Stabilized formulations containing anti-interleukin-6 receptor (IL-6R) antibodies
First Claim
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1. 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.
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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.
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17 Claims
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1. 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
- (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;
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16. 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.
- (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;
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17. 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.
- (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;
Specification