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before we create

we listen.

before we create

we listen.

Patients, and what they are living with, are at the center of everything we do. We want to take 
therapeutic-experience-driven development to a new level.  We make sure we stay in constant touch with patients and physicians through all stages of development, with their insights transforming how we define both the questions and the answers.

A rich portfolio of smart pinpoint solutions

Our pipeline is defined by major unmet needs and is aimed at helping patients regain a sense of balance, health, and a life worth living.

patient’s despair.

our commitment.

Depression is a mood disorder that causes a persistent feeling of sadness and loss of interest. The efficacy rates of most common treatments are low, with about 30% of patients with major depressive Disorder failing to respond to currently available antidepressants.

I don’t feel happiness and sadness, I don’t feel anything, I just don’t have enough energy to do the basic. I don’t want to talk with people, my energy disappear so fast and I want to go home, for my bed, for my computer.” (Patients forum 2017)

Clexio is developing CLE-100, an oral NMDA modulator, as an adjunctive treatment for patients suffering from Major Depressive Disorder with an inadequate response to anti-depressant treatments.

 

 

The onset of action for currently available antidepressants is typically 4 to 6 weeks. This lag, as well as a high non-response rate, underscores the need for new antidepressant medications.

patient’s pain.

our commitment.

Pain is a complex condition that affects more people than diabetes, heart disease and cancer combined.

“It is difficult for family, friends, and even your work associates to understand when you can never commit to any long-term plans, as you never know when your pain will flare up leaving you incapacitated.” (from FDA report “The Voice of the Patient” February, 2017)

At Clexio, we are developing a portfolio of novel non-opioids treatments to address various pain conditions, and to provide comfort, relief, and safety for pain sufferers. We are using well established mechanisms of action, and focusing on topical delivery in order to minimize systemic side effects.

 

Alleviating Painful Diabetic Neuropathy

Painful Diabetic Neuropathy (PDN) is a common and disabling complication of diabetes, and affect millions of people with around quarter of people with diabetes suffering from PDN. It involves symptoms of generally severe pain in a ‘glove-and-stocking’ distribution, usually beginning in the feet. 

It is hell to live with and is hard to treat. Currently approved drugs show treatment response in less than half of the patients.

Topical treatments are designed to bring relief to where it is needed. It also helps avoid many of the possible side affects and drug interactions issues of tablets or injections. This is particularly important for the diabetic population, which often suffers from cardiovascular comorbidities and uses multiple drugs. Currently there are no FDA approved topical treatments for PDN.

At Clexio, we are developing CLE-400, a topical formulation, about to enter clinical stage development, on the alpha 2 agonist Detomidine, for the treatment of Painful Diabetic Nauropathy.

Easing Cluster headaches

Cluster headaches, which occur in cyclical patterns or clusters, are one of the most painful types of headache. Cluster Headaches are characterized by intense and severe head pain that can lead to suicidal tendencies, at times called “the most painful conditions known to mankind”. A cluster headache commonly awakens patients in the middle of the night with intense pain in or around one eye on one side of their head. Bouts of frequent attacks, known as cluster periods, can last from weeks to months, usually followed by remission periods when the headaches stop.

CLE-500 is being developed as a patient-controlled drug-device combination for the immediate relief of cluster headaches. 

clexio technology

platform

for oral long-acting drugs

Clexio is developing a Novel Oral Long Acting Release (OLAR®) platform designed for continuous drug delivery to the GI tract allowing for more efficient drug absorption and lower drug plasma fluctuations, targeting therapeutic drug levels for 8 – 24 hours, under fast and fed conditions.

 

pipeline

Program & Indication

Pre clinical

Phase 1

Phase 2

Phase 3

CLE-100

Major Depressive Disorder (MDD) is a common and serious mental health condition affecting ~5% of the global population. Despite the availability of many antidepressant drugs, 1 in 3 patients suffering from MDD does not achieve remission following several treatment trials with antidepressant medications.

Clexio is on a mission to change this and is committed to finding an effective treatment for patients suffering from MDD, with an emphasis on patients who fail to respond to currently available treatments.

CLE-100 is an oral NMDA receptor antagonist, which is being developed by Clexio as an adjunctive treatment for patients suffering from MDD who inadequately respond to anti-depressant treatments.

CLE-100 is currently being tested in the CLEO study, a two part Phase 2 study conducted in the US.

We completed Part A of the CLEO study, which assessed the safety profile of CLE-100 given daily for one week to MDD patients.

Based on the results from Part A, we are now enrolling for Part B of the study.

CLEO Part B is a randomized, double-blind, placebo-controlled, multicenter Phase 2 trial of CLE-100 as an adjunct therapy in subjects with Major Depressive Disorder with inadequate response to standard antidepressant therapy. Approximately 120 patients will be randomized to receive CLE-100 or placebo for 4 weeks. Patients will be assessed throughout the study using different measures including safety parameters, the Montgomery-Åsberg Depression Rating Scale (MADRS), other clinician-rated scales, as well as patient-reported outcome measures.

 

CLE-600

Parkinson’s disease (PD) is the second most common neurodegenerative disease after Alzheimer’s disease, with US prevalence estimated at ~1,000,000 individuals with Parkinson, growing due to aging population. Parkinson’s disease occurs when dopamine- producing nerve cells in an area of the brain that controls movement die,  resulting in a reduced production of dopamine, which causes the movement problems characteristic to Parkinson’s. Thus, Parkinson’s disease symptoms include stiffness, tremors and difficulty with balance and coordination occurring during the day and at night.

One of the common struggles for Parkinson’s patients is troubled nights and morning akinesia.

Nocturnal symptoms and Early Morning Akinesia (EMO) are estimated to be prevalent in more than 60% of Parkinsonian patients, having a negative impact on patients’ quality of life and daytime function. Current available dopaminergic treatments do not cover the duration and levels required for clinical efficacy over the entire night.

Clexio is developing CLE-600, a night pill for the treatment of Parkinson’s disease nocturnal symptoms and Early Morning OFF.

CLE-600 uses Clexio’s proprietary Oral Long Acting Release (OLAR®) drug delivery platform. The development is designed to achieve stable and prolonged levels of Levodopa, aiming to enable Parkinson patients symptomatic control during the night and into the early morning.

Clexio conducted Phase 1 studies with CLE-600 in order to check safety and tolerability and Pharmacokinetic profile under food and fast conditions. The administration of CLE-600 was safe and well tolerated, and a prolonged pharmacokinetic profile was achieved.

Clexio is progressing the program into the next clinical phase.

CLE-600 is a new investigational product that has not been approved for commercial distribution.

CLE-400

CLE-400: Developing a novel non-opioid topical product to alleviate peripheral neuropathic pain

Overview
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.

 

Unmet Need in the Treatment of Neuropathic Pain

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*:

“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.”

* 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.

Our program

Scientific Aspects

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 as soon as day 1 of treatment and a cumulative analgesic effect was observed following repeated dosing.

Clinical aspects

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 launching a Multiple Ascending Dose study and preparing for a Phase 2 study to test safety and efficacy in patients.

 

CLE-400

CLE-400: Developing a novel topical drug to alleviate neuropathic itch

Overview

Clexio is developing CLE-400, a topical gel formulation containing a non-opioid, non-steroid, active compound, to alleviate neuropathic itch – chronic pruritus caused by nerve fiber damage, which is often underdiagnosed and has no approved treatment.

CLE-400 is a new investigational drug that has not been approved for commercial distribution.

 

Unmet Need in the Treatment of Neuropathic Itch

Between 23 and 44 million Americans are estimated to suffer from chronic pruritus. This condition can be debilitating, affects sleep and mood and can cause symptoms of anxiety and depression that can lead to a significantly reduced quality of life. Chronic pruritus is now known to be as debilitating as chronic pain and represents a serious public health concern*.

Neuropathic pruritus (or itch) is one of the types of chronic pruritus. Often underdiagnosed, it is caused by neuronal or glial damage along the sensory neural pathway. Neuropathic itch can be widespread or localized, and may be a debilitating condition associated with a markedly reduced quality of life.

Peripheral neuropathies that may involve neuropathic itch include peripheral diabetic neuropathy, post-herpetic neuralgia, small fiber neuropathy, Brachioradial pruritus and Notalgia paresthetica.

No therapies for neuropathic itch have been approved.   In some cases, neuropathic itch can be very severe, and unfortunately there is a scarcity of effective treatments, underscoring that neuropathic itch is an important unmet clinical need**.

These conditions affect not only thousands of patients, but their families as well. Some of their stories are described below:

“I feel like I was going insane, and no one could relate or understand what I’ve been going through for the past 5 or 6 years…”.

“BRP is an untamable, unpredictable, relentless beast. It strikes me in my sleep and leaves me with blood and tears. In moments of BRP-induced madness, I have fantasized removing my limbs by any means possible. Unable to reach REM sleep. Unable to hold down steady work. Unable to keep a positive attitude. This is a beast that rules me.”

*Curr Derm Rep, Nicholas K. Mollanazar et al, 26 Jan 2015.

**Pain, J Hachisuka et al. March 2018; 159(3): 603–609

Our Program

Scientific Aspects

CLE-400 is a topical gel containing Detomidine, a potent α2-adrenergic receptor agonist.

We hypothesize that detomidine activates α2-adrenergic receptors on skin nociceptors, leading to inhibition of receptor excitability and attenuation of neural itch signaling.

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 as soon as day 1 of treatment and a cumulative analgesic effect was observed following repeated dosing.

 

Clinical aspects

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 launching a Multiple Ascending Dose study and preparing for a Phase 2 study to test safety and efficacy in patients. 

CLE-500

Cluster headaches are a neurological disorder characterized by recurrent severe headaches on one side of the head, typically around the eye. It affects about 0.1% of the global population and is often said to be the “most severe pain known to man”. The age at onset is usually 20-40 years and men are afflicted three times more often than are women.

Cluster headache attacks usually last between 15 to 180 minutes. They usually occur with clock-like regularity with most people having one to three attacks per day, although some have up to eight attacks daily. A bout of regular attacks, known as a cluster bout, can last weeks to months.

Cluster headaches severely affect people’s quality of life and are associated with increased suicidality.

Patients with cluster headaches currently have limited treatment options.

Clexio is on a mission to develop a safe and effective treatment to relieve the pain experienced during a Cluster Headache attack and quickly. The target is to relieve pain within minutes.

CLE-500 targets the block of a specific nerve pathway associated with cluster headache pain. It is being developed as an intra-nasal drug-device combination that can be self-administrated by the patient.

Clexio completed two Human Factor studies in Cluster Headache patients to get feedback from patients on the device prototypes and the ease-of-use, and to make sure that the device is developed to best-fit patients’ needs.

OLAR©

Clexio’s proprietary Oral Long Acting Release (OLAR®) platform is designed for continuous drug delivery to the GI tract, allowing for more efficient drug absorption and lower drug plasma fluctuations.

It targets therapeutic drug levels for 8 – 24 hours.

OLAR® is administered orally and is non-invasive. It is a versatile platform, suitable for multiple APIs and enabling high drug loading (up to total of 750 mg drug and excipients loading).

The OLAR® is designed to be swallowed in a folded configuration, within a capsule. After swallowing, the OLAR® unfolds to a triangle with a size bigger than average pylorus allowing it to be retained in the stomach while releasing its inner formulation (multiple tablets). After the formulation’s dissolution, the OLAR® disassembles to parts smaller than the pyloric size, empties from the stomach and softens/degrades in the intestines.

Clexio conducted Phase 1 studies with OLAR® in order to check safety and tolerability, gastric retention and Pharmacokinetic profile: the administration of OLAR® was safe and well tolerated, and a prolonged pharmacokinetic profile was achieved.

For more details, please watch the OLAR® animation movie.

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