Drug intelligence / Profile preview

technetium (99mTc) exametazime (GE HealthCare)

Development stage
Unknown
Lead developer
General Electric
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

Technetium (99mTc) exametazime (commonly known as technetium-99m-hexamethylpropyleneamine oxime or 99mTc-HMPAO) is a lipophilic radiopharmaceutical diagnostic agent used in nuclear medicine. It consists of the chelating agent exametazime (HMPAO) complexed with the radioactive isotope technetium-99m. Due to its lipophilic nature, the primary complex of technetium (99mTc) exametazime crosses the blood-brain barrier and is rapidly taken up by brain tissue, where it is converted into a hydrophilic secondary complex that is trapped intracellularly. This retention is proportional to regional cerebral blood flow, making it a valuable single-photon emission computed tomography (SPECT) imaging agent for detecting altered regional cerebral perfusion in stroke, dementia (such as Alzheimer's disease and frontotemporal dementia), and brain death. Additionally, it is used for the ex vivo radiolabeling of autologous leukocytes (white blood cells) to localize intra-abdominal infections and inflammatory bowel disease.

Brand names
CeretecDrax ExametazimeMedi-Exametazim
Other names
99mTc-HMPAO99mTc-exametazimeexametazimehexamethylpropylene amine oximehexamethylpropyleneamine oximetechnetium Tc 99m exametazimetechnetium Tc-99m exametazimetechnetium-99m exametazimetechnetium99m exametazimetechnetium 99m exametazimetechnetium-99m-hexamethylpropyleneamine oximetechnetium99m-hexamethylpropyleneamine oximetechnetium 99m-hexamethylpropyleneamine oxime
02

Targets

GSH (Glutathione)

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