Drug intelligence / Profile preview

methotrexate + Iodine I 131 tositumomab

Development stage
Unknown
Lead developer
Corixa
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

This combination therapy consists of low-dose methotrexate and the radioimmunotherapy Iodine I 131 tositumomab (Bexxar). It was specifically investigated by the University of Michigan Rogel Cancer Center for the treatment of previously untreated, advanced-stage follicular lymphoma. In this regimen, methotrexate, a small molecule antifolate, is used as an immunomodulatory agent to prevent the development of Human Anti-Mouse Antibodies (HAMA), which are common immune reactions against the murine-derived tositumomab protein. Iodine I 131 tositumomab targets the CD20 antigen on B-lymphocytes, allowing for the targeted delivery of ionizing radiation from the Iodine-131 isotope to malignant cells. The primary goal of adding methotrexate is to enhance the safety and potential for repeat dosing of the radioimmunotherapy by mitigating immunogenicity.

Brand names
Bexxar
Other names
low-dose methotrexate and BexxarIodine I 131 tositumomab and methotrexate
02

Targets

FcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)CD20 (B-lymphocyte antigen CD20)DHFR (Dihydrofolate reductase)DNA

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