Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE versus EMTRIVA.
DOLUTEGRAVIR;LAMIVUDINE;TENOFOVIR ALAFENAMIDE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dolutegravir: HIV integrase strand transfer inhibitor; inhibits viral DNA integration. Lamivudine: Nucleoside reverse transcriptase inhibitor (NRTI); chain terminator. Tenofovir alafenamide: Nucleotide reverse transcriptase inhibitor (NRTI); prodrug that converts to tenofovir diphosphate.
Nucleoside reverse transcriptase inhibitor; emtricitabine is phosphorylated to emtricitabine 5'-triphosphate which competes with deoxycytidine 5'-triphosphate for incorporation into viral DNA, resulting in chain termination.
One tablet (50 mg dolutegravir, 300 mg lamivudine, 25 mg tenofovir alafenamide) orally once daily with or without food.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Dolutegravir: ~14 hours (once daily dosing). Lamivudine: ~13-19 hours (once daily). Tenofovir alafenamide: ~0.51 hours (terminal half-life of tenofovir ~34-46 hours).
Terminal elimination half-life ~10 hours (mean 10 h, range 7-14 h) in adults; prolonged in renal impairment (up to 90 h in severe impairment)
Dolutegravir: ~53% unchanged in feces, ~34% unchanged in urine. Lamivudine: ~70% unchanged in urine via glomerular filtration and active tubular secretion. Tenofovir alafenamide: <1% renal as unchanged, mostly metabolized to tenofovir (which is eliminated renally via tubular secretion) and other metabolites.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI