Optimized Non-Addictive Biologics Targeting Sodium Channels Involved In Pain Signaling

Abstract

Researchers at the University of California, Davis have developed high potency and selective peptide inhibitors that act as a non-addictive analgesic for relief of chronic and/or severe pain in humans.

Full Description

Local anesthetics that inhibit Nav channels, sodium-voltage gated channels, are commonly used in pain management. Pain signals primarily originate in a subset of peripheral neurons that harbor a distinct subset of these Nav channels. Genetic studies have identified the key subsets of Nav channels involved in pain signaling. These subsets of Nav channels includes the channel Nav1.7. Current use of Nav channel blockers as an anesthetic is wide-spread due to their non-addictive properties and ability to inhibit Nav channels in peripheral sensory neurons. Unfortunately, current anesthetics are non-selective and block Nav channels vital for the function of the heart, muscle, and central nervous system.

Researchers at the University of California, Davis have established highly potent and moderately selective peptides that inhibits human Nav1.7 activation. Through optimizing the selectivity, potency, and stability of ProTx-II based peptides, researchers have developed a non-additive alternative to opioid analgesics for relief of chronic and/or severe pain in humans. These novel peptides are active against neuropathic pain in human sensory neurons and are stable in artificial cerebrospinal. When administered intrathecally the peptides are also effective againstchronic pain.

Applications

• Relief of chronic and/or severe pain in humans

Features/Benefits

• Optimization of wild-type ProTx-II peptide selectivity and potency 
• Non-addictive alternative to opioid analgesic

Patent Status

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• Computational design of peptides to target NaV1.7 channel with high potency and selectivity for the treatment of pain - 07/22/2022