Introduction: Calcium Entry Blockers (CEBs)

Abstract

The following review relates the cardiovascular new drug discoveries of the organic chemicals called calcium entry blockers ¹⁾ of the recent past, to the present development of additional agents with similar mechanisms of action, and to the understanding of calcium metabolism which holds the key to meaningful future new drug discovery. CEBs are a special group of chemicals because they

• 1) can display dramatic therapeutic efficacy (e.g. in vasospastic angina),

• 2) demonstrate very potent biological activity preclinically,

• 3) share a common mechanism of action — a mechanism that supports other new therapeutic indications and

• 4) provide important tools by which to characterize calcium metabolism and its relationship to excitation-contraction or excitation-secretion coupling. There is widespread interest in CEBs as evidenced by the rapidly expanding scientific literature and the number of excellent reviews that have been published (see individual sections below).