IP Library Granted Patent US 10,765,672
Granted Patent B2
US 10,765,672 · App. 16/035,503 · Granted Sep 8, 2020

Pharmaceutical formulations of a HIF hydroxylase inhibitor

Inventors: David Conca (San Francisco, CA); Lee Allen Flippin (Woodside, CA); Scott David Leigh (Castro Valley, CA); Claudia Witschi (San Francisco, CA); Lee Robert Wright (Redwood City, CA)
Assignee: FibroGen, Inc.
A61K31/472A61K9/2009A61K9/282A61K9/2813A61K9/485A61K9/4816A61K9/4858A61K9/4883A61K9/4891A61K9/2013A61K9/2018A61K9/2027A61K9/2054A61K9/4825
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Quick Facts
Patent No.
US 10,765,672
App. No.
16/035,503
Granted
Sep 8, 2020
Kind
B2
Abstract

The present disclosure relates to pharmaceutical formulations of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid and methods of use thereof.

Claims (15)

1. A tablet comprising a tablet core and a coating, wherein the tablet core comprises [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, and the coating comprises a photostabilizing agent, wherein the photostabilizing agent:

i) consists essentially of from about 0.1 to about 2 mg/cm 2 titanium dioxide and from about 0.1 to about 0.4 mg/cm 2 Allura Red AC or from about 0.1 to about 0.4 mg/cm 2 Allura Red AC in aluminum lake; and

optionally at least one additional dye selected from the group consisting of:

from about 0.004 to about 0.4 mg/cm 2 iron oxide red;

from about 0.009 to about 0.2 mg/cm 2 iron oxide yellow;

from about 0.01 to about 0.03 mg/cm 2 Sunset Yellow FCF; and

from about 0.01 to about 0.03 mg/cm 2 Sunset Yellow FCF in aluminum lake;

wherein the amount of photostabilizing agent is based on surface area of the tablet core; and

ii) prevents the transmission of light at a wavelength range of between about 200 nm and 550 nm

and further wherein the tablet contains less than about 0.2% w/w photodegradation product of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid relative to the amount of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid.

2. The tablet of claim 1 , comprising from about 20 mg to about 200 mg of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid.

3. The tablet of claim 1 , comprising about 20 mg, about 50 mg, or about 100 mg of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid.

4. The tablet of claim 1 , wherein the tablet comprises a tablet core and a coating and the tablet core comprises [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, and the coating comprises the photostabilizing agent, and the coating is present in an amount from about 3% to about 8% w/w based on the weight of the tablet core.

5. The tablet of claim 4 , wherein the coating comprises from about 0.1 to about 0.4 mg/cm 2 titanium dioxide and from about 0.1 to about 0.4 mg/cm 2 Allura Red AC in aluminum lake, and wherein the amount of titanium dioxide and Allura Red AC in aluminum lake is based on surface area of the tablet core.

6. The tablet of claim 5 , wherein the tablet core comprises about 20 mg, about 50 mg or about 100 mg of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, lactose monohydrate, microcrystalline cellulose, povidone, croscarmellose sodium, and magnesium stearate; and wherein the photostabilizing agent comprises 0.1 to about 0.4 mg/cm 2 titanium dioxide and from about 0.1 to about 0.4 mg/cm 2 Allura Red AC in aluminum lake wherein the amount of titanium dioxide and Allura Red AC in aluminum lake is based on surface area of the tablet core.

Assignments (4)
CHANGE OF NAME Recorded Feb 18, 2026
From: FIBROGEN, INC.
To: KYNTRA BIO, INC.
Reel/Frame 074923/0352 →
RELEASE OF SECURITY INTEREST Recorded Sep 3, 2025
From: WILMINGTON TRUST, NATIONAL ASSOCIATION, AS AGENT
To: FIBROGEN, INC.
Reel/Frame 072785/0760 →
SECURITY INTEREST Recorded May 1, 2023
From: FIBROGEN, INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 063504/0221 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2019
From: CONCA, DAVID; FLIPPIN, LEE ALLEN; LEIGH, SCOTT DAVID; WITSCHI, CLAUDIA; WRIGHT, LEE ROBERT
To: FIBROGEN, INC.
Reel/Frame 049211/0196 →
Continuity (3)
Continuation 14896353
Provisional Application 61831909 · Jun 6, 2013
Related Publication 20190008846A1 · Jan 10, 2019