FDA (US): Not approved (reached phase 2; no phase 3 is known to have started)
EMA (EU): Not approved
Dose
In the phase 2 IDEAL trial, 150 mg or 450 mg orally twice a day for 12 weeks was used; the dose that showed a signal of efficacy was 150 mg twice a day (Protagonist Therapeutics, 2022). There is no approved dose.
Safety
In healthy volunteers it was well tolerated and is barely absorbed into the blood. In phase 2, the safety of 150 mg was similar to placebo. Investigational drug: only in clinical trials.
Interactions
A high-fat meal reduced its exposure in healthy volunteers.
Differences between women and men
The single- and multiple-dose phase 1 studies were conducted only in healthy males. View the study →
Effect by goal · level of evidence
Gut-restricted action in healthy volunteers
no clear effectModerateclinical trial (A)in people
Phase 1 studies in healthy volunteers: minimal blood exposure, almost entirely eliminated in feces, and dose-dependent receptor occupancy in blood. Well tolerated.
Blocks the α4β7 integrin, a 'key' that certain white blood cells use to enter the intestinal wall. It is the same target as the antibody vedolizumab, but as a peptide that is taken by mouth and barely passes into the blood.
What the evidence says
In people
Action limited to the gut in healthy volunteers. Phase 1 studies in healthy volunteers: minimal blood exposure, nearly all eliminated in feces, and dose-dependent receptor occupancy in blood. Well tolerated. PubMed 33942566