公开(公告)号：US20200048367A1

公开(公告)日：2020-02-13

申请号：US16607673

申请日：2018-04-27

Applicant: AMGEN INC.

Inventor： Neeraj Jagdish AGRAWAL ,  Pavan GHATTYVENKATAKRISHNA ,  Sekhar KANAPURAM ,  Christopher James SLOEY

IPC: C07K16/40 ,  A61K38/05 ,  A61K31/198 ,  A61K31/4172 ,  A61K31/401 ,  A61K47/26 ,  A61K9/08 ,  A61K9/19

Abstract: Provided herein are excipients capable of effectively reducing the viscosity of polypeptide (e.g., therapeutic polypeptide) formulations. The viscosity reducing excipients are dipeptides containing arginine at the carboxy terminus and N-acetylated serine or N-acetylated proline at the N-terminus. Glutamate-arginine is also disclosed as a viscosity-reducing dipeptide. Among the disclosed methods, methods of reducing the viscosities of such formulations are also provided.

公开(公告)号：US20220226477A1

公开(公告)日：2022-07-21

申请号：US17605512

申请日：2020-04-22

Applicant: AMGEN INC.

Inventor： Christopher James SLOEY

IPC: A61K47/32 ,  A61K9/00 ,  A61K9/19

Abstract: Disclosed herein are pharmaceutical compositions (formulations) having reduced viscosity, using a low molecular weight polyvinylpyrrolidone (povidone) in the case of high therapeutic protein concentration (≥70 mg/ml) formulations. The addition of arginine, such as arginine monohydrochloride or N-acetyl arginine, can further reduce viscosity. Appropriate therapeutic proteins include antibodies, such as monoclonal antibodies, and derivatives, fragments, and analogues thereof.

公开(公告)号：US20180237501A1

公开(公告)日：2018-08-23

申请号：US15902775

申请日：2018-02-22

Applicant: AMGEN INC.

Inventor： Christopher James SLOEY ,  Sekhar KANAPURAM ,  Huanchun CUI ,  Chio Mui CHAN ,  Elaheh BINABAJI

IPC: C07K16/06 ,  C07K16/22 ,  C07K1/36 ,  A61K39/395 ,  A61K47/18 ,  A61K9/00 ,  C07K1/16

CPC classification number: C07K16/065 ,  A61K9/0019 ,  A61K39/3955 ,  A61K39/39591 ,  A61K47/183 ,  C07K1/16 ,  C07K1/36 ,  C07K16/22 ,  C07K16/40 ,  C07K2317/565 ,  C07K2317/76 ,  C07K2317/90

Abstract: Provided herein are formulations of PCSK9-binding polypeptides, such as those comprising evolocumab, that comprise N-acetyl arginine and have reduced viscosities when compared to formulations lacking N-acetyl arginine. Provided herein are also methods of formulating such compositions that are advantageous in that they conserve certain components. Such formulations comprising PCSK9-binding polypeptides can be administered to patients to treat and/or prevent PCSK9-related diseases, conditions, and disorders.

公开(公告)号：US20240066124A1

公开(公告)日：2024-02-29

申请号：US18383121

申请日：2023-10-24

Applicant: AMGEN INC.

Inventor： Christopher James SLOEY ,  Sekhar KANAPURAM

IPC: A61K39/395 ,  A61K9/19 ,  A61K47/18

CPC classification number: A61K39/39591 ,  A61K9/19 ,  A61K39/3955 ,  A61K47/183 ,  A61K9/0019

Abstract: A method for reducing the viscosity of a pharmaceutical formulation is provided that utilizes a viscosity-reducing concentration of an excipient selected from the group consisting of the n-acetyl arginine, n-acetyl lysine, n-acetyl proline and mixtures thereof in combination with a therapeutiv protein. A stable pharmaceutical formulation is also provided.

公开(公告)号：US20230226177A1

公开(公告)日：2023-07-20

申请号：US17893515

申请日：2022-08-23

Applicant: AMGEN INC.

Inventor： Christopher James SLOEY ,  Sekhar KANAPURAM ,  Huanchun CUI ,  Chio Mui CHAN ,  Elaheh BINABAJI

IPC: A61K39/395 ,  C07K1/36 ,  A61K9/00 ,  C07K1/16 ,  A61K47/18 ,  C07K16/40

CPC classification number: A61K39/3955 ,  A61K9/0019 ,  A61K39/39591 ,  A61K47/183 ,  C07K1/16 ,  C07K1/36 ,  C07K16/40 ,  C07K16/065

Abstract: Provided herein are formulations of PCSK9-binding polypeptides, such as those comprising evolocumab, that comprise N-acetyl arginine and have reduced viscosities when compared to formulations lacking N-acetyl arginine. Provided herein are also methods of formulating such compositions that are advantageous in that they conserve certain components. Such formulations comprising PCSK9-binding polypeptides can be administered to patients to treat and/or prevent PCSK9-related diseases, conditions, and disorders.

公开(公告)号：US20210069334A1

公开(公告)日：2021-03-11

申请号：US16855896

申请日：2020-04-22

Applicant: Amgen Inc.

Inventor： Tiansheng LI ,  Christopher James SLOEY

IPC: A61K47/10 ,  A61K39/395 ,  A61K9/00 ,  A61K9/19 ,  A61K38/18 ,  A61K38/19 ,  A61K47/02 ,  A61K47/18 ,  A61K47/26

Abstract: A method of stabilizing an aqueous protein or antibody formulation is disclosed herein. Additionally, stable pharmaceutical formulations are contemplated which comprise a biologically active protein, a destabilizing concentration of preservative and a stabilizing concentration of osmolyte.

公开(公告)号：US20170333559A1

公开(公告)日：2017-11-23

申请号：US15521057

申请日：2015-10-22

Applicant: AMGEN INC.

Inventor： Christopher James SLOEY ,  Sekhar KANAPURAM

IPC: A61K39/395 ,  A61K47/18 ,  A61K9/19 ,  A61K9/00

CPC classification number: A61K39/39591 ,  A61K9/0019 ,  A61K9/19 ,  A61K39/3955 ,  A61K47/183 ,  C07K2317/90

Abstract: A method for reducing the viscosity of a pharmaceutical formulation is provided that utilizes a viscosity-reducing concentration of an excipient selected from the group consisting of the n-acetyl arginine, n-acetyl lysine, n-acetyl proline and mixtures thereof in combination with a therapeutiv protein. A stable pharmaceutical formulation is also provided.