IP Library Granted Patent US 11,471,408
Granted Patent B2
US 11,471,408 · App. 16/875,710 · Granted Oct 18, 2022

Isotretinoin formulations and uses and methods thereof

Inventors: Zachary Rome (Nyack, NY); Charles Rodney Greenaway Evans (Worthing, GB); Marc Barry Brown (Hertfordshire, GB); Francesco Caserta (Morrisville, NC)
Assignee: TIMBER PHARMACEUTICALS LLC
A61K9/06A61K31/198A61K31/202A61K31/203A61K45/06A61K47/10A61K47/14A61P17/04A61Q19/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,471,408
App. No.
16/875,710
Granted
Oct 18, 2022
Kind
B2
Abstract

Provided herein are novel isotretinoin formulations that provide an enhanced targeted dermal delivery system for the drug isotretinoin with improved thermodynamic activity using no to a small level of ethanol relative to existing isotretinoin gel products, and methods for treatment of ichthyosis and other skin conditions using the same.

Claims (17)

1. A method of treating congenital ichthyosis in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition consisting of PEG 400, PEG 3350, PEG 1450, about 0.01% w/w to about 0.6% w/w isotretinoin, at least one preservative, and at least one antioxidant, wherein the pharmaceutical composition has 0% w/w of ethanol and 0% w/w of water, and is formulated as a gel, ointment, lotion, emulsion or cream.

2. The method of claim 1 , wherein the at least one antioxidant is butylated hydroxytoluene (BHT).

3. The method of claim 1 , wherein the at least one preservative is methyl paraben, propyl paraben, or a combination thereof.

4. The method of claim 1 , wherein the pharmaceutical composition has about 69% w/w to about 70% w/w PEG 400, about 15% w/w PEG 3350, and about 15% w/w PEG 1450.

5. The method of claim 2 , wherein the pharmaceutical composition has about 0.1% w/w BHT.

6. The method of claim 3 , wherein the pharmaceutical composition has about 0.2% w/w methyl paraben and about 0.02% w/w propyl paraben.

7. The method of claim 1 , wherein the pharmaceutical composition has about 0.01% w/w, about 0.025% w/w, about 0.05% w/w, about 0.1% w/w, about 0.15% w/w, or about 0.2% w/w isotretinoin.

8. A method of treating congenital ichthyosis in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition consisting of 0.01% w/w to 0.2% isotretinoin, 69% w/w to 70% w/w PEG 400, 14.78% PEG 3350, and 15% w/w PEG 1450, at least one preservative, and at least one antioxidant wherein the pharmaceutical composition has 0% w/w of ethanol and 0% w/w of water, and is formulated as a gel, ointment, lotion, emulsion or cream.

9. The method of claim 8 , wherein the at least one antioxidant is 0.1% w/w BHT.

10. The method of claim 8 , wherein the at least one preservative is 0.2% w/w methyl paraben and 0.02% w/w propyl paraben.

11. The method of claim 8 , wherein the pharmaceutical composition has 0.01% w/w, 0.025% w/w, 0.05% w/w, 0.1% w/w, 0.15% w/w, or 0.2% w/w isotretinoin.

12. The method of claim 1 , wherein the congenital ichthyosis is selected from the group consisting of Ichthyosis Vulgaris, X-linked Ichthyosis, Lamellar Ichthyosis, Congenital Ichthyosiform Erythroderma, Epidermolytic Ichthyosis, Erythrokeratodermia Variablis, Pachyonychia Congenital, Palmoplantar Keratodermas, Harlequin Type Ichthyosis, Refsum Disease, Conradi-Hunermann-Happle Syndrome, CHILD Syndrome, Ichthyosis En Confettis, Epidermolytic Nevus, Loricrin Keratoderma, Voihwinkel's Disease, and Sjógren-Larsson Syndrome.

13. The method of claim 1 , wherein the subject is human.

14. The method of claim 1 , wherein the congenital ichthyosis is X-linked Ichthyosis or Lamellar Ichthyosis.

15. The method of claim 8 , wherein the congenital ichthyosis is selected from the group consisting of Ichthyosis Vulgaris, X-linked Ichthyosis, Lamellar Ichthyosis, Congenital Ichthyosiform Erythroderma, Epidermolytic Ichthyosis, Erythrokeratodermia Variablis, Pachyonychia Congenital, Palmoplantar Keratodermas, Harlequin Type Ichthyosis, Refsum Disease, Conradi-Hunermann-Happle Syndrome, CHILD Syndrome, Ichthyosis En Confettis, Epidermolytic Nevus, Loricrin Keratoderma, Voihwinkel's Disease, and Sjogren-Larsson Syndrome.

16. The method of claim 8 , wherein the subject is human.

17. The method of claim 8 , wherein the congenital ichthyosis is X-linked Ichthyosis or Lamellar Ichthyosis.

Assignments (11)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2024
From: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS, LLC; BIOPHARMX, INC.
To: LEO PHARMA A/S
Reel/Frame 066782/0409 →
RELEASE OF SECURITY INTEREST Recorded Jan 23, 2024
From: LEO US HOLDING, INC.
To: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
Reel/Frame 066216/0835 →
RELEASE OF SECURITY INTEREST Recorded Jan 23, 2024
From: LEO US HOLDING, INC.
To: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
Reel/Frame 066216/0619 →
SECURITY INTEREST Recorded Nov 29, 2023
From: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
To: LEO US HOLDING, INC.
Reel/Frame 065702/0064 →
SECURITY INTEREST Recorded Aug 31, 2023
From: TIMBER PHARMACEUTICALS, INC.; TIMBER PHARMACEUTICALS LLC
To: LEO US HOLDING, INC.
Reel/Frame 064766/0151 →
RELEASE OF SECURITY INTEREST Recorded Aug 23, 2023
From: TIMBER PHARMACEUTICALS LLC
To: PATAGONIA PHARMACEUTICALS LLC
Reel/Frame 064682/0001 →
CORRECTIVE ASSIGNMENT TO CORRECT THE FIRST PAGE OF THE UCC FINANCING STATMENT TO NAME PATAGONIA PHARMACEUTICALS LLC AS THE SECURED PARTY PREVIOUSLY RECORDED AT REEL: 060624 FRAME: 0380. ASSIGNOR(S) HEREBY CONFIRMS THE SECURITY INTEREST . Recorded Jul 29, 2022
From: TIMBER PHARMACEUTICALS LLC
To: PATAGONIA PHARMACEUTICALS LLC
Reel/Frame 060978/0984 →
SECURITY INTEREST Recorded Jul 26, 2022
From: TIMBER PHARMACEUTICALS LLC
To: PATAGONIA PHARMACEUTICALS LLC
Reel/Frame 060624/0380 →
CHANGE OF ADDRESS FOR ASSIGNEE Recorded Feb 14, 2022
From: TIMBER PHARMACEUTICALS LLC
To: TIMBER PHARMACEUTICALS LLC
Reel/Frame 059086/0384 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2020
From: ROME, ZACHARY; EVANS, CHARLES RODNEY GREENAWAY; BROWN, PHD., MARC BARRY; CASERTA, FRANCESCO, DR.
To: PATAGONIA PHARMACEUTICALS, LLC
Reel/Frame 052723/0520 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2020
From: PATAGONIA PHARMACEUTICALS, LLC
To: TIMBER PHARMACEUTICALS LLC
Reel/Frame 052723/0668 →
Continuity (4)
Division 15772456
Provisional Application 62301759 · Mar 1, 2016
Provisional Application 62248760 · Oct 30, 2015
Related Publication 20200297627A1 · Sep 24, 2020