Clinical applications of receptor-binding radiopharmaceutical 99m Tc-Tilmanocept: sentinel node biopsy and beyond
- PDF / 465,233 Bytes
- 6 Pages / 595.276 x 790.866 pts Page_size
- 65 Downloads / 194 Views
MINI-REVIEW
Clinical applications of receptor‑binding radiopharmaceutical 99m Tc‑Tilmanocept: sentinel node biopsy and beyond Alice Lorenzoni1 · Mario Santinami2 · Marco Maccauro1 Received: 1 October 2020 / Accepted: 21 October 2020 © Italian Association of Nuclear Medicine and Molecular Imaging 2020
Abstract Purpose 99mTc-tilmanocept is the first mannose-containing, receptor-directed, radiopharmaceutical for molecular imaging and mapping of sentinel lymph nodes (SLNs) in solid tumor staging. This review focuses on the approved and innovative clinical application of 99mTc-tilmanocept. Results and conclusion 99mTc-Tilmanocept is a new-generation radiotracer designed to overcome certain limitations of the conventionally used radiocolloids. The superior efficacy profile of 99mTc-tilmanocept has been demonstrated in several preclinical and clinical studies based on its specific properties like rapid injection site clearance, high uptake in the first node, and low distal node accumulation. The capability of 99mTc-tilmanocept for selective molecular imaging of the CD206 receptor may be used for diagnosis and treatment of several macrophage mediated diseases, including autoimmune diseases, infectious diseases (HIV and tuberculosis), neurodegenerative disorders (dementias) and cardiovascular disease (vulnerable plaque and atherosclerosis). Keywords 99mTc-tilmanocept · Sentinel node biopsy · CD206 receptor · Tumor-associated macrophages
Introduction 99m
Tc-tilmanocept is the first mannose-containing, receptordirected, radiopharmaceutical for molecular imaging and mapping of sentinel lymph nodes (SLNs) in solid tumor staging. It is a synthetic nanomolecule (∼18 kDa; 7 nm) consisting of multiple units of mannose and diethylene triamine penta-acetic acid, attached to a 10-kDa dextran backbone designed for selective molecular imaging of tissues bearing the CD206 receptor [1]. The mannose residues serve as a ligand for receptors expressed on myeloid cells for recognition and binding. The diethylene triamine penta-acetic acid serves as an attachment site for labeling the macromolecule with Technetium-99 m [2]. The presence of mannose predicts its binding to mannose-binding lectins, such as the mannose receptor (MR;CD206), a member of the C-type lectin family, that is expressed on most types * Alice Lorenzoni [email protected] 1
Nuclear Medicine, Fondazione IRCCS Istituto Nazionale Tumori, Milan, Italy
Melanoma and Sarcoma, Department of Surgery, Fondazione IRCCS Istituto Nazionale Tumori, Milan, Italy
2
of macrophages and on dendritic cell subsets, but not on monocytes [3]. The MR is considered to be a prototypic and widely used marker for alternatively activated type 2 (M2) macrophages. It preferentially recognizes glycoconjugates containing terminal mannose, fucose, GlcNAc, and glucose [4]. Apart from its function as a phagocytic receptor for numerous mannose-coated microbes, the MR functions in endocytosis as a scavenger receptor for clearing unwanted mammalian high mannose N-linked glyc
Data Loading...
