The NINLARO® (ixazomib) Mechanism of Action

NINLARO is a targeted, reversible proteasome inhibitor.1

Mechanism of Action

Illustration of NINLARO® (ixazomib) Mechanism of Action.

NINLARO binds the β5 subunit of the 20S proteasome and inhibits its chymotrypsin-like activity1

A buildup of proteins results from the inhibition of proteasome activity, leading to cytotoxicity and apoptosis of multiple myeloma cells2

Proteasome inhibition is a cornerstone of multiple myeloma treatment because cancer cells have a higher level of proteasome activity and are more sensitive to its proapoptotic effects3

Effects of proteasome inhibition with NINLARO

  • NINLARO demonstrated in vitro cytotoxicity against myeloma cells from patients who had relapsed after multiple prior therapies1
  • The combination of NINLARO+lenalidomide demonstrated synergistic cytotoxic effects in multiple myeloma cell lines1

PHARMACOKINETICS

Absorption and distribution

  • After NINLARO oral administration, the median time to achieve peak plasma concentrations was 1 hour1
  • The mean absolute oral bioavailability was 58%, based on population PK analysis1

Metabolism and elimination

  • The terminal half-life of NINLARO is 9.5 days1
  • There was no clinically meaningful effect of age, sex, body surface area, or race on the clearance of NINLARO based on population PK analysis1

NINLARO patient profiles

Different patient types are appropriate for treatment with NINLARO.

NINLARO dosing

Find the dosing schedule for the NINLARO all-oral triplet regimen and information on dosage modifications.