Clexio is developing CLE-400, a topical gel formulation containing a non-opioid, non-steroid, analgesic compound, to treat patients suffering from peripheral neuropathic pain.
CLE-400 is a new investigational drug that has not been approved for commercial distribution.
Neuropathic pain is a complex, chronic painful state that is usually caused by peripheral nerve injury. The damaged sensory nerve fibers send incorrect signals to the central nervous system, resulting in chronic pain, often accompanied by additional sensory symptoms. Patients experience numerous pain sensations (e.g. pricking, tingling, burning pain), particularly in their hands and feet, which may make their simple daily tasks difficult. Some patients describe loss or significant changes to their careers, limited social interactions, decreased quality time with family, and feelings of hopelessness due to their disease. They report on reduced and/or unrestful sleep, bad mood, cognitive interference, and reduced overall daily function. Currently available treatments are only partially helpful. This chronic pain may severely alter the patient’s quality of life and is a significant economic burden.
Patients struggle daily with their symptoms. The following quotes represent some patients‘ voices.*
* The Voice of the Patient – A series of reports from the U.S. Food and Drug Administration’s (FDA’s) Patient-Focused Drug Development Initiative Neuropathic Pain Associated with Peripheral Neuropathy June 10 2016.
This pain is 24/7, it doesn’t go away.
I can’t sit for long periods. So even just going to the movies or play a game is uncomfortable.
I must often choose between meeting [family] responsibilities or taking the time to accommodate my pain and treatment.
CLE-400 is a topical gel containing Detomidine, a potent α2-adrenergic receptor agonist.
We hypothesize that by activating these receptors on skin nociceptors, detomidine can potentially lead to inhibition of receptor excitability and attenuate neural pain signaling. Detomidine also activates two secondary targets, histamine 4 (H4) and somatostatin 4 (sst4) receptors, which are known to be involved in the pathophysiology of pain.
CLE-400’s unique gel formulation enables maximal skin penetration while limiting systemic exposure. In addition, by creating a depot in the skin, CLE-400 is aimed at providing a long-lasting effect.
CLE-400, when administered topically, has shown effects in 3 different validated preclinical pharmacological models: Painful Peripheral Neuropathies, post-operative-pain and pruritus models. These studies each included placebo and positive controls. Rapid onset of effects was observed from day 1 of treatment and a cumulative analgesic effect was observed following repeated dosing.
CLE-400 is currently in Phase 1. The first Phase 1 study – a Single Ascending Dose study testing 3 different doses of CLE-400 – has been successfully completed. The company is now conducting a Multiple Ascending Dose study and preparing for a Phase 2 study to test safety and efficacy in patients.