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Novel emulsion-based formulation of the anti-glaucoma MSH-1001 for improved…

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
Program Year/Program:
2011 / SBIR
Agency Tracking Number:
R43EY021074
Solicitation Year:
2011
Solicitation Topic Code:
NEI
Solicitation Number:
PA10-050
Small Business Information
CHARLESSON, LLP
800 Research Parkway OKLAHOMA CITY, OK 73104
View profile »
Woman-Owned: Yes
Minority-Owned: Yes
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2011
Title: Novel emulsion-based formulation of the anti-glaucoma MSH-1001 for improved topic
Agency: HHS
Contract: 1R43EY021074-01A1
Award Amount: $287,947.00
 

Abstract:

DESCRIPTION (provided by applicant): This Small Business Innovation project aims to develop an innovative eye drop formulation for the treatment of glaucoma and ocular hypertension. Charlesson has acquired from Danube Pharmaceuticals MSH-1001, a new smallmolecule compound (previously known as DNB-001 or KR- 31378). MSH-1001 is has both ocular hypotensive and neuroprotectant properties. It is an ATP- sensitive K channel opener. The goal of this project is to demonstrate that an emulsion based eye drop can deliver therapeutic levels of MSH-100, to the aqueous humor with the long term goal (Phase 2) of reducing intraocular pressure in an appropriate animal model of ocular hypertension and conducting the IND-enabling studies supporting a first-on-man study. Thegoal of this proposal is to 1) Make three different types of emulsion based eye drops that can incorporate MSH-1001. 2) Take the three most promising emulsions that meet all of our criteria (i.e. the desired osmolality, pH, viscosity and droplet size) andtest them in-vivo for ocular tolerance and histology in Dutch Belted rabbits. Ocular pharmacokinetic properties of the tolerated formulations will be compared to the pharmacologically active experimental suspension. Eyedrops (one drop of 40 5L/eye) will be administered to Dutch Belted rabbits. At different time points (0.25, 0.5, 1, 2, 4, and 8hrs), eyes will be enucleated following euthanasia. Aqueous humor will then carefully be dissected and The MSH- 1001 quantified by LC-MS. The successful ophthalmic emulsion will show ocular distribution at least equal or superior to the experimental suspension. PUBLIC HEALTH RELEVANCE: Glaucoma is primarily treated by administering drugs to decrease intraocular pressure (IOP). Prostaglandins are commonly used to lower IOP by increasing the uveoscleral outflow as first-line therapy. Despite their robust efficacy, many patients often require multiple medications, or glaucoma surgery in the cases refractory to pharmacological treatments, to achieve target pressurecontrol. There is a highly need to develop novel potent IOP lowering drugs so that ophthalmologists can more effectively achieve a better control of the target pressure in those patients. Research has been focused on identifying novel molecular targets with the potential to better the current therapies as a stand-alone or an adjunct to the first-line prostaglandin. The goal of this proposal is to develop a clinical ophthalmic emulsion of MSH-1001, a novel small molecule that effectively lowers IOP by enhancing the trabecular outflow through a novel mechanism of action,. .

Principal Investigator:

Ronald A. Wassel
405-271-2552
dwassel@charlessonllc.com

Business Contact:

Ronald Wassel
405-271-2552
dwassel@charlessonllc.com
Small Business Information at Submission:

CHARLESSON, LLP
800 Research Parkway OKLAHOMA CITY, OK -

EIN/Tax ID: 120008884
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No