Drug intelligence / Profile preview

lutetium Lu 177 dotatate + capecitabine + somatostatin analogue LAR

Development stage
Unknown
Lead developer
Advanced Accelerator Applications
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous, Oral, Intramuscular, Subcutaneous
01

Overview

This combination therapy regimen is being investigated by the Istituto Romagnolo per lo Studio dei Tumori (IRST) for the treatment of FDG-positive, well-differentiated gastro-entero-pancreatic neuroendocrine tumors (GEP-NETs). The regimen consists of peptide receptor radionuclide therapy (PRRT) using lutetium Lu 177 dotatate, which targets somatostatin receptors (primarily SSTR2) to deliver localized beta-emitting radiation directly to tumor cells. This is combined with low-dose metronomic capecitabine, an oral fluoropyrimidine chemotherapy agent that acts as a radiosensitizer to enhance the cytotoxic effects of the PRRT. Following the completion of the PRRT cycles, patients receive maintenance therapy with long-acting release (LAR) somatostatin analogues (SS-LAR), such as octreotide LAR or lanreotide, to provide ongoing symptomatic and biochemical control. The regimen is specifically designed for patients with aggressive, metabolically active tumors that demonstrate both somatostatin receptor expression and high glucose metabolism (FDG-positivity).

Other names
Lu-PRRT + capecitabine + SS-LAR177Lu-DOTATATE + capecitabine + SS-LARLu-PRRT-Cap regimen
02

Targets

SSTR5 (Somatostatin receptor 5)SSTR (Somatostatin receptors)SSTR2 (Somatostatin receptor type 2)TS (Thymidylate synthase)

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