Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE versus EMTRIVA.
DOLUTEGRAVIR; LAMIVUDINE; TENOFOVIR DISOPROXIL FUMARATE vs EMTRIVA
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.
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 orally once daily containing dolutegravir 50 mg, lamivudine 300 mg, and tenofovir disoproxil fumarate 300 mg.
Emtricitabine 200 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.
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: ~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.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI