Comparative Pharmacology
Head-to-head clinical analysis: OLAPARIB versus ZEJULA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: OLAPARIB versus ZEJULA.
OLAPARIB vs ZEJULA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Poly (ADP-ribose) polymerase (PARP) inhibitor that blocks base excision repair, leading to accumulation of DNA double-strand breaks and cell death in tumors with homologous recombination repair deficiency.
Poly (ADP-ribose) polymerase (PARP) enzyme inhibitor, including PARP1, PARP2, and PARP3. Inhibits PARP catalytic activity and traps PARP-DNA complexes, leading to accumulation of DNA damage and apoptosis in BRCA-deficient tumor cells.
300 mg orally twice daily, taken with or without food. For patients with BRCA-mutated advanced ovarian cancer after ≥3 prior lines of chemotherapy; or as maintenance therapy after platinum-based chemotherapy for recurrent ovarian cancer; or for HER2-negative metastatic breast cancer with germline BRCA mutation; or for metastatic pancreatic adenocarcinoma with germline BRCA mutation after first-line platinum-based chemotherapy; or for metastatic castration-resistant prostate cancer with HRR gene mutations.
300 mg orally once daily with or without food.
None Documented
None Documented
Clinical Note
moderateOlaparib + Digoxin
"Olaparib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateOlaparib + Digitoxin
"Olaparib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateOlaparib + Deslanoside
"Olaparib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateOlaparib + Acetyldigitoxin
"Olaparib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life ~11-12 hours; steady-state reached by day 3-5; supports BID dosing
36 ± 13 hours; supports twice-daily dosing; in moderate hepatic impairment (Child-Pugh B), t1/2 prolonged to 58 hours.
Fecal (84%), renal (6%) as unchanged drug; <1% in urine as metabolites
Renal: 70.9% (11.1% unchanged); fecal: 15.5%; metabolism via carboxylesterases (CES1/CES2) and renal excretion of metabolites.
Category C
Category C
PARP Inhibitor
PARP Inhibitor