Stabilized formulations containing anti-interleukin-4 receptor (IL-4R) antibodies
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsDaniel B. Dix, Xiaolin Tang
Life of this patent
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Abstract
The present invention provides pharmaceutical formulations comprising a human antibody that specifically binds to human interleukin-4 receptor (hIL-4R). The formulations may contain, in addition to an anti-hIL-4R antibody, at least one amino acid, at least one sugar, or at least one non-ionic surfactant. The pharmaceutical formulations of the present invention exhibit a substantial degree of antibody stability after storage for several months.
Claims25
A stable pharmaceutical formulation comprising:
- (i) a human antibody at a concentration of from 100 mg/ml to 200 mg/ml, wherein the antibody specifically binds to human interleukin-4 receptor alpha (hIL-4Rα) and comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO:1 and a light chain variable region comprising the amino acid sequence of SEQ ID NO:5;
- (ii) acetate at a concentration of from 10 mM to 15 mM;
- (iii) histidine at a concentration of from 15 mM to 25 mM;
- (iv) sucrose at a concentration of from 2.5% w/v to 10% w/v;
- (v) polysorbate at a concentration of from 0.1% w/v to 0.3% w/v;
- and
- (vi) arginine at a concentration of from 20 mM to 100 mM,
- wherein the formulation has a pH of from 5.6 to 6.2.
A stable pharmaceutical formulation comprising:
- (i) 150 mg/ml±50 mg/ml of a human antibody that specifically binds to hIL-4Rα, wherein said antibody comprises a heavy chain and light chain variable region (HCVR/LCVR) amino acid sequence pair of SEQ ID NOs:1/5;
- (ii) 12.5 mM±2 mM acetate;
- (iii) 20 mM±3 mM histidine;
- (iv) 5%±0.75% sucrose;
- (v) 0.2%±0.03% polysorbate 20;
- and
- (vi) 25 mM±3.75 mM arginine,
- at a pH of 5.9±0.5.
A stable pharmaceutical formulation comprising:
- (i) 175 mg/ml of a human antibody that specifically binds to hIL-4Rα, wherein said antibody comprises a heavy chain and light chain variable region (HCVR/LCVR) amino acid sequence pair of SEQ ID NOs:1/5;
- (ii) 12.5 mM±2 mM acetate;
- (iii) 20 mM±3 mM histidine;
- (iv) 5%±0.75% sucrose;
- (v) 0.2%±0.03% polysorbate 20;
- and
- (vi) 50 mM±3.75 mM arginine,
- at a pH of 5.9±0.5.
A stable pharmaceutical formulation comprising:
- (i) 175 mg/ml of a human antibody that specifically binds to hIL-4Rα, wherein said antibody comprises a heavy chain and light chain variable region (HCVR/LCVR) amino acid sequence pair of SEQ ID NOs:1/5;
- (ii) 12.5 mM±2 mM acetate;
- (iii) 20 mM±3 mM histidine;
- (iv) 5%±0.75% sucrose;
- (v) 0.2%±0.03% polysorbate 80;
- and
- (vi) 50 mM±3.75 mM arginine,
- at a pH of 5.9±0.5.
A stable pharmaceutical formulation comprising:
- (i) 150 mg/ml±50 mg/ml of a human antibody that specifically binds to hIL-4Rα, wherein said antibody comprises a heavy chain and light chain variable region (HCVR/LCVR) amino acid sequence pair of SEQ ID NOs:1/5;
- (ii) 12.5 mM±2 mM acetate;
- (iii) 20 mM±3 mM histidine;
- (iv) 5%±0.75% sucrose;
- (v) 0.2%±0.03% polysorbate 80;
- and
- (vi) 25 mM±3.75 mM arginine,
- at a pH of 5.9±0.5.
Dependencies are inferred from the claim text.