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KDDF-201306-01 Development of a Ras degrading small molecule, through modulation of Wnt/β-catenin signaling, for treatment of colorectal cancer(Oncology, Chemical) [10.07.2013]

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Development and Market Objectives

Our goal is to develop novel anti-cancer drug, suppressing cancer related multiple signaling pathways (Ras-ERK, PI3K/mTOR, Wnt/β-catenin pathways) via degradation of Ras through Wnt/β-catenin signaling, which could overcome current limitations of the receptor tyrosine kinase targeted therapies, attributed by Ras mutation.

Unmet Medical Need & Target Patients

Colorectal cancer is the 3rd most incident cancer world-wide (Jemal et al., 2009), its incidence rate is increasing rapidly (annually 16%). Current targeted therapies are only allowed to be used on K-ras wildtype patients, hence there is significant need for drugs acting on K-ras mutant patients. 

Status

Proof-of-principle has been demonstrated with intra peritoneal administration of lead compound, KY1797 in mouse model with APC and Ras mutation, Apcmin/+/K-RasG12DLA2. Tumor growth was inhibited and the incidence of tumorigenesis was significantly lowered in the drug treated group of mouse.
KY1797 has just entered early optimization phase. Current data show that the lead compound does not show any significant toxic effect in normal cells, but only in tumor cells.

Intellectual Property

Patent applications for compounds in development are pending.

Competitive Advantages

The competitive feature of KY1797 is its efficacy on Ras mutant colorectal cancer cells. So far, there is no known drug to be active in K-Ras mutant cancer, thus having this anti-cancer effect on K-ras mutant cells gives KY1797 a competitive edge.
KY1797 demonstrate anti-cancer effect on K-Ras mutant cells by degrading Ras protein, and also by degrading β-catenin, which is known to be a key factor in colorectal cancer development. This unique feature of degrading both β-catenin and Ras is potentially first-in-class mechanism of action.

Indication

colorectal cancer

Research Period

Sep. 01, 2013~Feb. 28, 2015

Company

Handok

Developmental Stage

drug candidate

Additional Information

Contact Information

Contact
Address Company Name: Handok Inc.
WebSite Homepage: http://www.handok.co.kr/english/ Contact Person: Dooseop Kim
E-mail: dooseop.kim@handok.com Contact: +82-31-628-0390

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