Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Tacrolimus
Drug ID BADD_D02105
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 inhibits calcineurin which inhibits T-lymphocyte signal transduction and IL-2 transcription.
Indications and Usage 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.
Marketing Status Prescription; Discontinued
ATC Code D11AH01; L04AD02
DrugBank ID DB00864
KEGG ID D00107
MeSH ID D016559
PubChem ID 445643
TTD Drug ID D06OMK
NDC Product Code 16729-041; 0781-2104; 70748-219; 52972-0040; 0168-0416; 70748-220; 70377-014; 16729-043; 43353-317; 68254-0002; 49629-022; 0469-1330; 68084-450; 49629-020; 70518-3022; 68462-534; 69452-153; 55111-527; 55111-525; 47848-018; 16714-098; 65897-1010; 38779-2698; 62250-665; 68084-449; 52928-006; 0904-6623; 50222-211; 49629-021; 68992-3075; 45802-700; 43817-423; 63629-8726; 70748-221; 68254-5005; 68462-685; 0781-2103; 69452-154; 50090-2245; 69452-155; 0469-3016; 54288-135; 0904-7097; 0904-6425; 68254-0020; 0378-2047; 73377-010; 60429-378; 50090-5596; 65050-0321; 50222-203; 0781-2102; 16729-042; 68084-451; 0168-0417; 0378-2045; 63629-8725; 0904-6624; 55154-4080; 55486-1576; 45802-390; 51927-0092; 0469-0607; 68308-703; 68254-5004; 60429-377; 68462-686; 64380-721; 0469-0617; 0378-2046; 62991-3072; 67877-278; 43817-421; 64380-720; 51079-028; 64380-722; 70518-3216; 51079-818; 68254-2502; 51187-0006; 55111-526; 70377-015; 70518-2996; 67877-279; 0469-1230; 68254-5006; 65727-009; 0469-0657; 70377-016; 70518-2593; 16729-422; 51079-817; 60429-379; 16729-421; 68992-3040; 16714-100; 70518-2124; 63629-8723; 72572-761; 67877-280; 55500-0010; 50090-5581; 68992-3010; 51552-1403; 72572-760; 16714-099; 68462-687; 82160-124; 70518-3388; 43817-422; 52076-6222
Synonyms Tacrolimus | Prograf | Prograft | FR-900506 | FR 900506 | FR900506 | Anhydrous Tacrolimus | Tacrolimus, Anhydrous | Tacrolimus Anhydrous | Anhydrous, Tacrolimus | FK-506 | FK 506 | FK506
Chemical Information
Molecular Formula C44H69NO12
CAS Registry Number 104987-11-3
SMILES CC1CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC(=O)C(C=C(C1)C)CC=C)O)C)C(=CC 4CCC(C(C4)OC)O)C)O)C)OC)OC
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Nephropathy toxicCalcineurin subunit B type 1P63098Not Available8591053; 7694398; 7592869; 7533090
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Altered state of consciousness19.07.01.003; 17.02.04.0010.005678%Not Available
Alveolar proteinosis22.01.02.0090.002037%Not Available
Amblyopia06.02.01.001--Not Available
Amnesia19.20.01.001; 17.03.02.001--
Amylase increased13.05.01.009--
Amyloidosis10.02.05.0010.000555%Not Available
Anaemia01.03.02.001--
Anaphylactic reaction24.06.03.006; 10.01.07.0010.014904%
Anaphylactic shock24.06.02.004; 10.01.07.002--Not Available
Anaphylactoid reaction10.01.07.003; 24.06.03.0070.002129%Not Available
Angina pectoris24.04.04.002; 02.02.02.002--
Angioedema23.04.01.001; 10.01.05.0090.019871%Not Available
Ankle fracture15.08.03.005; 12.04.01.005--
Anorectal disorder07.03.01.001--Not Available
Anuria20.01.03.0020.009226%Not Available
Anxiety19.06.02.002--
Aortic dissection24.02.03.0020.000370%Not Available
Aortic stenosis24.04.01.0010.005678%Not Available
Aphasia19.21.01.001; 17.02.03.0010.011355%
Aphthous ulcer07.05.06.002--Not Available
Aplasia pure red cell10.02.01.003; 01.03.03.0010.003548%Not Available
Apnoea22.02.01.0010.003548%
Appendicitis11.01.07.001; 07.19.01.0010.001419%
Application site erythema23.03.06.005; 12.07.01.001; 08.02.01.001--Not Available
Application site irritation12.07.01.003; 08.02.01.003--Not Available
Application site oedema08.02.01.020; 12.07.01.020--Not Available
Application site pain12.07.01.004; 08.02.01.004--Not Available
Application site pruritus23.03.12.004; 12.07.01.005; 08.02.01.005--Not Available
Application site rash12.07.01.016; 08.02.01.016; 23.03.13.008--Not Available
Application site warmth12.07.01.029; 08.02.01.029--Not Available
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