Bexagliflozin (Brenzavvy): Advancing Diabetes Management With SGLT-2 Inhibition


Beyond its primary role in diabetes treatment, SGLT-2 inhibitors have demonstrated versatility in various health aspects, offering benefits beyond glucose reduction.

Bexagliflozin (Brenzavvy), an oral sodium-glucose co-transporter 2 (SGLT2) inhibitor, has gained recognition for enhancing glycemic control in adults with type 2 diabetes mellitus. Developed by TheracosBio, this SGLT-2 inhibitor received FDA approval in January 2023, following comprehensive evaluation in 23 clinical trials involving more than 5000 adult participants.

Image Credit: Minerva Studio -

Image Credit: Minerva Studio -

Beyond its primary role in diabetes treatment, SGLT-2 inhibitors have demonstrated versatility in various health aspects, offering benefits beyond glucose reduction. This drug class has exhibited unique kidney protective actions, improved cardiovascular (CV) outcomes, and other physical benefits.1


When combined with proper diet and exercise, bexagliflozin can improve glycemic control in adults with type 2 diabetes mellitus. It can be used alone or in combination with other diabetes medications. It is essential to note that bexagliflozin is not indicated for patients with type 1 diabetes because it may elevate the risk of diabetic ketoacidosis (DKA) in these patients.2

Mechanism of Action

Bexagliflozin is a highly selective inhibitor of SGLT2. This transporter is responsible for reabsorption of the majority of glucose from the renal glomerular filtrate in the renal proximal tubule. Through inhibition of SGLT2, less glucose is reabsorbed, thus lowering the renal threshold for glucose and increasing its excretion in the urine.2 This process of eliminating excess glucose through the urine aids in diabetic management by effectively lowering blood sugar levels.

Dosing and Administration

Bexagliflozin is a tablet taken orally. The recommended dosage is 20 mg orally taken once daily in the morning, with or without food.2

Clinical Studies

Bexagliflozin Efficacy and Safety Trial (BEST) was a phase 3, randomized, double-blind, placebo controlled study that investigated the impact of bexagliflozin on reduced HbA1c levels in patients with type 2 diabetes mellitus and increased risk of cardiovascular adverse events (AEs). Treatment with bexagliflozin provided a statistically significant reduction in HbA1c in patients at high risk of cardiovascular (CV) events, and positive effects on systolic blood pressure and weight. Additionally, noninferiority was demonstrated for the composite outcome of cardiovascular death, myocardial infarction, stroke, or unstable angina.3

Safety and Efficacy in T2DM Patients with Moderate Renal Impairment was a phase 3, multi-center, randomized, double-blind, placebo-controlled, parallel-group study that evaluated the efficacy and safety of once-daily oral administration of bexagliflozin to placebo in patients with type 2 diabetes mellitus, moderate renal impairment (eGFR between 30 and 59 mL/min/1.73m2), and inadequate glycemic control (HbA1c between 7.0% and 10.5%). Treatment with bexagliflozin provided a statistically significant reduction (0.37%) in HbA1c compared to placebo.4


Bexagliflozin is contraindicated in patients with hypersensitivity to bexagliflozin or any excipient and patients on dialysis or those with end-stage renal disease with an estimated glomerular filtration rate of <30 mL/min/1.73m2.2

Drug Interaction Studies

Bexagliflozin may interact with other medicines, such as UGT enzyme inducers, insulin and/or insulin secretagogues, and lithium.2

Use in Special Populations

Pregnancy: Based on animal data, bexagliflozin is not recommended during the second and third trimesters of pregnancy.2

Lactation: Use is not recommended while breastfeeding due to the potential for serious AEs in a breastfed infant, including the potential for bexagliflozin to affect postnatal renal development.2

Pediatrics: Safety and efficacy have not been established in pediatric patients.2

Geriatrics: Higher incidence related to volume depletion.2

Renal Impairment: Contraindicated in patients receiving dialysis and is not recommended in patients with an eGFR <30 mL/min/1.73m2 due to the decline of the glucose lowering effect and reduction in urine output in these patients.2

Hepatic Impairment: Not recommended for patients with severe hepatic impairment.2


Common AEs of SGLT-2 inhibitors include female genital mycotic infections, urinary tract infection, and increased urination. Bexagliflozin may be associated with an increased risk of ketoacidosis, lower limb amputations, volume depletion, urosepsis, pyelonephritis, and hypoglycemia when used with insulin and/or insulin secretagogues, and necrotizing fasciitis of the perineum in patients with type 2 diabetes.2

Storage and Handling

Bexagliflozin should be stored at room temperature between 68°F to 77°F (20°C to 25°C). Excursions permitted to 59°F to 86°F (15°C to 30°C).2


1. Munteanu MA, Swarnkar S, Popescu RI, et al. SGLT2 Inhibitor: an Emerging Pillar in Heart Failure Therapeutics?. Maedica (Bucur). 2023;18(1):102-110. doi:10.26574/maedica.2023.18.1.102

2. Package insert. TheracosBio; 2023. Accessed July 13, 2023.

3. McMurray JJV, Freeman MW, Massaro J, Solomon S, Lock P, Riddle MC, Lewis E, Halvorsen YDC. The Bexagliflozin Efficacy and Safety Trial (BEST): A Randomized, Double-Blind, Placebo-Controlled, Phase III Clinical Trial. Diabetes. June 1, 2020;69(Supplement_1):32-OR. Doi: 10.2337/db20-32-OR

4. Allegretti AS, Zhang W, Zhou W, et al. Safety and Effectiveness of Bexagliflozin in Patients With Type 2 Diabetes Mellitus and Stage 3a/3b CKD. Am J Kidney Dis. 2019;74(3):328-337. doi:10.1053/j.ajkd.2019.03.417

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