Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
DOLUTEGRAVIR; EMTRICITABINE; 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 the integration of HIV-1 DNA into host genomic DNA. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV-1 reverse transcriptase by competing with the natural substrate and causing chain termination. Tenofovir alafenamide is an NRTI that is converted to tenofovir, which inhibits HIV-1 reverse transcriptase after phosphorylation.
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 (dolutegravir 50 mg; emtricitabine 200 mg; tenofovir alafenamide 25 mg) orally once daily.
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; active metabolite tenofovir diphosphate intracellular half-life ~150-180 hours.
abacavir: 1.5 hr; lamivudine: 5-7 hr; dolutegravir: 14 hr. Twice-daily dosing for abacavir/lamivudine, once-daily for dolutegravir
Dolutegravir: 64% fecal (unchanged), 31% renal (parent and metabolites). Emtricitabine: 86% renal (unchanged). Tenofovir alafenamide: ~80% renal (as tenofovir); <1% fecal.
abacavir: 83% renal (metabolites), 16% fecal; lamivudine: 70% renal (unchanged); dolutegravir: 64% fecal, 32% renal
Category A/B
Category A/B
NRTI
NRTI