Comparative Pharmacology
Head-to-head clinical analysis: CRIXIVAN versus SYMTUZA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CRIXIVAN versus SYMTUZA.
CRIXIVAN vs SYMTUZA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Indinavir is a specific, potent, reversible inhibitor of HIV-1 protease. It binds to the active site of the viral protease, preventing the cleavage of viral polyprotein precursors into functional proteins, resulting in the formation of immature, non-infectious virions.
SYMTUZA is a fixed-dose combination of darunavir (a HIV-1 protease inhibitor), cobicistat (a CYP3A inhibitor), emtricitabine (a nucleoside reverse transcriptase inhibitor), and tenofovir alafenamide (a nucleotide reverse transcriptase inhibitor). Darunavir inhibits HIV-1 protease, preventing cleavage of viral polyproteins and resulting in immature, non-infectious virus. Emtricitabine and tenofovir alafenamide inhibit HIV reverse transcriptase by competing with natural substrates and causing DNA chain termination. Cobicistat inhibits CYP3A, boosting darunavir exposure.
800 mg orally every 8 hours on an empty stomach (1 hour before or 2 hours after meals) or with a light meal.
One tablet (darunavir 800 mg/cobicistat 150 mg/emtricitabine 200 mg/tenofovir alafenamide 10 mg) orally once daily with food.
None Documented
None Documented
Terminal elimination half-life is 1.8 to 2.5 hours in healthy adults; requires dosing every 8 hours.
Darunavir: 15 hours (when boosted with cobicistat). Cobicistat: 3-4 hours. Emtricitabine: 10 hours. Tenofovir alafenamide: 0.5 hours (active metabolite tenofovir diphosphate intracellular half-life >60 hours).
Primarily fecal (78-82%) with approximately 20% renal excretion of unchanged drug.
Darunavir: ~80% feces (mostly metabolites), ~14% urine (unchanged 1.5%). Cobicistat: ~86% feces, ~8% urine. Emtricitabine: ~86% urine (unchanged), ~14% feces. Tenofovir alafenamide: ~31% urine, ~47% feces (as tenofovir).
Category C
Category C
Antiretroviral
Antiretroviral