Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE.
DOLUTEGRAVIR;LAMIVUDINE;TENOFOVIR ALAFENAMIDE vs DOLUTEGRAVIR; LAMIVUDINE; TENOFOVIR DISOPROXIL FUMARATE
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.
Dolutegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) that blocks the integration of HIV-1 DNA into host genomic DNA. Lamivudine and tenofovir disoproxil fumarate are nucleoside reverse transcriptase inhibitors (NRTIs) that inhibit HIV-1 reverse transcriptase by competing with natural substrates and causing chain termination.
One tablet (50 mg dolutegravir, 300 mg lamivudine, 25 mg tenofovir alafenamide) orally once daily with or without food.
One tablet orally once daily containing dolutegravir 50 mg, lamivudine 300 mg, and tenofovir disoproxil fumarate 300 mg.
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).
Dolutegravir: ~14 hours (range 11-18) in HIV-1-infected adults, supports once-daily dosing. Lamivudine: ~18-19 hours in HIV-infected adults, allows once-daily dosing; prolonged in renal impairment. Tenofovir disoproxil fumarate: ~17 hours (tenofovir) in HIV-infected adults, supports once-daily dosing; extended in renal 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.
Dolutegravir: ~64% feces (as unchanged drug), 31% urine (as unchanged and metabolites). Lamivudine: ~70% urine (as unchanged drug) via active tubular secretion, ~6% as inactive trans-sulfoxide metabolite. Tenofovir disoproxil fumarate: ~70-80% urine (as unchanged tenofovir) via glomerular filtration and active tubular secretion.
Category A/B
Category A/B
NRTI
NRTI