Tacrolimus: A Complete Overview

Tacrolimus is a prescription immunosuppressant medication used primarily to prevent organ rejection in people who have received a kidney, liver, or heart transplant.

If you or a loved one has been prescribed Tacrolimus, you probably have questions — what it does, how to take it, what it costs, and what to watch out for. This guide covers everything you need to know in plain language.

What Is Tacrolimus?

Tacrolimus is a calcineurin inhibitor, a type of immunosuppressant drug that works by calming down your immune system so it doesn't attack a transplanted organ. It was first approved by the FDA in 1994 and has become one of the most widely used anti-rejection medications worldwide.

Brand Names

• Prograf — immediate-release capsules and injectable solution (manufactured by Astellas Pharma)
• Astagraf XL — extended-release capsules (Astellas Pharma)
• Envarsus XR — extended-release tablets (Veloxis Pharmaceuticals)
• Protopic — topical ointment for skin conditions (Astellas Pharma)

Generic Availability

Yes, generic Tacrolimus is widely available for the immediate-release oral capsules. Generic versions of extended-release formulations may also be available. Generic Tacrolimus is significantly cheaper than brand-name versions.

Controlled Substance Status

Tacrolimus is not a controlled substance. It does not have a DEA schedule. However, it is a prescription-only medication that requires careful medical supervision.

What Is Tacrolimus Used For?

FDA-Approved Uses

• Kidney transplant — Prevention of organ rejection
• Liver transplant — Prevention of organ rejection
• Heart transplant — Prevention of organ rejection
• Atopic dermatitis — Moderate to severe eczema (topical Protopic only)

Off-Label Uses

Doctors sometimes prescribe Tacrolimus for conditions beyond its FDA-approved uses, including:

• Lung transplant rejection prevention
• Graft-versus-host disease (GVHD)
• Crohn's disease and ulcerative colitis
• Lupus nephritis
• Myasthenia gravis
• Rheumatoid arthritis
• Vitiligo (topical use)

How Is Tacrolimus Taken?

Tacrolimus comes in several forms, and the right one depends on your condition and your doctor's recommendation:

Dosage Forms

• Immediate-release capsules (Prograf) — 0.5 mg, 1 mg, 5 mg. Taken twice daily, approximately 12 hours apart.
• Extended-release capsules (Astagraf XL) — 0.5 mg, 1 mg, 5 mg. Taken once daily in the morning.
• Extended-release tablets (Envarsus XR) — 0.75 mg, 1 mg, 4 mg. Taken once daily in the morning.
• Oral granules for suspension (Prograf) — 0.2 mg and 1 mg packets. For patients who can't swallow capsules.
• Injectable solution (Prograf) — 5 mg/mL. Used in hospitals when patients can't take oral medications.
• Topical ointment (Protopic) — 0.03% and 0.1%. Applied to the skin for eczema.

Typical Dosing

For transplant patients, the typical starting dose range is 0.075–0.2 mg/kg/day, divided into two doses (for immediate-release) or taken once daily (for extended-release). Your doctor will adjust the dose based on regular blood level monitoring (trough levels). Doses vary by transplant type:

• Kidney transplant: 0.1–0.2 mg/kg/day
• Liver transplant: 0.1–0.15 mg/kg/day
• Heart transplant: 0.075 mg/kg/day

Important Instructions

• Take at the same times every day — consistency matters
• Swallow capsules whole; do not crush or chew
• You can take it with or without food, but be consistent day to day
• Avoid grapefruit and grapefruit juice — they increase Tacrolimus levels dangerously
• Do not drink alcohol with extended-release formulations
• Never skip doses without talking to your doctor

Critical warning: Prograf, Envarsus XR, and Astagraf XL are not interchangeable. Do not switch between formulations without your doctor's supervision.

Who Should Not Take Tacrolimus?

Tacrolimus is not right for everyone. You should not take it if you have:

• An allergy to Tacrolimus or any ingredient in the formulation
• An allergy to polyoxyl 60 hydrogenated castor oil (HCO-60) — this applies to the IV formulation only

Special caution is needed for:

• Patients with liver disease — Lower doses may be required
• Patients with kidney disease — Tacrolimus can worsen kidney function
• Pregnant women — Tacrolimus crosses the placenta and may harm the baby, though transplant patients may need to continue with monitoring
• Breastfeeding women — Tacrolimus passes into breast milk; breastfeeding is not recommended

For a detailed look at potential side effects, read our guide on Tacrolimus side effects.

How Much Does Tacrolimus Cost?

Cost varies significantly depending on whether you're getting the brand-name or generic version:

• Generic Tacrolimus IR capsules: approximately $30–$65 for 60 capsules (1 mg) with discount coupons like GoodRx. Without coupons, retail price may be $150–$300+.
• Brand-name Prograf: approximately $570–$722 for 60 capsules (1 mg)
• Extended-release formulations: Typically more expensive than immediate-release generics

Insurance Coverage

Most insurance plans and Medicare Part D cover generic Tacrolimus. Brand-name formulations may require prior authorization or step therapy. Medicare covers immunosuppressive drugs for transplant recipients. Transplant patients often have specialty pharmacy requirements.

Ways to Save

Several programs can help reduce your costs:

• Manufacturer copay cards — Astagraf XL and Envarsus XR offer copay assistance for commercially insured patients
• Patient assistance programs — Astellas Cares provides Prograf and Astagraf XL at no cost for eligible uninsured or underinsured patients
• Discount coupons — GoodRx, SingleCare, and other platforms offer savings on generic Tacrolimus
• The American Kidney Fund — Offers financial assistance for transplant patients including medication costs

For the full breakdown, see our guide to saving money on Tacrolimus.

Final Thoughts

Tacrolimus is one of the most important medications in transplant medicine, helping hundreds of thousands of people keep their transplanted organs functioning. Understanding what it is, how to take it properly, and what it costs puts you in a better position to manage your health.

If you need help finding Tacrolimus at a pharmacy near you, Medfinder can help you locate it in stock. And if you have questions about whether Tacrolimus is right for you, talk to your transplant specialist or prescribing doctor.