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 DOTA-peptide of Formula (I)
or a salt thereof,
an antioxidant, and
a bulking agent, wherein the bulking agent is arginine, and
wherein the weight ratio of the arginine over the DOTA-peptide is of from 15:1 to 45:1.
2. The composition of claim 1 , further comprising:
a buffering agent, and
a surfactant.
3. The composition of claim 1 , wherein the weight ratio of the antioxidant over the DOTA-peptide is at least 20:1.
4. The composition of claim 1 , wherein:
the antioxidant is ascorbic acid or a salt thereof, and
the composition further comprises a surfactant, 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 DOTA-peptide is in a salt form and is present in the range of 0.10% to 3.00% by weight relative to the total weight of the composition.
7. The composition of claim 5 , wherein the antioxidant is ascorbic acid and is present in the range of 40% to 70% by weight relative to the total weight of the composition.
8. The composition of claim 5 , wherein arginine is present in the range of 25% to 55% by weight relative to the total weight of the composition.
9. The composition of claim 5 , further comprising a surfactant, wherein the surfactant is polysorbate 80 and is present in the range of 0.01% to 0.10% by weight relative to the total weight of the composition.
10. The composition of claim 5 , comprising:
DOTA-peptide acetate salt in the range of 0.10% to 3.00% by weight;
ascorbic acid in the range of 40% to 70% by weight;
arginine in the range of 25% to 55% by weight; and
a polysorbate in the range of 0.01% to 0.10% by weight;
wherein the DOTA-peptide acetate salt, ascorbic acid, arginine, and the polysorbate, taken together, represent at least 98% of the total weight of the composition.
11. The composition of claim 1 , wherein the composition is in a liquid aqueous form.
12. The composition of claim 11 , wherein the composition comprises:
a polysorbate and water for injection,
and wherein the antioxidant comprises ascorbic acid or a salt thereof,
and the DOTA-peptide is in a salt form.
13. The composition of claim 11 , wherein the DOTA-peptide is in a salt form and is present at a concentration of 0.1 to 2.0 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:
a polysorbate;
DTPA; and water for injection,
and wherein the antioxidant comprises ascorbic acid or a salt thereof,
and the DOTA-peptide is 177 Lu 3+ radiolabeled.
16. A kit comprising a suitable container containing the composition of claim 1 .
17. The kit of claim 16 comprising:
a first vial containing the composition, wherein the composition is in a lyophilized form; and
a second vial containing a sterile stabilizing solution comprising an antioxidant.
18. The kit of claim 17 , wherein the sterile stabilizing solution comprises water for injection, sodium ascorbate, DTPA and polysorbate 80.
19. A method for treating SSTR2 receptor positive tumors comprising administering to a mammal in need of such treatment an efficient quantity of the composition of claim 14 .
20. The method of claim 19 , wherein the tumor is selected from: neuroendocrine tumors (NETs) and tumors of prostate, breast, lung or lymphoma cancer.
21. The method of claim 19 , wherein the tumor is a gastroenteropancreatic neuroendocrine tumor (GEP NET).