Preclinical Evaluation and First-in-Human Study of [⁶⁸Ga]Ga-αvβ6–2: A Novel Dimeric Integrin αvβ6-Targeted PET Probe for Pancreatic Cancer Imaging

Molecular Pharmaceutics, Год журнала: 2025, Номер unknown

Опубликована: Апрель 7, 2025

Integrin αvβ6 is highly expressed in pancreatic cancer, making it an ideal target for molecular imaging diagnosis. Multimerization considered effective strategy to increase the accumulation of probes tumors. Here, we synthesized monomeric and dimeric αvβ6-targeting probes, labeled with 68Ga, designated them [68Ga]Ga-αvβ6-1 [68Ga]Ga-αvβ6-2, respectively. Both vitro vivo studies were conducted using human cancer BxPC-3 cells tumor-bearing mice. Additionally, positron emission tomography/computed tomography (PET/CT) [68Ga]Ga-αvβ6-2 was performed three patients cancer. In demonstrated that exhibited greater binding affinity, cellular uptake, internalization than did [68Ga]Ga-αvβ6-1. Micro-PET/CT biodistribution revealed superior performance [68Ga]Ga-αvβ6-2. Furthermore, first-in-human evaluation highlighted favorable distribution diagnostic efficacy These results underscore effectiveness multimerization application αvβ6-targeted suggesting may possess clinical translation potential.

Язык: Английский

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Engineering IgG antibodies for intracellular targeting and drug delivery

Journal of Controlled Release, Год журнала: 2025, Номер unknown, С. 113727 - 113727

Опубликована: Апрель 1, 2025

Язык: Английский

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Development of a PSMA and EphA2 dual-receptor-activated fluorescent probe for wash-free prostate cancer cell imaging

Bioorganic & Medicinal Chemistry, Год журнала: 2025, Номер 125, С. 118217 - 118217

Опубликована: Апрель 27, 2025

Язык: Английский

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Nanotechnology-mediated precision drug delivery strategies for breast cancer treatment

Biomedicine & Pharmacotherapy, Год журнала: 2025, Номер 188, С. 118224 - 118224

Опубликована: Июнь 1, 2025

Язык: Английский

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