Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR AND LAMIVUDINE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR AND LAMIVUDINE versus EMTRIVA.
DOLUTEGRAVIR AND LAMIVUDINE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration. Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) that is phosphorylated to its active metabolite, which competes with endogenous deoxycytidine triphosphate for incorporation into viral DNA, leading to 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 (dolutegravir 50 mg/lamivudine 300 mg) orally once daily.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Dolutegravir: ~14 hours (terminal). Lamivudine: ~13-19 hours (terminal). Both support once-daily dosing.
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: ~53% excreted unchanged in feces via biliary secretion, ~31% in urine. Lamivudine: ~70% excreted unchanged in urine 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