Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
DOLUTEGRAVIR, LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE 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 integrase strand transfer inhibitor that blocks HIV-1 integration into host DNA. Lamivudine and tenofovir disoproxil fumarate are nucleoside reverse transcriptase inhibitors that inhibit HIV-1 reverse transcriptase via DNA chain termination.
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/300 mg tenofovir disoproxil fumarate) orally once daily
One tablet (dolutegravir 50 mg / abacavir 600 mg / lamivudine 300 mg) orally once daily.
None Documented
None Documented
Dolutegravir: ~14 hours (terminal), supports once-daily dosing with moderate PK variability. Lamivudine: ~18-22 hours (terminal), allows once-daily dosing; intracellular active metabolite (lamivudine triphosphate) has much longer half-life (~22-27 hours). Tenofovir: ~17 hours (terminal), increased to ~32 hours in intracellular diphosphate form; supports once-daily dosing.
abacavir: 1.5 hr; lamivudine: 5-7 hr; dolutegravir: 14 hr. Twice-daily dosing for abacavir/lamivudine, once-daily for dolutegravir
Dolutegravir: ~64% feces (primarily as parent drug), ~32% urine (parent drug and glucuronide conjugate). Lamivudine: ~70% urine as unchanged drug (renal tubular secretion). Tenofovir disoproxil fumarate (TDF): Pro-drug; tenofovir is renally excreted ~70-80% unchanged (glomerular filtration and tubular secretion).
abacavir: 83% renal (metabolites), 16% fecal; lamivudine: 70% renal (unchanged); dolutegravir: 64% fecal, 32% renal
Category A/B
Category A/B
NRTI
NRTI