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KDDF-201406-15 Development of analgesic compounds for the treatment of chemotherapy-induced peripheral neuropathy(CNS Diseases, Chemical) [10.01.2014]

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Development and Market Objectives

The development of 2 candidate substances for the treatment of chemotherapy-induced neuropathic pain, using FY-304, a derivative of 5-membered heterocyclic compounds and FY-504, the lead candidate from the Korean government’s new therapeutic development project [KDDF201304-06] in order to synthesize a new compounds with excellent efficacy, high stability and fewer side effects, and which is also appropriate for broad indications.

Unmet Medical Need & Target Patients

▷ Chemotherapy-induced Peripheral Neuropathy, CIPN
Table 1. Clinical research data for existing and combination CIPN therapies

Drug/Combination Tested

Study Result

Lyrica

Failed

Lidoderm

Failed

Procrit

Failed

Amitriptyine/ketamine/baclofen

Limited efficacy

 

▷ Neuropathic Pain : Issues with existing medication
- Analysis of currently-available medications highlights issues related to their efficacy and side effects. Improved pain alleviation and decreased side effects related to the central nervous system are the most important factors for the development of a new medication for the neuropathic pain.
- Gabapentin, pregabalin and similar drugs are allopathic medications used to ease neuropathic pain, but their level of efficacy is currently low effective for less than 30% of patients → an improvement of more than 50% is needed).
- Side effects such as dizziness and drowsiness are associated with CNS-targeted medications and none are currently capable of addressing the underlying cause of the disease.
- High-capacity administration is currently not possible with low stability candidates.

Status

In vitro and in vivo data show that FY-304 inhibits the TTX-resistant Na channel, highlighting the possibility for development as a CIPN alleviator.
▷ Using the properties of FY-304 and FY-504 from previous research efforts as the foundation, and via the synthesis of novel compounds, we are developing new substances for chemotherapy-induced neuropathic pain with excellent efficacy, high stability and fewer side effects, and which is also appropriate for broad indications.

Intellectual Property

▷ Patent Title: 5-membered heterocyclic derivatives, their method of manufacture and the pharmaceutical compositions arising from it (Patent No: 10-2013-0046117)
▷ Extent of Rights: 5-membered heterocyclic derivatives and their hydrates or pharmacologically active substances including pharmaceutical compositions that decrease pain including acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, and arthralgia.

Competitive Advantages

▷ Patent: Extensive literature analysis suggests that the potential for exclusive patent rights is very high with no intellectual property issues identified worldwide. As a highly novel candidate, broad patent rights are expected.
▷ Efficacy: Neuropathic pain relief or inhibition.

▷ Mechanism of Action: Selective inhibition of Nav1.8 (IC50>10pM)

▷ Toxicity: Single dose tox(oral), Bacterial Reverse Mutation Test (Ames Test), In vitro Chromosome Aberration Assay, In vivo Micronucleus Assay and  hERG assay were finished. The results were suited for goal.

Indication

CNS Disease (Chemotherapy-induced Peripheral Neuropathy, CIPN)

Research Period

Sep. 01, 2014 - May 31, 2016

Company

Hallym University

Developmental Stage

Lead optimization

Additional Information

Contact Information

Contact
Address Company Name: Hanlim University
WebSite Homepage: http://www.hallym.ac.kr Contact Person: Soo-Hyun Park
E-mail: shyun1017@hanmail.net Contact: +82-33-248-3181

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