The Capton Approach

Captons, Treating Traumatic Brain Injury by Tackling Excitotoxicity

At Mercaptor Discoveries, we design therapeutics to treat TBI (traumatic brain injury) and neurodegenerative diseases utilizing our proprietary platform — a new class of molecules called CaptonsTM.

Our Efforts Combat COVID19: Mercaptor has directed its drug-development efforts toward epilepsy and traumatic brain injury, which share key features of pathophysiology relevant to COVID19. By pivoting our approach in the lab we are poised to begin studies to ease the suffering caused by the pandemic. Each of the three drug candidates selected for accelerated development at Mercaptor brings documented anti-inflammatory potency acting on separate, but complementary, pathways.

Treating Acute & Chronic Brain Trauma
Mercaptor’s mission is to leverage the Capton platform to develop an orally administered medicine engineered to mitigate the acute brain trauma triggered by blunt force injury. Taken as a daily “supplement” Captons would also prevent long term debilitating conditions that can result from TBI associated repetitive injuries and concussions, such as CTE, Parkinson’s disease, ALS and more. Captons could not only transform neurological medicine, but it could also save the game of football and other competitive sports and protect members of the armed forces.

Captons: Guardians of the Brain
Captons are taken orally. Capton molecules easily cross the blood-brain barrier and remain in inactive form – standing on guard until needed. When a Capton encounters an area of damaged tissue in the brain, it activates. A Capton becomes ACTIVE at the distressed location and at the dose needed. The more significant the tissue damage, the more the Capton will be activated, resulting in disease-metered dosing.

Captons: Calming Excitotoxicity to Restore Neuronal Communication
Excitotoxicity occurs when brain tissue is damaged, which in turn disrupts and destabilizes excitation, a normal process by which brain cells (neurons) communicate with each other.
This communication is how our brains keep up vital signs, enable us to think, sense the outside world, and generate responses.

Too much excitation, known as hyper-excitation, causes neurons to need more energy from the mitochondria – the main source of energy inside a cell.
The overworked mitochondria begin to fail, generating toxic molecules termed ROS (reactive oxygen species) triggering the release of glutamate.
When a Capton encounters an area of damaged tissue in the brain, it activates, binding up ROS, thereby lowering the levels of oxidative stress and calming excitotoxity. And yes, we have the data to back it up.

Proof of Concept
Captons have demonstrated reproducible proof-of-concept (POC), generating the active form of the therapeutic upon encountering damaged brain tissue. Furthermore, the lead Capton demonstrated efficacy in the Epilepsy Therapy Screening Program (ETSP) run by the National Institutes of Health – National Institute of Neurological Disorders and Stroke (NIH-NINDS).
These data support the penetration of Captons into the brain and activation solely in the presence of brain trauma.

Captons’ Competitive Advantage

  • Blood Brain Barrier: Captons cross the blood brain barrier more easily and effectively than other drugs
  • Injury-activated: Captons generate the neurotherapeutic drug at the site of injury at the time of injury.
  • Fewer side effects: Captons selectively act upon damaged areas of the brain, which would result in fewer side effects.

These unique properties could transform neurology and give relief for millions who suffer from neurodegenerative disorders like TBI, CTE, ALS, Parkinson’s disease, and more.

Partnering with the Pharma Industry
We are a disruptive technology – there’s no doubt about that — but we have such an abundant wealth of transformational technology that we are willing to share.

Most current drugs on the market treat TBI, CTE, seizures and related conditions are ineffective due to their indiscriminate flooding throughout the body, with very little of the active ingredient of the medicine treating the disease. In many cases, the enormous levels of dosing needed to achieve a small improvement come at the expense of high toxicity and intolerable side-effects (i.e. dizziness, fatigue, weakness, irritability, anxiety, and confusion). Many patients and medical professionals consider the remedy to be far worse than the disease.

The Capton platform could rescue these remedies. Along with the Captons Mercaptor is developing for TBI, CTE and other chronic brain conditions, we have identified several Capton lead molecules that could be paired with ineffective drugs to make them viable. In a process called “captonization” Captons modify ineffective neurotherapeutic drugs to have vastly improved brain penetration and be distributed in a manner that greatly reduces toxicity.

Many drugs have the right chemical properties to be “captonized.” When drugs are ‘captonized,” using a chemical “trick” to turn them into a Capton, they become inactive versions of themselves. As a Capton, a drug has higher brain penetration. Evenly distributed throughout the brain, the drug will remain inactive until a traumatic brain event such as a seizure or concussion. When the traumatic brain event occurs, the drug is then activated in the exact place where it is needed, and not everywhere in the brain.

Capton technology makes it possible to create innovative neurotherapeutic drugs with unprecedented potencies. Pharmaceutical companies could apply Capton technology to modify their molecules that have stumbled in the clinic due to poor efficacy, intolerable side effects, or low brain penetration.

Mercaptor has already identified several potential candidates (established molecules with neurotherapeutic properties) that can be transformed into Captons. These molecules can be out-licensed, sold, or developed by Mercaptor inhouse.

Other Applications
Captons have the potential to facilitate other groundbreaking therapeutic approaches, including stem cell therapies for neurological indications, which have faltered in the clinic.

By making ineffective neurotherapeutics viable, Captons have the potential to transform neurology from the weakest branch of medicine to the strongest, becoming the standard-of-care for neurodegenerative disorders.