Studied in registered human trials with published pharmacokinetic data, but not approved. Dosing outside a trial protocol has no established safety margin.
Larazotide is a non-systemic, gut-restricted oral peptide: it is not meaningfully absorbed. In humans, oral 12 mg gave plasma concentrations below the assay LLOQ (0.5 ng/mL), so a systemic plasma half-life cannot be defined. Molecular weight 725.8 is the free peptide (CID 9810532); the acetate salt is ~785.9 (CID 44146842).
Celiac phase 2 trial tested 0.5, 1 and 2 mg TID; only the 0.5 mg dose met the primary endpoint (inverse dose-response). Given orally, not by injection.
Multiple randomized controlled human trials in celiac disease; PK well-characterized as essentially non-absorbed (local gut action).
No boxed warning (unapproved). Well tolerated in trials; because it is not absorbed, systemic toxicity risk is low. Not a systemic/injectable peptide.