Exenatide

Summary

Exenatide (CHEMBL414357) is an approved protein (ATC A10BJ01) targeting GLP1R; indicated across 23 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: A10BJ01
• Targets: 1 (GLP1R)
• Indications: 23 conditions
• Clinical trials: 215

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL414357
Name	Exenatide
Type	Protein
Max phase	4
ATC	A10BJ01

Also known as: AC 2993, AC-002993, AC-2993, AC-2993A, AC-2993LAR, AC002993, AC2993, AC2993A, Bydureon, Bydureon bcise, Bydureon pen, Byetta

Patent coverage: 7,005 distinct patent families (17,302 SureChEMBL compound mentions), from 4 matched compound structure(s). 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	Agonist	9.18	0.2%	P43220

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

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	10.8	EC50	0.02	nM	CHEMBL_ACT_22810112
GLP1R	10.28	Ki	0.05	nM	CHEMBL_ACT_24929142
GLP1R	10.21	EC50	0.06	nM	CHEMBL_ACT_24929057
GLP1R	10.04	Ki	0.09	nM	CHEMBL_ACT_24929138
GLP1R	10	EC50	0.1	nM	CHEMBL_ACT_3372828
GLP1R	9.96	EC50	0.11	nM	CHEMBL_ACT_24929073
P32301	9.85	IC50	0.14	nM	CHEMBL_ACT_3256493
GLP1R	9.4	IC50	0.4	nM	CHEMBL_ACT_24784019
GLP1R	9.22	EC50	0.6	nM	CHEMBL_ACT_24929065
GLP1R	9.18	IC50	0.66	nM	CHEMBL_ACT_2353537
GLP1R	8.22	IC50	5.98	nM	CHEMBL_ACT_22810156
GLP1R	8.05	EC50	9	nM	CHEMBL_ACT_24929128
GLP1R	7.85	EC50	14	nM	CHEMBL_ACT_24929120
GLP1R	7.6	EC50	25.12	nM	CHEMBL_ACT_24784085
GLP1R	7.3	EC50	50.12	nM	CHEMBL_ACT_24784107
GLP1R	6.1	EC50	794.3	nM	CHEMBL_ACT_24784063

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

23 indications (2 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	MONDO:0005148
myocardial infarction	3	MONDO:0005068	EFO:0000612
obesity disorder	3	MONDO:0011122	EFO:0001073
coronary artery disorder	3	MONDO:0005010	EFO:0001645
acute myocardial infarction	3	MONDO:0004781	EFO:0008583
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
Parkinson disease	3	MONDO:0005180	MONDO:0005180
morbid obesity	2	MONDO:0005139	EFO:0001074
hyperglycemia	2	MONDO:0002909	HP:0003074
metabolic dysfunction-associated steatotic liver disease	2	MONDO:0013209	EFO:0003095
stroke disorder	2	MONDO:0005098	EFO:0000712
polycystic ovary syndrome	2	MONDO:0008487	EFO:0000660
prediabetes syndrome	2	MONDO:0006920	EFO:1001121
multiple system atrophy	2	MONDO:0007803	EFO:1001050
alcohol abuse	2	MONDO:0002046	MONDO:0007079
cocaine dependence	1	MONDO:0005186	EFO:0002610
hyperinsulinemic hypoglycemia	1	MONDO:0005803	EFO:0007318
kidney failure	1	MONDO:0001106	HP:0000083

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

Clinical trials

Total trials: 215.

Phase distribution

Phase	Trials
PHASE4	70
PHASE3	49
Not specified	30
PHASE2	29
PHASE1	22
PHASE2/PHASE3	9
PHASE1/PHASE2	5
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05482789	PHASE4	RECRUITING	Exenatide Pharmacokinetics and Pharmacodynamics in Gestational Diabetes
NCT00353834	PHASE4	COMPLETED	The Effect of Exenatide Compared to Lantus Insulin on Vascular Function in Type 2 Diabetes
NCT00456885	PHASE4	COMPLETED	The Effect of Exenatide on Weight and Hunger in Obese, Healthy Women
NCT00477581	PHASE4	COMPLETED	A Study to Compare the Effects of Exenatide and Sitagliptin on Postprandial Glucose in Subjects With Type 2 Diabetes Mellitus
NCT00546728	PHASE4	COMPLETED	The Vascular Effects of Exenatide Versus Metformin in Patients With Pre-Diabetes
NCT00572689	PHASE4	WITHDRAWN	Pilot Study of Exenatide Pharmacokinetics and Pharmacodynamics in Gestational Diabetes
NCT00623545	PHASE4	COMPLETED	Bioenergetic Alterations After Exenatide Administration
NCT00667732	PHASE4	COMPLETED	How Glargine Insulin, Oral Diabetes Medications and Exenatide May Improve Blood Sugar Control and Weight Gain in Type 2 Diabetics
NCT00729326	PHASE4	COMPLETED	Comparison of the Effect of Exenatide Versus Sitagliptin on 24-hour Average Glucose in Patients With Type 2 Diabetes on Metformin or a Thiazolidinedione
NCT00736229	PHASE4	COMPLETED	Intravenous Exenatide in Coronary Intensive Care Unit (ICU) Patients
NCT00766857	PHASE4	COMPLETED	Effects of Exenatide in Type 2 Diabetic Patients With Congestive Heart Failure
NCT00799435	PHASE4	TERMINATED	Evaluating the Use of Exenatide in People With Type 2 Diabetes and Diastolic Heart Failure
NCT00835848	PHASE4	COMPLETED	Pharmacological Postconditioning to Reduce Infarct Size Following Primary PCI
NCT00845182	PHASE4	COMPLETED	Effect of Pioglitazone and Exenatide on Body Weight and Beta Cell Function
NCT00845507	PHASE4	COMPLETED	Exenatide for the Treatment of Weight Gain Associated With Olanzapine in Obese Adults
NCT00845559	PHASE4	WITHDRAWN	The Effects of Exenatide on Post-Meal Sugar Peaks and Vascular Health in Obese/Pre-Diabetic Young Adults
NCT00870194	PHASE4	COMPLETED	A Comparison of Adding Exenatide With Switching to Exenatide in Patients With Type 2 Diabetes Experiencing Inadequate Glycemic Control With Sitagliptin Plus Metformin
NCT00948168	PHASE4	COMPLETED	Effect of Exenatide on Glucose Homeostasis Determinants in Type 2 Diabetes
NCT00950677	PHASE4	COMPLETED	The Effect of Byetta and Symlin on Post-meal Meal Blood Sugar Levels in Children With Type 2 Diabetes
NCT00974272	PHASE4	COMPLETED	Effects of Exenatide on Postprandial Hyperlipidemia and Inflammation
NCT01006889	PHASE4	COMPLETED	Adding Exenatide to Insulin Therapy for Patients With Type 2 Diabetes and Non-Alcoholic Fatty Liver Disease
NCT01208649	PHASE4	COMPLETED	Effects of Exenatide (Byetta®) on Liver Function in Patients With Nonalcoholic Steatohepatitis (NASH)
NCT01235819	PHASE4	COMPLETED	Comparison Between GLP 1 Analogues and DPP 4 Inhibitors in Type 1 Diabetes Mellitus
NCT01269034	PHASE4	COMPLETED	New Onset Type 1 Diabetes: Role of Exenatide
NCT01269047	PHASE4	COMPLETED	Use of Exenatide and Pramlintide to Decrease Post-prandial Hyperglycemia
NCT01270191	PHASE4	UNKNOWN	The Effects of Short-Term Exenatide Therapy in Newly Diagnosed Type 2 Diabetic Patients
NCT01381926	PHASE4	TERMINATED	Changes in Bone Turnover With Exposure to a GLP-1 Receptor Agonist
NCT01432405	PHASE4	COMPLETED	Effect Of Exenatide Treatment on Liver Fat Content in Patients With Diabetes
NCT01435980	PHASE4	UNKNOWN	Study of Comparison the Treatment Effect Between Gastric Bypass and Exenatide in Type 2 Diabetes
NCT01524705	PHASE4	COMPLETED	FLuctuATion Reduction With inSULin and Glp-1 Added togetheR (FLAT-SUGAR)
NCT01588418	PHASE4	COMPLETED	Acute Effect of Exenatide on Brain Glucose Metabolism
NCT01590433	PHASE4	COMPLETED	Weight Loss With Exenatide Treatment
NCT01744236	PHASE4	COMPLETED	SAFEGUARD: Pleiotropic Effects of Incretin Based Therapies
NCT01791465	PHASE4	TERMINATED	Pilot Study of Bydureon to Treat Diabetes in HIV-infected Adults
NCT01818648	PHASE4	WITHDRAWN	Exenatide on GI Motor Function and Permeability in Short Bowel Syndrome
NCT01951651	PHASE4	COMPLETED	Effect of Exenatide on Liver and Heart Fat and Inflammation
NCT02058940	PHASE4	COMPLETED	Intravenous Exenatide in Patients With Acute Brain Injury
NCT02092597	PHASE4	COMPLETED	Safety Evaluation of Adverse Reactions in Diabetes
NCT02104739	PHASE4	COMPLETED	Effects of Antidiabetic Medications on the Postprandial State in Prediabetes
NCT02129985	PHASE4	UNKNOWN	Effect on Beta Cell Function and Glycaemic Control After Insulin and Exenatide Sequential Therapy

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
LIRAGLUTIDE	ChEMBL + PubChem	Phase 4 (approved)	GLP1R
DIHYDROERGOTAMINE	ChEMBL	Phase 4 (approved)	GLP1R
ELAGOLIX	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