Identification

Summary

Dulaglutide is a GLP-1 agonist used to manage type 2 diabetes mellitus.

Brand Names
Trulicity
Generic Name
Dulaglutide
DrugBank Accession Number
DB09045
Background

Dulaglutide, marketed by Eli Lilly as Trulicity, is a once-weekly subcutaneous glucagon-like peptide-1 (GLP-1) receptor agonist designed using recombinant DNA technology; it has been approved as an adjunct therapy to diet and exercise in the management of 2 diabetes (T2DM).5 Dulaglutide was initially approved by the FDA in 2014, and in February 2020 was approved for use in patients with T2DM and multiple cardiovascular risk factors for the prevention of cardiovascular events. It is the first T2DM drug approved to reduce major adverse cardiovascular events (MACE) risk in primary and secondary prevention populations.8

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Fusion proteins / Hormones
Protein Structure
Db09045
Protein Chemical Formula
C2646H4044N704O836S18
Protein Average Weight
59669.81 Da
Sequences
> Dulaglutide Sequence
HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGSAESKYGPPCPPCPA
PEAAGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKP
REEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTL
PPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLT
VDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLG
Download FASTA Format
Synonyms
  • Dulaglutida
  • Dulaglutide
External IDs
  • LY-2189265

Pharmacology

Indication

Dulaglutide is as an adjunct therapy to diet and exercise for glycemic control in adults with type 2 diabetes mellitus. Additionally, it is indicated to reduce the risk of major adverse cardiovascular events (MACE) in adult type 2 diabetes mellitus patients with cardiovascular disease or multiple cardiovascular risk factors.7

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Dulaglutide reduces fasting glucose concentrations and reduces postprandial glucose (PPG) concentrations in patients with type 2 diabetes mellitus through the agonism of the GLP-1 receptor.7 This drug primarily acts as an incretin mimetic hormone or analog of human glucagon-like peptide-1, which normally acts on the GLP-1 receptor.6

Mechanism of action

Dulaglutide activates the GLP-1 receptor found in pancreatic beta cells, increasing intracellular cyclic AMP (cAMP) in beta cells, leading to insulin release and subsequent reduction of blood glucose concentrations. Additionally, dulaglutide decreases glucagon secretion and slows gastric emptying.6,7

TargetActionsOrganism
AGlucagon-like peptide 1 receptor
agonist
Humans
Absorption

Dulaglutide is slowly absorbed after subcutaneous injection.9 In a pharmacokinetic study of 20 healthy adults, Cmax occurred within 24-48 hours after dosing.3 The average absolute bioavailability of dulaglutide after subcutaneous injections of single 0.75 mg and 1.5 mg doses was 65% and 47%, respectively.7

Volume of distribution

The apparent volume of distribution of dulaglutide was 3.09 L in a pharmacokinetic study; the apparent population mean peripheral volume of distribution was approximately 6 L.7

Protein binding

Protein binding information for dulaglutide is not readily available in the literature.7,9

Metabolism

Dulaglutide is presumed to be degraded into its component amino acids by general protein catabolism pathways.7

Route of elimination

Elimination of dulaglutide is expected to occur through degradation to individual amino acids.7

Half-life

In a pharmacokinetic study of 20 healthy adults, the average half-life of dulaglutide administered at various doses was approximately 3.75 days (89.9 hours). This extended half-life allows for once-weekly dosing.3 Prescribing information indicates a half-life of approximately 5 days.7

Clearance

The apparent population mean clearance of dulaglutide was 0.142 L/h in a pharmacokinetic study.7

Adverse Effects
Adverseeffects
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Toxicity

LD50 information for dulaglutide is not readily available in the literature.10 Cases of overdose with dulaglutide have resulted in gastrointestinal disturbance. Appropriate supportive treatment is recommended to manage signs and symptoms.9 Additionally, hypoglycemia has been observed after an overdose with dulaglutide; frequent plasma glucose monitoring should be performed.7

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
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Dulaglutide.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Dulaglutide.
AcebutololThe therapeutic efficacy of Dulaglutide can be increased when used in combination with Acebutolol.
AcetazolamideThe therapeutic efficacy of Dulaglutide can be increased when used in combination with Acetazolamide.
AcetohexamideDulaglutide may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Dulaglutide can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Dulaglutide.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Dulaglutide.
AducanumabThe risk or severity of adverse effects can be increased when Dulaglutide is combined with Aducanumab.
AlbiglutideThe risk or severity of hypoglycemia can be increased when Albiglutide is combined with Dulaglutide.
Interactions
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Food Interactions
  • Take with or without food.

Products

Products2
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
TrulicityInjection, solution3 mgSubcutaneousEli Lilly Nederland B.V.2021-03-03Not applicableEU flag
TrulicityInjection, solution0.75 mg/0.5mLSubcutaneousA-S Medication Solutions2014-09-18Not applicableUS flag
TrulicityInjection, solution4.5 mgSubcutaneousEli Lilly Nederland B.V.2021-03-03Not applicableEU flag
TrulicityInjection, solution3.0 mg/0.5mLSubcutaneousA-S Medication Solutions2020-09-03Not applicableUS flag
TrulicityInjection, solution1.5 mgSubcutaneousEli Lilly Nederland B.V.2021-01-12Not applicableEU flag
TrulicityInjection, solution3 mgSubcutaneousEli Lilly Nederland B.V.2021-03-03Not applicableEU flag
TrulicitySolution1.5 mg / 0.5 mLSubcutaneousEli Lilly & Co. Ltd.2015-11-24Not applicableCanada flag
TrulicityInjection, solution0.75 mg/0.5mLSubcutaneousEli Lilly Italia SPA2014-11-072017-10-23US flag
TrulicityInjection, solution1.5 mg/0.5mLSubcutaneousEli Lilly and Company2014-09-18Not applicableUS flag
TrulicityInjection, solution0.75 mgSubcutaneousEli Lilly Nederland B.V.2021-01-12Not applicableEU flag

Categories

ATC Codes
A10BJ05 — Dulaglutide
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
WTT295HSY5
CAS number
923950-08-7

References

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. [Article]
  2. Sanford M: Dulaglutide: first global approval. Drugs. 2014 Nov;74(17):2097-103. doi: 10.1007/s40265-014-0320-7. [Article]
  3. Amblee A: Mode of administration of dulaglutide: implications for treatment adherence. Patient Prefer Adherence. 2016 Jun 2;10:975-82. doi: 10.2147/PPA.S82866. eCollection 2016. [Article]
  4. Geiser JS, Heathman MA, Cui X, Martin J, Loghin C, Chien JY, de la Pena A: Clinical Pharmacokinetics of Dulaglutide in Patients with Type 2 Diabetes: Analyses of Data from Clinical Trials. Clin Pharmacokinet. 2016 May;55(5):625-34. doi: 10.1007/s40262-015-0338-3. [Article]
  5. Burness CB, Scott LJ: Dulaglutide: A Review in Type 2 Diabetes. BioDrugs. 2015 Dec;29(6):407-18. doi: 10.1007/s40259-015-0143-4. [Article]
  6. Smith LL, Mosley JF 2nd, Parke C, Brown J, Barris LS, Phan LD: Dulaglutide (Trulicity): The Third Once-Weekly GLP-1 Agonist. P T. 2016 Jun;41(6):357-60. [Article]
  7. FDA Approved Drug Products: Trulicity (dulaglutide) subcutaneous injection [Link]
  8. AJMC: FDA Approves Dulaglutide for Adults With T2D, Regardless of CVD [Link]
  9. EMA Assessment Report: Trulicity (dulaglutide) solution for injection [Link]
  10. Eli Lilly MSDS: Trulicity (dulaglutide) [Link]
UniProt
P43220
KEGG Drug
D09889
PubChem Substance
347910397
RxNav
1551291
ChEMBL
CHEMBL2108027
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dulaglutide
MSDS
Download (97.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentHyperglycemia / Type 2 Diabetes Mellitus1
4CompletedOtherType 2 Diabetes Mellitus1
4CompletedTreatmentBMI >27 kg/m2 / Healthy Subjects (HS) / Obesity (Disorder) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus2
4Enrolling by InvitationTreatmentPolycystic Ovarian Syndrome (PCOS)1
4Not Yet RecruitingTreatmentNon Alcoholic Steatohepatitis (NASH) / Type 2 Diabetes Mellitus1
4RecruitingBasic ScienceAdiposity / Decreased carbohydrate and glucose tolerance / Effect of Drugs / Overweight and Obesity1
4RecruitingPreventionStress Hyperglycaemia1
4RecruitingTreatmentOverweight or Obesity / Type 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionSubcutaneous0.75 mg
InjectionSubcutaneous1.5 mg
Injection, solutionParenteral; Subcutaneous0.75 MG
Injection, solutionParenteral; Subcutaneous1.5 MG
Injection, solutionParenteral; Subcutaneous3 MG
Injection, solutionParenteral; Subcutaneous4.5 MG
Injection, solutionSubcutaneous0.75 mg/0.5mL
Injection, solutionSubcutaneous0.75 mg
Injection, solutionSubcutaneous1.5 mg
Injection, solutionSubcutaneous1.5 mg/0.5mL
Injection, solutionSubcutaneous3 mg
Injection, solutionSubcutaneous3.0 mg/0.5mL
Injection, solutionSubcutaneous4.5 mg
Injection, solutionSubcutaneous4.5 mg/0.5mL
SolutionSubcutaneous0.75 mg / 0.5 mL
SolutionSubcutaneous1.5 mg / 0.5 mL
Injection, solutionSubcutaneous
SolutionSubcutaneous0.75 mg
SolutionSubcutaneous1.5 mg
Injection, solution0.75 mg/0.5ml
Injection, solution1.5 mg/0.5ml
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets2
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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. Sanford M: Dulaglutide: first global approval. Drugs. 2014 Nov;74(17):2097-103. doi: 10.1007/s40265-014-0320-7. [Article]
  2. FDA Approved Drug Products: Trulicity (dulaglutide) subcutaneous injection [Link]

Drug created at April 29, 2015 18:08 / Updated at October 26, 2021 21:40