FORMULATIONS OF ANTI-INTERLEUKIN 1 RECEPTOR 1 ANTIBODIES
The present invention provides, among other things, stable formulations comprising an anti-Interleukin 1 Receptor 1 (IL1R1) antibody at a concentration of greater than 80 mg/ml with a pH ranging from 4.4-5.7, wherein the amount of HMW species in the formulation increases less than 2% upon storage at 25° C. for at least 4 weeks.
1 . A stable formulation comprising an anti-interleukin-1 receptor 1 (IL1R1) antibody,
wherein the formulation comprises less than 130 mM arginine and a pH of 4.4-6.5,
wherein the anti-IL1R1 antibody comprises a HCDR1 of SEQ ID NO: 5 (FHWIA), a HCDR2 or SEQ ID NO: 6 (IIHPGASDTRYSPSFQG), a HCDR3 of SEQ ID NO: 7 (QRELDYFDY), a LCDR1 of SEQ ID NO: 8 (RASQSIGSSLH), a LCDR2 of SEQ ID NO: 9 (YASQSFS), and a LCDR3 of SEQ ID NO: 10 (HQSSSLPLT), and
wherein the anti-IL1R1 antibody is present at a concentration of greater than 80 mg/ml.
2 - 3 . (canceled)
4 . The stable formulation of claim 1 , wherein the formulation comprises a buffer.
5 - 10 . (canceled)
11 . The stable formulation of claim 1 , wherein the pH is 4.4-5.7.
12 - 21 . (canceled)
22 . The stable formulation of claim 1 , wherein the formulation comprises a sugar.
23 - 25 . (canceled)
26 . The stable formulation of claim 1 , wherein the formulation comprises a surfactant.
27 - 28 . (canceled)
29 . The stable formulation of claim 1 , wherein the formulation comprises salt.
30 - 32 . (canceled)
33 . The stable formulation of claim 1 , wherein the formulation comprises an amino acid.
34 - 37 . (canceled)
38 . The stable formulation of claim 1 , wherein the formulation comprises 20-60 mM acetate, a basic amino acid, and pH of 4.4-5.7.
39 - 43 . (canceled)
44 . The stable formulation of claim 1 , wherein the formulation comprises 20-60 mM acetate a sugar and a pH of 4.4-5.7.
45 - 53 . (canceled)
54 . The stable formulation of claim 1 , wherein the formulation comprises 10-50 mM histidine, an amino acid, and a pH of 5.5-6.5.
55 - 61 . (canceled)
62 . The stable formulation of claim 1 , wherein the formulation comprises 10-50 mM histidine, a sugar, and a pH of 5.5-6.5.
63 - 70 . (canceled)
71 . The stable formulation of claim 1 , wherein the formulation comprises 25-75 mM succinate, a basic amino acid, and a pH of 5.0-6.0.
72 . The stable formulation of claim 1 , wherein the formulation comprises 25-75 mM succinate, a salt, and a pH of 5.0-6.0.
73 - 79 . (canceled)
80 . The stable formulation of claim 1 , wherein the formulation comprises 20-60 mM succinate, a sugar, and a pH of 5.0-6.0.
81 - 97 . (canceled)
98 . The stable formulation of claim 1 , wherein the formulation comprises 135 mg/ml-165 mg/ml the anti-IL1R1 antibody.
99 - 102 . (canceled)
103 . A stable formulation comprising an anti-interleukin-1 receptor 1 (IL1R1) antibody, wherein the formulation comprises:
(i) 150 mg/mL anti-IL1R1 antibody,
(ii) 25 mM sodium acetate,
(iii) a pH of 4.5-5.7,
(iv) 7% w/v sucrose, and
(v) 0.02% w/v polysorbate 20, and
wherein the anti-IL1R1 antibody comprises a HCDR1 of SEQ ID NO: 5 (FHWIA), a HCDR2 or SEQ ID NO: 6 (IIHPGASDTRYSPSFQG), a HCDR3 of SEQ ID NO: 7 (QRELDYFDY), a LCDR1 of SEQ ID NO: 8 (RASQSIGSSLH), a LCDR2 of SEQ ID NO: 9 (YASQSFS), and a LCDR3 of SEQ ID NO: 10 (HQSSSLPLT).
104 - 108 . (canceled)
109 . A stable formulation comprising an anti-interleukin-1 receptor 1 (IL1R1) antibody, wherein the formulation comprises:
(i) 150 mg/mL anti-IL1R1 antibody,
(ii) 25 mM sodium acetate,
(iii) a pH of 4.4-5.4,
(iv) 25.9 mg/ml proline, and
(v) 0.02% w/v polysorbate 20, and
wherein the anti-IL1R1 antibody comprises a HCDR1 of SEQ ID NO: 5 (FHWIA), a HCDR2 of SEQ ID NO: 6 (IIHPGASDTRYSPSFQG), a HCDR3 of SEQ ID NO: 7 (QRELDYFDY), a LCDR1 of SEQ ID NO: 8 (RASQSIGSSLH), a LCDR2 of SEQ ID NO: 9 (YASQSFS), and a LCDR3 of SEQ ID NO: 10 (HQSSSLPLT).
110 - 114 . (canceled)
115 . The stable formulation of claim 1 , wherein the formulation comprises:
(i) 150 mg/mL anti-IL1R1 antibody,
(ii) 25 mM sodium acetate,
(iii) a pH 5.0,
(iv) 66.5 mM arginine, and
(v) 3.5% w/v sucrose, and
(vi) 0.02% w/v polysorbate 20.
116 . The stable formulation of claim 1 , wherein the anti-IL1R1 antibody comprises a variable heavy chain (VH) of SEQ ID NO: 3 and a variable light chain (VL) of SEQ ID NO: 4.
117 . (canceled)
118 . The stable formulation of claim 1 , wherein the anti-IL1R1 antibody comprises a heavy chain of SEQ ID NO: 1 and a light chain of SEQ ID NO: 2.
119 - 134 . (canceled)