177Lu-FAP-2286 is a molecule from the FAPI family developed as a theranostic pair with the diagnostic counterpart labeled with 68Ga.

177Lu-FAP-2286 is a radiolabeled drug based on a Fibroplast Activation Protein (FAP)-specific enzyme inhibitor (FAPI). FAPIs targets cancer-associated fibroblasts, which is apparently relevant as target in more than 90% of all solid tumors. Besides cancer, FAPIs may also be used for benign diseases such as fibroses, atherosclerosis, rheumatoid arthritis, sarcoidosis, etc.

Both molecules (68Ga and 177Lu-labeled molecules) were tested in a Phase 0 trial in Bad Berka in individual patients with breast cancer, colorectal cancer and pancreatic cancer. The molecule does have a very long retention time and stays in the lesion for more than 7 days. Apparently, the therapeutic trial in colorectal cancer failed.  A Phase I study is under preparation.

Target/Mechanism: Fibroblasts

Leading Emitter: beta electrons (β–)