This study suggested the possible application of FAPI radioligand therapy in FAP-expressing pancreatic cancer. Further evaluation is necessary to find the best radionuclide with shorter half-life, as well as the combination with therapies targeting tumour cells directly.

2023年11月7日 · The findings suggest that [¹⁷⁷Lu]Lu-DOTAGA.FAPi dimer therapy is well-tolerated, safe, and effective for treating end-stage metastatic breast cancer patients. [¹⁷⁷Lu]Lu-DOTAGA.FAPi dimer treatment demonstrated promising efficacy in patients with advanced breast cancer, as indic …

2021年9月18日 · Fibroblast activation protein (FAP), which has high expression in cancer-associated fibroblasts of epithelial cancers, can be used as a theranostic target. Our previous study used 64 Cu and 225 Ac-labelled FAP inhibitors (FAPI-04) for a FAP-expressing pancreatic cancer xenograft imaging and therapy.

2023年11月7日 · Between November 2020 and March 2023, a compassionate treatment approach was utilized to administer [177 Lu]Lu-DOTAGA.FAPi dimer radionuclide therapy to heavily pretreated patients with advanced breast cancer. Nineteen patients (18 females, 1 male) with metastatic breast cancer participated in the study, with an average age of 44.6 ± 10.7 years.

2024年7月27日 · [177 Lu]Lu-FAPI-2286 PTRT, utilized for diverse cancer types, exhibited favorable tolerability in sarcoma patients, with minimal side effects, long-lasting retention of the radiopeptide within the tumor, and promising therapeutic effects.

2025年1月9日 · Fibroblast activation protein (FAP), which is overexpressed in cancer-associated fibroblasts (CAFs), represents a promising target for cancer diagnosis and therapy. Hypoxia is a common feature of solid tumors. A bivalent agent, DOTA-NI-FAPI-04 (<b>1</b>), was developed by incorporating hypoxia-sensi …

2023年5月26日 · Beside DOTA-TOC and PSMA-analogues, FAP analogues also received attention as theranostic radiopharmaceuticals (Fig. 1) (Treglia et al. 2021). Recently, FAPI-46 was successfully radiolabeled with lutetium-177 by Eryilmaz and Kilbas et al. (2021).

2024年11月12日 · [177Lu]Lu-FAPI-XT注射液是一种 靶向FAP的放射性体内治疗药物，通过将放射性核素镥-177靶向运送至FAP阳性表达的实体瘤 实现肿瘤的精准治疗。 研究药物： [177Lu]Lu-FAPI-XT注射液 试验类型： 单臂试验 适应症： 甲状腺癌等晚期实体瘤（二线及以上） 用药周期

2024年6月1日 · In this study, nitroimidazole was added to FAPI-04 to give DOTA-NI-FAPI-04 (compound 1) which led to excellent tumor accumulation and prolonged residence time after labeling with Ga-68 and Lu-177. Methods: Compound 1 was synthesized and labeled with Ga-68 and Lu-177 at 95℃ for 10 min and 30 min, respectively.

2021年4月16日 · A fully automated synthesis of [177Lu]Lu-FAPI derivatives was achieved on the Modular Lab Eazy (ML Eazy) with high radiochemical yield ( [177Lu]Lu-FAPI-04; 88% ± 3, [177Lu]Lu-FAPI-46; 86% ± 3). Chromatographic analysis indicated the formation of radiosynthesis with an absolute radiochemical purity (99%).