Comparative Pharmacology
Head-to-head clinical analysis: BORTEZOMIB versus NINLARO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BORTEZOMIB versus NINLARO.
BORTEZOMIB vs NINLARO
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Reversible inhibition of the 26S proteasome, disrupting protein homeostasis and leading to apoptosis in cancer cells.
Ixazomib is a reversible proteasome inhibitor that preferentially binds and inhibits the chymotrypsin-like activity of the 20S proteasome, leading to accumulation of misfolded proteins, induction of apoptosis, and inhibition of cell growth in multiple myeloma cells.
1.3 mg/m2 intravenously or subcutaneously twice weekly for 2 weeks (days 1, 4, 8, 11) followed by a 10-day rest period (days 12-21) for cycles 1-8; for cycles 9-16, administer once weekly on days 1, 8, 15, 22 followed by a 13-day rest period.
4 mg orally once weekly on days 1, 8, and 15 of a 28-day cycle, in combination with lenalidomide and dexamethasone.
None Documented
None Documented
Clinical Note
moderateBortezomib + Digoxin
"Bortezomib may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateBortezomib + Digitoxin
"Bortezomib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateBortezomib + Deslanoside
"Bortezomib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateBortezomib + Acetyldigitoxin
"Bortezomib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life 40-100 hours (mean ~76 hours); supports twice-weekly dosing schedule.
The terminal elimination half-life of ixazomib is 9.5 days, supporting once-weekly dosing.
Primarily hepatic metabolism via CYP3A4 and CYP2C19; <10% excreted unchanged in urine; fecal elimination accounts for ~40% of total clearance.
Following oral administration of 14C-ixazomib, approximately 80% of the radioactivity is recovered in urine (11% as unchanged drug) and 5% in feces.
Category D/X
Category C
Proteasome Inhibitor
Proteasome Inhibitor