← Search & browse all drugs
ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Integrase inhibitors
elvitegravir
J05AJ02
Forms & Strengths
- Tablets: 85 mg (as component of Stribild)
- Tablets: 150 mg (as component of Stribild, Genvoya)
- Available primarily as a component of fixed-dose combination products
Adult Dosing
- Treatment-naive HIV-1 infection: 150 mg once daily administered orally with food as part of a fixed-dose combination regimen (e.g., Stribild or Genvoya)
Pediatric Dosing
- Pediatric patients weighing >= 35 kg: 150 mg once daily with food as part of a fixed-dose combination regimen
- Not recommended in pediatric patients with CrCl < 50 mL/min
Indications
- Treatment of HIV-1 infection in antiretroviral treatment-naive adults and pediatric patients weighing >= 35 kg
- Used strictly in combination with other antiretroviral agents
Mechanism of Action
- HIV-1 integrase strand transfer inhibitor (INSTI)
- Binds to integrase active site and blocks the strand transfer step of viral DNA integration into host cell genome, inhibiting viral replication
Contraindications
- Coadministration with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious/life-threatening events (e.g., alfuzosin, amiodarone, cisapride, pimozide, ergot derivatives, lovastatin, simvastatin, sildenafil for PAH, triazolam, midazolam)
- Coadministration with strong CYP3A inducers due to risk of significant loss of virologic response (e.g., rifampin, carbamazepine, phenobarbital, phenytoin, St. John's wort)
Adverse Reactions
- Nausea
- Diarrhea
- Headache
- Fatigue
- Insomnia
- Depressive disorders
- Abnormal hepatic transaminases
- Elevated serum creatinine (due to inhibition of tubular secretion)
Drug Interactions
- Coadministration with strong CYP3A inducers (e.g., rifampin, carbamazepine) significantly decreases elvitegravir concentrations
- Coadministration with antacids or polyvalent cations (Mg, Al, Ca, Fe) decreases elvitegravir absorption; administer antacids at least 2 hours before or after
- Co-administered with pharmacokinetic enhancers (cobicistat or ritonavir) which inhibit CYP3A-mediated metabolism to maintain therapeutic levels
- Potential interactions with statins metabolized by CYP3A4 (increased risk of myopathy)
Curated Content: Needs Vetting Before Put to Clinical Use