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KDDF-201603-01 Development of drug candidate as a G-protein coupled receptor kinase 5 inhibitor(Cardiovascular Diseases, Chemical) [08.16.2016]

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Development and Market Objectives

The aim of the present project is to develop the global new drug candidates for the treatment of chronic heart failure through the inhibition of G-protein coupled receptor kinase 5 (GRK5) and to verify IND profiling of drug candidates.

 

Unmet Medical Need & Target Patients

Target Patients:

Patients with heart failure who have low normal blood pressure

 

Unmet Medical Need:

Heart failure is a leading cause of morbidity and mortality worldwide. Despite significant advances in therapy, there is still a major unmet need (52%) because of limitation of currently available palliative treatments by an increase in adverse events, including an undesirable reduction in blood pressure. Especially, between 15% and 25% of patients with chronic heart failure have low systolic blood pressure, and are at higher risk of mortality and morbidity. Therefore, development of mechanism based and blood pressure-neutral therapeutic options are urgently required.

Status

- We identified several hit/lead compounds with high activity and selectivity for GRK5.

- The hit/lead compounds have shown significant efficacy in cellular hypertrophy and animal models of heart failure.

- Experiments are in progress to improve permeability, in vivo PK and to optimize hit/lead compound through structure-activity relationship (SAR) studies.

 

Intellectual Property

- Patents are under preparation.

 

Competitive Advantages

- The hit/lead compounds have a novel chemical structure and unique mechanism of action.

- ‘First-in-class’ drug with potent GRK5 inhibitory effects could overcome the limitations of use of currently available agents and provide incremental benefit to treat chronic heart failure.

- The hit/lead compounds exhibited outstanding in vitro/in vivo efficacies in heart failure models without a lowering effect of systolic blood pressure.

- The combination therapy with currently available drugs in clinics could synergistically enhance their therapeutic potential.

 

Indication

Heart Failure

Research Period

Aug. 1, 2016 ~ May. 31, 2018

Company

Korea Research Institute of Chemical Technology

Developmental Stage

Optimization

Additional Information

Contact Information

Contact
Address Company Name: Korea Research Institute of Chemical Technology
WebSite Homepage: http://www.krict.re.kr Contact Person: Byung Ho Lee
E-mail: bhlee@krict.re.kr Contact: 82-42-860-7415

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