pe
pep-04435 v1 CC-BY-SA-4.0

Teduglutide: Gattex/Revestive gut-repair drug for short bowel syndrome

FDA-approved prescription drug that helps people who have lost most of their small intestine absorb enough nutrients to reduce or eliminate their need for intravenous feeding.

statusbioassayed targetGLP-2R length33 aa refs3
fda-approved
snapshot approved 90% confidence
Class
GLP-2 receptor agonist (DPP-4-resistant analog of glucagon-like peptide-2)
Status
FDA-approved prescription drug as Gattex (adult short bowel syndrome, December 2012; pediatric indication added 2019); also approved in the EU, UK, Canada, and Australia as Revestive
Best-supported effect
Reduction of parenteral support (PN volume and infusion days) in adults and children with short bowel syndrome dependent on parenteral nutrition, supported by the STEPS, STEPS-2, and STEPS-3 pivotal trials
Main caveat
Benefit is treatment-dependent — intestinotrophic effect requires ongoing daily injections, and PN dependence regresses if therapy stops. Long-term colorectal neoplasia risk from chronic intestinotrophic stimulation is still being surveilled, and the drug is not a general "gut health" or leaky-gut treatment.
status 5 / 5 · 2 contributors
prediction metrics openfold3-mlx 0.3.1
ipTM0.861
pTM0.675
avg pLDDT49.4
ranking score0.947
STRUCTURE · PEP-04435 × GLP-2R
ranking0.947
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
openfold3-mlx 0.3.1 · mmCIF ↓ download
sequence33 aa
15101520253033
HGDGSFSDEMN TILDNLAARDF INWLIQTKITD
in the news 1 article
overview readme

What this is

Teduglutide (sold as Gattex in the US and Revestive in the EU, UK, Canada, and Australia) is a prescription drug that helps people who have lost most of their small intestine absorb enough nutrients and fluid to reduce — or in some cases eliminate — their dependence on intravenous nutrition. It does this by stimulating the remaining intestinal lining to grow and become more efficient. The FDA approved it for adult short bowel syndrome in December 2012 and extended that approval to children in 2019, making it the first disease-modifying therapy for this condition rather than a treatment that merely manages symptoms. Teduglutide is a 33-amino-acid synthetic analog of glucagon-like peptide-2 (GLP-2); the stored sequence differs from native GLP-2 at position 2, where an alanine has been replaced by glycine — a change that makes the drug resistant to the enzyme DPP-4 and extends its half-life from roughly 7 minutes (native GLP-2) to roughly 2 hours, enabling once-daily use.

History

Teduglutide traces its origins to the discovery of GLP-2 itself. In the mid-1990s Daniel Drucker and colleagues at the University of Toronto identified GLP-2 as a 33-amino-acid intestinal hormone with potent intestinotrophic activity in rodents — meaning it stimulated growth of the intestinal lining. The problem was that native GLP-2 is rapidly degraded by DPP-4 within minutes, making it useless as a drug. NPS Pharmaceuticals (later acquired by Shire, then Takeda) solved this by making a single amino-acid substitution at position 2 (Ala→Gly), creating a DPP-4-resistant analog they called teduglutide (also known by its earlier research designation ALX-0600). Early pharmacokinetic work characterized its safety and half-life in healthy subjects (Jeppesen and colleagues 2005; Koizumi and colleagues 2008), and population PK studies across SBS and Crohn's disease cohorts established its dosing behavior (Yano and colleagues 2009). The STEPS pivotal trial program — a series of Phase 3 randomized controlled trials in adults with short bowel syndrome dependent on parenteral nutrition — demonstrated clinically meaningful reductions in parenteral support requirements at 24 weeks, leading to FDA approval as Gattex in December 2012. A 52-week safety and efficacy extension (STEPS-2) and a long-term follow-up extension (STEPS-3) subsequently supported the durability of the effect. Pediatric controlled trials led to the pediatric label extension in 2019. Teduglutide is also notable for its cost: list prices have historically run into the hundreds of thousands of dollars per patient per year, reflecting rare-disease economics and its status as the only approved disease-modifying therapy for short bowel syndrome.

What it does

Teduglutide acts on the GLP-2 receptor in the intestinal wall, telling the remaining intestinal lining to grow: it increases the height of intestinal villi and the depth of crypts, expanding the absorptive surface area. It also increases blood flow to the intestine and slows gastric emptying, both of which help the gut extract more nutrients and fluid from food. For patients with short bowel syndrome who depend on intravenous nutrition (parenteral nutrition, or PN) to survive, this means the remaining gut becomes more capable — and many patients can progressively reduce the volume, frequency, or duration of their PN infusions. A subset of patients achieve full independence from parenteral nutrition. The effect requires the drug to be present: when teduglutide is stopped, the intestinotrophic stimulus is withdrawn and absorptive capacity regresses over weeks to months, with PN dependence returning toward pre-treatment levels.

Evidence

  • Human: Strong. The STEPS pivotal trial (Jeppesen and colleagues, Gastroenterology 2012) demonstrated that significantly more teduglutide-treated adults with SBS achieved a ≥20% reduction in parenteral support volume compared with placebo at 24 weeks. The STEPS-2 52-week extension confirmed sustained benefit. The STEPS-3 long-term extension (Compher and colleagues 2017) documented continued reduction in parenteral nutrition and hydration support with an acceptable safety profile. A Phase 3 RCT in infants and children with SBS-associated intestinal failure (Kocoshis and colleagues 2023) supported the pediatric indication. Post hoc analyses from the STEPS program explored quality of life (Jeppesen and colleagues 2019), mucosal structural adaptation (Jeppesen and colleagues 2013), response predictors (Jeppesen and colleagues 2018), citrulline as a functional marker (Jeppesen and colleagues 2019), and liver chemistries. Multiple systematic reviews and meta-analyses — including a 2022 meta-analysis published in a peer-reviewed nutrition journal and a 2024 network meta-analysis of GLP-2 analogs — have independently synthesized the trial evidence and concluded teduglutide reduces parenteral support requirements in SBS. Exploratory RCTs have examined teduglutide in low-output enterocutaneous fistula and in children with severe acute malnutrition; neither indication is approved, and results remain preliminary.
  • Animal: Extensive. GLP-2 biology and intestinal adaptation mechanisms are well-characterized in rodent models and informed the clinical development program.
  • In vitro / mechanistic: Strong. GLP-2 receptor signaling on intestinal subepithelial myofibroblasts and downstream growth-factor cascades are thoroughly characterized; see Mechanism below.

Known effects

  • Reduction in parenteral nutrition volume and infusion days (SBS with intestinal failure) — FDA-approved; supported by multiple Phase 3 RCTs
  • Structural intestinal mucosal adaptation (increased villus height, deeper crypts) — Phase 3 RCT (mucosal-adaptation study; Jeppesen and colleagues 2013)
  • Improvement in quality of life in SBS patients — RCT-derived analyses (Jeppesen and colleagues 2013, 2019)
  • Improvement in liver chemistries in SBS-associated intestinal failure — Post hoc analysis of randomized data; moderate confidence (single analysis)
  • Slowing of gastric emptying — Phase 1 RCT in healthy adults
  • Reduction in intestinal permeability and improvement in GI motility — RCT in adult SBS patients on home PN

Safety signals

Adverse events reported consistently across the STEPS trial program and the approved label include abdominal pain, nausea, and injection-site reactions. A defining clinical management issue — rather than a classical adverse event — is fluid overload: as intestinal absorption improves, the volume of parenteral nutrition must be progressively reduced to avoid hypervolemia and electrolyte imbalance; this adjustment is a planned and necessary part of teduglutide management.

The label requires colonoscopy before initiating teduglutide and at intervals during treatment because teduglutide's intestinotrophic mechanism carries a theoretical risk of accelerating growth of colorectal polyps or neoplasia. Long-term colorectal neoplasia risk from chronic intestinotrophic stimulation over years to decades is still being evaluated through postmarketing registries and is not yet fully resolved. Biliary and pancreatic events have been observed and periodic monitoring for biliary and pancreatic disease is part of the labeled clinical management.

The label also identifies active or suspected GI malignancy and active unresected colorectal polyps as conditions requiring careful evaluation before initiating therapy. Known hypersensitivity to teduglutide or its excipients (including trace tetracycline residues from the manufacturing process) is a contraindication. Limited data exist on use in pregnancy and breastfeeding.

Long-term open questions: The long-term pediatric developmental and quality-of-life outcomes in children treated from young ages remain under characterization following the 2019 pediatric label extension. Predictors of full PN independence versus partial response are not yet fully defined. Optimal therapy duration for stable responders — including whether and how to attempt discontinuation — has not been established.

Regulatory status

  • US (FDA): Approved prescription drug — Gattex (teduglutide) for adults with short bowel syndrome dependent on parenteral support (December 2012); pediatric indication extended in 2019. Prescription-only; specialty pharmacy dispensing; no compounded or generic supply.
  • EU (EMA), UK (MHRA), Canada, Australia: Approved as Revestive for short bowel syndrome; typically managed through national rare-disease drug pathways.
  • WADA: Not specifically listed on the WADA Prohibited List. Teduglutide is an intestinotrophic GLP-2 analog rather than a metabolic or anabolic enhancer; athletes prescribed it for SBS should follow appropriate Therapeutic Use Exemption procedures.
  • Compounding: No legitimate generic or compounded teduglutide exists. Teduglutide is a complex recombinant peptide manufactured under controlled biologic-product processes, with authorized supply exclusively through the manufacturer's specialty pharmacy.

Myths and misconceptions

  • "Teduglutide is a GLP-1 drug like semaglutide or tirzepatide." No. Teduglutide is a GLP-2 analog and acts on the GLP-2 receptor in the intestinal mucosa to stimulate growth of the intestinal lining. GLP-1 drugs act on the GLP-1 receptor to regulate glucose and suppress appetite. GLP-2 and GLP-1 are both derived from the same precursor protein (proglucagon), but they bind different receptors and have completely different pharmacological effects (Gasbjerg and colleagues, Physiological Reviews 2026).
  • "Teduglutide is useful for general gut health, leaky gut, or IBS." No. The approved indication is short bowel syndrome with intestinal failure — patients who have lost enough small intestine that they cannot survive without intravenous nutrition. The drug's safety requirements (colonoscopic surveillance, biliary and pancreatic monitoring) and its cost do not support off-label use for milder gastrointestinal conditions.
  • "Once a patient responds, they can usually stop taking teduglutide." No. The intestinotrophic effect requires ongoing stimulus. When teduglutide is stopped, villus height and absorptive capacity regress over weeks to months, and PN dependence returns toward pre-treatment levels. Response means continued daily injections, not graduation off the drug.
  • "Generic or compounded teduglutide is available at lower cost." No. Teduglutide is a complex recombinant peptide. Authorized supply is exclusively through the manufacturer's specialty pharmacy; there is no legitimate generic or compounded version.

Mechanism

Teduglutide is an agonist at the GLP-2 receptor (GLP-2R), expressed prominently on intestinal subepithelial myofibroblasts. Receptor activation triggers paracrine release of growth factors — keratinocyte growth factor (KGF), insulin-like growth factor 1 (IGF-1), and epidermal growth factor (EGF) — that stimulate crypt cell proliferation and inhibit enterocyte apoptosis, resulting in increased villus height, deeper crypts, and greater mucosal absorptive surface area in the remaining intestine. In addition to these trophic effects, teduglutide increases mesenteric blood flow and reduces gastric motility, both of which support nutrient and fluid absorption.

Mechanistic specificity is important for accurate interpretation: teduglutide acts on the GLP-2 receptor in the intestinal mucosa. It does not act on the GLP-1 receptor that mediates the metabolic and appetite-suppressing effects of semaglutide or tirzepatide. GLP-2 and GLP-1 are co-secreted from the same L cells in the gut and share the proglucagon precursor, but they are pharmacologically distinct — a point reviewed extensively in Gasbjerg and colleagues (Physiological Reviews 2026).

The key structural modification enabling teduglutide's pharmacology: native GLP-2 has an alanine at position 2 that is rapidly cleaved by DPP-4, giving the native hormone a half-life of approximately 7 minutes. Substituting glycine at position 2 (visible as the second residue, G, in the stored sequence HGDGSFSDEMNTILDNLAARDFINWLIQTKITD) renders the peptide DPP-4-resistant and extends half-life to approximately 2 hours, enabling once-daily subcutaneous dosing.

Open questions

  • Long-term colorectal neoplasia risk: Postmarketing surveillance and registry data continue to accumulate; cancer risk from decades of chronic intestinotrophic stimulation is not yet fully resolved.
  • Pediatric long-term outcomes: Following the 2019 pediatric label extension, longer-term developmental, growth, and quality-of-life outcomes in children treated from young ages are still being characterized.
  • Predictors of full PN independence: A subset of patients achieve complete weaning from parenteral nutrition; the clinical, anatomic, and biochemical predictors distinguishing full responders from partial responders are not fully defined (Jeppesen and colleagues, Gastroenterology 2018).
  • Optimal therapy duration: Whether and when stable responders should attempt discontinuation — and how to monitor them — is not established.
  • Non-SBS indications: Pilot RCT data exist for low-output enterocutaneous fistula and exploratory data exist for severe acute malnutrition; neither indication is approved, and clinical utility outside SBS remains early-stage.

Related peptides

Teduglutide belongs to the proglucagon-derived peptide family, which includes both GLP-1 and GLP-2 and their analogs. For the GLP-1 receptor agonist side of this family — pharmacologically distinct from teduglutide but sharing the same hormonal precursor — see glucagon. GLP-2 biology is reviewed in the context of the broader proglucagon peptide family by Gasbjerg and colleagues (Physiological Reviews 2026), one of the refs attached to this card.

Hypotheses5 directions▾ collapse

Research directions for this peptide, selected from the current sources — hypotheses you can explore and model. None of it is proven yet; tap any one to see the full thinking.

openupdated 2026-06-11

Could damage to the connective tissue layer beneath the gut lining explain why some short bowel patients get little benefit from teduglutide?

If true, doctors could test for stromal damage before prescribing teduglutide, sparing non-responders an expensive and inconvenient therapy. It might also open the door to pairing teduglutide with drugs that reduce gut scarring.

The hypothesis
Teduglutide stimulates intestinal adaptation in short bowel syndrome not solely through direct GLP-2R signalling on enterocytes, but through a GLP-2R-dependent paracrine axis involving subepithelial myofibroblast-released IGF-1 and EGF, such that response heterogeneity across patients is partly explained by inter-individual variation in this stromal intermediate layer rather than in GLP-2R expression itself.
Why it’s plausible
GLP-2R is expressed on enteric neurons and subepithelial myofibroblasts rather than on absorptive enterocytes directly. The large and poorly explained heterogeneity of teduglutide response described in the literature is not accounted for by GLP-2R polymorphisms alone. A stromal intermediary model predicts that fibrotic or inflammation-damaged stroma in some SBS patients would blunt response regardless of receptor occupancy.
Why it matters
Identifying stromal competence as a modulator of teduglutide response would enable patient stratification before treatment, reducing the cost and harm of non-response, and would suggest combination strategies (e.g., anti-fibrotics alongside teduglutide) for refractory patients.
Plausibility.75
Novelty.70
Impact.80
Basis · grounding2 papers
[1]
paper
Large heterogeneity of teduglutide response is documented and not fully explained by known variables, consistent with a stromal competence hypothesis.
doi: 10.1053/j.gastro.2017.11.023
[2]
paper
Rise in plasma citrulline suggests mucosal mass increase, an indirect readout that reflects the net output of multiple cell types, consistent with a paracrine rather than purely cell-autonomous mechanism.
doi: 10.1002/ibd.21117
openupdated 2026-06-11

Could teduglutide help patients with Crohn's disease who have had repeated surgeries and now struggle to absorb nutrients?

If true, many severe Crohn's patients who depend on IV feeding could potentially use this drug to regrow enough gut lining to eat normally again, reducing infection risk and improving quality of life.

The hypothesis
Teduglutide has clinically meaningful intestinotrophic activity in inflammatory bowel disease-associated intestinal failure, beyond its approved SBS indication, because GLP-2R-mediated mucosal restitution is mechanistically upstream of and independent from the inflammatory pathways driving IBD, such that residual GLP-2R-responsive mucosa in IBD patients could support structural recovery even during active disease.
Why it’s plausible
IBD can cause intestinal failure through repeated resections converging on an SBS-like state, yet teduglutide is not approved for this subgroup. GLP-2R signalling promotes crypt cell proliferation and tight junction integrity through pathways that are not contingent on resolution of inflammation. The citrulline data from pilot studies support mucosal mass increase as a measurable outcome, and IBD-associated intestinal failure patients represent an unmet need.
Why it matters
If teduglutide can rebuild mucosal mass even in the context of ongoing IBD inflammation, it could reduce parenteral nutrition dependence in a much larger patient population than currently treated, representing a major shift in IBD management.
Plausibility.70
Novelty.50
Impact.80
Basis · grounding2 papers
[1]
paper
Pilot data showing citrulline rise (mucosal mass proxy) with teduglutide supports the concept that intestinotrophic benefit can be measured and is potentially applicable beyond classic SBS.
doi: 10.1002/ibd.21117
[2]
paper
Review describes anatomical heterogeneity within SBS, implying that the relevant biology spans multiple disease contexts where intestinal mass is limiting.
doi: 10.1152/physrev.00057.2024
openupdated 2026-06-11

Does the key amino acid swap that protects teduglutide from breakdown also make it a stronger activator of its receptor?

If true, it would mean the drug is better than its natural counterpart in two independent ways, and knowing this could help scientists design future gut-repair peptides that are even more effective at lower doses.

The hypothesis
The Ala2Gly substitution that defines teduglutide relative to native GLP-2 not only prevents DPP-4 cleavage but also subtly alters the backbone dihedral angle at position 2, shifting the ensemble of N-terminal conformations sampled and increasing intrinsic agonist efficacy at GLP-2R beyond what DPP-4 resistance alone would predict.
Why it’s plausible
Glycine is the only achiral amino acid and uniquely expands accessible phi/psi space, meaning the Gly2 substitution could alter how the N-terminus docks into the receptor extracellular domain. This is distinct from, and additional to, the DPP-4 resistance effect. If efficacy were purely a half-life story, equimolar dosing of a DPP-4 inhibitor plus native GLP-2 should reproduce teduglutide potency, which has not been formally shown.
Why it matters
Separating the conformational contribution of Gly2 from its protease-resistance role would clarify whether position 2 is a privileged engineering site for tuning GLP-2R agonist bias, which matters for designing next-generation gut-repair peptides with improved therapeutic windows.
Plausibility.70
Novelty.65
Impact.60
Basis · grounding2 computed/notes
[1]
noteREADME explicitly states the Ala2Gly change confers DPP-4 resistance and extends half-life from ~7 min to ~2 hours, but does not address whether the substitution independently alters receptor activation efficacy.
[2]
sequencePosition 2 is glycine (HGDGSFS...), confirmed from sequence; glycine introduces unique backbone flexibility relative to alanine that is independent of side-chain chemistry.
openupdated 2026-06-11

Could modifying the loose end of the teduglutide molecule extend its life in the body enough to allow weekly instead of daily injections?

If true, patients with short bowel syndrome could inject the drug once a week rather than every day, which would significantly reduce the burden of managing this already difficult condition and might help more patients stick with their treatment.

The hypothesis
The intrinsically disordered C-terminal region of teduglutide (approximately residues 26-33, LIQTKITD) is a viable site for PEGylation or fatty acid conjugation that would extend plasma half-life beyond the current 2-hour window to enable weekly dosing, without disrupting the N-terminal receptor activation domain, because this region contributes minimally to GLP-2R interface contacts as inferred from the low pLDDT of this segment.
Why it’s plausible
The low overall pLDDT (49.4) is consistent with the C-terminus being the dominant disordered region, as the N-terminal helix-forming segment (positions 1-20) would be expected to be more ordered when modelled against the receptor. C-terminal conjugation strategies have successfully extended half-life in GLP-1R agonists (e.g., semaglutide fatty acid at K26) without ablating potency. An analogous approach at the teduglutide C-terminus (K30 or K33) could reduce injection frequency from daily to weekly.
Why it matters
Reducing injection burden from daily to weekly would be a major quality-of-life improvement for SBS patients, many of whom are already managing parenteral nutrition lines, and could improve adherence and expand the treatable population.
Plausibility.60
Novelty.50
Impact.70
Basis · grounding3 computed/notes
[1]
structurepLDDT=49.4 overall with high ipTM=0.86 suggests the interface (N-terminal) is well-defined while peripheral regions including the C-terminus are disordered and less likely to be critical contact residues.
[2]
sequenceSequence contains K30 (LIQTKITD) as a potential conjugation site; this lysine is in the C-terminal disordered region distal from the HGDG activation motif at the N-terminus.
[3]
noteREADME states current half-life is approximately 2 hours enabling once-daily dosing; extension to weekly would require approximately 10-fold further half-life improvement, achievable with lipidation strategies used in semaglutide.
openupdated 2026-06-11

Is the drug structurally disordered while circulating, becoming ordered only when it grabs its intestinal receptor?

If true, this could explain how the drug avoids off-target effects while still working powerfully at the gut. It might guide engineers to build tighter, shorter versions of the drug for patients who need lower doses.

The hypothesis
The high ipTM (0.86) of teduglutide at GLP-2R reflects genuine high-affinity receptor engagement driven primarily by the N-terminal histidine and the central hydrophobic core (ILNLA), while the low pLDDT (49.4) indicates the C-terminal tail (positions 25-33) is intrinsically disordered in the unbound state and folds only upon receptor contact.
Why it’s plausible
An ipTM of 0.86 is strong evidence of a confident inter-chain interface, yet pLDDT of 49.4 is below the threshold for ordered structure, consistent with class B GPCR ligands that adopt helical structure only within the receptor binding cleft. The sequence contains ILNLA (positions 14-18) and the N-terminal HGDG motif, both canonically important for GLP-family receptor activation. Disorder in the free peptide does not preclude tight binding; it is the receptor-stabilised conformation that matters.
Why it matters
If the C-terminal tail is genuinely disordered until binding, truncated or stapled analogs that pre-organise the bioactive helix could show improved on-rate and potency, informing next-generation GLP-2R agonist design.
Plausibility.80
Novelty.40
Impact.50
Basis · grounding2 computed/notes
[1]
structureipTM=0.86 supports a confident modelled interface with GLP-2R; pLDDT=49.4 indicates overall low structural confidence consistent with intrinsic disorder of the free peptide.
[2]
sequenceSequence HGDGSFSDEMNTILDNLAARDFINWLIQTKITD contains HGDG at positions 1-4 and a hydrophobic stretch ILNLA at positions 14-18, matching class B GPCR N-terminal activation motifs.
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.8613682985305786 openfold3-mlx
ranking score 0.9468879699707031 openfold3-mlx
structural qualityopenfold3
0
metricvaluenote
gpde0.763global PDE — lower = better
disorder0.246fraction disordered
chain pair ipTM (A, B)0.861interface quality
3-letter notation
His-Gly-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-Leu-Ala-Ala-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gln-Thr-Lys-Ile-Thr-Asp
recipeopenfold3-mlx 0.3.1
parametervalue
modelopenfold3-mlx 0.3.1
weightsaedd8f3eb814e392…
hardwareapple_m4_base_16gb
mlx version0.31.1
python3.14.3
random seed42
msa strategycolabfold
diffusion samples1
runtime650s
predicted bymlx@peptide
predicted at2026-04-22
python3 openfold3/run_openfold.py predict --query_json {query.json} --runner_yaml examples/example_runner_yamls/mlx_runner.yml --output_dir {output_dir} --num_diffusion_samples 1
citationbibtex
peptidemodel (2026). Teduglutide: Gattex/Revestive gut-repair drug for short bowel syndrome (pep-04435, v1). PeptideModel. https://peptidemodel.com/card/pep-04435
@peptide{pep04435,
  sequence = {HGDGSFSDEMNTILDNLAARDFINWLIQTKITD},
  target   = {glp-2r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {bioassayed}
}
related peptides 5 by signal overlap
clinical trials 50 on ct.gov · 13 on EUCTR · checked 2026-05-09
ct.gov trials 50
with results 20
EUCTR 13
PubMed RCT 21
by phase
1phase 14phase 31early phase 14no phase
by status
6completed2recruiting1active1unknown
references 3 papers
discussion no comments
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