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111In-untagged-G3
- Development stage
- Preclinical
- Lead developer
- UCL Cancer Institute
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Recombinant Proteins and Enzymes
- Administration
- Intravenous
01
Overview
111In-untagged-G3 is a radiolabeled designed ankyrin repeat protein (DARPin) targeting human epidermal growth factor receptor 2 (HER2). It consists of the G3 DARPin, which lacks N-terminal purification tags (such as hexahistidine or histidine-glutamate tags), conjugated to the chelator DOTA via a C-terminal cysteine and radiolabeled with indium-111 (111In). The G3 DARPin binds with picomolar affinity to domain IV of the extracellular domain of HER2 at an epitope that does not overlap with trastuzumab. 111In-untagged-G3 was developed for single-photon emission computed tomography (SPECT) imaging to assess HER2 expression in vivo, particularly in breast and gastric cancers, to help identify disease relapse and guide HER2-targeted therapies. Preclinical studies evaluated its biodistribution and tumor-targeting properties in comparison to tagged variants.
- Other names
- 111In-DOTA-untagged-G3111In-DOTA-untagged-G3 DARPin111In-untagged-G3111In-untagged-G3 DARPin
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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