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lopinavir/ritonavir and raltegravir
Lopinavir/ritonavir inhibits HIV protease to block viral replication, while raltegravir inhibits HIV integrase to prevent viral DNA integration into the host genome.
Lopinavir/ritonavir inhibits HIV protease to block viral replication, while raltegravir inhibits HIV integrase to prevent viral DNA integration into the host genome. Used for HIV-1 infection in treatment-experienced patients, HIV-1 infection in treatment-naïve patients.
At a glance
| Generic name | lopinavir/ritonavir and raltegravir |
|---|---|
| Also known as | Kaletra, Isentress |
| Sponsor | Saint Michael's Medical Center |
| Drug class | Protease inhibitor (lopinavir/ritonavir) and integrase strand transfer inhibitor (raltegravir) |
| Target | HIV protease (lopinavir/ritonavir) and HIV integrase (raltegravir) |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease |
| Phase | FDA-approved |
Mechanism of action
Lopinavir is a protease inhibitor that prevents the cleavage of HIV polyproteins, resulting in immature, non-infectious viral particles. Ritonavir is a potent protease inhibitor used as a pharmacokinetic booster to increase lopinavir levels. Raltegravir is an integrase strand transfer inhibitor (INSTI) that blocks the integration of HIV DNA into the host cell chromosome, preventing establishment of persistent infection.
Approved indications
- HIV-1 infection in treatment-experienced patients
- HIV-1 infection in treatment-naïve patients
Common side effects
- Diarrhea
- Nausea
- Abdominal pain
- Headache
- Lipid elevation (hypertriglyceridemia)
- Hepatotoxicity
- Rash
Key clinical trials
- A Trial of 2 Options for Second Line Combination Antiretroviral Therapy Following Virological Failure of a Standard Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI)+2N(t)RTI First Line Regimen (PHASE4)
- Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV (PHASE2, PHASE3)
- A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments (PHASE4)
- Trial to Evaluate the Interest of a Reductive Anti Retroviral Strategy Using Dual Therapy Inspite of Triple Therapy (PHASE3)
- Pharmacokinetic Study of Antiretroviral Drugs and Related Drugs During and After Pregnancy
- Very Early Intensive Treatment of Infants Living With HIV to Achieve HIV Remission (PHASE1, PHASE2)
- Post-Exposure Prophylaxis in Health Care Workers (PHASE4)
- Research on the Psychological Status of Patients With HIV-1 Infection
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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