Mathematical Derivation of Therapeutic Index Based on hERG IC_50 Taking Into Account Fraction Unbound in Plasma and Clinical C_max

Abstract

have offered some guidelines regarding what might bedeemed an appropriate therapeutic index (TI) to mitigate therisk of hERG-mediated arrhythmias for clinical candidates.Regardless of the actual TI desired, there is, at times, a degreeof confusion regarding how to calculate this value given the dif-ferent units oftentimes ascribed to an IC