Drug intelligence / Profile preview

fulvestrant + 177Lu-DOTATATE

Development stage
Phase 1
Lead developer
University of Chicago Comprehensive Cancer Center
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules, Peptides
Administration
Intramuscular, Intravenous
01

Overview

fulvestrant + 177Lu-DOTATATE is a combination therapy being investigated for the treatment of advanced pancreatic neuroendocrine tumors (pNETs). The regimen consists of fulvestrant, a selective estrogen receptor degrader (SERD) that binds to and promotes the degradation of estrogen receptors, and 177Lu-DOTATATE, a radiolabeled somatostatin analog. 177Lu-DOTATATE functions as a peptide receptor radionuclide therapy (PRRT), specifically targeting somatostatin receptors (primarily SSTR2) overexpressed on the surface of neuroendocrine tumor cells to deliver cytotoxic beta radiation from the Lutetium-177 isotope directly to the cancer cells. This combination, evaluated in clinical trials led by the University of Chicago, explores the potential for hormonal modulation to enhance the therapeutic profile of PRRT in patients with advanced pNETs.

Other names
Fulvestrant and 177Lu-DOTATATE177Lu-DOTA-TATE and FulvestrantFulvestrant + Lutathera
02

Targets

ER (Estrogen receptor)SSTR2 (Somatostatin receptor type 2)DNA

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