Science & Technology

Product Candidates

CTX01

CTX01 is a proprietary formulation of pharmaceutical cannabidiol being developed for the treatment of heart failure with preserved ejection fraction. Published third-party research has shown that cannabidiol reduces inflammatory activation of the endothelial lining of blood vessels and aids endothelial vasorelaxation, resulting in improved blood flow. Cannabidiol has also been shown to attenuate a number of measures of inflammation in models of diabetes, a common co-morbidity in heart failure patients, and to reduce myocardial fibrosis in a model of inflammatory heart disease.

Cannabidiol is fat soluble, virtually insoluble in water, highly sensitive to deactivation in the liver via first-pass metabolism, and is rapidly cleared from the body. This results in low active blood levels and overall bioavailability of less than 10% when taken orally. Cardiol’s CTX01 formulation for subcutaneous administration is designed to avoid first-pass metabolism, optimize and maintain blood levels of the drug, and target cannabidiol to areas of inflammation and increased fibrosis in the heart. Cardiol believes that overcoming the low bioavailability issues associated with cannabidiol and targeting the drug to sites of disease, will significantly broaden the therapeutic potential of this molecule.

CTX02

Cardiol is also developing CTX02, a proprietary formulation of methotrexate for the treatment of heart failure. Methotrexate, an inhibitor of cell division, was originally developed for cancer therapy, but lower doses were found to suppress the immune system, resulting in a dose-dependent down regulation of chronic inflammation. Low dose methotrexate is currently used as a disease-modifying agent in the treatment of rheumatoid arthritis.

Recent experimental data have shown that methotrexate improves cardiac function after acute myocardial infarction and has anti-fibrotic properties. Low dose methotrexate is currently being investigated in a clinical trial of 7,000 patients with diabetes or metabolic syndrome to determine whether its anti-inflammatory effects lead to a reduction in serious cardiovascular events (the Cardiovascular Inflammation Reduction Trial – theCIRT.org).

The ongoing CIRT trial is expected to generate significant interest within the cardiology community. In the context of this growing interest, Cardiol plans to play a leadership role in developing methotrexate for the treatment of heart failure.