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Identification
NameDulaglutide
Accession NumberDB09045
TypeBiotech
GroupsApproved
Description

Dulaglutide is a novel glucagon-like peptide-1 agonist (GLP-1) biologic drug consisting of a dipeptidyl peptidase-IV-protected GLP-1 analogue covalently linked to a human IgG4-Fc heavy chain by a small peptide linker. Dulaglutide is indicated in the treatment of type 2 diabetes and can be used once a week. It was approved by the FDA in September 2014. Dulaglutide is manufactured and marketed by Eli Lily under the brand Trulicity™. It is not known if dulaglutide can increase the risk of medullary thyroid carcinoma or multiple endocrine neoplasia syndrome type 2, and is thus not recommended for use in populations with a personal or family history of these conditions.

Protein structureDb09045
Related Articles
Protein chemical formulaC2646H4044N704O836S18
Protein average weight59669.81 Da
Sequences
> Dulaglutide Sequence
HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGSAESKYGPPCPPCPA
PEAAGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKP
REEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTL
PPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLT
VDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLG
Download FASTA Format
SynonymsNot Available
External Identifiers
  • LY-2189265
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Trulicityinjection, solution.75 mg/.5mLsubcutaneousEli Lilly and Company2014-11-07Not applicableUs
Trulicitysolution1.5 mgsubcutaneousEli Lilly Canada IncNot applicableNot applicableCanada
Trulicitysolution0.75 mgsubcutaneousEli Lilly Canada IncNot applicableNot applicableCanada
Trulicitysolution1.5 mgsubcutaneousEli Lilly Canada Inc2015-11-24Not applicableCanada
Trulicitysolution0.75 mgsubcutaneousEli Lilly Canada Inc2016-01-08Not applicableCanada
Trulicityinjection, solution1.5 mg/.5mLsubcutaneousEli Lilly and Company2014-11-07Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIWTT295HSY5
CAS number923950-08-7
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
Pharmacology
IndicationIndicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
PharmacodynamicsDulaglutide activates human glucagon-like peptide-1 receptors, thus increasing intracellular cyclic AMP in beta cells. This, in turn, increases glucose-dependent insulin release. Dulaglutide also reduces glucagon secretion and slows gastric emptying.
Mechanism of actionDulaglutide is a human GLP-1 receptor agonist with 90% amino acid sequence homology to endogenous human GLP-1 (7-37). Dulaglutide activates the GLP-1 receptor, a membrane-bound cell-surface receptor coupled to adenylyl cyclase in pancreatic beta cells. Dulaglutide increases intracellular cyclic AMP (cAMP) in beta cells leading to glucose-dependent insulin release. Dulaglutide also decreases glucagon secretion and slows gastric emptying.
Related Articles
AbsorptionMaximum plasma concentration (Cmax) is achieved in 24–72 h (median 48 h) after a subcutaneous injection administered at a steady state.
Volume of distribution

After subcutaneous administration of 0.75 mg and 1.5 mg to steady state were approximately 19.2 L (range 14.3 to 26.4 L) and 17.4 L (range 9.3 to 33 L), respectively.

Protein bindingNot Available
Metabolism

Dulaglutide is presumed to be degraded into its component amino acids by general protein catabolism pathways.

Route of eliminationNot Available
Half lifeApproximately 5 days.
Clearance

The mean apparent clearance at steady state of dulaglutide is approximately 0.111 L/h for the 0.75 mg dose, and 0.107 L/h for the 1.5 mg dose.

Toxicity-RISK OF THYROID C-CELL TUMORS -Dulaglutide is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN2). Routine serum calcitonin or thyroid ultrasound monitoring is of uncertain value in patients treated with Dulaglutide.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, solutionsubcutaneous.75 mg/.5mL
Injection, solutionsubcutaneous1.5 mg/.5mL
Solutionsubcutaneous0.75 mg
Solutionsubcutaneous1.5 mg
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Nadkarni P, Chepurny OG, Holz GG: Regulation of glucose homeostasis by GLP-1. Prog Mol Biol Transl Sci. 2014;121:23-65. doi: 10.1016/B978-0-12-800101-1.00002-8. [PubMed:24373234 ]
  2. Sanford M: Dulaglutide: first global approval. Drugs. 2014 Nov;74(17):2097-103. doi: 10.1007/s40265-014-0320-7. [PubMed:25367716 ]
External Links
ATC CodesA10BX14
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (97.1 KB)
Interactions
Drug Interactions
Drug
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Dulaglutide.
ChlorpropamideDulaglutide may increase the hypoglycemic activities of Chlorpropamide.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Dulaglutide.
Insulin HumanDulaglutide may increase the hypoglycemic activities of Insulin Regular.
Insulin LisproDulaglutide may increase the hypoglycemic activities of Insulin Lispro.
LeuprolideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Leuprolide.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Dulaglutide.
OxandroloneOxandrolone may increase the hypoglycemic activities of Dulaglutide.
ParoxetineParoxetine may increase the hypoglycemic activities of Dulaglutide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Dulaglutide.
PhenelzinePhenelzine may increase the hypoglycemic activities of Dulaglutide.
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Dulaglutide.
TestosteroneTestosterone may increase the hypoglycemic activities of Dulaglutide.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Dulaglutide.
TrichlormethiazideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Trichlormethiazide.
Food InteractionsNot 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. Sanford M: Dulaglutide: first global approval. Drugs. 2014 Nov;74(17):2097-103. doi: 10.1007/s40265-014-0320-7. [PubMed:25367716 ]
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Drug created on April 29, 2015 12:08 / Updated on August 17, 2016 12:24