Pipeline

Introduction

We have a broad clinical and preclinical pipeline focused on neuronal excitability conditions of the central and peripheral nervous system. Each program has a clinically validated mechanism of action for the diseases it is addressing. Our two lead drug candidates are ETX-810 for chronic pain and ETX-155 for major depressive disorder (MDD), hormone-related mood disorders and focal onset seizures (FOS).

Product Indications Preclinical Phase 1 Phase 2 Planned Program Timing
ETX-810
(PEA prodrug)
Diabetic
neuropathic pain
Lumbosacral pain
(sciatica)
Phase 2a
Phase 2a
Topline data 1H 2022
Topline data 1H 2022
ETX-155
(GABAA PAM – positive allosteric modulator)
Major depressive
disorder
Hormone-related
depressive disorders
Focal onset seizure
Phase 1 MAD
Phase 1b and Phase 2 initiations 2H 2021
Preclinical Pipeline
Kv7 Program
Next Generation Anxiolytic
Pain
Epilepsy
Generalized
anxiety
Clinical Candidate 2H 2021
Clinical Candidate 1H 2022
Product ETX-810
(PEA prodrug)
ETX-155
(GABAA PAM – positive allosteric modulator)
Preclinical
Pipeline
Indications
Diabetic
neuropathic
pain
Lumbosacral
pain
(sciatica)
Major depressive disorder Hormone-related depressive disorders Focal onset seizure
Kv7 Program
Pain
Epilepsy
Next Generation Anxiolytic
Generalized
anxiety
Preclinical
Phase 2a
Phase 2a
Phase 1 MAD
Phase 1
Phase 2
Planned Program Timing
Topline data 1H 2022
Topline data 1H 2022
Phase 1b and Phase 2 initiations 2H 2021
Clinical Candidate 2H 2021
Clinical Candidate 1H 2022

ETX-810

Our most advanced program is ETX-810 for chronic pain conditions. ETX-810 is an investigational first-in-class, non-opioid, new chemical entity (NCE) designed for enhanced efficacy, limited drug-to-drug interactions and a favorable safety and tolerability profile. We believe it has the potential to address the shortfalls of current therapies across a range of chronic pain conditions.

Unmet Clinical Need
There is significant unmet need for the treatment of chronic pain. Despite a massive global chronic pain therapeutics market that is expected to pass $29 billion in the next decade1, currently approved therapies have demonstrated inadequate efficacy, with less than half of patients achieving a 50 percent reduction in their pain in multiple pain indications2. In addition to limited efficacy, the current standard of care is hindered by dose-limiting side effects, including dizziness, sedation, gastrointestinal disturbances, as well as concerns over abuse liability.

The Science of ETX-810
ETX-810 is an investigational oral, non-opioid prodrug that exerts its therapeutic effects through the palmitoylethanolamide (PEA) pathway, which is known to broadly modulate neuroinflammation and pain signaling3. PEA is an endogenous bioactive lipid that has been validated as a therapeutic agent in more than 25 clinical trials across a range of chronic pain indications, where it consistently demonstrated statistically significant reductions in pain with favorable safety and tolerability4,5,6. Leveraging this data, ETX-810 was designed to significantly improve the oral bioavailability and systemic exposure of PEA to maximize the therapeutic effect. In addition to its potential to significantly reduce chronic pain, ETX-810 has no known drug-to-drug interactions or abuse liability, and in clinical testing to date has demonstrated an encouraging safety and tolerability profile.

In chronic pain (center panel), synthesis of PEA decreases and metabolism increases, leading to a net decrease in PEA beyond the level needed to maintain its anti-inflammatory and analgesic activity in healthy physiology (left panel). ETX-810 is an investigational novel, small molecule prodrug with the ability to supplement endogenous PEA, ensuring sufficient PEA levels are reached to exert its therapeutic effect (right panel).

PEA is a broad modulator of inflammatory processes which also affect pain sensation and neuroprotection. Its mode of action has multiple effects (i.e., pleiotropic), as it involves many pathways and targets in both the peripheral and central nervous systems.

Clinical Trials for ETX-810

Phase 2a clinical trials for ETX-810 are underway in lumbosacral radicular pain (chronic sciatica) and in diabetic peripheral neuropathic pain. 

ETX-155

Our other clinical program is ETX-155 for use in multiple disorders of high unmet need, including major depressive disorder (MDD), hormone-related depressive disorders and focal onset seizures (FOS). ETX-155 is an investigational oral, next generation, neuroactive steroid NCE that acts as a GABAA positive allosteric modulator (PAM) designed to address the shortcomings of other molecules targeting the GABAA channel. We believe it has the potential to be a best-in-class treatment.

Unmet Clinical Need

There is significant unmet need for new treatments for mood disorders and epilepsy.

MDD affects approximately 35 million adults globally, causing significant impairment to daily life7. While there are effective therapies available for individuals suffering from MDD, there is considerable variability in patient responsiveness. There is a pressing need for safe, well tolerated, and rapidly acting antidepressants that reliably provide clinical improvement faster than the up to 6 weeks associated with standard of care SSRIs/SNRIs.

Epilepsy affects approximately 4.7 million people globally, with approximately 1 million of these patients experiencing uncontrolled FOS that are refractory to multiple anti-epileptic drugs (AEDs)8,9,10. FOS patients have a high prevalence of psychiatric co-morbidities like depression, and for many patients, their current AEDs have a negative impact on mood. There is a pressing need for new AEDs that not only reduce the number of seizures but also provide a positive effect on mood.

The Science of ETX-155

ETX-155 is an investigational novel, oral, next generation, neurosteroid GABAA PAM that demonstrates dual synaptic and extrasynaptic receptor activity with an approximate 24-hour half-life and no clinically meaningful food effect. Preclinical and Phase 1 clinical data demonstrate the potential for ETX-155 to be a best-in-class treatment for multiple neuronal excitability disorders.

ETX-155 is an investigational oral neuroactive steroid GABAA receptor positive allosteric modulator (PAM) that binds at the neurosteroid site on extrasynaptic and synaptic receptors. Binding at the extrasynaptic and synaptic receptors causes enhanced GABAergic tone and GABAergic synaptic transmission, respectively, leading to decreased neuron excitability and firing.

Clinical Trials for ETX-155

ETX-155 is being evaluated in Phase 1 studies with plans to initiate proof of concept trials targeting multiple disorders, including MDD, hormone-related mood disorders (e.g., hormone-related depression) and FOS. Phase 2 clinical trials across multiple indications are planned to begin in the second half of 2021.

Preclinical Pipeline

Eliem is progressing a pipeline of preclinical candidates for other neuronal excitability disorders, with two programs currently in advanced discovery stage.  Our lead preclinical program is a Kv7.2/3 channel opener. The Kv7.2/3 mechanism has been validated through regulatory approvals of multiple first generation Kv7.2/3 channel openers, which showed powerful efficacy but subsequently had to be withdrawn from the market due to significant safety issues. Eliem is focused on harnessing the efficacy of the Kv7.2/3 channel approach while significantly enhancing its safety and tolerability profile.  Eliem is also developing a next generation non-sedating anxiolytic based upon a clinically validated mechanism.

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Eliem Therapeutics, Inc.
23515 NE Novelty Hill Road, Suite B221 #125
Redmond, WA 98053

Eliem Therapeutics (UK) Ltd: Reg. 11893311
3rd Floor, 1 Ashley Road
Altrincham, Cheshire WA14 2DT