Drug intelligence / Profile preview

methotrexate + Iodine I 131 tositumomab

Development stage
Discontinued
Lead developer
GSK
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
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.

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

Targets

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

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