IP Library › Granted Patent US 12,616,699
Granted Patent B2
US 12,616,699 · App. 17/753,721 · Granted May 5, 2026

Ophthalmic formulations of methotrexate

Inventors: Dean Eliott (Carlsbad, CA); Stephen Gitu Machatha (Wilmington, MA); Pramod Sarpotdar (Roseville, CA); Tomasz Stryjewski (Somerville, MA)
Assignee: Aldeyra Therapeutics, Inc.
A61K31/519A61K9/0048A61K47/02A61K47/26
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Quick Facts
Patent No.
US 12,616,699
App. No.
17/753,721
Granted
May 5, 2026
Kind
B2
Abstract

The present disclosure provides formulations of methotrexate for ocular administration, including intravitreal administration, and use of the formulations for treating proliferative vitreoretinopathy (PVR), intraocular lymphoma (e.g., PVRL), and intraocular inflammation.

Claims (20)

1 . A composition suitable for intravitreal administration, comprising:

methotrexate at a concentration of about 7 mg/mL to about 9 mg/mL, and a density enhancing agent selected from sucrose, trehalose, glucose, polyvinyl acetate, polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), carboxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, polyethylene glycol (PEG), glycerol, poly(lactide) (PLA), poly(lactide-co-glycolide) (PLGA), polyglycolide (PGA), polyhydroxybutyric acid, polycaprolactone, polyvalerolactone, polyphosphazene, polyorthoester, cyclodextrin, or mixtures thereof,

wherein the composition has a density of about 1.0 to about 1.20 g/cm 3 at 20° C.

2 . The composition of claim 1 , wherein the composition has a transit rate of less than 10 min in 1 mL of silicone oil (SiO) having a viscosity of at least 1000 centistoke and depth of 1 cm.

3 . The composition of claim 2 , wherein the SiO is polydimethyl siloxane 5000 centistoke oil or polydimethyl siloxane 1000 centistoke oil.

4 . The composition of claim 1 , wherein the composition has a density of at least about 1.03 g/cm 3 at 20° C.

5 . The composition of claim 1 , wherein the density enhancing agent is PEG.

6 . The composition of claim 5 , wherein the PEG is PEG 4000.

7 . The composition of claim 6 , wherein the PEG 4000 is at a concentration of about 5% to 10% w/v of the composition.

8 . The composition of claim 7 , wherein the PEG 4000 is at about 7.5% w/v of the composition.

9 . The composition of claim 1 , further comprising a surfactant.

10 . The composition of claim 9 , wherein the surfactant comprises a non-ionic surfactant.

11 . The composition of claim 9 , wherein the surfactant is selected from polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monopalmitate, polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan mono-oleate, polyoxyethylene (20) sorbitan tristearate, polyoxyethylene (20) sorbitan tri-oleate, sorbitan monopalmitate, sorbitan monostearate, sorbitan mono-oleate, sorbitan tristearate, and sorbitan trioleate.

12 . The composition of claim 11 , wherein the surfactant is polyoxyethylene (20) sorbitan monolaurate or polyoxyethylene (20) sorbitan mono-oleate.

13 . The composition of claim 10 , wherein the surfactant is present at a concentration of 0.0015% w/v to about 0.05% w/v.

14 . The composition of claim 1 , further comprising a buffering agent.

15 . The composition of claim 14 , wherein the buffering agent is selected from borate, phosphate, bicarbonate, carbonate, citrate, tetraborate, biphosphate, tromethamine, hydroxyethyl morpholine, and THAM (trishydroxymethylamino-methane).

16 . The composition of claim 1 , wherein the composition is at a pH of about 5.5 to about 8.5.

17 . The composition of claim 16 , wherein the pH is about 6.5 to about 7.5.

18 . The composition of claim 1 , wherein the density enhancing agent is sucrose present at a concentration of about 7.5% w/v of the composition.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 8, 2023
From: ELIOTT, DEAN; MACHATHA, STEPHEN GITU; SARPOTDAR, PRAMOD; STRYJEWSKI, TOMASZ
To: ALDEYRA THERAPEUTICS, INC.
Reel/Frame 062920/0667 →
Continuity (3)
Provisional Application 63044288 · Jun 25, 2020
Provisional Application 62900060 · Sep 13, 2019
Related Publication 20220370460A1 · Nov 24, 2022
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