tirzepatide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| peptides and glycopeptides | 5516 | 2023788-19-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tirzepatide is a GIP receptor and GLP-1 receptor agonist. It is a 39-amino-acid modified peptide with a C20 fatty diacid moiety that enables albumin binding and prolongs the half-life. Tirzepatide selectively binds to and activates both the GIP and GLP-1 receptors, the targets for native GIP and GLP-1. Tirzepatide enhances first- and second-phase insulin secretion, and reduces glucagon levels, both in a glucosedependent manner.
|
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 15, 2022 | EMA | ELI LILLY NEDERLAND B.V. | |
| May 13, 2022 | FDA | ELI LILLY CO | |
| Sept. 26, 2022 | PMDA | ELI LILLY JAPAN K.K |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Incorrect dose administered | 451.56 | 42.42 | 123 | 1169 | 59845 | 63427885 |
| Injection site pain | 140.90 | 42.42 | 63 | 1229 | 129737 | 63357993 |
| Off label use | 127.82 | 42.42 | 106 | 1186 | 674356 | 62813374 |
| Inappropriate schedule of product administration | 77.30 | 42.42 | 39 | 1253 | 103926 | 63383804 |
| Nausea | 72.40 | 42.42 | 87 | 1205 | 854384 | 62633346 |
| Injection site erythema | 61.17 | 42.42 | 31 | 1261 | 83143 | 63404587 |
| Injection site rash | 59.65 | 42.42 | 20 | 1272 | 18789 | 63468941 |
| Injection site pruritus | 45.80 | 42.42 | 21 | 1271 | 45095 | 63442635 |
| Extra dose administered | 42.56 | 42.42 | 12 | 1280 | 6338 | 63481392 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Incorrect dose administered | 65.23 | 53.22 | 22 | 356 | 40493 | 34916060 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Incorrect dose administered | 216.77 | 48.63 | 61 | 645 | 76569 | 79667113 |
| Off label use | 81.34 | 48.63 | 65 | 641 | 907150 | 78836532 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BX16 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Other blood glucose lowering drugs, excl. insulins |
| MeSH PA | D006728 | Hormones |
| MeSH PA | D054795 | Incretins |
| FDA MoA | N0000000152 | G-Protein-linked Receptor Interactions |
| FDA MoA | N0000020058 | Glucagon-like Peptide-1 (GLP-1) Agonists |
| FDA EPC | N0000178480 | GLP-1 Receptor Agonist |
| CHEBI has role | CHEBI:35526 | antidiabetic |
| CHEBI has role | CHEBI:64088 | incretin mimetics |
| CHEBI has role | CHEBI:71196 | GLP-1 receptor agonist |
| CHEBI has role | CHEBI:74518 | anti-obestic agents |
| CHEBI has role | CHEBI:194187 | gastric inhibitory polypeptide receptor agonists |
| FDA EPC | N0000194015 | Glucose-dependent Insulinotropic Polypeptide Receptor Agonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
| Multiple endocrine neoplasia, type 2 | contraindication | 61808009 | |
| Medullary thyroid carcinoma | contraindication | 255032005 | DOID:3973 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 10MG/0.5ML (10MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9474780 | Jan. 5, 2036 | MOUNJARO IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS |
| 12.5MG/0.5ML (12.5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9474780 | Jan. 5, 2036 | MOUNJARO IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS |
| 15MG/0.5ML (15MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9474780 | Jan. 5, 2036 | MOUNJARO IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS |
| 2.5MG/0.5ML (2.5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9474780 | Jan. 5, 2036 | MOUNJARO IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS |
| 5MG/0.5ML (5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9474780 | Jan. 5, 2036 | MOUNJARO IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS |
| 7.5MG/0.5ML (7.5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9474780 | Jan. 5, 2036 | MOUNJARO IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 10MG/0.5ML (10MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | May 13, 2027 | NEW CHEMICAL ENTITY |
| 12.5MG/0.5ML (12.5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | May 13, 2027 | NEW CHEMICAL ENTITY |
| 15MG/0.5ML (15MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | May 13, 2027 | NEW CHEMICAL ENTITY |
| 2.5MG/0.5ML (2.5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | May 13, 2027 | NEW CHEMICAL ENTITY |
| 5MG/0.5ML (5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | May 13, 2027 | NEW CHEMICAL ENTITY |
| 7.5MG/0.5ML (7.5MG/0.5ML) | MOUNJARO | ELI LILLY AND CO | N215866 | May 13, 2022 | RX | SOLUTION | SUBCUTANEOUS | May 13, 2027 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Glucagon-like peptide 1 receptor | GPCR | AGONIST | Ki | 8.37 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Gastric inhibitory polypeptide receptor | GPCR | AGONIST | Ki | 9.87 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:194186 | CHEBI |
| CHEMBL4297839 | ChEMBL_ID |
| C000629749 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11429 | IUPHAR_LIGAND_ID |
| DB15171 | DRUGBANK_ID |
| 019067 | NDDF |
| 4041425 | VANDF |
| C5139934 | UMLSCUI |
| D11360 | KEGG_DRUG |
| 10849 | INN_ID |
| 2023788-19-2 | SECONDARY_CAS_RN |
| 163285897 | PUBCHEM_CID |
| 2601723 | RXNORM |
| 359156 | MMSL |
| 40683 | MMSL |
| d09892 | MMSL |
| OYN3CCI6QE | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1152 | INJECTION, SOLUTION | 2.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1243 | INJECTION, SOLUTION | 5 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1457 | INJECTION, SOLUTION | 15 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1457 | INJECTION, SOLUTION | 15 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1457 | INJECTION, SOLUTION | 15 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1460 | INJECTION, SOLUTION | 12.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1460 | INJECTION, SOLUTION | 12.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1460 | INJECTION, SOLUTION | 12.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1471 | INJECTION, SOLUTION | 10 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1471 | INJECTION, SOLUTION | 10 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1471 | INJECTION, SOLUTION | 10 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1484 | INJECTION, SOLUTION | 7.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1484 | INJECTION, SOLUTION | 7.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1484 | INJECTION, SOLUTION | 7.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1495 | INJECTION, SOLUTION | 5 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1495 | INJECTION, SOLUTION | 5 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1495 | INJECTION, SOLUTION | 5 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1506 | INJECTION, SOLUTION | 2.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1506 | INJECTION, SOLUTION | 2.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-1506 | INJECTION, SOLUTION | 2.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-2214 | INJECTION, SOLUTION | 7.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-2340 | INJECTION, SOLUTION | 10 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-2423 | INJECTION, SOLUTION | 12.50 mg | SUBCUTANEOUS | NDA | 36 sections |
| MOUNJARO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-3002 | INJECTION, SOLUTION | 15 mg | SUBCUTANEOUS | NDA | 36 sections |