Comparative Pharmacology
Head-to-head clinical analysis: APTIVUS versus DESCOVY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APTIVUS versus DESCOVY.
APTIVUS vs DESCOVY
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Tipranavir is a nonpeptidic HIV-1 protease inhibitor that binds to the active site of HIV-1 protease, thereby preventing the cleavage of viral polyprotein precursors into functional proteins, resulting in the production of immature, noninfectious viral particles.
DESCOVY is a fixed-dose combination of emtricitabine and tenofovir alafenamide. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV-1 reverse transcriptase by competing with the natural substrate deoxycytidine-5'-triphosphate and incorporating into viral DNA, causing chain termination. Tenofovir alafenamide is a prodrug of tenofovir, which is also an NRTI; it is taken up by cells and converted to tenofovir diphosphate, which inhibits HIV-1 reverse transcriptase via chain termination after incorporation into viral DNA.
Oral: 500 mg twice daily with ritonavir 200 mg twice daily. Oral solution: 500 mg (1.25 mL) twice daily with ritonavir 200 mg twice daily. Must be taken with food.
One tablet (emtricitabine 200 mg / tenofovir alafenamide 25 mg) orally once daily with or without food.
None Documented
None Documented
Terminal elimination half-life is 2.1 hours during multiple dosing with ritonavir (due to CYP3A inhibition), 5.5 hours when given alone.
TAF: 0.51 hours (intracellular tenofovir diphosphate ~150 hours). FTC: 10 hours (intracellular triphosphate >39 hours). Clinical context: Long intracellular half-life supports once-daily dosing.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Tenofovir alafenamide (TAF): 80% excreted renally as unchanged drug via glomerular filtration and active tubular secretion; 15% recovered in feces. Emtricitabine (FTC): 70% excreted renally as unchanged drug via glomerular filtration and active tubular secretion; 14% as metabolites; remainder in feces.
Category C
Category C
Antiretroviral
Antiretroviral