Exenatide is a glucagon-like peptide-1 (GLP-1) analog^Label. It functions to activate the GLP-1 receptor and increases insulin secretion, decrease glucagon secretion, and slow gastric emptying to improve glycemic control^Label. Exenatide was given FDA approval on April 28, 2005⁴.

Protein structure

Protein chemical formula

C₁₈₄H₂₈₂N₅₀O₆₀S

Protein average weight

4186.6 Da

Sequences

>Exenatide
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS

Download FASTA Format

Synonyms

Exenatida
Exenatide
Exenatide synthetic
Exendin 4
Exendin-4
Synthetic exendin-4

External IDs

AC 2993 / AC-002993 / AC-2993 / AC-2993A / AC-2993LAR / AC002993 / AC2993 / AC2993A / DA-3091 / ITCA-650 / LY-2148568 / LY2148568

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Bydureon	Injection, suspension, extended release	2 mg/0.65mL	Subcutaneous	AstraZeneca Pharmaceuticals LP	2014-09-08	Not applicable
Bydureon	Kit	2 mg/0.65mL	Subcutaneous	Amylin Pharmaceuticals, Llc.	2012-01-27	2018-01-31
Bydureon	Kit	2 mg/0.65mL	Subcutaneous	Amylin Pharmaceuticals, Llc.	2012-01-27	2018-01-31
Bydureon	Injection, powder, for suspension, extended release	2 mg	Subcutaneous	Astra Zeneca Ab	2011-06-17	Not applicable
Bydureon	Injection, powder, for suspension, extended release	2 mg	Subcutaneous	Astra Zeneca Ab	2011-06-17	Not applicable
Bydureon	Injection, powder, for suspension, extended release	2 mg	Subcutaneous	Astra Zeneca Ab	2011-06-17	Not applicable
Bydureon	Injection, powder, for suspension, extended release; Kit	2 mg	Subcutaneous	Astra Zeneca	2016-02-16	Not applicable
Bydureon	Injection, powder, for suspension, extended release	2 mg	Subcutaneous	Astra Zeneca Ab	2011-06-17	Not applicable
Bydureon		2 mg/0.65mL	Subcutaneous	AstraZeneca Pharmaceuticals LP	2015-02-01	Not applicable
BYDUREON BCise	Suspension, extended release	2 mg	Subcutaneous	Astra Zeneca	Not applicable	Not applicable

Additional Data Available

Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

UNII

9P1872D4OL

CAS number

141758-74-9

Pharmacology

Indication

Exenatide is indicated for improving glycemic control in adults with type 2 diabetes mellitus along with diet and exercise^Label.

Associated Conditions

Type 2 Diabetes Mellitus

Pharmacodynamics

When patients take exenatide the body's natural response to glucose is modulated^Label. More insulin and less glucagon are released in response to glucose, though in cases of hypoglycemia a normal amount of glucagon is released^Label. Exenatide also slows gastric emptying, leading to a slower and prolonged release of glucose into the systemic circulation^Label. Together these effects prevent hyper and hypoglycemia^Label.

Mechanism of action

Exenatide is a human glucacon-like peptide-1(GLP-1) receptor agonist^Label. By activating this receptor, insulin secretion is increased and glucagon secretion is decreased in a glucose dependant manner^Label. Exenatide also slows gastric emptying and decreases food intake^Label. These effects work synergistically to improve glycemic control by reducing the likelihood of hyper and hypoglycemia^Label.

Target	Actions	Organism
AGlucagon-like peptide 1 receptor	agonist	Humans

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Additional Data Available

Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available

Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Exenatide reaches a peak plasma concentration in 2.1 hours^Label. Because exenatide is administerd subcutaneously, the bioavailability is 1¹.

Volume of distribution

28.3L^Label.

Protein binding

Protein binding of exenatide has not been determined⁵.

Metabolism

Exenatide is filtered through the glomerulus before being degraded to smaller peptides and amino acids by dipeptidyl peptidase-4, metalloproteases, endopeptidase 24-11, amino proteases, and serine proteases^Label,3. It is currently believed that the metalloproteases are responsible for most of the degradation of exenatide³. Exenatide is metabolised to small peptides <3 amino acids in length by enzymes in the kidney².

Route of elimination

Exenatide is mainly eliminated by glomerular filtration followed by proteolysis before finally being eliminated in the urine^Label,2.

Half life

2.4 hours^Label

Clearance

9.1 L/hour^Label.

Toxicity

In animal studies, exenatide was associated with fetal deformities of ribs and vertebrae as well as slowed growth^Label. In humans, uncontrolled hyperglycemia can be associated with an up to 25% risk of miscarriage^Label. No human studies in pregnancy have been performed with exenatide and so exenatide should only be prescribed in pregnancy if the benefit to the mother and fetus outweigh the risks^Label. In mice, exenatide is excreted in the milk at a concentration 2.5% of the plasma concentration though this data may not be applicable to humans^Label. The effect of exenatide on breastfed infants is also unknown and so the risk and benefit of breastfeeding while taking exenatide must be weighed^Label. There is no data for the use of exenatide in pediatric patients^Label. Geriatric patients do not have different results for safety and efficacy of exenatide though caution should still be used in this group as they are at higher risk of renal impairment or other comorbidities that may affect the liklihood of adverse effects^Label. No dosage adjustments are necessary for patients with creatinine clearance ≥50mL/min, though prescribing to patients with creatinine clearance 30-50mL/min should be done cautiously^Label. Exenatide is not recommended for patients with creatinine clearance <30mL/min^Label. Hepatic impairment is not expected to affect clearance of exenatide though no studies have been performed to confirm this^Label.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
Unlock Additional Data
(R)-warfarin	Exenatide can cause an increase in the absorption of (R)-warfarin resulting in an increased serum concentration and potentially a worsening of adverse effects.
(S)-Warfarin	Exenatide can cause an increase in the absorption of (S)-Warfarin resulting in an increased serum concentration and potentially a worsening of adverse effects.
2,4-thiazolidinedione	The risk or severity of hypoglycemia can be increased when Exenatide is combined with 2,4-thiazolidinedione.
4-hydroxycoumarin	Exenatide can cause an increase in the absorption of 4-hydroxycoumarin resulting in an increased serum concentration and potentially a worsening of adverse effects.
5-(2-methylpiperazine-1-sulfonyl)isoquinoline	The therapeutic efficacy of Exenatide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline	7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Exenatide.
Acarbose	The risk or severity of hypoglycemia can be increased when Acarbose is combined with Exenatide.
Acebutolol	The therapeutic efficacy of Exenatide can be increased when used in combination with Acebutolol.
Acenocoumarol	Exenatide can cause an increase in the absorption of Acenocoumarol resulting in an increased serum concentration and potentially a worsening of adverse effects.
Acetazolamide	The therapeutic efficacy of Exenatide can be increased when used in combination with Acetazolamide.

Additional Data Available

Extended Description

Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

A severity rating for each drug interaction, from minor to major.

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Evidence Level

A rating for the strength of the evidence supporting each drug interaction.

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Action

An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions

Take before a meal. Inject subcutaneously within 60 minutes before morning and evening meals.

References

Synthesis Reference

Matthieu Giraud, Anne-Sophie Droz, Stephane Varray, El Djouhar Rekai, Marie-Helene Brichard, Daniel Latassa, Christine Devijver, Pascal Gilles, Jeanne-Marie Cauvin, Fernando Albericio, Marta Paradis Bas, "PROCESS FOR THE PRODUCTION OF EXENATIDE AND OF AN EXENATIDE ANALOGUE." U.S. Patent US20110046349, issued February 24, 2011.

US20110046349

General References

Gao W, Jusko WJ: Target-mediated pharmacokinetic and pharmacodynamic model of exendin-4 in rats, monkeys, and humans. Drug Metab Dispos. 2012 May;40(5):990-7. doi: 10.1124/dmd.111.042291. Epub 2012 Feb 15. [PubMed:22338110]
Copley K, McCowen K, Hiles R, Nielsen LL, Young A, Parkes DG: Investigation of exenatide elimination and its in vivo and in vitro degradation. Curr Drug Metab. 2006 May;7(4):367-74. [PubMed:16724926]
Liao S, Liang Y, Zhang Z, Li J, Wang J, Wang X, Dou G, Zhang Z, Liu K: In vitro metabolic stability of exendin-4: pharmacokinetics and identification of cleavage products. PLoS One. 2015 Feb 27;10(2):e0116805. doi: 10.1371/journal.pone.0116805. eCollection 2015. [PubMed:25723538]
FDA Drug Approval Package: Exenatide [Link]
FDA Pharmacology Review: Exenatide [Link]

External Links

KEGG Drug: D04121
PubChem Substance: 46509017
RxNav: 60548
ChEMBL: CHEMBL414357
Therapeutic Targets Database: DAP001038
PharmGKB: PA164749238
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Exenatide

ATC Codes

A10BJ01 — Exenatide

AHFS Codes

68:20.06 — Incretin Mimetics

FDA label

Download (1.34 MB)

MSDS

Download (22.2 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
0	Active Not Recruiting	Other	Alcohol Dependence / BMI >30 kg/m2 / Cessation, Smoking	1
0	Recruiting	Diagnostic	Insulinoma / Nesidioblastosis	1
1	Active Not Recruiting	Other	Dependence, Cocaine	1
1	Active Not Recruiting	Treatment	Parkinson's Disease (PD)	1
1	Completed	Not Available	Healthy Volunteers	1
1	Completed	Not Available	Insulin Resistance / Pre Diabetes / Pre-Diabetic	1
1	Completed	Basic Science	BMI >30 kg/m2	1
1	Completed	Basic Science	Healthy Volunteers	1
1	Completed	Basic Science	Type 2 Diabetes Mellitus	1
1	Completed	Diagnostic	The Methodology Assessment of Glucose Dependent Insulin Secretion	1
1	Completed	Other	Healthy Volunteers	1
1	Completed	Treatment	BMI >30 kg/m2	1
1	Completed	Treatment	Diabetes Mellitus	1
1	Completed	Treatment	Healthy Adult Male and Female Volunteers	1
1	Completed	Treatment	Healthy Volunteers	1
1	Completed	Treatment	Hyperinsulinemic Hypoglycemia	1
1	Completed	Treatment	Type 1 Diabetes Mellitus	1
1	Completed	Treatment	Type 2 Diabetes Mellitus	12
1	Completed	Treatment	Type2 Diabetes Mellitus	1
1	Completed	Treatment	Impaired kidney function	1
1	Not Yet Recruiting	Other	Type 2 Diabetes Mellitus	1
1	Suspended	Treatment	Alcohol Use Disorder (AUD)	1
1	Unknown Status	Treatment	Diabetes Mellitus	1
1, 2	Active Not Recruiting	Treatment	Type 1 Diabetes Mellitus	1
1, 2	Completed	Treatment	Euglycemia / Hyperglycemia / Hypoglycemia	1
1, 2	Completed	Treatment	Hypothalamic Obesity	1
1, 2	Completed	Treatment	Type 2 Diabetes Mellitus	1
1, 2	Not Yet Recruiting	Treatment	Autoimmune Diseases / Diabetes Mellitus / Hypoglycemia / Type 1 Diabetes Mellitus	1
1, 2	Recruiting	Treatment	Cessation, Smoking	1
1, 2	Terminated	Treatment	Type 2 Diabetes Mellitus	1
1, 2	Withdrawn	Treatment	Glucose Homeostasis / Health-Related Quality of Life / Inflammatory Reaction / Organ Dysfunction / Shock, Septic	1
2	Active Not Recruiting	Treatment	Alcohol Dependence / Alcohol Dependence, in Remission	1
2	Active Not Recruiting	Treatment	BMI >30 kg/m2	1
2	Active Not Recruiting	Treatment	Obesity, Severe	1
2	Completed	Treatment	BMI >27 kg/m2 / BMI >30 kg/m2 / Postsurgical craniopharyngioma	1
2	Completed	Treatment	BMI >30 kg/m2	3
2	Completed	Treatment	Diabetes Mellitus	1
2	Completed	Treatment	Diabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus	1
2	Completed	Treatment	Obesity, Morbid	1
2	Completed	Treatment	Parkinson's Disease (PD)	1
2	Completed	Treatment	Polycystic Ovaries Syndrome	1
2	Completed	Treatment	Stroke	1
2	Completed	Treatment	Type 1 Diabetes Mellitus	2
2	Completed	Treatment	Type 2 Diabetes Mellitus	13
2	Completed	Treatment	Type I Diabetes	1
2	Recruiting	Treatment	Acute Ischemic Stroke (AIS)	1
2	Recruiting	Treatment	Myocardial Infarction	1
2	Recruiting	Treatment	Parkinson's Disease (PD)	1
2	Recruiting	Treatment	Pre Diabetes / Pre-Diabetic	1
2	Recruiting	Treatment	Stroke, Ischemic	1
2	Terminated	Treatment	Alzheimer's Disease (AD) / Mild Cognitive Impairment (MCI)	1
2	Terminated	Treatment	Diabetes Complications / Fatty Liver	1
2	Terminated	Treatment	Diabetes Mellitus	1
2	Unknown Status	Treatment	Parkinson's Disease (PD)	1
2, 3	Active Not Recruiting	Other	BMI >30 kg/m2 / Hepatic Steatosis / Polycystic Ovarian Syndrome	1
2, 3	Completed	Not Available	(NAFLD) / Nonalcoholic Fatty Liver Disease	1
2, 3	Completed	Basic Science	Type 2 Diabetes Mellitus	1
2, 3	Completed	Treatment	Hypoglycemia / Type 1 Diabetes Mellitus	1
2, 3	Completed	Treatment	Stress Hyperglycaemia	1
2, 3	Enrolling by Invitation	Treatment	Type 1 Diabetes Mellitus	1
2, 3	Recruiting	Treatment	Quality of Life	1
2, 3	Recruiting	Treatment	Type 2 Diabetes Mellitus	1
2, 3	Unknown Status	Treatment	Obesity, Morbid	1
3	Active Not Recruiting	Treatment	BMI >30 kg/m2 / Polycystic Ovaries Syndrome	1
3	Active Not Recruiting	Treatment	Children and Adolescent With Type 2 Diabetes	1
3	Active Not Recruiting	Treatment	Hypothalamic Obesity	1
3	Active Not Recruiting	Treatment	ST Elevation Acute Myocardial Infarction	1
3	Active Not Recruiting	Treatment	Type 1 Diabetes Mellitus	1
3	Completed	Treatment	BMI >30 kg/m2 / Diabetes	1
3	Completed	Treatment	BMI >30 kg/m2 / Drug-induced Obesity / Metabolic Syndromes / Schizophrenia	1
3	Completed	Treatment	BMI >30 kg/m2 / Weight Loss	1
3	Completed	Treatment	Coronary Artery Disease / Decreased Left Ventricular Function	1
3	Completed	Treatment	Diabetes Mellitus	2
3	Completed	Treatment	Diabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus	2
3	Completed	Treatment	Diabetes / Type 2 Diabetes Mellitus	4
3	Completed	Treatment	Hypothalamic Obesity / Postsurgical craniopharyngioma	1
3	Completed	Treatment	Type 2 Diabetes Mellitus	46
3	Recruiting	Treatment	BMI >30 kg/m2	1
3	Recruiting	Treatment	Chronic Kidney Disease (CKD) / Left Ventricular Diastolic Dysfunction / Type 2 Diabetes Mellitus	1
3	Recruiting	Treatment	Cognitive Deficits / Dysglycaemia	1
3	Recruiting	Treatment	Parkinson's Disease (PD)	1
3	Recruiting	Treatment	Type 2 Diabetes Mellitus	1
3	Terminated	Treatment	BMI >30 kg/m2 / Type 2 Diabetes Mellitus	1
3	Terminated	Treatment	Type 2 Diabetes Mellitus	2
3	Unknown Status	Treatment	Patients With a First Acute Myocardial Infarction to be Treated With Primary Percutaneous Coronary Intervention (PCI)	1
3	Unknown Status	Treatment	Type 1 Diabetes Mellitus	1
3	Withdrawn	Treatment	Type 2 Diabetes Mellitus	3
4	Active Not Recruiting	Treatment	Diabetes	1
4	Active Not Recruiting	Treatment	Schizoaffective Disorders / Schizophrenia	1
4	Active Not Recruiting	Treatment	Type 2 Diabetes Mellitus	1
4	Completed	Basic Science	Diabetes / Impaired Glucose Tolerance	1
4	Completed	Basic Science	Type 2 Diabetes Mellitus	1
4	Completed	Diagnostic	Healthy Volunteers	1
4	Completed	Health Services Research	Type 2 Diabetes Mellitus	1
4	Completed	Prevention	Diabetic Nephropathies	1
4	Completed	Treatment	Acute Coronary Syndromes (ACS) / Hyperglycemia / Myocardial Infarction	1
4	Completed	Treatment	BMI >30 kg/m2	3
4	Completed	Treatment	BMI >30 kg/m2 / Impaired Glucose Tolerance	1
4	Completed	Treatment	BMI >30 kg/m2 / Pre-Diabetic	1
4	Completed	Treatment	Congestive Heart Failure / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Diabetes Mellitus / Human Immunodeficiency Virus (HIV) Infections	1
4	Completed	Treatment	Disorder of Glucose Regulation / Overweight and Obesity / Polycystic Ovaries Syndrome	1
4	Completed	Treatment	Healthy Volunteers	1
4	Completed	Treatment	Healthy Volunteers / Impaired Glucose Tolerance / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Impaired Glucose Tolerance	1
4	Completed	Treatment	Impaired Glucose Tolerance / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Myocardial Infarction	2
4	Completed	Treatment	Non-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Nonalcoholic Fatty Liver Disease	1
4	Completed	Treatment	Nonalcoholic Fatty Liver Disease / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Steatosis, Liver / Type2 Diabetes	1
4	Completed	Treatment	Type 1 Diabetes Mellitus	2
4	Completed	Treatment	Type 2 Diabetes Mellitus	20
4	Completed	Treatment	The Therapeutic Effect of Exenatide and Metformin / Type2 Diabetes	1
4	Completed	Treatment	Weight Gain	1
4	Not Yet Recruiting	Basic Science	BMI >30 kg/m2 / Type2 Diabetes	1
4	Not Yet Recruiting	Treatment	BMI >30 kg/m2 / Insulin Resistance / Pre Diabetes / Pre-Diabetic / Spinal Cord Injuries (SCI)	1
4	Not Yet Recruiting	Treatment	Coronary Endothelial Function	1
4	Not Yet Recruiting	Treatment	Evaluate Ketogenic Stress	1
4	Not Yet Recruiting	Treatment	Impaired Glucose Tolerance / Polycystic Ovarian Syndrome	1
4	Not Yet Recruiting	Treatment	Kidney Diseases / Type2 Diabetes	1
4	Not Yet Recruiting	Treatment	Type 2 Diabetes Mellitus	2
4	Recruiting	Basic Science	Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Atherosclerosis / Diabetes / Restenosis	1
4	Recruiting	Treatment	BMI >27 kg/m2 / BMI >30 kg/m2 / Polycystic Ovary Syndrome (PCOS)	1
4	Recruiting	Treatment	BMI >30 kg/m2	1
4	Recruiting	Treatment	BMI >30 kg/m2 / Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Injuries, Brain	1
4	Recruiting	Treatment	Polycystic Ovaries Syndrome	1
4	Recruiting	Treatment	Type 1 Diabetes Mellitus	1
4	Recruiting	Treatment	Type 2 Diabetes Mellitus	4
4	Terminated	Treatment	Diabetes Mellitus	1
4	Terminated	Treatment	Heart Failure, Diastolic / Type 2 Diabetes Mellitus	1
4	Terminated	Treatment	Type 2 Diabetes Mellitus	2
4	Unknown Status	Treatment	Type 2 Diabetes Mellitus	3
4	Withdrawn	Not Available	Gestational Diabetes Mellitus (GDM)	1
4	Withdrawn	Treatment	BMI >30 kg/m2 / Cardiovascular Heart Disease / Impaired Glucose Tolerance / Insulin Resistance	1
4	Withdrawn	Treatment	Short bowel condition / Short Bowel Syndrome (SBS)	1
4	Withdrawn	Treatment	Type 2 Diabetes Mellitus	1
Not Available	Completed	Not Available	BMI >30 kg/m2 / Diabetes Mellitus / Type 2 Diabetes Mellitus	1
Not Available	Completed	Not Available	Diabetic Nephropathies / Type 2 Diabetes Mellitus	1
Not Available	Completed	Not Available	Healthy Subjects (Treated With no Diabetes Therapies) / Type 2 Diabetes (Treated With Exenatide or Other Oral Antidiabetic Therapies)	1
Not Available	Completed	Not Available	Type 2 Diabetes Mellitus	10
Not Available	Completed	Basic Science	Diabetes	1
Not Available	Completed	Basic Science	Hyperlipidemias	1
Not Available	Completed	Basic Science	Type 2 Diabetes Mellitus	1
Not Available	Completed	Diagnostic	BMI >30 kg/m2 / Type 2 Diabetes Mellitus	1
Not Available	Completed	Other	Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Cardiac Arrest (CA) / Comatose	1
Not Available	Completed	Treatment	Diabetic Peripheral Neuropathy (DPN) / Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Glucocorticoid-induced Beta-cell Dysfunction / Glucocorticoid-induced Glucometabolic Abnormalities	1
Not Available	Completed	Treatment	Newly Diagnosed / Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Prader-Willi Syndrome	1
Not Available	Completed	Treatment	Pre-Diabetic / Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Psoriasis / Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Sleep Disordered Breathing (SDB) / Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Type 2 Diabetes Mellitus	2
Not Available	Not Yet Recruiting	Not Available	Type 2 Diabetes Mellitus in Obese	1
Not Available	Recruiting	Not Available	Type 2 Diabetes Mellitus	1
Not Available	Recruiting	Prevention	Incretinomimetics / Pancreas / Type 2 Diabetes Mellitus	1
Not Available	Recruiting	Treatment	Aortic Valve Disorder / Coronary Heart Disease (CHD) / Injuries, Brain / Renal Failure / Shock, Cardiogenic / Stroke	1
Not Available	Recruiting	Treatment	Type 2 Diabetes Mellitus	1
Not Available	Unknown Status	Treatment	BMI >30 kg/m2	1
Not Available	Unknown Status	Treatment	Diabetes Mellitus Associated With Genetic Syndrome / Wolfram Syndrome	1
Not Available	Unknown Status	Treatment	Diabetes Mellitus / Hypothalamic Obesity	1
Not Available	Unknown Status	Treatment	Heart Failure / Type 2 Diabetes Mellitus	1
Not Available	Unknown Status	Treatment	Prader-Willi Syndrome	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Amylin Pharmaceuticals
Baxter International Inc.
CP Pharmaceuticals Ltd.
Eli Lilly & Co.
Physicians Total Care Inc.

Dosage forms

Form	Route	Strength
Injection, powder, for suspension, extended release	Subcutaneous	2 mg
Injection, powder, for suspension, extended release; kit	Subcutaneous	2 mg
Injection, suspension, extended release	Subcutaneous	2 mg/0.65mL
Kit	Subcutaneous	2 mg/0.65mL
Injection, suspension, extended release	Subcutaneous	2 mg/0.85mL
Suspension, extended release	Subcutaneous	2 mg
Injection	Subcutaneous	250 ug/1mL
Injection, solution	Subcutaneous	10 micrograms
Injection, solution	Subcutaneous	5 micrograms
Solution	Subcutaneous	10 mcg
Solution	Subcutaneous	5 mcg

Prices

Unit description	Cost	Unit
Byetta 10 MCG Pen 10 mcg/0.04ml Solution 2.4ml Pen	324.23USD	pen
Byetta 5 mcg dose pen inj	316.76USD	ml
Byetta 5 MCG Pen 5 mcg/0.02ml Solution 1.2ml Pen	276.57USD	pen

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
Unlock Additional Data
US8216180	No	2012-07-10	2028-01-12
US8439864	No	2013-05-14	2028-03-25
US6667061	Yes	2003-12-23	2020-11-25
US6495164	No	2002-12-17	2020-05-25
US5424286	No	1995-06-13	2016-12-01
US6858576	No	2005-02-22	2017-01-06
US6872700	No	2005-03-29	2020-01-14
US6956026	No	2005-10-18	2018-01-07
US7741269	No	2010-06-22	2018-01-07
US7297761	No	2007-11-20	2017-10-15
US7521423	No	2009-04-21	2017-10-15
US6902744	No	2005-06-07	2020-01-14
US9238076	No	2016-01-19	2024-04-15
US8906851	No	2014-12-09	2026-08-18
US7612176	No	2009-11-03	2025-04-13
US8431685	No	2013-04-30	2025-04-13
US8461105	No	2013-06-11	2025-04-13
US8329648	No	2012-12-11	2026-08-18
US7456254	No	2008-11-25	2025-06-30
US7563871	No	2009-07-21	2024-04-15
US6824822	No	2004-11-30	2022-10-09
US6479065	No	2002-11-12	2020-08-10
US7223440	No	2007-05-29	2021-08-31
US8685934	No	2014-04-01	2030-05-26
US8501698	No	2013-08-06	2027-06-20
US6414126	No	2002-07-02	2020-10-04
US6515117	No	2003-02-04	2020-10-04
US6936590	No	2005-08-30	2020-10-04
US9198925	No	2015-12-01	2020-10-04
US7919598	No	2011-04-05	2029-12-16
US8361972	No	2013-01-29	2028-03-21
US8716251	No	2014-05-06	2028-03-21
US7851502	No	2010-12-14	2028-08-19
US8221786	No	2012-07-17	2028-03-21
US9320853	No	2016-04-26	2028-03-25
US8827963	No	2014-09-09	2029-02-04
US8712615	No	2014-04-29	2030-01-18
US8998876	No	2015-04-07	2030-01-07
US8758292	No	2014-06-24	2027-11-12
US8690837	No	2014-04-08	2029-05-19
US8895033	No	2014-11-25	2030-10-04
US8721615	No	2014-05-13	2030-01-18
US9884092	No	2018-02-06	2026-08-18

Additional Data Available

Filed On

The date on which a patent was filed with the relevant government.

Learn more

Properties

State

Solid

Experimental Properties

Property	Value	Source
isoelectric point	4.86	https://www.karger.com/Article/FullText/492409

Taxonomy

Description: Not Available
Kingdom: Organic Compounds
Super Class: Organic Acids
Class: Carboxylic Acids and Derivatives
Sub Class: Amino Acids, Peptides, and Analogues
Direct Parent: Peptides
Alternative Parents: Not Available
Substituents: Not Available
Molecular Framework: Not Available
External Descriptors: Not Available

Targets

Details1. Glucagon-like peptide 1 receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Transmembrane signaling receptor activity
Specific Function: This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name: GLP1R
Uniprot ID: P43220
Uniprot Name: Glucagon-like peptide 1 receptor
Molecular Weight: 53025.22 Da

References

Briones M, Bajaj M: Exenatide: a GLP-1 receptor agonist as novel therapy for Type 2 diabetes mellitus. Expert Opin Pharmacother. 2006 Jun;7(8):1055-64. [PubMed:16722815]
Hargrove DM, Kendall ES, Reynolds JM, Lwin AN, Herich JP, Smith PA, Gedulin BR, Flanagan SD, Jodka CM, Hoyt JA, McCowen KM, Parkes DG, Anderson CM: Biological activity of AC3174, a peptide analog of exendin-4. Regul Pept. 2007 Jun 7;141(1-3):113-9. Epub 2007 Jan 11. [PubMed:17292977]
Wajchenberg BL: beta-cell failure in diabetes and preservation by clinical treatment. Endocr Rev. 2007 Apr;28(2):187-218. Epub 2007 Mar 12. [PubMed:17353295]
Mack CM, Moore CX, Jodka CM, Bhavsar S, Wilson JK, Hoyt JA, Roan JL, Vu C, Laugero KD, Parkes DG, Young AA: Antiobesity action of peripheral exenatide (exendin-4) in rodents: effects on food intake, body weight, metabolic status and side-effect measures. Int J Obes (Lond). 2006 Sep;30(9):1332-40. Epub 2006 Mar 14. [PubMed:16534527]
Geelhoed-Duijvestijn PH: Incretins: a new treatment option for type 2 diabetes? Neth J Med. 2007 Feb;65(2):60-4. [PubMed:17379930]
Mann RJ, Nasr NE, Sinfield JK, Paci E, Donnelly D: The major determinant of exendin-4/glucagon-like peptide 1 differential affinity at the rat glucagon-like peptide 1 receptor N-terminal domain is a hydrogen bond from SER-32 of exendin-4. Br J Pharmacol. 2010 Aug;160(8):1973-84. doi: 10.1111/j.1476-5381.2010.00834.x. [PubMed:20649595]
Degn KB, Brock B, Juhl CB, Djurhuus CB, Grubert J, Kim D, Han J, Taylor K, Fineman M, Schmitz O: Effect of intravenous infusion of exenatide (synthetic exendin-4) on glucose-dependent insulin secretion and counterregulation during hypoglycemia. Diabetes. 2004 Sep;53(9):2397-403. [PubMed:15331551]
Diamant M, Bunck MC, Heine RJ: [Analogs of glucagon-like peptide-1 (GLP-1): an old concept as a new treatment of patients with diabetes mellitus type 2]. Ned Tijdschr Geneeskd. 2004 Sep 25;148(39):1912-7. [PubMed:15495988]
Kolterman OG, Kim DD, Shen L, Ruggles JA, Nielsen LL, Fineman MS, Baron AD: Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus. Am J Health Syst Pharm. 2005 Jan 15;62(2):173-81. [PubMed:15700891]
Barnett AH: Exenatide. Drugs Today (Barc). 2005 Sep;41(9):563-78. [PubMed:16341288]
Lebovitz HE: Therapeutic options in development for management of diabetes: pharmacologic agents and new technologies. Endocr Pract. 2006 Jan-Feb;12 Suppl 1:142-7. [PubMed:16627399]
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Enzymes

Details1. Dipeptidyl peptidase 4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Virus receptor activity
Specific Function: Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
Gene Name: DPP4
Uniprot ID: P27487
Uniprot Name: Dipeptidyl peptidase 4
Molecular Weight: 88277.935 Da

References

Liao S, Liang Y, Zhang Z, Li J, Wang J, Wang X, Dou G, Zhang Z, Liu K: In vitro metabolic stability of exendin-4: pharmacokinetics and identification of cleavage products. PLoS One. 2015 Feb 27;10(2):e0116805. doi: 10.1371/journal.pone.0116805. eCollection 2015. [PubMed:25723538]

Carriers

Details1. Serum albumin

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Toxic substance binding
Specific Function: Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name: ALB
Uniprot ID: P02768
Uniprot Name: Serum albumin
Molecular Weight: 69365.94 Da

References

Chae SY, Jin CH, Shin JH, Son S, Kim TH, Lee S, Youn YS, Byun Y, Lee MS, Lee KC: Biochemical, pharmaceutical and therapeutic properties of long-acting lithocholic acid derivatized exendin-4 analogs. J Control Release. 2010 Mar 3;142(2):206-13. doi: 10.1016/j.jconrel.2009.10.025. Epub 2009 Nov 10. [PubMed:19900495]

Drug created on May 16, 2007 14:43 / Updated on May 25, 2020 23:44