Dulaglutide

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

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 indicated as an adjunct to diet and exercise to improve glycemic control in adults and pediatric patients ≥10 years of age with type 2 diabetes mellitus.⁷ It is also indicated to reduce the risk of major adverse cardiovascular events in adults with type 2 diabetes mellitus who have established cardiovascular disease or multiple cardiovascular risk factors.⁷

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Associated Conditions

Contraindications & Blackbox Warnings

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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

Target	Actions	Organism
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

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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.

Drug	Interaction
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Abciximab	The risk or severity of adverse effects can be increased when Abciximab is combined with Dulaglutide.
Acarbose	The risk or severity of hypoglycemia can be increased when Acarbose is combined with Dulaglutide.
Acebutolol	The therapeutic efficacy of Dulaglutide can be increased when used in combination with Acebutolol.
Acetazolamide	The therapeutic efficacy of Dulaglutide can be increased when used in combination with Acetazolamide.
Acetohexamide	Dulaglutide may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazole	The therapeutic efficacy of Dulaglutide can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acid	The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Dulaglutide.
Adalimumab	The risk or severity of adverse effects can be increased when Adalimumab is combined with Dulaglutide.
Aducanumab	The risk or severity of adverse effects can be increased when Dulaglutide is combined with Aducanumab.
Albiglutide	The risk or severity of hypoglycemia can be increased when Albiglutide is combined with Dulaglutide.

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Food Interactions

Take with or without food.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Trulicity	Injection, solution	3 mg	Subcutaneous	Eli Lilly Nederland B.V.	2021-03-03	Not applicable
Trulicity	Injection, solution	0.75 mg	Subcutaneous	Eli Lilly Nederland B.V.	2021-01-12	Not applicable
Trulicity	Solution	0.75 mg / 0.5 mL	Subcutaneous	Eli Lilly & Co. Ltd.	2016-01-08	Not applicable
Trulicity	Injection, solution	1.5 mg	Subcutaneous	Eli Lilly Nederland B.V.	2021-01-12	Not applicable
Trulicity	Injection, solution	0.75 mg/0.5mL	Subcutaneous	Eli Lilly Italia SPA	2014-11-07	2017-10-23
Trulicity	Injection, solution	1.5 mg	Subcutaneous	Eli Lilly Nederland B.V.	2021-01-12	2021-05-19
Trulicity	Injection, solution	4.5 mg/0.5mL	Subcutaneous	Eli Lilly and Company	2020-09-03	Not applicable
Trulicity	Solution	3 mg / 0.5 mL	Subcutaneous	Eli Lilly & Co. Ltd.	Not applicable	Not applicable
Trulicity	Injection, solution	1.5 mg/0.5mL	Subcutaneous	A-S Medication Solutions	2014-09-18	Not applicable
Trulicity	Injection, solution	4.5 mg	Subcutaneous	Eli Lilly Nederland B.V.	2021-03-03	Not applicable

Chemical Identifiers

UNII: WTT295HSY5
CAS number: 923950-08-7

References

General References

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]
Sanford M: Dulaglutide: first global approval. Drugs. 2014 Nov;74(17):2097-103. doi: 10.1007/s40265-014-0320-7. [Article]
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]
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]
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]
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]
FDA Approved Drug Products: Trulicity (dulaglutide) subcutaneous injection [Link]
AJMC: FDA Approves Dulaglutide for Adults With T2D, Regardless of CVD [Link]
EMA Assessment Report: Trulicity (dulaglutide) solution for injection [Link]
Eli Lilly MSDS: Trulicity (dulaglutide) [Link]

External Links

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

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Basic Science	Adiposity / Decreased carbohydrate and glucose tolerance / Effect of Drugs / Overweight and Obesity	1
4	Active Not Recruiting	Treatment	Hyperglycemia / Type 2 Diabetes Mellitus	1
4	Active Not Recruiting	Treatment	Type 2 Diabetes Mellitus	1
4	Completed	Other	Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Diabetes Mellitus	1
4	Completed	Treatment	Healthy Subjects (HS) / Obesity / Overweight / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Polycystic Ovarian Syndrome (PCOS)	1
4	Completed	Treatment	Type 2 Diabetes Mellitus	2
4	Not Yet Recruiting	Treatment	Metabolic-associated Fatty Liver Disease / Type 2 Diabetes Mellitus	1
4	Not Yet Recruiting	Treatment	Non Alcoholic Steatohepatitis (NASH) / Type 2 Diabetes Mellitus	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection	Subcutaneous	0.75 mg
Injection	Subcutaneous	1.5 mg
Injection, solution	Parenteral; Subcutaneous	0.75 MG
Injection, solution	Parenteral; Subcutaneous	1.5 MG
Injection, solution	Parenteral; Subcutaneous	3 MG
Injection, solution	Parenteral; Subcutaneous	4.5 MG
Injection, solution	Subcutaneous	0.75 mg/0.5mL
Injection, solution	Subcutaneous	1.5 mg/0.5mL
Injection, solution	Subcutaneous	3 mg
Injection, solution	Subcutaneous	3.0 mg/0.5mL
Injection, solution	Subcutaneous	4.5 mg
Injection, solution	Subcutaneous	4.5 mg/0.5mL
Solution	Subcutaneous	0.75 mg / 0.5 mL
Solution	Subcutaneous	1.5 mg / 0.5 mL
Solution	Subcutaneous	1.500 mg
Solution	Subcutaneous	3 mg / 0.5 mL
Solution	Subcutaneous	4.5 mg / 0.5 mL
Injection, solution	Subcutaneous	0.75 mg
Injection, solution	Subcutaneous	1.5 mg
Solution	Subcutaneous	0.75 mg
Solution	Subcutaneous	1.5 mg
Injection, solution		0.75 mg/0.5ml
Injection, solution		1.5 mg/0.5ml

Prices

Not Available

Patents

Not Available

Properties

State: Liquid
Experimental Properties: Not Available

Targets

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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

Sanford M: Dulaglutide: first global approval. Drugs. 2014 Nov;74(17):2097-103. doi: 10.1007/s40265-014-0320-7. [Article]
Umpierrez G, Tofe Povedano S, Perez Manghi F, Shurzinske L, Pechtner V: Efficacy and safety of dulaglutide monotherapy versus metformin in type 2 diabetes in a randomized controlled trial (AWARD-3). Diabetes Care. 2014 Aug;37(8):2168-76. doi: 10.2337/dc13-2759. Epub 2014 May 19. [Article]
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]
Skrivanek Z, Gaydos BL, Chien JY, Geiger MJ, Heathman MA, Berry S, Anderson JH, Forst T, Milicevic Z, Berry D: Dose-finding results in an adaptive, seamless, randomized trial of once-weekly dulaglutide combined with metformin in type 2 diabetes patients (AWARD-5). Diabetes Obes Metab. 2014 Aug;16(8):748-56. doi: 10.1111/dom.12305. Epub 2014 May 22. [Article]
Lorenz M, Lawson F, Owens D, Raccah D, Roy-Duval C, Lehmann A, Perfetti R, Blonde L: Differential effects of glucagon-like peptide-1 receptor agonists on heart rate. Cardiovasc Diabetol. 2017 Jan 13;16(1):6. doi: 10.1186/s12933-016-0490-6. [Article]
Giorgino F, Benroubi M, Sun JH, Zimmermann AG, Pechtner V: Efficacy and Safety of Once-Weekly Dulaglutide Versus Insulin Glargine in Patients With Type 2 Diabetes on Metformin and Glimepiride (AWARD-2). Diabetes Care. 2015 Dec;38(12):2241-9. doi: 10.2337/dc14-1625. Epub 2015 Jun 18. [Article]
Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [Article]
Miyagawa J, Odawara M, Takamura T, Iwamoto N, Takita Y, Imaoka T: Once-weekly glucagon-like peptide-1 receptor agonist dulaglutide is non-inferior to once-daily liraglutide and superior to placebo in Japanese patients with type 2 diabetes: a 26-week randomized phase III study. Diabetes Obes Metab. 2015 Oct;17(10):974-83. doi: 10.1111/dom.12534. Epub 2015 Aug 20. [Article]
Htike ZZ, Zaccardi F, Papamargaritis D, Webb DR, Khunti K, Davies MJ: Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis. Diabetes Obes Metab. 2017 Apr;19(4):524-536. doi: 10.1111/dom.12849. Epub 2017 Feb 17. [Article]
Nauck M, Weinstock RS, Umpierrez GE, Guerci B, Skrivanek Z, Milicevic Z: Efficacy and safety of dulaglutide versus sitagliptin after 52 weeks in type 2 diabetes in a randomized controlled trial (AWARD-5). Diabetes Care. 2014 Aug;37(8):2149-58. doi: 10.2337/dc13-2761. Epub 2014 Apr 17. [Article]
Tamaki C, Takeuchi M, Iwamoto N, Glaesner W: [Pharmacological profile and clinical trial results of a long-acting, once weekly human GLP-1 receptor agonist Dulaglutide (Genetical Recombination)]. Nihon Yakurigaku Zasshi. 2015 Oct;146(4):215-24. doi: 10.1254/fpj.146.215. [Article]
FDA Approved Drug Products: Trulicity (dulaglutide) subcutaneous injection [Link]

Drug created at April 29, 2015 18:08 / Updated at November 22, 2022 18:59

Dulaglutide

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References