¹⁷⁷Lu-OncoFAP-23 is a small molecule radiotracer with ultra high affinity for Fibroblast Activation Protein (FAP). The molecule consists of a (i) small organic ligand targeting FAP, (ii) an innovative spacer structure and (iii) a DOTAGA chelator for the labelling with 177Lutetium.
Since FAP is overexpressed in more than 90% of epithelial cancers (e.g., malignant breast, colorectal, ovarian, lung, skin, prostate and pancreatic cancers, as well as in some soft tissue and bone sarcomas), ¹⁷⁷Lu-OncoFAP-23 is being developed for the treatment of different FAP-positive tumor entities.
¹⁷⁷Lu-OncoFAP-23 displays best-in-class performance both in vitro and in vivo with the highest reported affinity to the FAP antigen. In preclinical models of cancer, the product has shown a rapid and selective accumulation in the tumor mass with an exceptionally long tumor residence time. The molecule has shown potent anti-tumor activity both as single agent and in combination with the immunocytokine L19-IL2 (Darleukin) .
A first-in-human trial with ¹⁷⁷Lu-OncoFAP-23 alone and in combination with the immunocytokine L19-IL2 has been approved by regulatory authorities and the first patients are expected to be treated around Q1 2026.
ONGOING CLINICAL TRIALS
- OncoFAP-68Ga has recently entered in a first-in-man imaging study in patients with advanced solid cancers
- Additional studies with OncoFAP-68Ga (Imaging) and OncoFAP-177Lu (Therapy) are about to start
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- A first-in-human trial with ¹⁷⁷Lu-OncoFAP-23 alone and in combination with the immunocytokine L19-IL2 (Darleukin) has been approved by regulatory authorities and the first patients are expected to be treated around Q1 2025 (NCT06640413).
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References
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Backhaus et al. (2021) Eur J Nucl Med Mol Imaging, 10.21203/rs.3.rs-969176/v1
Millul et al. (2021) PNAS, 118, 16, e2101852118