Completed Projects

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

KDDF-201504-01 Tankyrase inhibitors as anti-cancer therapeutic reagents(Oncology, Chemical) [10.05.2015]


Development and Market Objectives

Almost 80% of colorectal cancers (CRC) are driven by aberrantly-activated Wnt signaling, mainly through APC mutations. The activation of the Wnt pathway allows ?-catenin levels to increase, leading to the expression of multiple tumorigenic gene products. The enzyme, tankyrase parsylates Axin which leads to dissociation of the “destruction complex” (APC, Axin, GSK3?, and CK1?), resulting in the increase of ?-catenin levels. Blocking of enzyme activity of the tankyrase will restore the destruction complex and maintain homeostasis of the level of ?-catenin. 

The project goal is to identify selective Tankyrase 1&2 inhibitors that are suitable for oral administration (once daily) and to profile for tumor growth inhibition in a variety of models of colorectal and breast cancers.

Unmet Medical Need & Target Patients

According to the worldwide statistics, colorectal cancer is the 3rd most common cancer in men and the 2nd in women, and 1.2 million incidences and 609,000 mortalities by the CRC were reported in 2010. The incidence rates in several Asian and Eastern European countries are still increasing. The sales amount of colorectal cancer therapeutics reached $2.5 billion in seven global markets (US, Japan, France, Germany, Italy, Spain, UK) in 2012.

While Erbitux (Cetuximab) is well-known anti-cancer therapeutics for colorectal cancers, its application is limited to the patients with wild-type KRas and there are no remarkable medicines developed for the patients with mutant KRas, approximately 40% of the total CRC patient population.

ST Pharm’s STP06-1002 aims to target the patient population with mutant KRas (750,000 patients in 2014) and also the Erbitux non-responders (210,000 patients in 2014) with strong predictive biomarker strategies. 


(1) On-going studies 
Pre-formulation study, process development and manufacture 
Pharmacokinetics study 
Preclinical toxicology study (non-GLP toxicity in rodent and non-rodent) 
In vivo efficacy study (pharmacodynamics)

(2) Existing study results   
Excellent in vitro potency and PARP selectivity 
Excellent stability (xML, plasma, CYPs)
Good solubility (FaSSGF, FaSSIF, FeSSIF)
No toxicity issues observed (hERG, cytotoxicity, Ames)
Excellent PK profiles in mouse & rat
PD POC in Xenograft DLD-1 model study
No abnormalities detected in vivo toxicity study and ileum histology
No toxicity issues in single acute, 10-day DRF, and Toxicokinetic studies
No activity in pan-kinase and off-target binding assay 

Intellectual Property

Strong IP positions

Competitive Advantages

(1) Competitiveness of STP06-1002 
STP06-1002 is a small molecule tankyrase inhibitor targeting CRC with novel MOA and has been developed as first-in-class anti-cancer therapeutics with predictive biomarker strategies.  

(2) Internal capability of ST Pharm
ST Pharm is a “Top-Tier GMP Chemical Service Provider” with outstanding cGMP compliance based on ICH Q7. 
ST Pharm has been audited by numerous domestic and foreign regulatory agencies (MFDS, US FDA, EDQM, PMDA, TGA, and etc.) and approved successfully its cGMP quality system. The non-and clinical-samples will be manufactured using the internal capacities.

(3) Business development strategy  
ST Pharm maintains long-term relationships with lots of global pharmaceuticals and biotechs from discovery to commercial stage. 
A broad range of collaborations by virtual R&D strategy is being developed to facilitate the new drug development process in an efficient and effective manner.


Colorectal Cancer

Research Period

Sep, 2015 ~ July, 2016


ST Pharm

Developmental Stage


Additional Information

Contact Information

Address Company Name: ST Pharm Co., Ltd.
WebSite Homepage: Contact Person: Jin Ha Hwang
E-mail: Contact: +82-31-488-1415

Related Projects

Related Project