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). This molecule is also developed as 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

Carrier/Ligand: IPN-01087

Radiation Type: beta electrons (β^–)