Lutetium Lu 177 Dotatate is a radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential imaging and antineoplastic activities. Lutetium Lu 177 dotatate binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Tyr3-octreotate (TATE) is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NET and their metastases, while most other normal tissues express low levels of SSTRs.
CAT No: 10-101-328
CAS No:437608-50-9
Synonyms/Alias:Lutetium (177Lu) oxodotreotide
Chemical Name:2-[4-[2-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-[[(1S,2R)-1-carboxy-2-hydroxypropyl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]-7,10-bis(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate;lutetium-177(3+)
Lutetium Lu177-DOTA-TATE is a radiolabeled peptide compound that combines the somatostatin analog DOTA-TATE with the beta-emitting radionuclide Lutetium-177. As a member of the peptide receptor radionuclide conjugates, it is designed to bind with high affinity to somatostatin receptor subtype 2 (SSTR2), which is overexpressed in certain neuroendocrine cell types. The integration of DOTA-TATE as a chelator ensures stable complexation with the radiometal, enabling precise delivery of the radionuclide to target sites. In research settings, Lutetium Lu177-DOTA-TATE plays a significant role in advancing the understanding of receptor-targeted radiochemistry and the development of novel radiopharmaceuticals for molecular imaging and targeted radiolabeling studies.
Radioligand Binding Studies: Lutetium Lu177-DOTA-TATE is extensively utilized in radioligand binding assays to characterize the affinity and specificity of somatostatin analogs for SSTR2-expressing cells. By leveraging its radiolabeled properties, researchers can quantitatively assess receptor density, binding kinetics, and competitive inhibition profiles in various in vitro and ex vivo systems. This application is instrumental in validating new somatostatin analogs, optimizing receptor-targeted therapies, and elucidating receptor pharmacology in neuroendocrine tumor models.
Peptide Receptor Targeting Research: The compound is a valuable tool for investigating mechanisms of peptide receptor targeting and internalization. Its selective binding to SSTR2 allows for precise tracking of receptor-mediated endocytosis, intracellular trafficking, and subsequent processing of radiolabeled peptides. These studies provide critical insights into the dynamics of ligand-receptor interactions, receptor recycling, and the fate of conjugated radionuclides within target cells, informing the rational design of next-generation peptide-based radioconjugates.
Radiochemistry Method Development: Lutetium Lu177-DOTA-TATE supports the advancement of radiochemistry protocols related to peptide conjugation and radiometal chelation. Researchers employ this compound to optimize labeling conditions, assess radiochemical stability, and evaluate the efficiency of DOTA-based chelators under varying experimental parameters. Methodological refinements enabled by such studies are essential for ensuring reproducible synthesis, robust quality control, and scalability of peptide-radiometal conjugates for research and preclinical applications.
Biodistribution and Pharmacokinetic Profiling: The radiolabeled peptide serves as a model compound for in vivo biodistribution and pharmacokinetic investigations in animal models. By tracking the fate of Lutetium-177 within biological systems, scientists can map tissue uptake, clearance rates, and organ-specific accumulation of SSTR2-targeted conjugates. These data facilitate the evaluation of targeting efficiency, off-target effects, and dosimetry calculations, which are critical for refining the design of receptor-targeted radioligands and improving their translational potential.
Imaging Probe Validation: Lutetium Lu177-DOTA-TATE is frequently employed in the validation of novel imaging probes and detection platforms for SSTR2-expressing tissues. Its well-characterized receptor-binding profile and radiophysical properties make it an ideal standard in comparative studies assessing the sensitivity, specificity, and resolution of emerging imaging technologies. These validation efforts are essential for benchmarking new radiotracers, calibrating detection instruments, and establishing robust protocols for molecular imaging research focused on neuroendocrine and other receptor-rich tumor models.
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