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FAP-2286 is an investigational radiopharmaceutical, a type of medicine that combines a radioactive substance with a targeting molecule. It is designed to bind to fibroblast activation protein (FAP), a protein found in large amounts on the surface of cancer-associated fibroblasts, which are cells that support tumor growth. The substance is not yet authorised as a medicine and is being investigated in clinical trials. The full name used in the trial registry is [177Lu]Lu-FAP-2286, where 177Lu (lutetium-177) is the radioactive component.[1] A related imaging agent, called [⁶⁸Ga]Ga-HKG301 or AAA514, is also being studied to detect cancer using PET/CT scans.[2]
FAP-2286 works by attaching to fibroblast activation protein on the surface of cancer-associated fibroblasts. Once bound, the radioactive lutetium-177 delivers radiation directly to the tumor area. This approach is called peptide-targeted radionuclide therapy, meaning a small peptide carries the radioactive element to the cancer cells. The first-in-humans study of [177Lu]Lu-FAP-2286 reported that the substance was taken up by tumors in people with various adenocarcinomas, which are cancers that start in glandular tissue.[3]
FAP-2286 is given by intravenous infusion, meaning it is delivered directly into a vein. In the main trial, the dose is reported in gigabecquerels (GBq), a unit of radioactivity. The imaging agent AAA514 is given by intravenous administration at a dose of 240 megabecquerels (MBq) in the breast cancer imaging trial.[2]
Two clinical trials involving FAP-2286 or its related imaging agent are currently authorised. The main trial, called LuMIERE, is a Phase 1/2 study that will evaluate the safety, tolerability, and preliminary activity of [177Lu]Lu-FAP-2286 in 156 participants with advanced solid tumors. It includes a Phase 2 dose expansion part to measure the objective response rate (ORR), which is the proportion of participants whose tumors shrink or disappear after treatment, using RECIST v1.1 criteria.[1] The trial also tests the substance in combination with chemotherapy regimens: mFOLFIRINOX in PDAC and nab-paclitaxel in NSCLC.
The second trial is a Phase 2 imaging study called FAPILOUS. It will evaluate the accuracy of [⁶⁸Ga]Ga-HKG301 PET/CT for staging and restaging 65 patients with newly diagnosed primary breast cancer. The primary outcomes are sensitivity, specificity, predictive values, and accuracy of the imaging method.[2]
The LuMIERE trial is open to adults with metastatic breast carcinoma, recurrent or metastatic NSCLC, or locally advanced unresectable or metastatic PDAC. The FAPILOUS imaging trial is open to patients with newly diagnosed primary breast cancer. Both trials are currently in the authorised status, meaning they have received regulatory approval but may not yet be recruiting participants.[1][2]
The LuMIERE trial measures investigator-assessed objective response rate per RECIST v1.1, as well as dose-limiting toxicities, adverse events, serious adverse events, and clinical laboratory abnormalities. These measures help researchers understand both how well the treatment works and how safe it is. The FAPILOUS trial measures the diagnostic accuracy of the imaging agent, including sensitivity, specificity, and predictive values for staging and restaging breast cancer.[1][2]
The first-in-humans study of [177Lu]Lu-FAP-2286 reported feasibility, biodistribution, and preliminary dosimetry results, but specific side effects were not detailed in the available summary.[3] The ongoing LuMIERE trial is designed to evaluate safety and tolerability, including dose-limiting toxicities and adverse events, but results are not yet available.[1]
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