Envarsus XR

The active ingredient in Envarsus XR is tacrolimus ER. Tacrolimus is a calcineurin inhibitor that suppresses certain immune cells that normally help defend the body. In kidney transplant recipients, these same immune cells may mistakenly see the new organ as a threat. Tacrolimus blocks a pathway called calcineurin, which reduces immune activity and lowers the risk of rejection following an organ transplant.

Follow all directions given to you by your doctor and read all documents provided, including the full Prescribing Information, FDA-Approved Product Labeling, Instructions for Use, and Medication Guide before using Envarsus XR. However, the following is a synopsis of the general guidelines for the use of Envarsus XR:

• Take Envarsus XR once a day, preferably in the morning. Swallow the tacrolimus extended-release tablets whole. Do not chew, crush, or split them, as doing so can change how the medicine is absorbed.
• Always take it on an empty stomach, usually at least 1 hour before or 2 hours after a meal. Take the medication at the same time every day to help maintain stable tacrolimus levels.
• Do not drink grapefruit juice, as it can significantly increase tacrolimus levels and raise the risk of toxicity.
• If you miss a dose, take the next dose at the usual time. Do not take extra doses to make up for a missed dose.
• Your healthcare provider will order regular blood tests to check tacrolimus levels, kidney function, potassium levels, creatinine, and other labs during follow-up.
• Do not switch between Envarsus XR, Prograf, or other tacrolimus products unless your healthcare provider specifically instructs you to do so. Different tacrolimus formulations are not interchangeable.

Some mild or common side effects of Envarsus XR include:

• Increased risk of infections.
• Constipation.
• Tremor.
• Diarrhea.
• High blood pressure.
• Stomach pain.
• Edema (swelling).
• Sleep problems.
• High blood sugar (hyperglycemia).
• Increased potassium levels (hyperkalemia).

Some individuals may experience serious side effects while using Envarsus XR. These side effects may require immediate medical attention. If you experience any of the following, contact your healthcare provider or seek emergency medical help:

• Serious infections, including bacterial, viral, or fungal infections.
• Signs of kidney problems, such as decreased urine output or rising creatinine.
• Symptoms of posterior reversible encephalopathy syndrome (PRES) include confusion, seizures, or vision changes.
• A rare brain infection called progressive multifocal leukoencephalopathy (PML).
• Signs of organ rejection.
• Irregular heartbeat or symptoms related to QT prolongation.
• Symptoms of lymphomas or other cancers, including post-transplant lymphoproliferative disorder, are especially common in Epstein-Barr virus–negative patients.
• Severe tremors or symptoms related to tacrolimus toxicity.
• Low red blood cell counts, anemia, or signs of pure red cell aplasia.
• Severe abdominal pain may indicate infections such as polyomavirus-associated nephropathy.
• Symptoms of hemolytic uremic syndrome or thrombotic thrombocytopenic purpura.
• Trouble breathing or signs of heart failure.

These are not all of the possible side effects of Envarsus XR. You should always seek medical advice from your healthcare provider for any questions or concerns about your medical condition or treatment. Read all patient information, medication guides, or drug information sheets that come with this medication. You can also report adverse effects to the Food and Drug Administration at www.fda.gov/medwatch or 1-800-FDA-1088.

Before starting Envarsus XR, it is crucial to discuss any existing health conditions with your healthcare provider. You should be sure that your healthcare provider is aware of all your medical conditions, including if you have:

• A history of kidney disease or liver disease.
• Heart problems, including heart failure, heart rhythm problems, or QT prolongation.
• High blood pressure.
• Diabetes or risk factors for high blood sugar.
• A weakened immune system.
• Any type of cancer or a family history of cancer.
• High potassium levels.
• A history of seizures or nervous system problems.
• A history of serious infections.
• Whether you have received live vaccines recently or plan to receive them.

Boxed Warning

• Envarsus XR has an increased risk of serious infections and certain cancers, including lymphoma and skin cancer. This is because Envarsus XR suppresses the immune system. Regular monitoring and sun protection are important.

Allergic to tacrolimus or any of the ingredients in the tablet.

Envarsus XR begins working as soon as you start treatment, but it may take several days for tacrolimus levels to stabilize. Because it is an extended-release formulation, blood levels rise gradually and remain more consistent compared to immediate-release tacrolimus.

When Envarsus XR is taken with other prescription drugs, over-the-counter medications, vitamins, and supplements, it may change how they work or increase the frequency or severity of side effects. Make sure that you tell your healthcare professional about anything that you are taking to avoid any negative drug interactions, including:

• Strong CYP3A4 inhibitors such as ketoconazole, clarithromycin, diltiazem, amiodarone, or certain antivirals
• Strong CYP3A4 inducers such as rifampin or St. John’s wort.
• Other immunosuppressants like cyclosporine, sirolimus, or everolimus.
• Medicines that increase potassium levels.
• Diuretics.
• Antifungal medications.
• Seizure medications.
• Heart rhythm medications.
• Herbal supplements, especially St. John’s wort.
• Grapefruit juice, which raises tacrolimus levels.

Envarsus XR extended-release tablets are available in multiple strengths. Available dosage forms include 0.75 mg, 1 mg, and 4 mg. Your healthcare provider will choose the dose that is right for you based on your tacrolimus blood levels, kidney function, and how your body responds.

Store Envarsus XR at room temperature, out of reach of children and pets.

Envarsus XR is manufactured by Veloxis Pharmaceuticals.

At this time, Envarsus XR is available only as a brand-name product. Generic tacrolimus products exist, but they are not the same formulation as Envarsus XR and cannot be substituted unless your healthcare provider approves it.

Do not stop taking Envarsus XR on your own. Suddenly stopping tacrolimus can lead to organ rejection and other serious complications. If your healthcare provider decides that your treatment should change, they will create a plan to adjust your dose safely or transition you to another medication.

Envarsus XR can cause fetal harm when used in pregnancy. Risks include prematurity, birth defects, and low birth weight. If you or your partner can have a child, you should use effective birth control before and during treatment with this medication.

Envarsus XR can pass into breast milk, and your healthcare provider will help determine if breastfeeding is safe in your situation. It’s important to weigh the benefits and risks. Talk to your doctor if you are already breastfeeding or if you have any plans to breastfeed.