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ertugliflozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sodium glucose co-transporter inhibitors, phlorizin derivatives | 5270 | 1210344-57-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
SGLT2 is the predominant transporter responsible for reabsorption of glucose from the glomerular filtrate back into the circulation. Ertugliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, ertugliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.64 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1 | 16 | |||
| kinase-selectivity-class | AXL,GRK2,MAP2K6 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 21, 2018 | EMA | Merck Sharp & Dohme Limited | |
| Dec. 19, 2017 | FDA | MERCK SHARP DOHME |
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 |
|---|---|---|---|---|---|---|
| Diabetes mellitus inadequate control | 79.32 | 59.16 | 17 | 278 | 18667 | 90609485 |
| BRASH syndrome | 79.23 | 59.16 | 12 | 283 | 1867 | 90626285 |
| Diabetic ketoacidosis | 64.07 | 59.16 | 15 | 280 | 24392 | 90603760 |
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 |
|---|---|---|---|---|---|---|
| Diabetic ketosis | 106.19 | 55.08 | 13 | 210 | 254 | 42620858 |
| Diabetic ketoacidosis | 89.12 | 55.08 | 21 | 202 | 22346 | 42598766 |
| Urine ketone body present | 62.47 | 55.08 | 10 | 213 | 1384 | 42619728 |
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 |
|---|---|---|---|---|---|---|
| Diabetic ketoacidosis | 145.80 | 47.05 | 35 | 511 | 42023 | 110546730 |
| Diabetic ketosis | 139.45 | 47.05 | 19 | 527 | 917 | 110587836 |
| Urine ketone body present | 92.04 | 47.05 | 16 | 530 | 3830 | 110584923 |
| BRASH syndrome | 65.93 | 47.05 | 12 | 534 | 3711 | 110585042 |
| Diabetes mellitus inadequate control | 64.17 | 47.05 | 17 | 529 | 29758 | 110558995 |
| Euglycaemic diabetic ketoacidosis | 63.20 | 47.05 | 14 | 532 | 11609 | 110577144 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BD23 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs |
| ATC | A10BD24 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs |
| ATC | A10BK04 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sodium-glucose co-transporter 2 (SGLT2) inhibitors |
| MeSH PA | D000077203 | Sodium-Glucose Transporter 2 Inhibitors |
| MeSH PA | D007004 | Hypoglycemic Agents |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
A10BD Combinations of oral blood glucose lowering drugs 19 drugs
A10BK Sodium-glucose co-transporter 2 (SGLT2) inhibitors 7 drugs
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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.68 | acidic |
| pKa2 | 12.61 | acidic |
| pKa3 | 13.22 | acidic |
| pKa4 | 13.51 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 15MG;EQ 100MG BASE | STEGLUJAN | MSD SUB MERCK | N209805 | Dec. 19, 2017 | RX | TABLET | ORAL | 7326708 | Nov. 24, 2026 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 5MG;EQ 100MG BASE | STEGLUJAN | MSD SUB MERCK | N209805 | Dec. 19, 2017 | RX | TABLET | ORAL | 7326708 | Nov. 24, 2026 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 15MG;EQ 100MG BASE | STEGLUJAN | MSD SUB MERCK | N209805 | Dec. 19, 2017 | RX | TABLET | ORAL | 9439901 | Oct. 21, 2030 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 5MG;EQ 100MG BASE | STEGLUJAN | MSD SUB MERCK | N209805 | Dec. 19, 2017 | RX | TABLET | ORAL | 9439901 | Oct. 21, 2030 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 2.5MG;1GM | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 9439902 | Oct. 21, 2030 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 2.5MG;500MG | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 9439902 | Oct. 21, 2030 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 7.5MG;1GM | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 9439902 | Oct. 21, 2030 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 7.5MG;500MG | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 9439902 | Oct. 21, 2030 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 15MG | STEGLATRO | MSD SUB MERCK | N209803 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 5MG | STEGLATRO | MSD SUB MERCK | N209803 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 15MG;EQ 100MG BASE | STEGLUJAN | MSD SUB MERCK | N209805 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 5MG;EQ 100MG BASE | STEGLUJAN | MSD SUB MERCK | N209805 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 2.5MG;1GM | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 2.5MG;500MG | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 7.5MG;1GM | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 7.5MG;500MG | SEGLUROMET | MSD SUB MERCK | N209806 | Dec. 19, 2017 | RX | TABLET | ORAL | 8080580 | Dec. 19, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium/glucose cotransporter 2 | Transporter | INHIBITOR | IC50 | 9.06 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Low affinity sodium-glucose cotransporter | Transporter | IC50 | 9.06 | CHEMBL | |||||
| Sodium/glucose cotransporter 1 | Transporter | INHIBITOR | IC50 | 5.71 | SCIENTIFIC LITERATURE | ||||
| Sodium/glucose cotransporter 2 | Transporter | IC50 | 8.94 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 6C282481IP | UNII |
| 4037222 | VANDF |
| C4079805 | UMLSCUI |
| CHEBI:188719 | CHEBI |
| CHEMBL1770248 | ChEMBL_ID |
| CHEMBL5315054 | ChEMBL_ID |
| 44814423 | PUBCHEM_CID |
| DB11827 | DRUGBANK_ID |
| D10313 | KEGG_DRUG |
| 9460 | INN_ID |
| C570288 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8376 | IUPHAR_LIGAND_ID |
| 1162393006 | SNOMEDCT_US |
| 764274008 | SNOMEDCT_US |
| 764275009 | SNOMEDCT_US |
| 267231 | MMSL |
| 33351 | MMSL |
| d08689 | MMSL |
| 017435 | NDDF |
| 017436 | NDDF |
| 1992672 | RXNORM |
Pharmaceutical products:
None