Our lead product candidate, Gencaro™ (bucindolol hydrochloride), is a pharmacologically unique beta-blocker and mild vasodilator that we are evaluating in a clinical trial for the treatment and prevention of recurrent atrial fibrillation, or AF, in patients with heart failure with mid-range ejection fraction, or HFmrEF.
Beta-blockers, a well characterized class of drugs, target cardiac myocytes to reduce adverse beta1- adrenergic signaling that causes cardiac chamber remodeling. We believe Gencaro’s mechanism of action (MOA) is unique among beta-blockers due to its sympatholytic (norepinephrine lowering) and inverse agonism (inactivation of constitutively active receptors) properties.
We have identified common genetic variations in receptors in the cardiovascular system that we believe interact with Gencaro’s pharmacology and may predict patient response to the drug. The genotype which responds most favorably to Gencaro, beta-1 389 arginine homozygous, is present in approximately 50% of the U.S. population.
The approved therapies for the treatment or prevention AF have certain disadvantages in heart failure patients, such as toxic or cardiovascular adverse effects, and most of the approved drugs for AF are contraindicated or have warnings in their prescribing information for such patients. We believe there is an unmet medical need for new AF treatments that have fewer side effects than currently available therapies and are more effective, particularly in heart failure patients.