Drug intelligence / Profile preview

ranolazine + dronedarone

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

**ranolazine + dronedarone** is a combination of two antiarrhythmic small molecules used together to treat atrial fibrillation (AF). Ranolazine acts by selectively inhibiting the late sodium current (INa) in cardiac cells, leading to atrial-selective depression of sodium channel–dependent parameters including the maximal rate of rise of the action potential upstroke and the development of post-repolarization refractoriness. Dronedarone is a noniodinated derivative of amiodarone that blocks multiple cardiac ion channels including sodium, potassium, and calcium channels, as well as adrenergic receptors. When combined, ranolazine and dronedarone exert a potent synergistic effect, causing significant atrial-selective depression of sodium channel–dependent parameters and effective suppression and prevention of AF. This combination has been shown in preclinical and clinical studies to provide greater reduction in AF burden than either drug alone, with improved safety and tolerability at reduced individual doses[1][2][3][4].

Other names
ranolazine + dronedarone
02

Targets

LTCC (Voltage-gated calcium channel (L-type))ADRA1A (α1A)KCNH2 (Voltage-gated potassium channel subfamily H member 2)ADRB1 (β1)SCN5A (Sodium channel protein type 5 subunit alpha)

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