Drug intelligence / Profile preview

technetium Tc-99m sestamibi

Development stage
Approved
Lead developer
Lantheus
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Technetium Tc-99m sestamibi is a lipophilic cationic radiopharmaceutical used as a diagnostic imaging agent in single-photon emission computed tomography (SPECT). It consists of the radionuclide technetium-99m coordinated to six sestamibi (methoxyisobutylisonitrile) ligands. Upon intravenous administration, the tracer distributes in the myocardium proportionally to blood flow and is sequestered within cells, particularly those with high mitochondrial density, via passive diffusion across plasma and mitochondrial membranes. It is primarily indicated for myocardial perfusion imaging to detect coronary artery disease and myocardial infarction. Additionally, it is used for the localization of parathyroid adenomas, breast cancer imaging (scintimammography), and the evaluation of renal masses. The specific mention of Central Hospital, Nancy, France, relates to its use in the D-SPECT BIS clinical trial evaluating optimized imaging protocols.

Brand names
CardioliteMiraluma
Other names
technetium (99mTc) sestamibiMIBI99mTc-methoxy isobutyl isonitrile
02

Targets

ABCC1 (MRP1)ABCB1 (P-glycoprotein)

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