COMPOUND

Compounds / Healing

Teduglutide

Teduglutide (Gattex / Revestive, GLP-2 analog)

Healing SubQ FDA approved

33-amino-acid GLP-2 analog (alanine-to-glycine substitution at position 2) that resists DPP-4 degradation, extending GLP-2's plasma half-life from ~7 min to ~2 h. FDA-approved December 2012 (NDA 203441) as Gattex (US) / Revestive (EU) for adult and pediatric (≥1 yr) short bowel syndrome (SBS) requiring parenteral nutrition. Off-label biohacker use for IBD (Crohn's, UC), 'leaky gut,' and NSAID-induced enteropathy. CRITICAL: carries an FDA boxed warning for intestinal polyp / neoplasia risk. GLP-2 receptor agonism is mitogenic to intestinal epithelium and may accelerate growth of pre-existing polyps or cancer. BASELINE COLONOSCOPY IS A HARD PREREQUISITE, not a soft warning, with repeat colonoscopy at year 1 and every 5 years thereafter. Full label dose costs ~$295,000/year US wholesale.

At a glance

Half-life
~2 h Plasma t½ ~2 h after SC injection (vs ~7 min for native GLP-2). Bioavailability ~88% SC. Clinical effect (mucosal growth) outlasts plasma residence by many days. Marier 2008 PK data (PMID 18055850).
Routes
SubQ
Vial sizes
5 mg
Evidence base
3 studies 3 human

Mechanism

Selective GLP-2 receptor agonist. Activates GLP-2 receptors on enteroendocrine L-cells, enteric neurons, and subepithelial myofibroblasts. Drives increased crypt cell proliferation, villus height (40-60% increase in trial subjects), reduced enterocyte apoptosis, increased mesenteric blood flow, decreased gastric acid secretion, and improved intestinal barrier integrity. Net: more functional absorptive surface, less permeability, better nutrient and fluid uptake.

Dosing

Any amounts shown here are reported from published studies only. 3 of 3 catalogued studies involved human subjects. COMPOUND does not publish its own dosing guidance.

Where a study reports an amount, it appears in that study's entry below, attributed to the source.

Published evidence

  1. Human RCT 2011

    Teduglutide reduces need for parenteral support among patients with short bowel syndrome with intestinal failure

    Jeppesen PB, Pertkiewicz M, Messing B, Iyer K, Seidner DL, O'Keefe SJ, Forbes A, Heinze H, Joelsson B Gastroenterology

    STEPS trial: 24-week phase 3 in 83 SBS-IF adults. 0.05 mg/kg/day SC: 16/35 (45.7%) achieved ≥20% reduction in parenteral volume vs placebo (p=0.007). Higher dose (0.10 mg/kg/d) missed significance. Pivotal for FDA approval.

    PMID 21317170

  2. Human RCT 2010

    Teduglutide, a novel mucosally active analog of GLP-2 for the treatment of moderate to severe Crohn's disease

    Buchman AL, Katz S, Fang JC, Bernstein CN, Abou-Assi SG; Teduglutide Study Group Inflamm Bowel Dis

    Phase 2 RCT in 100 active Crohn's disease adults, 8 weeks: teduglutide 0.20 mg/kg/d achieved clinical remission in 32% vs 20% with placebo (no significant difference). Lower doses underperformed. Trial did not establish efficacy in CD.

    PMID 19821509

  3. Human RCT 2008

    Pharmacokinetics, safety, and tolerability of teduglutide in healthy adults and adults with Crohn's disease

    Marier JF, Beliveau M, Mouksassi MS, Shaw P, Cyran J, Kesavan J, Wallens J, Zahir H, Wallin BA, Berner B J Clin Pharmacol

    Established human PK: bioavailability 88% SC, t½ ~2 h, no accumulation with daily dosing.

    PMID 18055850

Reported side effects

Intestinal polyp / neoplasia (FDA BOXED WARNING)
Occasional Serious · FDA boxed warning. GLP-2 receptor agonism is mitogenic to intestinal epithelium and may accelerate growth of pre-existing polyps or neoplasia. The Gattex US label requires colonoscopy at baseline, at one year, and every five years thereafter, and directs discontinuation if malignancy is detected.
Intestinal obstruction
Occasional Serious · From mucosal hyperplasia. Surgical referral if symptoms (severe abdominal pain, distension, vomiting).
Pancreatitis (acute or chronic)
Rare Serious · Monitor lipase / amylase if abdominal pain persists.
Fluid overload (CHF risk in cardiac patients)
Rare Serious · From improved intestinal absorption: adjust diuretics in cardiac patients.
Abdominal pain / discomfort
Very common Moderate · 49% in trials. Often improves over first month.
Upper respiratory tract infection
Common Mild · 28% in trials.
Nausea
Common Mild · 27% in trials.
Injection site reaction
Common Mild · 21% in trials.
Headache
Common Mild · 17% in trials.
Vomiting
Common Moderate · 14% in trials.

Interactions

  • Oral medications (general) Caution

    Increased intestinal absorptive capacity may increase systemic exposure of co-administered oral drugs, especially narrow-therapeutic-index drugs (warfarin, digoxin, cyclosporine).

Reconstitution and storage

Single-use 5 mg powder vial reconstituted with 0.5 mL supplied diluent → 10 mg/mL solution. Swirl gently (do NOT shake: peptide foams). Use within 3 hours of reconstitution. Discard any unused portion.

Unopened vials: refrigerate 2-8 °C. Do NOT freeze. Reconstituted: room temp <3 hours, then discard. Original packaging: light-sensitive.

Open the reconstitution calculator for Teduglutide