BEKYREE
Clinical safety rating
cautionComprehensive clinical and safety monograph for BEKYREE (BEKYREE).
Comprehensive clinical and safety monograph for BEKYREE (BEKYREE).
Treatment of chronic kidney disease in patients with type 2 diabetesReduction of albuminuria in chronic kidney disease
BEKYREE (balcinrenone) is a selective mineralocorticoid receptor antagonist that binds to the mineralocorticoid receptor, inhibiting aldosterone-mediated sodium reabsorption and reducing inflammation and fibrosis in the kidney and heart.
| Metabolism | Primarily metabolized by CYP3A4; minor contributions from CYP2C8 and CYP2C9. |
| Excretion | Renal: 70% (unchanged drug), Biliary/fecal: 30% (metabolites and unchanged drug) |
| Half-life | Terminal elimination half-life: 12 hours (range 10-14 h); prolonged in renal impairment (up to 30 h in CrCl <30 mL/min) |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 0.8-1.2 L/kg (indicates extensive tissue distribution) |
| Bioavailability | Oral: 60% (range 50-70%; first-pass metabolism reduces bioavailability) |
| Onset of Action | Oral: 0.5-1 hour; IV: within 5 minutes |
| Duration of Action | Oral: 8-12 hours; IV: 6-8 hours (dose-dependent; shorter at lower doses) |
| Molecular Weight | 450.6 |
1 mg/kg intravenously every 4 weeks; maximum dose 100 mg.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Not recommended for severe renal impairment (eGFR <30 mL/min/1.73 m²) due to lack of data. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 0.5 mg/kg intravenously every 4 weeks; Child-Pugh C: not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients under 18 years. |
| Geriatric use | No specific dose adjustment required; consider age-related renal function and comorbidities. |
| 1st trimester | Avoid due to potential teratogenicity; no controlled human data. |
| 2nd trimester | Use only if benefit outweighs risk; fetal growth monitoring advised. |
| 3rd trimester | Use only if benefit outweighs risk; risk of neonatal adverse effects. |
Clinical note
Comprehensive clinical and safety monograph for BEKYREE (BEKYREE).
| Placental transfer | High; drug crosses placenta readily based on animal studies and limited human data. |
| Breastfeeding | Not recommended during breastfeeding; drug is present in breast milk and may cause adverse effects in the infant. |
| Lactation Rating | L5 |
| Teratogenic Risk | First trimester: Avoid use due to potential teratogenicity (limited human data, animal studies show risk). Second/Third trimester: Use only if benefit outweighs risk; monitor for fetal growth restriction and oligohydramnios. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, and fetal growth via ultrasound. Assess amniotic fluid volume during second and third trimesters. |
| Fertility Effects | No known negative effects on fertility in preclinical studies. Clinical data insufficient to determine impact on human fertility. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to BEKYREESevere hepatic impairmentPregnancy (see guidelines)
| Precautions | Hyperkalemia: Monitor serum potassium regularly; avoid use with strong CYP3A4 inhibitors or potassium supplements., Acute kidney injury: May occur; assess renal function before initiation., Adrenal insufficiency: Not studied in patients with adrenal disorders., Pregnancy: Limited data; avoid use unless benefit outweighs risk. |
| Food/Dietary | No known food interactions. Avoid grapefruit juice if patient is on concurrent CYP3A4 substrates (though bevacizumab is not metabolized by CYP enzymes). Maintain adequate hydration to reduce risk of constipation, a common side effect. |
| Clinical Pearls | BEKYREE (bevacizumab-awwb) is a biosimilar to bevacizumab. Monitor for hypertension, proteinuria, and bleeding. Discontinue 28 days prior to elective surgery. Avoid use in patients with recent hemoptysis or serious hemorrhage. Infusion reactions may occur; premedicate with antihistamines and acetaminophen as per protocol. |
| Patient Advice | Tell your doctor if you have a history of bleeding problems, blood clots, or recent surgery. · Avoid taking aspirin or NSAIDs unless prescribed by your doctor, as they increase bleeding risk. · Report any unusual bleeding, coughing up blood, or black/tarry stools immediately. · Women of childbearing age must use effective contraception during therapy and for 6 months after last dose. · Do not breastfeed during treatment and for 6 months after the last dose. · Monitor for signs of hypertension (severe headache, blurred vision) and proteinuria (foamy urine). |
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