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KDDF-201404-06 (Metabolic Disorders, Chemical) [08.05.2014]


Development and Market Objectives

The objective is to extract and optimize a lead compound that can accelerate osteogenesis by stimulating Wnt signal transmission in weakened and compromised bone as a new developmental concept. We aim to identify a small molecule or PPI which can selectively target sclerostin, a known endogenous Wnt signal transmission inhibitor, to promote LRP5/6 activity. 

Unmet Medical Need & Target Patients

Target patient group:
1) Osteoporosis patients:
a) Postmenopausal osteoporosis
- Patients aged over 65 with loss of cortical bone density, increased porosity and patients with multiple fractures
- Patients who do not respond to bisphosphonate treatment and those on drug holiday
b) Goal direct Rx, initial treatment
A new treatment strategy that dramatically increases bone density and decreases the risk of fracture at the initial stages, and maintains existing bone resorption suppressants; could be used as an initial stage medicine.
c) Osteoporosis, post steroid treatment
Sclerostin levels are high in patients on long-term steroid treatment.
d) Osteoporosis in males
e) Osteoporosis with diabetes
Sclerostin levels are increased in patients with diabetes.
f) Osteoporosis caused by limb movement disorders such as hemiplegia
Sclerostin is increased in all patients with immobilization.
2) Fractures: Can be used for rapid recovery.
3) Chronic periodontal diseases: No specialized medicines exist for periodontal diseases at present.
4) Osteogenesis imperfect: Rare disease.
Unmet medical needs:
A. Bisphosphonate is a typical bone resorption suppressant but causes severe side effects such as BRONJ and atypical femoral fractures, and thereby treatment is limited (3~5 years).
B. Inadequate efficacy of SERM limits its effective treatment for fractures.
C. Available bone resorption suppressants have already saturated the market to an extent that the development of new candidates is relatively insignificant. 
Available bone resorption suppressants: Bisphosphonates, SERMs, Denosumab (RANKL inhibitor), and Odanakatib (Cathepsin K inhibitor).
D. Treating all patients with a single medicine is impossible for chronic diseases like osteoporosis.
E. The biggest limitation for existing osteoporosis medicines is the lack of effective promoters of bone formation. Therefore, such “Goal Direct Treatment” is impossible.     
F.  Deficiency of medicines targeting cortical bones.
After the age of 65, cortical bone loss becomes most significant, and trabecularization of cortical bone becomes an issue.  


Hit compounds are currently being identified and a lead substance is to be selected by Milestone 1 and will be optimized for Milestone 2. 

Intellectual Property

Registration of a patent is scheduled after identifying a lead substance.

Competitive Advantages

  Advantages Disadvantages Remarks
Bisphosphonate Low cost
Proven efficacy
Serious side effects
(BRONZ and atypical femoral fracture).
Stoppage after 3-5 years use (drug holiday)
Bone resorption inhibitor
Denosumab Strong inhibition of bone resorption
Continuous increase in bone density
Injected, expensive
Side effects such as BRONZ
Bone resorption inhibitor
Expected 2015 domestic
Odanacatib Bone resorption inhibition
No inhibition of bone formation
Increased incidence of skin adverse events, infections and cancer Bone resorption inhibitor
Expected 2016 domestic
PTH & Biased PTH (BA058 Osteogenesis promoter
Trabecular bone
Endocortical bone
Treatment up to two years
Bone-cancer risk
Narrow therapeutic window
Injected, expensive
Endocortical porosity increases
Osteogenesis promoter
- On the market (PTH)
- Phase 3 (BA058)
Sclerostin Monoclonal Ab Osteogenesis promoter
Cortical bone
Trabecular bone
Cortical porosity reduction
2nd Ab generation
Injected (monthly)
No fracture data
Osteogenesis promoter
Phase 3 started
Sclerostin Inhibitor OGX5-28 (small molecule Osteogenesis promoter (predicted)
Can be administered orally
Lead substance
No published data
Osteogenesis promoter
In development


Metabolic Disorders (Osteoporosis )

Research Period

Jul. 15, 2014 - Jan. 14, 2016


Yonsei University     

Developmental Stage

Lead Generation

Additional Information

Contact Information

Address Company Name: School of Medicine, Yonsei University
WebSite Homepage: Contact Person: Im Seung-Kil
E-mail: Contact: +82-2-2228-1948

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