Last reviewed 2026-04-20 · How we verify

Prograf (TACROLIMUS)

Prograf works by inhibiting the activation of T-lymphocytes, a type of immune cell.

Prograf (TACROLIMUS) is a calcineurin inhibitor immunosuppressant developed by Astellas, targeting interferon gamma to prevent transplant rejection and treat atopic dermatitis and intractable eczema. It is a small molecule with a half-life of 26 hours and bioavailability of 25%. Prograf is off-patent with 18 generic manufacturers, approved for various transplant rejection indications since 1994. Key safety considerations include monitoring of blood levels and potential side effects such as tremors, hypertension, and kidney damage. As a calcineurin inhibitor, Prograf works by inhibiting the activation of T-lymphocytes.

At a glance

Mechanism of action

Mechanism of Action. The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This effect has been shown to prevent the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), nuclear component thought to initiate gene transcription for the formation of lymphokines (such as interleukin-2, gamma interferon). Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediato

Approved indications

• Atopic dermatitis
• Intractable Eczema
• Liver transplant rejection
• Prevention of Cardiac Transplant Rejection
• Prevention of Kidney Transplant Rejection
• Prevention of Liver Transplant Rejection
• Prevention of Transplant Rejection
• Renal transplant rejection
• Transplanted organ rejection

Boxed warnings

• WARNING: MALIGNANCIES AND SERIOUS INFECTIONS IN TRANSPLANT PATIENTS; AND INCREASED MORTALITY IN FEMALE LIVER TRANSPLANT PATIENTS Increased risk for developing serious infections and malignancies with tacrolimus extended-release capsulest or other immunosuppressants that may lead to hospitalization or death. [see Warnings and Precautions ( 5.1 , 5.2 )] Increased mortality in female liver transplant patients with tacrolimus extended-release capsulest. Tacrolimus extended-release capsulest is not approved for use in liver transplantation. [see Warnings and Precautions ( 5.3 )] WARNING: MALIGNANCIES AND SERIOUS INFECTIONS IN TRANSPLANT PATIENTS; and INCREASED MORTALITY IN FEMALE LIVER TRANSPLANT PATIENTS See full prescribing information for complete boxed warning. Increased risk for developing serious infections and malignancies with with tacrolimus extended-release capsules or other immunosuppressants that may lead to hospitalization or death. ( 5.1 , 5.2 ) Increased mortality in female liver transplant patients with with tacrolimus extended-release capsules. Not approved for use in liver transplantation. ( 5.3 )

Common side effects

• Transplant rejection
• Cytomegalovirus infection
• Post transplant lymphoproliferative disorder
• Thrombotic microangiopathy
• Immunosuppressant drug level increased
• Polyomavirus-associated nephropathy
• BK virus infection
• Acute graft versus host disease
• Cytomegalovirus viraemia
• Complications of transplanted kidney
• Transplant dysfunction
• Epstein-Barr virus infection

Drug interactions

• P-glycoprotein Substrates
• amobarbital
• aprobarbital
• barbital
• butalbital
• carbamazepine
• dexlansoprazole
• ethotoin
• fosphenytoin
• hexobarbital
• mephenytoin
• metharbital

Key clinical trials

• Intensity Modulated Total Marrow Irradiation, Fludarabine Phosphate, and Melphalan in Treating Patients With Relapsed Hematologic Cancers Undergoing a Second Donor Stem Cell Transplant (PHASE1)
• A Phase II Study of Allogeneic Hematopoietic Stem Cell Transplant for Subjects With VEXAS (Vacuoles, E1 Enzyme, X-linked, Autoinflammatory, Somatic) Syndrome (PHASE2)
• A Study to Evaluate Efficacy, Safety, and Tolerability of Povetacicept in Participants With Primary Membranous Nephropathy (pMN) (PHASE2,PHASE3)
• Combination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia (PHASE2)
• JAK Inhibitor Before Donor Stem Cell Transplant in Treating Patients With Primary or Secondary Myelofibrosis (PHASE2)
• Itacitinib, Tacrolimus, and Sirolimus for the Prevention of GVHD in Patients With Acute Leukemia, Myelodysplastic Syndrome, or Myelofibrosis Undergoing Reduced Intensity Conditioning Donor Stem Cell Transplantation (PHASE2)
• A Study to Investigate the Efficacy and Safety of Frexalimab Versus Tacrolimus in Adults Undergoing Kidney Transplantation (PHASE2,PHASE3)
• Tocilizumab in Lung Transplantation (PHASE2)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Prograf CI brief — competitive landscape report
• Prograf updates RSS · CI watch RSS
• Astellas Pharma portfolio CI