Treatment of ocular hypertension - Dual Targeting in a New Class of Anti-Glaucoma Agents

Ref.-Nr. 6789

Keywords: increased intraocular pressure (IOP); glaucoma, oxidative stress, H3R antagonist, carbonic anhydrase inhibitor, carbonic anhydrase (CA), CAI, CAXI, dual H3R antagonist and CA inhibitor, ophthalmic agent

Increased intraocular pressure (IOP), also known as ocular hypertension, is widely associated with open-angle and narrow-angle glaucoma. These servere eye diseases may lead to blindness. Current therapeutic approaches use carbonic anhydrase inhibitors (CA Inhibitors), beta blockers, alpha2-receptor agonists, prostaglandins and cholinergics. It was recently found that histamine H3-receptor (H3R) antagonists  also exhibit a specific mode of action for the efficient reduction of IOP. However, all treatments have the common disadvantage that only one active compound has to be selected. In addition, the IOP is caused by various factors that should ideally be addressed simultaneously.

The invention addresses these disadvantages. Novel compounds based on a combination of classical pharmacophore modes of action are provided whereby the compounds exhibit inhibitory effects atf H3R  and at CA both in the nanomolar concentration range. This combination as a newly-synthezised single compound with two simultaneous modes of action has the advantages of uniform pharmacokinetics and improves the ways of application due to their physicochemical properties. Through the simultaneous attack of two target structures, broader applications, longer duration and thereby improved effects can be realized as new therapeutic principle.

Vorteile

  • Innovative combination of a histamine H3R-Antagonist and a Carboanhydrase Inhibitor into one agent with two different targets and modes of action
  • Promising therapeutic potential for IOP treatment by a dual mode of action
  • Exploitation of two known and approved active compounds in one compound.

Kommerzielle Anwendung

A European Patent Application has been filed on February 23rd, 2024. On behalf of the Heinrich Heine University Düsseldorf, PROvendis offers an access to rights for method development and commercial use of this invention.

Technologie-Reifegrad

1 2 3 4 5 6 7 8 9
Nachweis der Funktionstüchtigkeit

Relevante Veröffentlichungen

In vitro data as well as data on mice models have been generated, but have not been published yet.

An invention from Heinrich Heine University Düsseldorf.

Dr. Wolfram Schleich

ws@provendis.info
+49 208 9410535