177Lu-DOTA-2P(FAPI)2 / Xiamen University - LARVOL DELTA

Fibroblast Activation Protein-Based Radio-Theranostics Attenuates Postinfarction Myocardial Fibrosis. (PubMed, ACS Appl Mater Interfaces) - "To enable precise diagnosis and intervention, we developed a FAP-dimer-based imaging/therapeutic platform using 68Ga-DOTA-2P(FAPI)2 for noninvasive visualization of fibroblast activation and its therapeutic analogue 177Lu-DOTA-2P(FAPI)2 for radionuclide therapy...No significant toxicity was observed within 7 days post-treatment. scRNA-seq revealed selective depletion of activated fibroblasts and suppression of pro-inflammatory signaling in the infarct border zone, confirming the antifibrotic mechanism."

Journal • Cardiovascular • Fibrosis • Immunology • Myocardial Infarction

FAP-targeted radioligand therapy with 68Ga/177Lu-DOTA-2P(FAPI)2 enhance immunogenicity and synergize with PD-L1 inhibitors for improved antitumor efficacy (SNMMI 2025) - "Our findings indicated that FAP-targeting radiopharmaceuticals can induce DNA double-strand breaks and up-regulate PD-L1 expression, with 177Lu-DOTA-2P(FAPI)2 proving to be more effective than 68Ga-DOTA-2P(FAPI)2. Both 68Ga-DOTA-2P(FAPI)2 and 177Lu-DOTA-2P(FAPI)2 radiopharmaceuticals significantly improved therapeutic outcomes when combined with anti-PD-L1 monoclonal antibody (αPD-L1 mAb). Notably, the combination of 177Lu-DOTA-2P(FAPI)2 with αPD-L1 mAb immunotherapy eliminated tumors in mouse models."

Clinical • IO biomarker • Oncology • CD8 • FAP • FASLG