Marizomib: A Potent IV/PO Proteasome Inhibitor

Marizomib is a novel, brain-penetrant proteasome inhibitor, which inhibits all three proteasome subunits.

Celgene acquired the assets related to marizomib from Triphase in November 2016 and Triphase continues to support Celgene with development – including completing a Phase 1 study in relapsed refractory multiple myeloma, a Phase 2 study in recurrent glioma and a Phase 1 study in newly diagnosed glioma. Marizomib is under development in both intravenous (IV) and oral formulations as a proteasome inhibitor for hematologic malignancies and solid tumors. The IV formulation has been evaluated in more than 350 patients in multiple clinical studies in patients with solid and hematologic malignancies, either as a single agent or in combination with dexamethasone, a histone deacetylase inhibitor, or an immunomodulatory drug.

Marizomib is currently being evaluated in a proof-of-concept clinical study in combination with bevacizumab (Avastin®) in patients with Grade IV malignant glioma (glioblastoma), and has received Orphan Drug designation in glioblastoma in the United States from the FDA. In addition, marizomib is also being developed in combination with pomalidomide and dexamethasone in patients with relapsed and refractory multiple myeloma, and has received Orphan Drug designation for marizomib in multiple myeloma in the United States and the European Union.