Drug intelligence / Profile preview

Iofetamine I-123

Development stage
Discontinued
Lead developer
Medi-Physics
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Iofetamine I-123 is a radiopharmaceutical and amphetamine analog used primarily for cerebral blood perfusion imaging with single-photon emission computed tomography (SPECT). Labeled with the radioactive isotope iodine‑123, it is rapidly taken up by the lungs and redistributed mainly to the brain and liver. Its high lipophilicity allows it to cross the blood–brain barrier efficiently. The drug acts by inhibiting the reuptake of serotonin and norepinephrine, as well as inducing their release along with dopamine, similar to other amphetamines. It was approved in the United States under brand names such as Spectamine for diagnostic use in evaluating non-lacunar stroke, complex partial seizures, and early diagnosis of Alzheimer's disease. The mechanism of localization in brain tissue is believed to be due to nonspecific receptor binding rather than a specific molecular target[1][4][5][6].

Brand names
SpectaminePerfusamine
Other names
iofetamine (123I)iofetamine, I-123iofetamine I 123
02

Targets

SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)

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