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Penggambaran struktur ideal untuk Liraglutide

Konformer ideal yang dibangun dari urutan; bukan struktur eksperimental atau prediksi.

Sekilas

ENTRY TYPE
approved drug
IDENTITY
Sequence verified

No structure asset recorded

TOP EVIDENCE
Grade A — Glycemic control (T2D)
MAJOR STATUS
Jurisdiction-specific — see status table
SPORT
Prohibited — as of 2026-08-06
VERIFIED
2026-08-06

Bottom line

Liraglutide is a once-daily with a C16 palmitoyl fatty acid side chain for non-covalent albumin binding. Approved as Victoza for T2D (2010) and Saxenda for chronic weight management (2014), it was the first GLP-1 RA to demonstrate cardiovascular benefit in a dedicated outcomes trial. The LEADER trial (N=9,340) showed a 13% reduction in 3-point MACE. The first generic liraglutide was approved in 2024. It also holds the distinction of being the first GLP-1 RA approved for adolescent weight management (2020).

Identity and composition

FieldVerified information
Preferred nameLiraglutide
Key aliasesVictoza, Saxenda, NN 2211
Molecular/sequence identity31-amino-acid human GLP-1 analog with a palmitoyl side chain: H-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(γ-Glu-palmitoyl)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH
Modifications/formArg³⁴→Lys substitution; a palmitoyl (C16) fatty acid linked via a γ-glutamyl spacer to the Lys²⁶ side chain; DPP-IV resistant through its albumin-binding self-assembly rather than sequence modification
Stable identifiers: 16134956; CAS: 204656-20-2; DrugBank: DB06655; UNII: 839I73S42A
Identity caveatsDistinguish from semaglutide (C18 fatty diacid, once-weekly); the molecular weight (3,751 Da) and fatty acid length differ

Development and approval status

JurisdictionStatus and indicationProduct/sourceAs of
US (FDA)Approved Jan 2010 for T2D glycemic controlVictoza (NDA 022341)2026-08-06
US (FDA)Approved Dec 2014 for chronic weight management (BMI ≥30 or ≥27 + comorbidity)Saxenda (NDA 206321)2026-08-06
US (FDA)CV risk reduction label expansion Aug 2017 (adults with T2D + established CVD)Victoza label update (based on LEADER)2026-08-06
US (FDA)Approved for adolescent weight management (12–17 yr) Dec 2020Saxenda2026-08-06
US (FDA)First generic liraglutide approved Feb 2024Multiple manufacturers2026-08-06
EU (EMA)Approved Jul 2009 (Victoza), Mar 2015 (Saxenda)Victoza, Saxenda2026-08-06
Status is multi-axis
Liraglutide authorization and sport-status profileFour medicine-authorization axes reproduce only documented status rows; sport status is shown separately.UNITED STATES5 status rows — see tableApproved Jan 2010 for T2DSOURCE / AS OFROW 1 / 2026-08-06EU/EEAApproved Jul 2009 (Victoza),Mar 2015 (Saxenda)SOURCE / AS OFROW 6 / 2026-08-06UNITED KINGDOMSOURCE ROW OMITTEDSEE AUDIT REASONSOURCE / AS OFNOT PRESENT / NOT RECORDEDOTHER DOCUMENTEDSOURCE ROW OMITTEDSEE AUDIT REASONSOURCE / AS OFNOT PRESENT / NOT RECORDEDSPORT STATUS — SEPARATE FROM MEDICINE AUTHORIZATIONWADA: GLP-1 receptor agonists are not prohibited. Not on the WADA Prohibited List.
Authorization belongs to the named product, use, place, and date; sport status is independent.
Alternatif teks
UNITED STATES
US (FDA): Approved Jan 2010 for T2D glycemic control; US (FDA): Approved Dec 2014 for chronic weight management (BMI ≥30 or ≥27 + comorbidity); US (FDA): CV risk reduction label expansion Aug 2017 (adults with T2D + established CVD); US (FDA): Approved for adolescent weight management (12–17 yr) Dec 2020; US (FDA): First generic liraglutide approved Feb 2024
EU/EEA
EU (EMA): Approved Jul 2009 (Victoza), Mar 2015 (Saxenda)
UNITED KINGDOM
No UNITED KINGDOM row is present in the source status table
OTHER DOCUMENTED
No OTHER DOCUMENTED row is present in the source status table

Sport status: WADA: GLP-1 receptor agonists are not prohibited. Not on the WADA Prohibited List.

Mechanism and pharmacology

Liraglutide is a human GLP-1 analog with 97% sequence homology to native GLP-1. The addition of a C16 palmitoyl fatty acid chain covalently bound via a γ-glutamyl spacer at Lys²⁶ promotes non-covalent albumin binding and self-association into heptamers, slowing absorption from the depot and reducing renal clearance. The plasma is approximately 13 hours, enabling once-daily SC dosing. Liraglutide activates the GLP-1 receptor with similar potency to native GLP-1, increasing glucose-dependent insulin secretion, suppressing glucagon, slowing gastric emptying, and reducing appetite via central hypothalamic GLP-1 receptors (Drucker, Cell Metab 2018).

Evidence by claim

Claim/indicationStageGradeBest human evidenceMain resultImportant limitations
Glycemic control (T2D)ApprovedALEAD program (6 trials, >4,000 pts)HbA1c reduction 1.0–1.5%; 40–50% achieved HbA1c <7%Comparator-dependent; vs , sulfonylureas, insulin
CV risk reduction (T2D+CVD)Approved [1]ALEADER (N=9,340; median 3.8 yr)3-point MACE HR 0.87 (0.78–0.97); CV death HR 0.78Required established CVD/high risk; generalizability to lower-risk patients unclear
Chronic weight management (adults)ApprovedASCALE program (obesity, prediabetes, OSA)Mean weight loss 8.0–9.2% vs 2.6% placebo; 63% achieved ≥5% lossGI dropouts; Saxenda label only for ≥1 weight-related comorbidity
Adolescent weight managementApprovedASCALE Teens (N=251, 12–17 yr)BMI reduction 4.6% vs 0.6%; −1.66 BMI unit differenceSmall N; no long-term safety data in adolescents
Prediabetes preventionNot approvedBSCALE prediabetes (3-yr extension)66% reduction in progression to T2D vs 2.6% placeboSecondary analysis; not an approved indication
Tingkat bukti
  • AKelas A: Mapan untuk penggunaan berlabel tertentu
  • BKelas B: Bukti manusia moderat
  • CKelas C: Bukti manusia awal
  • DKelas D: Hanya praklinis
  • EKelas E: Klaim anekdot/pemasaran
  • XKelas X: Bukti bertentangan atau tidak mendukung klaim
Pelajari lebih lanjut tentang penilaian bukti
Claim-evidence profile
Liraglutide claim-evidence profileA: 4 claims; B: 1 claim; C: 0 claims; D: 0 claims; E: 0 claims; X: 0 claimsCONTRADICTORY / NON-SUPPORTIVEA — Established for a specific labeled useGrade A: Established for a specific labeled use — current approval plus adequate controlled trials and post-market context.4 claimsGlycemic control (T2D)CV risk reduction (T2D+CVD)+2 moreB — Moderate human evidenceGrade B: Moderate human evidence — multiple controlled studies or a strong pivotal study, but no current approval for the claim.1 claimPrediabetes preventionC — Preliminary human evidenceGrade C: Preliminary human evidence — small, uncontrolled, surrogate-endpoint, or early-phase studies.0 claimsD — Preclinical onlyGrade D: Preclinical only — in vitro or animal evidence with no adequate human efficacy evidence.0 claimsE — Anecdotal/marketing claimGrade E: Anecdotal/marketing claim — testimonials, extrapolation, or vendor claims without adequate scientific support.0 claimsX — Evidence contradicts or does not support the claimGrade X: Evidence contradicts or does not support the claim — adequate negative evidence, failed program, or claim inconsistent with the studied material.0 claims
This counts the page's claim rows; it does not average them into a score. All claims: Glycemic control (T2D); CV risk reduction (T2D+CVD); Chronic weight management (adults); Adolescent weight management; Prediabetes prevention.
Alternatif teks

Text alternative for the claim-evidence diagram. Each grade is defined below:

AEstablished for a specific labeled use
4 claims: Glycemic control (T2D); CV risk reduction (T2D+CVD); Chronic weight management (adults); Adolescent weight management
BModerate human evidence
1 claim: Prediabetes prevention
CPreliminary human evidence
0 claims
DPreclinical only
0 claims
EAnecdotal/marketing claim
0 claims
XEvidence contradicts or does not support the claim
0 claims
United StatesApproved Jan 2010 for T2D glycemic controlApproved Dec 2014 for chronic weight management (BMI ≥30 or ≥27 + comorbidity)CV risk reduction label expansion Aug 2017 (adults with T2D + established CVD)Approved for adolescent weight management (12–17 yr) Dec 2020First generic liraglutide approved Feb 2024
EU/EEAApproved Jul 2009 (Victoza), Mar 2015 (Saxenda)

Key studies

StudyDesign/populationExposure studiedEndpoints and resultLimitations
LEADER; Marso et al., NEJM 2016; PMID: 27295427CVOT; N=9,340 T2D + high CV risk; median 3.8 yr [1]Liraglutide 1.8 mg daily (Victoza) vs 3-point MACE HR 0.87 (0.78–0.97); CV death HR 0.78 (0.66–0.93); all-cause death HR 0.85 (0.74–0.97); on top of standard care; very high comparator use of statins and antiplatelet agents
SCALE Obesity; Pi-Sunyer et al., NEJM 2015; PMID: 26132939; N=3,731 adults with BMI ≥30 or ≥27 + comorbidity; 56 wk [1]Liraglutide 3.0 mg SC daily (Saxenda) vs placeboMean weight loss −8.4% vs −2.8%; 63.2% vs 27.1% achieved ≥5%; 33.1% vs 10.6% achieved ≥10%High discontinuation rate (35% liraglutide, 40% placebo); lifestyle modification in both arms
SCALE Prediabetes; le Roux et al., Lancet 2017; PMID: 28126352RCT with 3-yr extension; N=2,254 with prediabetes [1]Liraglutide 3.0 mg daily vs placebo66% reduction in T2D onset (HR 0.34, 0.22–0.53); sustained weight loss at 3 yrOpen-label extension; high loss to follow-up
SCALE Teens; Kelly et al., NEJM 2020; PMID: 33147628RCT; N=251 adolescents 12–17 yr with obesity; 56 wk [1]Liraglutide 3.0 mg vs placeboBMI change −4.6% vs −0.6% (difference −4.4%); GI events 80% vs 54%Small sample; no data on weight maintenance after discontinuation
ELIXA comparisonSee lixisenatide monograph; liraglutide LEADER was 3rd CVOT after ELIXA (lixisenatide, neutral) and prior to SUSTAIN-6 (semaglutide, positive)LEADER was the first positive GLP-1 RA CVOT

Dose and administration evidence

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

The entries summarize the cited US FDA labels for the named products and their distinct approved indications.

Studied regimens (not recommendations)

  • Doses up to 3.0 mg daily in weight management trials (Saxenda).

  • No studied regimen exceeds 3.0 mg daily.

What is not established

  • Efficacy for weight management without lifestyle intervention.

  • Long-term (≥5 year) weight maintenance.

  • Effectiveness of generic liraglutide bioequivalence versus reference product in clinical outcomes (approved via ANDA pathway based on ).

Safety

Established label risks

  • Boxed warning: Thyroid C-cell tumors. Rodent studies showed dose-dependent C-cell hyperplasia and carcinoma; human relevance uncertain. Contraindicated in patients with personal/family history of MTC or MEN 2.

  • Gastrointestinal: Nausea (40–50%), vomiting, diarrhea, constipation. Most events during titration.

  • Pancreatitis: Postmarketing cases of acute pancreatitis; discontinue if suspected.

  • Acute kidney injury: In context of severe GI effects causing volume depletion.

  • Cholelithiasis: Increased risk, especially with substantial weight loss.

  • Heart rate increase: Mean +2–3 bpm; clinical significance unclear.

  • Hypoglycemia: Low risk as monotherapy; increased with sulfonylurea or insulin.

Human-study signals

  • LEADER: liraglutide associated with 36% increase in gallbladder-related events (HR 1.36, 1.14–1.62).

  • LEADER: no increase in pancreatitis (0.4% vs 0.5%), pancreatic cancer (0.3% vs 0.3%).

  • Injection-site reactions reported in 0.5–1% across trials.

Unknowns and product-quality risks

  • Human thyroid C-cell tumor risk is not excluded despite no signal in LEADER (N=9,340, limited follow-up).

  • Birth defect risk: Animal studies show early embryonic death and structural abnormalities; the 2026 Saxenda label removed pregnancy from contraindications and says to discontinue when pregnancy is recognized.

  • Generic liraglutide (2024) requires post-marketing pharmacovigilance for equivalence in immunogenicity.

Interactions and special populations

  • Slows gastric emptying, which may affect absorption of oral medications.

  • Insulin or sulfonylurea coadministration increases hypoglycemia risk.

  • Renal impairment: No dose adjustment for mild/moderate; limited experience with severe (eGFR <30) or ESRD.

  • Hepatic impairment: No dose adjustment; limited data in severe impairment.

  • Pregnancy: May cause fetal harm. The 2026 Saxenda label removed pregnancy from contraindications; discontinue when pregnancy is recognized. The two-month washout recommendation belongs to semaglutide, not liraglutide.

Regulatory, compounding, and sport notes

Evidence gaps

  • Long-term (≥10 year) safety data for weight management

  • Comparative effectiveness vs semaglutide 2.4 mg and tirzepatide for obesity

  • CV outcomes in patients without T2D (LEADER included only T2D)

  • Pediatric safety data beyond 1 year

  • Data in patients with T2D and eGFR <30 mL/min

  • Immunogenicity profile of generic formulations vs reference product

Search notes

Sources

  1. Marso SP et al. Liraglutide and cardiovascular outcomes in type 2 diabetes (LEADER). N Engl J Med. 2016;375(4):311-322. PMID: 27295427. https://doi.org/10.1056/NEJMoa1603827

  2. Pi-Sunyer X et al. A randomized, controlled trial of 3.0 mg of liraglutide in weight management (SCALE). N Engl J Med. 2015;373(1):11-22. PMID: 26132939. https://doi.org/10.1056/NEJMoa1411892

  3. Kelly AS et al. A randomized trial of liraglutide for obesity in adolescents (SCALE Teens). N Engl J Med. 2020;382(22):2117-2128. PMID: 33147628. https://doi.org/10.1056/NEJMoa1916038

  4. FDA. Victoza (liraglutide) injection label. NDA 022341. DailyMed. Accessed 2026-08-06. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5a9ef4ea-c76a-4d34-a604-27c5b505f5a4

  5. FDA. Saxenda (liraglutide) injection label. NDA 206321. DailyMed. Accessed 2026-08-06. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3946d389-0926-4f77-a708-0acb8153b143

  6. Drucker DJ. Mechanisms of action and therapeutic application of GLP-1 and GIP receptor agonists. Cell Metab. 2018;27(4):740-756. PMID: 29617641. https://doi.org/10.1016/j.cmet.2018.03.001

  7. le Roux CW et al. 3-year liraglutide effect on prediabetes progression (SCALE). Lancet. 2017;389(10077):1399-1409. PMID: 28126352. https://doi.org/10.1016/S0140-6736(17)30069-7

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Pertanyaan

What is liraglutide approved for?

Liraglutide is FDA-approved as Victoza (2010) for T2D glycemic control and as Saxenda (2014) for chronic weight management. It also carries a CV risk reduction label (2017, based on LEADER) and is approved for adolescent weight management ages 12–17 (2020).

What is liraglutide and how does it work?

Liraglutide is a 31-amino-acid GLP-1 analog with 97% sequence homology to native GLP-1. A C16 palmitoyl fatty acid chain promotes non-covalent albumin binding, extending its action for daily administration. It activates the GLP-1 receptor, increasing glucose-dependent insulin secretion, suppressing glucagon, slowing gastric emptying, and reducing appetite via central hypothalamic GLP-1 receptors.

What does the evidence show for liraglutide and cardiovascular outcomes?

The LEADER trial (n=9,340, T2D with high CV risk, median 3.8 years) showed a 13% reduction in 3-point MACE (HR 0.87) and an HR of 0.78 for CV death — the first positive CVOT for a GLP-1 RA. Generalizability to lower-risk patients is unclear as the trial required established CVD or high risk.

Is liraglutide the same as semaglutide?

No. Both are GLP-1 RAs but differ in molecular structure (C16 palmitoyl for liraglutide vs C18 fatty diacid for semaglutide) and administration frequency (daily vs weekly). They are not interchangeable; comparative effectiveness for obesity has not been established in a dedicated trial.

What are the main safety concerns with liraglutide?

FDA boxed warning for thyroid C-cell tumors (rodent data). Common GI effects (nausea 40–50%). LEADER found increased gallbladder-related events (HR 1.36). Pancreatitis and acute kidney injury are rare but labeled. Heart rate increase (~2–3 bpm) observed. Hypoglycemia risk increases with sulfonylurea or insulin coadministration.

Is liraglutide available as a generic?

Yes. The first generic liraglutide was approved by the FDA in February 2024 via the ANDA pathway, with multiple manufacturers. The generic was approved based on pharmacokinetic bioequivalence rather than clinical outcome studies. Post-marketing pharmacovigilance for immunogenicity equivalence is ongoing.

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