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Adenosine a3 receptor agonists for the treatment of dry eye disorders

An adenosine receptor and agonist technology, applied in the field of compounds for the treatment of dry eye, can solve problems that cannot be prevented or reversed

Inactive Publication Date: 2009-02-11
CAN-FITE BIOPHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These solutions and ointments give some temporary relief, but do little to prevent or reverse any of the damage

Method used

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  • Adenosine a3 receptor agonists for the treatment of dry eye disorders
  • Adenosine a3 receptor agonists for the treatment of dry eye disorders
  • Adenosine a3 receptor agonists for the treatment of dry eye disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0152] IB-MECA improves dry eye symptoms in rheumatoid arthritis patients

[0153] drug:

[0154] A used 3 AR agonists are clinical grade compounds traditionally known as 1-deoxy-1-[6-[[(3-iodophenyl)methyl]amino]-9H-purin-9-yl]-N-methyl -D-Ribofuranamide or N 6 -(3-iodophenyl)-adenosine-5′-N-methyluronic acid amide (IB-MECA), which was synthesized by Can-Fite BioPharma in accordance with Albany Molecular ResearchInc, Albany, NY, USA Good Clinical Practice (GMP).

[0155] IB-MECA is formulated as oval-shaped softgel capsules. The capsules contain a solution of IB-MECA in CremophorRH 40 and Miglyol 812. The capsules contain 0.1, 1 or 4 mg doses of IB-MECA, the exact composition of each capsule type is shown in Tables 1-3 below:

[0156] Table 1: Composition of 0.1 mg IB-MECA Softgel Capsules

[0157] Element capsule %W / W IB-MECA 0.105mg 0.021 Polyoxyl 45 castor oil,

USP (Cremophor RH 40) 326.495mg

65.299

Miglyol 812 173.400mg...

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Abstract

The present invention concerns methods and compositions for treating dry eye. The method comprises providing an individual exhibiting ophthalmologic clinical symptoms and signs of dry eye with an A3 adenosine receptor (A3AR) agonist. The A3AR agonist is preferably administered to the subject either topically or orally.

Description

field of invention [0001] The present invention relates to compounds and methods for the treatment of dry eye. Background of the invention [0002] The tear film at the front of the eye plays an important role in maintaining the integrity of the cornea, protecting it from infection and preserving visual acuity. These functions are critically dependent on the stability, elasticity and / or composition of the tear film structure. Alternatively, lack or loss of the tear film may lead to undesired drying of the corneal epithelium, corneal ulceration and perforation, increased incidence of infectious disease, and ultimately severe visual impairment and blindness. [0003] Dry eye disease is often referred to as a syndrome or disease; it is known by many other terms. Keratoconjunctivitis sicca (KCS), or more commonly keratitis sicca, can involve some degree of dryness in any eye. [0004] In dry eye, the eye becomes dry due to an abnormally high rate of evaporation of tears or du...

Claims

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Application Information

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IPC IPC(8): A61K31/00A61K31/7076A61P27/02
CPCA61K31/00A61K31/7076A61P27/02A61P27/04A61P43/00
Inventor P·菲什曼T·瑞特布莱特
Owner CAN-FITE BIOPHARMA LTD
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