iN Therapeutics
Revamping Ion Channel Neuroscience

An estimated 100 million people suffer from pain, and the cost of treating it is approximately two billion dollars. Opioids and non-inflammatory drugs (NSAIDs) or Selective CoX2 inhibitors, which are conventionally used to treat pain, often exhibit side effects. Opioids carry the risk of addiction, whereas NSAIDs are relatively less effective and cause gastrointestinal disorders.

There is a need for more efficient treatment methods with lower central nervous system (CNS) side effects.

This is where iN Therapeutics comes in. It has developed drugs having opioid-like efficacy, which have low CNS side effects and are safer for long-term use.

“Our technological prowess has enabled us to create a new drug development research environment and ion channel platform, which have greatly improved our research,” says Chongdeok Park, CEO of iN Therapeutics.

The ion channel platform, along with specialized pharmaceutical chemical synthesis and electrophysiology researchers, ensure a seamless drug development process. Cutting-edge technologies and ion channel target-specific research capabilities enable iN Therapeutics to produce effective treatments for intractable nervous system diseases like chronic pain, hearing loss, and amyotrophic lateral sclerosis (ALS).

iN Therapeutics’ pipeline targets various ion channels, with the lead pipeline targeting Nav1.7 (sodium channel) for osteoarthritis pains and trigeminal neuralgias (iN1011-N17).

Despite the many attempts to develop novel analgesics to target Nav1.7, a genetically validated target for pain sensation, there has not been a successful innovation due to a lack of efficacy and a non tolerable safety profile.

However, iN1011-N17 shows exceptional selectivity value and improved preclinical efficacy compared to competitors, along with excellent preclinical safety with no increase in low-density lipoprotein (LDL). Currently, this product is in the clinical stage in Australia.

Multiple pipelines are in the development stage to target potassium channels with target indications that include hearing loss (iN2011-K74), amyotrophic lateral sclerosis (iN3011-K23), epilepsy (iN4011-K74), and Alzheimer’s disease (iN5011-K74).

iN Therapeutics has built the VITVO platform utilizing patch clamp technique of all levels for developing ion channel target therapeutics. It can verify anything from compound synthesis and HIT derivation to in vivo drug efficacy evaluation and PoC with the assistance of professional researchers.

The conventional patch clamping method assesses efficacy at the cellular and tissue level of a dead animal. VITVO’s patch clamping technique allows candidate assessment from in vitro to in vivo animal models. The platform assesses a candidate’s efficacy, allowing a single-step innovative link from fluorescencebased assays to the in vivo efficacy model using the live animal model. This is an innovational de-risking tool far beyond industry standards. This platform ultimately allows IVIVC linkages to correlate in-vivo to in-vitro assay in an integrated process. It enables assessment of the efficacy via an electrical signal, allowing quantitative assessment of the effectiveness.

The process is structured into four steps, with the first being a quick screening of an iN Therapeutics chemical library using an auto patch clamp. This is followed by an assessment of excitability at the cellular level using manual patch clamping, the gold standard assessment method. The efficacy candidate is then assessed at the tissue level, employing a slice patch clamp. Slice patch clamping has been the standard practice, however, iN Therapeutics has developed a unique platform that enables in vivo patch clamping using live animal models, allowing its effectiveness to be assessed in vivo.

Moving forward, iN Therapeutics aims to develop first-in-class drugs with a novel mechanism targeting ion channels for patients suffering from intractable neurological diseases worldwide. Concerning neurological disorders, it concentrates on using Nav1.7 Inhibitor to treat pain, Kv7.4 Activator for hearing loss, and Kv7.2/3 Activator to treat CNS diseases.

iN Therapeutics grew exponentially over the past 15 years from its humble beginnings of innovative research. Its unmatched R&D capabilities have made it a leader in ion channel technology. iN Therapeutics will continue developing drugs for the treatment of incurable diseases.