IP Library › Patent Application 18432780

Patent Application

App. No. 18/432,780

Stabilized Formulations Containing Anti-Interleukin-4 Receptor (IL-4R) Antibodies

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Patent No.: US None
App. No.: 18/432,780

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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.

Claims (86)

1 - 29 . (canceled)

30 . A pharmaceutical formulation comprising:

(i) an antibody or antigen-binding fragment thereof that specifically binds to human interleukin-4 receptor alpha (hIL-4Rα), wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 15 mg/ml to about 200 mg/ml, and wherein the antibody or antigen-binding fragment thereof comprises: (a) a heavy chain variable region (HCVR) comprising heavy chain complementarity determining regions 1, 2, and 3 (HCDR1, HCDR2, and HCDR3) that comprise the amino acid sequences of SEQ ID NO:2, SEQ ID NO:3, and SEQ ID NO:4, respectively; and (b) a light chain variable region (LCVR) comprising light chain complementarity determining regions 1, 2, and 3 (LCDR1, LCDR2, and LCDR3) that comprise the amino acid sequences of SEQ ID NO:6, SEQ ID NO:7, and SEQ ID NO:8, respectively;

(ii) one or more buffers that can buffer from pH 5.6 to pH 6.2;

(iii) a polysorbate at a concentration of from 0.2% w/v to 2% w/v;

(iv) sucrose, mannitol, or trehalose at a concentration of about 2.5% w/v to about 10% w/v; and

(v) arginine at a concentration of about 25 mM to about 100 mM;

wherein the pharmaceutical formulation has a pH of from 5.6 to 6.2.

31 . The pharmaceutical formulation of claim 30 , wherein the buffer comprises acetate at a concentration of 2.5 mM to 22.5 mM.

32 . The pharmaceutical formulation of claim 31 , wherein the acetate is present at a concentration of 10 mM to 15 mM.

33 . The pharmaceutical formulation of claim 30 , wherein the buffer comprises histidine at a concentration of about 10 mM to about 30 mM.

34 . The pharmaceutical formulation of claim 33 , wherein the histidine is present at a concentration of 15 mM to 25 mM.

35 . The pharmaceutical formulation of claim 30 , wherein the buffer comprises acetate and histidine.

36 . The pharmaceutical formulation of claim 35 , wherein the acetate is present at a concentration of 2.5 mM to 22.5 mM and the histidine is present at a concentration of about 10 mM to about 30 mM.

37 . The pharmaceutical formulation of claim 35 , wherein the acetate is present at a concentration of 10 mM to 15 mM and the histidine is present at a concentration of 15 mM to 25 mM.

38 . The pharmaceutical formulation of claim 30 , wherein the polysorbate is polysorbate 20 or polysorbate 80.

39 . The pharmaceutical formulation of claim 30 , wherein the polysorbate is present at a concentration of 0.2% w/v.

40 . The pharmaceutical formulation of claim 30 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of at least 100 mg/ml.

41 . The pharmaceutical formulation of claim 30 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 150 mg/ml.

42 . The pharmaceutical formulation of claim 30 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 175 mg/ml.

43 . The pharmaceutical formulation of claim 30 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 200 mg/ml.

44 . The pharmaceutical formulation of claim 30 , wherein the antibody or antigen-binding fragment thereof comprises an HCVR comprising SEQ ID NO:1 and an LCVR comprising SEQ ID NO:5.

45 . The pharmaceutical formulation of claim 30 , wherein the pharmaceutical formulation is contained in a glass vial, a syringe, a microinfusor, an autoinjector delivery device, or a pen delivery device.

46 . A syringe comprising a pharmaceutical formulation, wherein the pharmaceutical formulation comprises:

(ii) one or more buffers that can buffer from pH 5.6 to pH 6.2;

(iii) a polysorbate at a concentration of from 0.2% w/v to 2% w/v;

(iv) sucrose, mannitol, or trehalose at a concentration of about 2.5% w/v to about 10% w/v; and

(v) arginine at a concentration of about 25 mM to about 100 mM;

wherein the pharmaceutical formulation has a pH of from 5.6 to 6.2.

47 . The syringe of claim 46 , wherein the buffer comprises acetate at a concentration of 2.5 mM to 22.5 mM.

48 . The syringe of claim 47 , wherein the acetate is present at a concentration of 10 mM to 15 mM.

49 . The syringe of claim 46 , wherein the buffer comprises histidine at a concentration of about 10 mM to about 30 mM.

50 . The syringe of claim 49 , wherein the histidine is present at a concentration of 15 mM to 25 mM.

51 . The syringe of claim 46 , wherein the buffer comprises acetate and histidine.

52 . The syringe of claim 51 , wherein the acetate is present at a concentration of 2.5 mM to 22.5 mM and the histidine is present at a concentration of about 10 mM to about 30 mM.

53 . The syringe of claim 51 , wherein the acetate is present at a concentration of 10 mM to 15 mM and the histidine is present at a concentration of 15 mM to 25 mM.

54 . The syringe of claim 46 , wherein the polysorbate is polysorbate 20 or polysorbate 80.

55 . The syringe of claim 46 , wherein the polysorbate is present at a concentration of 0.2% w/v.

56 . The syringe of claim 46 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of at least 100 mg/ml.

57 . The syringe of claim 46 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 150 mg/ml.

58 . The syringe of claim 46 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 175 mg/ml.

59 . The syringe of claim 46 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 200 mg/ml.

60 . The syringe of claim 30 , wherein the antibody or antigen-binding fragment thereof comprises an HCVR comprising SEQ ID NO:1 and an LCVR comprising SEQ ID NO:5.

61 . An autoinjector delivery device comprising a pharmaceutical formulation, wherein the pharmaceutical formulation comprises:

(ii) one or more buffers that can buffer from pH 5.6 to pH 6.2;

(iii) a polysorbate at a concentration of from 0.2% w/v to 2% w/v;

(iv) sucrose, mannitol, or trehalose at a concentration of about 2.5% w/v to about 10% w/v; and

(v) arginine at a concentration of about 25 mM to about 100 mM;

wherein the pharmaceutical formulation has a pH of from 5.6 to 6.2.

62 . The autoinjector delivery device of claim 61 , wherein the buffer comprises acetate at a concentration of 2.5 mM to 22.5 mM.

63 . The autoinjector delivery device of claim 62 , wherein the acetate is present at a concentration of 10 mM to 15 mM.

64 . The autoinjector delivery device of claim 61 , wherein the buffer comprises histidine at a concentration of about 10 mM to about 30 mM.

65 . The autoinjector delivery device of claim 64 , wherein the histidine is present at a concentration of 15 mM to 25 mM.

66 . The autoinjector delivery device of claim 61 , wherein the buffer comprises acetate and histidine.

67 . The autoinjector delivery device of claim 66 , wherein the acetate is present at a concentration of 2.5 mM to 22.5 mM and the histidine is present at a concentration of about 10 mM to about 30 mM.

68 . The autoinjector delivery device of claim 66 , wherein the acetate is present at a concentration of 10 mM to 15 mM and the histidine is present at a concentration of 15 mM to 25 mM.

69 . The autoinjector delivery device of claim 61 , wherein the polysorbate is polysorbate 20 or polysorbate 80.

70 . The autoinjector delivery device of claim 61 , wherein the polysorbate is present at a concentration of 0.2% w/v.

71 . The autoinjector delivery device of claim 61 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of at least 100 mg/ml.

72 . The autoinjector delivery device of claim 61 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 150 mg/ml.

73 . The autoinjector delivery device of claim 61 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 175 mg/ml.

74 . The autoinjector delivery device of claim 61 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 200 mg/ml.

75 . The autoinjector delivery device of claim 61 , wherein the antibody or antigen-binding fragment thereof comprises an HCVR comprising SEQ ID NO:1 and an LCVR comprising SEQ ID NO:5.

76 . A pen delivery device comprising a pharmaceutical formulation, wherein the pharmaceutical formulation comprises:

(ii) one or more buffers that can buffer from pH 5.6 to pH 6.2;

(iii) a polysorbate at a concentration of from 0.2% w/v to 2% w/v;

(iv) sucrose, mannitol, or trehalose at a concentration of about 2.5% w/v to about 10% w/v; and

(v) arginine at a concentration of about 25 mM to about 100 mM;

wherein the pharmaceutical formulation has a pH of from 5.6 to 6.2.

77 . The pen delivery device of claim 76 , wherein the buffer comprises acetate at a concentration of 2.5 mM to 22.5 mM.

78 . The pen delivery device of claim 77 , wherein the acetate is present at a concentration of 10 mM to 15 mM.

79 . The pen delivery device of claim 76 , wherein the buffer comprises histidine at a concentration of about 10 mM to about 30 mM.

80 . The pen delivery device of claim 79 , wherein the histidine is present at a concentration of 15 mM to 25 mM.

81 . The pen delivery device of claim 76 , wherein the buffer comprises acetate and histidine.

82 . The pen delivery device of claim 81 , wherein the acetate is present at a concentration of 2.5 mM to 22.5 mM and the histidine is present at a concentration of about 10 mM to about 30 mM.

83 . The pen delivery device of claim 81 , wherein the acetate is present at a concentration of 10 mM to 15 mM and the histidine is present at a concentration of 15 mM to 25 mM.

84 . The pen delivery device of claim 76 , wherein the polysorbate is polysorbate 20 or polysorbate 80.

85 . The pen delivery device of claim 76 , wherein the polysorbate is present at a concentration of 0.2% w/v.

86 . The pen delivery device of claim 76 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of at least 100 mg/ml.

87 . The pen delivery device of claim 76 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 150 mg/ml.

88 . The pen delivery device of claim 76 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 175 mg/ml.

89 . The pen delivery device of claim 76 , wherein the antibody or antigen-binding fragment thereof is present at a concentration of about 200 mg/ml.

90 . The pen delivery device of claim 76 , wherein the antibody or antigen-binding fragment thereof comprises an HCVR comprising SEQ ID NO:1 and an LCVR comprising SEQ ID NO:5.

Assignments (1)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2024

From: DIX, DANIEL B.; TANG, XIAOLIN

To: REGENERON PHARMACEUTICALS, INC.

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