A first-in-man study to evaluate the safety, tolerability, and pharmacokinetics of pasireotide (SOM230), a multireceptor-targeted somatostatin analog, in healthy volunteers.

Pasireotide (SOM230) is a multireceptor-targeted somatostatin analog with high binding affinity for four of the five somatostatin receptor subtypes (sst(1,2,3) and sst(5)), and potential clinical activity in several neuroendocrine and oncologic conditions, including acromegaly, Cushing's disease, and neuroendocrine tumors (NET). This manuscript reports the first-in-man dose-escalation study of pasireotide, evaluating its safety, tolerability, and pharmacokinetics (PK) in healthy male volunteers. A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo.