Excerpts of Human Studies of Pretargeted Nuclear Medicine Using bsAb–Hapten System
| Antibody radioligand pair and pretargeting timeline | Radioligand dose | Target antigen and study population | Main findings | Reference |
|---|---|---|---|---|
| Hour 0: anti-CEA × anti-DTPA indium bsAb Hour 96–120: 111In-bivalent DTPA hapten | 100–200 MBq | CEA and medullary thyroid carcinoma | Immunogenic response in 61% of the patients. 80% true-positive tumor visualization. | (23) |
| Hour 0: hMN-14 × m734 bsAb Hour 120/168: 131I-bivalent hapten | 2.6–5.5 GBq | CEA and varied patient population with CEA-positive tumors | Tumor dose of 131I-bsAb and pretargeted 131I-hapten 2.0 Gy/GBq and 3.9 Gy/GBq, respectively. Tumor–to–whole-body ratio higher with 131I-hapten. | (28) |
| Hour 0: TF2 bsAb Hour 24–30: 68Ga-IMP288 (premedicated with antihistamine and corticosteroid) | 150 MBq | CEA and HER2-negative metastatic breast cancer | Immuno-PET showed higher total lesion sensitivity (94.7%) than 18F-FDG PET (89.6%). Immunogenic response in 16% of the patients. | ((21); NCT01730612) |
| Hour 0: TF2 bsAb Hour 30: 68Ga-IMP288 (premedicated with antihistamine and corticosteroid) | 150 MBq | CEA and metastatic colorectal cancer | Immuno-PET showed higher sensitivity (88%) and specificity (100%) than 18F-FDG PET (76% and 67%, respectively), no immunogenic response. | ((20); NCT02587247) |
| Hour 0: TF2 bsAb Hour 24/120: 111In/177Lu-IMP288 | 185 MBq (111In) 2.5–7.4 GBq (177Lu) | CEA and advanced colorectal malignancy | 10% patients experienced grade III–IV hematologic toxicity, no therapeutic effect detected. | ((17,18); NCT00860860) |
HER2 = human epidermal growth factor receptor 2.