Bexagliflozin

Bexagliflozin is an inhibitor of sodium-glucose co-transporter 2 (SGLT2), the transporter responsible for reabsorption of the majority of glucose from the renal glomerular filtrate in the renal proximal tubule. By inhibiting SGLT2, bexagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.

• Bexagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use Bexagliflozin is not recommended for use to improve glycemic control in patients with type 1 diabetes mellitus.ICD-10: E10.9, E11.9

• Bexagliflozin tablets are contraindicated in patients: With hypersensitivity to bexagliflozin or any excipient in bexagliflozin tablets. Anaphylaxis and angioedema have been reported with sodium-glucose co-transporter 2 (SGLT2) inhibitors.contraindicated

• Recommended dose: 20 mg once daily, taken in the morning, with or without food. Do not crush or chew the tablet. ( 2.2 ) • Assess renal function before initiating bexagliflozin tablets and as clinically indicated. Correct volume depletion before initiating ( 2.1 ) • Not recommended if eGFR less than 30 mL/min/1.73 m 2 . ( 2.1 ) • Withhold bexagliflozin tablets for at least 3 days, if possible, prior to major surgery or procedures associated with prolonged fasting ( 2.3 ). 2.1 Testing Prior to Initiation and During Treatment with Bexagliflozin Tablets • Assess renal function prior to initiation of bexagliflozin tablets and periodically thereafter as clinically indicated [see Warnings and Precautions ( 5.3 )] . Bexagliflozin is not recommended in patients with an eGFR less than 30 mL/min/1.73 m 2 • Assess volume status. In patients with volume depletion, correct this condition before initiating bexagliflozin tablets [see Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.5 , 8.6 )]. 2.2 Recommended Dosage • The recommended dosage of bexagliflozin tablets is 20 mg orally taken once daily in the morning, with or without food [see Clinical Pharmacology ( 12.3 )] . • Do not crush or chew the tablet. • If a dose is missed, take the missed dose as soon as possible. Do not double the next dose. 2.3 Temporary Interruption for Surgery • Withhold bexagliflozin tablets for at least 3 days, if possible, prior to major surgery or procedures associated with prolonged fasting.

Diabetic Ketoacidosis in Patients with Type 1 Diabetes Mellitus and Other Ketoacidosis: Consider ketone monitoring in patients at risk for ketoacidosis, as indicated. Assess for ketoacidosis regardless of presenting blood glucose levels and discontinue bexagliflozin tablets if ketoacidosis is suspected. Monitor patients for resolution of ketoacidosis before restarting. ( 5.1 ) Lower limb amputation: Consider factors that may increase the risk for amputations before initiating bexagliflozin tablets. Monitor patients for signs and symptoms of infection, or ulcers of the lower limbs, and discontinue if these occur ( 5.2 ) . Volume depletion: May result in acute kidney injury. Before initiating bexagliflozin tablets, assess and correct volume status in patients with impaired renal function or low systolic blood pressure, elderly patients or patients on diuretics. Monitor for signs and symptoms during therapy ( 5.3 ) Urosepsis and pyelonephritis: Evaluate patients for signs and symptoms of urinary tract infections and treat promptly, if indicated. ( 5.4 ) Hypoglycemia: Consider a lower dose of insulin or insulin secretagogue to reduce risk of hypoglycemia when used in combination with bexagliflozin tablets ( 5.5 ) Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene): Serious, life-threatening cases have occurred in both females and males treated with SGLT2 inhibitors. Assess patients presenting with pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise. If suspected, institute prompt treatment ( 5.6 ).

The following important adverse reactions are described below and elsewhere in the labeling: Diabetic Ketoacidosis in Patients with Type 1 Diabetes Mellitus and Other Ketoacidosis [see Warnings and Precautions ( 5.1 )] Lower Limb Amputation [see Warnings and Precautions ( 5.2 ) ] Volume Depletion [see Warnings and Precautions ( 5.3 )] Urosepsis and Pyelonephritis [see Warnings and Precautions ( 5.4 )] Hypoglycemia with Concomitant Use with Insulin and Insulin Secretagogues [see Warnings and Precautions ( 5.5 )] Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene) [see Warnings and Precautions ( 5.6 )] Genital Mycotic Infections [see Warnings and Precautions ( 5.7 )] Most common adverse reactions (incidence > 5%) are female genital mycotic infections, urinary tract infection and increased urination ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact the bexagliflozin information line at 1-855-273-6928 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Pregnancy: Advise females of the potential risk to a fetus especially during the second and third trimesters. Bexagliflozin tablets are not recommended during the second and third trimesters of pregnancy ( 8.1 ) Lactation: Not recommended when breastfeeding. ( 8.2 ) Geriatric patients: Higher incidence of adverse reactions related to volume depletion. ( 5.3 , 8.5 ) Renal Impairment: Higher incidence of adverse reactions related to reduced renal function ( 5.3 , 8.6 ) Hepatic Impairment: Not recommended for patients with severe hepatic impairment ( 8.7 ) 8.1 Pregnancy Risk Summary Based on animal data showing adverse renal effects, bexagliflozin is not recommended during the second and third trimesters of pregnancy. The available data on use of bexagliflozin tablets during pregnancy are insufficient to determine a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations ) . In animal studies, adverse renal pelvic and tubule dilatations that were not fully reversible were observed in rats when bexagliflozin was administered during a period of renal development corresponding to the late second and third trimesters of human pregnancy at exposures 11 times the 20 mg clinical dose (see Data ) .

Metabolism

The pharmacokinetics of bexagliflozin are similar in healthy subjects and adults with type 2 diabetes mellitus. Following dosing in the fasted state, mean C max and AUC 0-∞ were 134 ng/mL and 1,162 ng·h/mL, respectively.

In the event of an overdose of bexagliflozin tablets, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Employ the usual supportive measures as dictated by the patient’s clinical status. Removal of bexagliflozin by hemodialysis has not been studied.

• Jan 20, 2023NDANDA214373Theracosbio

1. 1Weight Decreased728%
2. 2Headache624%
3. 3Nausea624%
4. 4Cough520%
5. 5Decreased Appetite520%
6. 6Chest Discomfort416%
7. 7Dyspnoea416%
8. 8Fatigue416%
9. 9Gastrointestinal Disorder416%
10. 10Oropharyngeal Pain416%
11. 11Throat Irritation416%
12. 12Throat Tightness416%
13. 13Abdominal Pain Upper312%
14. 14Asthenia312%
15. 15Blood Glucose Increased312%

The 10 most recently updated of 20 ClinicalTrials.gov registrations naming Bexagliflozin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
  Not yet recruiting · Phase 4 · Interventional · 64 enrolled · Baylor Research Institute
  NCT07547878updated 2026-05-08
• Beta Cell Function in Type 2 Diabetes: Differential Effects of SGLT2 Inhibitors and GLIP-Receptor Agonists
  Active not recruiting · Phase 4 · Interventional · 60 enrolled · MaryAnn Banerji
  NCT07325435updated 2026-01-08
• Using Secondary Data to Evaluate Sex-based Heterogeneity of GLP-1 Agonists and SGLT2 Inhibitors on Cardiovascular-Kidney-Metabolic Health (CKMH) Outcomes in Real-world Settings (DASH-CKMH)
  Active not recruiting · Observational · 23,280,000 enrolled · Ohio State University
  NCT07188545updated 2025-09-23
• Adipose Dysfunction, Imaging, Physiology, and Outcomes With Sodium Glucose Cotransporter 2 Inhibitor (SGLT2i) for Sleep Apnea: The ADIPOSA Study
  Recruiting · Phase 4 · Interventional · 164 enrolled · Yale University
  NCT05612594updated 2025-09-11
• An Integrated Assessment of the Safety and Effectiveness of Bexagliflozin for the Management of Essential Hypertension
  Completed · Phase 2 · Phase 3 · Interventional · 673 enrolled · Theracos
  NCT03514641updated 2021-09-21
• Bexagliflozin Drug/Drug Interaction Study With Digoxin
  Completed · Phase 1 · Interventional · 20 enrolled · Theracos
  NCT03197324updated 2021-07-23
• Interaction of Bexagliflozin With Metformin, Glimepiride and Sitagliptin
  Completed · Phase 1 · Interventional · 54 enrolled · Theracos
  NCT02956044updated 2021-07-22
• Bexagliflozin Efficacy and Safety Trial
  Completed · Phase 3 · Interventional · 1,700 enrolled · Theracos
  NCT02558296updated 2021-07-14
• Safety and Efficacy of Bexagliflozin Compared to Placebo as Add-on Therapy to Metformin in Type 2 Diabetes Subjects
  Completed · Phase 3 · Interventional · 351 enrolled · Theracos
  NCT03259789updated 2021-07-07
• Study to Evaluate Effects of Probenecid, Rifampin and Verapamil on Bexagliflozin in Healthy Subjects
  Completed · Phase 1 · Interventional · 48 enrolled · Theracos
  NCT03296800updated 2021-07-01

Frequently asked questions

How does Bexagliflozin work?

Bexagliflozin is an inhibitor of sodium-glucose co-transporter 2 (SGLT2), the transporter responsible for reabsorption of the majority of glucose from the renal glomerular filtrate in the renal proximal tubule. By inhibiting SGLT2, bexagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.

What is Bexagliflozin used for?

According to FDA labeling, Bexagliflozin carries indications including: Bexagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use Bexagliflozin is not recommended for use to improve glycemic control in patients with type 1 diabetes mellitus.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bexagliflozin?

Bexagliflozin is classified as Sodium-glucose co-transporter 2 (SGLT2) inhibitors, Sodium-Glucose Cotransporter 2 Inhibitor, Sodium-Glucose Transporter 2 Inhibitors.

What are the brand names for Bexagliflozin?

Bexagliflozin is marketed under brand names including Bexacat, Brenzavvy.

What are the contraindications for Bexagliflozin?

Bexagliflozin labeling lists contraindications including: Bexagliflozin tablets are contraindicated in patients: With hypersensitivity to bexagliflozin or any excipient in bexagliflozin tablets. Anaphylaxis and angioedema have been reported with sodium-glucose co-transporter 2 (SGLT2) inhibitors.. Always consult the full prescribing information and a clinician.