Claims for Patent: 9,415,102

Summary for Patent: 9,415,102

Title:	High concentration formulations of anti-C5 antibodies
Abstract:	The present disclosure relates to, inter alia, stable aqueous solutions comprising a high concentration of an antibody that binds to human complement component C5 and methods for preparing the solutions. The disclosure also provides methods for treating or preventing complement-associated disorders (for example, age-related macular degeneration or rheumatoid arthritis) using the solutions. Also featured are therapeutic kits containing one or more of the solutions and a means for administering the solutions to a patient in need such a treatment.
Inventor(s):	Zhou; Xiao-Hong (Madison, CT), Wang; Yi (Woodbridge, CT)
Assignee:	Alexion Pharmaceuticals, Inc. (New Haven, CT)
Application Number:	13/413,268
Patent Claims:	1. A stable aqueous solution comprising: (a) an anti-C5 antibody at a concentration of about 100 mg/mL to about 200 mg/mL, wherein the anti-C5 antibody comprises CDR1, CDR2, and CDR3 domains of a heavy chain comprising the amino acid sequence set forth in SEQ ID NO:13 and CDR1, CDR2, and CDR3 domains of a light chain comprising the amino acid sequence set forth in SEQ ID NO:12, (b) about 20 mM histidine, (c) about 50 mM serine, (d) about 3% (w/v) sorbitol, and (e) about 1.5% (w/v) mannitol. 2. A stable aqueous solution consisting of: (a) an anti-C5 antibody at a concentration of about 100 mg/mL to about 200 mg/mL, wherein the anti-C5 antibody comprises CDR1, CDR2, and CDR3 domains of a heavy chain comprising the amino acid sequence set forth in SEQ ID NO:13 and CDR1, CDR2, and CDR3 domains of a light chain comprising the amino acid sequence set forth in SEQ ID NO:12, (b) about 20 mM histidine, (c) about 50 mM serine, (d) about 3% (w/v) sorbitol, and (e) about 1.5% (w/v) mannitol. 3. The stable aqueous solution of claim 1, wherein the anti-C5 antibody comprises a heavy chain comprising the amino acid sequence set forth in SEQ ID NO:13 and a light chain comprising the amino acid sequence set forth in SEQ ID NO:12. 4. The stable aqueous solution of claim 1, wherein the anti-C5 antibody is eculizumab. 5. The stable aqueous solution of claim 1, wherein the pH of the solution is between 6.5 and 7.5. 6. The stable aqueous solution of claim 5, wherein the pH of the solution is 7.0. 7. The stable aqueous solution of claim 1, wherein the anti-C5 antibody is at a concentration of 100 mg/mL. 8. The stable aqueous solution of claim 1, wherein the solution is sterile. 9. The stable aqueous solution of claim 1, wherein the anti-C5 antibody remains at least 97% monomeric during storage at 2.degree. C. to 8.degree. C. for at least six months as determined by SEC-HPLC. 10. The stable aqueous solution of claim 1, wherein the anti-C5 antibody remains at least 97% monomeric during storage at 2.degree. C. to 8.degree. C. for at least one year as determined by SEC-HPLC. 11. The stable aqueous solution of claim 1, wherein less than 2% of the anti-C5 antibody in the solution is aggregated as determined by SEC-HPLC. 12. The stable aqueous solution of claim 1, wherein less than 1% of the anti-C5 antibody in the solution is fragmented as determined by SEC-HPLC. 13. The stable aqueous solution of claim 1, wherein during storage at 2.degree. C. to 8.degree. C. for at least six months the anti-C5 antibody retains at least 90% of its C5-binding activity, as compared to a reference anti-C5 antibody corresponding to the anti-C5 antibody prior to storage. 14. The stable aqueous solution of claim 1, wherein during storage at 2.degree. C. to 8.degree. C. for at least six months the anti-C5 antibody retains at least 95% of its ability to inhibit hemolysis, as compared to a reference anti-C5 antibody corresponding to the anti-C5 antibody prior to storage. 15. A stable aqueous solution comprising: (a) eculizumab, (b) about 20 mM histidine, (c) about 50 mM serine, (d) about 3% (w/v) sorbitol, and (e) about 1.5% (w/v) mannitol.

Details for Patent 9,415,102

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Alexion Pharmaceuticals, Inc.	SOLIRIS	eculizumab	Injection	125166	03/16/2007		2031-03-08