On January 23, 2023, BRENZAVVY (bexagliflozin tablet) won a nod from the FDA to help improve glycemic control in adults with Type 2 diabetes. BRENZAVVY, which comes in 20-mg tablets, is taken once a day alongside diet and exercise. BRENZAVVY shouldn’t be used in Type 2 diabetes patients with end-stage renal disease on dialysis, TheracosBio stressed, (1)
Appl. No. N214373
Proprietary Name: BRENZAVVY
Active Ingredients: BEXAGLIFLOZIN
Applicant Holder: THERACOSBIO LLC
INDICATION
BRENZAVVY tablets for oral use contain bexagliflozin, an SGLT2 inhibitor.
BRENZAVVY is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
DOSAGE AND ADMININSTATION
The recommended dosage of BRENZAVVY is 20 mg orally taken once daily in the morning, with or without food.
DOSAGE FORM AND STRENGTHS
Tablets: 20 mg, blue, caplet shaped.
Each film-coated tablet contains 20 mg of bexagliflozin and the inactive ingredients colloidal silicon dioxide, glyceryl dibehenate, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene oxide, and poloxamer 188. It also has an Opadry film.
API PROPERTIES
Bexagliflozin is a white/off-white to pale yellow powder. It is very slightly soluble in water and freely soluble in methanol, acetone, ethylene glycol, and propylene glycol. Crystalline bexagliflozin is not hygroscopic.
PK
Tmax: 2 - 4 h.
Dose-proportional manner: 3 mg to 90 mg.
half-life: 12 h.
Food Effect: Cmax increased by 31%, AUC 10%, Tmax to 5 h.
However, the effects of food on bexagliflozin pharmacokinetics are not considered clinically relevant.
Bexagliflozin is mainly metabolized by UGT1A9 and, to a lesser extent, CYP3A. In plasma the most abundant metabolite is the pharmacologically inactive 3′-O-glucuronide.
Following administration of an oral [14C]-bexagliflozin solution to healthy subjects, 91.6% of input radioactivity was recovered, 51.1% in feces, the majority as bexagliflozin, and 40.5% in urine, largely as the 3′-O-glucuronide. The proportion of input radioactivity recovered as bexagliflozin in urine and feces was 1.5% and 28.7%, respectively.
GENERIC COMPETITION
01/19/2024:
IP
ORANGE BOOK PATENTS
Patent Data
AN INTERESTING PATENTS/APPLICATION
US20220117898A1 (Theracosbio LLC; filed on 2021-10-05 in US; pending as of 01/19/2024) claims: An extended-release tablet comprising bexagliflozin.
US Novel Drug Approvals for 2023
REFERENCE
Orange book
US patent office
Fraiser Kansteiner, With TheracosBio green light, another SGLT2 inhibitor wades into diabetes arena, Fierce Pharma, Jan 23, 2023.
