Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE versus DOLUTEGRAVIR SODIUM AND ABACAVIR SULFATE AND LAMIVUDINE.
DOLUTEGRAVIR; LAMIVUDINE; 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 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.
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 orally once daily containing dolutegravir 50 mg, lamivudine 300 mg, and tenofovir disoproxil fumarate 300 mg.
One tablet (dolutegravir 50 mg / abacavir 600 mg / lamivudine 300 mg) orally once daily.
None Documented
None Documented
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.
abacavir: 1.5 hr; lamivudine: 5-7 hr; dolutegravir: 14 hr. Twice-daily dosing for abacavir/lamivudine, once-daily for dolutegravir
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.
abacavir: 83% renal (metabolites), 16% fecal; lamivudine: 70% renal (unchanged); dolutegravir: 64% fecal, 32% renal
Category A/B
Category A/B
NRTI
NRTI