Drug intelligence / Profile preview

177Lu-fresolimumab

Development stage
Preclinical
Lead developer
University of California, San Francisco
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

177Lu-fresolimumab is a preclinical-stage therapeutic radiopharmaceutical consisting of the pan-TGFβ-neutralizing monoclonal antibody fresolimumab conjugated to the beta-emitting radionuclide lutetium-177 (177Lu) via a DOTA chelator. Developed by the University of California, San Francisco (UCSF), it targets transforming growth factor beta (TGFβ), which is highly active and dysregulated in the tumor microenvironment of various cancers. By delivering targeted radiation to sites of active TGFβ, 177Lu-fresolimumab aims to treat solid tumors, particularly those with high TGFβ activity or where external beam radiation therapy can prime and enhance its uptake.

Other names
177Lu-DOTA-fresolimumab177Lu-freso[177Lu]Lu-fresolimumablutetium (177Lu) fresolimumab
02

Targets

TGFB1 (Transforming growth factor Beta-1 proprotein)TGFB2 (Transforming growth factor beta 2)TGFB3 (Transforming growth factor beta 3)

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