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Integrase strand transfer inhibitors
Integrase strand transfer inhibitors block HIV integrase, preventing the virus from inserting its genetic material into the host cell's DNA.
Integrase strand transfer inhibitors block HIV integrase, preventing the virus from inserting its genetic material into the host cell's DNA. Used for HIV-1 infection (treatment-naïve and treatment-experienced patients), HIV-1 infection in combination antiretroviral therapy.
At a glance
| Generic name | Integrase strand transfer inhibitors |
|---|---|
| Also known as | INSTI |
| Sponsor | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal |
| Drug class | Integrase strand transfer inhibitor (INSTI) |
| Target | HIV integrase |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease |
| Phase | FDA-approved |
Mechanism of action
These drugs inhibit the integrase enzyme, which HIV uses to integrate its RNA genome into the human host cell chromosome. By blocking this critical step in the viral replication cycle, the drugs prevent establishment of persistent infection and reduce viral load. This class represents a major advance in antiretroviral therapy with a distinct mechanism from reverse transcriptase and protease inhibitors.
Approved indications
- HIV-1 infection (treatment-naïve and treatment-experienced patients)
- HIV-1 infection in combination antiretroviral therapy
Common side effects
- Diarrhea
- Nausea
- Headache
- Insomnia
- Rash
- Elevated creatine kinase
Key clinical trials
- Early Metabolic Effects of Dolutegravir or Tenofovir Alefenamide in Healthy Volunteers (PHASE2)
- Study to Compare an Oral Weekly Islatravir/Lenacapavir Regimen With Standard of Care in Virologically Suppressed People With HIV-1 (PHASE3)
- Doravirine for Obese Persons on Integrase Inhibitors and Tenofovir Alafenamide (PHASE4)
- Real-Life Outcomes of TAF/FTC/BIC in HIV Patients in Colombia
- 'COMBINE-2': Real-world Evidence for Effectiveness of Two Drug Regimen, Antiretroviral Therapy With Integrase Inhibitors Plus a Reverse Transcriptase Inhibitor
- Regimen Switch to Dolutegravir + Rilpivirine From Current Antiretroviral Regimen in Human Immunodeficiency Virus Type 1 Infected and Virologically Suppressed Adults (SWORD-1) (PHASE3)
- Regimen Switch to Dolutegravir + Rilpivirine From Current Antiretroviral Regimen in Human Immunodeficiency Virus Type 1 Infected and Virologically Suppressed Adults (SWORD-2) (PHASE3)
- Post-Injectable Cabotegravir Antiretroviral Salvage Strategy Options Trial (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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