Development and Evaluation of [68Ga]Ga-DOTA-BT1718: A Novel Imaging Agent Targeting MT1-MMP for Malignant Tumor Diagnosis.

Membrane-type 1 matrix metalloproteinase (MT1-MMP) is highly expressed in various malignant tumors. Therefore, evaluating the expression level of MT1-MMP in tumors is crucial. We designed and synthesized [68Ga]Ga-DOTA-BT1718, which targets MT1-MMP, to monitor MT1-MMP expression levels in malignant tumors via positron emission tomography/computed tomography. The results demonstrated that [68Ga]Ga-DOTA-BT1718 exhibited a high uptake in HT1080, Capan2, and U87MG tumors with high MT1-MMP expression. In contrast, it demonstrated low uptake in A549 tumors with low MT1-MMP expression. Notably, this difference was significant (p < 0.05). Preliminary clinical translation results demonstrated that [68Ga]Ga-DOTA-BT1718 exhibited significant uptake in patients with pancreatic cancer and glioma, indicating its great potential for clinical application.