Ixazomib

Information about Ixazomib

Ixazomib is a small molecule proteasome inhibitor that is used in combination with other antineoplastic agents to treat refractory multiple myeloma.

Liver safety of Ixazomib

Ixazomib is associated with a low rate of serum enzyme elevations during treatment and to rare instances of clinically apparent, acute liver injury. 

Mechanism of action of Ixazomib

Ixazomib (ix az' oh mib) is an orally available, small molecule inhibitor of the 26S proteasome, the intracellular complex that degrades proteins involved in cell signaling and cell cycle regulation.  Blocking proteasome activity prevents activation of factors involved in cell growth and resistance to chemotherapy induced apoptosis, thereby leading to cancer cell death.  Preclinical studies in vitro and in vivo suggested that ixazomib had activity against several hematologic malignancies.  Clinical trials of the addition of ixazomib to lenalidomide and dexamethasone in patients with multiple myeloma showed improvements in progression free survival. 

FDA approval information for Ixazomib

Ixazomib given in combination with lenalidomide and dexamethasone received approval for use in the United States in 2015 for therapy of refractory multiple myeloma. 

Dosage and administration for Ixazomib

Ixazomib is available in capsules of 2.3, 3 and 4 mg under the brand name Ninlaro.  The recommended starting dose is 4 mg orally on days 1, 8 and 15 of 28-day cycles of lenalidomide and dexamethasone.  A lower daily dose (3 mg) is recommended for patients with renal or hepatic impairment. 

Side effects of Ixazomib

Common side effects include nausea, diarrhea, constipation, anorexia, fatigue, peripheral edema, thrombocytopenia, neutropenia, anemia peripheral neuropathy, rash and fever.  Uncommon, but potentially severe side effects include peripheral neuropathy, bone marrow suppression, thrombocytopenia, severe diarrhea and dehydration and embryo-fetal toxicity.

 

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