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Lopinavir | CAS No: 192725-17-0 | GMP-certified suppliers
A medication that supports combination antiretroviral therapy by inhibiting HIV-1 protease to treat HIV-1 infection in adults and pediatric patients aged 14 days and older.
Therapeutic categories
Anti-HIV AgentsAnti-Infective AgentsAnti-Retroviral AgentsAntiinfectives for Systemic UseAntiviral AgentsAntivirals for Systemic Use
Generic name
Lopinavir
Molecule type
small molecule
CAS number
192725-17-0
DrugBank ID
DB01601
Approval status
Approved drug
ATC code
J05AR10
Primary indications
- The combination product lopinavir/ritonavir, marketed under the brand name Kaletra, is indicated in combination with other antiretrovirals for the treatment of HIV-1 infection in adults and pediatric patients ≥14 days old
Product Snapshot
- Lopinavir is available as oral solid and liquid formulations including capsules, tablets, and syrup
- It is primarily used in fixed-dose combination with ritonavir for antiretroviral therapy targeting HIV-1 infection
- The product is approved for marketing in the US, Canada, and EU regulatory jurisdictions
Clinical Overview
Lopinavir is an antiretroviral agent classified as an HIV-1 protease inhibitor, used exclusively in fixed-dose combination with ritonavir for the treatment of HIV-1 infection in adults and pediatric patients aged 14 days and older. Its clinical utility is confined to combination antiretroviral therapy, where it contributes to viral suppression alongside other agents.
Pharmacologically, lopinavir targets the HIV-1 protease enzyme, a dimeric aspartic protease essential for viral maturation. By binding to the active site of the protease, it mimics the natural peptide substrate via a hydroxyethylene scaffold that resists cleavage, thereby preventing the proteolytic processing of the Gag polyprotein. This interruption yields immature, non-infectious viral particles, inhibiting viral replication.
Lopinavir is characterized by limited oral bioavailability due to extensive first-pass metabolism primarily mediated by cytochrome P450 3A4 (CYP3A4). Co-administration with ritonavir, a potent CYP3A4 inhibitor, enhances lopinavir plasma concentrations by reducing its metabolic clearance. The pharmacokinetic profile supports once or twice daily dosing. Lopinavir demonstrates a moderate duration of action and is a substrate and inhibitor of various cytochrome P450 isoforms, necessitating careful consideration of drug-drug interactions during therapy.
Safety concerns include the risk of hepatotoxicity and pancreatitis, with reported cases of fatal outcomes. Patients with pre-existing hepatic impairment or risk factors for pancreatitis require close monitoring. Other adverse effects may arise from its metabolic and transporter-mediated interactions. Lopinavir has also been noted as an inhibitor or inducer of multiple cytochrome P450 enzymes and organic anion transporting polypeptides, further complicating polypharmacy scenarios.
The combination product lopinavir/ritonavir is marketed under the brand name Kaletra, introduced by Abbott in 2000. Although previously investigated for coronavirus disease 2019 (COVID-19), lopinavir remains indicated solely for HIV-1 infection.
From an API procurement standpoint, quality considerations include confirmation of chemical purity consistent with pharmacopoeial standards, control of residual solvents, and verification of polymorphic form to ensure consistent bioavailability and stability. Given lopinavir’s susceptibility to metabolism-driven variability, sourcing APIs with rigorous characterization and impurity profiling is critical for robust formulation development and regulatory compliance.
Pharmacologically, lopinavir targets the HIV-1 protease enzyme, a dimeric aspartic protease essential for viral maturation. By binding to the active site of the protease, it mimics the natural peptide substrate via a hydroxyethylene scaffold that resists cleavage, thereby preventing the proteolytic processing of the Gag polyprotein. This interruption yields immature, non-infectious viral particles, inhibiting viral replication.
Lopinavir is characterized by limited oral bioavailability due to extensive first-pass metabolism primarily mediated by cytochrome P450 3A4 (CYP3A4). Co-administration with ritonavir, a potent CYP3A4 inhibitor, enhances lopinavir plasma concentrations by reducing its metabolic clearance. The pharmacokinetic profile supports once or twice daily dosing. Lopinavir demonstrates a moderate duration of action and is a substrate and inhibitor of various cytochrome P450 isoforms, necessitating careful consideration of drug-drug interactions during therapy.
Safety concerns include the risk of hepatotoxicity and pancreatitis, with reported cases of fatal outcomes. Patients with pre-existing hepatic impairment or risk factors for pancreatitis require close monitoring. Other adverse effects may arise from its metabolic and transporter-mediated interactions. Lopinavir has also been noted as an inhibitor or inducer of multiple cytochrome P450 enzymes and organic anion transporting polypeptides, further complicating polypharmacy scenarios.
The combination product lopinavir/ritonavir is marketed under the brand name Kaletra, introduced by Abbott in 2000. Although previously investigated for coronavirus disease 2019 (COVID-19), lopinavir remains indicated solely for HIV-1 infection.
From an API procurement standpoint, quality considerations include confirmation of chemical purity consistent with pharmacopoeial standards, control of residual solvents, and verification of polymorphic form to ensure consistent bioavailability and stability. Given lopinavir’s susceptibility to metabolism-driven variability, sourcing APIs with rigorous characterization and impurity profiling is critical for robust formulation development and regulatory compliance.
Identification & chemistry
| Generic name | Lopinavir |
|---|---|
| Molecule type | Small molecule |
| CAS | 192725-17-0 |
| UNII | 2494G1JF75 |
| DrugBank ID | DB01601 |
Pharmacology
| Summary | Lopinavir is an antiretroviral agent that inhibits the HIV-1 protease enzyme, interrupting the proteolytic cleavage of the Gag polyprotein essential for viral maturation. By blocking this enzymatic activity, lopinavir prevents the formation of mature, infectious HIV particles. Its pharmacodynamic profile includes potential drug interactions due to protease inhibition and requires monitoring for hepatotoxicity and pancreatitis risk. |
|---|---|
| Mechanism of action | The HIV lifecycle is comprised of 3 distinct stages: assembly, involving creation and packaging of essential viral components; budding, wherein the viral particle crosses the host cell plasma membrane and forms a lipid envelope; and maturation, wherein the viral particle alters its structure and becomes infectious. At the center of this lifecycle is the Gag polyprotein which, along with the products of its proteolysis, coordinate these stages and function as the major structural proteins of the virus. The HIV-1 protease enzyme, a dimeric aspartic protease, is the enzyme responsible for cleaving the Gag polyprotein and thus plays a critical role in many aspects of the HIV viral lifecycle. Lopinavir is an inhibitor of the HIV-1 protease enzyme. Its design is based on the "peptidomimetic" principle, wherein the molecule contains a hydroxyethylene scaffold which mimics the normal peptide linkage (cleaved by HIV protease) but which itself cannot be cleaved. By preventing HIV-1 protease activity, and thus the proteolysis of the Gag polyprotein, lopinavir results in the production of immature, non-infectious viral particles. |
| Pharmacodynamics | Lopinavir inhibits the activity of an enzyme critical for the HIV viral lifecycle. It has a moderate duration of action necessitating once or twice daily dosing. Lopinavir, like other protease inhibitors, has a propensity for participating in drug interactions - use caution when administering lopinavir to patients maintained on other pharmaceutical agents as pharmacodynamic and pharmacokinetic interactions are common. Fatal hepatotoxicity and pancreatitis have been noted in patients undergoing therapy with lopinavir and patients with an increased baseline risk of these events should be monitored closely throughout therapy. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Human immunodeficiency virus type 1 protease | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | When administered alone, lopinavir has exceptionally low oral bioavailability (~25%) - for this reason, it is exclusively co-administered with ritonavir, which dramatically improves bioavailability, hinders drug metabolism, and allows for the attainment of therapeutic lopinavir concentrations. Following oral administration of lopinavir/ritonavir, maximal plasma concentrations are achieved at approximately 4.4 hours (T<sub>max</sub>), and the C<sub>max</sub> and AUC<sub>tau</sub> are 9.8 ± 3.7 - 11.8 ± 3.7 µg/mL and 92.6 ± 36.7 - 154.1 ± 61.4 μg•h/mL, respectively. Relative to administration in the fasted state, administration with a meal increases the AUC of the tablet formulation slightly (~19%) but dramatically increases the AUC of the oral solution formulation (~130%). |
|---|---|
| Half-life | The elimination half-life of lopinavir is 6.9 ± 2.2 hours. |
| Protein binding | Lopinavir is >98% protein-bound in plasma. It binds to both alpha-1-acid glycoprotein and albumin, but exhibits a greater affinity for alpha-1-acid glycoprotein. |
| Metabolism | Lopinavir undergoes extensive oxidative metabolism, almost exclusively via hepatic CYP3A isozymes. Co-administration with ritonavir, a potent inhibitor of CYP3A enzymes, helps to stave off lopinavir's biotransformation and increase plasma levels of active antiviral drug. Twelve metabolites have been identified _in vitro_, with the C-4 oxidation products M1, M3, and M4 being the predominant metabolites found in plasma. The structures of these primary metabolites have been identified, but precise structural information regarding the remaining minor metabolites has not been elucidated. |
| Route of elimination | Lopinavir is primarily eliminated in the feces. Following oral administration, approximately 10.4 ± 2.3% of the administered dose is excreted in the urine and 82.6 ± 2.5% is excreted in the feces. Unchanged parent drug accounted for 2.2% and 19.8% of the administered dose in urine and feces, respectively. |
| Volume of distribution | The volume of distribution of lopinavir following oral administration is approximately 16.9 L. |
| Clearance | The estimated apparent clearance following oral administration is approximately 6-7 L/h. |
Formulation & handling
- Lopinavir is a small molecule API primarily formulated for oral administration in various solid and liquid dosage forms.
- The compound exhibits low water solubility and high lipophilicity (LogP 4.69), which should be considered in formulation development to optimize bioavailability.
- Food intake influences absorption; the oral solution must be administered with food, while tablet forms have flexible administration with respect to meals.
Regulatory status
| Lifecycle | The API's key patents in the United States expired between 2016 and 2020, indicating the market is in a mature phase with generic competition present. It is marketed in the US, Canada, and the EU, regions where patent expirations have broadly enabled generic product entry. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Lopinavir is primarily associated with a single originator brand marketed across the US, Canada, and EU regions. Multiple US patents related to the product have expiration dates spanning from late 2016 through 2020, indicating that patent protection has recently ended or is close to ending. This patent expiry suggests the presence of existing or imminent generic competition in the market. |
|---|
Safety
| Toxicity | As lopinavir is only available in combination with ritonavir, experience with acute lopinavir overdose in isolation is limited. The risk related to overdose appears more pronounced in pediatric patients. One case report detailed a fatal cardiogenic shock in a 2.1kg infant following an approximately 10-fold overdose of Kaletra oral solution, while other reported reactions to overdose in infants include complete AV block, cardiomyopathy, lactic acidosis, and acute renal failure. The oral Kaletra solution is highly concentrated, posing a greater risk of overdose, and contains approximately 42% (v/v) ethanol, further increasing risk in children and infants. There is no antidote for lopinavir overdose. Treatment of overdose should consist largely of supportive measures and close observation of vital signs and clinical status of the affected patient. Consideration should be given to the removal of unabsorbed drug using gastric lavage or activated charcoal, if clinically indicated. Dialysis is unlikely to be of benefit as lopinavir is highly protein-bound, but may help to remove ethanol and propylene glycol from the circulation in the case of overdose with Kaletra oral solution. |
|---|
High Level Warnings:
- Lopinavir/ritonavir oral solution contains approximately 42% ethanol (v/v), increasing toxicity risk, especially in pediatric patients
- Overdose may result in severe cardiotoxicity, including cardiogenic shock, AV block, and cardiomyopathy
- No specific antidote is available
Lopinavir is a type of Anti-HIV
The Anti-HIV category of pharmaceutical APIs comprises a range of active pharmaceutical ingredients (APIs) specifically designed to combat the human immunodeficiency virus (HIV). These APIs play a critical role in the development and production of antiretroviral drugs, which are used to treat HIV infections and prevent the progression to acquired immunodeficiency syndrome (AIDS).
Anti-HIV APIs work by targeting various stages of the HIV life cycle, inhibiting viral replication and reducing the viral load in the body. Some commonly used APIs in this category include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), and integrase inhibitors (INIs).
NRTIs, such as tenofovir and emtricitabine, act by blocking the reverse transcriptase enzyme, an essential component in the replication of the virus. NNRTIs, such as efavirenz and nevirapine, bind to the reverse transcriptase enzyme, preventing its proper functioning. PIs, like ritonavir and atazanavir, inhibit the protease enzyme, crucial for viral maturation and assembly. INIs, such as raltegravir and dolutegravir, target the integrase enzyme, impeding viral integration into the host's DNA.
These APIs are carefully synthesized and undergo rigorous quality testing to ensure their safety, efficacy, and compliance with regulatory standards. Pharmaceutical companies utilize these APIs as key building blocks to formulate antiretroviral medications, which are then prescribed to individuals living with HIV/AIDS worldwide.
Overall, the Anti-HIV API category plays a vital role in the ongoing battle against HIV/AIDS, offering effective treatment options and improved quality of life for patients affected by this challenging condition.
