PIPELINE > TRIAL OVERVIEW

177Lu-FAP
LY4337713
[Lu-177]-FAP

Lindner T, et al1; Xin L, et al2

Target

177Lu-FAP is a next-generation FAP radioligand. It contains the beta-emitting radioisotope 177-Lutetium and a linker that binds the ligand to FAP on CAFs.

Molecule
FAP, a 170kDa membrane-bound prolyl endopeptidase,3,4 is expressed during developmental stages5 but is rarely present in healthy adult tissues.6,7 It is also upregulated at sites of active tissue remodeling, such as during wound healing.8 FAP is prominently expressed on cancer-associated fibroblasts (CAFs).9 It is highly upregulated in cancer due to overexpression on CAFs6,7,10,11 and in some mesenchymal-origin tumors like sarcoma and mesothelioma.12
Clinical Development

LY4337713 preclinical data support further evaluation in clinical trials.

References

  1. Lindner T, et al. Cancers (Basel). 2021;13(22):5744. 
  2. Xin L, et al. Front Oncol. 2021;11:648187.
  3. Bodei L, et al. J Clin Oncol. 2023;41(16 suppl):TPS3161. doi:10.1200/JCO.2023.41.16_suppl.TPS3161 
  4. Domen A, et al. Cancers (Basel). 2021;13(5):987. doi:10.3390/cancers13050987
  5. Niedermeyer J, et al. Int J Dev Biol. 2001;45(2):445-447.
  6. Rettig WJ, et al. Proc Natl Acad Sci U S A. 1988;85(9):3110-3114. doi:10.1073/pnas.85.9.3110
  7. Dolznig H, et al. Cancer Immun. 2005;5:10.
  8. Jacob M, et al. Curr Mol Med. 2012;12(10):1220-1243. doi:10.2174/156652412803833607
  9. Qin Y, et al. Ann Surg Oncol. 2025;32(3):1941-1952. doi:10.1245/s10434-024-16593-y
  10. Garin-Chesa P, et al. Proc Natl Acad Sci U S A. 1990;87(18):7235-7239. doi:10.1073/pnas.87.18.7235
  11. Scanlan MJ, et al. Proc Natl Acad Sci U S A. 1994;91(12):5657-5661. doi:10.1073/pnas.91.12.5657
  12. Dohi O, et al. Histopathology. 2009;55(4):432-440. doi:10.1111/j.1365-2559.2009.03399.x
For information on trial enrollment, locations, and more, call 1-800-545-5979.