Patent application EP19177024A (EP), filed 2019-05-28
Publication number: EP3744319A1
Title: A STABLE LYOPHILIZED FORMULATION FOR HYBRID FC FUSED G-CSF
Abstract: [0001]    The present formulation comprises a stable lyophilized formulation, suitable for administration via a subcutaneous (SC) route, comprising Fc fused to Granulocyte Colony Stimulating Factor (G-CSF) molecules via peptide bond, stabilizer, surfactant and buffer, at pH value of the preparation that is between 3.8 and 5.2.
IPC codes: A61K  38/    19            A I
A61K  47/    10            A I
A61K  47/    26            A I
A61K   9/    19            A I
A61K  39/    00            A I
Claims: number: 1
text: A stable pharmaceutical lyophilized formulation comprising at least 10 mg/mL hybrid Fc fused G-CSF; at least one stabilizer; at least one surfactant; and a buffer system; wherein the pH value of the preparation is between 3.8 and 5.2 and the stabilizer is the combination of trehalose and sorbitol.
number: 2
text: The lyophilized formulation of claim 1, wherein the pH value of the preparation is between 4.0 and 5.0.
number: 3
text: The lyophilized formulation of claim 1, wherein concentration of trehalose dihydrate of the preparation is between 5.0% (w/v) and 7.0% (w/v) based on the total volume of the formulation.
number: 4
text: The lyophilized formulation of claim 1, wherein concentration of sorbitol of the preparation is between 1.5% (w/v) and 2.5% (w/v) based on the total volume of the formulation.
number: 5
text: The lyophilized formulation of claim 1, wherein weight ratio of trehalose dihydrate to sorbitol is between 2:1 and 4:1.
number: 6
text: The lyophilized formulation of claim 1, wherein concentration of total stabilizer is between 6.5% (w/v) and 9.5% (w/v).
number: 7
text: The lyophilized formulation of claim 1, wherein the surfactant is poloxamer-based non-ionic surfactant.
number: 8
text: The lyophilized formulation of claim 7, wherein poloxamer-based non-ionic surfactant is used at a concentration between 0.08 % (w/v) and 0.15 % (w/v) based on the total volume of the formulation.
number: 9
text: The lyophilized formulation of claim 1, wherein the buffer is selected from the group consisting of citrate, citro-phosphate, alanine, glycine, arginine, acetate, succinate, histidine or a combination thereof.
number: 10
text: The lyophilized formulation of claim 9, wherein acetate buffer is used as the buffer system.
number: 11
text: The lyophilized formulation of claim 1, wherein the concentration of hybrid Fc fused G-CSF is between 10 mg/mL and 80 mg/mL.
number: 12
text: The lyophilized formulation of claim 11, wherein the concentration of hybrid Fc fused G-CSF is between 20 mg/mL and 40 mg/mL.
number: 13
text: A stable pharmaceutical 20 mg/mL hybrid Fc fused G-CSF lyophilized formulation comprising ;
number: 14
text: The lyophilized formulation of claim 13, wherein the pH value of the preparation is between 4.0 and 5.0.
number: 15
text: The lyophilized formulation of claim 13, wherein weight ratio of trehalose dihydrate to sorbitol is between 2:1 and 4:1.
Office action: search_report, dated 2020-12-02
Rejection reasons: inventive_step_epc_56
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Final disposition: pending (2020-12-02)