BRENZAVVY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BRENZAVVY (BRENZAVVY).
Brenzavvy (bexagliflozin) is a sodium-glucose cotransporter 2 (SGLT2) inhibitor. It inhibits SGLT2 in the proximal renal tubule, reducing glucose reabsorption and increasing urinary glucose excretion, thereby lowering blood glucose levels. It also promotes osmotic diuresis and may improve cardiovascular and renal outcomes through hemodynamic and metabolic effects.
| Metabolism | Primarily metabolized via glucuronidation by UGT1A9 and UGT2B7 to inactive metabolites. Minor role of CYP-mediated metabolism. The drug is largely excreted unchanged in urine (up to 15%) and feces (about 30%). |
| Excretion | Approximately 65% of the dose is excreted renally as unchanged drug, and about 35% is eliminated via biliary/fecal routes as metabolites. |
| Half-life | The terminal elimination half-life is approximately 12-15 hours in patients with normal renal function, supporting once-daily dosing. |
| Protein binding | Plasma protein binding is about 90%, primarily to albumin. |
| Volume of Distribution | The volume of distribution is approximately 1.5 L/kg, indicating extensive distribution into tissues. |
| Bioavailability | Oral bioavailability is approximately 75%. |
| Onset of Action | Oral administration: onset of glucose-lowering effect occurs within 1-2 hours post-dose. |
| Duration of Action | Duration of action is approximately 24 hours, allowing once-daily dosing for sustained glycemic control. |
Recommended dose: 1 tablet (200 mg finerenone) orally once daily.
| Dosage form | TABLET |
| Renal impairment | eGFR 25-60 mL/min/1.73 m²: no dose adjustment. eGFR <25 mL/min/1.73 m²: not recommended. When initiating, if eGFR <60, monitor potassium and eGFR. If eGFR decreases to <25 during treatment, discontinue. |
| Liver impairment | Child-Pugh A: no dose adjustment. Child-Pugh B: not recommended. Child-Pugh C: contraindicated. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no approved dose. |
| Geriatric use | No specific dose adjustment required; monitor renal function and potassium more frequently due to age-related decline in renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BRENZAVVY (BRENZAVVY).
| Breastfeeding | No human data on bexagliflozin in breast milk. In animal studies, bexagliflozin was excreted in milk of lactating rats at concentrations similar to maternal plasma. M/P ratio not established in humans. Due to potential for serious adverse reactions in nursing infants (e.g., hypoglycemia, renal effects), breastfeeding is not recommended during therapy and for 2 weeks after last dose. |
| Teratogenic Risk | BRENZAVVY (bexagliflozin) is an SGLT2 inhibitor. In animal studies, bexagliflozin caused fetal toxicity (reduced fetal weights, increased skeletal malformations) at exposures ≥4 times the maximum recommended human dose (MRHD). There are no adequate human data in pregnancy. First trimester: Potential risk based on animal data. Second and third trimesters: Theoretical risk of impaired fetal renal development due to SGLT2 inhibition; may affect fetal glucose metabolism. Increased risk of neonatal hypoglycemia. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Severe renal impairment (eGFR < 30 mL/min/1.73 m²)","End-stage renal disease or on dialysis","Hypersensitivity to bexagliflozin or any excipients"]
| Precautions | ["Diabetic ketoacidosis (DKA): Atypical euglycemic DKA may occur; discontinue if suspected","Acute kidney injury: Monitor renal function; contraindicated in eGFR < 30 mL/min/1.73 m²","Hypotension: Risk in volume-depleted patients; assess and correct volume status before initiation","Lower limb amputation: Increased risk of toe and foot amputations; monitor for signs of infection or new pain","Necrotizing fasciitis of the perineum (Fournier gangrene): Rare but serious; discontinue and treat if suspected","Genital mycotic infections: Increased risk, especially in patients with history of infections","Urosepsis and pyelonephritis: Rare but serious; evaluate for urinary tract infections","Hypoglycemia: When used with insulin or sulfonylureas"] |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase BRENZAVVY levels. Avoid alcohol. No other specific food restrictions; maintain a balanced diet. Do not take with St. John's wort. |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, eGFR) throughout pregnancy due to risk of acute kidney injury. Monitor maternal blood glucose and HbA1c. Monitor fetal growth via ultrasound due to potential for altered fetal growth. Assess for neonatal hypoglycemia after delivery. |
| Fertility Effects | In animal studies, bexagliflozin did not affect male or female fertility at exposures up to 4 times the MRHD. Human data are lacking. Reversible endocrine changes (e.g., decreased testosterone) reported in some SGLT2 inhibitors, but clinical significance unknown. |
| Clinical Pearls | Monitor renal function and electrolytes before and during therapy. Contraindicated in patients with eGFR < 25 mL/min/1.73 m² or on dialysis. Avoid use with strong CYP3A4 inducers (e.g., rifampin). Dose adjustment required for moderate hepatic impairment (Child-Pugh B). Hypersensitivity reactions have been reported; discontinue if signs of angioedema occur. Assess for volume depletion before initiation; correct if present. Advise patients to avoid alcohol due to increased risk of acute kidney injury. |
| Patient Advice | Take BRENZAVVY exactly as prescribed; do not change dose or stop without consulting your doctor. · Avoid alcohol consumption while taking this medication. · Drink adequate fluids to prevent dehydration, but consult your doctor about fluid intake if you have heart or kidney problems. · Report any symptoms of allergic reaction (rash, hives, swelling) or kidney issues (decreased urine output, swelling in legs) immediately. · Do not take with strong CYP3A4 inducers (e.g., rifampin, St. John's wort); inform your doctor of all medications. · Frequent monitoring of kidney function and electrolytes will be required. |