Review

  • Marizomib, a Proteasome Inhibitor for All Seasons: Preclinical Profile and a Framework for Clinical Trials; Potts BC et al, Curr. Cancer Drug Targets, 2011 – article
  • A novel proteasome inhibitor NPI-0052 as an anticancer therapy; Chauhan et al, Brit. J. Cancer, 2006 – article

Chemistry

  • Discovery and Development of the Anticancer Agent Salinosporamide A (NPI-0052), Fenical et al, Bioorganic & Medicinal Chemistry, 2009 – article
  • Proteasome Structure, Function, and Lessons Learned from Beta-Lactone Inhibitors, Groll and Potts, Curr. Top. Med. Chem., 2011 – article

PRECLINICAL BIOLOGY AND MECHANISM OF ACTION

Lymphoid Tumors

  • Synergistic Anti-Myeloma Activity of the Proteasome Inhibitor Marizomib and the IMiD® Immunomodulatory Drug Pomalidomide, Das et al, British Journal of Haematology, 2015 – article
  • Combination of Novel Proteasome Inhibitor NPI-0052 and Lenalidomide Trigger In Vitro and In Vivo Synergistic Cytotoxicity in Multiple Myeloma, Chauhan et al, Blood, 2010– article
  • Pharmacodynamic and Efficacy Studies of the Novel Proteasome Inhibitor NPI-0052 (Marizomib) in a Human Plasmacytoma Xenograft Murine Model, Singh et al British Journal of Haematology, 2010 – article
  • NPI-0052 and Bortezomib Combinations Exhibit Synergistic Anti-Myeloma Activity, Chauhan et al, Blood, 2008 – article
  • NPI-0052 Down-regulates NF-kB Related Genes, Ahn et al, Blood, 2007– article
  • NPI-0052 Induces Caspase 8 and ROS Induced Apoptosis Alone and in Combination with HDAC Inhibitors in Leukemia Cells, Miller et al, Blood, 2007 – article
  • The Proteasome Inhibitor NPI-0052 is More Active than Bortezomib in Lymphocytes from Patients with Chronic Lymphocytic Leukemia, Ruiz et al, Mol. Cancer Ther., 2006– article
  • A Novel Orally Active Proteasome Inhibitor Induces Apoptosis in Multiple Myeloma Cells with Mechanisms Distinct from Bortezomib, Chauhan et al, Cancer Cell, 2005 – article

Solid Tumors

  • Inhibition of Epithelial to Mesenchymal Transition in Metastatic Prostate Cancer Cells by the Novel Proteasome Inhibitor, NPI-0052: Pivotal Roles of Snail Repression and Rkip Induction, Baritaki et al, Oncogene, 2009 – article
  • Proteasome Inhibition Activates EGF Receptors in Pancreatic Cancer Cells, Sloss et al, Clinical Cancer Res., 2008– article
  • NPI-0052 Blocks Proteasome and Augments Conventional Therapy in Colon Carcinoma Models Cusack et al, Clinical Cancer Res., 2006– article

Glioblastoma

  • Induction of cell death by the novel proteasome inhibitor marizomib in glioblastoma in vitro and in vivo, Manton et al, Nature, 2016 – article
  • Marizomib Activity as a Single Agent in Malignant Gliomas: Ability to Cross the Blood-Brain Barrier; Di et al, Neuro-Oncology, 2015 – article

clinical

  • Marizomib for central nervous system-multiple myeloma: Badros et al, British Journal of Haematology, 2017 – article
  • Marizomib Irreversibly Inhibits Proteasome to Overcome Compensatory Hyperactivation in Multiple Myeloma and Solid Tumour Patients: Levin et al, British Journal of Haematology, 2016 – article
  • Phase 1 Clinical Trial of Marizomib (NPI-0052) in Patients with Advanced Malignancies including Multiple Myeloma: Study NPI-0052-102 Final Results, Harrison et al, Clinical Cancer Res., 2016 – article
  • Phase 1 Study of Marizomib in Relapsed or Relapsed and Refractory Multiple Myeloma; NPI-0052-101 Part 1, Richardson et al, Blood, 2016 – article
  • Phase I Clinical Trial of Marizomib in Combination with HDAC Inhibitor Vorinostat in Patients with Melanoma, Lung and Pancreatic Carcinomas, Millward et al, Invest New Drugs, 2011 – article