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KDDF-201609-12 Drug repositioning of dipeptidyl peptidase (DPP)-4 inhibitor for treatment of calcific aortic valve disease(Cardiovascular Diseases, Chemical) [2019-01-30]

Ongoing Project
Section Lead
Preclinical Phase I Phase II Phase III

Development and Market Objectives

The purpose of this study is to determine whether DPP-4 can be key target molecules associated with progression of calcific aortic valve disease (CAVD). Specifically, a major focus of this study is to confirm possibility and feasibility of drug repositioning of DPP-4 inhibitor for an effective treatment option for patients with mild to moderate CAVD.

Unmet Medical Need & Target Patients

CAVD is a chronic degenerative cardiac disease characterized by progressive valvular fibrosis and calcification. Despite marked increase in the prevalence of CAVD in the aging society, there is no effective pharmacological treatment to prevent progression of this disease.


To select a candidate of DPP-4 inhibitor for clinical trials and IND approve, we plan the tissue distribution study using SD male rats to compare tissue plasma ratio in heart (H/P ratio) among the various commercialized DPP-4 inhibitors. Also, we compare in vitro efficacy of DPP-4 inhibitors on valvular calcification and by use of eNOS knock out mouse as an animal model of CAVD to compare in vivo efficacy to prevent calcification using Osteosense imaging. At the same time, we perform retrospective multi-center cohort study for the proof of concept (POC) determining of DPP-4 inhibitor efficacy in patients with CAVD. We analyze serial echocardiographic follow-up data of patients with CAVD and diabetes mellitus with or without DPP-4 inhibitors.

Intellectual Property

We successfully obtained an United States patent which is titled as “Composition for prophylaxis or treatment of vascular or cardiac valvular calcification comprising dipeptidyl peptidase-4 inhibitor” on Aug 16, 2016. This application claims the benefit of Korean Patent Applicaion No. 10-2013-0103189 filed on Aug 29, 2013, with the Korean Intellectual Property Office. An aspect of the present disclosure may provide a pharmaceutical composition for prophylaxis or treatment of vascular or valvular calcification including a DPP-4 inhibitor.

Competitive Advantages

If this study provides positive supporting data for successful drug repositioning of DPP-4 inhibitors for prevention of CAVD progression, it will ultimately change the current paradigm of the management guideline and will contribute to decrease the extra-cost and risks associated with an invasive and expensive valve replacement procedure either through open heart surgery or percutaneous technique.

Contact & Company Overview

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