Comparative Pharmacology
Head-to-head clinical analysis: ATMEKSI versus REVATIO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ATMEKSI versus REVATIO.
ATMEKSI vs REVATIO
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
ATMEKSI (atazanavir/cobicistat) is a fixed-dose combination of atazanavir, an HIV-1 protease inhibitor that inhibits viral protease, preventing cleavage of viral polyproteins and resulting in immature non-infectious virions, and cobicistat, a pharmacokinetic enhancer that inhibits CYP3A, increasing atazanavir exposure.
REVATIO (sildenafil) is a phosphodiesterase type 5 (PDE5) inhibitor. By inhibiting PDE5, it increases cyclic guanosine monophosphate (cGMP) levels in pulmonary vascular smooth muscle, leading to vasodilation and reduced pulmonary vascular resistance.
1.5 mg/kg IV every 4 weeks
20 mg orally three times daily, administered 4-6 hours apart.
None Documented
None Documented
Terminal elimination half-life is 12 hours; renally impaired patients have prolonged half-life up to 24 hours.
Terminal elimination half-life ~4 hours (range 3-5 hours) in steady state; similar in pulmonary arterial hypertension patients.
Primarily renal (80% unchanged) and biliary/fecal (15% as metabolites).
Primarily hepatic metabolism (CYP3A4) to N-desmethyl sildenafil (active). Renal excretion accounts for ~80% as metabolites; ~13% fecal.
Category C
Category C
PDE5 Inhibitor
PDE5 Inhibitor