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Integrase Strand Transfer Inhibitor
Aka: Integrase Strand Transfer Inhibitor, Integrase Inhibitor, Raltegravir, Isentress, InSTI, RAL, Bictegravir, Biktarvy, Dolutegravir, Tivacay, Cabotegravir, Vocabria, Cabenuva
- See Also
- Anti-Retroviral Therapy
- Class
- Anti-retroviral agent
- Integrase Strand Transfer Inhibitor
- Mechanism
- Integrase Strand Transfer Inhibitor prevents viral DNA from integrating into host DNA
- Blocks the integrase enzyme
- Indications
- Anti-retroviral naive patients
- Anti-retroviral experienced patients
- Preparations: Single Agents
- Bictegravir (Biktarvy)
- Dolutegravir (Tivacay)
- Cabotegravir (Vocabria)
- Available as oral agent, as well as monthly IM Injection (administered as part of Cabenuva)
- Raltegravir (Isentress)
- Dose: One 400 mg tablet orally twice daily
- Preparations: Cabenuva (Cabotegravir and Rilpivirine)
- Cabenuva combines Integrase Inhibitor and Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
- Integrase Inhibitor: Cabotegravir
- Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI): Rilpivirine)
- Dosing
- Two Intramuscular Injections in gluteal Muscle (one for each drug) once monthly
- Administered in clinic, at $4000 per month
- Requires one month of oral "lead-in" daily therapy to evaluate tolerability before IM Injection
- Efficacy
- Appears as effective as triple therapy combinations
- Drug Interactions
- Less effective when combined with CYP 3A4 inducers (e.g. Phenytoin)
- References
- Orkin (2020) N Engl J Med 382(12):1124-35 [PubMed]
- Swindells (2020) N Engl J Med 382(12):1112-23 [PubMed]
- (2021) presc lett 28(3): 18
- Efficacy
- Drug resistance is common
- Adverse Effects: Raltegravir
- Diarrhea
- Nausea
- Headache
- Serum Creatinine phosphokinase (CPK) increases
- Mild Serum Creatinine increase without affecting Renal Function (Dolutegravir)
- Myopathy
- Rhabdomyolysis
- Insomnia
-
Drug Interactions
- Typically fewer Drug Interactions than other Anti-Retroviral Agents
- Phenytoin
- Rifampin
- St John's Wort
- Avoid taking at the same time as Calcium, Magnesium, aluminum and iron containing agents
- References
- (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
- Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]