US2019134196A1PendingUtilityA1

Etar antibody, and pharmaceutical compositions and use thereof

49
Assignee: GMAX BIOPHARM LLCPriority: May 31, 2016Filed: May 27, 2017Published: May 9, 2019
Est. expiryMay 31, 2036(~9.9 yrs left)· nominal 20-yr term from priority
C07K 2317/94A61P 9/12A61K 47/26C07K 16/2869A61K 47/183A61K 47/12A61K 47/10A61K 39/39591C07K 2317/24A61K 2039/505A61P 35/00A61K 47/22A61P 11/00A61K 39/395C07K 16/28A61K 47/20
49
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Claims

Abstract

Provided herein are a stable solution formulation of an ET A R antibody, and use thereof in treating, preventing, or alleviating one or more symptoms of pulmonary arterial hypertension or one or more symptoms of cancer of a reproductive organ.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A stable pharmaceutical solution formulation of an ET A R antibody, comprising an ET A R antibody and a buffer, wherein the formulation has a pH approximately ranging from 5 to 7. 
     
     
         2 . The formulation of  claim 1 , wherein the ET A R antibody comprises 1, 2, 3, 4, 5, or 6 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below:
 a. light chain CDR1 amino acid sequences: SEQ ID NO: 8, SEQ ID NO: 10, SEQ ID NO: 12, SEQ ID NO: 14, SEQ ID NO: 16, SEQ ID NO: 18, SEQ ID NO: 20, SEQ ID NO: 22, SEQ ID NO: 24, SEQ ID NO: 26, SEQ ID NO: 28, and SEQ ID NO: 30;   b. light chain CDR2 amino acid sequences: SEQ ID NO: 32, SEQ ID NO: 34, SEQ ID NO: 36, SEQ ID NO: 38, SEQ ID NO: 40, SEQ ID NO: 42, SEQ ID NO: 44, SEQ ID NO: 46, and SEQ ID NO: 48;   c. light chain CDR3 amino acid sequences: SEQ ID NO: 50, SEQ ID NO: 52, SEQ ID NO: 54, SEQ ID NO: 56, SEQ ID NO: 58, SEQ ID NO: 60, SEQ ID NO: 62, SEQ ID NO: 64, SEQ ID NO: 66, and SEQ ID NO: 68;   d. heavy chain CDR1 amino acid sequences: SEQ ID NO: 70, SEQ ID NO: 72, SEQ ID NO: 74, SEQ ID NO: 76, SEQ ID NO: 78, SEQ ID NO: 80, SEQ ID NO: 82, SEQ ID NO: 84, SEQ ID NO: 86, SEQ ID NO: 88, and SEQ ID NO: 90;   e. heavy chain CDR2 amino acid sequences: SEQ ID NO: 92, SEQ ID NO: 94, SEQ ID NO: 96, SEQ ID NO: 98, SEQ ID NO: 100, SEQ ID NO: 102, SEQ ID NO: 104, SEQ ID NO: 106, SEQ ID NO: 108, SEQ ID NO: 110, SEQ ID NO: 112, and SEQ ID NO: 114; and   f. heavy chain CDR3 amino acid sequences: SEQ ID NO: 116, SEQ ID NO: 118, SEQ ID NO: 120, SEQ ID NO: 122, SEQ ID NO: 124, SEQ ID NO: 126, SEQ ID NO: 128, SEQ ID NO: 130, SEQ ID NO: 132, SEQ ID NO: 134, and SEQ ID NO: 136.   
     
     
         3 . The formulation of  claim 1  or  2 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below:
 a. light chain CDR1 amino acid sequences: SEQ ID NO: 8, SEQ ID NO: 10, SEQ ID NO: 12, SEQ ID NO: 14, SEQ ID NO: 16, SEQ ID NO: 18, SEQ ID NO: 20, SEQ ID NO: 22, SEQ ID NO: 24, SEQ ID NO: 26, SEQ ID NO: 28, and SEQ ID NO: 30; and 
 b. heavy chain CDR1 amino acid sequences: SEQ ID NO: 70, SEQ ID NO: 72, SEQ ID NO: 74, SEQ ID NO: 76, SEQ ID NO: 78, SEQ ID NO: 80, SEQ ID NO: 82, SEQ ID NO: 84, SEQ ID NO: 86, SEQ ID NO: 88, and SEQ ID NO: 90. 
 
     
     
         4 . The formulation of any one of  claims 1  to  3 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below:
 a. light chain CDR2 amino acid sequences: SEQ ID NO: 32, SEQ ID NO: 34, SEQ ID NO: 36, SEQ ID NO: 38, SEQ ID NO: 40, SEQ ID NO: 42, SEQ ID NO: 44, SEQ ID NO: 46, and SEQ ID NO: 48; and 
 b. heavy chain CDR2 amino acid sequences: SEQ ID NO: 92, SEQ ID NO: 94, SEQ ID NO: 96, SEQ ID NO: 98, SEQ ID NO: 100, SEQ ID NO: 102, SEQ ID NO: 104, SEQ ID NO: 106, SEQ ID NO: 108, SEQ ID NO: 110, SEQ ID NO: 112, and SEQ ID NO: 114. 
 
     
     
         5 . The formulation of any one of  claims 1  to  4 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below:
 a. light chain CDR3 amino acid sequences: SEQ ID NO: 50, SEQ ID NO: 52, SEQ ID NO: 54, SEQ ID NO: 56, SEQ ID NO: 58, SEQ ID NO: 60, SEQ ID NO: 62, SEQ ID NO: 64, SEQ ID NO: 66, and SEQ ID NO: 68; and 
 b. heavy chain CDR3 amino acid sequences: SEQ ID NO: 116, SEQ ID NO: 118, SEQ ID NO: 120, SEQ ID NO: 122, SEQ ID NO: 124, SEQ ID NO: 126, SEQ ID NO: 128, SEQ ID NO: 130, SEQ ID NO: 132, SEQ ID NO: 134, and SEQ ID NO: 136. 
 
     
     
         6 . The formulation of any one of  claims 1  to  5 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below: SEQ ID NO: 8, SEQ ID NO: 20, SEQ ID NO: 22, SEQ ID NO: 24, SEQ ID NO: 26, SEQ ID NO: 28, SEQ ID NO: 30, SEQ ID NO: 32, SEQ ID NO: 44, SEQ ID NO: 46, SEQ ID NO: 48, SEQ ID NO: 50, SEQ ID NO: 62, SEQ ID NO: 64, SEQ ID NO: 66, and SEQ ID NO: 68. 
     
     
         7 . The formulation of any one of  claims 1  to  6 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below: SEQ ID NO: 70, SEQ ID NO: 82, SEQ ID NO: 84, SEQ ID NO: 86, SEQ ID NO: 88, SEQ ID NO: 90, SEQ ID NO: 92, SEQ ID NO: 104, SEQ ID NO: 106, SEQ ID NO: 108, SEQ ID NO: 110, SEQ ID NO: 112, SEQ ID NO: 114, SEQ ID NO: 116, SEQ ID NO: 128, SEQ ID NO: 130, SEQ ID NO: 132, SEQ ID NO: 134, and SEQ ID NO: 136. 
     
     
         8 . The formulation of any one of  claims 1  to  7 , wherein the ET A R antibody comprises a combination of amino acid sequences of light chain and heavy chain CDR3 independently selected from the list below: SEQ ID NO: 50 and SEQ ID NO: 116, SEQ ID NO: 62 and SEQ ID NO: 128, SEQ ID NO: 62 and SEQ ID NO: 130, SEQ ID NO: 64 and SEQ ID NO: 132, SEQ ID NO: 66 and SEQ ID NO: 134, and SEQ ID NO: 68 and SEQ ID NO: 136. 
     
     
         9 . The formulation of any one of  claims 1  to  8 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below:
 a. amino acid sequences of light chain variable domains: SEQ ID NO: 138, SEQ ID NO: 140, SEQ ID NO: 142, SEQ ID NO: 144, SEQ ID NO: 146, SEQ ID NO: 148, SEQ ID NO: 150, SEQ ID NO: 152, SEQ ID NO: 154, SEQ ID NO: 156, SEQ ID NO: 158, SEQ ID NO: 160, SEQ ID NO: 162, and SEQ ID NO: 164; and 
 b. amino acid sequences of heavy chain variable domains: SEQ ID NO: 166, SEQ ID NO: 168, SEQ ID NO: 170, SEQ ID NO: 172, SEQ ID NO: 174, SEQ ID NO: 176, SEQ ID NO: 178, SEQ ID NO: 180, SEQ ID NO: 182, SEQ ID NO: 184, SEQ ID NO: 186, SEQ ID NO: 188, SEQ ID NO: 190, and SEQ ID NO: 192. 
 
     
     
         10 . The formulation of any one of  claims 1  to  9 , wherein a polynucleotide coding sequence of the ET A R antibody comprises 1 or 2 polynucleotide sequences, wherein each polynucleotide sequence is independently selected from the polynucleotide sequences listed below:
 a. The polynucleotide coding sequences of the light chain variable domains: SEQ ID NO: 137, SEQ ID NO: 139, SEQ ID NO: 141, SEQ ID NO: 143, SEQ ID NO: 145, SEQ ID NO: 147, SEQ ID NO: 149, SEQ ID NO: 151, SEQ ID NO: 153, SEQ ID NO: 155, SEQ ID NO: 157, SEQ ID NO: 159, SEQ ID NO: 161, and SEQ ID NO: 163; and 
 b. The polynucleotide coding sequences of the heavy chain variable domains: SEQ ID NO: 165, SEQ ID NO: 167, SEQ ID NO: 169, SEQ ID NO: 171, SEQ ID NO: 173, SEQ ID NO: 175, SEQ ID NO: 177, SEQ ID NO: 179, SEQ ID NO: 181, SEQ ID NO: 183, SEQ ID NO: 185, SEQ ID NO: 187, SEQ ID NO: 189, and SEQ ID NO: 191. 
 
     
     
         11 . The formulation of any one of  claims 1  to  10 , wherein the ET A R antibody comprises a combination of amino acid sequences independently selected from the list below: SEQ ID NO: 138 and SEQ ID NO: 166, SEQ ID NO: 140 and SEQ ID NO: 168, SEQ ID NO: 142 and SEQ ID NO: 170, SEQ ID NO: 144 and SEQ ID NO: 172, SEQ ID NO: 146 and SEQ ID NO: 174, SEQ ID NO: 148 and SEQ ID NO: 176, SEQ ID NO: 150 and SEQ ID NO: 178, SEQ ID NO: 152 and SEQ ID NO: 180, SEQ ID NO: 154 and SEQ ID NO: 182, SEQ ID NO: 156 and SEQ ID NO: 184, SEQ ID NO: 158 and SEQ ID NO: 186, SEQ ID NO: 160 and SEQ ID NO: 188, SEQ ID NO: 162 and SEQ ID NO: 190, and SEQ ID NO: 164 and SEQ ID NO: 192. 
     
     
         12 . The formulation of any one of  claims 1  to  11 , wherein the ET A R antibody comprises an amino acid sequence independently selected from the list below: SEQ ID NO: 138, SEQ ID NO: 150, SEQ ID NO: 152, SEQ ID NO: 154, SEQ ID NO: 156, SEQ ID NO: 158, SEQ ID NO: 160, SEQ ID NO: 162, and SEQ ID NO: 164. 
     
     
         13 . The formulation of any one of  claims 1  to  12 , wherein the ET A R antibody comprises an amino acid sequence independently selected from the list below: SEQ ID NO: 166, SEQ ID NO: 178, SEQ ID NO: 180, SEQ ID NO: 182, SEQ ID NO: 184, SEQ ID NO: 186, SEQ ID NO: 188, SEQ ID NO: 190, and SEQ ID NO: 192. 
     
     
         14 . The formulation of any one of  claims 1  to  13 , wherein the ET A R antibody comprises a combination of amino acid sequences of light chain and heavy chain variable domains independently selected from the list below: SEQ ID NO: 138 and SEQ ID NO: 166, SEQ ID NO: 150 and SEQ ID NO: 178, SEQ ID NO: 152 and SEQ ID NO: 180, SEQ ID NO: 154 and SEQ ID NO: 182, SEQ ID NO: 156 and SEQ ID NO: 184, SEQ ID NO: 158 and SEQ ID NO: 186, SEQ ID NO: 160 and SEQ ID NO: 188, SEQ ID NO: 162 and SEQ ID NO: 190, and SEQ ID NO: 164 and SEQ ID NO: 192. 
     
     
         15 . The formulation of any one of  claims 1  to  14 , wherein the ET A R antibody comprises amino acid sequence SEQ ID NO: 138 or SEQ ID NO: 166. 
     
     
         16 . The formulation of any one of  claims 1  to  15 , wherein the ET A R antibody comprises the combination of amino acid sequences SEQ ID NO: 138 and SEQ ID NO: 166. 
     
     
         17 . The formulation of any one of  claims 2  to  16 , wherein the ET A R antibody comprises 1 or 2 amino acid sequences, wherein each amino acid sequence is independently selected from the amino acid sequences listed below:
 a. amino acid sequences of light chain constant domains: SEQ ID NO: 194 and SEQ ID NO: 196; and 
 b. amino acid sequence of heavy chain constant domain: SEQ ID NO: 198. 
 
     
     
         18 . The formulation of any one of  claims 1  to  17 , wherein the ET A R antibody comprises a murine ET A R antibody or a humanized ET A R antibody. 
     
     
         19 . The formulation of any one of  claims 1  to  18 , wherein the ET A R antibody comprises a monoclonal ET A R antibody. 
     
     
         20 . The formulation of any one of  claims 1  to  19 , wherein the ET A R antibody comprises a monoclonal antibody, wherein the monoclonal antibody comprises SEQ ID NO: 138 and SEQ ID NO: 166, SEQ ID NO: 150 and SEQ ID NO: 178, SEQ ID NO: 152 and SEQ ID NO: 180, SEQ ID NO: 154 and SEQ ID NO: 182, SEQ ID NO: 156 and SEQ ID NO: 184, SEQ ID NO: 158 and SEQ ID NO: 186, SEQ ID NO: 160 and SEQ ID NO: 188, SEQ ID NO: 162 and SEQ ID NO: 190, or SEQ ID NO: 164 and SEQ ID NO: 192. 
     
     
         21 . The formulation of any one of  claims 1  to  20 , wherein the ET A R antibody has an IC 50  of approximately ranging from 1 nM to 200 nM or from 10 nM to 100 nM in reducing the signal transduction of endothelin. 
     
     
         22 . The formulation of any one of  claims 1  to  21 , wherein the concentration of the ET A R antibody is approximately ranging from 10 to 200 mg/mL or from 10 to 100 mg/mL. 
     
     
         23 . The formulation of  claim 22 , wherein the concentration of the ET A R antibody is approximately 25 mg/mL, 50 mg/mL, 75 mg/mL, or 100 mg/mL. 
     
     
         24 . The formulation of any one of  claims 1  to  23 , wherein the concentration of the buffer is approximately ranging from 1 mM to 200 mM, from 2 mM to 50 mM, or from 5 mM to 25 mM. 
     
     
         25 . The formulation of any one of  claims 1  to  24 , wherein the concentration of the buffer is approximately 10 mM, 15 mM, 20 mM, 25 mM, or 30 mM. 
     
     
         26 . The formulation of any one of  claims 1  to  25 , wherein the buffer comprises a salt of citric acid or histidine. 
     
     
         27 . The formulation of any one of  claims 1  to  26 , further comprising a surfactant. 
     
     
         28 . The formulation of  claim 27 , wherein the surfactant comprises a polysorbate. 
     
     
         29 . The formulation of  claim 27  or  28 , wherein the surfactant comprises polysorbate 20 or polysorbate 80. 
     
     
         30 . The formulation of  claim 27  or  29 , wherein the concentration of the surfactant is approximately ranging from 0.001 to 1 weight/volume percent, from 0.01 to 0.5 weight/volume percent, or from 0.01 to 0.1 weight/volume percent. 
     
     
         31 . The formulation of  claim 30 , wherein the concentration of the surfactant is approximately 0.02, 0.03, 0.04, 0.05, or 0.06 weight/volume percent. 
     
     
         32 . The formulation of any one of  claims 1  to  31 , further comprising an amino acid protectant. 
     
     
         33 . The formulation of  claim 32 , wherein the amino acid protectant comprises arginine or a salt thereof. 
     
     
         34 . The formulation of  claim 32  or  33 , wherein the amino acid protectant comprises arginine hydrochloride. 
     
     
         35 . The formulation of any one of  claims 32  to  34 , wherein the concentration of the amino acid protectant is approximately ranging from 1 mM to 500 mM or from 10 mM to 200 mM. 
     
     
         36 . The formulation of  claim 35 , wherein the concentration of the amino acid protectant is approximately 120 mM, 130 mM, 140 mM, 150 mM, or 160 mM. 
     
     
         37 . The formulation of any one of  claims 32  to  36 , wherein the concentration of the ET A R antibody is approximately ranging 10 to 200 mg/mL; the concentration of the surfactant is approximately ranging from 0.01 to 0.1 weight/volume percent; the concentration of the amino acid protectant is approximately ranging from 10 to 200 mM; and the concentration of the buffer is approximately ranging from 1 to 50 mM; wherein the pH of the formulation is approximately ranging from 5 to 7. 
     
     
         38 . The formulation of  claim 37 , wherein the concentration of the ET A R antibody is approximately 25, 50, 75, or 100 mg/mL; the concentration of the surfactant is approximately 0.04 weight/volume percent; the concentration of the amino acid protectant is approximately 140 mM; and the concentration of the buffer is approximately 20 mM; wherein the pH of the formulation is approximately ranging from 5 to 6. 
     
     
         39 . The stable solution formulation of any one of  claims 1  to  38 , further comprising a polyol protectant. 
     
     
         40 . The formulation of  claim 39 , wherein the polyol protectant comprises sorbitol, mannitol, sucrose, or trehalose. 
     
     
         41 . The formulation of  claim 39  or  40 , wherein the polyol protectant comprises sorbitol, mannitol, or sucrose. 
     
     
         42 . The formulation of  claim 39  or  41 , wherein the concentration of the polyol protectant is approximately ranging from 0.1 to 50 weight/volume percent, from 1 to 20 weight/volume percent, or from 1 to 10 weight/volume percent. 
     
     
         43 . The formulation of  claim 42 , wherein the concentration of the polyol protectant is approximately ranging from 4 to 10 weight/volume percent. 
     
     
         44 . The formulation of any one of  claims 39  to  43 , wherein the concentration of the ET A R antibody is approximately ranging from 10 to 200 mg/mL; the concentration of the surfactant is approximately ranging from 0.01 to 0.1 weight/volume percent; the concentration of the polyol protectant is approximately ranging from 1 to 20 weight/volume percent; and the concentration of the buffer is approximately ranging from 1 to 50 mM; wherein the pH of the formulation is approximately ranging from 5 to 7. 
     
     
         45 . The formulation of  claim 44 , wherein the concentration of the ET A R antibody is approximately 25, 50, 75, or 100 mg/mL; the concentration of the surfactant is approximately 0.04 weight/volume percent; the concentration of the polyol protectant is approximately ranging from 4 to 10 weight/volume percent; and the concentration of the buffer is approximately 20 mM; wherein the pH of the formulation is approximately ranging from 5 to 6. 
     
     
         46 . The formulation of any one of  claims 1  to  45 , further comprising a metal chelator. 
     
     
         47 . The formulation of  claim 46 , wherein the metal chelator comprises ethylenediaminetetraacetic acid, diethylenetriaminepentaacetic acid, or ethylene glycol diethyl ether diaminetetraacetic acid. 
     
     
         48 . The formulation of  claim 47 , wherein the metal chelator comprises ethylenediaminetetraacetic acid. 
     
     
         49 . The formulation of any one of  claims 46  to  48 , wherein the concentration of the metal chelator is approximately ranging from 0.001 mM to 1 mM, from 0.005 mM to 0.5 mM, or from 0.01 mM to 0.2 mM. 
     
     
         50 . The formulation of  claim 49 , wherein the concentration of the metal chelator is approximately 0.03 mM, 0.04 mM, 0.05 mM, 0.06 mM, or 0.07 mM. 
     
     
         51 . The formulation of any one of  claims 46  to  50 , wherein the concentration of the ET A R antibody is approximately ranging from 10 to 200 mg/mL; the concentration of the metal chelator is approximately ranging from 0.01 mM to 0.2 mM; the concentration of the surfactant is approximately ranging from 0.01 to 0.1 weight/volume percent; the concentration of the amino acid protectant is approximately ranging from 10 to 200 mM; and the concentration of the buffer is approximately ranging from 1 to 50 mM; wherein the pH of the formulation is approximately ranging from 5 to 7. 
     
     
         52 . The formulation of  claim 51 , wherein the concentration of the ET A R antibody is approximately 25, 50, 75, or 100 mg/mL; the concentration of the metal chelator is approximately 0.05 mM; the concentration of the surfactant is approximately ranging from 0.04 weight/volume percent; the concentration of the amino acid protectant is approximately 140 mM; and the concentration of the buffer is approximately 20 mM; wherein the pH of the formulation is approximately ranging from 5 to 6. 
     
     
         53 . The formulation of any one of the  claims 46  to  50 , wherein the concentration of the ET A R antibody is approximately ranging from 10 to 200 mg/mL; the concentration of the metal chelator is approximately ranging from 0.01 mM to 0.2 mM; the concentration of the surfactant is approximately ranging from 0.01 to 0.1 weight/volume percent; the concentration of the polyol protectant is approximately ranging from 1 to 20 weight/volume percent; and the concentration of the buffer is approximately ranging from 1 to 50 mM; wherein the pH of the formulation is approximately ranging from 5 to 7. 
     
     
         54 . The formulation of the  claim 53 , wherein the concentration of the ET A R antibody is approximately 25, 50, 75, or 100 mg/mL; the concentration of the metal chelator is approximately 0.05 mM; the concentration of the surfactant is approximately 0.04 weight/volume percent; the concentration of the polyol protectant is approximately ranging from 4 to 10 weight/volume percent; and the concentration of the buffer is approximately 20 mM; wherein the pH of the formulation is approximately ranging from 5 to 6. 
     
     
         55 . The formulation of any one of the  claims 1  to  54 , further comprising an antioxidant. 
     
     
         56 . The formulation of the  claim 55 , wherein the antioxidant comprises methionine, vitamin C, thiosulfate, thiosulfate, or benzyl methionine. 
     
     
         57 . The formulation of the  claim 55  or  56 , wherein the antioxidant comprises methionine. 
     
     
         58 . The formulation of the  claims 55  to  57 , wherein the concentration of the antioxidant is approximately ranging from 0.5 mM to 20 mM or from 1 mM to 10 mM. 
     
     
         59 . The formulation of the  claim 58 , wherein the concentration of the antioxidant is approximately 3 mM, 4 mM, 5 mM, 6 mM, or 7 mM. 
     
     
         60 . The formulation of any one of the  claims 55  to  59 , wherein the concentration of the ET A R antibody is approximately ranging from 10 to 200 mg/mL; the concentration of the antioxidant is approximately ranging from 1 mM to 10 mM; the concentration of the surfactant is approximately ranging from 0.01 to 0.1 weight/volume percent; the concentration of the amino acid protectant is approximately ranging from 10 to 200 mM; and the concentration of the buffer is approximately ranging from 1 to 50 mM; wherein the pH of the formulation is approximately ranging from 5 to 7. 
     
     
         61 . The formulation of the  claim 60 , wherein the concentration of the ET A R antibody is approximately 25, 50, 75, or 100 mg/mL; the concentration of the antioxidant is approximately 5 mM; the concentration of the surfactant is approximately 0.04 weight/volume percent; the concentration of the amino acid protectant is approximately 140 mM; and the concentration of the buffer is approximately 20 mM; wherein the pH of the formulation is approximately ranging from 5 to 6. 
     
     
         62 . The formulation of any one of the  claims 55  to  59 , wherein the concentration of the ET A R antibody is approximately ranging from 10 to 200 mg/mL; the concentration of the antioxidant is approximately ranging from 1 mM to 10 mM; the concentration of the surfactant is approximately ranging from 0.01 to 0.1 weight/volume percent; the concentration of the polyol protectant is approximately ranging from 1 to 20 weight/volume percent; and the concentration of the buffer is approximately ranging from 1 to 50 mM; wherein the pH of the formulation is approximately ranging from 5 to 7. 
     
     
         63 . The formulation of the  claim 62 , wherein the concentration of the ET A R antibody is approximately 25, 50, 75, or 100 mg/mL; the concentration of the antioxidant is approximately 5 mM; the concentration of the surfactant is approximately ranging from 0.04 weight/volume percent; the concentration of the polyol protectant is approximately ranging from 4 to 10 weight/volume percent; and the concentration of the buffer is approximately ranging from 20 mM; wherein the pH of the formulation is approximately ranging from 5 to 6. 
     
     
         64 . The formulation of any one of the  claims 1  to  63 , wherein the formulation is an aqueous solution. 
     
     
         65 . The formulation of any one of the  claims 1  to  64 , wherein the formulation contains no more than about 10% of an aggregated ET A R antibody after 12-month of storage at 2-8° C. 
     
     
         66 . The formulation of any one of the  claims 1  to  65 , wherein the extent of antibody degradation does not exceed about 10% after 12-month of storage at 2-8° C. 
     
     
         67 . The formulation of any one of the  claims 1  to  66 , wherein the biological activity of the ET A R antibody is no less than 50% of the original biological activity after 12-month of storage at 2-8° C. 
     
     
         68 . A method of treating, preventing, or alleviating one or more symptoms of pulmonary arterial hypertension in a subject, comprising administering to the subject a therapeutically effective amount of the formulation of any one of  claims 1  to  67 . 
     
     
         69 . A method of treating, preventing, or alleviating one or more symptoms of a disease associated with elevated pulmonary arterial pressure in a subject, comprising administering to the subject a therapeutically effective amount of the formulation of any one of  claims 1  to  67 . 
     
     
         70 . A method of treating, preventing, or alleviating one or more symptoms of cancer of a reproductive organ in a subject, comprising administering to the subject a therapeutically effective amount of the formulation of any one of  claims 1  to  67 . 
     
     
         71 . The method of the  claim 70 , wherein the cancer of a reproductive organ is cancer of a reproductive organ accompanied with elevated pulmonary arterial pressure. 
     
     
         72 . The formulation of any one of the claims  78  to  71 , wherein the subject is a human. 
     
     
         73 . The formulation of any one of the claims  78  to  72 , wherein the formulation is administered intravenously or subcutaneously.

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