Last reviewed 2026-05-25 · How we verify

Tc99m sestamibi

Tc99m sestamibi is a Radiotracer / Diagnostic imaging agent Small molecule drug developed by M.D. Anderson Cancer Center. It is currently FDA-approved for Myocardial perfusion imaging for detection of coronary artery disease, Assessment of myocardial viability, Evaluation of left ventricular function.

Tc-99m sestamibi is a radiotracer that accumulates in mitochondria of viable cells, allowing visualization of myocardial perfusion and detection of ischemia via nuclear imaging.

Tc99m sestamibi is a radiopharmaceutical used in clinical trials to study various types of cancer, including cervical, ovarian, lung, breast, and renal cancer. It is also used in a pharmacodynamic study to investigate the function of P-glycoprotein, a protein involved in multidrug resistance in cancer cells.

At a glance

Mechanism of action

Tc-99m sestamibi is a lipophilic cationic complex that crosses cell membranes and localizes in mitochondria based on the negative membrane potential of viable cells. The radioisotope Tc-99m emits gamma radiation that is detected by gamma cameras, enabling single-photon emission computed tomography (SPECT) imaging. Differential uptake between ischemic and normally perfused myocardium allows assessment of coronary artery disease and myocardial viability.

Approved indications

• Myocardial perfusion imaging for detection of coronary artery disease
• Assessment of myocardial viability
• Evaluation of left ventricular function

Common side effects

• Radiation exposure
• Allergic reaction (rare)

Key clinical trials

• SPECT/CT for the Characterization of Renal Masses
• Tc99m Sestamibi Molecular Breast Imaging (NA)
• Molecular Breast Imaging and Digital Breast Tomosynthesis in Screening Patients With Dense Breast Tissue (NA)
• Comparative Performance of Molecular Breast Imaging (MBI) to Magnetic Resonance Imaging (MRI) of the Breast in Identifying and Excluding Breast Carcinoma in Women at High Risk for Breast Cancer (NA)
• DCE-MRI and MBI in Assessing Tumor Response to Chemotherapy in Patients With Triple Negative Breast Cancer (EARLY_PHASE1)
• Molecular Breast Imaging Guidance for Breast Biopsy for Patients With Breast Abnormalities (NA)
• 99mTc Sestamibi SPECT/CT vs 18F Fluorocholine PET/CT (PHASE2, PHASE3)
• F-18 PSMA for Localization of Parathyroid Adenoma

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Tc99m sestamibi CI brief — competitive landscape report
• Tc99m sestamibi updates RSS · CI watch RSS
• M.D. Anderson Cancer Center portfolio CI

Frequently asked questions about Tc99m sestamibi

Related

• Drug class: All Radiotracer / Diagnostic imaging agent drugs
• Target: All drugs targeting Mitochondrial membrane potential
• Manufacturer: M.D. Anderson Cancer Center — full pipeline
• Therapeutic area: All drugs in Cardiology / Nuclear Medicine
• Indication: Drugs for Myocardial perfusion imaging for detection of coronary artery disease
• Indication: Drugs for Assessment of myocardial viability
• Indication: Drugs for Evaluation of left ventricular function

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing