维贝格龙(vibegron)详细说明书

Vibegron, developed by Japan's Sumitomo Pharmaceuticals, was approved by the FDA on December 23, 2024, becoming the world's first beta-3 adrenoceptor agonist approved for the treatment of overactive bladder combined with benign prostatic hyperplasia. By selectively activating β3 receptors, the bladder detrusor relaxes to increase urine storage capacity and improve related symptoms.

1. Indications

1. Overactive bladder in adults

Vibegron is suitable for the treatment of overactive bladder in adults with symptoms of urge urinary incontinence, urinary urgency and frequency.

2. Overactive bladder in adult men with benign prostatic hyperplasia

Vibegron is suitable for the treatment of overactive bladder in adult men receiving drug treatment for benign prostatic hyperplasia, accompanied by symptoms of urge urinary incontinence, urinary urgency and frequency.

2. Usage and Dosage

1. Recommended dose

Take 75 mg of Vibegroron orally once a day.

2. How to take it

Vibegron can be taken with a meal or alone. Swallow the whole tablet with a glass of water. For adult patients who have difficulty swallowing, crush Vibegroron tablets, mix with one tablespoon (approximately 15 mL) of applesauce, and take immediately with a glass of water.

Due to limited space, please refer to the original instructions of the drug for details. Please follow the guidance of your doctor for specific medication.

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3. Adverse reactions

Common adverse reactions (≥2%)

Common adverse reactions of Vibegroron include headache, urinary tract infection, nasopharyngitis, diarrhea, nausea, and upper respiratory tract infection.

Due to limited space, please refer to the original instructions of the drug for details. Please follow the guidance of your doctor for specific medication.

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IV. Specifications and properties

Tablets: 75mg, oval, light green, film-coated, with V75 embossing on one side and no embossing on the other side.

5. Precautions

1. Urinary retention

It is reported that patients taking Vibegroron will experience urinary retention. Patients with bladder outlet obstruction and those taking muscarinic antagonist medications to treat overactive bladder may be at increased risk for urinary retention. Monitor patients for signs and symptoms of urinary retention, particularly in patients with bladder outlet obstruction or those taking muscarinic antagonist medications for overactive bladder. Discontinue Vibegeron in patients who develop urinary retention

2. Angioedema

Angioedema of the face and/or throat has been reported with Vibegeron. Angioedema has been reported to occur hours after the first dose or after multiple doses. Angioedema is associated with swelling of the upper respiratory tract and can be life-threatening. If tongue, hypopharynx, or laryngeal involvement occurs, discontinue Vibegroron immediately and provide appropriate treatment and/or measures necessary to ensure a patent airway.

VI. Medication in Special Populations

1. Pregnancy

There are no available data on the use of Vibegroron in pregnant women to assess drug-related risks of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

2. Lactation

There are no data on the presence of Vibegroron in breast milk, the effects of this drug on breastfed infants, or the effects on milk production.

The developmental and health benefits of breastfeeding should be considered, as well as the mother's clinical need for vedebegron and any potential adverse effects of vertebegron or the underlying maternal condition on the breastfed infant.

3. Pediatric patients

The safety and effectiveness of Vibegroron in pediatric patients have not been determined.

4. Elderly patients

No overall differences were observed in the safety and effectiveness of Vibegroron in elderly patients aged 65 years and above (including patients aged 75 years and above) compared with younger adult patients.

5. Renal function impairment

For mild, moderate or severe renal insufficiency (eGFR15-<90mL/min/1.73m), it is not recommended to adjust the dose of Vibegroron). Vibegroron has not been studied in patients with eGFR <15mL/min/1.73m (with or without hemodialysis) and is not recommended for use in these patients.

6. Hepatic Impairment

For patients with mild to moderate hepatic impairment (Child-Pugh A and B), it is not recommended to adjust the dose of Vibegroron. Verbegaron has not been studied in patients with severe hepatic impairment (Child-PughC) and is not recommended for use in this patient population.

7. Drug Interactions

Concomitant use of Vibegaron will increase the maximum concentration and systemic exposure of digoxin. Serum digoxin concentrations should be monitored before and during treatment with GEMTESA and used to titrate the digoxin dose to obtain the desired clinical effect. Continue to monitor digoxin concentrations after discontinuation of vertebegron and adjust digoxin dosage as needed.

8. Overdose

Currently, there is no experience of unintentional overdose of Vibegroron. If overdose is suspected, treatment should be symptomatic and supportive.

9. Contraindications

It is prohibited to be used in patients who are allergic to any component of Vibegroron.

10. Validity period

24 months

11. Storage conditions

Vibegron should be stored at 20°C to 25°C, with an allowed deviation of 15°C to 30°C.

12. Pharmacokinetics

1. Distribution

The average apparent volume of distribution is 6304 liters. Vibegroron is approximately 50% human plasma protein bound. The average blood drug concentration to plasma concentration ratio is approximately 0.9.

2. Elimination

The effective half-life of Vibegroron in all populations is 30.8 hours.

3. Metabolism

Metabolism plays a minor role in the elimination of Vibegroron. CYP3A4 is the enzyme primarily responsible for in vitro metabolism.