Stable, concentrated radionuclide complex solutions
AssigneeAdvanced Accelerator Applications SA
InventorsDonato Barbato, Clementina Brambati, Daniela Chicco, Francesco de Palo, Lorenza Fugazza, Maurizio Mariani, Giovanni Tesoriere
Life of this patent
Estimating the term…
Abstract
The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.
Claims31
1-21. (canceled)
A pharmaceutical aqueous solution comprising:
- (a) a complex comprising
- (ai) the radionuclide 177Lu present in a concentration that provides a volumetric radioactivity of 250 to 500 MBq/mL, and
- (aii) a somatostatin receptor binding peptide linked to the chelating agent DOTA;
- and
- (b) at least one stabilizer(s) against radiolytic degradation selected from gentisic acid or a salt thereof, ascorbic acid or a salt thereof, methionine, histidine, melatonine, and Se-methionine present in a total concentration of 0.2 mg/mL to 15.0 mg/mL;
- and
- wherein the activity of the solution is 7.4 GBq±10%,
- and wherein the pharmaceutical aqueous solution comprises less than 5% ethanol.
A method of treating a tumor in a patient in need thereof, the method comprising administering to the patient 10 mL to 50 mL of a pharmaceutical aqueous solution comprising:
- (a) a complex comprising
- (ai) the radionuclide 177Lu present in a concentration that provides a volumetric radioactivity of 250 to 500 MBq/mL, and
- (aii) a somatostatin receptor binding peptide linked to the chelating agent DOTA;
- and
- (b) at least one stabilizer(s) against radiolytic degradation selected from gentisic acid or a salt thereof, ascorbic acid or a salt thereof, methionine, histidine, melatonine, and Se-methionine present in a total concentration of 0.2 mg/mL to 15.0 mg/mL,
- wherein the pharmaceutical aqueous solution comprises less than 5% ethanol.
Dependencies are inferred from the claim text.