Premium
Preparation, evaluation, and first clinical use of 177 Lu‐labeled hydroxyapatite (HA) particles in the treatment of rheumatoid arthritis: utility of cold kits for convenient dose formulation at hospital radiopharmacy
Author(s) -
Chakraborty Sudipta,
Vimalnath K. V.,
Rajeswari A.,
Shinto Ajit,
Sarma H. D.,
Kamaleshwaran K.,
Thirumalaisamy P.,
Dash Ashutosh
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3202
Subject(s) - chemistry , rheumatoid arthritis , radiochemistry , nuclear medicine , nuclear chemistry , medicine
While radiation synovectomy (RSV) constitutes a successful paradigm for the treatment of arthritis, a major cornerstone of its success resides in the selection of appropriate radiolabeled agent. Among the radionuclide used for RSV, the scope of using 177 Lu [ T 1/2 = 6.65 d, E β (max) = 497 keV, E γ = 113 KeV (6.4%), 208 KeV (11%)] seemed to be attractive owing to its suitable decay characteristics, easy availability, and cost‐effective production route. The present article describes a formulation of 177 Lu‐labeled hydroxyapatite (HA) using ready‐to‐use kits of HA particles of 1–10 µm size range. The developed kits enable convenient one‐step preparation of 177 Lu‐HA (400 ± 30 MBq doses) in high radiochemical purity (>99%) and stability at hospital radiopharmacy. The preparation showed promising results in pre‐clinical studies carried out in Wistar rats bearing arthritis in knee joints. In preliminary clinical investigation, significant improvement in the disease conditions was reported in 10 patients with rheumatoid arthritis of knee joints treated with 333 ± 46 MBq doses of 177 Lu‐HA. The studies reveal that while 177 Lu labeled HA particles holds considerable promise as a cost‐effective agent for RSV, the adopted strategy of using HA kits could be a potential step toward wider clinical utilization of radiolanthanide‐labeled HA particles. Copyright © 2014 John Wiley & Sons, Ltd.