Granted Patent B2

US 12,508,234 · App. 18/475,930 · Granted Dec 30, 2025

Inventors: Eva Byröd (Mölndal, SE); Per-Göran Gillberg (Mölndal, SE); Anna-Maria Tivert (Gothenburg, SE); Rikard Bryland (Limhamn, SE); Ann-Charlotte Dahlquist (Lund, SE); Jessica Elversson (Dalby, SE); Nils Ove Gustafsson (Löddeköpinge, SE); Robert Lundqvist (Hälsö, SE); Ingvar Ymen (Saltsjö-Boo, SE); Martin Bohlin (Johanneshov, SE)

Assignee: ALBIREO AB

A61K9/5047A61K9/009A61K9/10A61K9/4808A61K9/4816A61K9/4866A61K9/5042A61K9/5078A61K9/5089A61K31/554C07D285/36C07B2200/13

Abstract

Claims (28)

1 . A method for treating a liver disease comprising administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical formulation of odevixibat,

wherein the pharmaceutical formulation of odevixibat comprises a plurality of particles,

wherein each particle is between about 0.1 and about 1.5 mm in size and contains odevixibat, or a pharmaceutically acceptable salt thereof, in an amount of from about 0.1% w/w to about 5.0% w/w based on the total weight of the particle, and

wherein each particle comprises odevixibat agglomerates having a d 90 particle size distribution of less than 15 μm.

2 . The method according to claim 1 , wherein the liver disease is a cholestatic liver disease.

3 . The method according to claim 2 , wherein the cholestatic liver disease is selected from the group consisting of: biliary atresia; progressive familial intrahepatic cholestasis (PFIC); Alagille syndrome (ALGS); and primary biliary cirrhosis (PBC).

4 . The method according to claim 2 , wherein the cholestatic liver disease is cholestatic pruritus.

5 . The method according to claim 2 , wherein the cholestatic liver disease is biliary atresia.

6 . The method according to claim 5 , wherein the biliary atresia is post-Kasai biliary atresia or post-liver transplantation biliary atresia.

7 . The method according to claim 2 , wherein the cholestatic liver disease is PFIC.

8 . The method according to claim 7 , wherein the PFIC is PFIC-1, PFIC-2, PFIC-3, non-specified PFIC, post-biliary diversion PFIC, or post-liver transplant PFIC.

9 . The method according to claim 2 , wherein the cholestatic liver disease is ALGS.

10 . The method according to claim 1 , wherein each particle contains odevixibat, or a pharmaceutically acceptable salt thereof, in an amount of from about 0.5% w/w to about 2.0% w/w based on the total weight of the particle.

11 . The method according to claim 1 , wherein each particle comprises a core and a coating layer surrounding the core.

12 . The method according to claim 11 , wherein the coating layer comprises odevixibat, or a pharmaceutically acceptable salt thereof.

13 . The method according to claim 11 , wherein the core does not contain odevixibat, or a pharmaceutically acceptable salt thereof.

14 . The method according to claim 1 , wherein odevixibat is present as a crystalline hydrate of odevixibat.

15 . The method according to claim 1 , wherein odevixibat is present as crystal modification 1 of odevixibat.

16 . The method according to claim 15 , wherein crystal modification 1 of odevixibat has an X-ray powder diffraction (XRPD) pattern, obtained with CuKα1-radiation, with at least specific peaks at °2θ positions 5.6±0.2, 6.7±0.2 and/or 12.1±0.2.

17 . The method according to claim 1 , wherein the subject is a pediatric subject.

18 . A process for the preparation of a pharmaceutical formulation of odevixibat, the process comprising the step of preparing a homogeneous aqueous suspension of odevixibat.

19 . The process according to claim 18 , wherein the homogenous aqueous suspension is prepared by dispersing odevixibat in water by wet milling.

20 . A process for the preparation of a pharmaceutical formulation of odevixibat, or a pharmaceutically acceptable salt thereof, the process comprising the steps of:

a) wetting odevixibat in water using a homogenizer;

b) dispersing the wetted odevixibat in water by wet milling, thereby obtaining a homogeneous aqueous suspension of odevixibat; and

c) spraying the homogeneous aqueous suspension of odevixibat onto a plurality of cores, thereby forming a plurality of particles;

wherein each particle is between about 0.1 and about 1.5 mm in size and contains odevixibat, or pharmaceutically acceptable salt thereof, in an amount of from about 0.1% w/w to about 5.0% w/w based on the total weight of the particle, and

wherein each particle comprises odevixibat agglomerates having a d 90 particle size distribution of less than 15 μm.

Assignments (27)

Priority Claims (2)

Continuity (2)

References Cited (400)