Ixazomib | Proteasome inhibitor

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Ixazomib (1072833-77-2) is a selective, potent, and reversible proteasome inhibitor, which targets the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50 of 3.4 nM) and the caspase-like (β1) site (IC50 of 31 nM).1 Ixazomib displays more potent, dose-dependent and time-dependent cytotoxicity and inhibition of cell proliferation than bortezomib.2 It is a clinically useful agent  (in cotreatment with other drugs) for multiple myeloma.3 It has also been shown to be effective in Light Chain (AL) Amyloidosis and is often used in combination with cyclophosphamide and dexamethasone.4

References/Citations:

  1. Gupta et al. (2018), Clinical Pharmacology of Ixazomib: The First Oral Proteasome Inhibitor; Clin. Pharmacokinet. 58 431
  2. Gu et al. (2013), MLN2238, a proteasome inhibitor, induces caspase-dependent cell death, cell cycle arrest, and potentiates the cytotoxic activity of chemotherapy agents in rituximab-chemotherapy-sensitive or rituximab-chemotherapy-resistant B-cell lymphoma preclinical models; Anticancer Drugs 24 1030
  3. Muz et al. (2016), Spotlight on ixazomib: potential in the treatment of multiple myeloma; Drug Des. Devel. Ther. 10 217
  4. Muchtar et al. (2022), Phase 2 trial of ixazomib, cyclophosphamide, and dexamethasone for previously untreated light chain amyloidosis.; Blood Adv. 6 5429
1072833-77-2, ixazomib, Ixazomib supplier, MLN2238, Proteasome inhibitor
Alternate Name:
MLN2238

Safety Data Sheet:

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Ixazomib (1072833-77-2) is a selective, potent, and reversible proteasome inhibitor, which targets the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50 of 3.4 nM) and the caspase-like (β1) site (IC50 of 31 nM).1 Ixazomib displays more potent, dose-dependent and time-dependent cytotoxicity and inhibition of cell proliferation than bortezomib.2 It is a clinically useful agent  (in cotreatment with other drugs) for multiple myeloma.3 It has also been shown to be effective in Light Chain (AL) Amyloidosis and is often used in combination with cyclophosphamide and dexamethasone.4

References/Citations:

  1. Gupta et al. (2018), Clinical Pharmacology of Ixazomib: The First Oral Proteasome Inhibitor; Clin. Pharmacokinet. 58 431
  2. Gu et al. (2013), MLN2238, a proteasome inhibitor, induces caspase-dependent cell death, cell cycle arrest, and potentiates the cytotoxic activity of chemotherapy agents in rituximab-chemotherapy-sensitive or rituximab-chemotherapy-resistant B-cell lymphoma preclinical models; Anticancer Drugs 24 1030
  3. Muz et al. (2016), Spotlight on ixazomib: potential in the treatment of multiple myeloma; Drug Des. Devel. Ther. 10 217
  4. Muchtar et al. (2022), Phase 2 trial of ixazomib, cyclophosphamide, and dexamethasone for previously untreated light chain amyloidosis.; Blood Adv. 6 5429