Completed Projects

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

KDDF-201402-12 YKP10811, A Drug for Functional Gastrointestinal Disorder : Global Clinical Phase 2b Development(Gastrointestinal Diseases, Chemical) [06.02.2014]

PRINT

Development and Market Objectives

SK Biopharmaceuticals Co., Ltd. has developed a partial agonist for the 5-HT4 receptor and completed extensive preclinical efficacy tests for chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). Phase I clinical trials have verified its excellent safety and tolerability. Phase IIa clinical trial have focused on its ability to improve motility in the upper and lower gastrointestinal tract in patients with CIC, and further confirmed its efficacy and safety. On the basis of these results, phase IIb clinical trial is currently in progress to determine the optimal dosage.

A technology transfer agreement is currently planned, by entering into a partnership with a multinational corporation or a professional pharmaceutical company specializing in gastroenterology at the completion of phase IIb trial, so that the candidate can enter the market with maximal sales potential.

Unmet Medical Need & Target Patients

● Unmet medical needs
Propulsid (cisapride) and Zelnorm (tegaserod), accelerate gastrointestinal motility and received considerable attention when first marketed. However, due to issues with potential side effects on the cardiovascular system, they were withdrawn in 2001 and 2007, respectively. Unmet medical needs then increased for IBS-C, CIC and gastroparesis. Existing laxatives, bulk agents and stool softeners retain many issues including lack of potency, potential side effects and a lack of long-term efficacy. Recently launched secretogogues(Amitiza/Linzess)) have made some progress in the CIC field by increasing moisture content in the colon, but disadvantages include lack of efficacy for an approximate 20% of patients with very slow intestinal movement, or no improvement in upper bowel movement and questionable efficacy for reducing pain in patients with CIC. Therefore, new therapeutic options that will provide significant and effective improvement in both upper/lower gastrointestinal motility, less side effects, and long term efficacy is strongly needed. 

● Target patient group
The target patient groups for YKP-10811 are CIC and IBS-c patients. In regards to CIC, there are currently 92 million patients in the world’s 7 major markets, including the USA, which includes approximately 14% of the adult population. For IBS-c, approximately 15% of the adult population suffer from IBS-C.

Status

The development of a prokinetic drug is currently in progress to optimize a selective partial agonist of the 5-HT4 receptor which can address the unmet medical needs described above.
Through various preclinical tests, its efficacy has been verified with extensive and strong improvements in upper/lower gastrointestinal motility and lasting effects during long term treatment. Phase I trials verified its excellent in pharmacodynamic properties, favorable side effects, and its tolerability safety margin is at least 50 times higher than its effective dose range.

A phase IIa trial (http://www.clinicaltrial.gov/, NCT01523184) verified its efficacy in human, while safety parameters were confirmed for long-term treatment via preclinical long-term toxicity tests (six months in rats, six and nine months in dogs). 

Currently, a phase IIb trial is underway (http://www.clinicaltrial.gov/, NCT01989234) to determine the optimal dosage, in addition to carcinogenicity testing as mandatory requirements for approval. Phase II trials are also in progress for Korean patients with IBS-c through a domestic technology transfer agreement with SK Chemical Co., Ltd. (http://www.clinicaltrial.gov/, NCT02082457). Business development is in progress to seek a global technology transfer agreement at the completion of the phase IIb trials.

Intellectual Property

A. Current patent status: International patents applied for in 2008
B.  Patent coverage: substance patent including YKP10811

Competitive Advantages

A. Superior efficacy compared to existing medications
YKP10811 exhibits a superior effect in animal models compared to existing medications such as tegaserod and prucalopride, suggesting the potential for strong efficacy in clinical trials. 

B. Possibility of indication expansion
(1)  Potential extensive efficacy in the entire gastrointestinal tract
Animal model tests and phase IIa results show that YKP10811 accelerates motility throughout the upper and lower gastrointestinal tracks. This underlines the potential for an expansion of indications to other disorders such as functional dyspepsia or gastroparesis. 
(2) Reduction of abdominal pain
YKP10811 exhibits efficacy in an abdominal pain model, and is therefore expected to be efficacious for IBS-c, to be verified in clinical trials conducted by SK Chemical Co., Ltd. 
(3) Safety
In comparison to existing drugs with identical mechanism of action including cisapride, YKP10811 exhibits high selectivity in terms of hERG and its QTc risk is very low. In addition, compared to tegaserod, it does not act on other subtype serotonin receptors (5-HT1B/1D, etc.) implying that the risk of cardiovascular ischemia would be relatively low.
(4) Long-term efficacy
Unlike existing 5-HT4 agonists in which efficacy is disappeared if treated for long-term, YKP-10811 has been confirmed to have long-term efficacy in animal models of abdominal pain.

Indication

Gastrointestinal Disease

Research Period

Apr. 28, 2014 ~ Jun. 30, 2015

Company

SK Biopharmaceuticals

Developmental Stage

Phase IIb

Additional Information

Contact Information

Contact
Address Company Name: SK biopharmaceuticals
WebSite Homepage: http://www.skbp.com Contact Person: Taeg Sang You
E-mail: taegsang.you@sk.com Contact: +82-2-2121-5379

Related Projects

Related Project
Late phase global clinical development of YKP10811, a drug for functional gastrointestinal disorder Project view
list
Update to 2013 © KOREA DRUG DEVELOPMENT FUND. ALL RIGHTS RESERVED. QR Code