Vedolizumab is a gut-selective α4β7 integrin antagonist that blocks adhesion of memory T cells to mucosal addressin cell adhesion molecule-1 (MAdCAM-1), thereby decreasing infiltration of these inflammatory cells into gut mucosal tissue and suppressing gut inflammation.

Vedolizumab undergoes a rapid, saturable, non-linear, target-mediated elimination process at low concentrations and a slower, linear, non-specific elimination process at higher concentrations. At therapeutic concentrations, vedolizumab primarily undergoes linear elimination.

Vedolizumab linear clearance (CLL) was similar in patients with ulcerative colitis (UC) and patients with Crohn’s disease (CD). The terminal elimination half-life (t ½ β) of vedolizumab is 25.5 days. Only extreme low albumin concentrations (<3.2 g/dL) and extreme high body weight values (>120 kg) were identified as potential clinically important predictors of vedolizumab CLL.

Positive exposure–efficacy relationships for clinical remission and clinical response were evident for vedolizumab induction therapy, which appeared to be steeper in patients with UC than in patients with CD.

Off drug, 10% of patients with UC or CD were positive for anti-drug antibodies (ADAs). Patients who were persistently ADA positive during treatment (positive at two or more consecutive visits) had decreased vedolizumab trough serum concentrations.