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[68Ga]TIQ15-DOTA
- Development stage
- Preclinical
- Lead developer
- Chulabhorn Cancer Center
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[68Ga]TIQ15-DOTA (also referred to as [68Ga]Ga-TD-01) is a novel gallium-68-labeled positron emission tomography (PET) radiotracer developed for imaging C-X-C chemokine receptor type 4 (CXCR4) expression in tumors. It is synthesized by conjugating the potent tetrahydroquinoline-based CXCR4 antagonist TIQ15 with a DOTA-derived bifunctional chelator (such as p-NCS-Bz-DOTA, yielding the precursor TD-01) and subsequently radiolabeling with gallium-68. CXCR4 is a G-protein-coupled receptor that is highly overexpressed in more than 20 types of cancers, including glioblastoma multiforme (GBM), where it drives tumor growth, invasion, angiogenesis, and metastasis. Preclinical evaluation of [68Ga]TIQ15-DOTA in orthotopic mouse models of glioblastoma has demonstrated high binding specificity, favorable biodistribution, rapid renal clearance, and excellent in vitro stability in human plasma, highlighting its potential as a diagnostic imaging agent for CXCR4-positive malignancies.
- Other names
- 68Ga-TD-01Ga-68-TD-01Ga68-TD-01Ga 68-TD-01[68Ga]Ga-TD-01[68Ga]TIQ15-DOTA1[68Ga]TIQ15-DOTA2
02
Targets
CXCR4 (C-X-C motif chemokine receptor 4)
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