title: The use of ranolazine in cardiovascular disease.
abstract: Ranolazine is a novel drug that has shown promise in the treatment of cardiovascular disease. Ranolazine exerts its effect by shifting myocardial energy metabolism away from free fatty acids and toward glucose as the substrate for production of adenosine triphosphate. Preclinical data have confirmed that ranolazine reduces myocardial ischaemic injury in various animal models. Researchers are continuing to gather clinical data but findings to date support the conclusion that ranolazine has anti-ischaemic effects without inducing the typical reduction in blood pressure and heart rate associated with the use of traditional anti-ischaemic agents. Given the absence of haemodynamic effects associated with ranolazine, it has great promise as a drug that could be added to existing therapy without concern for hypotensive or bradycardic side effects. Ranolazine has been shown to improve exercise-induced myocardial ischaemia and to lessen the severity of angina in the setting of chronic ischaemic heart disease. Early preclinical observations also suggest positive effects of ranolazine in the management of congestive heart failure; however, trials in this area are ongoing. Several recently completed Phase III clinical studies in patients with chronic ischaemic heart disease have confirmed the findings of smaller trials and should satisfy regulatory concerns necessary to place ranolazine on the commercial market in the US. The maker of ranolazine, CV Therapeutics (Palo Alto, California), will file a New Drug Application (NDA) with the US FDA for the approval of ranolazine as an anti-anginal in the near future.
authors.affiliation: Division of Cardiovascular Medicine, University of Florida College of Medicine, 1600 S.W. Archer Road, Box 100277, Gainesville, FL 32610, USA. schofrs@medicine.ufl.edu
authors.forename: Richard S
authors.initials: RS
authors.lastname: Schofield
authors.forename: James A
authors.initials: JA
authors.lastname: Hill
mesh_terms: D000083:Acetanilides; D000787:Angina Pectoris / Q000188:drug therapy / Q000378:metabolism; D000818:Animals; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000378:metabolism; D002986:Clinical Trials as Topic; D017277:Drug Approval; D004734:Energy Metabolism / Q000187:drug effects; D006801:Humans; D010879:Piperazines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D000069458:Ranolazine
chemical_list: D000083:Acetanilides; D010879:Piperazines; D000069458:Ranolazine