Liraglutide

Summary

Liraglutide (CHEMBL4084119) is an approved protein glucagon-like peptide-1 receptor agonist (ATC A10BJ02) targeting GLP1R; indicated across 27 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: A10BJ02
• Targets: 1 (GLP1R)
• Indications: 27 conditions
• Clinical trials: 377
• Chemistry: 3751 Da · C172H265N43O51

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4084119
Name	Liraglutide
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	16134956
ChEBI	CHEBI:71193
ATC	A10BJ02
Molecular formula	C172H265N43O51
Molecular weight	3751
InChIKey	YSDQQAXHVYUZIW-QCIJIYAXSA-N

SMILES: CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC6=CN=CN6)N)C(=O)O

IUPAC name: (2S)-5-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-(hexadecanoylamino)-5-oxopentanoic acid

ChEBI definition: A lipopeptide that is an analogue of human GLP-1 in which the lysine residue at position 27 is replaced by arginine and a hexadecanoyl group attached to the remaining lysine via a glutamic acid spacer. Used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Pharmacological roles (ChEBI): glucagon-like peptide-1 receptor agonist, neuroprotective agent.

Also known as: Liraglutida, Liraglutide, Liraglutide (rdna origin), Liraglutide recombinant, NN-2211, NN-9924, NN2211, NN9924, Saxenda, Victoza, LIRAGLUTIDE, liraglutide

Patent coverage: 4,208 distinct patent families (10,473 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 10,469 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GLP1R	GLP-1 receptor	Full agonist	10.52	0.2%	P43220

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Glucagon-like peptide 1 receptor, MUS81-ECE1.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GLP1R	10.2	EC50	0.06	nM	CHEMBL_ACT_25940291
GLP1R	10.2	EC50	0.06	nM	CHEMBL_ACT_29092174
GLP1R	10.18	EC50	0.07	nM	CHEMBL_ACT_19243572
GLP1R	9.96	IC50	0.11	nM	CHEMBL_ACT_15712917
GLP1R	9.41	EC50	0.39	nM	CHEMBL_ACT_24929058
GLP1R	9.02	EC50	0.95	nM	CHEMBL_ACT_24929074
GLP1R	8.74	EC50	1.8	nM	CHEMBL_ACT_24929066
GLP1R	8.36	Ki	4.4	nM	CHEMBL_ACT_24929139
GLP1R	8.32	IC50	4.78	nM	CHEMBL_ACT_15713276
GLP1R	8.2	Ki	6.3	nM	CHEMBL_ACT_24929143
GLP1R	8.12	EC50	7.6	nM	CHEMBL_ACT_29092169
GLP1R	7.77	EC50	17	nM	CHEMBL_ACT_24929096
GLP1R	7.7	EC50	20	nM	CHEMBL_ACT_24929129
GLP1R	7.47	EC50	34	nM	CHEMBL_ACT_24929121
ECE1	5.93	IC50	1170	nM	CHEMBL_ACT_25482639
GLP1R	5.2	Kd	6270	nM	CHEMBL_ACT_24755228

Target pathways

Aggregated over 1 target gene(s): GLP1R.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
Glucagon-like Peptide-1 (GLP1) regulates insulin secretion	1	GLP1R
G alpha (s) signalling events	1	GLP1R
Glucagon-type ligand receptors	1	GLP1R

Dominant GO biological processes

GO term	Targets
cell surface receptor signaling pathway	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
activation of adenylate cyclase activity	1
positive regulation of cytosolic calcium ion concentration	1
learning or memory	1
regulation of heart contraction	1
post-translational protein targeting to membrane, translocation	1
negative regulation of blood pressure	1
positive regulation of blood pressure	1
hormone secretion	1
response to psychosocial stress	1
signal transduction	1
G protein-coupled receptor signaling pathway	1
regulation of biological quality	1
cellular response to glucagon stimulus	1

Indications & clinical

Indications

27 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
diabetes mellitus	4	MONDO:0005015	EFO:0000400
type 2 diabetes mellitus	4	MONDO:0005148	Orphanet:552
obesity disorder	4	MONDO:0011122	EFO:0001073
glucose intolerance	3	MONDO:0001076	EFO:0002546
hyperglycemia	3	MONDO:0002909	HP:0003074
diabetic kidney disease	3	MONDO:0005016	EFO:0000401
eating disorder	3	MONDO:0005451	EFO:0005203
prediabetes syndrome	3	MONDO:0006920	EFO:1001121
metabolic syndrome X	3	MONDO:0011565	EFO:0000195
major depressive disorder	3	MONDO:0002009	MONDO:0002009
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
bipolar disorder	3	MONDO:0004985	MONDO:0004985
polycystic ovary syndrome	3	MONDO:0008487	EFO:0000660
nutritional disorder	3	MONDO:0005137	EFO:0001069
delirium	3	MONDO:0045057	EFO:0009267
heart failure	2	MONDO:0005252	EFO:0003144
metabolic dysfunction-associated steatohepatitis	2	MONDO:0007027	EFO:1001249
short bowel syndrome	2	MONDO:0015183	MONDO:0015183
pouchitis	2	MONDO:0005312	EFO:0003921
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
Parkinson disease	2	MONDO:0005180	MONDO:0005180
sleep apnea syndrome	1	MONDO:0005296	EFO:0003877
opiate dependence	1	MONDO:0005530	EFO:0005611

4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 377.

Phase distribution

Phase	Trials
PHASE4	98
PHASE3	94
PHASE1	61
Not specified	60
PHASE2	49
PHASE2/PHASE3	6
PHASE1/PHASE2	5
EARLY_PHASE1	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02944500	PHASE4	ACTIVE_NOT_RECRUITING	Saxenda: Underlying Mechanisms and Clinical Outcomes
NCT03087032	PHASE4	RECRUITING	Liraglutide-bolus vs Glargine-bolus Therapy in Overweight/Obese Type 2 Diabetes Patients (LiraGooD)
NCT03856632	PHASE4	ACTIVE_NOT_RECRUITING	Liraglutide Effect in Atrial Fibrillation
NCT04575844	PHASE4	RECRUITING	Effects of Exercise and GLP-1 Agonism on Muscle Microvascular Perfusion and Insulin Action in Adults With Metabolic Syndrome
NCT05681299	PHASE4	RECRUITING	Effects of GH and Lirglutide on AgRP
NCT06438146	PHASE4	RECRUITING	LIROH - Liraglutide for Obesity in HIV
NCT06742710	PHASE4	RECRUITING	Liraglutide Treatment in Obese Infertile PCOS Women
NCT07244003	PHASE4	RECRUITING	Efficacy and Safety of the Met+SGLT-2i+GLP-1RA in Patients With Type 2 Diabetes With Poor Glycemic Control
NCT07301437	PHASE4	NOT_YET_RECRUITING	RWS of of Liraglutide Alone and in Combination With Orlistat for Weight Loss in Overweight/Obese Patients.
NCT01117350	PHASE4	COMPLETED	Efficacy Assessment of Insulin Glargine Versus LiraglutidE After Oral Agents Failure
NCT01394341	PHASE4	COMPLETED	Liraglutide Treatment to Patients With Severe Renal Insufficiency
NCT01455441	PHASE4	COMPLETED	The Effects of Physical Training and GLP-1 Receptor Agonist Liraglutide Treatment in Patients With Type 2 Diabetes
NCT01499108	PHASE4	COMPLETED	Time Course of the Blood Pressure Lowering Effect of Liraglutide Therapy in Type 2 Diabetes
NCT01505673	PHASE4	COMPLETED	Adding Liraglutide to High Dose Insulin: Breaking the Cycle
NCT01518101	PHASE4	COMPLETED	Vildagliptin Versus Liraglutide - Patient Preference After Receiving Both Medications
NCT01542242	PHASE4	TERMINATED	Liraglutide Use in Prader-Willi Syndrome
NCT01562678	PHASE4	COMPLETED	Liraglutide in Obesity and Diabetes: Identification of CNS Targets Using fMRI
NCT01592279	PHASE4	UNKNOWN	GLP-1 Analogue Treatment in Uncontrolled Type 1 Diabetic Patients
NCT01593137	PHASE4	WITHDRAWN	A Long-term Trial to Compare the Effects of Liraglutide and Sulphonylurea (Glimepiride) Both in Combination With Metformin on Clinical, Endothelial and Image Markers of Cardiovascular Risk in Patients With Type 2 Diabetes
NCT01595789	PHASE4	COMPLETED	The Effect of Liraglutide on the Treatment of Coronary Artery Disease and Type 2 Diabetes
NCT01597531	PHASE4	TERMINATED	Combinatorial Therapy for Peristent Type 2 Diabetes After Gastric Banding
NCT01612468	PHASE4	COMPLETED	Liraglutide in Type 1 Diabetes
NCT01638260	PHASE4	TERMINATED	GLP-1 and Non-exercise Activity Thermogenesis in RHZ
NCT01654120	PHASE4	COMPLETED	Study of Effectiveness of Liraglutide Added to High Dose Insulin in Type II Diabetics
NCT01664676	PHASE4	COMPLETED	Effects of Liraglutide on Kidney Function in Type 2 Diabetic Patients
NCT01695109	PHASE4	COMPLETED	The Influence of Liraglutide on the Reward Properties of Food: an fMRI Study on Healthy Volunteers
NCT01739049	PHASE4	COMPLETED	Influence of Appetite Related Hormones in Binge Eating Behaviour Among the Overweight and Obese
NCT01744236	PHASE4	COMPLETED	SAFEGUARD: Pleiotropic Effects of Incretin Based Therapies
NCT01755572	PHASE4	COMPLETED	Blood Pressure Outcomes With Liraglutide Therapy
NCT01761318	PHASE4	COMPLETED	Effect of Liraglutide on Cardiovascular Endpoints in Diabetes Mellitus Type 2 Patients
NCT01785043	PHASE4	COMPLETED	Differences in Endothelial Function Amongst Sitagliptin and Liraglutide Users
NCT01787916	PHASE4	COMPLETED	52 Week Trial of Liraglutide in Type 1 Diabetes
NCT01790308	PHASE4	UNKNOWN	Effect of Liraglutide Combined With Short-term CSII on Long-term Glycemic Remission and β Cell Function
NCT01795248	PHASE4	COMPLETED	The Impact of Liraglutide on Glucose Tolerance and the Risk of Type 2 Diabetes in Women With Previous Pregnancy-induced Diabetes
NCT01899430	PHASE4	COMPLETED	Polycystic Ovary Syndrome and Liraglutide
NCT01907854	PHASE4	COMPLETED	Efficacy and Safety of Switching From Sitagliptin to Liraglutide in Subjects With Type 2 Diabetes Not Achieving Adequate Glycaemic Control on Sitagliptin and Metformin
NCT01911468	PHASE4	COMPLETED	Polycystic Ovary Syndrome and Liraglutide as Add-on Therapy on Metformin
NCT01917656	PHASE4	COMPLETED	Efficacy and Safety of Liraglutide Versus Sulphonylurea Both in Combination With Metformin During Ramadan in Subjects With Type 2 Diabetes
NCT01919489	PHASE4	COMPLETED	Liraglutide Hospital Discharge Trial
NCT01931982	PHASE4	COMPLETED	Effect of Glucagon-like Peptide 1 (GLP-1) on Microvascular Myocardial Function in Patients With Type 2 Diabetes.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

17 molecules share ≥1 primary target. Top 17 by shared-target count:

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL	Phase 4 (approved)	GLP1R
ELAGOLIX	ChEMBL	Phase 4 (approved)	GLP1R
EXENATIDE	ChEMBL	Phase 4 (approved)	GLP1R
GLUCAGON	ChEMBL	Phase 4 (approved)	GLP1R
LOPERAMIDE	ChEMBL	Phase 4 (approved)	GLP1R
PERPHENAZINE	ChEMBL	Phase 4 (approved)	GLP1R
SECRETIN	ChEMBL	Phase 4 (approved)	GLP1R
SEMAGLUTIDE	ChEMBL	Phase 4 (approved)	GLP1R
TIRZEPATIDE	ChEMBL	Phase 4 (approved)	GLP1R
TOLVAPTAN	ChEMBL	Phase 4 (approved)	GLP1R
ORFORGLIPRON	ChEMBL	Phase 3	GLP1R
COTADUTIDE	ChEMBL	Phase 2	GLP1R
DANUGLIPRON	ChEMBL	Phase 2	GLP1R
DEVAZEPIDE	ChEMBL	Phase 2	GLP1R
GLP-1	ChEMBL	Phase 2	GLP1R
LOTIGLIPRON	ChEMBL	Phase 2	GLP1R
PF-06291874	ChEMBL	Phase 2	GLP1R