IP Library › Granted Patent US 12,636,253
Granted Patent B2
US 12,636,253 · App. 17/689,255 · Granted May 26, 2026

Modified release compositions of nafamostat and methods of using same

Inventor: Lynn Kirkpatrick (La Jolla, CA)
Assignee: Ensysce Biosciences Inc.
A61K9/1676A61K9/1611A61K9/1623A61K9/1647A61K9/1652A61K31/216A61K9/0053
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Quick Facts
Patent No.
US 12,636,253
App. No.
17/689,255
Granted
May 26, 2026
Kind
B2
Abstract

Aspects of the present disclosure include a composition of nafamostat or a pharmaceutically acceptable salt thereof that provides for controlled release of nafamostat or pharmaceutically acceptable salt thereof to a subject for an extended period of time. Compositions according to certain embodiments include a plurality of controlled release beads where each bead includes a core, an active agent layer having nafamostat or a pharmaceutically acceptable salt thereof and a controlled release layer having one or more polymers formulated in an amount sufficient to provide for controlled release of the nafamostat or pharmaceutically 10 acceptable salt thereof. Methods for administering (e.g., orally) the controlled release nafamostat compositions to a subject are also described.

Claims (35)

1 . A composition comprising nafamostat or a pharmaceutically acceptable salt thereof, wherein the composition provides for controlled release of the nafamostat or pharmaceutically acceptable salt thereof to a subject for an extended period of time, the composition comprising a plurality of controlled release beads, each bead comprising:

a core;

an active agent layer comprising nafamostat or a pharmaceutically acceptable salt thereof; and

a controlled release layer comprising one or more polymers formulated in an amount sufficient to provide for controlled release of the nafamostat or pharmaceutically acceptable salt thereof.

2 . The composition of claim 1 , wherein the core comprises a cellulose polymer, or silicon dioxide, or a sugar selected from the group consisting of glucose, sucrose, lactose, mannitol, xylitol, and sorbitol.

3 . The composition of claim 1 , wherein the active agent layer further comprises a binder.

4 . The composition of claim 1 , wherein the controlled release layer comprises a combination of:

acrylate copolymer A comprising poly(ethylacrylate, methyl-methacrylate and chlorotrimethyl-ammonioethyl methacrylate) comprising about 50 mEq of quaternary ammonium groups per 100 g of polymer; and

acrylate copolymer B comprising poly(ethylacrylate, methyl-methacrylate and chlorotrimethyl-ammonioethyl methacrylate) comprising about 25 mEq of quaternary ammonium groups per 100 g of polymer.

5 . The composition of claim 4 , wherein the controlled release layer comprises:

acrylate copolymer comprises: 95% by weight acrylate copolymer B and 5% by weight acrylate copolymer A; or

acrylate copolymer comprises: 93% by weight acrylate copolymer B and 7% by weight acrylate copolymer A; or

acrylate copolymer comprises: 92% by weight acrylate copolymer B and 8% by weight acrylate copolymer A; or

acrylate copolymer comprises: 90% by weight acrylate copolymer B and 10% by weight acrylate copolymer A; or

acrylate copolymer comprises 87% by weight acrylate copolymer B and 13% by weight acrylate copolymer A; or

acrylate copolymer comprises: 80% by weight acrylate copolymer B and 20% by weight acrylate copolymer A; or

acrylate copolymer comprises: 70% by weight acrylate copolymer B and 30% by weight acrylate copolymer A.

6 . The composition of claim 1 , wherein the controlled release layer comprises from 5% to 30% by weight of each of the plurality of beads.

7 . The composition of claim 1 , wherein one or more of the active agent layer and the controlled release layer further comprise a plasticizer.

8 . The composition of claim 1 , wherein each of the plurality of beads comprises from 5% to 20% by weight of the nafamostat or a pharmaceutically acceptable salt thereof.

9 . The composition of claim 1 , wherein the composition comprises a plurality of controlled release beads, each bead comprising:

a microcrystalline cellulose core;

an active agent layer comprising nafamostat or a pharmaceutically acceptable salt thereof and a water soluble methylcellulose polymer; and

a controlled release layer comprising:

a first polymer comprising poly(ethylacrylate, methyl-methacrylate and chlorotrimethyl-ammonioethyl methacrylate) containing about 50 mEq of quaternary ammonium groups per 100 g of polymer;

a second polymer comprising poly(ethylacrylate, methyl-methacrylate and chlorotrimethyl-ammonioethyl methacrylate) containing about 25 mEq of quaternary ammonium groups per 100 g of polymer;

triethyl citrate; and

a glidant selected from micronized talc and an amorphous silica,

wherein the controlled release layer is formulated to provide for controlled release of the nafamostat or pharmaceutically acceptable salt thereof.

10 . The composition of claim 9 , wherein the controlled release layer is formulated to provide for release of 60% or more of the nafamostat or pharmaceutically acceptable salt thereof within 6 hours after administration.

11 . The composition of claim 1 , wherein the controlled release layer is formulated to provide for release of 90% or more of the nafamostat or pharmaceutically acceptable salt thereof within 6 hours of administration.

12 . The composition of claim 1 , further comprising nafamostat or a pharmaceutically acceptable salt thereof in an immediate release form that provides for an immediate release of nafamostat or pharmaceutically acceptable salt thereof to the subject.

13 . A method comprising administering to the respiratory system of a subject in need thereof a composition of claim 1 , wherein administering to the respiratory system of the subject comprises inhalation, intratracheal instillation, intratracheal delivery, insufflation, nebulization or a combination thereof.

14 . The composition of claim 1 , wherein the controlled release layer is formulated to provide for release of 90% or more of the nafamostat or pharmaceutically acceptable salt thereof within 4 hours of administration.

15 . The composition of claim 1 , wherein the controlled release layer is formulated to provide for release of 90% or more of the nafamostat or pharmaceutically acceptable salt thereof within 9 hours of administration.

Assignments (3)
SECURITY INTEREST Recorded Dec 18, 2023
From: ENSYSCE BIOSCIENCES, INC.; EBI OPCO, INC.; EBI OPERATING, INC.; EBIR, INC.
To: 3I, LP
Reel/Frame 065902/0035 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 9, 2023
From: KIRKPATRICK, LYNN
To: ENSYSCE BIOSCIENCES INC.
Reel/Frame 062642/0845 →
SECURITY INTEREST Recorded Jul 8, 2022
From: ENSYSCE BIOSCIENCES, INC.; EBI OPCO, INC.; EBI OPERATING, INC.; COVISTAT, INC.
To: 3I, LP
Reel/Frame 060616/0487 →
Continuity (2)
Provisional Application 63158654 · Mar 9, 2021
Related Publication 20220287975A1 · Sep 15, 2022
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