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

Fibroblast Activation Protein–Directed Radiotheranostic Strategy for Post-Infarction Myocardial Fibrosis (SNMMI 2026) - " The imaging probe 68Ga-DOTA-2P(FAPI)2 was synthesized to enable non-invasive evaluation of its specific accumulation in fibrotic regions following myocardial infarction (MI), whereas the therapeutic counterpart 177Lu-DOTA-2P(FAPI)2 was designed to selectively target activated fibroblasts with high fibroblast activation protein (FAP) expression... These findings suggest that radiopharmaceuticals based on DOTA-2P(FAPI)_2 offer a promising theranostic strategy for the precise targeting and modulation of post–myocardial infarction fibrosis, thereby improving adverse cardiac remodeling and promoting functional recovery from myocardial fibrosis."

Cardiovascular • Fibrosis • Immunology • Myocardial Infarction • FAP

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