177Lu-DOTA-FAPI / Xiamen University - LARVOL DELTA

Linker-Driven Breakthrough: Design of a Novel Linker for Enhanced Theranostic Performance of FAPI Trimer. (PubMed, J Med Chem) - "Moreover, 177Lu-DOTA-FAPI-FUSCC-Tri highlights its potential as a dual-purpose agent for the integrated diagnosis and treatment of FAP-expressing tumors. This study identified a novel FAP trimer linker and successfully developed a high-performance FAP trimer based on it."

Breakthrough therapy • Journal • Oncology • FAP

Safety, Biodistribution, and Dosimetry of Fibroblast Activation Protein and Integrin α v β 3 dual Targeting radioligand 177 Lu-DOTA-FAPI-RGD: Preclinical and First-in-Human Results (EANM 2025) - No abstract available

First-in-human • P1 data • Preclinical • Oncology

68Ga/177Lu-DOTA-FAPI-RGD in Radioiodine-refractory Differentiated Thyroid Cancer: A Case Analysis (ATA 2025) - "After 10 days of treatment with lenvatinib (12 mg qd), the patient experienced cardiac discomfort. The patient continued to be followed up and was provided with symptomatic treatment.Conclusion : We report for the first time the practical application of ⁶⁸Ga/¹⁷⁷Lu-DOTA-FAPI-RGD in the theranostic approach for iodine-refractory differentiated thyroid cancer. Future studies should focus on further optimizing treatment protocols to enhance efficacy and ensure safety."

Clinical • Anemia • Oncology • Solid Tumor • Thrombocytopenia • Thyroid Gland Carcinoma • Thyroid Gland Papillary Carcinoma

Preliminary Safety, Biodistribution, and Dosimetry of Fibroblast activation protein and Integrin αvβ3 dual targeting radioligand 177Lu-DOTA-FAPI-RGD: First-in-Human Results (SNMMI 2025) - "Administration of 177Lu-DOTA-FAPI-RGD was well tolerated by all patients, with no reports or observations of adverse symptoms and clinically detectable pharmacological effects. The whole-body effective dose was 0.06±0.03 Gy/GBq. The mean absorbed doses of red marrow, liver, spleen and kidneys were 0.04±0.02 Gy/GBq, 0.56±0.44 Gy/GBq, 0.28±0.13 Gy/GBq, 0.34±0.27 Gy/GBq, respectively. Significant uptake and long tumor retention of 177Lu-FAPI-RGD resulted in high absorbed tumor doses, such as 4.3±0.7 Gy/GBq in lung metastases, and 4.0±1.8 Gy/GBq in peri metastases."

Clinical • P1 data • Anemia • Hematological Disorders • Leukopenia • Oncology • Pain • Pancreatic Cancer • Thrombocytopenia

Development of dual targeting heterodimer 177Lu-LNC1009 for cancer theranostics (SNMMI 2024) - "For the comparison, SPECT images of 177Lu-DOTA-NC1007, 177Lu-EB-RGD, and 177Lu-LNC1004 (177Lu-EB-FAPI) were also performed in U87MG tumor model...SPECT imaging of 177Lu-LNC1009 showed significantly improved tumor uptake and retention than those of 177Lu-DOTA-FAPI-RGD... 177Lu-LNC1009 was successfully synthesized and radiolabeled with high radiochemical purity and stability. With significantly improved absolute tumor uptake and decreased normal organ uptake, 177Lu-LNC1009 has the potential to enhance therapy effect that promises clinical translation for the treatment of many types of solid tumors that are FAP+/αvβ3-, FAP-/αvβ3+, or FAP+/αvβ3+."

Oncology • Solid Tumor • FAP