Stabilized formulations containing anti-interleukin-6 receptor (IL-6R) antibodies
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsDaniel B. Dix, Kenneth S. Graham, Douglas Kamen, Scott M. Walsh
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-6 receptor (hIL-6R). The formulations may contain, in addition to an anti-hIL-6R antibody, at least one amino acid, at least one sugar, and/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.
Claims17
A stable pharmaceutical formulation comprising:
- (i) 5 mg/mL to 200 mg/mL of a human antibody that specifically binds to human interleukin-6 receptor (hIL-6R), wherein the antibody comprises a heavy chain variable region having the amino acid sequence of SEQ ID NO:18 and a light chain variable region having the amino acid sequence of SEQ ID NO:26;
- (ii) histidine at a concentration of from 25 mM to 100 mM;
- (iii) arginine at a concentration of from 25 mM to 50 mM;
- (iv) sucrose in an amount of from 3% to 10% w/v;
- and (v) polysorbate 20 in an amount of from 0.1% to 0.2%, wherein the formulation has a pH of about 5.8, about 6.0, or about 6.2, and at least 90% of the native form of the antibody is recovered after 1 month of storage at 45° C., as determined by size exclusion chromatography.
A stable pharmaceutical formulation comprising:
- (i) about 175 mg/mL of a human antibody that specifically binds to human interleukin-6 receptor (hIL-6R), wherein said antibody comprises a heavy chain and light chain variable region (HCVR/LCVR) amino acid sequence pair of SEQ ID NOs:18/26;
- (ii) about 25 mM histidine;
- (iii) about 5% sucrose;
- (iv) about 0.2% polysorbate 20;
- and (v) about 50 mM arginine, wherein the formulation has a pH of about 6.0 and at least 90% of the native form of the antibody is recovered after 1 month of storage at 45° C., as determined by size exclusion chromatography.
A stable pharmaceutical formulation comprising:
- (i) 25 mg/mL to 200 mg/mL of a human antibody that specifically binds to human interleukin-6 receptor (hIL-6R), wherein the antibody comprises a heavy chain variable region having the amino acid sequence of SEQ ID NO:18 and a light chain variable region having the amino acid sequence of SEQ ID NO:26;
- (ii) about 25 mM histidine;
- (iii) about 25 mM or about 50 mM arginine;
- (iv) about 5% w/v sucrose;
- and (v) about 0.2% w/v polysorbate 20, wherein the formulation has a pH of about 6, and at least 90% of the native form of the antibody is recovered after 1 month of storage at 45° C., as determined by size exclusion chromatography.
Dependencies are inferred from the claim text.