Overview

Bexagliflozin is a highly specific and potent sodium-glucose co-transporter 2 (SGLT2) inhibitor. Similar to other SGLT2 inhibitors, bexagliflozin contains three basic moieties: glucose, two benzene rings and a methylene bridge. SGLT2 is responsible for 60% to 90% of renal glucose re-uptake, and unlike other isoforms such as SGLT1, SGLT2 is mainly expressed in the kidney. By inhibiting SGLT2, bexagliflozin reduces renal reabsorption of filtered glucose and increases urinary glucose excretion, which reduces blood glucose levels independently of insulin sensitivity. In January 2023, bexagliflozin was approved by the FDA for the treatment of adults with type 2 diabetes. Its use is not recommended in patients with type 1 diabetes since it may increase their risk of diabetic ketoacidosis.

Indication

Bexagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Associated Conditions

Type 2 Diabetes Mellitus

Research Report

Published: Aug 28, 2025

Bexagliflozin (Brenzavvy™): A Comprehensive Monograph on a Novel SGLT2 Inhibitor for Glycemic Control

Executive Summary & Drug Classification

Introduction to Bexagliflozin

Bexagliflozin is an orally administered, potent, and highly selective small molecule inhibitor of the sodium-glucose cotransporter 2 (SGLT2).[1] Developed by TheracosBio, LLC, and marketed under the brand name Brenzavvy™, it represents a significant addition to the therapeutic armamentarium for the management of type 2 diabetes mellitus (T2DM).[3] On January 20, 2023, bexagliflozin received approval from the U.S. Food and Drug Administration (FDA), becoming the fifth orally administered SGLT2 inhibitor to enter the U.S. market for this indication, following the precedent set by dapagliflozin, canagliflozin, empagliflozin, and ertugliflozin.[4] Its approval was supported by a comprehensive clinical development program involving 23 trials and over 5,000 adult participants, which established its efficacy in improving glycemic control as an adjunct to diet and exercise.[6]

Continue reading the full research report

Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
Adipose Dysfunction, Imaging, Physiology, and Outcomes With Sodium Glucose Cotransporter 2 Inhibitor (SGLT2i) for Sleep Apnea: The ADIPOSA Study	2022/11/10	NCT05612594	Phase 4	Recruiting	Yale University
Safety and Efficacy of Bexagliflozin in Subjects With Moderate Hepatic Impairment	2018/06/15	NCT03557658	Phase 1	Completed	Theracos
An Integrated Assessment of the Safety and Effectiveness of Bexagliflozin for the Management of Essential Hypertension	2018/05/02	NCT03514641	Phase 2	Completed	Theracos
Absolute Bioavailability Study With Bexagliflozin	2018/01/31	NCT03417076	Phase 1	Withdrawn	Theracos
Study to Evaluate Effects of Probenecid, Rifampin and Verapamil on Bexagliflozin in Healthy Subjects	2017/09/28	NCT03296800	Phase 1	Completed	Theracos
Safety and Efficacy of Bexagliflozin Compared to Placebo as Add-on Therapy to Metformin in Type 2 Diabetes Subjects	2017/08/24	NCT03259789	Phase 3	Completed	Theracos
Bexagliflozin Drug/Drug Interaction Study With Digoxin	2017/06/23	NCT03197324	Phase 1	Completed	Theracos
Bexagliflozin Drug/Drug Interaction Study With Exenatide Injection	2017/05/30	NCT03167411	Phase 1	Completed	Theracos
Safety and Efficacy of Bexagliflozin Compared to Sitagliptin as Add-on Therapy to Metformin in Type 2 Diabetes Subjects	2017/04/14	NCT03115112	Phase 3	Completed	Theracos
Interaction of Bexagliflozin With Metformin, Glimepiride and Sitagliptin	2016/11/04	NCT02956044	Phase 1	Completed	Theracos

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
Bexagliflozin	TheracosBio, LLC	82381-2000	ORAL	20 mg in 1 1	3/21/2024
BRENZAVVY	TheracosBio, LLC	82381-2174	ORAL	20 mg in 1 1	2/8/2024
Bexagliflozin	Golden State Medical Supply, Inc.	51407-918	ORAL	20 mg in 1 1	4/15/2025

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
No TGA approvals found for this drug.

Health Canada Drug Approvals

Approved Product	Company	DIN	Dosage Form	Strength	Market Date
No Health Canada approvals found for this drug.

CIMA AEMPS Drug Approvals

Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product	Company	Registration Number	Dosage Form	Strength	Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

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