Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE TENOFOVIR ALAFENAMIDE versus EMTRICITABINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE TENOFOVIR ALAFENAMIDE versus EMTRICITABINE.
DOLUTEGRAVIR; EMTRICITABINE; TENOFOVIR ALAFENAMIDE vs EMTRICITABINE
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. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV-1 reverse transcriptase by competing with the natural substrate and causing chain termination. Tenofovir alafenamide is an NRTI that is converted to tenofovir, which inhibits HIV-1 reverse transcriptase after phosphorylation.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
One tablet (dolutegravir 50 mg; emtricitabine 200 mg; tenofovir alafenamide 25 mg) orally once daily.
200 mg orally once daily, typically in combination with other antiretroviral agents.
None Documented
None Documented
Clinical Note
moderateEmtricitabine + Ribavirin
"Emtricitabine may increase the hepatotoxic activities of Ribavirin."
Clinical Note
moderateLamivudine + Emtricitabine
"The risk or severity of adverse effects can be increased when Lamivudine is combined with Emtricitabine."
Clinical Note
moderateGanciclovir + Emtricitabine
"The risk or severity of adverse effects can be increased when Ganciclovir is combined with Emtricitabine."
Clinical Note
moderateValganciclovir + Emtricitabine
Dolutegravir: ~14 hours (single dose), ~12 hours (steady state). Emtricitabine: ~10 hours. Tenofovir alafenamide: ~0.5 hours; active metabolite tenofovir diphosphate intracellular half-life ~150-180 hours.
Terminal elimination half-life is approximately 10 hours (range 8–12 hours) in adults with normal renal function; prolonged to >20 hours in severe renal impairment (CrCl <30 mL/min).
Dolutegravir: 64% fecal (unchanged), 31% renal (parent and metabolites). Emtricitabine: 86% renal (unchanged). Tenofovir alafenamide: ~80% renal (as tenofovir); <1% fecal.
Renal: approximately 86% of the dose is excreted unchanged in urine via glomerular filtration and active tubular secretion. Biliary/fecal: minimal (<14% as unchanged drug and metabolites in feces).
Category A/B
Category C
NRTI
Antiretroviral, NRTI
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."