Drug intelligence / Profile preview

[111In]In-DOTA-HE3-ZCAIX:2

Development stage
Preclinical
Lead developer
KTH Royal Institute of Technology
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

[111In]In-DOTA-HE3-ZCAIX:2 is a radiopharmaceutical tracer composed of an affibody molecule, ZCAIX:2, that specifically binds to carbonic anhydrase IX (CAIX), a tumor-associated cell surface antigen highly expressed in renal cell carcinoma and other hypoxic tumors. The molecule is modified at the N-terminus with a histidine-glutamate (HE)3 tag to minimize off-target interactions, and conjugated site-specifically at the C-terminus with a DOTA chelator, allowing stable radiolabeling with indium-111 for SPECT imaging. The agent demonstrates high affinity (KD ~1.2 nM) for CAIX, rapid blood clearance, high tumor uptake, and high tumor-to-background contrast, making it a promising candidate for non-invasive imaging of CAIX expression in metastatic renal cell carcinoma and potentially other CAIX-positive cancers. The molecule is produced recombinantly in Escherichia coli and purified to high homogeneity[2][4][7][10].

Other names
DOTA-HE3-ZCAIX:2111In-labeled DOTA-HE3-ZCAIX:2
02

Targets

CA9 (Carbonic anhydrase IX)

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