Enriched and stable radioligand therapy formulations and pharmaceutical compositions comprising same
OwnerJulie CUPIDO, Alex SUTTON +3inventors
InventorsJulie CUPIDO, Alex SUTTON, Henry MOK, Bernard LAMBERT, Wei ZHANG
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Abstract
The present disclosure relates to stable compositions comprising a radiolabeled compound, and related pharmaceutical compositions and methods of manufacture. Such compositions are useful in both the diagnostic imaging of and the treatment of diseases (e.g., cancer).
Claims55
A method of making a stabilized composition of a radiolabeled compound, comprising:
- a. eluting a mixture comprising the radiolabeled compound and a corresponding unlabeled compound through a chromatography column, thereby separating the radiolabeled compound from the unlabeled compound;
- b. collecting an eluate containing the separated radiolabeled compound in a vessel containing a stabilizing solution to afford the stabilized composition of the radiolabeled compound.
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A pharmaceutical composition comprising a radiolabeled compound and a stabilizing solution,
- wherein the stabilizing solution comprises ascorbic acid or a pharmaceutically acceptable salt thereof and a polysorbate, and one or more components selected from the group consisting of ethanol, L-methionine, selenomethionine, histidine, melatonin, acetic acid or a pharmaceutically acceptable salt thereof, benzyl alcohol, p-aminobenzoic acid or a pharmaceutically acceptable salt thereof, cysteamine, 5-amino-2-hydroxybenzoic acid or a pharmaceutically acceptable salt thereof, nicotinic acid or a pharmaceutically acceptable salt thereof, nicotinamide, cysteine, monothioglycerol, sodium bisulfite, sodium metabisulfite, gentisic acid, and inositol, and
- wherein the mass ratio of ascorbic acid or a pharmaceutically acceptable salt thereof to polysorbate in the pharmaceutical composition is from 50:1 to 150:1.
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A pharmaceutical composition comprising:
- a radiolabeled compound comprising (i) a peptide comprising a chelator, and (ii) a radioisotope, wherein radioisotope is chelated with the chelator;
- ascorbic acid or a pharmaceutically acceptable salt thereof;
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- a polysorbate;
- wherein the pharmaceutical composition has a radiochemical purity (RCP) of >90% after 72 hours at 2-8° C.
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Dependencies are inferred from the claim text.