Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE RILPIVIRINE TENOFOVIR ALAFENAMIDE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE RILPIVIRINE TENOFOVIR ALAFENAMIDE versus EMTRIVA.
EMTRICITABINE; RILPIVIRINE; TENOFOVIR ALAFENAMIDE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI); rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI); tenofovir alafenamide is an NRTI. Combination inhibits HIV-1 replication by blocking reverse transcriptase.
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 (emtricitabine 200 mg, rilpivirine 25 mg, tenofovir alafenamide 25 mg) orally once daily with a meal.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Emtricitabine: 10 h (healthy subjects); 8-9 h (HIV-1 infected, once-daily dosing achieves therapeutic plasma concentrations). Rilpivirine: 45 h (terminal, supports once-daily dosing). Tenofovir alafenamide: 0.51 h (parent); tenofovir metabolite: 32-37 h (intracellular, 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)
Emtricitabine: 86% renal (glomerular filtration and active tubular secretion), 14% fecal. Rilpivirine: 85% fecal (65% as parent drug), 6.1% renal (negligible unchanged). Tenofovir alafenamide: <1% renal; >80% fecal as metabolites; hydrolyzed intracellularly to tenofovir, which is eliminated renally (70-80% unchanged) 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