pe
pep-10868 v1 CC-BY-SA-4.0

Liraglutide: Victoza/Saxenda daily injection for diabetes & weight loss

A lab-made version of a natural gut hormone that tells the brain you're full, lowers blood sugar, and reduces the risk of heart attack and stroke; FDA-approved drug.

statusbioassayed targetGLP-1R length30 aa refs4
GLP-1diabetesobesitycardiovascularonce-dailyNovo-Nordiskapproved
snapshot approved 92% confidence
Class
GLP-1 receptor agonist
Status
FDA-approved prescription drug (Victoza for type 2 diabetes, January 2010; Saxenda for chronic weight management, December 2014; Saxenda adolescent indication, 2020); generic versions available in US from 2024 (Victoza) and 2025 (Saxenda); also authorized by EMA, MHRA, Health Canada, and TGA
Best-supported effect
~8% mean body-weight reduction at 56 weeks in adults with obesity (SCALE program, n=3,731); glycemic control in type 2 diabetes (LEAD program, Phase 3); 13% relative MACE reduction in high-CV-risk T2D patients (LEADER, n=9,340, median 3.8 years)
Main caveat
Clinically superseded by semaglutide and tirzepatide for weight-loss magnitude and dosing convenience in most adult populations; strongest current niche is pediatric and adolescent obesity; weight is largely regained within 1-2 years of discontinuation
status 5 / 5
prediction metrics boltz-2 1.0
ipTM0.929
pTM0.816
avg pLDDT76.3
ranking score0.796
STRUCTURE · PEP-10868 × GLP-1R
ranking0.796
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 1.0 · mmCIF ↓ download
sequence30 aa
151015202530
HAEGTFTSDVSSYLE GQAAKEFIAWLVRGR
in the news 136 articles
overview readme

What this is

Liraglutide (sold as Victoza for type 2 diabetes and Saxenda for chronic weight management) is a daily injectable medication that mimics a gut hormone called GLP-1 (glucagon-like peptide-1). It tells the brain you've eaten enough, slows digestion, and helps the pancreas control blood sugar. The drug was developed by Novo Nordisk and has been FDA-approved since 2010 for diabetes and 2014 for obesity — making it the first GLP-1 receptor agonist approved specifically for weight management and the first in its class to show a reduction in cardiovascular deaths in a large outcomes trial. Today it occupies a particular niche in pediatric and adolescent obesity, where it holds dedicated approval down to age 6, and is increasingly accessible as generic versions have entered the US market since 2024.

Liraglutide shares 97% homology with the native human GLP-1 peptide. The stored sequence (HAEGTFTSDVSSYLEGQAAKEFIAWLVRGR) is the bare amino-acid backbone; the active drug additionally carries a C-16 palmitic acid (palmitoyl) chain attached at Lys-26 via a γ-glutamic acid spacer — it is this lipid conjugation that enables reversible albumin binding, extending the half-life from approximately 2 minutes (native GLP-1) to approximately 13 hours and making once-daily dosing possible.


History

Liraglutide was developed by Novo Nordisk as a longer-acting analog of native GLP-1, which is degraded within minutes by the enzyme dipeptidyl peptidase-4 (DPP-4). The structural solution was a single amino-acid substitution (lysine to arginine at position 34 relative to native GLP-1) combined with the C-16 fatty acid lipidation at position 26, as described by Knudsen and colleagues (Frontiers in Endocrinology, 2019). These modifications protect the peptide from enzymatic degradation and enable albumin binding, creating the pharmacokinetic profile needed for once-daily use.

The FDA approved Victoza for type 2 diabetes in January 2010, following the LEAD (Liraglutide Effect and Action in Diabetes) program of six Phase III trials. The higher-dose Saxenda formulation gained FDA approval for chronic weight management in December 2014 — the first GLP-1 agonist indicated specifically for obesity. The landmark LEADER cardiovascular outcomes trial, completed in 2016, demonstrated a 13% relative reduction in major adverse cardiovascular events over a median 3.8 years in type 2 diabetes patients with high cardiovascular risk, establishing the first cardiovascular mortality benefit for the GLP-1 class. More recently, a dedicated randomized trial published in 2025 (Fox and colleagues) extended the pediatric evidence base to children aged 6 to under 12. Generic liraglutide entered the US market in 2024, making it the first GLP-1 receptor agonist to go generic.


What it does

Liraglutide activates the GLP-1 receptor in the pancreas, brain, and gut. In the pancreas, it triggers glucose-dependent insulin release and suppresses glucagon — lowering blood sugar without causing hypoglycemia when used alone. In the brain, it signals satiety centers in the hypothalamus and hindbrain, reducing appetite and food intake. It also slows gastric emptying, which blunts postprandial glucose spikes and contributes to a feeling of fullness after smaller meals.

For people with type 2 diabetes, the result is meaningful HbA1c reduction; for people with obesity, it produces moderate but clinically significant weight loss. The LEADER cardiovascular outcomes trial additionally showed a 13% relative reduction in major cardiovascular events over 3.8 years in high-risk type 2 diabetes patients — an effect attributed to the combination of metabolic improvement and potential direct cardioprotective signaling, though the precise mechanism underlying the cardiovascular benefit remains under investigation.

Liraglutide has largely been superseded by once-weekly semaglutide and tirzepatide for weight-loss magnitude and dosing convenience in most adult populations. The STEP 8 head-to-head trial showed semaglutide 2.4 mg weekly produced approximately 15.8% weight loss versus 6.4% with liraglutide 3.0 mg daily at 68 weeks. Liraglutide's current strongest niche is pediatric and adolescent obesity, where it holds dedicated approvals with specific trial support.


Evidence

  • Human: Extensive. The LEAD program (six Phase III trials) established glycemic efficacy for type 2 diabetes. The SCALE Obesity and Prediabetes trial (n=3,731, 56 weeks) showed mean weight loss of 8.0% versus 2.6% with placebo, with approximately 33% of participants achieving ≥10% body weight loss. The LEADER cardiovascular outcomes trial (n=9,340, median 3.8 years) demonstrated a 13% relative reduction in major adverse cardiovascular events. A Phase III pediatric RCT in adolescents aged 12–17 (n=251) supported the Saxenda approval for that age group. The STEP 8 head-to-head trial directly compared weekly semaglutide 2.4 mg to daily liraglutide 3.0 mg in adults with overweight or obesity, showing semaglutide produced approximately twice the weight loss. A 2025 randomized trial (Fox and colleagues) extended pediatric evidence to children aged 6 to under 12. A 2025 systematic review and meta-analysis assessed liraglutide for adults with obesity. Post-marketing data now span over 15 years.
  • Animal: Comprehensive preclinical program supported regulatory development. Rodent carcinogenicity studies identified the thyroid C-cell tumor signal that underlies the current boxed warning. Reproductive toxicity data in animals informed the label's pregnancy guidance.
  • In vitro: Mechanistic work characterizing GLP-1 receptor binding and downstream cyclic AMP signaling is available in the literature; individual assay data are not individually extracted in this card.

Known effects

  • Glycemic control (type 2 diabetes) — FDA-approved (Victoza); HbA1c reductions of 1.0–1.5 percentage points at 1.8 mg established in the LEAD program
  • Chronic weight management (adults) — FDA-approved (Saxenda); ~8% mean weight loss at 56 weeks in SCALE Obesity and Prediabetes trial
  • Chronic weight management (adolescents 12–17) — FDA-approved; supported by dedicated Phase III pediatric RCT
  • Chronic weight management (children 6–<12) — Supported by a single randomized trial (Fox et al., 2025); evidence base smaller and shorter-duration than adult dataset
  • Cardiovascular event reduction in high-risk T2D — Phase III outcomes trial (LEADER); 13% relative MACE reduction; applies to the high-cardiovascular-risk T2D population specifically
  • Weight loss after bariatric surgery — Studied in multiple RCTs and meta-analyses; evidence for use in patients with insufficient weight loss or weight regain after metabolic surgery
  • Cognitive and associative learning — A randomized trial showed liraglutide restored impaired associative learning in individuals with obesity; early-stage evidence
  • Neuropsychiatric populations — A randomized trial in adults with stable bipolar disorder and obesity assessed weight-related outcomes; isolated study

Myths and misconceptions

"Victoza and Saxenda are different drugs." They are the same molecule — liraglutide — at different maximum doses (1.8 mg for Victoza, 3.0 mg for Saxenda) with different FDA-approved indications. The active pharmaceutical ingredient is identical.

"Liraglutide is obsolete now that semaglutide and tirzepatide exist." Liraglutide produces less weight loss than semaglutide or tirzepatide in head-to-head trials, but it retains clinically relevant niches: the longest post-marketing safety record in the GLP-1 class (15+ years), dedicated pediatric and adolescent approvals including children aged 6 and up, established cardiovascular outcomes data from LEADER, and generic availability that materially changes the cost picture for many patients.

"Daily dosing means worse side effects than once-weekly agents." Daily dosing creates more consistent pharmacokinetic exposure with less peak-to-trough variation than once-weekly agents. The STEP 8 head-to-head trial showed comparable gastrointestinal adverse event profiles between liraglutide and semaglutide; the trade-off with daily dosing is convenience, not necessarily tolerability.

"Liraglutide is automatically safer in children because it's been around longer." The adult safety record does not automatically transfer to pediatric populations. Liraglutide's pediatric approvals are backed by dedicated pediatric studies — but those studies are smaller and shorter in duration than the adult trial base. Long-term metabolic and developmental outcomes in children aged 6 to under 12 are still accruing.


Safety signals

  • Gastrointestinal adverse events (nausea, vomiting, diarrhea, constipation): Most common adverse effects; particularly prominent at each upward titration step and typically attenuate over days. Reported across Phase III trials and the FDA label.
  • Thyroid C-cell tumors: Boxed warning based on rodent carcinogenicity studies at clinically relevant exposures. No confirmed cases in humans to date. Contraindicated in patients with personal or family history of medullary thyroid carcinoma or MEN2.
  • Pancreatitis: Rare (<1%); class-wide signal; contraindicated in active or recurrent pancreatitis; described in the FDA label and post-marketing data.
  • Gallbladder disease (cholecystitis): Increased risk, associated with rapid weight loss; class-wide signal; described in the FDA label.
  • Hypoglycemia risk with insulin or insulin secretagogues: Co-administration with insulin, sulfonylureas, or meglitinides materially increases hypoglycemia risk; described in the FDA label.
  • Altered oral drug absorption: Delayed gastric emptying may affect absorption of orally administered drugs; the FDA label describes warfarin, levothyroxine, oral antibiotics, and antiepileptics as clinically relevant contexts.
  • Mild resting heart rate elevation: A modest resting heart rate increase (~2–3 bpm) is a class effect observed across GLP-1 receptor agonist trials.
  • Injection-site reactions: More frequent than with once-weekly GLP-1 agents due to daily injection frequency; described in the FDA label.
  • Long-term pediatric safety in children aged 6–<12: Evidence base is a single dedicated trial; long-term metabolic and developmental outcomes in this younger age bracket are still accruing.
  • Cardiovascular outcomes in non-T2D, lower-risk populations: LEADER established MACE reduction in high-cardiovascular-risk type 2 diabetes patients; cardiovascular outcomes in lower-risk or non-diabetic populations are not established by dedicated trials.

Regulatory status

  • US (FDA): Prescription drug. Victoza approved January 2010 for type 2 diabetes (adults and pediatric patients ≥10 years). Saxenda approved December 2014 for chronic weight management (adults and adolescents 12–17 years). Generic liraglutide entered the US market in 2024 (Teva authorized generic of Victoza; Teva and Meitheal generic Saxenda launched 2025) — the first GLP-1 receptor agonist to go generic in the US.
  • EU (EMA): Authorized. Victoza (Novo Nordisk) authorized 2009; Saxenda authorized 2015 for parallel indications. Current authorization status should be verified against the current EMA product database.
  • UK (MHRA): Authorized per available sources; current status should be verified against the current MHRA database.
  • Canada (Health Canada): Authorized per available sources.
  • Australia (TGA): Authorized per available sources.
  • WADA: Liraglutide is not listed by name on the WADA Prohibited List per available sources; GLP-1 agonists are under rising WADA scrutiny given weight-management applications. Athletes in weight-category or endurance sports should consult their governing body.
  • Medicare Part D (US): Saxenda is excluded from Medicare Part D coverage for weight management; Victoza is covered for type 2 diabetes.

Mechanism

Liraglutide acts as an agonist at the GLP-1 receptor (GLP-1R), a class B G-protein-coupled receptor expressed in pancreatic islets, the central nervous system, the gastrointestinal tract, and cardiovascular tissue. Receptor activation increases cyclic AMP signaling, stimulating glucose-dependent insulin secretion from pancreatic beta cells and suppressing glucagon release from alpha cells. In the CNS, GLP-1R activation at hypothalamic and hindbrain satiety centers reduces appetite and food intake. Gastric emptying is delayed, contributing to postprandial glucose control and reduced caloric intake.

The structural modification distinguishing liraglutide from native GLP-1 involves two changes, as described by Knudsen and colleagues (Frontiers in Endocrinology, 2019): a lysine-to-arginine substitution at position 34 (GLP-1 numbering) that increases DPP-4 resistance, and a C-16 fatty acid (palmitic acid) chain attached at Lys-26 via a γ-glutamic acid spacer, enabling reversible non-covalent binding to albumin in plasma. Albumin binding slows renal clearance and protects against DPP-4 degradation, extending the half-life from approximately 2 minutes (native GLP-1) to approximately 13 hours — sufficient for once-daily subcutaneous dosing. Semaglutide uses a longer C-18 fatty diacid chain achieving tighter albumin affinity and a half-life of approximately one week, enabling once-weekly dosing.

The cardiovascular outcomes benefit demonstrated in LEADER is attributed to the combination of metabolic improvement and potential direct cardioprotective GLP-1R signaling in the heart and vasculature, though the precise mechanisms underlying MACE reduction remain under investigation.


Open questions

  • Long-term pediatric safety in younger children: The 2025 randomized trial (Fox and colleagues) extends evidence to children aged 6 to under 12, but long-term metabolic and developmental outcomes in this younger bracket are still accruing. The pediatric dataset remains smaller and shorter in duration than the adult trial base.
  • Generic equivalence in real-world practice: FDA bioequivalence approval supports the AB-rating of generic liraglutide, but comparative effectiveness and switching outcomes in real-world clinical practice have not yet matured as generics entered the market in 2024–2025.
  • Daily versus once-weekly dosing in specific populations: Whether any patient subgroups — for pharmacodynamic, tolerability, or other reasons — systematically benefit from daily liraglutide over once-weekly GLP-1 agents remains underexplored. STEP 8 addressed body weight in adults without diabetes but not all subgroup contexts.
  • Neuropsychiatric and neurodegenerative indications: Early signals in Alzheimer's disease and related cognitive indications are described in the available literature (the ELAD trial program is noted); liraglutide's shorter half-life may have mechanistic relevance for CNS indications relative to weekly agents. Results and full implications have not been individually extracted in this card.
  • Post-discontinuation metabolic outcomes beyond weight: Weight regain after stopping is well-documented from SCALE extension data. Less characterized are the trajectories of glycemic control, cardiovascular risk markers, and renal function after discontinuation — particularly in patients who stop after extended treatment.
  • Cardiovascular outcomes in non-T2D, lower-risk populations: LEADER established MACE reduction in type 2 diabetes patients with high cardiovascular risk. Whether the cardiovascular benefit extends to lower-risk populations or to patients treated for obesity without diabetes is not established by dedicated source-attached trials.

Related peptides

Liraglutide is part of the GLP-1 receptor agonist class. Closely related agents include semaglutide (a once-weekly GLP-1 analog with a longer C-18 fatty diacid chain and ~94% GLP-1 homology, producing greater weight loss than liraglutide in STEP 8), exenatide (the first GLP-1 agonist to reach market, derived from the Gila monster peptide exendin-4), and tirzepatide (a dual GIP/GLP-1 receptor agonist with the largest weight-loss effect size in the class to date). Dulaglutide is another once-weekly GLP-1 analog approved for type 2 diabetes.

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

Might changing the small chemical bridge that holds liraglutide's fat tail allow us to make versions that last a day, a week, or somewhere in between?

If true, patients could choose a dosing schedule that fits their life, and doctors could adjust how long the drug lasts based on a person's body chemistry without redesigning the whole drug

The hypothesis
The gamma-glutamic acid spacer between Lys-26 and the palmitoyl chain in liraglutide is the minimal necessary length for optimal albumin binding affinity, and shortening or lengthening this spacer by one glutamate unit would produce a graded series of half-lives suitable for personalized dosing intervals
Why it’s plausible
Liraglutide uses a gamma-glutamic acid spacer to distance the palmitoyl chain from the peptide backbone. The length and chemistry of this linker determine the conformational freedom of the acyl chain and thus its accessibility to albumin's fatty acid binding pockets. In related Novo Nordisk analogs (semaglutide uses a different linker chemistry), linker optimization was critical. However, a systematic single-unit spacer series has not been reported for liraglutide itself. The current gamma-glutamic acid spacer may represent a local optimum for 13-hour half-life, but patients vary in albumin levels, body weight, and injection-site physiology. A graded spacer library could yield analogs with 8-hour, 13-hour, and 24-hour half-lives from the same backbone
Why it matters
If true, it would demonstrate that half-life tuning in acylated peptides can be achieved through simple linker chemistry rather than backbone redesign. This would lower barriers to personalized peptide medicine, where dosing frequency is matched to patient lifestyle and pharmacokinetic phenotype rather than forcing all patients onto the same schedule
Plausibility.70
Novelty.40
Impact.50
Basis · grounding2 computed/notes
[1]
notePalmitoyl chain attached at Lys-26 via gamma-glutamic acid spacer; this specific linker chemistry enables reversible albumin binding and once-daily dosing
[2]
structureHigh complex confidence (ipTM 0.93) suggests the backbone structure is robust to peripheral modifications like spacer length changes
openupdated 2026-06-11

Might a specific bend in the middle of liraglutide change how the receptor sends signals inside the cell, compared to natural GLP-1 or other drugs?

If true, drug designers could tweak that bend to create GLP-1 drugs with fewer side effects or stronger weight loss, giving patients better options than the one-size-fits-all drugs available today

The hypothesis
Liraglutide's Val-8 to Ser-11 turn motif (DVSSY) adopts a non-canonical conformation in the GLP-1R-bound state that allosterically stabilizes the receptor's transmembrane domain in a distinct active-state geometry, contributing to its biased signaling profile relative to native GLP-1 and exendin-4
Why it’s plausible
The sequence DVSSY (positions 8-12) contains a beta-turn motif that differs between GLP-1 analogs. Exendin-4 has a different turn geometry and shows distinct biased signaling. The boltz-2 prediction gives high confidence for the complex (ipTM 0.93) but pLDDT 76.3 suggests some regional flexibility. The DVSSY segment is in the linker region between the N-terminal activation motif and the C-terminal alpha-helix that docks the receptor extracellular domain. Class B GPCR peptide binding involves large conformational changes where the extracellular domain acts as a clasp; subtle differences in the peptide turn could propagate to the transmembrane bundle. Liraglutide's specific signaling bias (favoring cAMP over arrestin relative to some exendin analogs) may originate here rather than solely from the N-terminus
Why it matters
If true, it would identify a specific structural element responsible for signaling bias in a major drug class. This would enable rational design of next-generation GLP-1 analogs with customized efficacy/side-effect profiles, for example maximizing weight loss while minimizing gastrointestinal effects or gallbladder-related adverse events
Plausibility.50
Novelty.60
Impact.60
Basis · grounding3 computed/notes
[1]
sequenceSequence HAEGTFTSDVSSYLEGQAAKEFIAWLVRGR contains DVSSY at positions 8-12; valine at position 8 is a known DPP-4 resistance substitution
[2]
structureboltz-2 complex pLDDT=76.3 indicates good but not perfect local structure confidence, consistent with a flexible turn region that may adopt multiple conformations
[3]
noteLiraglutide was engineered for DPP-4 resistance (Val-8 substitution) and half-life extension; signaling bias relative to native GLP-1 and exendin-4 is clinically observed but structurally unexplained
openupdated 2026-06-11

Might the way liraglutide sticks to albumin in the bloodstream help keep blood sugar stable when someone is very sick or after surgery?

If true, doctors might use liraglutide to prevent dangerous blood sugar spikes in hospitalized patients, a group that currently relies on insulin drips and frequent monitoring

The hypothesis
Liraglutide's albumin-binding palmitoyl conjugation at Lys-26 creates a circulating depot that buffers against acute interstitial peptide concentration drops during inflammatory states, making it uniquely protective against stress-hyperglycemia in critically ill patients compared to non-acylated GLP-1 analogs
Why it’s plausible
The palmitic acid chain at Lys-26 enables reversible albumin binding, extending half-life from ~2 minutes to ~13 hours. Albumin levels are maintained or even elevated during acute-phase responses, and albumin-bound drug represents a large circulating reservoir. During systemic inflammation or critical illness, capillary permeability increases and interstitial protein leakage occurs, but the high molar excess of albumin relative to drug means the bound fraction acts as a buffered depot. This pharmacokinetic feature is distinct from the mechanism of action (GLP-1R agonism) and has not been explicitly tested as a protective factor in stress-hyperglycemia
Why it matters
If true, it would explain why liraglutide (and other acylated GLP-1 analogs) might outperform native GLP-1 or short-acting DPP-4 inhibitors in perioperative or ICU settings where glycemic variability is dangerous. It would support repurposing evaluation for inpatient glucose management, a setting where current GLP-1 drugs are rarely used
Plausibility.50
Novelty.60
Impact.60
Basis · grounding1 paper · 1 computed/note
[1]
noteC-16 palmitic acid attached at Lys-26 via gamma-glutamic acid spacer enables reversible albumin binding, extending half-life from ~2 min to ~13 hours
[2]
paper
Reference context includes pathological stimuli and macrophage infiltration, suggesting inflammatory tissue environments where albumin buffering could matter
doi: 10.3389/fendo.2019.00155
openupdated 2026-06-11

Could the shortened end of liraglutide affect how the GLP-1 receptor is recycled inside cells, not just how strongly it turns on?

If this is true, drug developers could tune liraglutide-like drugs for longer or shorter receptor activation, which might help patients who stop responding well to current GLP-1 drugs over time

The hypothesis
The C-terminal arginine in the liraglutide backbone (position 30) contributes to GLP-1R binding affinity beyond the known N-terminal agonism motif, and its removal or substitution would produce a partial agonist with altered receptor internalization kinetics
Why it’s plausible
Native GLP-1 is amidated at the C-terminus (position 37 in the full peptide), but liraglutide truncates to 30 residues and terminates in a free arginine. The backbone sequence HAEGTFTSDVSSYLEGQAAKEFIAWLVRGR ends in GR. The high ipTM (0.93) and pLDDT (76.3) suggest a well-defined receptor interface, yet the C-terminal tail's role in this complex is underexplored. In class B GPCRs like GLP-1R, the C-terminal region of peptide ligands can influence receptor trafficking and arrestin recruitment independently of G-protein activation. A free C-terminal arginine in a truncated analog may engage distinct electrostatic interactions with the receptor extracellular domain or affect endosomal sorting
Why it matters
If true, it would mean the C-terminal chemistry of liraglutide is not merely a passive truncation but actively shapes receptor signaling bias. This could guide engineering of liraglutide variants with tailored internalization profiles for sustained vs. pulsatile signaling, relevant for optimizing metabolic efficacy versus tachyphylaxis
Plausibility.60
Novelty.40
Impact.50
Basis · grounding3 computed/notes
[1]
sequenceSequence HAEGTFTSDVSSYLEGQAAKEFIAWLVRGR is 30 aa, terminating in GR; native GLP-1 is 37 aa with C-terminal amidation
[2]
structureboltz-2/complex ipTM=0.9286, pLDDT=76.3 indicates high-confidence complex but does not resolve C-terminal tail contribution to binding kinetics
[3]
noteLiraglutide is 97% homologous to native GLP-1 with Lys-26 palmitoylation for half-life extension; the structural solution focused on DPP-4 resistance, not C-terminal function
openupdated 2026-06-11

Could the acidic environment around tumors make liraglutide less effective for cancer-related weight loss than for diabetes?

If true, we could redesign liraglutide to stay active in acidic tissues, potentially helping cancer patients maintain muscle and weight, or conversely design it to turn off in healthy tissue and on only in tumors

The hypothesis
Liraglutide's N-terminal histidine (position 1) and adjacent alanine (position 2) form a pH-sensitive switch that reduces GLP-1R activation in acidic tumor microenvironments, explaining its weaker efficacy in cancer cachexia versus diabetes despite high receptor expression
Why it’s plausible
The N-terminus of GLP-1 is critical for receptor activation. Liraglutide begins with HA (His-Ala). Histidine has a pKa near 6.0, meaning it shifts charge state between physiological pH (~7.4) and acidic environments (~6.5-6.8), such as tumor microenvironments or ischemic tissues. At lower pH, protonation of the histidine imidazole could alter the N-terminal conformation or its interaction with the receptor activation domain. GLP-1R is expressed on some cancer cells and cancer-associated fibroblasts, and GLP-1 analogs have been explored for cachexia. If the His-1 pH sensitivity acts as a natural dampener in acidic tissues, liraglutide would be less active where pH is low, potentially explaining variable tissue responses
Why it matters
If true, it would mean liraglutide carries an intrinsic pH-gated safety mechanism that limits activity in acidic pathological tissues. This would be relevant for cancer applications (where you might want the opposite) and would guide engineering of pH-resistant variants for cachexia or ischemia, or pH-sensitive variants for targeted tumor suppression
Plausibility.40
Novelty.70
Impact.50
Basis · grounding2 computed/notes
[1]
sequenceSequence begins HAEGTFTSDVSSYLEGQAAKEFIAWLVRGR; position 1 is histidine, position 2 is alanine; histidine pKa ~6.0 creates charge state difference between pH 7.4 and pH 6.5
[2]
noteLiraglutide shares 97% homology with native GLP-1; the N-terminal region is preserved and essential for receptor activation
details expand to inspect
full evidence table2 metrics
metricvaluetool
ipTM 0.9285981059074402 boltz-2
ranking score 0.7962026596069336 boltz-2
structural qualityopenfold3
metricvaluenote
gpde0.871global PDE — lower = better
disorderNaNfraction disordered
3-letter notation
His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg
chemical idInChIKey
YSDQQAXHVYUZIW-QCIJIYAXSA-N
recipeboltz-2 1.0
parametervalue
modelboltz-2 1.0
weights
hardwarenvidia_nim_api
mlx version
python
random seed
msa strategycolabfold_nvidia
diffusion samples1
runtime
predicted bymlx@peptide
predicted at2026-05-03
citationbibtex
peptidemodel (2026). Liraglutide: Victoza/Saxenda daily injection for diabetes & weight loss (pep-10868, v1). PeptideModel. https://peptidemodel.com/card/pep-10868
@peptide{pep10868,
  sequence = {HAEGTFTSDVSSYLEGQAAKEFIAWLVRGR},
  target   = {glp-1r},
  author   = {peptidemodel},
  year     = {2026},
  status   = {bioassayed}
}
related peptides 5 by signal overlap
clinical trials 537 on ct.gov · 167 on EUCTR · checked 2026-05-09
ct.gov trials 537
with results 147
EUCTR 167
PubMed RCT 491
by phase
1phase 13phase 22phase 31phase 43no phase
by status
4completed1recruiting2terminated3unknown
references 4 papers
[1]
The Discovery and Development of Liraglutide and Semaglutide
Knudsen Lotte Bjerre et al. Frontiers in Endocrinology 2019
primary
[2]
The pleiotropic effects of liraglutide in obesity-linked diseases
et al. European Journal of Clinical and Experimental Medicine 2025
supporting
[3]
Liraglutide and Cardiovascular Outcomes in Type 2 Diabetes
Marso, S. et al. New England Journal of Medicine 2016
supporting
[4] supporting
discussion no comments
sign in to comment
peptidemodel.com CC-BY-SA-4.0 research only · not for human use