Teverelix-TFA composition
A teverelix-TFA composition having a molar ratio of teverelix to trifluoroacetate composition of at least 1:2.2 is provided. Such a molar ratio will prevent undesirable gel-formation and provide a homogenous suspension, whereby a unique bioavailablity of teverelix is obtained.
1. A homogeneous teverelix-TFA composition having a molar ratio of teverelix (Ac-D-Nal-D-pClPhe-D-Pal-Ser-Tyr-D-Hci-Leu-Lys(iPr)-Pro-D-Ala-NH 2 ) to trifluoroacetate of at least 1:2.2 and at or below 1:2.8, such that for each mole of teverelix in the composition, the composition comprises at least 2.2 mol of trifluoroacetate and at or below 2.8 mol of trifluoroacetate, wherein the amount of insoluble microcrystalline teverelix in said composition is at least 80 weight % based on the weight of the homogeneous teverelix-TFA composition, and wherein increase in degradation products caused by deamidation is below 6% in the composition of teverelix-TFA of 10 mg/ml after storage at 40° C. for 1 month.
2. The teverelix-TFA composition according to claim 1 for use as a medicament.
3. A pharmaceutical formulation comprising the teverelix-TFA composition according to claim 1 .
4. A package filled with the teverelix-TFA composition according to claim 1 .
5. The package according to claim 4 , comprising a unit dosage of the teverelix-TFA composition.
6. The package according to claim 4 , wherein the package is a syringe suitable for providing a subcutaneous and/or intramuscularly injection.
7. A pharmaceutical formulation comprising a teverelix-TFA composition having a molar ratio of teverelix (Ac-D-Nal-D-pClPhe-D-Pal-Ser-Tyr-D-Hci-Leu-Lys(iPr)-Pro-D-Ala-NH2) to trifluoroacetate is between 1:2.2 and 1:2.8, such that for each mole of teverelix in the composition, the composition comprises between 2.2 and 2.8 mol of trifluoroacetate, wherein the pharmaceutical formulation is in the form of a microcrystalline homogenous aqueous suspension, and wherein the increase in degradation products caused by deamidation is below 6% in the composition of teverelix-TFA of 10 mg/ml after storage at 40° C. for 1 month.