinavir is marketed and administered exclusively in combination with ritonavir - this combination, first marketed by Abbott under the brand name Kaletra in 2000, is necessary due to lopinavir's poor oral bioavailability and extensive biotransformation. Ritonavir is a potent inhibitor of the enzymes responsible for lopinavir metabolism, and its co-administration "boosts" lopinavir exposure and improves antiviral activity. Like many other protease inhibitors (e.g. saquinavir, nelfinavir), lopinavir is a peptidomimetic molecule - it contains a hydroxyethylene scaffold that mimics the peptide linkage typically targeted by the HIV-1 protease enzyme but which itself cannot be cleaved, thus preventing the activity of the HIV-1 protease. Lopinavir was previously under investigation in combination with ritonavir for the treatment of COVID-19 caused by SARS-CoV-2.

Indication

用于高效抗逆转录病毒疗法(HAART)的组成药物。

Associated Conditions

  • Human Immunodeficiency Virus Type 1 (HIV-1) Infection

FDA Approved Products

Kaletra
Manufacturer:AbbVie Inc.
Route:ORAL
Strength:100 mg in 1 1
Approved: 2023/07/10
NDC:0074-0522
Lopinavir and Ritonavir
Manufacturer:NuCare Pharmaceuticals,Inc.
Route:ORAL
Strength:200 mg in 1 1
Approved: 2023/03/06
NDC:68071-2949
Kaletra
Manufacturer:AbbVie Inc.
Route:ORAL
Strength:100 mg in 1 1
Approved: 2023/07/10
NDC:0074-1575
Lopinavir and ritonavir
Manufacturer:Camber Pharmaceuticals, Inc.
Route:ORAL
Strength:100 mg in 1 1
Approved: 2021/06/03
NDC:31722-603
Lopinavir and Ritonavir
Manufacturer:Laurus Labs Limited
Route:ORAL
Strength:200 mg in 1 1
Approved: 2022/03/23
NDC:42385-934

Singapore Approved Products

KALETRA ORAL SOLUTION
Manufacturer:AbbVie Inc.
Form:SYRUP
Strength:80 mg
Online:Yes
Approved: 2001/04/18
Approval:SIN11492P
Kaletra Tablet 200mg/50mg
Manufacturer:AbbVie Deutschland GmbH & Co. KG
Form:TABLET, FILM COATED
Strength:200.0mg
Online:Yes
Approved: 2007/04/12
Approval:SIN13250P

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