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MK-0518
MK-0518 is an integrase strand transfer inhibitor that blocks HIV integrase, preventing the virus from inserting its genetic material into human host cell DNA.
MK-0518 is an integrase strand transfer inhibitor that blocks HIV integrase, preventing the virus from inserting its genetic material into human host cell DNA. Used for HIV-1 infection in treatment-naïve and treatment-experienced patients, HIV-1 infection in combination antiretroviral therapy.
At a glance
| Generic name | MK-0518 |
|---|---|
| Also known as | raltegravir, Isentress® |
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Integrase strand transfer inhibitor (INSTI) |
| Target | HIV integrase |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease |
| Phase | Phase 3 |
Mechanism of action
By inhibiting HIV integrase, MK-0518 (raltegravir) prevents the integration of viral DNA into the host genome, a critical step in HIV replication. This mechanism allows the drug to suppress viral replication and reduce HIV RNA levels in infected individuals. It represents a novel class of antiretroviral agents distinct from reverse transcriptase and protease inhibitors.
Approved indications
- HIV-1 infection in treatment-naïve and treatment-experienced patients
- HIV-1 infection in combination antiretroviral therapy
Common side effects
- Diarrhea
- Nausea
- Headache
- Elevated creatine kinase
- 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)
- Pregnancy, Anti-integrase and Lymphocyte Repertoire of the Newborn
- Trial to Evaluate the Interest of a Reductive Anti Retroviral Strategy Using Dual Therapy Inspite of Triple Therapy (PHASE3)
- Therapeutic Drug Monitoring to oPtimize ANtiretroviral regimeNs in HIV-infected Women Who wAnt to Breastfeed
- Pharmacokinetic Study of Antiretroviral Drugs and Related Drugs During and After Pregnancy
- Study to Compare an Oral Weekly Islatravir/Lenacapavir Regimen With Standard of Care in Virologically Suppressed People With HIV-1 (PHASE3)
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 |