Flotufolastat ¹⁸F Other names: Flotufolastat F-18

Chemical formula: C₆₃H₉₉FN₁₂O₂₅Si  Molecular mass: 1,471.612 g/mol  PubChem compound: 166177191

Pharmacodynamic properties

Flotufolastat (18F) binds to PSMA (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells, and is internalized. Prostate cancer cells usually overexpress PSMA. Fluorine-18 is a β+ emitting radionuclide that can be detected using positron emission tomography.

The relationship between flotufolastat (18F) plasma concentrations and image interpretation has not been fully characterized.

Pharmacokinetic properties

Distribution

Following intravenous administration, flotufolastat (18F) distributes to liver (15.8% of administered activity), heart blood pool (7.4%), and kidneys (3.2%) and is cleared from the blood.

Elimination

Metabolism

Flotufolastat (18F) does not undergo metabolism up to 50 minutes post injection.

Excretion

Elimination is by urinary excretion. Approximately 7% of the administered activity was excreted in the urine in the first 2 hours post-injection with approximately 15% excreted by 4.5 hours post-injection.

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