Completed Projects

HOME > R&D Pipeline > Current status > Completed Projects

KDDF-201509-06 A study on long-term in vivo efficacy and toxicity of KDS2010, a novel inhibitor of aberrant GABA synthesis(CNS Diseases, Chemical) [01.25.2016]

PRINT

Development and Market Objectives

We found that reactive astrocytes aberrantly and abundantly produce the inhibitory transmitter GABA by over-expressed monoamine oxidase-B (MAO-B) in Alzheimer’s disease (AD). Based on this novel target, we developed a lead compound, KDS2010, which showed potent and selective inhibitor of aberrant GABA synthesis and excellent drug-like properties in ADME/Tox. Thus we plan to evaluate KDS2010 for a pre-clinical candidate, which will serve as an effective treatment for memory impairment in Alzheimer’s disease by targeting aberrant GABA synthesis in reactive astrocytes.

Unmet Medical Need & Target Patients

Drug candidate: Inhibitor of aberrant GABA synthesis in reactive astrocytes for treatment of memory impairment in AD
Target Patients: Alzheimer’s disease (MCI to mild)
Unmet Medical Need: There are major two categories for AD therapy. However, the existing AD therapies are only effective temporarily. Novel treatments with a long-term effectiveness are needed for the improvement of memory impairment in AD.
-ChEIs [acetylcholine esterase inhibitors: (Aricept®, donepezil), (Exelon®, rivastigmine),  (Razadyne®, galantmine)]
-NMDA antagonist: (Namenda®, memantine)

 

Status

The safety evaluation of the candidate is ongoing including off-target selectivity test with ~100 CNS receptors and 2 weeks repeated toxicity test with rat.

The long-term effectiveness is being evaluated with low dose of the candidate in APP/PS1 mouse model.

Intellectual Property

-Patent application: Korea & PCT
-Preparation of patent application: end of 2016, (USA, EU, China etc)
 

Competitive Advantages

-A novel therapeutic strategy to address the disease-modifying therapy in AD through inhibition of aberrant GABA synthesis in reactive astrocytes.
-The candidate can be expanded for other disease indications by targeting aberrant GABA synthesis in reactive astrocytes.
 

Indication

CNS disease (Alzhemer’s disease )

Research Period

Dec. 15, 2015 - Dec. 14, 2016

Company

Korea Institute of Science and Technology

Developmental Stage

Lead optimization

Additional Information

Contact Information

Contact
Address Company Name: Korea Institute of Science and Technology
WebSite Homepage: http://www.kist.re.kr Contact Person: Dr. Ki Duk Park
E-mail: kdpark@kist.re.kr Contact: +82-2-958-5132

Related Projects

Related Project
list
Update to 2013 © KOREA DRUG DEVELOPMENT FUND. ALL RIGHTS RESERVED. QR Code