Dosing regimens and related compositions and methods

Patent metadata

Field	Value
Publication number	US-12458695-B2
Application number	US-202519054696-A
Country	US
Kind code	B2
Filing date	Feb 14, 2025
Priority date	Dec 15, 2017
Publication date	Nov 4, 2025
Grant date	Nov 4, 2025

Abstract

In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ.

First claim

We claim:

1 . A composition comprising:
(i) a long-acting compstatin analog (LACA) having a structure:

wherein the (CH 2 CH 2 O) n moiety has an average molecular weight of about 40,000 Daltons;
(ii) a pharmaceutically acceptable carrier; and
(iii) trehalose,
wherein the pH of the composition is 4.9 to 5.1.

2 . The composition of claim 1 , wherein the LACA is at a concentration of about 150 mg/mL.

3 . The composition of claim 2 , wherein the composition has an osmolality between 180 mOsm/kg and 500 mOsm/kg.

4 . The composition of claim 3 , wherein the composition comprises an acetate buffer.

5 . The composition of claim 4 , wherein the acetate buffer comprises sodium acetate and acetic acid.

6 . The composition of claim 5 , wherein the pharmaceutically acceptable carrier is water.

7 . The composition of claim 6 , wherein the pH of the composition is 5.0.

8 . A single dose vial containing the composition of claim 6 for delivery of a 100 microliter dose of said composition.

9 . The composition of claim 2 , wherein the composition has an osmolality between 200 mOsm/kg and 400 mOsm/kg.

10 . The composition of claim 9 , wherein the composition comprises an acetate buffer.

11 . The composition of claim 10 , wherein the acetate buffer comprises sodium acetate and acetic acid.

12 . The composition of claim 1 , wherein the pharmaceutically acceptable carrier is water.

13 . The composition of claim 1 , consisting essentially of the LACA, trehalose, acetate buffer, and water.

14 . The composition of claim 13 , wherein the acetate buffer comprises sodium acetate and acetic acid.

15 . The composition of claim 13 , wherein the LACA is at a concentration of about 150 mg/mL and the composition has an osmolality between 180 mOsm/kg and 500 mOsm/kg.

16 . The composition of claim 15 , wherein the pH of the composition is 5.0.

17 . A single dose vial containing the composition of claim 15 , for delivery of a 100 microliter dose of said composition.

18 . The composition of claim 15 , wherein the LACA is at a concentration of about 150 mg/mL and the composition has an osmolality between 200 mOsm/kg and 400 mOsm/kg.

19 . A composition comprising:
(i) a long-acting compstatin analog (LACA) having a structure:

wherein the (CH 2 CH 2 O) n moiety has an average molecular weight of about 40,000 Daltons;
(ii) a pharmaceutically acceptable carrier; and
(iii) trehalose,
wherein the pH of the composition is 4.5 to 5.0.

20 . The composition of claim 19 , wherein the LACA is at a concentration of about 150 mg/mL.

21 . The composition of claim 20 , wherein the composition has an osmolality between 180 mOsm/kg and 500 mOsm/kg.

22 . The composition of claim 21 , wherein the composition comprises an acetate buffer.

23 . The composition of claim 20 , wherein the composition has an osmolality between 200 mOsm/kg and 400 mOsm/kg.

24 . The composition of claim 23 , wherein the composition comprises an acetate buffer.

25 . The composition of claim 24 , wherein the pharmaceutically acceptable carrier is water.

26 . The composition of claim 19 , consisting essentially of the LACA, trehalose, acetate buffer, and water.

27 . The composition of claim 26 , wherein the acetate buffer comprises sodium acetate and acetic acid.

28 . The composition of claim 26 , wherein the LACA is at a concentration of about 150 mg/mL and the composition has an osmolality between 180 mOsm/kg and 500 mOsm/kg.

29 . A single dose vial containing the composition of claim 28 , for delivery of a 100 microliter dose of said composition.

30 . The composition of claim 19 , wherein the pH of the composition is 4.5.

Assignees

• Apellis Pharmaceuticals Inc

Inventors

• Grossi Federico
• Deschatelets Pascal
• Francois Cedric
• Johnson Patrick
• Vega Carolina

Classifications

• A61K38/12 Primary

  Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)} · CPC title

• A61K38/10

  Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)} · CPC title

• C07K7/08

  having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68) · CPC title

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title

• A61K47/183

  Amino acids, e.g. glycine, EDTA or aspartame · CPC title