Antev Limited

Aptys Pharmaceuticals Sas

Francois Boutignon

Guy Poland

Finn Larsen

Claudie Masson-Sinteff

The present invention relates to a reconstitutable teverelix-TFA composition having a predefined molar ratio of teverelix to trifluoroacetate which is below the molar ratio required for microcrystal formation. Said composition remains stable during storage e.g., at a temperature around 2-8° C. Upon reconstitution a fixed amount of trifluoroacetate can be added to said composition thereby effectively and simply achieving an exact and desired molar ratio in order to obtain a fluid, milky microcrystalline aqueous teverelix-TFA suspension.

Reconstitutable teverelix-TFA composition

Provided is a teverelix-TFA composition having a molar ratio of teverelix to trifluoroacetate composition of at least 1:2.2. Such a molar ratio will prevent undesirable gel-formation and provide a homogenous suspension, whereby a unique bioavailablity of teverelix is obtained.

Teverelix-TFA composition

The present invention relates to a lyophilization process for preparing a teverelix-TFA lyophilizate, said process comprises the following steps: a) providing a lyophilization suspension by mixing teverelix and trifluoroacetate at a molar ratio sufficient for providing a microcrystalline teverelix-TFA suspension without formation of a gel, and b) lyophilizating the lyophilization suspension, thereby providing a teverelix-TFA lyophilizate. The process provides the possibility of obtaining a 'pure' teverelix-TFA lyophilizate i.e. without any undesirable residues in the composition.

Lyophilization process and a teverelix-TFA lyophilizate obtained thereby

The present invention relates to a reconstitutable teverelix-TFA composition having a predefined molar ratio of teverelix to trifluoroacetate which is below the molar ratio required for microcrystal formation. Said composition remains stable during storage e.g. at a temperature around 2-8&#xb0; C. Upon reconstitution a fixed amount of trifluoroacetate can be added to said composition thereby effectively and simply achieving an exact and desired molar ratio in order to obtain a fluid, milky microcrystalline aqueous teverelix-TFA suspension.

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.

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Clermont-Ferrand, France

Francois Boutignon