IP Library Granted Patent US 12,285,404
Granted Patent B2
US 12,285,404 · App. 17/834,626 · Granted Apr 29, 2025

Prevention of rosacea inflammation

Inventors: Richard L. Gallo (San Diego, CA); Anna Di Nardo (La Jolla, CA); Yumiko Muto (La Jolla, CA)
Assignee: The Regents of the University of California
A61K31/352A61K9/0014A61K31/277A61K31/4741A61K31/519A61K45/06
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Quick Facts
Patent No.
US 12,285,404
App. No.
17/834,626
Granted
Apr 29, 2025
Kind
B2
Abstract

The disclosure demonstrates the role of mast cell stabilizers in treating rosacea. The disclosure also shows the role of mast cells, cathelicidin, serine protease and/or vitamin D3 in rosacea pathology and the use of antagonists and inhibitors thereof to treat rosacea.

Claims (12)

1. A composition, comprising:

a mast cell stabilizer selected from the group consisting of lodoxamide, nedocromil, cromolyn, pemirolast, pharmaceutical salts thereof, and any combination thereof;

a serine protease inhibitor selected from the group consisting of Cystatin, aprotinin, 4-(2-aminoethyl)-benzenesulfonylfluoride, aminocaproic acid, kunitz-type protease inhibitor, amyloid beta protein precursor, TFPI (Tissue Factor Pathway Inhibitor), collagen alpha 3, collagen alpha 3 (VI) chain precursor, HKIB9 (Human Kunitz-type Inhibitor type 9), ITI-KD1 (Inter-Trypsin Inhibitor, Kunitz Domain 1), ITI-KD2 (Inter-Trypsin Inhibitor, Kunitz Domain 2), Beta-1-Bungarotoxin B chain, snake venom protease inhibitors, and any combination thereof; and

an agent that inhibits a neuropeptide selected from the group consisting of substance P (SP), calcitonin gene-related peptide (CGRP), vasoactive intestinal peptide (VIP), neurokinin A (NKA), pituitary adenylate cyclase-activating peptide (PACAP), and any combination thereof.

2. The composition of claim 1 , wherein the composition further comprises a vitamin D receptor inhibitor, wherein the vitamin D receptor inhibitor comprises a small molecule, a soluble vitamin D receptor polypeptide, or any combination thereof.

3. The composition of claim 2 , wherein the vitamin D receptor inhibitor comprises 6-fluoro-vitamin D3 (6-F-D3).

4. The composition of claim 1 , wherein the composition is formulated for topical administration.

5. The composition of claim 4 , wherein the composition comprises a sugar, polysaccharide, sugar alcohol or an oil.

6. The composition of claim 5 , wherein the sugar, polysaccharide, sugar alcohol, or oil comprises one or more of lactose, 1,2-propylene glycol, a polygycol, a fatty alcohol, dextrose, glucose, glycogen, a glycolipid, glycerin, tocopheryl glucoside, inositol, lactitol, maltitol, maltose, mannitol, mannose, methoxy polyethylene glycol, polyglyceryl sorbitol, sorbitol, sucrose, vegetable oil, ethyl oleate, jojoba oil, avocado oil, sunflower seed oil, lanosterol, linoleic acid, linolenic acid, a phytosterol, a placental lipid, Vitis vinifera seed oil, a sphingolipid, stearamidopropylbetaine, stearyl palmitate, tocopherol, tocopheryl acetate, tocopheryl linoleate, mineral oil, petrolatum, acetylated lanolin, apricot kernel oil, butoxyethyl stearate, ethylhexyl myristate, glyceryl isostearates, glyceryl oleate, hexyldecyl stearate, hexyl isostearate, hydrogenated palm glycerides, hydrogenated soy glycerides, hydrogenated tallow glycerides, isostearyl neopentanoate, isostearyl palmitate, isotridecyl isononanoate, laureth-2 acetate, lauryl polyglyceryl-6 cetearyl glycol ether, methyl gluceth-20 benzoate, mineral oil, myreth-3 palmitate, octyldecanol, octyldodecanol, odontella aurita oil, 2-oleamido-1,3 octadecanediol, polyethylene glycol castor oil, palm oil, coconut oil, beeswax, corn oil, sodium caproyl lactylate, sodium caprylate, sodium cocoate, sodium isostearate, sodium tocopheryl phosphate, steareths, ceramides, ceteareth-7, cetyl alcohol, glyceryl isostearate, propylene glycol, silicon oil, or trideceths or any combination thereof.

7. The composition of claim 4 , wherein the composition is formulated in petrolatum, sorbitol, and/or propylene glycol.

8. The composition of claim 1 , wherein the composition comprises a skin lightening agent, a sunscreen agent, a skin conditioning agent, a skin protectant, an emollient, a humectant, or any combination thereof.

9. The composition of claim 1 , wherein the composition further comprises a matrix metalloproteinase inhibitor.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 7, 2024
From: GALLO, RICHARD; DI NARDO, ANNA; MUTO, YUMIKO
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 067333/0863 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2023
From: GALLO, RICHARD L.; DI NARDO, ANNA; MUTO, YUMIKO
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 065562/0611 →
Continuity (5)
Continuation 16576730 · Sep 19, 2019
Division 15726069 · Oct 5, 2017
Division 14774892
Provisional Application 61780758 · Mar 13, 2013
Related Publication 20230181518A1 · Jun 15, 2023
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