Identification
NameExenatide
Accession NumberDB01276
TypeBiotech
GroupsApproved, Investigational
Description

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 structureDb01276
Related Articles
Protein chemical formulaC184H282N50O60S
Protein average weight4186.6 Da
Sequences
>Exenatide
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Download FASTA Format
Synonyms
AC 2993
AC-2993
AC002993
AC2993
AC2993a
Bydureon
Byetta
Exenatide
Exenatide synthetic
Synthetic exendin-4
External IDs AC2993
Product Ingredients Not Available
Approved 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
BydureonKitAstra Zeneca Lp2015-02-01Not applicableUs
BydureonKitAmylin Pharmaceuticals, Llc.2012-01-27Not applicableUs
BydureonInjection, powder, for suspension, extended release2 mgSubcutaneousAstra Zeneca Ab2011-06-17Not applicableEu
BydureonInjection, suspension, extended release2 mg/.65mLSubcutaneousAstra Zeneca Lp2014-09-08Not applicableUs
BydureonInjection, powder, for suspension, extended release2 mgSubcutaneousAstra Zeneca Ab2011-06-17Not applicableEu
BydureonKitAmylin Pharmaceuticals, Llc.2012-01-27Not applicableUs
BydureonInjection, powder, for suspension, extended release; Kit2 mgSubcutaneousAstra Zeneca2016-02-16Not applicableCanada
ByettaInjection250 ug/mLSubcutaneousAstra Zeneca Lp2014-12-10Not applicableUs
ByettaInjection, solution5 microgramsSubcutaneousAstra Zeneca Ab2006-11-20Not applicableEu
ByettaInjection250 ug/mLSubcutaneousAmylin Pharmaceuticals, Llc.2005-04-282016-04-30Us
ByettaSolution250 mcgSubcutaneousAstra Zeneca2011-06-01Not applicableCanada
ByettaInjection, solution10 microgramsSubcutaneousAstra Zeneca Ab2006-11-20Not applicableEu
ByettaInjection250 ug/mLSubcutaneousAstra Zeneca Lp2014-12-12Not applicableUs
ByettaInjection250 ug/mLSubcutaneousAmylin Pharmaceuticals, Llc.2005-04-282016-10-31Us
ByettaSolution250 mcgSubcutaneousAstra Zeneca2011-05-31Not applicableCanada
ByettaInjection, solution5 microgramsSubcutaneousAstra Zeneca Ab2006-11-20Not applicableEu
ByettaInjection, solution10 microgramsSubcutaneousAstra Zeneca Ab2006-11-20Not applicableEu
ByettaInjection250 ug/mLSubcutaneousPhysicians Total Care, Inc.2005-08-09Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNII9P1872D4OL
CAS number141758-74-9
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.

Structured Indications
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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Glucagon-like peptide 1 receptorProteinyes
agonist
HumanP43220 details
Related Articles
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 bindingNot Available
MetabolismNot 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
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Exenatide.Experimental
AcenocoumarolExenatide may increase the anticoagulant activities of Acenocoumarol.Approved
AcetohexamideExenatide may increase the hypoglycemic activities of Acetohexamide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Exenatide.Approved, Vet Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Exenatide.Approved
AripiprazoleThe therapeutic efficacy of Exenatide can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Asenapine.Approved
AtazanavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Atazanavir.Approved, Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Exenatide.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Exenatide.Withdrawn
BetamethasoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BrexpiprazoleThe therapeutic efficacy of Exenatide can be decreased when used in combination with Brexpiprazole.Approved
BumetanideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Exenatide can be decreased when used in combination with Buserelin.Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Exenatide.Withdrawn
CeritinibThe therapeutic efficacy of Exenatide can be decreased when used in combination with Ceritinib.Approved
ChlorothiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Exenatide.Withdrawn
ChlorpropamideExenatide may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Chlorthalidone.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Exenatide.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
CitalopramCitalopram may increase the hypoglycemic activities of Exenatide.Approved
ClozapineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Clozapine.Approved
Conjugated estrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Exenatide.Approved
CorticotropinThe therapeutic efficacy of Exenatide can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Exenatide can be decreased when used in combination with Cortisone acetate.Approved
Cyproterone acetateThe therapeutic efficacy of Exenatide can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe therapeutic efficacy of Exenatide can be decreased when used in combination with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Exenatide can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Exenatide.Investigational
DarunavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Darunavir.Approved
DesogestrelThe serum concentration of Desogestrel can be decreased when it is combined with Exenatide.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Exenatide.Approved
DexamethasoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Diazoxide.Approved
DicoumarolExenatide may increase the anticoagulant activities of Dicoumarol.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Exenatide.Approved
DienogestThe therapeutic efficacy of Exenatide can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Exenatide.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Exenatide.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Exenatide.Illicit
DisopyramideExenatide may increase the hypoglycemic activities of Disopyramide.Approved
DrospirenoneThe serum concentration of Drospirenone can be decreased when it is combined with Exenatide.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Exenatide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Exenatide.Approved
EpinephrineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Exenatide.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Exenatide.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Exenatide.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Exenatide.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Exenatide.Approved
Etacrynic acidThe therapeutic efficacy of Exenatide can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Exenatide.Approved
Ethyl biscoumacetateExenatide may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ethynodiol diacetateThe serum concentration of Ethynodiol diacetate can be decreased when it is combined with Exenatide.Approved
EtonogestrelThe serum concentration of Etonogestrel can be decreased when it is combined with Exenatide.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Exenatide.Approved
EverolimusThe therapeutic efficacy of Exenatide can be decreased when used in combination with Everolimus.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Exenatide.Approved
FludrocortisoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Fludrocortisone.Approved
FluindioneExenatide may increase the anticoagulant activities of Fluindione.Investigational
FlumequineFlumequine may increase the hypoglycemic activities of Exenatide.Withdrawn
FluoxetineFluoxetine may increase the hypoglycemic activities of Exenatide.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Exenatide.Approved, Illicit
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Exenatide.Approved, Investigational
FosamprenavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Fosamprenavir.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Exenatide.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Furosemide.Approved, Vet Approved
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
GestodeneThe serum concentration of Gestodene can be decreased when it is combined with Exenatide.Approved
GlibornurideExenatide may increase the hypoglycemic activities of Glibornuride.Withdrawn
GliclazideExenatide may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideExenatide may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideExenatide may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneExenatide may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideExenatide may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideExenatide may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Exenatide can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Exenatide.Withdrawn
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Exenatide.Withdrawn
HistrelinThe therapeutic efficacy of Exenatide can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Exenatide.Experimental
HydrochlorothiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Exenatide can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Iloperidone.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Exenatide.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Indapamide.Approved
IndinavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Indinavir.Approved
Insulin AspartExenatide may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirExenatide may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineExenatide may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineExenatide may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanExenatide may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproExenatide may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin PorkExenatide may increase the hypoglycemic activities of Insulin Pork.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Exenatide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Exenatide.Withdrawn
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Exenatide.Approved
LanreotideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Exenatide.Approved
LevonorgestrelThe serum concentration of Levonorgestrel can be decreased when it is combined with Exenatide.Approved, Investigational
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Exenatide.Approved, Nutraceutical
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Exenatide.Approved
LopinavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Lopinavir.Approved
LurasidoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Lurasidone.Approved
LynestrenolThe serum concentration of Lynestrenol can be decreased when it is combined with Exenatide.Investigational
MebanazineMebanazine may increase the hypoglycemic activities of Exenatide.Withdrawn
MecaserminExenatide may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Exenatide can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Exenatide can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Exenatide.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Exenatide.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Exenatide.Experimental
MethotrimeprazineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Exenatide.Investigational
MethylprednisoloneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Exenatide.Approved
MetolazoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Metolazone.Approved
MifepristoneExenatide may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Exenatide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Exenatide.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Exenatide.Approved
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Exenatide.Approved
NateglinideExenatide may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Exenatide.Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Exenatide.Approved, Withdrawn
NelfinavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Nelfinavir.Approved
NiacinThe therapeutic efficacy of Exenatide can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Exenatide.Withdrawn
NilotinibThe therapeutic efficacy of Exenatide can be decreased when used in combination with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Exenatide.Investigational
NorelgestrominThe serum concentration of Norelgestromin can be decreased when it is combined with Exenatide.Approved
NorethisteroneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Exenatide.Approved
NorgestimateThe serum concentration of Norgestimate can be decreased when it is combined with Exenatide.Approved
NorgestrelThe serum concentration of Norgestrel can be decreased when it is combined with Exenatide.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Exenatide.Withdrawn
OctreotideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Exenatide.Approved
OlanzapineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Olanzapine.Approved, Investigational
OlsalazineOlsalazine may increase the hypoglycemic activities of Exenatide.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Exenatide.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Exenatide.Approved, Illicit
PaliperidoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Paliperidone.Approved
PargylinePargyline may increase the hypoglycemic activities of Exenatide.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Exenatide.Approved, Investigational
PasireotideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Exenatide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Exenatide.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Exenatide.Approved
PentamidineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Pentamidine.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Exenatide.Approved
PhenindioneExenatide may increase the anticoagulant activities of Phenindione.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Exenatide.Withdrawn
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Exenatide.Withdrawn
PhenprocoumonExenatide may increase the anticoagulant activities of Phenprocoumon.Approved
PiperazineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Exenatide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Exenatide.Withdrawn
PolythiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Polythiazide.Approved
PrednisoloneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Prednisone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Progesterone.Approved, Vet Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Exenatide.Investigational
QuetiapineThe therapeutic efficacy of Exenatide can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Quinethazone.Approved
QuinineExenatide may increase the hypoglycemic activities of Quinine.Approved
RasagilineRasagiline may increase the hypoglycemic activities of Exenatide.Approved
RepaglinideExenatide may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RisperidoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Ritonavir.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Exenatide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Exenatide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Exenatide.Approved, Vet Approved
SaquinavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Saquinavir.Approved, Investigational
SelegilineSelegiline may increase the hypoglycemic activities of Exenatide.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Exenatide.Approved
SirolimusThe therapeutic efficacy of Exenatide can be decreased when used in combination with Sirolimus.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Exenatide.Approved
StanozololStanozolol may increase the hypoglycemic activities of Exenatide.Approved, Vet Approved
SulfadiazineExenatide may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleExenatide may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleExenatide may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SunitinibExenatide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Exenatide.Approved
TacrolimusThe therapeutic efficacy of Exenatide can be decreased when used in combination with Tacrolimus.Approved, Investigational
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Exenatide.Withdrawn
TemsirolimusThe therapeutic efficacy of Exenatide can be decreased when used in combination with Temsirolimus.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Exenatide.Approved, Investigational
TipranavirThe therapeutic efficacy of Exenatide can be decreased when used in combination with Tipranavir.Approved, Investigational
TolazamideExenatide may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideExenatide may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Exenatide.Approved
TorasemideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Torasemide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Exenatide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Exenatide.Approved
TriamcinoloneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Exenatide can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Exenatide.Approved, Withdrawn
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Exenatide.Approved
VorinostatThe therapeutic efficacy of Exenatide can be decreased when used in combination with Vorinostat.Approved, Investigational
WarfarinExenatide may increase the anticoagulant activities of Warfarin.Approved
ZimelidineZimelidine may increase the hypoglycemic activities of Exenatide.Withdrawn
ZiprasidoneThe therapeutic efficacy of Exenatide can be decreased when used in combination with Ziprasidone.Approved
Food InteractionsNot 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. 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
ATC CodesA10BX04 — Exenatide
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (683 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingNot AvailableAlcoholism / BMI >30 kg/m2 / Cessation, Smoking1
1Active Not RecruitingTreatmentType2 Diabetes Mellitus1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableInsulin Resistance / Pre Diabetes1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedDiagnosticThe Methodology Assessment of Glucose Dependent Insulin Secretion1
1CompletedTreatmentBMI >30 kg/m21
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
1CompletedTreatmentHealthy Adult Male and Female Volunteers1
1CompletedTreatmentType 2 Diabetes Mellitus8
1RecruitingOtherDependence, Cocaine1
1, 2Active Not RecruitingTreatmentHypothalamic Obesity1
1, 2CompletedTreatmentEuglycemia / Hyperglycemias / Hypoglycemia1
1, 2Not Yet RecruitingTreatmentAutoimmune Diseases / Diabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
1, 2RecruitingTreatmentCessation, Smoking1
1, 2TerminatedTreatmentType 2 Diabetes Mellitus1
1, 2WithdrawnTreatmentGlucose Homeostasis / Health-Related Quality of Life / Inflammatory Reaction / Organ Dysfunction / Shock, Septic1
2Active Not RecruitingTreatmentBMI >30 kg/m21
2CompletedTreatmentAlzheimer's Disease (AD) / Mild Cognitive Impairment (MCI)1
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 2 Diabetes Mellitus8
2RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
2RecruitingTreatmentHyperinsulinemic Hypoglycemia1
2RecruitingTreatmentMyocardial Infarction (MI)1
2RecruitingTreatmentObesity, Severe1
2RecruitingTreatmentStroke, Ischemic1
2RecruitingTreatmentType I Diabetes1
2TerminatedTreatmentDiabetes Complications / Fatty Liver1
2TerminatedTreatmentDiabetes Mellitus (DM)1
2Unknown StatusTreatmentParkinson's Disease (PD)1
2, 3CompletedNot Available(NAFLD) / Nonalcoholic Fatty Liver Disease1
2, 3CompletedBasic ScienceType 2 Diabetes Mellitus1
2, 3CompletedTreatmentMinor burns1
2, 3Enrolling by InvitationTreatmentDiabetes, Diabetes Mellitus Type 11
2, 3RecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
2, 3RecruitingTreatmentQuality of Life1
2, 3RecruitingTreatmentStress Hyperglycaemia1
2, 3RecruitingTreatmentType 2 Diabetes Mellitus1
2, 3Unknown StatusTreatmentObesity, Morbid1
3CompletedTreatmentBMI >30 kg/m2 / Diabetes1
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)1
3CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent2
3CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus4
3CompletedTreatmentType 2 Diabetes Mellitus32
3Not Yet RecruitingTreatmentHypothalamic Obesity / Postsurgical craniopharyngioma1
3RecruitingTreatmentChildren and Adolescent With Type 2 Diabetes1
3RecruitingTreatmentChronic Kidney Disease (CKD) / Left Ventricular Diastolic Dysfunction / Type 2 Diabetes Mellitus1
3RecruitingTreatmentCognitive Deficits / Dysglycaemia1
3RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
3RecruitingTreatmentHypothalamic Obesity1
3RecruitingTreatmentST Elevation Acute Myocardial Infarction1
3RecruitingTreatmentType 2 Diabetes Mellitus3
3Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 11
3Unknown StatusTreatmentPatients With a First Acute Myocardial Infarction to be Treated With Primary Percutaneous Coronary Intervention (PCI)1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedHealth Services ResearchType 2 Diabetes Mellitus1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Hyperglycemias / Myocardial Infarction (MI)1
4CompletedTreatmentBMI >30 kg/m22
4CompletedTreatmentBMI >30 kg/m2 / Impaired Glucose Tolerance (IGT)1
4CompletedTreatmentCongestive Heart Failure (CHF) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus (DM) / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentDiabetes, Diabetes Mellitus Type 13
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 Infarction (MI)2
4CompletedTreatmentNonalcoholic Fatty Liver Disease1
4CompletedTreatmentNonalcoholic Fatty Liver Disease / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus15
4CompletedTreatmentWeight gain therapy1
4Not Yet RecruitingDiagnosticHealthy Volunteers1
4Not Yet RecruitingPreventionDiabetic Nephropathies1
4Not Yet RecruitingTreatmentCoronary Endothelial Function1
4Not Yet RecruitingTreatmentEvaluate Ketogenic Stress1
4Not Yet RecruitingTreatmentKidney Diseases / Type2 Diabetes1
4Not Yet RecruitingTreatmentSteatosis, Liver / Type2 Diabetes1
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus2
4RecruitingTreatmentAtherosclerosis / Diabetes / Restenosis1
4RecruitingTreatmentBMI >30 kg/m21
4RecruitingTreatmentBMI >30 kg/m2 / Pre-Diabetic1
4RecruitingTreatmentBrain Injury1
4RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
4RecruitingTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus1
4RecruitingTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
4RecruitingTreatmentType 2 Diabetes Mellitus7
4TerminatedTreatmentHeart Failure, Diastolic / Type 2 Diabetes Mellitus1
4TerminatedTreatmentType 2 Diabetes Mellitus1
4Unknown StatusHealth Services ResearchDiabetes / Impaired Glucose Tolerance (IGT)1
4Unknown StatusTreatmentType 2 Diabetes Mellitus3
4WithdrawnNot AvailableDiabetes, Gestational1
4WithdrawnTreatmentBMI >30 kg/m2 / Cardiovascular Disease (CVD) / Impaired Glucose Tolerance (IGT) / Insulin Resistance1
4WithdrawnTreatmentShort Bowel Syndrome (SBS)1
4WithdrawnTreatmentType 2 Diabetes Mellitus1
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 Mellitus8
Not AvailableCompletedBasic ScienceBMI >30 kg/m21
Not AvailableCompletedBasic ScienceHyperlipidemias1
Not AvailableCompletedBasic ScienceType 2 Diabetes Mellitus1
Not AvailableCompletedDiagnosticBMI >30 kg/m2 / Type 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 AvailableCompletedTreatmentSleep Disordered Breathing (SDB) / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus2
Not AvailableRecruitingNot AvailableType 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentAortic Valve Disorder / Brain Injury / Coronary Heart Disease (CHD) / Renal Failure / Shock, Cardiogenic / Strokes1
Not AvailableRecruitingTreatmentBMI >30 kg/m21
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableUnknown StatusBasic ScienceDiabetes1
Not AvailableUnknown StatusPreventionIncretinomimetics / Pancreas / Type 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, Unspecified / Type 2 Diabetes Mellitus1
Not AvailableUnknown StatusTreatmentPrader-Willi Syndrome1
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for suspension, extended releaseSubcutaneous2 mg
Injection, powder, for suspension, extended release; kitSubcutaneous2 mg
Injection, suspension, extended releaseSubcutaneous2 mg/.65mL
Kit
InjectionSubcutaneous250 ug/mL
Injection, solutionSubcutaneous10 micrograms
Injection, solutionSubcutaneous5 micrograms
SolutionSubcutaneous250 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)
US5424286 No1996-12-012016-12-01Us
US6479065 No2000-08-102020-08-10Us
US6495164 No2000-05-252020-05-25Us
US6667061 No2000-05-252020-05-25Us
US6824822 No2002-10-092022-10-09Us
US6858576 No1997-01-062017-01-06Us
US6872700 No2000-01-142020-01-14Us
US6902744 No2000-01-142020-01-14Us
US6956026 No1998-01-072018-01-07Us
US7223440 No2001-08-312021-08-31Us
US7297761 No1997-10-152017-10-15Us
US7456254 No2005-06-302025-06-30Us
US7521423 No1997-10-152017-10-15Us
US7563871 No2004-04-152024-04-15Us
US7612176 No2005-04-132025-04-13Us
US7741269 No1998-01-072018-01-07Us
US8216180 No2008-01-122028-01-12Us
US8329648 No2006-08-182026-08-18Us
US8431685 No2005-04-132025-04-13Us
US8439864 No2008-03-252028-03-25Us
US8461105 No2005-04-132025-04-13Us
US8906851 No2006-08-182026-08-18Us
US9238076 No2004-04-152024-04-15Us
Properties
StateSolid
Experimental PropertiesNot Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
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
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 ]

Carriers

Kind
Protein
Organism
Human
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
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 July 22, 2017 12:18