Drug intelligence / Profile preview

I-131-bivatuzumab

Development stage
Discontinued
Lead developer
Boehringer Ingelheim
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

I-131-A8 (also known as I-131-bivatuzumab or I-131-BIWA 8) is a radiopharmaceutical consisting of the humanized monoclonal antibody **bivatuzumab** labeled with the radioisotope **Iodine-131**. Bivatuzumab is designed to target the variant 6 isoform of CD44 (**CD44v6**), a cell surface glycoprotein that is overexpressed in various squamous cell carcinomas, particularly head and neck squamous cell carcinoma (HNSCC). The therapeutic strategy involves the antibody binding to CD44v6-positive tumor cells and delivering localized beta-radiation from the I-131 isotope, which induces DNA double-strand breaks and subsequent apoptosis. Developed by **Boehringer Ingelheim**, I-131-A8 reached Phase I/II clinical trials. However, the development of bivatuzumab-based therapies was halted due to severe and sometimes fatal skin toxicities, specifically toxic epidermal necrolysis (TEN), which resulted from the expression of CD44v6 in normal skin keratinocytes.

Other names
Iodine-131 bivatuzumabIodine131 bivatuzumabIodine 131 bivatuzumab131I-bivatuzumab131I-A8131I-BIWA 8I-131-labeled humanized monoclonal antibody A8I131-labeled humanized monoclonal antibody A8I 131-labeled humanized monoclonal antibody A8
02

Targets

CD44v6 (CD44 variant isoform 6)

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