Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE RILPIVIRINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE RILPIVIRINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
EMTRICITABINE, RILPIVIRINE, AND 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) 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.
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 (200 mg emtricitabine/25 mg rilpivirine/25 mg tenofovir alafenamide) orally once daily with a meal.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Emtricitabine: 10 h; Rilpivirine: 45 h (range 41–55 h); Tenofovir alafenamide: 0.51 h (converted to tenofovir), tenofovir: 32–49 h.
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 (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).
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI