Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
DOLUTEGRAVIR, EMTRICITABINE and TENOFOVIR ALAFENAMIDE vs DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dolutegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) that blocks viral DNA integration. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that terminates viral DNA chain elongation. Tenofovir alafenamide is an NRTI that inhibits HIV reverse transcriptase after intracellular conversion to tenofovir diphosphate.
Dolutegravir is an HIV integrase strand transfer inhibitor that blocks integration of HIV-1 DNA into host cell DNA. Abacavir and lamivudine are nucleoside reverse transcriptase inhibitors that inhibit HIV-1 reverse transcriptase via incorporation into viral DNA, causing chain termination.
One tablet (50 mg dolutegravir/200 mg emtricitabine/25 mg tenofovir alafenamide) taken orally once daily with or without food.
One tablet (dolutegravir 50 mg / abacavir 600 mg / lamivudine 300 mg) orally once daily.
None Documented
None Documented
Dolutegravir: ~14 hours (single dose), ~12 hours (steady state). Emtricitabine: ~10 hours. Tenofovir alafenamide: ~0.5 hours (parent), but its active metabolite tenofovir diphosphate has intracellular half-life >60 hours. Clinically, tenofovir alafenamide is dosed once daily due to intracellular accumulation.
abacavir: 1.5 hr; lamivudine: 5-7 hr; dolutegravir: 14 hr. Twice-daily dosing for abacavir/lamivudine, once-daily for dolutegravir
Dolutegravir: ~64% feces (as parent), ~31% urine (as glucuronide conjugate, <1% parent). Emtricitabine: ~86% urine (as parent and metabolites), ~14% feces. Tenofovir alafenamide: <1% renal (as parent), ~82% feces (as metabolite tenofovir).
abacavir: 83% renal (metabolites), 16% fecal; lamivudine: 70% renal (unchanged); dolutegravir: 64% fecal, 32% renal
Category A/B
Category A/B
NRTI
NRTI