Gallium ⁶⁸Ga edotreotide Other names: Edotreotide gallium Ga-68

Chemical formula: C₆₅H₈₉GaN₁₄O₁₈S₂  Molecular mass: 1,486.55 g/mol 

Mechanism of action

Gallium ⁶⁸Ga edotreotide binds to somatostatin receptors, with highest affinity (Ki = 2.5 ± 0.5 nanomolar) for subtype 2 receptors (sstr2). Gallium ⁶⁸Ga edotreotide binds to cells that express somatostatin receptors including malignant neuroendocrine cells, which overexpress sstr2 receptors. Gallium ⁶⁸Ga edotreotide is a β+ emitting radionuclide with associated 511 keV annihilation photons that allow positron emission tomography (PET) imaging.

Pharmacodynamic properties

The relationship between gallium ⁶⁸Ga edotreotide plasma concentrations and successful imaging was not explored in clinical trials.

Pharmacokinetic properties

Distribution

Gallium ⁶⁸Ga edotreotide distributes to all sstr2-expressing organs such as pituitary, thyroid, spleen, adrenals, kidney, pancreas, prostate, liver, and salivary glands. Uptake in the lung and lymph nodes are lower as compared to other sstr-2 expressing organs.

Elimination

Radiotracer elimination is exclusively via urine. Approximately 16% of the injected dose is excreted in urine in the first two to four hours post-injection.

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