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KDDF-201606-18 Preclinical Safety Evaluation of Novel Pain Killer SCN9A Antisense Oligonucleotide(CNS Diseases, Genetics) [11.01.2016]


Development and Market Objectives

People with SCN9A channelopathy are insensitive to severe pains, but normal in other sensory functions.   “OLP-1002” is an SCN9A antisense oligonucleotide inhibiting the expression of Nav1.7 encoded by the SCN9A gene.  OLP-1002 shows strong analgesic activity with excellent safety profiles, and therefore is considered to reproduce much of the pharmacological phenotypes of SCN9A channelopathy.  


OLP-1002 is being evaluated for 13W repeat dose safety in rats and monkeys, and shall be subjected to an IND filing in an European country or Australia.

Unmet Medical Need & Target Patients

Target Patients: Neuropathic pains, osteoarthritis pains, etc.


Unmet Medical Need:

Neuropathic pain develops as pain becomes chronic. The market potential for chronic pains is estimated to be in excess of 70 billion USD.  Neuropathic pains are intrinsically difficult to safely treat with currently available analgesics including pregabalin, opioids, NSAIDs, and so on.  Reflecting that pain is a defense mechanism of animals, attempts to develop safe but effective analgesics have repeatedly failed for the past several decades. 

Nav1.7 is the only safe and effective pain target well validated in human subjects by genomic findings. 


Paradoxically, small molecule Nav1.7 selective inhibitors to date have failed to show therapeutic activity in patients with neuropathic pains.  Those small molecule inhibitors show poor distribution to target tissues at therapeutic dose lacking cardiotoxicity.  Thus a Nav1.7 selective inhibitor is expected to claim much of the market potential for the unmet medical needs in chronic pains, if it possesses strong analgesic activity with excellent cardio-safety profiles.


OLP-1002 has been found to show analgesic efficacy in animal pain models for neuropathic pains, inflammatory pain, and formalin-induced pain.  Unlike small molecule competitors, OLP-1002 was found to be superior to pregabalin in a neuropathic pain model involving Nav1.7 upregulation in CNS tissues.

13W preclinical safety evaluations are ongoing in the US to successfully support an IND filing in an European country.

Methods development for GMP manufacturing of API and drug products are ongoing to support the IND.

Intellectual Property

OLP-1002 is a derivative of OliPass Oligonucleotide, a novel class of oligonucleotide which was developed by rationally modifying PNA to possess good membrane permeability as well as ultra strong affinity for nucleic acid.  OliPass Corporation owns the exclusive right to OliPass Oligonucleotide as directed by the patent application of PCT/KR2009/001256.

Competitive Advantages

Small molecule Nav1.7 selective inhibitors have been found to show poor analgesic activity in human subjects.  Nav1.7 selectivity has been improved by increasing the molecular size of inhibitors.  Thus, Nav1.7 selective inhibitors are doomed to possess poor distribution to target tissues of CNS.


OLP-1002 possesses an extremely high selectivity for Nav1.7 over Nav1.5, and distributes well to CNS tissues.  Taken the Nav1.7 selectivity and good distribution to CNS tissues together, OLP-1002 is to secure strong analgesic efficacy with good cardio-safety in patients of chronic neuropathic pains.


Given that the therapeutic dose of OLP-1002 is predicted to be as small as 10 to 20 mg per week in patients with chronic neuropathic pains, OLP-1002 may be developed for an annual treatment cost readily affordable by healthcare systems of most industrial countries.



Research Period



OliPass Corporation

Developmental Stage


Additional Information

Contact Information

Address Company Name: OliPass Corporation
WebSite Homepage: Contact Person: Hanyong Lee
E-mail: Contact: 031-8060-8202

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