Drug intelligence / Profile preview

iodine I-131 tositumomab + CHOP

Development stage
Unknown
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 (chop), Intravenous (iodine I-131 Tositumomab)
01

Overview

This regimen is a **combination therapy** used in the treatment of advanced follicular and other non-Hodgkin lymphomas. It consists of six cycles of standard CHOP chemotherapy (cyclophosphamide, doxorubicin, vincristine, prednisone) followed by radioimmunotherapy with iodine I-131-labeled tositumomab (Bexxar), a murine anti-CD20 monoclonal antibody conjugated to radioactive iodine. - **CHOP** is cytotoxic and targets rapidly dividing cancer cells via four drugs: cyclophosphamide (alkylates DNA), doxorubicin (intercalates DNA and inhibits topoisomerase II), vincristine (inhibits microtubule formation), and prednisone (glucocorticoid cytotoxic to lymphocytes)[2][4]. - **Iodine I-131 tositumomab** binds to the CD20 antigen on B-cells, delivering targeted radiation, resulting in cell death via both the antibody’s immune effects and the cytotoxicity of the radioactive isotope[1][3][7]. - The regimen showed improved rates of complete response in clinical trials compared to CHOP alone, with manageable toxicity and a high overall response rate[1][3][7]. - Developed for the treatment of advanced follicular lymphoma and investigated in diffuse large B-cell lymphoma[1][3][7].

Brand names
Bexxar
Other names
iodine I-131 tositumomabtositumomabCHOPcyclophosphamide + doxorubicin + vincristine + prednisone
02

Targets

CD20 (B-lymphocyte antigen CD20)DNAGR (Glucocorticoid receptor)TOP2A (DNA topoisomerase II)TUBB (Tubulin (alpha and beta subunits))

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