Integrase Strand Transfer Inhibitor

Aka: Integrase Strand Transfer Inhibitor, Integrase Inhibitor, Raltegravir, Isentress, InSTI, RAL, Bictegravir, Biktarvy, Dolutegravir, Tivacay, Cabotegravir, Vocabria, Cabenuva

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II. Class

  1. Anti-retroviral agent
  2. Integrase Strand Transfer Inhibitor

III. Mechanism

  1. Integrase Strand Transfer Inhibitor prevents viral DNA from integrating into host DNA
    1. Blocks the integrase enzyme

IV. Indications

  1. Anti-retroviral naive patients
  2. Anti-retroviral experienced patients

V. Preparations: Single Agents

  1. Bictegravir (Biktarvy)
  2. Dolutegravir (Tivacay)
  3. Cabotegravir (Vocabria)
    1. Available as oral agent, as well as monthly IM Injection (administered as part of Cabenuva)
  4. Raltegravir (Isentress)
    1. Dose: One 400 mg tablet orally twice daily

VI. Preparations: Cabenuva (Cabotegravir and Rilpivirine)

  1. Cabenuva combines Integrase Inhibitor and Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
    1. Integrase Inhibitor: Cabotegravir
    2. Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI): Rilpivirine)
  2. Dosing
    1. Two Intramuscular Injections in gluteal Muscle (one for each drug) once monthly
    2. Administered in clinic, at $4000 per month
    3. Requires one month of oral "lead-in" daily therapy to evaluate tolerability before IM Injection
  3. Efficacy
    1. Appears as effective as triple therapy combinations
  4. Drug Interactions
    1. Less effective when combined with CYP 3A4 inducers (e.g. Phenytoin)
  5. References
    1. Orkin (2020) N Engl J Med 382(12):1124-35 [PubMed]
    2. Swindells (2020) N Engl J Med 382(12):1112-23 [PubMed]
    3. (2021) presc lett 28(3): 18

VII. Efficacy

  1. Drug resistance is common

VIII. Adverse Effects: Raltegravir

  1. Diarrhea
  2. Nausea
  3. Headache
  4. Serum Creatinine phosphokinase (CPK) increases
  5. Mild Serum Creatinine increase without affecting Renal Function (Dolutegravir)
  6. Myopathy
  7. Rhabdomyolysis
  8. Insomnia

IX. Drug Interactions

  1. Typically fewer Drug Interactions than other Anti-Retroviral Agents
  2. Phenytoin
  3. Rifampin
  4. St John's Wort
  5. Avoid taking at the same time as Calcium, Magnesium, aluminum and iron containing agents

X. References

  1. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  2. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]

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Related Studies

Cost: Medications

isentress (on 1/6/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ISENTRESS 400 MG TABLET $29.50 each
ISENTRESS HD 600 MG TABLET $29.57 each
ral (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
RALOXIFENE HCL 60 MG TABLET Generic $0.28 each
biktarvy (on 12/7/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
BIKTARVY 50-200-25 MG TABLET $115.81 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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