First-in-Human Study of the Radioligand 68Ga- DOTA-EphA2

Development and Evaluation of 68Ga-DOTA-EphA2: A Novel Imaging Agent Targeting EphA2 for Malignant Tumor

Purpose Ephrin type-A receptor 2 (EphA2) is a receptor tyrosine kinase overexpressed in various solid tumors and associated with tumor progression, metastasis, and poor prognosis. However, noninvasive imaging tools for assessing EphA2 expression in vivo remain limited. This study aims to develop a novel 68Ga-labeled EphA2-targeting positron emission tomography (PET) tracer for specific imaging of EphA2-positive malignancies.

Purpose Ephrin type-A receptor 2 (EphA2) is a receptor tyrosine kinase overexpressed in various solid tumors and associated with tumor progression, metastasis, and poor prognosis. However, noninvasive imaging tools for assessing EphA2 expression in vivo remain limited. This study aims to develop a novel 68Ga-labeled EphA2-targeting positron emission tomography (PET) tracer for specific imaging of EphA2-positive malignancies.

Inclusion Criteria:

• Adults aged 18-80 years
• Patients with suspected or histologically confirmed malignant tumors At least one measurable lesion identified by conventional imaging (CT, MRI, or ultrasound)
• Eastern Cooperative Oncology Group (ECOG) performance status of 0-2
• Ability to understand the study procedures and provide written informed consent
• Adequate organ function allowing PET/CT examination

Exclusion Criteria:

• Pregnant or breastfeeding women
• Severe hepatic, renal, cardiovascular, or pulmonary dysfunction considered --unsuitable for PET/CT imaging
• Known allergy or hypersensitivity to study-related compounds
• Patients unable to tolerate PET/CT examination or remain still during image acquisition
• Participation in other investigational drug or radionuclide studies within 4 weeks prior to enrollment
• Any medical or psychiatric condition judged by the investigators to interfere with study participation or interpretation of imaging results