cilobradine

Cilobradine is a small molecule drug that acts as a highly selective blocker of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, also known as "funny" current (If) channels. These channels are crucial for regulating the electrical activity and pacemaker function in cardiac tissue, particularly within the sinoatrial node, and also play roles in neuronal excitability. Cilobradine reduces heart rate by inhibiting these HCN channels, leading to decreased pacemaker currents. It has been investigated primarily for its potential use in treating sinus tachycardia and other conditions where heart rate reduction is desirable. The drug demonstrates use-dependent blockade of HCN channels with both open-channel and closed-channel blocking properties, distinguishing it from related agents such as ivabradine. Clinical studies have shown that cilobradine can significantly lower heart rate but may be associated with QT interval prolongation at higher doses[3][5][7]. Development was led by Boehringer Ingelheim.

Other names

cilobradinaCilobradine hydrochloride