Cardiol Therapeutics Announces Topline Results from Phase I Single and Multiple Ascending Dose Clinical Trial of CardiolRx™

Cardiol Therapeutics Inc. (TSX: CRDL) (OTCQX: CRTPF) (FSE: CT9) (“Cardiol” or the “Company”), a clinical-stage biotechnology company focused on developing innovative anti-inflammatory therapies for the treatment of cardiovascular disease (CVD), today announced topline results from a Phase I single and multiple ascending dose clinical trial of CardiolRx™, a pharmaceutically produced oral cannabidiol formulation being developed for the treatment of acute and chronic inflammation associated with heart disease.

“As our study represents one of the most comprehensive Phase I clinical trials ever conducted in adults with a pharmaceutically produced cannabidiol formulation, we are pleased that the data are consistent with our expectations concerning the drug’s safety, tolerability, and PK profile,” said David Elsley, President and CEO of Cardiol Therapeutics. “Study results support the dosing regimen being utilized in our U.S. Phase II/III clinical trial investigating the cardioprotective properties of CardiolRx in 422 hospitalized patients with COVID-19 with a prior history of, or risk factors for, cardiovascular disease, and our plans to file a IND application with the FDA for a Phase II international trial in acute myocarditis, an inflammatory condition of the heart, which remains a leading cause of sudden cardiac death in children and young adults.”

The Phase I trial was a randomized, placebo-controlled, double-blind study designed to evaluate the safety, tolerability, and pharmacokinetic (PK) profile of CardiolRx at various dose levels. The study randomized 52 subjects (age range 25 to 60 years) to one of two groups. In Group A, there were three sub-groups, each involving 12 subjects (nine active and three placebo), with each subject receiving a single dose of 5 mg/kg or 15 mg/kg of CardiolRx, in either the fed or fasted state. In Group B, there were two sub-groups, each involving eight subjects (six active and two placebo) with each subject receiving 5 mg/kg or 15 mg/kg twice daily for six days. Serial blood samples were taken to measure the level of cannabidiol and its two main metabolites.

Topline results demonstrated that CardiolRx was safe and generally well tolerated at all dose levels, with no serious adverse events reported in the study. Fifty-one of the 52 enrolled subjects completed all requirements of the protocol. Each subject had repeated standard measures of safety including physical examination (with vital signs), electrocardiogram (ECG) to monitor cardiac time intervals (particularly, the QTc interval, which is an important measure of the risk for abnormal heart rhythms), as well as a number of biochemical and coagulation laboratory tests. Despite the relatively high doses of CardiolRx administered during the study, there were no ECG or abnormal laboratory findings after six days of dosing; specifically, no elevation of liver enzymes or QTc changes were detected. The recorded adverse events were all mild or moderate in severity and were primarily related to the gastro-intestinal tract.

PK studies determined that blood levels of the drug generally increased with increasing dose. Following a single dose of CardiolRx, the area under the time-concentration curve (AUC), which represents the extent of exposure to the drug, was 6-7-fold higher in the fed state than the fasted state. Furthermore, following single doses of CardiolRx in the fed state, the time to maximal blood level (Tmax) was in the range of five to seven hours, with a half-life of 26 to 29 hours. The above findings are consistent with published results for oral cannabidiol formulations and serve as a rationale for the dosing regimen that will be utilized in the Company’s Phase II/III study being initiated in the U.S. in COVID-19 patients who are hospitalized with a prior history of, or risk factors for CVD, and for the planned Phase II program in acute myocarditis.