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| Primary information |
|---|
| ID | 16384 |
| Therapeutic ID | Th1894 |
| Protein Name | Tirzepatide |
| Sequence | >Th1894_Tirzepatide
YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS
|
| Molecular Weight | 4810.52 Da |
| Chemical Formula | C225H348N48O68 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | ,The half-life is approximately five days. |
| Description | Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Dual GIP/GLP-1 agonists gained increasing attention as new therapeutic agents for glycemic and weight control as they demonstrated better glucose control and weight loss compared to selective GLP-1 receptor agonists in preclinical and clinical trials. |
| Indication/Disease | Tirzepatide is a dual GIP and GLP-1 receptor agonist used for the treatment of type II diabetes in adults as an adjunct to diet and exercise. |
| Pharmacodynamics | Tirzepatide is a synthetic peptide with glucose-lowering effects. It works to stimulate first- and second-phase insulin secretion, and reduces glucagon levels, both in a glucose-dependent manner. Tirzepatide was also shown to delay gastric emptying, lower fasting and postprandial glucose concentration, decrease food intake,4 and reduce body weight in patients with type 2 diabetes. Tirzepatide can increase insulin sensitivity. |
| Mechanism of Action | Glucagon-like peptide-1 (GLP-1) receptors (GLP-1R) are expressed throughout the body, including pancreatic beta-cells and the gastrointestinal tract. They have been implicated in the pathophysiology of type II diabetes mellitus as GLP-1R signalling is involved in glucose control by enhancing glucose-stimulated insulin secretion, delaying gastric transit, decreasing plasma glucagon levels, and reducing body weight by activating anorexigenic pathways in the brain. Both glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 are peptide hormones involved in glucose homeostasis: they promote glucose-stimulated insulin secretion from the pancreatic beta-cells. However, GIP is the main incretin hormone that exerts insulinotropic effects in response to food intake. |
| Toxicity | There is limited information regarding the LD50 and overdose of tirzepatide. In case of an overdosage, appropriate supportive treatment should be initiated with a sufficient amount of time for observation and treatment, as tirzepatide has a long half-life. |
| Metabolism | Tirzepatide is metabolized by proteolytic cleavage of the peptide backbone, beta-oxidation of the C20 fatty diacid moiety, and amide hydrolysis. |
| Absorption | Over the dose range of 1-5 mg, the Cmax of tirzepatide ranged from 108 to 397 ng/mL.The mean absolute bioavailability of tirzepatide following subcutaneous administration is 80%. Following subcutaneous administration, the Tmax ranged from eight to 72 hours. The steady-state plasma concentrations were achieved following four weeks of once-weekly subcutaneous administration. |
| Following subcutaneous administration, the mean steady-state volume of distribution was 9.5 L. The mean apparent steady-state volume of distribution of tirzepatide following subcutaneous administration in patients with type 2 diabetes mellitus was approximately 10.3 L. |
| Clearance | The apparent population mean clearance of tirzepatide is 0.061 L/h.4 The mean steady-state apparent clearance of tirzepatide was 0.056 L/h. |
| Categories | Amino Acids, Peptides, and Proteins,Blood Glucose Lowering Agents,Gastrointestinal Hormones,GLP-1 Agonists,Hormones,Hormones, Hormone Substitutes, and Hormone Antagonists,Incretins,Nerve Tissue Proteins,Neuropeptides,Peptide Hormones,Peptides,Proteins |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Glucagon-like peptide 1 receptor, Gastric inhibitory polypeptide |
| Brand Name | Mounjaro |
| Company | Eli Lilly and Company |
| Brand Description | Eli Lilly and Company |
| Prescribed For | Subcutaneous |
| Chemical Name | 12.5 mg/0.5mL |
| Formulation | MOUNJARO is contraindicated in patients with: A personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 |
| Physical Appearance | hives, difficulty breathing, swelling of your face, lips, tongue, or throat, dizziness, fast heart rate, shaking, sweating, nervousness, anxiety, irritability, confusion, dizziness, hunger, pain in the upper right side of your abdomen, pain spreading to your back or below the shoulder blade, nausea, vomiting, fever, yellowing of the skin and eyes (jaundice), clay-colored stools, and bloating of the abdomen |
| Route of Administration | MOUNJARO (tirzepatide) injection, for subcutaneous use, contains tirzepatide, a once weekly GIP receptor and GLP-1 receptor agonist. It is a 39-amino-acid modified peptide based on the GIP sequence. Tirzepatide contains 2 non-coded amino acids (aminoisobutyric acid, Aib) in positions 2 and 13, a C-terminal amide, and Lys residue at position 20 that is attached to 1,20-eicosanedioic acid via a linker. |
| Recommended Dosage | Mounjaro (tirzepatide) Injection is a prescription medicine used to treat the symptoms of Type 2 Diabetes Mellitus. |
| Contraindication | NA |
| Side Effects | MOUNJARO is a clear, colorless to slightly yellow, sterile, preservative-free solution for subcutaneous use. Each singledose pen contains a 0.5 mL solution of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg, or 15 mg of tirzepatide and the following excipients: sodium chloride (4.1 mg), sodium phosphate dibasic heptahydrate (0.7 mg), and water for injection. Hydrochloric acid solution and/or sodium hydroxide solution may have been added to adjust the pH. MOUNJARO has a pH of 6.5 – 7.5. |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |