Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE TENOFOVIR DISOPROXIL FUMARATE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE TENOFOVIR DISOPROXIL FUMARATE versus EMTRIVA.
EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE 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, which competes with the natural substrate deoxycytidine 5'-triphosphate and incorporates into viral DNA, causing chain termination. Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor (NtRTI) that is converted to tenofovir, which is phosphorylated to tenofovir diphosphate and competes with deoxyadenosine 5'-triphosphate, resulting in DNA chain termination. Both inhibit HIV-1 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 / tenofovir disoproxil fumarate 300 mg) orally once daily.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Emtricitabine: 10 hours (increased to 20-30 hours in renal impairment); Tenofovir: 17 hours (prolonged to 30-50 hours in renal impairment).
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; Tenofovir: 70-80% renal (glomerular filtration and active tubular secretion) as unchanged drug, remainder metabolized and excreted renally.
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI