Rhomed Incorporated

S.p. Pharmaceuticals

Michael J Marek

Paul O Zamora

Buck A Rhodes

Garnet G Smith

Thomas R Kovalcik

The subject invention relates to the use of ascorbic acid and derivatives thereof in stabilizing radiolabeled proteins and peptides against oxidation loss of radiolabel and autoradiolysis. Ascorbic acid is added after radiolabeling, including any required incubation period, but prior to patient administration.

Post-labeling stabilization of radiolabeled proteins and peptides

Post labeling stabilization of radiolabeled proteins and peptides

The invention relates to radiotherapy with somatostatin-derived peptides labeled with medically useful metal ions. The invention in particular provides for methods and reagents for labeling somatostatin-derived peptides with perrhenate, in which a solution including somatostatin-derived peptide analogue containing at least one disulfide bond is provided, the solution is reacted with stannous ions and with a radioisotope, wherein the stannous ions are sufficient to substantially reduce the disulfide bonds of the peptide and the radioisotope, and the radiolabeled somatostatin-derived peptide analogue recovered. Also provided are methods for regional administration of radiolabeled somatostatin-derived peptides, methods for enhanced regional retention of radiolabeled somatostatin-derived peptides, methods for treatment of arthritis using radiolabeled somatostatin derived peptides, and methods for stabilizing radiolabeled somatostatin derived peptides.

Peptide radiopharmaceutical applications

A method of lyophilizing an oxazaphosphorin and a preparation produced thereby including dissolving an oxazaphosphorin in water, adding an amino acid to a molar ratio of between 1 to 10 amino acid to 1 oxazaphosphorin to produce a mixture and lyophilizing said mixture to remove said water, is disclosed.

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Albuquerque, NM, United States of America

Michael J Marek