Identification

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Name
Exenatide
Accession Number
DB01276
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
Description

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

Protein structure
Db01276
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
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BydureonInjection, powder, for suspension, extended release2 mgSubcutaneousAstra Zeneca Ab2011-06-17Not applicableEu
BydureonInjection, powder, for suspension, extended release2 mgSubcutaneousAstra Zeneca Ab2011-06-17Not applicableEu
BydureonInjection, powder, for suspension, extended release; Kit2 mgSubcutaneousAstra Zeneca2016-02-16Not applicableCanada
BydureonKit2 mg/0.65mLSubcutaneousAmylin Pharmaceuticals, Llc.2012-01-272018-01-31Us
BydureonInjection, powder, for suspension, extended release2 mgSubcutaneousAstra Zeneca Ab2011-06-17Not applicableEu
BydureonKit2 mg/0.65mLSubcutaneousAstraZeneca Pharmaceuticals LP2015-02-01Not applicableUs
BydureonKit2 mg/0.65mLSubcutaneousAmylin Pharmaceuticals, Llc.2012-01-272018-01-31Us
BydureonInjection, powder, for suspension, extended release2 mgSubcutaneousAstra Zeneca Ab2011-06-17Not applicableEu
BydureonInjection, suspension, extended release2 mg/0.65mLSubcutaneousAstraZeneca Pharmaceuticals LP2014-09-08Not applicableUs
BYDUREON BCiseSuspension, extended release2 mgSubcutaneousAstra ZenecaNot applicableNot applicableCanada
Additional Data Available
  • Application Number
    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
    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 exerciseLabel.

Associated Conditions
Pharmacodynamics

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

Mechanism of action

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

TargetActionsOrganism
AGlucagon-like peptide 1 receptor
agonist
Humans
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 hoursLabel. Because exenatide is administerd subcutaneously, the bioavailability is 11.

Volume of distribution

28.3LLabel.

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 proteasesLabel,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 urineLabel,2.

Half life

2.4 hoursLabel

Clearance

9.1 L/hourLabel.

Toxicity

In animal studies, exenatide was associated with fetal deformities of ribs and vertebrae as well as slowed growthLabel. In humans, uncontrolled hyperglycemia can be associated with an up to 25% risk of miscarriageLabel. 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 risksLabel. 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 humansLabel. The effect of exenatide on breastfed infants is also unknown and so the risk and benefit of breastfeeding while taking exenatide must be weighedLabel. There is no data for the use of exenatide in pediatric patientsLabel. 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 effectsLabel. 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 cautiouslyLabel. Exenatide is not recommended for patients with creatinine clearance <30mL/minLabel. Hepatic impairment is not expected to affect clearance of exenatide though no studies have been performed to confirm thisLabel.

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.
DrugInteraction
(R)-warfarinExenatide can cause an increase in the absorption of (R)-warfarin resulting in an increased serum concentration and potentially a worsening of adverse effects.
(S)-WarfarinExenatide 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-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Exenatide is combined with 2,4-thiazolidinedione.
4-hydroxycoumarinExenatide 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)isoquinolineThe 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-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Exenatide.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Exenatide.
AcebutololThe therapeutic efficacy of Exenatide can be increased when used in combination with Acebutolol.
AcenocoumarolExenatide can cause an increase in the absorption of Acenocoumarol resulting in an increased serum concentration and potentially a worsening of adverse effects.
AcetazolamideThe therapeutic efficacy of Exenatide can be increased when used in combination with Acetazolamide.
Additional Data Available
  • Extended Description
    Extended Description

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

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  • Severity
    Severity

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

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  • Evidence Level
    Evidence Level

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

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  • Action
    Action

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

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Food Interactions
Not Available

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
  1. 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]
  2. 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]
  3. 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]
  4. FDA Drug Approval Package: Exenatide [Link]
  5. FDA Pharmacology Review: Exenatide [Link]
External Links
KEGG Drug
D04121
PubChem Substance
46509017
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
PhaseStatusPurposeConditionsCount
0RecruitingDiagnosticInsulinoma / Nesidioblastosis1
0RecruitingOtherAlcohol Dependence / BMI >30 kg/m2 / Cessation, Smoking1
1Active Not RecruitingOtherDependence, Cocaine1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableInsulin Resistance / Pre Diabetes1
1CompletedBasic ScienceBMI >30 kg/m21
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceType 2 Diabetes Mellitus1
1CompletedDiagnosticThe Methodology Assessment of Glucose Dependent Insulin Secretion1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentBMI >30 kg/m21
1CompletedTreatmentDiabetes Mellitus (DM)1
1CompletedTreatmentHealthy Adult Male and Female Volunteers1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentHyperinsulinemic Hypoglycemia1
1CompletedTreatmentImpaired Renal Function1
1CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
1CompletedTreatmentType 2 Diabetes Mellitus12
1CompletedTreatmentType2 Diabetes Mellitus1
1Not Yet RecruitingOtherType 2 Diabetes Mellitus1
1RecruitingTreatmentAlcohol Use Disorder (AUD)1
1RecruitingTreatmentParkinson's Disease (PD)1
1Unknown StatusTreatmentDiabetes Mellitus (DM)1
1, 2CompletedTreatmentEuglycemia / Hyperglycemias / Hypoglycemia1
1, 2CompletedTreatmentHypothalamic Obesity1
1, 2CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
1, 2CompletedTreatmentType 2 Diabetes Mellitus1
1, 2Not Yet RecruitingTreatmentAutoimmune Diseases / Diabetes Mellitus (DM) / Hypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus1
1, 2RecruitingTreatmentCessation, Smoking1
1, 2TerminatedTreatmentType 2 Diabetes Mellitus1
1, 2WithdrawnTreatmentGlucose Homeostasis / Health-Related Quality of Life / Inflammatory Reaction / Organ Dysfunction / Shock, Septic1
2Active Not RecruitingTreatmentAlcohol Dependence / Alcohol Dependence, in Remission1
2Active Not RecruitingTreatmentBMI >30 kg/m21
2CompletedTreatmentBMI >27 kg/m2 / BMI >30 kg/m2 / Postsurgical craniopharyngioma1
2CompletedTreatmentBMI >30 kg/m23
2CompletedTreatmentDiabetes Mellitus (DM)1
2CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent1
2CompletedTreatmentObesity, Morbid1
2CompletedTreatmentParkinson's Disease (PD)1
2CompletedTreatmentPolycystic Ovaries Syndrome1
2CompletedTreatmentStrokes1
2CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus2
2CompletedTreatmentType 2 Diabetes Mellitus13
2CompletedTreatmentType I Diabetes1
2RecruitingTreatmentAcute Ischemic Stroke (AIS)1
2RecruitingTreatmentMyocardial Infarction1
2RecruitingTreatmentObesity, Severe1
2RecruitingTreatmentPre Diabetes1
2RecruitingTreatmentStroke, Ischemic1
2TerminatedTreatmentAlzheimer's Disease (AD) / Mild Cognitive Impairment (MCI)1
2TerminatedTreatmentDiabetes Complications / Fatty Liver1
2TerminatedTreatmentDiabetes Mellitus (DM)1
2Unknown StatusTreatmentParkinson's Disease (PD)1
2, 3Active Not RecruitingOtherBMI >30 kg/m2 / Hepatic Steatosis / Polycystic Ovarian Syndrome1
2, 3CompletedNot Available(NAFLD) / Nonalcoholic Fatty Liver Disease1
2, 3CompletedBasic ScienceType 2 Diabetes Mellitus1
2, 3CompletedTreatmentHypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus1
2, 3CompletedTreatmentStress Hyperglycaemia1
2, 3CompletedTreatmentMinor burns1
2, 3Enrolling by InvitationTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
2, 3Not Yet RecruitingTreatmentNAFLD / Obesity, Adolescent / Polycystic Ovarian Syndrome1
2, 3RecruitingTreatmentQuality of Life1
2, 3RecruitingTreatmentType 2 Diabetes Mellitus1
2, 3Unknown StatusTreatmentObesity, Morbid1
3Active Not RecruitingTreatmentChildren and Adolescent With Type 2 Diabetes1
3Active Not RecruitingTreatmentHypothalamic Obesity1
3Active Not RecruitingTreatmentST Elevation Acute Myocardial Infarction1
3Active Not RecruitingTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
3CompletedTreatmentBMI >30 kg/m2 / Diabetes Mellitus (DM)1
3CompletedTreatmentBMI >30 kg/m2 / Drug-induced Obesity / Metabolic Syndromes / Schizophrenic Disorders1
3CompletedTreatmentBMI >30 kg/m2 / Obese experiencing rapid weight loss1
3CompletedTreatmentCoronary Artery Disease / Decreased Left Ventricular Function1
3CompletedTreatmentDiabetes Mellitus (DM)2
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus4
3CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent2
3CompletedTreatmentHypothalamic Obesity / Postsurgical craniopharyngioma1
3CompletedTreatmentType 2 Diabetes Mellitus45
3RecruitingTreatmentBMI >30 kg/m21
3RecruitingTreatmentBMI >30 kg/m2 / Polycystic Ovaries Syndrome1
3RecruitingTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
3RecruitingTreatmentChronic Kidney Disease (CKD) / Left Ventricular Diastolic Dysfunction / Type 2 Diabetes Mellitus1
3RecruitingTreatmentCognitive Deficits / Dysglycaemia1
3RecruitingTreatmentType 2 Diabetes Mellitus1
3SuspendedTreatmentType 2 Diabetes Mellitus1
3TerminatedTreatmentType 2 Diabetes Mellitus2
3Unknown StatusTreatmentPatients With a First Acute Myocardial Infarction to be Treated With Primary Percutaneous Coronary Intervention (PCI)1
3Unknown StatusTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
3WithdrawnTreatmentType 2 Diabetes Mellitus3
4Active Not RecruitingTreatmentBMI >30 kg/m21
4Active Not RecruitingTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
4Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
4CompletedBasic ScienceDiabetes Mellitus (DM) / Impaired Glucose Tolerance (IGT)1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedDiagnosticHealthy Volunteers1
4CompletedHealth Services ResearchType 2 Diabetes Mellitus1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Hyperglycemias / Myocardial Infarction1
4CompletedTreatmentBMI >30 kg/m22
4CompletedTreatmentBMI >30 kg/m2 / Impaired Glucose Tolerance (IGT)1
4CompletedTreatmentBMI >30 kg/m2 / Pre-Diabetic1
4CompletedTreatmentCongestive Heart Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus (DM) / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentDisorder of Glucose Regulation / Overweight and Obesity / Polycystic Ovaries Syndrome1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHealthy Volunteers / Impaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus1
4CompletedTreatmentImpaired Glucose Tolerance (IGT)1
4CompletedTreatmentImpaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus1
4CompletedTreatmentMyocardial Infarction2
4CompletedTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus1
4CompletedTreatmentNonalcoholic Fatty Liver Disease1
4CompletedTreatmentNonalcoholic Fatty Liver Disease / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus2
4CompletedTreatmentType 2 Diabetes Mellitus20
4CompletedTreatmentThe Therapeutic Effect of Exenatide and Metformin / Type2 Diabetes1
4CompletedTreatmentWeight Gain1
4Not Yet RecruitingPreventionDiabetic Nephropathies1
4Not Yet RecruitingTreatmentBMI >30 kg/m2 / Insulin Resistance / Pre Diabetes / Spinal Cord Injuries (SCI)1
4Not Yet RecruitingTreatmentCoronary Endothelial Function1
4Not Yet RecruitingTreatmentEvaluate Ketogenic Stress1
4Not Yet RecruitingTreatmentImpaired Glucose Tolerance (IGT) / Polycystic Ovarian Syndrome1
4Not Yet RecruitingTreatmentKidney Diseases / Type2 Diabetes1
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus2
4RecruitingBasic ScienceType 2 Diabetes Mellitus1
4RecruitingTreatmentAtherosclerosis / Diabetes Mellitus (DM) / Restenosis1
4RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m2 / Polycystic Ovary Syndrome (PCOS)1
4RecruitingTreatmentBMI >30 kg/m21
4RecruitingTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
4RecruitingTreatmentBrain Injury1
4RecruitingTreatmentPolycystic Ovaries Syndrome1
4RecruitingTreatmentSteatosis, Liver / Type2 Diabetes1
4RecruitingTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus4
4TerminatedTreatmentDiabetes Mellitus (DM)1
4TerminatedTreatmentHeart Failure, Diastolic / Type 2 Diabetes Mellitus1
4TerminatedTreatmentType 2 Diabetes Mellitus2
4Unknown StatusTreatmentType 2 Diabetes Mellitus3
4WithdrawnNot AvailableGestational Diabetes Mellitus (GDM)1
4WithdrawnTreatmentBMI >30 kg/m2 / Cardiovascular Disease (CVD) / Impaired Glucose Tolerance (IGT) / Insulin Resistance1
4WithdrawnTreatmentShort Bowel Syndrome (SBS)1
4WithdrawnTreatmentType 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingTreatmentDiabetes Mellitus (DM)1
Not AvailableCompletedNot AvailableBMI >30 kg/m2 / Diabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableDiabetic Nephropathies / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableHealthy Subjects (Treated With no Diabetes Therapies) / Type 2 Diabetes (Treated With Exenatide or Other Oral Antidiabetic Therapies)1
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus10
Not AvailableCompletedBasic ScienceDiabetes Mellitus (DM)1
Not AvailableCompletedBasic ScienceHyperlipidemias1
Not AvailableCompletedBasic ScienceType 2 Diabetes Mellitus1
Not AvailableCompletedDiagnosticBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
Not AvailableCompletedOtherType 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentCardiac Arrest / Comatose1
Not AvailableCompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentGlucocorticoid-induced Beta-cell Dysfunction / Glucocorticoid-induced Glucometabolic Abnormalities1
Not AvailableCompletedTreatmentNewly Diagnosed / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentPrader-Willi Syndrome1
Not AvailableCompletedTreatmentPre-Diabetic / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentPsoriasis / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentSleep Disordered Breathing (SDB) / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus2
Not AvailableRecruitingNot AvailableType 2 Diabetes Mellitus1
Not AvailableRecruitingPreventionIncretinomimetics / Pancreas / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentAortic Valve Disorder / Brain Injury / Coronary Heart Disease (CHD) / Renal Failure / Shock, Cardiogenic / Strokes1
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableUnknown StatusTreatmentBMI >30 kg/m21
Not AvailableUnknown StatusTreatmentDiabetes Mellitus (DM) / Hypothalamic Obesity1
Not AvailableUnknown StatusTreatmentDiabetes Mellitus Associated With Genetic Syndrome / Wolfram Syndrome1
Not AvailableUnknown StatusTreatmentHeart Failure / Type 2 Diabetes Mellitus1
Not AvailableUnknown StatusTreatmentPrader-Willi Syndrome1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amylin Pharmaceuticals
  • Baxter International Inc.
  • CP Pharmaceuticals Ltd.
  • Eli Lilly & Co.
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
Injection, powder, for suspension, extended releaseSubcutaneous2 mg
Injection, powder, for suspension, extended release; kitSubcutaneous2 mg
Injection, suspension, extended releaseSubcutaneous2 mg/0.65mL
KitSubcutaneous2 mg/0.65mL
Injection, suspension, extended releaseSubcutaneous2 mg/0.85mL
Suspension, extended releaseSubcutaneous2 mg
InjectionSubcutaneous250 ug/1mL
Injection, solutionSubcutaneous10 micrograms
Injection, solutionSubcutaneous5 micrograms
SolutionSubcutaneous10 mcg
SolutionSubcutaneous5 mcg
Prices
Unit descriptionCostUnit
Byetta 10 MCG Pen 10 mcg/0.04ml Solution 2.4ml Pen324.23USD pen
Byetta 5 mcg dose pen inj316.76USD ml
Byetta 5 MCG Pen 5 mcg/0.02ml Solution 1.2ml Pen276.57USD pen
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8216180No2012-07-102028-01-12Us
US8439864No2013-05-142028-03-25Us
US6667061Yes2003-12-232020-11-25Us
US6495164No2002-12-172020-05-25Us
US5424286No1995-06-132016-12-01Us
US6858576No2005-02-222017-01-06Us
US6872700No2005-03-292020-01-14Us
US6956026No2005-10-182018-01-07Us
US7741269No2010-06-222018-01-07Us
US7297761No2007-11-202017-10-15Us
US7521423No2009-04-212017-10-15Us
US6902744No2005-06-072020-01-14Us
US9238076No2016-01-192024-04-15Us
US8906851No2014-12-092026-08-18Us
US7612176No2009-11-032025-04-13Us
US8431685No2013-04-302025-04-13Us
US8461105No2013-06-112025-04-13Us
US8329648No2012-12-112026-08-18Us
US7456254No2008-11-252025-06-30Us
US7563871No2009-07-212024-04-15Us
US6824822No2004-11-302022-10-09Us
US6479065No2002-11-122020-08-10Us
US7223440No2007-05-292021-08-31Us
US8685934No2014-04-012030-05-26Us
US8501698No2013-08-062027-06-20Us
US6414126No2002-07-022020-10-04Us
US6515117No2003-02-042020-10-04Us
US6936590No2005-08-302020-10-04Us
US9198925No2015-12-012020-10-04Us
US7919598No2011-04-052029-12-16Us
US8361972No2013-01-292028-03-21Us
US8716251No2014-05-062028-03-21Us
US7851502No2010-12-142028-08-19Us
US8221786No2012-07-172028-03-21Us
US9320853No2016-04-262028-03-25Us
US8827963No2014-09-092029-02-04Us
US8712615No2014-04-292030-01-18Us
US8998876No2015-04-072030-01-07Us
US8758292No2014-06-242027-11-12Us
US8690837No2014-04-082029-05-19Us
US8895033No2014-11-252030-10-04Us
US8721615No2014-05-132030-01-18Us
US9884092No2018-02-062026-08-18Us
Additional Data Available
  • Filed On
    Filed On

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

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
isoelectric point4.86https://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

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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. Geelhoed-Duijvestijn PH: Incretins: a new treatment option for type 2 diabetes? Neth J Med. 2007 Feb;65(2):60-4. [PubMed:17379930]
  6. 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]
  7. 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]
  8. 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]
  9. 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]
  10. Barnett AH: Exenatide. Drugs Today (Barc). 2005 Sep;41(9):563-78. [PubMed:16341288]
  11. 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]
  12. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

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
  1. 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

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
  1. 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 November 11, 2019 06:49