177Lu-IPN-01087 (177Lu-3BP-227) is a neurotensin antagonist peptide labeled with 177Lu targeting NTR-1 (or NTSR1 – neurotensin receptor-1). The drug is developed for the treatment of ductal pancreatic adenocarcinoma (DPAC) and potentially other oncology indications. Neurotensin receptors of type 1 are highly expressed in both primary tumor and metastases of invasive cancer such as pancreatic intraepithelial neoplasia (PanIN). In March 2021, rights for this molecule were sold to Fusion Pharma for development of the 225Ac labeled analogue under the name 225Ac-FPI-2059.
177Lu-IPN-01087 has completed phase I trial and showed no particular side effects. Results of this phase I trial were published in April 2018. This initial report provided clinical evidence of the feasibility of treatment of ductal pancreatic adenocarcinoma using 177Lu-IPN-01087. A Phase I/II clinical trial in subjects with solid tumors expressing neurotensin receptor type-1 (pancreas, colorectal, gastric, H&N) was initiated in May 2018.
Target/Mechanism: NTR-1 (or NTSR1) – Neurotensin Receptor-1
Leading Emitter: beta electrons (β–)