Gemtesa (vibegron)

No dosing information is available for this tab.

Vibegron is administered orally once daily as a film-coated tablet without regard to meals.

Swallow tablets whole with a glass of water. Alternatively, tablets may be crushed, mixed with approximately 15 mL of applesauce, and taken immediately with a glass of water.

Store tablets at 20-25degreesC (excursions permitted between 15-30degreesC).

No dosing information is available for this tab.

Vibegron is a cytochrome P450 (CYP) 3A4 substrate. Vibegron does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4. Vibegron does not induce CYP1A2, CYP2B6, or CYP3A4.

Vibegron is a P-glycoprotein (P-gp) substrate. Vibegron does not inhibit P-gp, breast cancer resistance protein (BCRP), organic anion transporting polypeptide (OATP) 1B1, OATP1B3, organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 1, OCT2, multidrug and toxin extrusion protein (MATE) 1, or MATE2K.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

Moderate Interaction: Assess the risk to the patient and take action as needed.

P-Glycoprotein (P-Gp) Inhibitors/Digoxin

SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.

MECHANISM OF ACTION: P-glycoprotein (P-gp) inhibitors may inhibit cellular efflux of digoxin at the levels of intestinal absorption, renal tubular secretion, and biliary-intestinal secretion.(1)

CLINICAL EFFECTS: Concurrent administration of a P-gp inhibitor may result in elevated levels and toxicities of digoxin.(1) Symptoms of digoxin toxicity can include anorexia, nausea, vomiting, headache, fatigue, malaise, drowsiness, generalized muscle weakness, disorientation, hallucinations, visual disturbances, and arrhythmias.

PREDISPOSING FACTORS: Low body weight, advanced age, impaired renal function, hypokalemia, hypercalcemia, and/or hypomagnesemia may increase the risk of digoxin toxicity.

PATIENT MANAGEMENT: Monitor digoxin concentrations before initiating concomitant use with P-gp inhibitors and continue monitoring serum digoxin concentrations as recommended in the prescribing information for digoxin.(1) When digoxin levels are expected to be increased by over 50%, the manufacturer of digoxin recommends decreasing the dose of digoxin by approximately 30-50% or by modifying the dosing frequency to reduce digoxin concentrations.(1) When digoxin levels are expected to be increased by less than 50%, the manufacturer of digoxin recommends decreasing the dose of digoxin by approximately 15-30% or by modifying the dosing frequency to reduce digoxin concentrations.(1) For patients on daraxonrasib, the manufacturer of daraxonrasib states that it should be taken at least 4 hours apart from P-gp substrates.(2)

DISCUSSION: Digoxin is a known substrate of P-gp. Inhibitors of P-gp may increase toxicity of digoxin.(1) In a clinical study, elacestrant increased the area-under-curve (AUC) and maximum concentration (Cmax) of digoxin by 1.1-fold and 1.3-fold, respectively.(3,4) In another clinical study, imlunestrant increased the area-under-curve (AUC) and maximum concentration (Cmax) of digoxin by 1.4-fold and 1.6-fold, respectively.(5) In another clinical study, maribavir increased the AUC and Cmax of digoxin by 1.2-fold and 1.25-fold, respectively.(6) Inhibitors of P-gp linked to this monograph include: abrocitinib, aumolertinib, capmatinib, daraxonrasib, elacestrant, enzalutamide, imlunestrant, maribavir, selpercatinib, sparsentan, sotorasib, vepdegestrant, and vibegron.(2-8)

*Known hypersensitivity to vibegron or to any ingredient in the formulation.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

• Bladder outflow obstruction

Adverse effects that occurred in >=2% of patients receiving vibegron include headache, urinary tract infection, nasopharyngitis, diarrhea, nausea, and upper respiratory tract infection.

Rare or Very Rare

• Angioedema

More Frequent

• Diarrhea
• Headache disorder
• Hypertension
• Nausea
• Pharyngitis
• Upper respiratory infection
• Urinary tract infection

Less Frequent

• Bronchitis
• Constipation
• Drug-induced hot flash
• Xerostomia

Rare or Very Rare

• Eczema
• Hypersensitivity drug reaction
• Pruritus of skin
• Residual urine volume increased
• Skin rash
• Urinary retention
• Urticaria

No enhanced messaging available.

The safety and efficacy of vibegron in pediatric patients have not been established.

There are no available data on vibegron use in pregnant females to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In rat and rabbit studies, no effects on embryofetal development were observed following administration of vibegron during organogenesis at exposures approximately 275- and 285-fold greater than clinical exposure at the recommended daily dose of vibegron. Maternal toxicity and delayed fetal skeletal ossification were observed in rabbits at approximately 898-fold clinical exposure. In pregnant and lactating rats treated with vibegron, no effects on offspring were observed at 89-fold clinical exposure; however, at 458-fold clinical exposure, maternal and developmental toxicity were observed.

There are no data on the presence of vibegron in human milk, the effects of vibegron on the breast-fed infant, or the effects of vibegron on milk production. When a single oral dose of radiolabeled vibegron was administered to postnatal nursing rats, radioactivity was observed in milk. When a drug is present in animal milk, it is likely that the drug will be present in human milk.

Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for vibegron and any potential adverse effects on the breast-fed infant from vibegron or from the underlying maternal condition.

The manufacturer makes no specific dosage recommendations for geriatric patients.

Of 526 patients who received vibegron in the clinical studies for OAB, 242 (46%) were >=65 years of age, and 75 (14%) were >=75 years of age. No overall differences in safety or effectiveness of vibegron have been observed between patients >=65 years of age and younger adult patients.