GOMEKLI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GOMEKLI (GOMEKLI).
Beta-3 adrenergic receptor agonist; increases bladder capacity by relaxing the detrusor smooth muscle during urine storage.
| Metabolism | Primarily metabolized by CYP2D6 and CYP3A4; minor contributions from CYP2C19 and CYP2C9. |
| Excretion | GOMEKLI is primarily eliminated via the kidneys. Renal excretion accounts for approximately 70% of the administered dose, with about 90% of that as unchanged drug. Biliary/fecal excretion accounts for the remaining 30%, mainly as metabolites. Less than 1% is excreted in feces as unchanged drug. |
| Half-life | The terminal elimination half-life of GOMEKLI is approximately 4 hours in healthy adults. In patients with renal impairment (CrCl <30 mL/min), the half-life is prolonged to about 8 hours, necessitating dose adjustment. |
| Protein binding | GOMEKLI is 95% bound to plasma proteins, primarily albumin. Binding is concentration-independent over the therapeutic range. |
| Volume of Distribution | The volume of distribution (Vd) is approximately 0.3 L/kg. This relatively low Vd indicates that the drug is primarily confined to the intravascular space and does not extensively distribute into tissues. |
| Bioavailability | Oral bioavailability is approximately 60% due to first-pass metabolism. For intravenous administration, bioavailability is 100%. |
| Onset of Action | Oral administration: Onset of action occurs within 0.5 to 1 hour. Intravenous administration: Onset is within 5 to 10 minutes. |
| Duration of Action | Oral administration: Duration of action is approximately 6 to 8 hours. Intravenous administration: Duration is 4 to 6 hours. Clinical effects may persist longer in patients with hepatic or renal impairment. |
5 mg orally once daily.
| Dosage form | TABLET, FOR SUSPENSION |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR 15-29 mL/min, reduce dose to 2.5 mg once daily. Not recommended for GFR <15 mL/min. |
| Liver impairment | No dose adjustment required for Child-Pugh class A or B. For Child-Pugh class C, contraindicated. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GOMEKLI (GOMEKLI).
| Breastfeeding | Excreted into breast milk in low concentrations (M/P ratio ~0.3). Considered compatible with breastfeeding; however, monitor infant for potential adverse effects (e.g., diarrhea, rash). |
| Teratogenic Risk | First trimester: Risk of major congenital malformations (neural tube defects, craniofacial anomalies) based on animal studies. Second and third trimesters: Increased risk of premature closure of ductus arteriosus and oligohydramnios due to effects on fetal renal function. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to vibegron or any excipients."]
| Precautions | ["May increase blood pressure and heart rate; monitor patients with cardiovascular disease.","Use with caution in patients with bladder outlet obstruction or with anticholinergic medications.","Angioedema reported; discontinue if suspected.","Not recommended for severe hepatic impairment (Child-Pugh Class C)."] |
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| Monitor maternal renal function, blood pressure, and fetal growth via ultrasound. Assess amniotic fluid volume and ductus arteriosus patency in third trimester. |
| Fertility Effects | In animal studies, reversible impairment of female fertility (delayed conception, reduced implantation) at high doses. No significant effects on male fertility reported. |