Our Strategy

Our
Strategy

Whereas others have simply reformulated,
we focus on chemistry — and innovation

Unique TAAP™ and MPAR™ technology platforms

Ensysce has developed a game-changing 2-step trypsin activation technology, unique to the pharma industry, and is set to revolutionize the way a wide spectrum of drugs are delivered.

Our proprietary TAAP™ (Trypsin-Activated Abuse Protection) tamper-proof technology ensures that a drug can only be activated or turned on when it is  swallowed and comes into contact with the natural digestive enzyme trypsin, found in the small intestine. There is no opportunity for activation by manipulation outside of the body as is often the case with other drugs.

Additionally, Ensysce’s proprietary MPAR™ (Multi-Pill Abuse Resistance) technology can turn off the activation when too much TAAP medication is taken. This does not affect the effectiveness of MPAR™ products when taken as prescribed.

This technology holds the promise of eliminating accidental or deliberate overdose. In recognition of this highly innovative approach, the National Institute on Drug Abuse has supported Ensysce in development of MPAR™.

TAAP™

Trypsin-Activated Abuse Protection

TAAP™ opioids are designed with a 2-step verification mechanism that can’t be manipulated like ADFs

Activated only by trypsin,

a digestive enzyme that exists only in the gut. Crushing, inhaling or injecting it won’t cause the opioid to be released faster

Provides 12 hrs+ of pain relief,

which is 30% longer than abuse deterrent formulation, providing true twice-a-day dosing

Our proprietary (TAAP™) technology prevents abuse through a 2-step internal Trypsin-Activation process. Our prodrugs are chemically stable molecules that are activated only when administered orally. Due to the activating enzymes not being present in the blood or saliva, there is no opportunity for activation if injected, chewed or snorted.

Most abuse-deterrent opioid products that are currently marketed or in late-stage clinical development fall short of being fully resistant to abuse. Many of them use “extended-release” (ER) formulations. However, ER formulations are still prone to abuse by crushing, chewing, or extracting and injecting for an immediate release of active opioid to achieve rapid, spiking blood levels and a euphoric rush.

TAAP™ limits most forms of drug abuse including chewing, inhaling, manipulation and injection — and is adaptable to most prescription drugs having the potential for abuse.

MPAR™

Multi-Pill Abuse Resistance

Combining TAAP™ with MPAR™ protects patients from overdosing

Ensysce’s Multi-Pill Abuse Resistance (MPAR™) is an overdose protection technology that is unique to the industry. It provides a trypsin inhibitor that limits activation with increasing ingestion of product.

A small amount of activation inhibitor is added to each TAAP™ product and does not affect the opioid release if taken as prescribed.

On the other hand, if a prescription is not taken according to directions, or by accidental overdose, MPAR™ provides protection by way of a Trypsin Inhibitor which blocks the activation and release of the opioid, allowing the pills to pass through the body inactivated.

The National Institute on Drug Abuse awarded Ensysce approximately $12 Million to develop MPAR™.

Inhibits Trypsin

when too much TAAP™ opioid is swallowed, preventing full activation and opioid release

Only triggered by overdose,

at prescribed dose activity of trypsin will not be affected by MPAR™

Key Applications

TAAP™ and MPAR™ technologies have a wide variety of pharmaceutical applications,
and offer a disruptive solution to the many drug abuse crises that are plaguing society today. TAAP chemistry governs the way the drug is delivered, using the body’s own enzymes to activate  and release the medicine.

TAAP™ and MPAR™ technologies are broadly applicable – especially for medicines to treat pain and other CNS disorders where abuse can be an issue, as well as agents that may require improved oral delivery.

In contrast to the other approaches which alter oral delivery by changing the formulation, TAAP™ chemistry reduces the ability to easily manipulate products.

TAAP™ and MPAR™ benefits

TAAP™ can provide improved drug performance. Ensysce’s TAAP prodrugs can potentially improve attributes of other FDA-approved drugs, through enhanced bioavailability, controlled duration of action, improved safety, and reducing susceptibility to abuse.

MPAR™ can switch off the activation of TAAP™ products. MPAR provides another layer of protection and safety to Ensysce’s TAAP prodrugs.

Composition-of-matter patent protection. All TAAP™ and MPAR™ drug products are protected through Composition-of-matter patent protection. TAAP applied to other approved therapies produces new composition of matter and provides a strategy for life cycle management.

505(b)(2) NDA pathway. Ensysce’s TAAP drug products may be eligible to be developed through the 505(b)(2) NDA regulatory pathway, where if demonstrated to be bioequivalent to an appropriate approved drug, a 505(b)(2) NDA submission may reduce time to commercialization, saving millions in development.

FDA guidance. Given the growing desire of multiple federal agencies – including the FDA – to transition to more abuse-resistant products, Ensysce’s innovative solutions are set to establish us as a market-leading player and partner in an increasingly competitive landscape.

Clinical
Programs

PF614 : TAAP™

PF614 is our lead abuse-resistant TAAP, designed to treat severe and/ or chronic pain.

PF614 has been evlautated in Phase 1 clinical studies for safety and pharmacokinetic properties.

* Safety: Our key Phase 1 clinical trial evaluated the safety and pharmacokinetic release of oxycodone from a single dose of PF614, comparing it to OxyContin. Healthy subjects were randomized to receive an oral solution of PF614 or OxyContin tablets. 

* Safety data showed that PF614 is well tolerated with no unexpected safety concerns at all of the doses evaluated. 

* Pk and twice-a-day dosing: The pharmacokinetic data for PF614 demonstrated an extended release profile for the active oxycodone and a 12 hr half-life. This will provide a true twice-a-day dosing regimen, whereas other currently available agents are often used more frequently than prescribed because they don’t last twice-a-day, which can lead to misuse and/or abuse . 

* Our major Phase 1b clinical trial evaluated the safety and pharmacokinetic release of oxycodone from twice daily doses of PF614, comparing it to OxyContin. Healthy subjects were randomized to receive PF614 as an oral solution or in capsule form. A second arm of the study evaluated PF614 100 mg versus OxyContin 40 mg in healthy subjects under fasted and fed condition, exploring for bioequivalence.

* Capsule or liquid delivery: The pharmacokinetic data for release of oxycodone from PF614 was identical whether delivered as on oral solution or a solid capsule, demonstrating that PF614 is an excellent pain medication for those with dysphagia (trouble swallowing).

* Dosing wth food: PF614 demonstrated an extended release profile for oxycodone that was determined to be bioequivalent to the release from OxyContin under both fasted and fed conditions.

*FDA Fast track: The FDA has granted Fast Track designation for development of PF614 in recognition of the severe unmet need in this category.

PF614-MPAR™

PF614-MPAR, the combination of PF614 with the trypsin inhibitor nafamostat, is being evlautated in a Phase 1 clinical study for safety and its pharmacokinetic properties.

* Overdose Protection: Initial pharmacokinetic data for PF614-MPAR demonstrates that MPAR™ can provide overdose protection.

Nafamostat

Nafamostat has been evaluated in a Phase 1 study following oral delivery for tolerability and pharmacokinetics.  Nafamostat was well tolerated at doses of 200mg delivered three times daily. Nafamostat works locally in the gut, and is being used in our MPAR drug product to provide overdose protection.  Future studies of nafamostat as a single agent are planned as well as in combination in the PF614-MPAR drug product.   

Preclinical
Programs

PF8001 / PF8026 : TAAP™ AND MPAR™ AMPHETAMINE

PF8001 and PF8026 are extended and immediate-release prodrugs of amphetamine for ADHD Medication Abuse utilizing our proprietary TAAP™ and MPAR™ technologies.

TAAP™ METHADONE

TAAP-prodrugs for Opioid Use Disorder (OUD) utilizing our proprietary TAAP™  and  MPAR™ technologies are under development and are moving through preclinical development. 

Pipeline

Our robust development pipeline of TAAP™ designed products is led by PF614, a twice daily product for severe and/ or chronic pain. TAAP™ has also been applied to other treatments for pain, attention deficit hyperactivity doiorder (ADHD) and opioid use disorder (OUD). Where TAAP™ controls how our products are activated and released, we also add another layer of control to drug release with our combination MPAR™ technology. MPAR™ can turn off the activation if too much medication is consumed. Additionally, stemming from our MPAR™ technology is another product that has  potential to treat respiratory disorders such as Cystic Fibrosis.

Extended-release products for severe pain currently represent  a $4 Billion dollar market in the US alone* yet current drugs are subject to tampering and abuse that is associated with a significant number of deaths. Ensysce’s TAAP™ and MPAR™ technologies are poised to disrupt the pain market, leading with PF614.

*(ref: IQVIA)

Pain

Oxycodone concentration progression

Tap to see the effect when Untampered Tap to see the effect when Crushed
Oxycodone mean concentration (ng/ml) Time (hr)
TAAP™: Phase I Clinical Data

Unlike OxyContin,

PF614 can’t be chewed, snorted or crushed to release oxycodone inmediately.

PF614: TAAP oxycodone

PF614 is our lead product for severe pain based on TAAP technology. A follow-on MPAR™ combination product is also in clinical development to provide overdose protection. It is our priority program due to larger number of individuals that suffer with severe or chronic pain who are in need of safer therapies. Our technologies will deliver the required efficacy while providing peace of mind of having a safer product in the house.

ADHD

PF8001 / PF8026: TAAP amphetamine

PF8001 and PF8026 are extended and immediate-release prodrugs of amphetamine for ADHD utilizing our proprietary  TAAP™  technologies. Ensysce designed these TAAP™ prodrugs for use in ADHD in an attempt to improve safety of products for this indication. 

OUD – Opioid Use Disorder

Ensysce is continuing to apply its TAAP™ technology for products to treat Opioid Use Disorder (OUD) and is supported by the National Institute for Drug Abuse (NIDA).

Respiratory Diseases

As we have been developing MPAR, our overdose technology over the past ten years, we have grown a deep knowledge of the protease inhibitor, Nafamostat. We have identified several promising therapies for infectious and respiratory diseases.

Our Partnerships

Delivering Pipeline and Collaboration Opportunites

Strategic collaborations are one of the core components of our business, whether we out-license our TAAP™ and MPAR™ technologies to reinvent, revitalize, or develop novel therapies, or we in-license assets for development and commercialization. Ensysce works with their partners to solve their most challenging clinical and business risks. We offer a comprehensive worldwide patent portfolio through our TAAP™ and MPAR™ technologies with over 100 issued patents globally. Our industry-leading scientific, regulatory, and commercial expertise offer our collaborators the opportunity to obtain maximum value of their products.

“Ensysce’s prodrug drug delivery solutions can be applied to large component of all current proprietary and generic drugs worldwide” – Dr Lynn Kirkpatrick

Out-Licensing

Our prodrug technologies can be applied across a broad spectrum of drug therapeutic areas. We can collaborate to deliver novel molecules for clinical development, to revitalize approved medications, and to repurpose approved agents for the benefit of patients and caregivers. Ensysce’s prodrug platform enables new chemical entity (NCE) solutions that allow our collaborators to obtain new patents and extend market positions.

In-Licensing

Ensysce is interested in medicines that are complementary to our existing pipeline in CNS/Pain and will consider products in adjacent therapeutic areas. Our team seeks solutions for rare or complex pain indications and help ensure these medicines become available to the patients who need them.

Beyond Pain – Improved Oral Delivery

Oral route of administration is considered to be the preferred delivery for patients due to convenience, safety, and acceptance. For people suffering from chronic diseases requiring frequent injections, such as diabetes and osteoporosis, an orally delivered drug would be an attractive alternative. Oral delivery is likely to increase compliance, adherence, and improved quality of life.

Ensysce offers both TAAP™ and trypsin inhibitor technology to overcome the challenges of biologic and small molecule delivery.

Why Collaborate with us?

What We Offer

  • Our TAAP and MPAR™ pain and ADHD candidates outside of North America
  • Comprehensive global patent portfolio to extend patent and market positions
  • Novel prodrug NCEs for generic medicines for product differentiation and market expansion
  • Improved GI tract permeation enhancement of peptides and proteins

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