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Tacrolimus

Generic Name
Tacrolimus
Brand Names
Advagraf, Astagraf, Envarsus, Modigraf, Prograf, Protopic, Tacforius
Drug Type
Small Molecule
Chemical Formula
C44H69NO12
CAS Number
104987-11-3
Unique Ingredient Identifier
Y5L2157C4J
Background

Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex inhibits calcineurin which inhibits T-lymphocyte signal transduction and IL-2 transcription.

Indication

Immediate-release formulations of tacrolimus are indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving allogeneic liver, kidney, heart, or lung transplants, in combination with other immunosuppressants. Extended-release formulations of tacrolimus are indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving kidney transplants, in combination with other immunosuppressants, and may be used in patients converted from immediate-release formulations.

Topical tacrolimus ointment is indicated as second-line therapy for short-term and non-continuous treatment of moderate-to-severe atopic dermatitis in non-immunocompromised adults and children who have failed to respond adequately to other topical treatments or for whom alternative treatments are not advisable. Both available strengths are indicated in adult patients, while only the lower strength (0.03%) formulation is indicated in pediatric patients between 2 and 15 years of age.

Associated Conditions
Graft-versus-host Disease (GVHD), Heart Transplant Rejection, Kidney Transplant Rejection, Liver Transplant Rejection, Lung Transplant Rejection, Oral Lichen Planus, Psoriasis, Pyoderma Gangrenosum, Rheumatoid Arthritis, Severe Atopic Dermatitis, Vitiligo, Moderate Atopic dermatitis
Associated Therapies
-

Single or Double Donor Umbilical Cord Blood Transplant in Treating Patients With High-Risk Hematologic Malignancies

Phase 2
Withdrawn
Conditions
Accelerated Phase Chronic Myelogenous Leukemia
Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome
Adult Acute Lymphoblastic Leukemia in Remission
Adult Acute Myeloid Leukemia in Remission
Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities
Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)
Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)
Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)
Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)
Adult Nasal Type Extranodal NK/T-cell Lymphoma
Interventions
Drug: cyclophosphamide
Drug: fludarabine phosphate
Drug: mycophenolate mofetil
Procedure: allogeneic hematopoietic stem cell transplantation
Procedure: umbilical cord blood transplantation
Procedure: double-unit umbilical cord blood transplantation
Radiation: total-body irradiation
Drug: tacrolimus
Procedure: peripheral blood stem cell transplantation
First Posted Date
2012-07-27
Last Posted Date
2016-07-14
Lead Sponsor
University of Medicine and Dentistry of New Jersey
Registration Number
NCT01652014
Locations
🇺🇸

Cancer Institute of New Jersey, New Brunswick, New Jersey, United States

Comparison of a Tacrolimus Hexal® Based Regimen Versus a Prograf® Based Regimen in de Novo Renal Transplant Recipients

Phase 4
Completed
Conditions
Pharmacokinetics Study in de Novo Kidney Transplantation
Interventions
Drug: Tacrolimus Hexal
Drug: Prograf
First Posted Date
2012-07-25
Last Posted Date
2019-06-17
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
73
Registration Number
NCT01649427
Locations
🇩🇪

Novartis Investigative Site, Koeln-Merheim, Germany

Using mTOR Inhibitors in the Prevention of BK Nephropathy

Not Applicable
Completed
Conditions
BK Nephropathy
BK Viremia
Interventions
Drug: Tacrolimus
Drug: Mycophenolate acid
Drug: Sirolimus
First Posted Date
2012-07-25
Last Posted Date
2018-02-28
Lead Sponsor
Columbia University
Target Recruit Count
40
Registration Number
NCT01649609
Locations
🇺🇸

Columbia University Medical Center, New York, New York, United States

🇺🇸

Weill Cornell Medical Center, New York, New York, United States

Allogeneic Stem Cell Transplant for CLL

Phase 1
Terminated
Conditions
Chronic Lymphocytic Leukemia
Prolymphocytic Leukemia
Allogeneic Hematopoietic Stem Cell Transplantation Recipient
Richter Syndrome
Interventions
Procedure: Allogeneic Hematopoietic Stem Cell Transplantation
Biological: Anti-Thymocyte Globulin
Drug: Busulfan
Drug: Clofarabine
Biological: Filgrastim
Drug: Gemcitabine
Drug: Methotrexate
Drug: Tacrolimus
First Posted Date
2012-06-27
Last Posted Date
2020-02-24
Lead Sponsor
M.D. Anderson Cancer Center
Target Recruit Count
15
Registration Number
NCT01629511
Locations
🇺🇸

M D Anderson Cancer Center, Houston, Texas, United States

A National Multi-center Randomized, Open Label Study to Evaluate Efficacy and Safety of Everolimus With EC-MPS Compared to Standard Treatment Combination Tacrolimus and EC-MPS in de Novo Liver Transplant Recipients

Phase 3
Completed
Conditions
Liver Transplantation
Interventions
First Posted Date
2012-06-21
Last Posted Date
2016-04-27
Lead Sponsor
Novartis Pharmaceuticals
Target Recruit Count
188
Registration Number
NCT01625377
Locations
🇫🇷

Novartis Investigative Site, Villejuif, France

T-Cell Replete Haploidentical Donor Hematopoietic Stem Cell Plus Natural Killer (NK) Cell Transplantation in Patients With Hematologic Malignancies Relapsed or Refractory Despite Previous Allogeneic Transplant

Phase 2
Terminated
Conditions
Acute Lymphoblastic Leukemia
Chronic Myelocytic Leukemia
Juvenile Myelomonocytic Leukemia
Hodgkin or Non-Hodgkin Lymphoma
Sarcoma, Myeloid
Myelodysplastic Syndrome
Acute Myelocytic Leukemia
Interventions
First Posted Date
2012-06-18
Last Posted Date
2017-02-20
Lead Sponsor
St. Jude Children's Research Hospital
Target Recruit Count
34
Registration Number
NCT01621477
Locations
🇺🇸

St. Jude Children's Research Hospital, Memphis, Tennessee, United States

NK Cells in Cord Blood Transplantation

Phase 1
Conditions
Acute Lymphoblastic Leukemia in Remission
Myelodysplastic Syndrome
Recurrent Acute Lymphoblastic Leukemia
Recurrent Non-Hodgkin Lymphoma
Accelerated Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive
DS Stage III Plasma Cell Myeloma
High Grade B-Cell Lymphoma With MYC and BCL2 or BCL6 Rearrangements
ISS Stage III Plasma Cell Myeloma
Acute Biphenotypic Leukemia
Recurrent Acute Myeloid Leukemia
Interventions
Procedure: Allogeneic Hematopoietic Stem Cell Transplantation
Drug: Fludarabine Phosphate
Drug: Cyclophosphamide
Other: Laboratory Biomarker Analysis
Drug: Lenalidomide
Drug: Melphalan
Drug: Mycophenolate Mofetil
Biological: Natural Killer Cell Therapy
Biological: Rituximab
Drug: Tacrolimus
Procedure: Umbilical Cord Blood Transplantation
Radiation: Total-Body Irradiation
First Posted Date
2012-06-14
Last Posted Date
2020-02-11
Lead Sponsor
M.D. Anderson Cancer Center
Target Recruit Count
13
Registration Number
NCT01619761
Locations
🇺🇸

M D Anderson Cancer Center, Houston, Texas, United States

A Study to Compare How the Body Absorbs and Processes Two Different Formulations of the Anti-rejection Medication Tacrolimus (Advagraf® or Prograf®) in Children Receiving an Organ Transplant, and How Safe and Effective They Are Over a Longer Period of Time

Phase 2
Completed
Conditions
Heart Transplantation
Kidney Transplantation
Liver Transplantation
Interventions
Drug: Tacrolimus
Drug: Tacrolimus prolonged release
First Posted Date
2012-06-08
Last Posted Date
2024-11-01
Lead Sponsor
Astellas Pharma Europe Ltd.
Target Recruit Count
44
Registration Number
NCT01614665
Locations
🇫🇷

Site FR32, Paris Cedex 15, France

🇨🇿

Site CZ61, Prague 5, Czechia

🇫🇷

Site FR33, Bron Cedex, France

and more 7 locations

A Clinical Trial to Assess the Efficacy and Safety of the Conversion to Everolimus

Phase 4
Conditions
Kidney Transplant Recipients
Interventions
First Posted Date
2012-05-31
Last Posted Date
2012-05-31
Lead Sponsor
Hospital de Clinicas de Porto Alegre
Target Recruit Count
120
Registration Number
NCT01608412
Locations
🇧🇷

Hospital de Clínicas de Porto Alegre, Porto Alegre, RS, Brazil

Proactive Treatment of Tacrolimus Ointment for Adult Facial Seborrheic Dermatitis

Phase 4
Completed
Conditions
Seborrheic Dermatitis
Interventions
First Posted Date
2012-05-03
Last Posted Date
2012-08-08
Lead Sponsor
Pusan National University Hospital
Target Recruit Count
104
Registration Number
NCT01591070
Locations
🇰🇷

Department of dermatology, Pusan National University Hospital, Busan, Korea, Republic of

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