sotagliflozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sodium glucose co-transporter inhibitors, phlorizin derivatives | 5339 | 1018899-04-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Sotagliflozin is a dual inhibitor of sodium glucose cotransporter type 1 (SGLT1) and SGLT2. Local intestinal inhibition of SGLT1, the major transporter for glucose absorption, delays and reduces glucose absorption in the proximal intestine, resulting in a blunting and delay of postprandial hyperglycaemia. SGLT2 is the predominant transporter responsible for reabsorption of glucose from the glomerular filtrate back into the circulation. By inhibiting SGLT2, sotagliflozin 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:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 26, 2019 | EMA | SANOFI-AVENTIS GROUPE | |
| May 26, 2023 | FDA | LEXICON PHARMS INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BK06 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sodium-glucose co-transporter 2 (SGLT2) inhibitors |
| MeSH PA | D007004 | Hypoglycemic Agents |
| MeSH PA | D000077203 | Sodium-Glucose Transporter 2 Inhibitors |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000187058 | Sodium-Glucose Transporter 2 Inhibitors |
| FDA EPC | N0000187059 | Sodium-Glucose Cotransporter 2 Inhibitor |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 at increased risk of cardiovascular disease | indication | 44054006 | DOID:9352 |
| Diabetes mellitus type 1 | indication | 46635009 | DOID:9744 |
| Heart failure | indication | 84114007 | DOID:6000 |
| Chronic kidney disease at increased risk of cardiovascular disease | indication | 709044004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.45 | acidic |
| pKa2 | 13.37 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 200MG | INPEFA | LEXICON PHARMS INC | N216203 | May 26, 2023 | RX | TABLET | ORAL | 7781577 | May 4, 2028 | REDUCTION OF RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE IN ADULTS WITH HEART FAILURE OR TYPE 2 DIABETES MELLITUS, CHRONIC KIDNEY DISEASE, AND OTHER CARDIOVASCULAR RISK FACTORS |
| 400MG | INPEFA | LEXICON PHARMS INC | N216203 | May 26, 2023 | RX | TABLET | ORAL | 7781577 | May 4, 2028 | REDUCTION OF RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE IN ADULTS WITH HEART FAILURE OR TYPE 2 DIABETES MELLITUS, CHRONIC KIDNEY DISEASE, AND OTHER CARDIOVASCULAR RISK FACTORS |
| 200MG | INPEFA | LEXICON PHARMS INC | N216203 | May 26, 2023 | RX | TABLET | ORAL | 8476413 | May 29, 2028 | REDUCTION OF RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE IN ADULTS WITH HEART FAILURE OR TYPE 2 DIABETES MELLITUS, CHRONIC KIDNEY DISEASE, AND OTHER CARDIOVASCULAR RISK FACTORS |
| 400MG | INPEFA | LEXICON PHARMS INC | N216203 | May 26, 2023 | RX | TABLET | ORAL | 8476413 | May 29, 2028 | REDUCTION OF RISK OF CARDIOVASCULAR DEATH, HOSPITALIZATION FOR HEART FAILURE, AND URGENT HEART FAILURE IN ADULTS WITH HEART FAILURE OR TYPE 2 DIABETES MELLITUS, CHRONIC KIDNEY DISEASE, AND OTHER CARDIOVASCULAR RISK FACTORS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 200MG | INPEFA | LEXICON PHARMS INC | N216203 | May 26, 2023 | RX | TABLET | ORAL | May 26, 2028 | NEW CHEMICAL ENTITY |
| 400MG | INPEFA | LEXICON PHARMS INC | N216203 | May 26, 2023 | RX | TABLET | ORAL | May 26, 2028 | NEW CHEMICAL ENTITY |
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 | 8.75 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Sodium/glucose cotransporter 1 | Transporter | INHIBITOR | IC50 | 7.44 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 6B4ZBS263Y | UNII |
| C3502471 | UMLSCUI |
| CHEMBL3039507 | ChEMBL_ID |
| 24831714 | PUBCHEM_CID |
| DB12713 | DRUGBANK_ID |
| D10669 | KEGG_DRUG |
| 9824 | INN_ID |
| C575681 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8312 | IUPHAR_LIGAND_ID |
| 019461 | NDDF |
| 4042306 | VANDF |
| 2638675 | RXNORM |
| 367663 | MMSL |
| 41581 | MMSL |
| d10056 | MMSL |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| INPEFA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70183-220 | TABLET | 200 mg | ORAL | NDA | 29 sections |
| INPEFA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70183-240 | TABLET | 400 mg | ORAL | NDA | 29 sections |