R&D

RESEARCH & DEVELOPMENT

PIPELINE

iN Therapeutics possess pipeline of various nervous system diseases medicine such as medicine for chronic pains, hearing loss and Lou Gehrig’s disease based on synthesis technology of medicinal chemistry considering ion channel target and ion channel research platform (VITVOTM).

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Program Drug Mechanism Basic
research
Discovery of candidate
substance
Non-clinical
research
Phase 1
clinic
Phase 2
clinic
Nav 1.7 iN1011-N17 Osteoarthritis pains, oral
iN1012-N17 Pains after surgery, injections
iN1213-N17 Neuropathic pains, external application
iN1011-N17 Animal pharmaceuticals
Kv 7.4 iN2011-K74 Hearing loss
Kv 7.2/3 iN3011-K23 Amyotrophic lateral sclerosis
iN4011-K23 Epilepsy
iN5011-K23 Alzheimer

Nav1.7 (DWP17061)

DWP 17061 shows excellent excellent pharmacokinetics to the body compared to competing material when it acted after being administered to the body. It was confirmed to have excellent analgesic effect compared to nonsteroidal antiinflammatory drugs (NSAIDs) and Tramadol, representative analgesics. Nonopioid analgesic DWP17061 is a Nav1.7 blocker (Voltage Gated Sodium Channel 1.7 blocker) which blocks only Nav1.7 that is sodium channel acting directly to the pain and prevents pain signaling from being delivered to the central nervous system. Nav1.7 is an ion channel that allows sodium ion to enter the cell which is known to be an important mediator for delivering pain signal.

When DWP17061 is developed, it will contribute to relieve pains of patients all over the world with safe and effective new drug for pain and developing nonopioid chronic pain drugs into innovative global new drug will be possible. Currently, it is estimated that 20% of the population around the world are pain patients, but satisfied analgesic has not been developed yet. Narcotic analgesic and NSAIDs which is nonpioid are divided in the analgesic market, and narcotic analgesic has high effect, but accompanies side effects such as dose-dependence, hypopnea and constipation. On the other hand, NSAIDs has less side effects, but its effect is relatively low.

In addition, DWP17061 is nonpioid analgesic which has no side effect on the central nervous system and its efficacy is high, having differentiated advantage from existing analgesics. If it is commercialized, it will be great help for patients who have used narcotic analgesic frequently or who haven’t dosed it for a long time and will satisfy unmet needs of pain market. According to <Future Market Insight 2019> the size of global analgesic market is worth more than 70 trillion which is known as the largest size following the anticancer drugs.

It has excellent selectivity and secure efficacy
that is almost same
with Tramadol
,
a narcotic analgesic.

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Subtypes Tissue distribution DWP17061
IC 50 (nM)
Selectivity vs
Nav1/7(fold)
hNav1.7 Peripheral
Nervous System
46 -
hNav1.1 Brain 790 17
hNav1.2 Brain 49 1
hNav1.3 Brain 1,100 24
hNav1.4 * Skeletal muscle >10,000 >217
hNav1.5 * Cardiac muscle >10,000 >217
hNav1.6 Brain 240 5
hNav1.8 Peripheral Nervous System >10,000 >217
hNav1.9 Peripheral Nervous System >10,000 >217
Paw withDrawal threshold(g)
Normal
DWP17061 10 mpk
Vehicle
Tramadol 40 mpk

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