The integrase and fusion inhibitors used in anti retroviral therapy

1. Anti retroviral drugs
Utkarsh Jain
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2. Fusion Inhibitor

3. Entry Inhibitor

4. Enfurvirtide
• Binds to gp41, prevents conformational change
• Not active against HIV-2
• No cross resistance with other classes of ARV
• Administered s/c twice daily
• Given as add on drug to an optimised regimen in resistant cases
• Injections are painful and cause local irritation and nodules/cysts

5. CCR5 Receptor Inhibitor

6. Maraviroc
• Blocks CCR5 co-receptor
• No effect on CXCR4 receptor tropic strains
• Also used as an add on drug
• Orally administered
• No cross resistance with any other ARV drug
• Increased risk of infection/malignancy
• Metabolised by CYP450

7. Integrase inhibitor

8. Integrase Inhibitor

9. Integrase Inhibitors
• Raltegravir
• Elvitegravir
• Dolutegravir

10. Raltegravir
• Given orally
• Active against both HIV-1 and 2
• No cross resistance to other classes of ARV but cross resistance with
elvitegravir is present
• Given as add on drug in an optimised regimen
• Can also be given as a component of initial triple drug regimen( 2NRTI +
1NNRTI/Integrase inhibitor) in untreated patients
• Generally well tolerated
• Serious adverse effects – Muscle pain and rhabdomyolysis