Science

The neurotransmitter dopamine underlies the brain’s exquisitely precise regulation of physical movement. The neurotransmitter glutamate accounts for more than 80% of the brain’s activity. Restoring dopamine and glutamate balance is the key to reducing symptoms and improving health and well-being for many people with serious neuropsychiatric conditions.

Schizophrenia

People with schizophrenia have persistent, often disabling symptoms related to hallucinations, delusions, thinking, and feeling. Although there are medications that treat this condition, they often cause serious health problems and other problematic side effects, pointing to the need for better therapies.

Tourette Syndrome

Children and adults with Tourette syndrome experience involuntary repetitive movements and vocalize sounds or words that they cannot control, and often struggle with other serious neuropsychiatric conditions.

Autism Spectrum Disorder

Children and adults with autism spectrum disorder may struggle with social interactions, learning and communicating, become easily overwhelmed, and get stuck in loops of behavior or thinking.

Traumatic Brain Injury

There are more than 250,000 hospitalizations and 55,000 deaths a year in the US alone due to head injury, potentially leading to a wide range of long-term or  neurological disabilities. Excess glutamate may play a major role in causing neuronal damage.

Other indications

EuMentis is evaluating other neuropsychiatric conditions that involve dopamine imbalance for EM-221 to help patients in need of better effective, safe and well-tolerated treatments.

EM-221, a PDE10A Inhibitor

EM-221 precisely modulates dopaminergic and other brain circuits believed related to the symptoms of schizophrenia, Tourette syndrome and other serious mental conditions. EM-221 is expected to be safer and better tolerated than antipsychotic drugs for these and several other mental health conditions.

How EM-221 works for Schizophrenia and Movement Disorders

GPe = globus pallidus externus
STN == subthalamic nucleus
GPi = globus pallidus internus
SNc = substantia nigra pars compacta

GPe = globus pallidus externus
STN == subthalamic nucleus
GPi = globus pallidus internus
SNc = substantia nigra pars compacta

Brain Circuits

Schizophrenia is believed to be caused by overactive dopamine and other neurotransmitter pathways that cause changes in how a person thinks, feels, behaves, and perceives. Tourette syndrome and other movement disorders may also be related to imbalance of the neurotransmitter dopamine in the parts of the brain that regulate and coordinate motor movement and speech.

In the Striatum

Inside the neuron, the PDE10A enzyme normally breaks down cAMP, reducing their levels inside the cell. EM-221 inhibits this enzyme, increasing levels of cAMP inside the cell. The overall effect is to restore neurotransmitter balance in dopamine-related and other multiple circuits connected to the striatum, which may in turn improve symptoms in schizophrenia and movement disorders

EM-113 for Autism Spectrum Disorder

EM-113 is a noncompetitive, low-trapping glutamate antagonist designed to inhibit receptors on neurons that are overly active. EuMentis is combining this clinically-validated approach with novel imaging technology to identify patients with autism spectrum disorder who are most likely to benefit.

Autism Spectrum Disorder

So far, there are no approved medications for this condition, although an imbalance in regulation of brain glutamate may underly ASD. A low-trapping NMDA antagonist can restore glutamate equilibrium without causing new and serious side effects.

How NMDA antagonists can work for Autism Spectrum Disorder
NMDA antagonists block signaling of over-active glutamate receptors

Traumatic Brain Injury (TBI)

Excess glutamate released after traumatic brain injury can lead to further damage and death to exposed neurons. There are no approved medications for TBI. EuMentis is working to identify an NMDA antagonist treatment to accelerate recovery and reduce long-term disability, funded by a grant from the US Department of Defense.

EuMentis Product Pipeline

Product
Discovery
Preclinical
Phase 1
Phase 2
Phase 3
Pivotal Study

EM-221

Schizophrenia

EM-221

Schizophrenia

Discovery
Preclinical
Phase 1
Phase 2
Phase 2

EM-221

Tourette syndrome & other indications

EM-221

Tourette syndrome & other indications

Discovery
Preclinical
Phase 1
Phase 2
Phase 2

EM-113

For autism spectrum disorder

EM-113

For autism spectrum disorder

Discovery
Preclinical
Phase 1
Phase 2
Phase 2

NMDA Antagonist

For traumatic brain injury

NMDA Antagonist

For traumatic brain injury

Discovery
Preclinical
Phase 1
Phase 2
Phase 2

NMDA Antagonist

For other CNS indications

NMDA Antagonist

For other CNS indications

Discovery
Preclinical
Phase 1
Phase 2
Phase 2