Clinical data | |
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Trade names | Jardiance, others |
Other names | BI-10773 |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a614043 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth |
Drug class | Sodium-glucose cotransporter-2 (SGLT2) inhibitor [2] |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
ECHA InfoCard | 100.122.058 |
Chemical and physical data | |
Formula | C23H27ClO7 |
Molar mass | 450.91 g·mol−1 |
3D model ( JSmol) | |
| |
|
Empagliflozin, sold under the brand name Jardiance, among others, is an antidiabetic medication used to improve glucose control in people with type 2 diabetes. [10] [2] [12] It is not recommended for type 1 diabetes. [2] [13] It is taken by mouth. [2]
Common side effects include hyperventilation, anorexia, abdominal pain, nausea, vomiting, lethargy, mental status changes, hypotension, acute kidney injury, and vaginal yeast infections. [2] Rarer but more serious side effects include a skin infection of the groin called Fournier's gangrene and a form of diabetic ketoacidosis with normal blood sugar levels. [2] [14] Use during pregnancy or breastfeeding is not recommended. [15] Cautiously use empagliflozin with frequent monitoring of renal function in those with significant kidney disease, the use of empagliflozin for merely hyperglycaemia is not currently recommended given the risk of adverse events. The use of empagliflozin in patients with known cardiovascular disease may be beneficial, but risk and benefit ratio need to be considered and initiation of therapy should be individualised. It was also shown to help slow the progression of mild kidney problems.
Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), and works by increasing sugar loss in urine. [2]
Empagliflozin was approved for medical use in the United States and in the European Union in 2014. [11] [16] [17] It is on the World Health Organization's List of Essential Medicines. [18] In 2021, it was the 85th most commonly prescribed medication in the United States, with more than 8 million prescriptions. [19] [20] It has received approval as a generic medication from the US Food and Drug Administration (FDA). [21]
Empagliflozin is indicated in adults with heart failure (both reduced and preserved ejection fraction) to reduce the risk of hospitalisation for heart failure and to a lesser extent, cardiovascular death; in adults with type 2 diabetes and established cardiovascular disease to reduce the risk of cardiovascular death; and as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. [10] [13] [22]
In June 2023, the US Food and Drug Administration (FDA) expanded the indication, as an addition to diet and exercise, to improve blood sugar control in children 10 years and older with type 2 diabetes. [23]
Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood. Blocking SGLT-2 reduces blood glucose by blocking glucose reabsorption in the kidney and thereby excreting glucose (i.e., blood sugar) via the urine. [32] [33] [34] Of all the SGLT-2 Inhibitors currently available, empagliflozin has the highest degree of selectivity for SGLT-2 over SGLT-1, SGLT-4, SGLT-5 and SGLT-6. [35]
It was developed by Boehringer Ingelheim and is co-marketed by Eli Lilly and Company. It is also available as the combinations empagliflozin/linagliptin, empagliflozin/metformin, and empagliflozin/linagliptin/metformin.
For cardiovascular death, the FDA based its decision on a postmarketing study it required when it approved empagliflozin in 2014 as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. [16] [13] Empagliflozin was studied in a postmarket clinical trial of more than 7,000 participants with type 2 diabetes and cardiovascular disease. [13] In the trial, empagliflozin was shown to reduce the risk of cardiovascular death compared to a placebo when added to standard of care therapies for diabetes and atherosclerotic cardiovascular disease. [13]
For heart failure, the safety and effectiveness of empagliflozin were evaluated by the FDA as an adjunct to standard of care therapy in a randomized, double-blind, international trial comparing 2,997 participants who received empagliflozin, 10 mg, once daily to 2,991 participants who received the placebo. [22] The main efficacy measurement was the time to death from cardiovascular causes or need to be hospitalized for heart failure. [22] Of the individuals who received empagliflozin for an average of about two years, 14% died from cardiovascular causes or were hospitalized for heart failure, compared to 17% of the participants who received the placebo. [22] This benefit was mostly attributable to fewer participants being hospitalized for heart failure. [22]
The FDA granted the application for empagliflozin priority review and granted the approval of Jardiance to Boehringer Ingelheim. [22]
As of May 2013, Boehringer and Lilly had submitted applications for marketing approval to the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA). [36] The drug was approved in the European Union in May 2014, [11] and was approved in the United States in August 2014. [16] [17] [37] The FDA required four postmarketing studies: a cardiovascular outcomes trial, two studies in children, and a toxicity study in animals related to the pediatric trials. [16] [37]
A single study shows that half a tablet of empagliflozin 25 mg has similar glycemic efficacy as a full tablet. [38]
Empagliflozin causes moderate reductions in blood pressure and body weight. These effects are likely due to the excretion of glucose in the urine and a slight increase in urinary sodium excretion. [24] [39] In clinical trials, patients taking empagliflozin lost an average of 2% of their baseline body weight. [40] A higher percentage of people taking empagliflozin achieved weight loss greater than 5% from their baseline. [24] The medication reduced systolic blood pressure by 3 to 5 millimeters of mercury (mmHg). [24] The effects on blood pressure and body weight are generally viewed as favorable, as many patients with type 2 diabetes have high blood pressure or are overweight or obese. [31] [41]
Clinical data | |
---|---|
Trade names | Jardiance, others |
Other names | BI-10773 |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a614043 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth |
Drug class | Sodium-glucose cotransporter-2 (SGLT2) inhibitor [2] |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
ECHA InfoCard | 100.122.058 |
Chemical and physical data | |
Formula | C23H27ClO7 |
Molar mass | 450.91 g·mol−1 |
3D model ( JSmol) | |
| |
|
Empagliflozin, sold under the brand name Jardiance, among others, is an antidiabetic medication used to improve glucose control in people with type 2 diabetes. [10] [2] [12] It is not recommended for type 1 diabetes. [2] [13] It is taken by mouth. [2]
Common side effects include hyperventilation, anorexia, abdominal pain, nausea, vomiting, lethargy, mental status changes, hypotension, acute kidney injury, and vaginal yeast infections. [2] Rarer but more serious side effects include a skin infection of the groin called Fournier's gangrene and a form of diabetic ketoacidosis with normal blood sugar levels. [2] [14] Use during pregnancy or breastfeeding is not recommended. [15] Cautiously use empagliflozin with frequent monitoring of renal function in those with significant kidney disease, the use of empagliflozin for merely hyperglycaemia is not currently recommended given the risk of adverse events. The use of empagliflozin in patients with known cardiovascular disease may be beneficial, but risk and benefit ratio need to be considered and initiation of therapy should be individualised. It was also shown to help slow the progression of mild kidney problems.
Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), and works by increasing sugar loss in urine. [2]
Empagliflozin was approved for medical use in the United States and in the European Union in 2014. [11] [16] [17] It is on the World Health Organization's List of Essential Medicines. [18] In 2021, it was the 85th most commonly prescribed medication in the United States, with more than 8 million prescriptions. [19] [20] It has received approval as a generic medication from the US Food and Drug Administration (FDA). [21]
Empagliflozin is indicated in adults with heart failure (both reduced and preserved ejection fraction) to reduce the risk of hospitalisation for heart failure and to a lesser extent, cardiovascular death; in adults with type 2 diabetes and established cardiovascular disease to reduce the risk of cardiovascular death; and as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. [10] [13] [22]
In June 2023, the US Food and Drug Administration (FDA) expanded the indication, as an addition to diet and exercise, to improve blood sugar control in children 10 years and older with type 2 diabetes. [23]
Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood. Blocking SGLT-2 reduces blood glucose by blocking glucose reabsorption in the kidney and thereby excreting glucose (i.e., blood sugar) via the urine. [32] [33] [34] Of all the SGLT-2 Inhibitors currently available, empagliflozin has the highest degree of selectivity for SGLT-2 over SGLT-1, SGLT-4, SGLT-5 and SGLT-6. [35]
It was developed by Boehringer Ingelheim and is co-marketed by Eli Lilly and Company. It is also available as the combinations empagliflozin/linagliptin, empagliflozin/metformin, and empagliflozin/linagliptin/metformin.
For cardiovascular death, the FDA based its decision on a postmarketing study it required when it approved empagliflozin in 2014 as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. [16] [13] Empagliflozin was studied in a postmarket clinical trial of more than 7,000 participants with type 2 diabetes and cardiovascular disease. [13] In the trial, empagliflozin was shown to reduce the risk of cardiovascular death compared to a placebo when added to standard of care therapies for diabetes and atherosclerotic cardiovascular disease. [13]
For heart failure, the safety and effectiveness of empagliflozin were evaluated by the FDA as an adjunct to standard of care therapy in a randomized, double-blind, international trial comparing 2,997 participants who received empagliflozin, 10 mg, once daily to 2,991 participants who received the placebo. [22] The main efficacy measurement was the time to death from cardiovascular causes or need to be hospitalized for heart failure. [22] Of the individuals who received empagliflozin for an average of about two years, 14% died from cardiovascular causes or were hospitalized for heart failure, compared to 17% of the participants who received the placebo. [22] This benefit was mostly attributable to fewer participants being hospitalized for heart failure. [22]
The FDA granted the application for empagliflozin priority review and granted the approval of Jardiance to Boehringer Ingelheim. [22]
As of May 2013, Boehringer and Lilly had submitted applications for marketing approval to the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA). [36] The drug was approved in the European Union in May 2014, [11] and was approved in the United States in August 2014. [16] [17] [37] The FDA required four postmarketing studies: a cardiovascular outcomes trial, two studies in children, and a toxicity study in animals related to the pediatric trials. [16] [37]
A single study shows that half a tablet of empagliflozin 25 mg has similar glycemic efficacy as a full tablet. [38]
Empagliflozin causes moderate reductions in blood pressure and body weight. These effects are likely due to the excretion of glucose in the urine and a slight increase in urinary sodium excretion. [24] [39] In clinical trials, patients taking empagliflozin lost an average of 2% of their baseline body weight. [40] A higher percentage of people taking empagliflozin achieved weight loss greater than 5% from their baseline. [24] The medication reduced systolic blood pressure by 3 to 5 millimeters of mercury (mmHg). [24] The effects on blood pressure and body weight are generally viewed as favorable, as many patients with type 2 diabetes have high blood pressure or are overweight or obese. [31] [41]