Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
|Solubility (25°C)||DMSO 100 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Hanady A Elgamal, et al. Nanoscale Res Lett. PEG@ Carbon Nanotubes Composite as an Effective Nanocarrier of Ixazomib for Myeloma Cancer Therapy
 Marco Salvini, et al. Expert Opin Drug Metab Toxicol. Pharmacokinetic drug evaluation of ixazomib citrate for the treatment of multiple myeloma
 Beverly A Teicher, et al. Biochem Pharmacol. Proteasome inhibitors
 Paul G Richardson, et al. Future Oncol. The investigational proteasome inhibitor ixazomib for the treatment of multiple myeloma
 Massimo Offidani, et al. Onco Targets Ther. An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma
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Zetomipzomib (KZR-616) is the first immunoproteasome inhibitor that selectively targets the immunoproteasome subunits LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7). Zetomipzomib has potential for use in a variety of autoimmune diseases.
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