Composition containing a somatostatin analogue for radiopharmaceutical use
The present invention relates to a somatostatin analogue composition for radiopharmaceutical use, in particular for diagnostic or therapeutic use. More specifically the somatostatin analogue is a receptor-selective somatostatin peptide antagonist.
1. A receptor-selective somatostatin peptide antagonist composition comprising:
a NODAGA-peptide of formula (I),
or a salt thereof;
an antioxidant selected from ascorbic acid or a salt thereof and methionine; and
a bulking agent, wherein the bulking agent is trehalose.
2. The composition of claim 1 , further comprising a surfactant.
3. The composition of claim 1 , wherein the weight ratio of the antioxidant over the NODAGA-peptide is at least 50.
4. The composition of claim 2 , wherein the surfactant is a polysorbate.
5. The composition of claim 1 , wherein the composition is in a lyophilized form.
6. The composition of claim 5 , wherein;
the NODAGA-peptide is in a salt form and is present in the range of 0.02% to 0.20% by weight relative to the total weight of the composition;
the antioxidant is present in the range of 4% to 15% by weight relative to the total weight of the composition;
the bulking agent is present in the range of 80% to 96% by weight relative to the total weight of the composition; and/or
the composition further comprises a surfactant, wherein the surfactant is present in the range of 0.01% to 0.36% by weight relative to the total weight of the composition.
7. The composition of claim 6 , wherein the antioxidant is ascorbic acid.
8. The composition of claim 6 , wherein the surfactant is a polysorbate.
9. The composition of claim 5 , comprising:
NODAGA-peptide acetate salt in the range of 0.02% to 0.20% by weight;
ascorbic acid in the range of 4% to 15% by weight;
trehalose in the range of 80% to 96% by weight; and
a surfactant, wherein the surfactant is a polysorbate in the range of 0.10% to 0.36% by weight;
wherein the NODAGA-peptide acetate salt, ascorbic acid, trehalose and polysorbate, taken together, represent 98% of the total weight of the lyophilized composition.
10. The composition of claim 5 , further comprising a buffering agent.
11. The composition of claim 1 , wherein the composition is in a liquid aqueous form.
12. The composition of claim 11 , comprising:
ascorbic acid;
a polysorbate; and
a buffer solution; and
wherein the NODAGA-peptide is in a salt form.
13. The composition of claim 11 , wherein the NODAGA-peptide is in a salt form and is present at a concentration of 0.02 to 0.12 mg/mL.
14. The composition of claim 1 , wherein the composition is a radiolabeled composition.
15. The composition of claim 14 , wherein the composition comprises:
ascorbic acid;
a polysorbate; and
a buffer solution; and
the NODAGA-peptide is 68 Ga 3+ radiolabeled.
16. A kit comprising a first vial containing the composition of claim 1 , wherein the composition is in a lyophilized form.
17. The kit of claim 16 , further comprising a second vial containing a sterile reconstitution solution comprising a buffer solution.
18. A method for imaging a tumor in a mammal, comprising administering the radiolabeled composition of claim 14 to the mammal, optionally wherein the mammal is a human.
19. The method of claim 18 , wherein the tumor is a SSTR2 receptor positive tumor and the method further comprises detecting the radiolabeled composition by exposing the mammal to external imaging, by radioactive scanning or by magnetic resonance imaging.