Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
DOLUTEGRAVIR;LAMIVUDINE;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: 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 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, 300 mg lamivudine, 25 mg tenofovir alafenamide) 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 (once daily dosing). Lamivudine: ~13-19 hours (once daily). Tenofovir alafenamide: ~0.51 hours (terminal half-life of tenofovir ~34-46 hours).
abacavir: 1.5 hr; lamivudine: 5-7 hr; dolutegravir: 14 hr. Twice-daily dosing for abacavir/lamivudine, once-daily for dolutegravir
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.
abacavir: 83% renal (metabolites), 16% fecal; lamivudine: 70% renal (unchanged); dolutegravir: 64% fecal, 32% renal
Category A/B
Category A/B
NRTI
NRTI