Drug intelligence / Profile preview

rhenium-188-DOTA-cetuximab

Development stage
Unknown
Lead developer
Timothy Marr
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Rhenium-188-DOTA-cetuximab (188Re-DOTA-cetuximab) is an investigational radioimmunotherapy (radioimmunoconjugate) consisting of cetuximab, a chimeric IgG1 monoclonal antibody targeting the epidermal growth factor receptor (EGFR), conjugated via the macrocyclic chelator DOTA to the therapeutic beta-emitting radioisotope rhenium-188 (188Re). It is being investigated as a targeted radionuclide therapy for patients with advanced head and neck squamous cell carcinoma (HNSCC) who have exhausted standard surgical and radiotherapy options. In a theranostic approach (such as in the ReCHANCE study led by Dr. Timothy Marr), patients first undergo imaging with gallium-68-DOTA-cetuximab to assess EGFR-mediated tumor uptake; those with sufficient uptake can then proceed to salvage treatment with rhenium-188-DOTA-cetuximab or lutetium-177-DOTA-cetuximab to deliver localized cytotoxic radiation directly to the tumor cells.

Other names
rhenium-188-cetuximabrhenium188-cetuximabrhenium 188-cetuximab188Re-DOTA-cetuximab188Re-cetuximab
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)EGFRvIII (Epidermal growth factor receptor variant III)

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