CBD Cocrystal

At Artelo, we’re working towards a better CBD.

Artelo Biosciences Inc. has developed a patented novel CBD composition called ART12.11. Artelo’s approach to achieving patent protection for ART12.11 was to create a cocrystal. Cocrystalization is a proven pharmaceutical development strategy and follows FDA guidance for chemicals with properties similar to CBD.

Learn more and watch the summary video below.

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What is
CBD?

CBD
Limitations

What is a
Cocrystal?

introducing
ART12.11

What is CBD?

CBD—also known as cannabidiol [ca-nuh-bi-DYE-ol]—is a naturally-occurring chemical, or cannabinoid, that can be isolated from cannabis, hemp or made synthetically.

CBD is currently being evaluated in numerous clinical research studies for its neuroprotective, anti-anxiety, antiepileptic, antipsychotic, and anti-inflammatory properties.

In 2018, the US Food and Drug Administration approved a first-generation formulation of CBD for seizures associated with two rare childhood epilepsy syndromes.

CBD can exist in two or more solid crystalline forms

Can CBD be improved?

One limitation of CBD is it exhibits solid state polymorphism, which refers to its ability to exist in two or more solid crystalline forms. According to the FDA, polymorphic forms typically differ in their physicochemical properties which can have a direct effect on stability, dissolution, and bioavailability of a product as well as its manufacturing process.

“Polymorphic forms of a drug substance can have different chemical and physical properties… [which] can have a direct effect on… stability, dissolution, and bioavailability. Thus, polymorphism can affect the quality, safety, and efficacy of the drug product.”

Food and Drug AdministrationCenter for Drug Evaluation and Research (CDER), Guidance for Industry, ANDAs: Pharmaceutical Solid Polymorphism Chemistry, Manufacturing, and Controls Information, July 2007 – Read the FDA Guidance Document

Did you know?

Cocrystalization is a well-developed strategy to improve the pharmaceutical properties of a drug.

What is a Cocrystal?

Engineering of the crystalline structure of drug molecules by cocrystalization is a well-developed pharmaceutical strategy. Cocrystals are defined as crystalline materials composed of two or more molecules within the same crystal lattice. Compared to other classes of solid forms, cocrystals possess particular scientific and regulatory advantages. Although cocrystals may exhibit polymorphism, their rational design offers the opportunity to reduce polymorphism to a greater extent compared to other pharmaceutical forms. Importantly, cocrystals are viewed as patentable subject matter. To learn more about FDA’s guidance regarding cocrystals, click here.

Potential advantages of a CBD cocrystal –

Greater Consistency
Better Bioavailability
Improved Stability

No Polymorphism
THC-Free
Solid Dosage Formulation

Introducing ART12.11

To address the polymorphisms observed with CBD, Artelo Biosciences’ scientists worked with leading experts in cocrystalization to develop a second-generation CBD product candidate. Artelo’s novel, cocrystal, solid form of CBD, known as ART12.11, is the first and only CBD cocrystal to have an issued composition of matter patent from the US Patent and Trademark Office.

ART12.11 uses TMP (tetramethylpyrazine) as the coformer to form the cocrystal. TMP is a plant-derived compound which has been used in medicine and food flavoring applications throughout the world for several decades and has a favorable safety profile.

Artelo’s novel CBD cocrystal is expected to have superior pharmaceutical properties, including improved stability and more consistent drug exposure in patients.

In addition, ART12.11 is anticipated to benefit from the well-established perspective of FDA and other regulatory agencies regarding pharmaceutical cocrystals. Artelo Biosciences has the unique opportunity to develop a CBD drug product with the potential for improved safety and efficacy and with strong provisions for market exclusivity through 2038. Visit artelobio.com/pipeline for more information on where Artelo is developing ART12.11.

ART12.11 may offer several competitive advantages –

Superior Pharmaceutical Properties
Development of a CBD-based drug product with the potential for improved safety and efficacy

Intellectual Property Protection
Cocrystals are viewed as patentable subject matter, offering a strong proprietary position

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Artelo Biosciences is making important advancements in federally regulated cannabinoid-based drug development with ART12.11 and a diverse pipeline of other product candidates.

For more information, visit artelobio.com
Nasdaq: ARTL

Sources

Raw A.S., Regulatory Consideration on Pharmaceutical Solids: Polymorphs / Salts and Cocrystals. Presented at: Pharmaceutical Powder X-ray Diffraction Symposium 11; 2012 May 15-18; Fort Myers, FL, USA. http://www.icdd.com/assets/ppxrd/presentations/11/P24-Andre_Raw-Regulatory_Considerations-Polymorphs_and_CoCrystals.pdf
Mayr, T., Grassl, T., Korber, N., Christoffel, V. & Bodensteiner, M. Cannabidiol revisited. IUCrData 2, (2017). http://iucrdata.iucr.org/x/issues/2017/02/00/su4129/
Trask, A. V. An Overview of Pharmaceutical Cocrystals as Intellectual Property. Molecular Pharmaceutics 4, 301–309 (2007). https://pubs.acs.org/doi/10.1021/mp070001z
S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER). Guidance for Industry ANDAs: Pharmaceutical Solid Polymorphism Chemistry, Manufacturing, and Controls Information. (Office of Generic Drugs, 2007). https://www.fda.gov/media/71375/download
S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER). Regulatory Classification of Pharmaceutical Co-Crystals Guidance for Industry. (Office of Pharmaceutical Quality, 2018). https://www.fda.gov/media/81824/download
Karagianni, A., Malamatari, M. & Kachrimanis, K. Pharmaceutical Cocrystals: New Solid Phase Modification Approaches for the Formulation of APIs. Pharmaceutics 10, 18 (2018). https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5874831/
Guo et al., 2016: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4893570/
Donkor et al., 2016: https://www.ncbi.nlm.nih.gov/pubmed/27729283
Zou et al., 2019: https://www.ncbi.nlm.nih.gov/pubmed/31293426
http://www.efsa.europa.eu/sites/default/files/scientific_output/files/main_documents/295.pdf