10.1002/jlcr.1698
The study investigates the development of a new radiopharmaceutical for cancer imaging and therapy. The primary chemical involved is melphalan, a nitrogen mustard chemotherapeutic agent used for treating multiple myeloma. It is labeled with iodine-125 (125I) to create a radioligand, 125I-melphalan, which can be used for both diagnostic imaging and therapeutic applications. Chloramine-T (N-chloro-p-toluene sulfonamide sodium salt) serves as an oxidizing agent in the labeling process, facilitating the attachment of 125I to melphalan. The study optimizes the labeling conditions, achieving a high radiochemical yield of 96.8% under specific conditions: 200 mg of melphalan, 150 mg of chloramine-T, and 150 mL of phosphate buffer at pH 7, heated at 70°C for 15 minutes. The biodistribution studies in non-tumor bearing and tumor-bearing mice reveal that 125I-melphalan has a high affinity for tumor cells, localizes significantly in the tumor site, and is rapidly cleared from most organs, indicating its potential as a specific imaging and therapeutic agent for cancer.