Larazotide: Dosing Protocols

Important Disclaimer#

Larazotide acetate is an investigational compound whose Phase 3 trial was discontinued. It is not approved for clinical use in any jurisdiction. All dosing information is from published clinical trial data and is provided for educational purposes only.

Clinical Trial Dosing#

Phase 2b Study (Kelly et al., 2013)#

The Phase 2b study was a multicenter, randomized, double-blind, placebo-controlled trial evaluating larazotide acetate in 342 adults with celiac disease on a gluten-free diet for at least 12 months.

Study design:

• 4-week placebo run-in
• 12 weeks of active treatment
• 4-week placebo run-out
• Three dose arms: 0.5 mg, 1 mg, and 2 mg TID

Key findings at the 0.5 mg dose:

• Significant reduction in celiac disease symptoms versus placebo (P=0.022)
• 26% decrease in symptomatic days
• 31% increase in improved symptom days
• 50% or greater reduction from baseline in weekly average abdominal pain score for 6 or more of 12 treatment weeks

The inverted dose-response (0.5 mg superior to 1 mg and 2 mg) was an unexpected finding, potentially related to local receptor occupancy dynamics in the gut lumen.

Phase 3 CeDLara Trial (Discontinued)#

The Phase 3 CeDLara trial enrolled 525 patients across three arms (0.25 mg TID, 0.5 mg TID, placebo) for a 24-week treatment period. An interim analysis in 2022 determined that the treatment effect was too small relative to the placebo response to achieve statistical significance with a feasible sample size, and the trial was discontinued.

Administration#

Larazotide acetate was administered as oral capsules taken three times daily before meals. The pre-meal timing was designed to ensure the peptide was present in the gut lumen when dietary gluten exposure was most likely.

Dosing Context#

Larazotide belongs to the Immune category of research peptides. Dosing protocols for Larazotide are derived from available clinical trial data. These protocols are provided for research reference only and do not constitute medical advice. Actual dosing decisions should be made by qualified healthcare providers based on individual patient factors.

Research Protocols#

The following dosing protocols have been documented in clinical research for Larazotide:

Celiac Disease Symptom Reduction (Phase 2b)#

Dose: 0.5 mg oral capsules three times daily (TID) before meals. Higher doses of 1 mg and 2 mg TID were also tested but did not show superiority.

Frequency: Three times daily before meals

Duration: 12 weeks of treatment in Phase 2b trial

The 0.5 mg TID dose was the only dose to reach statistical significance versus placebo. The inverted dose-response (lower dose more effective) may reflect receptor occupancy dynamics at the gut surface.

Celiac Disease (Phase 3 CeDLara)#

Dose: 0.25 mg and 0.5 mg oral capsules three times daily in patients on a gluten-free diet with persistent symptoms.

Frequency: Three times daily

Duration: 24-week treatment period

Phase 3 trial was discontinued after interim analysis of 525 patients showed insufficient treatment effect to justify continuation.

Reconstitution and Preparation#

Larazotide acetate is administered as oral capsules. No reconstitution, mixing, or injection preparation is required.

Injection Sites#

Recommended injection sites for Larazotide include:

• Not applicable -- larazotide is an oral capsule formulation

Site rotation is recommended to minimize local tissue reactions and ensure consistent absorption.

Storage Requirements#

Clinical trial formulation stored under standard pharmaceutical conditions. Commercial storage guidelines not established as the product is not approved.

Related Reading#

• Larazotide overview and research guide
• Larazotide side effects profile
• Larazotide research evidence