Exenatide, derived from a compound found in the saliva of the Gila monster, a large lizard native to the southwestern US, is a functional analog of Glucagon-Like Peptide-1 (GLP-1), a naturally occuring peptide.

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
Bydureon	Injection, powder, for suspension, extended release	2 mg	Subcutaneous	Astra Zeneca Ab	2011-06-17	Not applicable
Bydureon	Kit	2 mg/0.65mL		AstraZeneca Pharmaceuticals LP	2015-02-01	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, suspension, extended release	2 mg/0.65mL	Subcutaneous	AstraZeneca Pharmaceuticals LP	2014-09-08	Not applicable
Bydureon	Injection, powder, for suspension, extended release	2 mg	Subcutaneous	Astra Zeneca Ab	2011-06-17	Not applicable
Bydureon	Kit	2 mg/0.65mL		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	Kit	2 mg/0.65mL		Amylin Pharmaceuticals, Llc.	2012-01-27	2018-01-31
BYDUREON BCise	Injection, suspension, extended release	2 mg/0.85mL	Subcutaneous	AstraZeneca Pharmaceuticals LP	2017-12-01	Not applicable

Categories

UNII

9P1872D4OL

CAS number

141758-74-9

Pharmacology

Indication

Indicated as adjunctive therapy to improve glycemic control in patients with Type 2 diabetes mellitus who are taking metformin, a sulfonylurea, or a combination of both, but have not achieved adequate glycemic control.

Associated Conditions

Type 2 Diabetes Mellitus

Pharmacodynamics

Exenatide is an incretin mimetic, which has glucoregulatory effects. While it is has blood-sugar lowering actions alone, it can also be combined with other medications such as pioglitazone, metformin, sulfonylureas, and/or insulin to improve glucose control. The approved use of exenatide is with either sulfonylureas, metformin and thiazolinediones. The medication is injected twice per day using a pre-filled pen device. Typical human responses to exenatide plus eating include improvements in the initial rapid release of endogenous insulin, suppression of glucagon release by the pancreas, regulation of gastric empyting and reduced appetite; all behaviors more typical of individuals without blood sugar control problems. Exenatide is self-regulating in that in lowers blood sugar when levels are elevated but does not continue to lower blood sugar when levels return to normal, unlike with sulfonylureas or insulins.

Mechanism of action

Exenatide is a functional analog of the human incretin Glucagon-Like Peptide-1 (GLP-1). Incretins enhance glucose-dependent insulin secretion and exhibit other antihyperglycemic actions following their release into the circulation from the gut. The GLP-1 system increases insulin secretion only in the presence of elevated plasma glucose levels, avoiding inappropriately high insulin levels during fasting. The drug also moderates peak serum glucagon levels during hyperglycemic periods following meals, but does not interfere with glucagon release in response to hypoglycemia. Secondary effects of drug administration reduces the rate of gastric emptying and decreases food intake, mitigating the potential severity of hyperglycemic events after meals.

Target	Actions	Organism
AGlucagon-like peptide 1 receptor	agonist	Humans

Absorption

Following subcutaneous administration to patients with type 2 diabetes, exenatide reaches median peak plasma concentrations in 2.1 hours.

Volume of distribution

28.3 L

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Nonclinical studies have shown that exenatide is predominantly eliminated by glomerular filtration with subsequent proteolytic degradation.

Half life

Mean terminal half-life is 2.4 hours.

Clearance

Apparent cl=9.1 L/hr

Toxicity

Effects of the overdoses included severe nausea, severe vomiting, and rapidly declining blood glucose concentrations.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction
(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.
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.
Acetohexamide	Exenatide may increase the hypoglycemic activities of Acetohexamide.

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

Heine RJ, Van Gaal LF, Johns D, Mihm MJ, Widel MH, Brodows RG: Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial. Ann Intern Med. 2005 Oct 18;143(8):559-69. [PubMed:16230722]

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 (683 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
0	Recruiting	Other	Alcohol Dependence / BMI >30 kg/m2 / Cessation, Smoking	1
1	Completed	Not Available	Healthy Volunteers	1
1	Completed	Not Available	Insulin Resistance / Pre Diabetes	1
1	Completed	Basic Science	BMI >30 kg/m2	1
1	Completed	Basic Science	Healthy Volunteers	1
1	Completed	Diagnostic	The Methodology Assessment of Glucose Dependent Insulin Secretion	1
1	Completed	Treatment	BMI >30 kg/m2	1
1	Completed	Treatment	Diabetes Mellitus (DM)	1
1	Completed	Treatment	Diabetes, Diabetes Mellitus Type 1	1
1	Completed	Treatment	Healthy Adult Male and Female Volunteers	1
1	Completed	Treatment	Type 2 Diabetes Mellitus	8
1	Completed	Treatment	Type2 Diabetes Mellitus	1
1	Not Yet Recruiting	Treatment	Alcohol Use Disorder (AUD)	1
1	Recruiting	Other	Dependence, Cocaine	1
1	Recruiting	Treatment	Parkinson's Disease (PD)	1
1, 2	Active Not Recruiting	Treatment	Hypothalamic Obesity	1
1, 2	Completed	Treatment	Euglycemia / Hyperglycemias / Hypoglycemia	1
1, 2	Not Yet Recruiting	Treatment	Autoimmune Diseases / Diabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 1 / Hypoglycemia	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	BMI >30 kg/m2	1
2	Active Not Recruiting	Treatment	Diabetes, Diabetes Mellitus Type 1	1
2	Active Not Recruiting	Treatment	Type I Diabetes	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 (DM)	1
2	Completed	Treatment	Diabetes Mellitus, Non-Insulin-Dependent	1
2	Completed	Treatment	Diabetes, Diabetes Mellitus Type 1	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	Strokes	1
2	Completed	Treatment	Type 2 Diabetes Mellitus	8
2	Recruiting	Treatment	Acute Ischemic Stroke (AIS)	1
2	Recruiting	Treatment	Alcohol Dependence / Alcohol Dependence, in Remission	1
2	Recruiting	Treatment	Hyperinsulinemic Hypoglycemia	1
2	Recruiting	Treatment	Myocardial Infarction	1
2	Recruiting	Treatment	Obesity, Severe	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 (DM)	1
2	Unknown Status	Treatment	Parkinson's Disease (PD)	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	Diabetes, Diabetes Mellitus Type 1 / Hypoglycemia	1
2, 3	Completed	Treatment	Stress Hyperglycaemia	1
2, 3	Completed	Treatment	Minor burns	1
2, 3	Enrolling by Invitation	Treatment	Diabetes, Diabetes Mellitus Type 1	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	Children and Adolescent With Type 2 Diabetes	1
3	Active Not Recruiting	Treatment	Diabetes, Diabetes Mellitus Type 1	1
3	Active Not Recruiting	Treatment	Hypothalamic Obesity	1
3	Completed	Treatment	BMI >30 kg/m2 / Diabetes Mellitus (DM)	1
3	Completed	Treatment	BMI >30 kg/m2 / Drug-induced Obesity / Metabolic Syndromes / Schizophrenic Disorders	1
3	Completed	Treatment	BMI >30 kg/m2 / Obese experiencing rapid weight loss	1
3	Completed	Treatment	Coronary Artery Disease / Decreased Left Ventricular Function	1
3	Completed	Treatment	Diabetes Mellitus (DM)	1
3	Completed	Treatment	Diabetes Mellitus (DM) / Type 2 Diabetes Mellitus	4
3	Completed	Treatment	Diabetes Mellitus, Non-Insulin-Dependent	2
3	Completed	Treatment	Hypothalamic Obesity / Postsurgical craniopharyngioma	1
3	Completed	Treatment	Type 2 Diabetes Mellitus	33
3	Recruiting	Treatment	BMI >30 kg/m2	1
3	Recruiting	Treatment	BMI >30 kg/m2 / Type 2 Diabetes Mellitus	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	ST Elevation Acute Myocardial Infarction	1
3	Recruiting	Treatment	Type 2 Diabetes Mellitus	2
3	Unknown Status	Treatment	Diabetes, Diabetes Mellitus Type 1	1
3	Unknown Status	Treatment	Patients With a First Acute Myocardial Infarction to be Treated With Primary Percutaneous Coronary Intervention (PCI)	1
4	Active Not Recruiting	Treatment	BMI >30 kg/m2	1
4	Active Not Recruiting	Treatment	Schizoaffective Disorders / Schizophrenic Disorders	1
4	Active Not Recruiting	Treatment	Type 2 Diabetes Mellitus	1
4	Completed	Basic Science	Diabetes Mellitus (DM) / Impaired Glucose Tolerance (IGT)	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	Treatment	Acute Coronary Syndromes (ACS) / Hyperglycemias / Myocardial Infarction	1
4	Completed	Treatment	BMI >30 kg/m2	2
4	Completed	Treatment	BMI >30 kg/m2 / Impaired Glucose Tolerance (IGT)	1
4	Completed	Treatment	BMI >30 kg/m2 / Pre-Diabetic	1
4	Completed	Treatment	Congestive Heart Failure (CHF) / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Diabetes Mellitus (DM) / Human Immunodeficiency Virus (HIV) Infections	1
4	Completed	Treatment	Diabetes, Diabetes Mellitus Type 1	2
4	Completed	Treatment	Healthy Volunteers	1
4	Completed	Treatment	Healthy Volunteers / Impaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Impaired Glucose Tolerance (IGT)	1
4	Completed	Treatment	Impaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Myocardial Infarction	2
4	Completed	Treatment	Nonalcoholic Fatty Liver Disease	1
4	Completed	Treatment	Nonalcoholic Fatty Liver Disease / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Type 2 Diabetes Mellitus	19
4	Completed	Treatment	Weight gain therapy	1
4	Not Yet Recruiting	Prevention	Diabetic Nephropathies	1
4	Not Yet Recruiting	Treatment	BMI >30 kg/m2 / Insulin Resistance / Pre Diabetes / 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 (IGT) / Polycystic Ovarian Syndrome	1
4	Not Yet Recruiting	Treatment	Kidney Diseases / Type2 Diabetes	1
4	Not Yet Recruiting	Treatment	Type 2 Diabetes Mellitus	1
4	Recruiting	Basic Science	Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Atherosclerosis / Diabetes Mellitus (DM) / Restenosis	1
4	Recruiting	Treatment	BMI >30 kg/m2	1
4	Recruiting	Treatment	BMI >30 kg/m2 / Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Brain Injury	1
4	Recruiting	Treatment	Diabetes, Diabetes Mellitus Type 1	1
4	Recruiting	Treatment	Disorder of Glucose Regulation / Overweight and Obesity / Polycystic Ovaries Syndrome	1
4	Recruiting	Treatment	Non-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Steatosis, Liver / Type2 Diabetes	1
4	Recruiting	Treatment	Type 2 Diabetes Mellitus	4
4	Terminated	Treatment	Heart Failure, Diastolic / Type 2 Diabetes Mellitus	1
4	Terminated	Treatment	Type 2 Diabetes Mellitus	1
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 Disease (CVD) / Impaired Glucose Tolerance (IGT) / Insulin Resistance	1
4	Withdrawn	Treatment	Short Bowel Syndrome (SBS)	1
4	Withdrawn	Treatment	Type 2 Diabetes Mellitus	1
Not Available	Completed	Not Available	BMI >30 kg/m2 / Diabetes Mellitus (DM) / 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	7
Not Available	Completed	Basic Science	Diabetes Mellitus (DM)	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 / 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	Sleep Disordered Breathing (SDB) / Type 2 Diabetes Mellitus	1
Not Available	Completed	Treatment	Type 2 Diabetes Mellitus	2
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 / Brain Injury / Coronary Heart Disease (CHD) / Renal Failure / Shock, Cardiogenic / Strokes	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 (DM) / Hypothalamic Obesity	1
Not Available	Unknown Status	Treatment	Diabetes Mellitus Associated With Genetic Syndrome / Wolfram Syndrome	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		2 mg/0.65mL
Injection, suspension, extended release	Subcutaneous	2 mg/0.85mL
Injection	Subcutaneous	250 ug/1mL
Injection, solution	Subcutaneous	10 micrograms
Injection, solution	Subcutaneous	5 micrograms
Solution	Subcutaneous	250 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)
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

Properties

State: Solid
Experimental Properties: Not Available

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]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

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 April 18, 2019 06:15