177Lu-BiOncoFAP / Philogen - LARVOL DELTA

Effect of molar dose on the in vivo tissue biodistribution profile of FAP-targeted radioligand therapeutics. (PubMed, Eur J Nucl Med Mol Imaging) - "177Lu-OncoFAP-23 presents a favorable in vivo biodistribution profile at molar doses ranging from 90 to 250 nmol/kg in tumor-bearing mice. Our results guide the design of the first-in-human Phase I clinical trial with this novel FAP-targeted radioligand therapeutic."

Journal • Preclinical • Oncology

Tumor-targeted interleukin-2 enhances the anti-cancer activity of multivalent OncoFAP radioligand therapeutics (AACR 2023) - "Moreover, when administered at very low dose 177Lu-OncoFAP-23 exhibited an enhanced anticancer activity compared to a monovalent (177Lu-OncoFAP-DOTAGA) and bivalent (177Lu-BiOncoFAP-DOTAGA) version of OncoFAP. This synergy is driven by NK-cell mediated immune response directed to the tumor, with the concomitant release of granzymes and other pro-apoptotic proteins in the tumor microenvironment. Our findings heighten OncoFAP-based RLTs as promising anti-cancer drugs for treatment of FAP-positive tumors, alone or in combination with targeted interleukin-2."

Oncology • Solid Tumor • FAP • IL2

A novel dimeric small molecule-radio conjugate targeting fibroblast activation protein with high and prolonged tumor uptake (AACR 2022) - "Notably, [177Lu]Lu-BiOncoFAP-DOTAGA did not significantly accumulate in healthy organs, thus showing an outstanding tumor-to-organ ratio (e.g., 12-to-1 tumor-to-kidney and 34-to-1 tumor-to-liver ratio, at the 24 h time point). These findings heighten BiOncoFAP as promising candidate for the development of anti-cancer radioligand therapeutics towards FAP-expressing tumor lesions."

Late-breaking abstract • Oncology • Solid Tumor

A novel dimeric FAP-targeting small molecule-radio conjugate with high and prolonged tumour uptake (bioRxiv) - "OncoFAP and BiOncoFAP displayed comparable sub-nanomolar dissociation constants towards hFAP in solution, but the bivalent BiOncoFAP bound more avidly to the target immobilized on solid supports. In a comparative biodistribution study, 177Lu-BiOncoFAP exhibited a more stable and prolonged tumour uptake than 177Lu-OncoFAP (~20% ID/g vs ~4% ID/g, at 24h p.i., respectively). Notably, 177Lu-BiOncoFAP showed favorable tumour-to-organ ratios with low kidney uptake. Both 177Lu-OncoFAP and 177Lu-BiOncoFAP displayed potent anti-tumour efficacy when administered at therapeutic doses in tumour bearing mice."

Preclinical • Oncology • Solid Tumor