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