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Lopinavir/r plus saquinavir
This combination of two protease inhibitors blocks HIV protease to prevent viral replication, with ritonavir boosting lopinavir levels.
This combination of two protease inhibitors blocks HIV protease to prevent viral replication, with ritonavir boosting lopinavir levels. Used for HIV-1 infection in treatment-experienced patients with protease inhibitor resistance.
At a glance
| Generic name | Lopinavir/r plus saquinavir |
|---|---|
| Sponsor | The HIV Netherlands Australia Thailand Research Collaboration |
| Drug class | HIV protease inhibitor combination |
| Target | HIV protease |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease / Virology |
| Phase | FDA-approved |
Mechanism of action
Lopinavir and saquinavir are both HIV protease inhibitors that bind to and inhibit the HIV protease enzyme, preventing the cleavage of viral polyproteins necessary for infectious particle maturation. Ritonavir (the '/r' component) is a potent CYP3A4 inhibitor that dramatically increases lopinavir plasma concentrations through pharmacokinetic boosting, allowing lower doses and improved efficacy. This triple-agent approach was used to overcome protease inhibitor resistance in treatment-experienced HIV patients.
Approved indications
- HIV-1 infection in treatment-experienced patients with protease inhibitor resistance
Common side effects
- Diarrhea
- Nausea
- Abdominal pain
- Lipid abnormalities (elevated cholesterol/triglycerides)
- Hepatotoxicity
- Hyperglycemia
Key clinical trials
- Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV (PHASE2, PHASE3)
- Anti-HIV Drug Regimens and Treatment-Switching Guidelines in HIV Infected Children (PHASE2, PHASE3)
- Study to Evaluate Switching to Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (E/C/F/TAF) Fixed Dose Combination (FDC) in Virologically-Suppressed HIV-1 Infected Adults Harboring the Archived Isolated NRTI Resistance Mutation M184V/M184I (PHASE3)
- Switching From a Tenofovir Disoproxil Fumarate (TDF) Containing Regimen to Elvitegravir/Cobicistat/Emtricitabine/ Tenofovir Alafenamide (E/C/F/TAF) Fixed-Dose Combination (FDC) in Virologically-Suppressed, HIV-1 Infected Adults Aged ≥ 60 Years (PHASE3)
- Safety and Efficacy of Switching From Regimens of ABC/3TC + a 3rd Agent to E/C/F/TAF Fixed-Dose Combination (FDC) in Virologically-Suppressed HIV 1 Infected Adults (PHASE3)
- Safety of EVG+RTV Administered With Other Antiretroviral Agents for the Treatment of HIV-1 Infection (PHASE2)
- A PK and Salvage Study for Children With HIV-infection (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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