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| Primary information |
|---|
| ID | 10756 |
| Therapeutic ID | Th1176 |
| Protein Name | Dulaglutide |
| Sequence | >Th1176_Dulaglutide
HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGSAESKYGPPCPPCPAPEAAGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLG
|
| Molecular Weight | 59669.81 |
| Chemical Formula | C2646H4044N704O836S18 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | Approximately 5 days. |
| 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 Trulicityâ„¢. 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. |
| Indication/Disease | Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. |
| Pharmacodynamics | Dulaglutide 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 Action | Dulaglutide 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. |
| Toxicity | LD50 information for dulaglutide is not readily available in the literature.[L34685] Cases of overdose with dulaglutide have resulted in gastrointestinal disturbance. Appropriate supportive treatment is recommended to manage signs and symptoms.[L34670] Additionally, hypoglycemia has been observed after an overdose with dulaglutide; frequent plasma glucose monitoring should be performed.[L30380] |
| Metabolism | Dulaglutide is presumed to be degraded into its component amino acids by general protein catabolism pathways.[L30380] |
| Absorption | Dulaglutide is slowly absorbed after subcutaneous injection.[L34670] In a pharmacokinetic study of 20 healthy adults, Cmax occurred within 24-48 hours after dosing.[A234419] The average absolute bioavailability of dulaglutide after subcutaneous injections of single 0.75 mg and 1.5 mg doses was 65% and 47%, respectively.[L30380] |
| 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.[L30380] |
| Clearance | The apparent population mean clearance of dulaglutide was 0.142 L/h in a pharmacokinetic study.[L30380] |
| Categories | Alimentary Tract and Metabolism,Amino Acids, Peptides, and Proteins,Blood Glucose Lowering Agents,Blood Proteins,Drugs Used in Diabetes,Gastrointestinal Hormones,Globulins,GLP-1 Agonists,Glucagon-like peptide-1 (GLP-1) analogues,Hormones,Hormones, Hormone Substitutes, and Hormone Antagonists,Immunoglobulin Fragments,Immunoglobulins,Immunoproteins,Incretin Mimetics,Pancreatic Hormones,Peptide Fragments,Peptide Hormones,Peptides,Proglucagon,Protein Precursors,Proteins,Recombinant Proteins,Serum Globulins |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Acetylsalicylic acid may increase the hypoglycemic activities of Dulaglutide; Dulaglutide may increase the hypoglycemic activities of Chlorpropamide; Dihydrotestosterone may increase the hypoglycemic activities of Dulaglutide; Dulaglutide may increase the hypoglycemic activities of Insulin Regular; Dulaglutide may increase the hypoglycemic activities of Insulin Lispro; The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Leuprolide; Lipoic Acid may increase the hypoglycemic activities of Dulaglutide; Oxandrolone may increase the hypoglycemic activities of Dulaglutide; Paroxetine may increase the hypoglycemic activities of Dulaglutide; Pegvisomant may increase the hypoglycemic activities of Dulaglutide. |
| Target | Glucagon-like peptide 1 receptor |
| Brand Name | NA |
| Company | NA |
| Brand Description | NA |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | NA |
| Useful Link 2 | NA |
| Remarks | NA |