Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE versus EMTRICITABINE RILPIVIRINE AND TENOFOVIR ALAFENAMIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE versus EMTRICITABINE RILPIVIRINE AND TENOFOVIR ALAFENAMIDE.
EMTRICITABINE vs EMTRICITABINE, RILPIVIRINE, AND TENOFOVIR ALAFENAMIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that is phosphorylated to its active metabolite, emtricitabine triphosphate, which competes with the natural substrate deoxycytidine 5'-triphosphate and incorporates into viral DNA, causing chain termination. Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to a hydrophobic pocket near the active site of reverse transcriptase, causing a conformational change that inhibits enzyme activity. Tenofovir alafenamide is a nucleotide reverse transcriptase inhibitor (NtRTI) that is converted intracellularly to tenofovir diphosphate, which competes with deoxyadenosine 5'-triphosphate and causes DNA chain termination.
200 mg orally once daily, typically in combination with other antiretroviral agents.
One tablet (200 mg emtricitabine/25 mg rilpivirine/25 mg tenofovir alafenamide) orally once daily with a meal.
None Documented
None Documented
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).
Emtricitabine: 10 h; Rilpivirine: 45 h (range 41–55 h); Tenofovir alafenamide: 0.51 h (converted to tenofovir), tenofovir: 32–49 h.
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).
Emtricitabine: 86% renal (glomerular filtration and active tubular secretion), 14% fecal; Rilpivirine: 85% fecal (unchanged and metabolites), 6.1% renal (0.03% unchanged); Tenofovir alafenamide: <1% renal (as tenofovir), 31.7% fecal (as tenofovir), 32% urine (as tenofovir; 18.2% as TAF and metabolites).
Category C
Category A/B
Antiretroviral, NRTI
NRTI