Detail

Tacrolimus

Description

Name: Tacrolimus
Type: small molecule
Groups: Array
Indication: For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.
Accession Number: DB00864 ( APRD00276, EXPT01437)
Description: 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 interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription.
Structure:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Advagrafcapsule (extended release)0.5 mgoral09-04-2008Canada
Advagrafcapsule (extended release)1 mgoral09-04-2008Canada
Advagrafcapsule (extended release)5 mgoral09-04-2008Canada
Advagrafcapsule (extended release)3 mgoral05-04-2010Canada
Astagraf XLcapsule, coated, extended release.5 mg/1oral19-07-2013US
Astagraf XLcapsule, coated, extended release1 mg/1oral19-07-2013US
Astagraf XLcapsule, coated, extended release5 mg/1oral19-07-2013US
Envarsus XRtablet, extended release1 mg/1oral01-09-2015US
Envarsus XRtablet, extended release4 mg/1oral01-09-2015US
Envarsus XRtablet, extended release.75 mg/1oral01-09-2015US
Prografcapsule5 mgoral14-08-1996Canada
Prografcapsule1 mgoral14-08-1996Canada
Prografsolution5 mgintravenous14-08-1996Canada
Prografcapsule0.5 mgoral02-04-2001Canada
Prografcapsule, gelatin coated1 mg/1oral08-04-1994US
Prografcapsule, gelatin coated.5 mg/1oral24-08-1998US
Prografcapsule, gelatin coated1 mg/1oral08-04-1994US
Prografcapsule, gelatin coated5 mg/1oral08-04-1994US
Prografinjection, solution5 mg/mLintravenous08-04-1994US
Prografcapsule, gelatin coated1 mg/1oral08-04-1994US
Protopicointment.3 mg/gtopical08-12-2000US
Protopicointment1 mg/gtopical08-12-2000US
Protopicointment1 mg/gtopical08-05-2008US
Protopicointment0.1 %topical06-09-2001Canada
Protopicointment0.03 %topical06-09-2001Canada
Sandoz Tacrolimuscapsule (immediate release)0.5 mgoral11-06-2014Canada
Sandoz Tacrolimuscapsule (immediate release)1 mgoral25-11-2013Canada
Sandoz Tacrolimuscapsule (immediate release)5 mgoral25-11-2013Canada
Tacrolimusointment.3 mg/gtopical20-11-2014US
Tacrolimusointment1 mg/gtopical20-11-2014US

Generic Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Hecoriacapsule.5 mg/1oral20-12-2011US
Hecoriacapsule1 mg/1oral20-12-2011US
Hecoriacapsule5 mg/1oral20-12-2011US
Tacrolimuscapsule1 mg/1oral10-08-2009US
Tacrolimuscapsule5 mg/1oral10-08-2009US
Tacrolimuscapsule1 mg/1oral15-06-2011US
Tacrolimuscapsule.5 mg/1oral15-06-2011US
Tacrolimusointment1 mg/gtopical09-09-2014US
Tacrolimusointment.3 mg/gtopical09-09-2014US
Tacrolimuscapsule1 mg/1oral10-12-2010US
Tacrolimuscapsule1 mg/1oral10-08-2009US
Tacrolimuscapsule1 mg/1oral10-08-2009US
Tacrolimuscapsule5 mg/1oral01-11-2010US
Tacrolimuscapsule.5 mg/1oral28-09-2012US
Tacrolimuscapsule.5 mg/1oral15-11-2010US
Tacrolimuscapsule1 mg/1oral28-09-2012US
Tacrolimuscapsule1 mg/1oral01-11-2010US
Tacrolimuscapsule5 mg/1oral28-09-2012US
Tacrolimuscapsule1 mg/1oral05-01-2015US
Tacrolimuscapsule, gelatin coated1 mg/1oral30-10-2012US
Tacrolimuscapsule1 mg/1oral17-07-2013US
Tacrolimuscapsule.5 mg/1oral14-05-2010US
Tacrolimuscapsule1 mg/1oral14-05-2010US
Tacrolimuscapsule5 mg/1oral14-05-2010US
Tacrolimuscapsule5 mg/1oral06-07-2010US
Tacrolimuscapsule.5 mg/1oral31-08-2011US
Tacrolimuscapsule1 mg/1oral31-08-2011US
Tacrolimuscapsule5 mg/1oral31-08-2011US
Tacrolimuscapsule.5 mg/1oral23-07-2012US
Tacrolimuscapsule1 mg/1oral23-07-2012US
Tacrolimuscapsule5 mg/1oral23-07-2012US
Tacrolimuscapsule.5 mg/1oral17-07-2013US
Tacrolimuscapsule1 mg/1oral17-07-2013US
Tacrolimuscapsule5 mg/1oral17-07-2013US
Tacrolimuscapsule.5 mg/1oral15-01-2012US
Tacrolimuscapsule1 mg/1oral15-01-2012US
Tacrolimuscapsule5 mg/1oral15-01-2012US
Tacrolimuscapsule.5 mg/1oral13-08-2014US
Tacrolimuscapsule1 mg/1oral13-08-2014US
Tacrolimuscapsule5 mg/1oral13-08-2014US
Tacrolimuscapsule, gelatin coated.5 mg/1oral30-07-2015US
Tacrolimuscapsule, gelatin coated1 mg/1oral30-07-2015US
Tacrolimuscapsule, gelatin coated5 mg/1oral30-07-2015US
Tacrolimuscapsule.5 mg/1oral10-08-2009US

Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
HecoriaTacrolimus
HecoriaTacrolimus
HecoriaTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
PrografTacrolimus
PrografTacrolimus
Astagraf XLTacrolimus
PrografTacrolimus
Astagraf XLTacrolimus
Astagraf XLTacrolimus
PrografTacrolimus
ProtopicTacrolimus
ProtopicTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
PrografTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
ProtopicTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
PrografTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
TacrolimusTacrolimus
Envarsus XRTacrolimus
Envarsus XRTacrolimus
Envarsus XRTacrolimus
PrografTacrolimus
PrografTacrolimus
PrografTacrolimus
PrografTacrolimus
AdvagrafTacrolimus
AdvagrafTacrolimus
AdvagrafTacrolimus
AdvagrafTacrolimus
Sandoz TacrolimusTacrolimus
Sandoz TacrolimusTacrolimus
Sandoz TacrolimusTacrolimus
ProtopicTacrolimus
ProtopicTacrolimus

Categories
  • No Category

Pharmacology

Indication: For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.
Pharmacodynamics: Not Available
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. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. 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 mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.
Absorption: Absorption of tacrolimus from the gastrointestinal tract after oral administration is incomplete and variable. The absolute bioavailability in adult kidney transplant patients is 17±10%; in adults liver transplant patients is 22±6%; in healthy subjects is 18±5%. The absolute bioavailability in pediatric liver transplant patients was 31±24%. Tacrolimus maximum blood concentrations (Cmax) and area under the curve (AUC) appeared to increase in a dose-proportional fashion in 18 fasted healthy volunteers receiving a single oral dose of 3, 7, and 10 mg. When given without food, the rate and extent of absorption were the greatest. The time of the meal also affected bioavailability. When given immediately after a meal, mean Cmax was reduced 71%, and mean AUC was reduced 39%, relative to the fasted condition. When administered 1.5 hours following the meal, mean Cmax was reduced 63%, and mean AUC was reduced 39%, relative to the fasted condition.
Volume of distribution:
  • 2.6 ± 2.1 L/kg [pediatric liver transplant patients]
  • 1.07 ± 0.20 L/kg [patients with renal impairment, 0.02 mg/kg/4 hr dose, IV]
  • 3.1 ± 1.6 L/kg [Mild Hepatic Impairment, 0.02 mg/kg/4 hr dose, IV]
  • 3.7 ± 4.7 L/kg [Mild Hepatic Impairment, 7.7 mg dose, PO]
  • 3.9 ± 1.0 L/kg [Severe hepatic impairment, 0.02 mg/kg/4 hr dose, IV]
  • 3.1 ± 3.4 L/kg [Severe hepatic impairment, 8 mg dose, PO]

Protein binding: ~99% bound to human plasma protein, primarily to albumin and alpha-1-acid glycoprotein. This is independent of concentration over a range of 5-50 ng/mL.
Metabolism: Not Available
Route of elimination: In man, less than 1% of the dose administered is excreted unchanged in urine. When administered IV, fecal elimination accounted for 92.6±30.7%, urinary elimination accounted for 2.3±1.1%.
Half life: The elimination half life in adult healthy volunteers, kidney transplant patients, liver transplants patients, and heart transplant patients are approximately 35, 19, 12, 24 hours, respectively. The elimination half life in pediatric liver transplant patients was 11.5±3.8 hours, in pediatric kidney transplant patients was 10.2±5.0 (range 3.4-25) hours.
Clearance: Not Available
Toxicity: Side effects can be severe and include blurred vision, liver and kidney problems (it is nephrotoxic), seizures, tremors, hypertension, hypomagnesemia, diabetes mellitus, hyperkalemia, itching, insomnia, confusion. LD50=134-194 mg/kg (rat).
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Astellas pharma us inc
  • Dr reddys laboratories ltd
  • Sandoz inc
  • Watson laboratories inc
  • Astellas Pharma US

Packagers:
Dosage forms
FormRouteStrength
Capsule (extended release)oral0.5 mg
Capsule (extended release)oral1 mg
Capsule (extended release)oral3 mg
Capsule (extended release)oral5 mg
Capsule, coated, extended releaseoral.5 mg/1
Capsule, coated, extended releaseoral1 mg/1
Capsule, coated, extended releaseoral5 mg/1
Tablet, extended releaseoral.75 mg/1
Tablet, extended releaseoral1 mg/1
Tablet, extended releaseoral4 mg/1
Capsuleoral.5 mg/1
Capsuleoral1 mg/1
Capsuleoral5 mg/1
Capsuleoral0.5 mg
Capsuleoral1 mg
Capsuleoral5 mg
Capsule, gelatin coatedoral.5 mg/1
Capsule, gelatin coatedoral1 mg/1
Capsule, gelatin coatedoral5 mg/1
Injection, solutionintravenous5 mg/mL
Solutionintravenous5 mg
Ointmenttopical0.03 %
Ointmenttopical0.1 %
Capsule (immediate release)oral0.5 mg
Capsule (immediate release)oral1 mg
Capsule (immediate release)oral5 mg
Ointmenttopical.3 mg/g
Ointmenttopical1 mg/g

Prices
Unit descriptionCostUnit
Tacrolimus anhydrous 0.5 mg cap$2.23each
Prograf 0.5 mg capsule$2.43capsule
Protopic 0.03% ointment$4.09g
Protopic 0.1% ointment$4.17g
Tacrolimus anhydrous 1 mg cap$4.46each
Tacrolimus 1 mg capsule$4.64capsule
Prograf 1 mg capsule$4.85capsule
Tacrolimus anhydrous 5 mg cap$22.3each
Prograf 5 mg capsule$24.26capsule
Protopic 0.1% Ointment 30 gm Tube$124.42tube
Protopic 0.03% Ointment 30 gm Tube$132.99tube
Prograf 5 mg/ml ampule$163.94ml
Protopic 0.03% Ointment 60 gm Tube$251.17tube
Protopic 0.1% Ointment 60 gm Tube$255.34tube
Tacrolimus micronized powder$2800.0g

Patents
CountryPatent NumberApprovedExpires (estimated)
1338491Canada1996-07-302013-07-30
2037408Canada2002-12-172011-03-01
5260301United States1994-02-282011-02-28
5665727United States1994-09-092014-09-09

Interactions

Drug Interactions
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Abatacept.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Tacrolimus.
AdalimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Adalimumab.
ado-trastuzumab emtansineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with ado-trastuzumab emtansine.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Tacrolimus.
AlemtuzumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Alemtuzumab.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Tacrolimus.
AltretamineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Altretamine.
AmilorideAmiloride may increase the hyperkalemic activities of Tacrolimus.
AmlodipineThe serum concentration of Tacrolimus can be increased when it is combined with Amlodipine.
AmsacrineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Amsacrine.
AnakinraThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Anakinra.
Anti-thymocyte Globulin (Rabbit)The risk or severity of adverse effects can be increased when Tacrolimus is combined with Anti-thymocyte Globulin (Rabbit).
AprepitantThe serum concentration of Tacrolimus can be increased when it is combined with Aprepitant.
AtazanavirThe metabolism of Tacrolimus can be decreased when combined with Atazanavir.
AzacitidineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Azacitidine.
AzathioprineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Azathioprine.
AzithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Azithromycin.
BasilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Basil.
BasiliximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Basiliximab.
BatimastatThe metabolism of Tacrolimus can be decreased when combined with Batimastat.
BelataceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belatacept.
BelimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belimumab.
BetamethasoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Betamethasone.
BexaroteneThe serum concentration of Tacrolimus can be decreased when it is combined with Bexarotene.
BleomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Bleomycin.
BlinatumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Blinatumomab.
BoceprevirThe serum concentration of Tacrolimus can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Tacrolimus can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Tacrolimus.
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Brentuximab vedotin.
BudesonideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Budesonide.
BusulfanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Busulfan.
CabazitaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cabazitaxel.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Tacrolimus.
CanakinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Canakinumab.
CapecitabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Capecitabine.
CarboplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carboplatin.
CarmustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carmustine.
CaspofunginThe serum concentration of Tacrolimus can be decreased when it is combined with Caspofungin.
CelecoxibCelecoxib may increase the nephrotoxic activities of Tacrolimus.
Certolizumab pegolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Certolizumab pegol.
ChlorambucilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Chlorambucil.
ChloramphenicolThe serum concentration of Tacrolimus can be increased when it is combined with Chloramphenicol.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Tacrolimus.
Choline fenofibrateTacrolimus may increase the nephrotoxic activities of Choline fenofibrate.
CinacalcetThe serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet.
CisplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cisplatin.
CitalopramTacrolimus may increase the QTc-prolonging activities of Citalopram.
CladribineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cladribine.
ClarithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Clarithromycin.
ClofarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clofarabine.
ClotrimazoleThe serum concentration of Tacrolimus can be increased when it is combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clozapine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Tacrolimus.
ConivaptanThe serum concentration of Tacrolimus can be increased when it is combined with Conivaptan.
CorticotropinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Corticotropin.
Cortisone acetateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cortisone acetate.
CrizotinibThe serum concentration of Tacrolimus can be increased when it is combined with Crizotinib.
CyclophosphamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cyclophosphamide.
CyclosporineTacrolimus may increase the nephrotoxic activities of Cyclosporine.
CytarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cytarabine.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Tacrolimus.
DabrafenibThe serum concentration of Tacrolimus can be decreased when it is combined with Dabrafenib.
DacarbazineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dacarbazine.
DactinomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dactinomycin.
DanazolThe serum concentration of Tacrolimus can be increased when it is combined with Danazol.
DarunavirThe metabolism of Tacrolimus can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Tacrolimus can be increased when it is combined with Dasatinib.
DaunorubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Daunorubicin.
DeferasiroxThe serum concentration of Tacrolimus can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tacrolimus.
DexamethasoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dexamethasone.
DiclofenacDiclofenac may increase the nephrotoxic activities of Tacrolimus.
DiflunisalDiflunisal may increase the nephrotoxic activities of Tacrolimus.
DiltiazemThe metabolism of Tacrolimus can be decreased when combined with Diltiazem.
DinutuximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dinutuximab.
DocetaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Docetaxel.
DofetilideTacrolimus may increase the QTc-prolonging activities of Dofetilide.
DoxorubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Doxorubicin.
DronedaroneTacrolimus may increase the QTc-prolonging activities of Dronedarone.
EculizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Eculizumab.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Tacrolimus.
EfavirenzThe serum concentration of Tacrolimus can be decreased when it is combined with Efavirenz.
EfonidipineThe serum concentration of Tacrolimus can be increased when it is combined with Efonidipine.
EnzalutamideThe serum concentration of Tacrolimus can be decreased when it is combined with Enzalutamide.
EpirubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Epirubicin.
EplerenoneEplerenone may increase the hyperkalemic activities of Tacrolimus.
ErtapenemThe serum concentration of Tacrolimus can be increased when it is combined with Ertapenem.
ErythromycinThe serum concentration of Tacrolimus can be increased when it is combined with Erythromycin.
EsomeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Esomeprazole.
EstramustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Estramustine.
EtanerceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Etanercept.
EthanolEthanol can cause an increase in the absorption of Tacrolimus resulting in an increased serum concentration and potentially a worsening of adverse effects.
EtodolacEtodolac may increase the nephrotoxic activities of Tacrolimus.
EtoposideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Etoposide.
EverolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Everolimus.
FelodipineThe serum concentration of Tacrolimus can be increased when it is combined with Felodipine.
FenofibrateTacrolimus may increase the nephrotoxic activities of Fenofibrate.
FenoprofenFenoprofen may increase the nephrotoxic activities of Tacrolimus.
FingolimodThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fingolimod.
FloctafenineFloctafenine may increase the nephrotoxic activities of Tacrolimus.
FloxuridineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Floxuridine.
FluconazoleThe metabolism of Tacrolimus can be decreased when combined with Fluconazole.
FludarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludarabine.
FludrocortisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludrocortisone.
FluorouracilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fluorouracil.
FlurbiprofenFlurbiprofen may increase the nephrotoxic activities of Tacrolimus.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fluticasone Propionate.
FosamprenavirThe metabolism of Tacrolimus can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Tacrolimus can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the nephrotoxic activities of Tacrolimus.
FosphenytoinThe serum concentration of Tacrolimus can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Tacrolimus can be increased when it is combined with Fusidic Acid.
GemcitabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemcitabine.
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemtuzumab ozogamicin.
Glatiramer AcetateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Glatiramer Acetate.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Tacrolimus.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Tacrolimus.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Tacrolimus.
golimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with golimumab.
GoserelinTacrolimus may increase the QTc-prolonging activities of Goserelin.
HydrocortisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydrocortisone.
HydroxyureaThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydroxyurea.
IbritumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibrutinib.
IbuprofenIbuprofen may increase the nephrotoxic activities of Tacrolimus.
IdarubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Idarubicin.
IdelalisibThe serum concentration of Tacrolimus can be increased when it is combined with Idelalisib.
IfosfamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ifosfamide.
ImatinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imatinib.
ImiquimodThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imiquimod.
IndinavirThe metabolism of Tacrolimus can be decreased when combined with Indinavir.
IndomethacinIndomethacin may increase the nephrotoxic activities of Tacrolimus.
InfliximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Infliximab.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Tacrolimus.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Tacrolimus.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Tacrolimus.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Tacrolimus.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Tacrolimus.
Insulin RegularThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Tacrolimus.
Insulin, isophaneThe therapeutic efficacy of Insulin, isophane can be decreased when used in combination with Tacrolimus.
IrinotecanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Irinotecan.
IsoflurophateThe metabolism of Tacrolimus can be decreased when combined with Isoflurophate.
IsradipineThe serum concentration of Tacrolimus can be increased when it is combined with Isradipine.
ItraconazoleThe metabolism of Tacrolimus can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Tacrolimus can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Tacrolimus can be decreased when combined with Ketoconazole.
KetoprofenKetoprofen may increase the nephrotoxic activities of Tacrolimus.
KetorolacKetorolac may increase the nephrotoxic activities of Tacrolimus.
L-PhenylalanineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with L-Phenylalanine.
LansoprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Lansoprazole.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Tacrolimus.
LeflunomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Leflunomide.
LenalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lenalidomide.
LeuprolideTacrolimus may increase the QTc-prolonging activities of Leuprolide.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Tacrolimus.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Tacrolimus.
LomustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lomustine.
LopinavirThe metabolism of Tacrolimus can be decreased when combined with Lopinavir.
LuliconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Luliconazole.
MechlorethamineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mechlorethamine.
Mefenamic acidMefenamic acid may increase the nephrotoxic activities of Tacrolimus.
MeloxicamMeloxicam may increase the nephrotoxic activities of Tacrolimus.
MelphalanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Melphalan.
MercaptopurineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mercaptopurine.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Tacrolimus.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Tacrolimus.
MethotrexateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Methotrexate.
MethylprednisoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Methylprednisolone.
MifepristoneMifepristone may increase the QTc-prolonging activities of Tacrolimus.
MitomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitomycin.
MitotaneThe serum concentration of Tacrolimus can be decreased when it is combined with Mitotane.
MitoxantroneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitoxantrone.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolate mofetil.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolic acid.
NabumetoneNabumetone may increase the nephrotoxic activities of Tacrolimus.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Tacrolimus.
NaproxenNaproxen may increase the nephrotoxic activities of Tacrolimus.
NatalizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Natalizumab.
NefazodoneThe metabolism of Tacrolimus can be decreased when combined with Nefazodone.
NelarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nelarabine.
NelfinavirThe metabolism of Tacrolimus can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Tacrolimus can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Tacrolimus can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Tacrolimus can be increased when it is combined with Nifedipine.
NilotinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nilotinib.
NimodipineThe serum concentration of Tacrolimus can be increased when it is combined with Nimodipine.
NisoldipineThe serum concentration of Tacrolimus can be increased when it is combined with Nisoldipine.
ObinutuzumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Obinutuzumab.
OmeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Omeprazole.
OsimertinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Osimertinib.
OxaliplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Oxaliplatin.
OxaprozinOxaprozin may increase the nephrotoxic activities of Tacrolimus.
PaclitaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Paclitaxel.
PalbociclibThe serum concentration of Tacrolimus can be increased when it is combined with Palbociclib.
PanobinostatThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Panobinostat.
PantoprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Pantoprazole.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Tacrolimus.
PegaspargaseThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pegaspargase.
PemetrexedThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pemetrexed.
PentostatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pentostatin.
PhenytoinThe serum concentration of Tacrolimus can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tacrolimus.
PiroxicamPiroxicam may increase the nephrotoxic activities of Tacrolimus.
PomalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pomalidomide.
PosaconazoleThe metabolism of Tacrolimus can be decreased when combined with Posaconazole.
PralatrexateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pralatrexate.
PrednisoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisolone.
PrednisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisone.
ProcarbazineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Procarbazine.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Tacrolimus.
RabeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Rabeprazole.
RanolazineThe serum concentration of Tacrolimus can be increased when it is combined with Ranolazine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tacrolimus.
Repository corticotropinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Repository corticotropin.
RifabutinThe serum concentration of Tacrolimus can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Tacrolimus can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Tacrolimus can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Tacrolimus.
RilonaceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rilonacept.
RitonavirThe metabolism of Tacrolimus can be decreased when combined with Ritonavir.
RituximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rituximab.
RoflumilastRoflumilast may increase the immunosuppressive activities of Tacrolimus.
RuxolitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ruxolitinib.
SaquinavirThe metabolism of Tacrolimus can be decreased when combined with Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus.
SecukinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Secukinumab.
SevelamerThe serum concentration of Tacrolimus can be decreased when it is combined with Sevelamer.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Tacrolimus.
SiltuximabThe serum concentration of Tacrolimus can be decreased when it is combined with Siltuximab.
SimeprevirThe metabolism of Tacrolimus can be decreased when combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tacrolimus.
SirolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sirolimus.
SorafenibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sorafenib.
SpironolactoneSpironolactone may increase the hyperkalemic activities of Tacrolimus.
St. John's WortThe serum concentration of Tacrolimus can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Tacrolimus can be increased when it is combined with Stiripentol.
StreptozocinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Streptozocin.
SulfisoxazoleThe serum concentration of Tacrolimus can be increased when it is combined with Sulfisoxazole.
SulindacSulindac may increase the nephrotoxic activities of Tacrolimus.
SunitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sunitinib.
TelaprevirThe serum concentration of Tacrolimus can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Telithromycin.
TemozolomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Temozolomide.
TemsirolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Temsirolimus.
TeniposideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Teniposide.
TeriflunomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Teriflunomide.
TesmilifeneThe serum concentration of Tacrolimus can be decreased when it is combined with Tesmilifene.
ThalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thalidomide.
ThiotepaThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thiotepa.
Tiaprofenic acidTiaprofenic acid may increase the nephrotoxic activities of Tacrolimus.
TioguanineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tioguanine.
TipranavirThe metabolism of Tacrolimus can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Tacrolimus can be decreased when it is combined with Tocilizumab.
TofacitinibTacrolimus may increase the immunosuppressive activities of Tofacitinib.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Tacrolimus.
TolmetinTolmetin may increase the nephrotoxic activities of Tacrolimus.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Tacrolimus.
TositumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tositumomab.
TrabectedinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trabectedin.
TrastuzumabTrastuzumab may increase the neutropenic activities of Tacrolimus.
TretinoinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tretinoin.
TriamcinoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Triamcinolone.
TriamtereneTriamterene may increase the hyperkalemic activities of Tacrolimus.
UstekinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ustekinumab.
VedolizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vedolizumab.
VerapamilThe metabolism of Tacrolimus can be decreased when combined with Verapamil.
VilanterolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vilanterol.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Tacrolimus.
VinblastineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinblastine.
VincristineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vincristine.
VindesineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vindesine.
VinorelbineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinorelbine.
VoriconazoleThe metabolism of Tacrolimus can be decreased when combined with Voriconazole.

Food Interactions:
  • Food, especially food with a high-fat content, decreases the rate and extent of absorption.
  • The time of the meal affects tacrolimus bioavailability. Take tacrolimus capsules consistently everyday either with or without food.

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Alpha amino acid esters
  • Azacyclic compounds
  • Carboxylic acid esters
  • Cyclic alcohols and derivatives
  • Cyclic ketones
  • Cyclohexanols
  • Dialkyl ethers
  • Hemiacetals
  • Hydrocarbon derivatives
  • Lactams
  • Lactones
  • Macrolides and analogues
  • Monocarboxylic acids and derivatives
  • Oxacyclic compounds
  • Oxanes
  • Piperidines
  • Tertiary amines
  • Tertiary carboxylic acid amides

substituent:
  • Alcohol
  • Aliphatic heteropolycyclic compound
  • Alpha-amino acid ester
  • Amine
  • Azacycle
  • Carbonyl group
  • Carboxamide group
  • Carboxylic acid derivative
  • Carboxylic acid ester
  • Cyclic alcohol
  • Cyclic ketone
  • Cyclohexanol
  • Dialkyl ether
  • Ether
  • Hemiacetal
  • Hydrocarbon derivative
  • Ketone
  • Lactam
  • Lactone
  • Macrolide
  • Macrolide lactam
  • Monocarboxylic acid or derivatives
  • Organoheterocyclic compound
  • Organonitrogen compound
  • Organooxygen compound
  • Oxacycle
  • Oxane
  • Piperidine
  • Secondary alcohol
  • Tertiary amine
  • Tertiary carboxylic acid amide

References

Synthesis Reference: Pan Sup Chang, Hoon Cho, "Water soluble polymer-tacrolimus conjugated compounds and process for preparing the same." U.S. Patent US5922729, issued April, 1997.
General Reference: # Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, Kohsaka M, Aoki H, Imanaka H: FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1987 Sep;40(9):1249-55. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/2445721 # Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15896681 # Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, Schreiber SL: Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/1715244 # Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike F, Takada Y, Inui K: Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient. Drug Metab Pharmacokinet. 2006 Apr;21(2):122-5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16702731 # Hanifin JM, Paller AS, Eichenfield L, Clark RA, Korman N, Weinstein G, Caro I, Jaracz E, Rico MJ: Efficacy and safety of tacrolimus ointment treatment for up to 4 years in patients with atopic dermatitis. J Am Acad Dermatol. 2005 Aug;53(2 Suppl 2):S186-94. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16021174 # FDA label
External Links:
ResourceLink
RxListhttp://www.rxlist.com/cgi/generic2/tacrolimus.htm
Drugs.comhttp://www.drugs.com/cdi/tacrolimus.html

ATC Codes:
  • Array
  • Array

AHFS Codes:
  • 84:92.00
  • 92:00.00

MSDS: Download
SiteLock

© Copyright 2022 The Purple Society, Purple Gladiator, Trialsmap, The Purple Drug Guide, and One Person CAN Make A Difference! are all registered trademarks of The Purple Society. The Purple Society, a not-for-profit, section 501(c)(3) #273785281.

The Purple Society website is designed for educational purposes only and is not engaged in rendering medical advice or professional services. The information provided through this site should not be used for diagnosing or treating a health problem or a disease. It is not a substitute for professional care. If you have or suspect you may have a health problem, you should consult your health care provider.

CONTACT US

The Purple Society team is here for you 24 hours a day, 7 days a week. Send us an email and we'll get right back to you.

Sending
or

Log in with your credentials

Forgot your details?