Drug intelligence / Profile preview

bortezomib + tositumomab

Development stage
Phase 1
Lead developer
Takeda
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Bortezomib + tositumomab is a combination of two anticancer agents with distinct mechanisms of action. Bortezomib is a small molecule proteasome inhibitor that blocks the 26S proteasome, leading to disruption of protein degradation and induction of apoptosis in cancer cells. It is primarily used for multiple myeloma and mantle cell lymphoma. Tositumomab is a murine monoclonal antibody targeting the CD20 antigen on B-cells, often conjugated with radioactive iodine (Iodine 131) to deliver targeted radiation therapy; it was developed for the treatment of B-cell non-Hodgkin's lymphoma. The combination would theoretically provide both direct cytotoxicity via proteasome inhibition and targeted immunotherapy/radioimmunotherapy against malignant B-cells[1][2][3][6].

Brand names
BEXXAR
Other names
Iodine I 131 tositumomab
02

Targets

CD20 (B-lymphocyte antigen CD20)PSMB9 (Immunoproteasome subunit beta type-1i)PSMB1 (26S Proteasome (β1-Subunit))PSMB5 (Proteasome subunit beta Type-5)

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