IP Library Granted Patent US 12,478,577
Granted Patent B2
US 12,478,577 · App. 16/810,149 · Granted Nov 25, 2025

Pharmaceutical compositions for treating ocular diseases or disorders

Inventors: Sanjib Kumar Das (Morrisville, NC); Cheng-Wen Lin (Cary, NC)
Assignee: Alcon Inc.
A61K9/0024A61K31/472A61K31/573A61K47/34A61K9/0048A61K45/06
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Quick Facts
Patent No.
US 12,478,577
App. No.
16/810,149
Granted
Nov 25, 2025
Kind
B2
Abstract

Provided herein are pharmaceutical compositions, intravitreal implants and particle suspensions comprising a polymer matrix and at least one therapeutic agent that is released in a substantially linear manner for a particular duration.

Claims (30)

1 . A pharmaceutical composition for treating an ocular disease or disorder, comprising:

(a) a biodegradable polymer matrix consisting of a mixture of a first polymer and a second polymer, wherein:

(1) the first polymer is a biodegradable polyester amide polymer, wherein the biodegradable polyester amide polymer comprises structure (II):

and

(2) the second polymer is a combination of an ester end-capped biodegradable poly (D,L-lactide-co-glycolide) copolymer and an acid end-capped biodegradable poly (D,L-lactide-co-glycolide) copolymer; and

(b) at least one therapeutic agent, pharmaceutically acceptable salt, zwitterion, polymorph, or solvate thereof, wherein the at least one therapeutic agent is selected from gefitinib, lapatinib, erlotinib, sunitinib, sorafenib, regorafenib, afatinib, vandetanib, semaxanib, cediranib, neratinib, axitinib, lestaurtinib, tivozanib, dexamethasone, or (1R,2R)—N-(4-methylisoquinolin-6-yl)-2-(4-(N-(pyridin-2-yl)sulfamoyl)phenyl)cyclopropane-1-carboxamide;

wherein the at least one therapeutic agent, pharmaceutically acceptable salt, zwitterion, polymorph, or solvate thereof is homogenously dispersed within the biodegradable polymer matrix;

wherein the pharmaceutical composition is formulated for intravitreal administration to a subject's eye, and the pharmaceutical composition is formulated to release the at least one therapeutic agent from the pharmaceutical composition in a substantially linear manner for at least 6 months;

wherein the biodegradable polymer matrix is about 59 weight % of the pharmaceutical composition, and the at least one therapeutic agent, pharmaceutically acceptable salt, zwitterion, polymorph, or solvate thereof is about 41 weight % of the pharmaceutical composition; and

wherein the first polymer is about 60 weight % of the biodegradable polymer matrix and the second polymer is about 40 weight % of the biodegradable polymer matrix.

2 . A pharmaceutical composition as in claim 1 , wherein the at least one therapeutic agent is selected from:

gefitinib;

lapatinib;

erlotinib;

sunitinib;

sorafenib;

regorafenib;

afatinib;

vandetanib;

semaxanib;

cediranib;

neratinib;

axitinib;

lestaurtinib;

tivozanib; or

a combination thereof.

3 . A pharmaceutical composition as in claim 1 , wherein the biodegradable polymer matrix is a mechanical blend of the first polymer and the second polymer.

4 . A pharmaceutical composition as in claim 1 , wherein:

the ester end-capped biodegradable poly (D,L-lactide-co-glycolide) copolymer is about 20 weight % of the biodegradable polymer matrix, and the acid end-capped biodegradable poly (D,L-lactide-co-glycolide) copolymer is about 20 weight % of the biodegradable polymer matrix.

5 . A pharmaceutical composition as in claim 1 , wherein the pharmaceutical composition is a particle comprising dimensions of about 200×200×4500 μm.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2024
From: AERIE PHARMACEUTICALS, INC.
To: ALCON INC.
Reel/Frame 067822/0168 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 5, 2020
From: DAS, SANJIB KUMAR; LIN, CHENG-WEN
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 052028/0472 →