Work

Synthesis and biological evaluation of 68Ga-DOTA-PLE: a Plectin-1-targeted radiotracer for PET/MR imaging of pancreatic cancer

Year: 2026

Type: article

Abstract: PURPOSE: Ga-DOTA-PLE, and evaluate its potential for pancreatic cancer imaging. METHODS: Ga, followed by radiochemical yield and stability evaluated. In vitro binding affinity and in vivo biological properties were evaluated using cell binding assays, pharmacokinetic analysis, biodistribution studies, and micro-PET/MR imaging in Plectin-1-positive BxPC-3 and Plectin-1-negative β-TC-6 models. RESULTS: Radiochemical analysis by radio-HPLC and TLC confirmed that ⁶⁸Ga-DOTA-PLE was obtained with high radiochemical purity with no detectable free ⁶⁸Ga or colloidal species. The tracer demonstrated excellent in vitro stability, maintaining a radiochemical purity (RCP) of > 90% after incubation in PBS and serum at 37 °C for 2 h. In vitro binding assays revealed specific binding of ⁶⁸Ga-DOTA-PLE to Plectin-1, as evidenced by significantly higher uptake in Plectin-1-positive BxPC-3 cells than in Plectin-1-negative β-TC-6 cells (P<0.001). Pharmacokinetic evaluation indicated rapid blood clearance, with distribution (T₁/₂α) and elimination (T₁/₂β) half-lives of 2.99 min and 18.99 min, respectively. Biodistribution studies performed prominent tumor accumulation (4.41 ± 1.05%ID/g) at 30 min post-injection. while the radiotracer was primarily excreted via the renal pathway (8.65 ± 1.61%ID/g), exhibiting low hepatic and intestinal background. Micro-PET/MR imaging clearly delineated tumor lesions, and identified 15-30 min post-injection as the optimal imaging window, during which the tumor-to-muscle (T/M) ratio reached its maximum (2.91 ± 0.38).

Source: European Journal of Pharmaceutical Sciences

DOI: 10.1016/j.ejps.2026.107638