Phytecs invests in exploratory, investigative research to follow the science wherever it may lead. This research serves as a foundational building block for continued drug discovery and development.

Lead Compounds

Phytecs’ focus on developing effective, efficient, and accessible ECS-targeting therapeutic agents, regardless of their source or origin, inspires and drives the company’s drug discovery program. Phytecs’ development pipeline includes both natural and semisynthetic compounds consistent with the company’s mission to harness and maximize the therapeutic potential of the ECS to address significant unmet needs for patients.  Pre-clinical research has led to the selection of these novel compounds and in vitro and in vivo laboratory assays support associating these lead compounds with particular therapeutic targets and indications.

Compound Description
PECS-F101a Fluorinated CBD derivative
PECS-F103b Fluorinated CBD derivative
PECS-F559(a)c Fluorinated CBD derivative
PECS-B201 Botanical compound
PECS-B202 Botanical compound

formerly HU474 and HUF101
formerly HU485 and HUF103
c formerly HU559(a)

Why Fluorination?

The increased frequency of anecdotal and clinical reports on the wide-ranging benefits of cannabidiol (CBD) in connection with an increasing array of therapeutic applications has fueled Phytecs’ interest in fluorinated variants of CBD due to CBD’s low bioavailability and the commensurate need for high doses to achieve the desired effect. Large doses are expected to be associated with higher prices and both dosage and cost can be expected to create obstacles for CBD treatment regimen compliance. Moreover, the chemical structure of CBD is not eligible for patent protection.

Fluorination enhances binding affinity, among other things, and is often used to make modern drugs more effective. Thirty percent (30%) of the best-selling pharmaceutical products worldwide contain fluorinated compounds, serving as testamentary, marketplace evidence of the value of fluorination in the drug development process. Preclinical data strongly suggests that fluorination can increase the potency of CBD, and Phytecs continues to build upon clinical research into prospective therapeutic applications for CBD with an interest in determining the opportunity to introduce F-CBD variants into the treatment landscape.

Cannabinoid Synergism

Over the last five decades, cannabinoid research has focused primarily on two lead phytocannabinoids: tetrahydrocannabinol (THC) and cannabidiol (CBD). However, in recent years, the therapeutic effects of other phytocannabinoids, including the propyl analogue of THC, tetrahydrocannabivarin (THCV), cannabigerol (CBG) and cannabichromene (CBC), as well as the acid forms of THC and CBD most commonly found in the plant, tetrahydrocannabinolic acid (THCA) and canabidiolic acid (CBDA), have received increased attention. Studies of these individual plant compounds have yielded critical data points demonstrating the variability and versatility of the cannabis plant as a phytocannabinoid factory.

In addition, ongoing research on certain combinations of plant derived compounds have generated data with even greater value, as a result of pronounced, often unexpected, synergistic effects originating from such combinations and interactions. Preclinical data strongly suggests that synergistic effects include, among others, modulation of adverse events, modified bioavailability, multi-targeting effects, and unexpected efficacy at lower concentrations and Phytecs is building upon this research as part of its botanical drug product development program.

Targets

In vitro and in vivo preclinical research has demonstrated that fluorinated cannabidiol compounds (F-CBDs) mimic the activity of CBD, and that certain F-CBDs exhibit significantly greater potency than CBD in various different models.  Research also demonstrates that combinations of naturally occurring phytocannabinoids may serve as effective pharmacologic agents to address symptoms and disease states.  Phytecs’ lead compounds have been found to be highly effective in predictive preclinical research, inviting further research and development to advance their therapeutic potential.

Model Research Center
In vivo animal models of anxiety, psychosis, obsessive-compulsive disorder, and schizophrenia Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo
http://www.fmrp.usp.br/
Principal investigator: Francisco Guimaraes
In vitro cellular model of epilepsy Università Campus Bio-Medico di Roma
European Brain Research Institute of Rome
http://www.ebri.it/
Principal investigators: Mauro Maccarrone and Robert Nistico
In vivo animal model of epilepsy Pharmaseed, Ltd.
http://www.pharmaseedltd.com/in-vivo-models/
Principal investigator: Dalia Shabashov Stone
In vivo animal models of pain Faculdade de Medicina de Ribeirão Preto
http://www.fmrp.usp.br/
Principal investigator: Francisco Guimaraes
In vitro cellular models of various skin diseases such as several types of dermatites, bacterial and viral skin inflammation, acne, and atopic eczema University of Debrecen
Principal investigator: Tamás Bíró
In vivo animal models of irritant dermatitis, psoriasis, and atopic eczema University of Debrecen
Principal investigator: Tamás Bíró
In vitro cellular models of inflammation University of Debrecen
Principal investigator: Tamás Bíró

Patent Protection

Phytecs has secured compound structure claims and use claims in the United States on its lead F-CBD variants, and is actively prosecuting these claims in Australia, China, Canada, Europe, Hong Kong, Japan, and Mexico with pending claims similar to those allowed in the United States.

Phytecs has filed for patent protection of proprietary botanical compounds and formulations, and will be activity prosecuting method and use claims related to such technology in each of the above-referenced jurisdictions.

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