Drug intelligence / Profile preview

lutetium Lu 177 LNC1004

Development stage
Phase 1
Lead developer
Yantai Lannacheng Biotechnology
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

lutetium Lu 177 LNC1004 (also known as 177Lu-LNC1004) is an investigational radiopharmaceutical and radioligand therapy targeting fibroblast activation protein (FAP). Developed by Yantai LNC Biotechnology (a subsidiary of Yantai Dongcheng Pharmaceutical Group), the drug consists of an Evans blue (EB)-modified fibroblast activation protein inhibitor (FAPi) conjugated with the chelator DOTA and radiolabeled with the beta-emitting radioisotope lutetium-177 (Lu-177). The Evans blue modification allows the compound to bind reversibly to serum albumin, extending its blood half-life and enhancing tumor accumulation and retention. Upon binding to FAP-expressing cancer-associated fibroblasts (CAFs) in the tumor microenvironment, the radioconjugate is internalized, delivering a localized cytotoxic dose of beta radiation to destroy tumor cells. It is being evaluated in clinical trials for the treatment of FAP-positive advanced malignant solid tumors, including metastatic radioiodine-refractory differentiated thyroid cancer (RAIR-DTC), for which it has received FDA Fast Track designation.

Other names
177Lu-EB-FAPI177Lu-Evans blue-FAP inhibitorlutetium Lu 177-LNC1004
02

Targets

FAP (Fibroblast activation protein alpha)

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