Drug intelligence / Profile preview

lutetium-177

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

Lutetium-177 is a radioactive isotope of the element lutetium used as the active component in several radiopharmaceuticals for targeted cancer therapy. It is most commonly found in drugs such as Lutathera (lutetium Lu 177 dotatate) and Pluvicto (lutetium Lu 177 vipivotide tetraxetan). These agents are classified as peptide receptor radionuclide therapies (PRRT), delivering targeted beta radiation to tumor cells that express specific receptors. Lutathera is approved for treating somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), while Pluvicto targets prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer. The mechanism involves binding to tumor cell surface receptors—such as somatostatin or PSMA—followed by internalization and localized emission of cytotoxic radiation that induces DNA damage and cell death[1][2][3][4][5][7].

Brand names
LutatheraPluvicto
Other names
lutetium Lu 177 dotatatelutetium Lu 177 vipivotide tetraxetanlutetium (177Lu) oxodotreotide177Lu-dotatate177Lu-PSMA-617
02

Targets

PSMA (Prostate-specific membrane antigen)SSTR2 (Somatostatin receptor type 2)

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