Prograf, Protopic(tacrolimus)
Advagraf, Astagraf, Envarsus, Modigraf, Prograf, Protopic (tacrolimus) is a small molecule pharmaceutical. Tacrolimus was first approved as Prograf on 1994-04-08. It is used to treat atopic dermatitis and graft vs host disease in the USA. It has been approved in Europe to treat atopic dermatitis, graft rejection, kidney transplantation, and liver transplantation. The pharmaceutical is active against peptidyl-prolyl cis-trans isomerase FKBP1A.
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Commercial
Trade Name
FDA
EMA
Astagraf, Envarsus, Prograf, Protopic (generic drugs available since 2009-08-10)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Tacrolimus
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| PROGRAF | Astellas Pharma | N-050708 RX | 1994-04-08 | 3 products, RLD, RS |
| PROGRAF | Astellas Pharma | N-050709 RX | 1994-04-08 | 1 products, RLD, RS |
| ASTAGRAF XL | Astellas Pharma | N-204096 RX | 2013-07-19 | 3 products, RLD, RS |
| PROGRAF | Astellas Pharma | N-210115 RX | 2018-05-24 | 2 products, RLD, RS |
| PROTOPIC | LEO Pharma | N-050777 RX | 2000-12-08 | 2 products, RLD, RS |
| ENVARSUS XR | Veloxis Pharmaceuticals | N-206406 RX | 2015-07-10 | 3 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| astagraf xl | New Drug Application | 2020-12-01 |
| envarsus | New Drug Application | 2020-09-25 |
| prograf | New Drug Application | 2020-12-01 |
| protopic | New Drug Application | 2019-04-29 |
| tacrolimus | New Drug Application | 2021-11-15 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| atopic dermatitis | EFO_0000274 | D003876 | L20 |
| graft vs host disease | — | D006086 | D89.81 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
TACROLIMUS, PROGRAF, ASTELLAS | |||
| 2028-07-16 | ODE-360 | ||
| 2025-05-24 | ODE-269, ODE-294 | ||
TACROLIMUS, ASTAGRAF XL, ASTELLAS | |||
| 2025-05-24 | ODE* | ||
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Tacrolimus, Envarsus Xr, Veloxis Pharms Inc | |||
| 8664239 | 2028-08-30 | U-1752, U-2677, U-2678 | |
| 8685998 | 2028-08-30 | DP | U-1752, U-2677, U-2678 |
| 9549918 | 2028-05-30 | DP | |
| 10166190 | 2028-05-30 | DP | |
| 10864199 | 2028-05-30 | U-2677, U-2678 | |
| 11110081 | 2028-05-30 | U-2678 | |
| 11123331 | 2028-05-30 | U-2677 | |
| 11419823 | 2028-05-30 | DP | |
| 7994214 | 2024-08-30 | DP | |
| 8486993 | 2024-08-30 | DP | U-1752 |
| 8586084 | 2024-08-30 | U-1752 | |
| 8591946 | 2024-08-30 | DP | |
| 8617599 | 2024-08-30 | DP | |
| 8623410 | 2024-08-30 | DP | |
| 8623411 | 2024-08-30 | U-1752 | |
| 8889185 | 2024-08-30 | U-1752 | |
| 8889186 | 2024-08-30 | U-1752 | |
| 9161907 | 2024-08-30 | DP | U-1752 |
| 9757362 | 2024-08-30 | DP | |
| 9763920 | 2024-08-30 | DP | |
| 10548880 | 2024-08-30 | U-2677, U-2678 | |
| 11077096 | 2024-08-30 | DP | |
ATC Codes
D: Dermatologicals
— D11: Other dermatological preparations in atc
— D11A: Other dermatological preparations in atc
— D11AH: Agents for dermatitis, excluding corticosteroids
— D11AH01: Tacrolimus
L: Antineoplastic and immunomodulating agents
— L04: Immunosuppressants
— L04A: Immunosuppressants
— L04AD: Calcineurin inhibitors
— L04AD02: Tacrolimus
Clinical
Clinical Trials
993 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Kidney transplantation | D016030 | 4 | 27 | 25 | 67 | 12 | 129 | ||
| Liver transplantation | D016031 | EFO_0010682 | 1 | 13 | 19 | 27 | 10 | 69 | |
| Graft vs host disease | D006086 | D89.81 | 16 | 50 | 7 | 2 | 2 | 64 | |
| Renal insufficiency | D051437 | HP_0000083 | N19 | 5 | 8 | 10 | 12 | 3 | 35 |
| Atopic dermatitis | D003876 | EFO_0000274 | L20 | 2 | 6 | 10 | 13 | 2 | 33 |
| Chronic kidney failure | D007676 | EFO_0003884 | N18.6 | 3 | 6 | 4 | 14 | 4 | 28 |
| Immunosuppression therapy | D007165 | 2 | 2 | 2 | 14 | 8 | 28 | ||
| Lupus nephritis | D008181 | EFO_0005761 | 1 | 1 | 7 | 5 | 5 | 19 | |
| Heart transplantation | D016027 | EFO_0010673 | — | 6 | 3 | 3 | 1 | 13 | |
| Kidney diseases | D007674 | EFO_0003086 | N08 | 3 | 5 | 4 | 4 | — | 13 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Myelodysplastic syndromes | D009190 | D46 | 29 | 89 | 7 | — | 6 | 119 | |
| Myeloid leukemia acute | D015470 | C92.0 | 18 | 60 | 7 | — | 3 | 79 | |
| Leukemia | D007938 | C95 | 22 | 54 | 2 | — | 3 | 72 | |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | C91.0 | 11 | 51 | 6 | — | 2 | 65 | |
| Lymphoma | D008223 | C85.9 | 14 | 43 | 2 | — | 4 | 59 | |
| Non-hodgkin lymphoma | D008228 | C85.9 | 10 | 35 | 3 | — | — | 44 | |
| Bcr-abl positive chronic myelogenous leukemia | D015464 | EFO_0000340 | 8 | 38 | 4 | — | — | 44 | |
| Multiple myeloma | D009101 | C90.0 | 13 | 30 | 1 | — | 1 | 40 | |
| Hodgkin disease | D006689 | C81 | 7 | 31 | 2 | — | — | 38 | |
| B-cell chronic lymphocytic leukemia | D015451 | C91.1 | 6 | 30 | 2 | — | — | 36 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Plasma cell neoplasms | D054219 | 8 | 23 | — | — | 3 | 32 | ||
| Hematologic neoplasms | D019337 | 12 | 20 | — | — | 1 | 25 | ||
| Myelomonocytic leukemia chronic | D015477 | C93.1 | 3 | 17 | — | — | — | 19 | |
| Follicular lymphoma | D008224 | C82 | 2 | 16 | — | — | — | 17 | |
| Mantle-cell lymphoma | D020522 | C83.1 | 3 | 16 | — | — | — | 17 | |
| Large b-cell lymphoma diffuse | D016403 | C83.3 | 3 | 15 | — | — | — | 16 | |
| Aplastic anemia | D000741 | HP_0001915 | D61.9 | 1 | 15 | — | — | — | 16 |
| Myelodysplastic-myeloproliferative diseases | D054437 | 4 | 14 | — | — | — | 16 | ||
| Myeloid leukemia chronic-phase | D015466 | 4 | 13 | — | — | — | 15 | ||
| Waldenstrom macroglobulinemia | D008258 | C88.0 | 1 | 12 | — | — | — | 12 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | 17 | — | — | — | 4 | 21 | ||
| Organ transplantation | D016377 | 2 | — | — | — | — | 2 | ||
| Venous thromboembolism | D054556 | EFO_0004286 | I74 | 1 | — | — | — | — | 1 |
| Homologous transplantation | D014184 | 1 | — | — | — | — | 1 | ||
| Peripheral blood stem cell transplantation | D036102 | 1 | — | — | — | — | 1 | ||
| Brain neoplasms | D001932 | EFO_0003833 | C71 | 1 | — | — | — | — | 1 |
| Glioma | D005910 | EFO_0000520 | 1 | — | — | — | — | 1 | |
| Germ cell and embryonal neoplasms | D009373 | 1 | — | — | — | — | 1 | ||
| Medulloblastoma | D008527 | 1 | — | — | — | — | 1 | ||
| Ependymoma | D004806 | 1 | — | — | — | — | 1 |
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Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Heart disease risk factors | D000082742 | — | — | — | — | 1 | 1 | ||
| Bone diseases | D001847 | M89.9 | — | — | — | — | 1 | 1 | |
| Death | D003643 | PATO_0001422 | — | — | — | — | 1 | 1 | |
| Antibody formation | D000917 | — | — | — | — | 1 | 1 | ||
| Delirium | D003693 | R41.0 | — | — | — | — | 1 | 1 | |
| Corneal transplantation | D016039 | EFO_0010676 | — | — | — | — | 1 | 1 | |
| Herpesviridae infections | D006566 | EFO_0007309 | B00.4 | — | — | — | — | 1 | 1 |
| Viremia | D014766 | B34.9 | — | — | — | — | 1 | 1 | |
| Plasmapheresis | D010956 | — | — | — | — | 1 | 1 | ||
| Immune reconstitution | D000074243 | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | TACROLIMUS |
| INN | tacrolimus |
| Description | Tacrolimus (anhydrous) is a macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. It has a role as an immunosuppressive agent and a bacterial metabolite. |
| Classification | Small molecule |
| Drug class | immunosuppressives |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC.O |
Identifiers
| PDB | — |
| CAS-ID | 104987-11-3 |
| RxCUI | 235991 |
| ChEMBL ID | CHEMBL3989887 |
| ChEBI ID | — |
| PubChem CID | 445643 |
| DrugBank | DB00864 |
| UNII ID | Y5L2157C4J (ChemIDplus, GSRS) |
Target
Agency Approved
FKBP1A
FKBP1A
Organism
Homo sapiens
Gene name
FKBP1A
Gene synonyms
FKBP1, FKBP12
NCBI Gene ID
Protein name
peptidyl-prolyl cis-trans isomerase FKBP1A
Protein synonyms
12 kDa FK506-binding protein, 12 kDa FKBP, Calstabin-1, FK506 binding protein 1A, 12kDa, FK506 binding protein12, FK506-binding protein 1, FK506-binding protein 12, FK506-binding protein 1A, FK506-binding protein, T-cell, 12-kD, FKBP-12, FKBP-1A, FKBP12-Exip3, Immunophilin FKBP12, PPIase FKBP1A, protein kinase C inhibitor 2, Rotamase
Uniprot ID
Mouse ortholog
Fkbp1a (14225)
peptidyl-prolyl cis-trans isomerase FKBP1A (Q545E9)
Alternate
No data
Variants
Clinical Variant
Identifier | Target mutation | Effect | Evaluation | Status |
|---|---|---|---|---|
| VCV002502287 | CYP3A4, 1026+12G>A | drug response | 2023-01-20 | 2A |
| VCV001327418 | CYP3A4, 671-202C>T | drug response | 2021-03-24 | 2A |
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
Black-box warning for: Astagraf xl, Envarsus, Prograf
Adverse Events
Top Adverse Reactions
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2,961 adverse events reported
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