What to Know About Gemtesa (Vibegron)

As a treatment for overactive bladder (OAB), Gemtesa (vibegron) was approved by the Food and Drug Administration (FDA) for commercial launch in the American market in April 2021. This once-daily prescription tablet acts on beta-3 receptors (also called beta-3 adrenoceptors) of the bladder to control smooth muscle function.

As such, it’s a first-line treatment for the excessive need to urinate and urinary incontinence—the inability to control bladder function—associated with OAB.    

Uses

Gemtesa is indicated to treat OAB in adults. It is a new drug and has not yet been approved for off-label use. To be diagnosed with OAB, you must have at least two of the following symptoms:

• You have to urinate eight or more times a day and/or two–three times at night.
• Your need to urinate is urgent, strong, and sudden.
• You leak urine after feeling a strong urge to urine.
• You experience incontinence, in which you can’t control your bladder.

Before Taking

Before Gemtesa can be prescribed, your healthcare provider will need to ensure you have OAB. Notably, this involves ruling out other disorders or diseases of the bladder. Typically, diagnosis involves the following:

• Assessment of medical history is the first step in diagnosis. A practitioner will also discuss your symptoms and assess the frequency and severity of your urge to urinate. You will be asked about medications you’re taking as well as other factors, such as diet.
• Physical examination of the rectum, abdomen, and organs and structures around the pelvis will follow. Your primary care provider may perform the exam or you may be referred to a specialist called a urologist.
• Keeping a bladder diary is another step that you may need to take. This involves a couple of weeks of tracking such things as the amount of liquid you drink and when, the frequency of urination, the amount of urine leakage you experience, and how often you have the sudden, uncontrollable urge to urinate.
• Urine testing may be necessary, especially to rule out other issues, such as bladder cancer, infection, or the presence of blood. This involves leaving a sample with the practitioner for laboratory testing.
• Imaging of the bladder (usually an ultrasound) may be necessary to determine the severity of your OAB and to assess how much urine is left after you urinate.
• Cystoscopy may be requested to aid in diagnosis. This involves examining the interior of the bladder and the urethra (the tube that carries urine out of the body) using a specialized, adjustable tube with an eyepiece and a lens on the end.
• Ureteroscopy is a procedure using a ureteroscope, which is a flexible, adjustable telescope used for assessing the kidneys and ureters (the ducts connecting the kidneys to the bladder). 

Precautions and Contraindications

As with any drug, Gemtesa may be dangerous to take under certain conditions. These include:

• Allergy: Some people may be allergic to this drug. Adverse reactions cause urine retention, skin rashes, eczema, and rashes, among other symptoms.
• Severe renal impairment: Gemtesa may be unsafe for people with advanced and severe kidney diseases, such as chronic kidney disease (CKD).
• Severe hepatic impairment: Because Gemtesa's safety in patients with advanced liver disease (cirrhosis) has not been established, it’s not recommended for use in this population.
• Digoxin use: If you take digoxin (sold under the names Digox and Lanoxin, among others), let your healthcare provider know. This drug, usually prescribed with others for heart failure, may interact poorly with Gemtesa.    
• Pediatric use: Whether this drug is safe for children and infants to take is unknown.
• Pregnancy: There are no available data on the use of Gemtesa in pregnant people, although animal studies have shown danger to a fetus only at extremely high dosages­—well over the recommended amounts.
• Breastfeeding: The safety of Gemtesa has not been established in people who are breastfeeding, though the presence of this drug has been detected in the milk of nursing rats, which may indicate a similar presence in human milk.

Other Beta-3 Agonists

Gemtesa is part of a broader family of pharmaceuticals that act on the beta-3 receptors, stimulating their activity. Though some of these drugs may be used for other reasons—including as an antidepressant or to treat irritable bowel syndrome—they’re mostly intended for use against OAB. These include:

• Myrbetriq (mirabegron)
• Amibegron (SR-58,611A)
• Solabegron (GW-427,353)
• Ritobegron (KUC-7483

Aside from Myrbetriq, which currently is available for use, the drugs in this list are still undergoing clinical trials; however, there is a great deal of research into their potential for treating OAB.

Dosage

Gemtesa comes in a tablet form, with a strength of 75 milligrams (mg); one tablet per day is indicated for OAB. These pills are oval-shaped, light green, and have “V75” engraved on one side.

Modifications

While there are no modifications of Gemtesa in terms of dosage amounts, users can crush the tablet, mix it with about 15 milliliters (ml) of applesauce (a little over 1 tablespoon), and drink that with a glass of water. For some, this approach can make taking Gemtesa more palatable.

How to Take and Store

Taking Gemtesa is straightforward. It can be taken with or without food, and it’s best with a glass of water. As for storage of this drug, there are several things to keep in mind:

• Store at room temperature (between 68 and 77 F)
• Keep in a safe place and out of the reach of children
• Dispose of any unused pills safely by taking them back to a pharmacy or a safe disposal site

Cases of overdose haven't yet been recorded. Contact your healthcare provider if you have taken more pills than directed, or if you are experiencing discomfort and severe side effects.

Side Effects

As with any drug, Gemtesa causes some side effects. These should be monitored, and you shouldn’t hesitate to let your healthcare provider know if you are experiencing any unusual symptoms.

Common

Common side effects of Gemtesa use are cause for concern if they’re disruptive and persistent. These include:

• Urinary tract infection (UTI)
• Headache
• Nasal congestion, runny nose, and/or sore throat
• Respiratory tract infection
• Diarrhea
• Nausea

Severe

Only one severe side effect of Gemtesa has been recorded: urninary retention, or the inability to empty the bladder. Chances of this occurring increase if you take other medications for OAB or experience bladder outlet obstruction (BOO).

Not being able to empty the bladder causes discomfort and can lead to infections, weakened urine flow, bladder stones, and kidney problems. If you're not able to empty your bladder, be sure to call your healthcare provider as soon as possible and stop taking this medication.

Warnings and Interactions

When you’re taking Gemtesa, you’ll need to be aware of the following warnings and indications:

• Digox: As noted above, the use of the heart failure drug, Digox, or other brands of digoxin, can lead to poor interaction with Gemtesa. Let your healthcare providers know if you take Digox, as they may need to alter dosages or consider alternatives.
• Pregnancy: If you become pregnant while taking this drug, tell your practitioner immediately. While specific risk has not been established, this medication may be unsafe for the fetus.
• Kidney health: If you experience signs of CKD while taking Gemtesa, let your healthcare provider know as soon as possible. These include nausea, fatigue, kidney pain, loss of appetite, and foamy urine, among others.
• Liver problems: Care should be taken, too, if you’re experiencing liver failure, as in chronic liver disease, cirrhosis, or other conditions. Liver failure can cause jaundice (yellowing of the skin and eyes), abdominal pain, fatigue, decreased appetite, diarrhea, dark urine, and abdominal swelling.