Comparative Pharmacology
Head-to-head clinical analysis: APALUTAMIDE versus ENZALUTAMIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APALUTAMIDE versus ENZALUTAMIDE.
APALUTAMIDE vs ENZALUTAMIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Apalutamide is a nonsteroidal antiandrogen that inhibits androgen receptor (AR) nuclear translocation, DNA binding, and transcription of AR target genes. It also decreases AR-mediated tumor cell proliferation and increases apoptosis.
Androgen receptor inhibitor; binds to the androgen receptor and inhibits androgen receptor nuclear translocation, DNA binding, and coactivator recruitment.
240 mg orally once daily with or without food.
160 mg orally once daily
None Documented
None Documented
Terminal elimination half-life is approximately 3 days (72 hours) for apalutamide and 3–5 days for the active metabolite N-desmethyl-apalutamide. The long half-life supports once-daily dosing and requires approximately 2–3 weeks to reach steady state.
Clinical Note
moderateEnzalutamide + Digoxin
"The serum concentration of Digoxin can be decreased when it is combined with Enzalutamide."
Clinical Note
moderateEnzalutamide + Digitoxin
"The serum concentration of Digitoxin can be decreased when it is combined with Enzalutamide."
Clinical Note
moderateEnzalutamide + Deslanoside
"Enzalutamide may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateEnzalutamide + Acetyldigitoxin
Terminal elimination half-life is approximately 5.8 days (range 2.8–10.2 days) after steady state; supports once-daily dosing.
Apalutamide and its active metabolite N-desmethyl-apalutamide are eliminated primarily via hepatic metabolism and subsequent fecal excretion. Approximately 65% of the dose is recovered in feces (as unchanged drug and metabolites) and 24% in urine (primarily as metabolites). Renal excretion of unchanged drug is negligible.
Primarily hepatic metabolism; ~70% of dose excreted in feces (as unchanged drug and metabolites), ~1% in urine as unchanged drug. Biliary excretion is a major route.
Category C
Category D/X
Androgen Receptor Inhibitor
Androgen Receptor Inhibitor
"Enzalutamide may decrease the cardiotoxic activities of Acetyldigitoxin."