Pharmacokinetics of single and repeat doses of icatibant

Purpose Icatibant is a bradykinin‐2 receptor antagonist approved to treat acute hereditary angioedema attacks in adults. To‐date, no thorough investigation of the clinical pharmacokinetic (PK) parameters of icatibant and its primary metabolites has been reported. Here we present the PK results of two phase I clinical studies of icatibant in healthy human volunteers. Methods Single‐ and multiple‐dose plasma pharmacokinetics of icatibant were characterized in healthy volunteers. Icatibant concentration‐time profiles and PK parameters were derived after a single 30‐ or 90‐mg dose or three 30‐mg doses given at 6‐hour intervals. Results Maximal plasma concentrations for the 30‐mg (979 ± 262 ng/mL) and 90‐mg doses (2,719 ± 666 ng/mL) were achieved at