Tacrolimus Anhydrous
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Also known as Anhydrous tacrolimusFujimycinPrographTacroTacrolimusanhydrousTsukubaenolideENVARSUSVIVADEXPERIXISCAPEXIONTACROLIMUS HYDRATEADOPORTTACNIMODIGRAFADVAGRAFFK5MOLECULAR-GLUEFK-506
Summary
Tacrolimus Anhydrous (CHEMBL269732) is an approved small-molecule immunosuppressive agent targeting FKBP1A and TRPM8; indicated across 131 conditions including hepatocellular carcinoma and hodgkins lymphoma.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- Targets: 2 (FKBP1A, TRPM8)
- Indications: 131 conditions
- Clinical trials: 891
- Chemistry: 804 Da · C44H69NO12
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL269732 |
| Name | Tacrolimus Anhydrous |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 445643 |
| ChEBI | CHEBI:61049 |
| Molecular formula | C44H69NO12 |
| Molecular weight | 804 |
| InChIKey | QJJXYPPXXYFBGM-LFZNUXCKSA-N |
SMILES: C[C@@H]1C[C@@H]([C@@H]2[C@H](C[C@H]([C@@](O2)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@@H]([C@@H]([C@H](CC(=O)[C@@H](/C=C(/C1)\C)CC=C)O)C)/C(=C/[C@@H]4CC[C@H]([C@@H](C4)OC)O)/C)O)C)OC)OC
IUPAC name: (1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
ChEBI definition: 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.
Pharmacological roles (ChEBI): immunosuppressive agent.
Other ChEBI roles (chemical / environmental): bacterial metabolite.
Also known as: Anhydrous tacrolimus, Fujimycin, Prograph, Tacro, Tacrolimus anhydrous, Tacrolimus, anhydrous, Tsukubaenolide, ENVARSUS, VIVADEX, PERIXIS, CAPEXION
Parent form; salt/anhydrous children: CHEMBL3989887
Patent coverage: 23,926 distinct patent families (95,168 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| FKBP1A | FKBP prolyl isomerase 1A | Inhibition | 9.4 | 21.5% | P62942 |
| TRPM8 | TRPM8 | Agonist | 4.85 | 0.5% | Q7Z2W7 |
Broader ChEMBL bioactivity targets: 27 (assay-derived). Sample: Splicing factor 3B subunit 3, Nuclear receptor ROR-gamma, Ferritin light chain, Solute carrier organic anion transporter family member 1B1, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Peptidyl-prolyl cis-trans isomerase FKBP1A, Sodium channel protein type 5 subunit alpha, Equilibrative nucleoside transporter 1, Peptidyl-prolyl cis-trans isomerase FKBP5.
Bioactivity
ChEMBL activities: 45 potent at pChembl ≥ 5 of 60 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| FKBP1A | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_1194515 |
| FKBP1A | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_188123 |
| FKBP1A | 9.7 | Kd | 0.2 | nM | CHEMBL_ACT_26165917 |
| FKBP1A | 9.4 | Ki | 0.4 | nM | CHEMBL_ACT_1007850 |
| FKBP1B | 9.4 | Kd | 0.4 | nM | CHEMBL_ACT_15049580 |
| FKBP1A | 9.4 | Kd | 0.4 | nM | CHEMBL_ACT_25072940 |
| FKBP1A | 9.05 | EC50 | 0.9 | nM | CHEMBL_ACT_378184 |
| MTOR | 9.02 | IC50 | 0.95 | nM | CHEMBL_ACT_1468060 |
| FKBP1B | 8.83 | Kd | 1.49 | nM | CHEMBL_ACT_26165920 |
| FKBP1A | 8.77 | Ki | 1.7 | nM | CHEMBL_ACT_25848558 |
| FKBP1A | 8.64 | IC50 | 2.3 | nM | CHEMBL_ACT_1086804 |
| FKBP1A | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_724502 |
| MTOR | 8.5 | IC50 | 3.16 | nM | CHEMBL_ACT_873240 |
| SF3B3 | 7.96 | IC50 | 10.9 | nM | CHEMBL_ACT_3441240 |
| SF3B3 | 7.86 | IC50 | 13.8 | nM | CHEMBL_ACT_3441228 |
| FKBP1A | 7.85 | IC50 | 14.05 | nM | CHEMBL_ACT_18083828 |
| PPP3CA | 7.83 | IC50 | 14.8 | nM | CHEMBL_ACT_378185 |
| PPP3CA | 7.7 | Kd | 20 | nM | CHEMBL_ACT_188124 |
| FKBP4 | 7.64 | Kd | 23 | nM | CHEMBL_ACT_25072935 |
| FKBP5 | 7.12 | Kd | 75.93 | nM | CHEMBL_ACT_26165923 |
| FKBP5 | 7.1 | Ki | 80 | nM | CHEMBL_ACT_12726905 |
| FKBP5 | 7.1 | Ki | 79 | nM | CHEMBL_ACT_16556235 |
| FKBP5 | 7.03 | Ki | 93 | nM | CHEMBL_ACT_25072933 |
| FKBP5 | 6.98 | Kd | 104 | nM | CHEMBL_ACT_25072929 |
| CYP3A4 | 6.92 | IC50 | 120 | nM | CHEMBL_ACT_15464653 |
| CYP3A5 | 6.85 | IC50 | 140 | nM | CHEMBL_ACT_15464659 |
| FKBP4 | 6.83 | Kd | 149.7 | nM | CHEMBL_ACT_26165926 |
| CYP3A4 | 6.44 | Ki | 360 | nM | CHEMBL_ACT_15464649 |
| CYP3A4 | 6.21 | IC50 | 620 | nM | CHEMBL_ACT_15464654 |
| CYP3A4 | 6.21 | Ki | 610 | nM | CHEMBL_ACT_15464661 |
Target pathways
Aggregated over 2 target gene(s): FKBP1A, TRPM8.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| mTORC1-mediated signalling | 1 | FKBP1A |
| Calcineurin activates NFAT | 1 | FKBP1A |
| TGF-beta receptor signaling activates SMADs | 1 | FKBP1A |
| TGF-beta receptor signaling in EMT (epithelial to mesenchymal transition) | 1 | FKBP1A |
| TRP channels | 1 | TRPM8 |
| TGFBR1 LBD Mutants in Cancer | 1 | FKBP1A |
| Potential therapeutics for SARS | 1 | FKBP1A |
| SARS-CoV-1 activates/modulates innate immune responses | 1 | FKBP1A |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| heart morphogenesis | 1 |
| protein folding | 1 |
| ‘de novo’ protein folding | 1 |
| regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ion | 1 |
| regulation of skeletal muscle contraction by regulation of release of sequestered calcium ion | 1 |
| negative regulation of transforming growth factor beta receptor signaling pathway | 1 |
| regulation of protein localization | 1 |
| negative regulation of activin receptor signaling pathway | 1 |
| protein refolding | 1 |
| T cell activation | 1 |
| positive regulation of canonical NF-kappaB signal transduction | 1 |
| regulation of immune response | 1 |
| protein maturation | 1 |
| ventricular cardiac muscle tissue morphogenesis | 1 |
| heart trabecula formation | 1 |
Indications & clinical
Indications
131 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| Hodgkins lymphoma | 3 | MONDO:0004952 | EFO:0000183 |
| atopic eczema | 3 | MONDO:0004980 | EFO:0000274 |
| infertility disorder | 3 | MONDO:0005047 | EFO:0000545 |
| injury | 3 | MONDO:0021178 | EFO:0000546 |
| psoriasis | 3 | MONDO:0005083 | EFO:0000676 |
| rheumatoid arthritis | 3 | MONDO:0008383 | EFO:0000685 |
| ulcerative colitis | 3 | MONDO:0005101 | EFO:0000729 |
| kidney disorder | 3 | MONDO:0005240 | EFO:0003086 |
| heart disorder | 3 | MONDO:0005267 | EFO:0003777 |
| chronic kidney disease | 3 | MONDO:0005300 | EFO:0003884 |
| vitiligo | 3 | MONDO:0008661 | EFO:0004208 |
| nephrotic syndrome | 3 | MONDO:0005377 | EFO:0004255 |
| graft versus host disease | 3 | MONDO:0013730 | EFO:0004599 |
| myasthenia gravis | 3 | MONDO:0009688 | EFO:0004991 |
| lupus nephritis | 3 | MONDO:0005556 | EFO:0005761 |
| non-Hodgkin lymphoma | 3 | MONDO:0018908 | EFO:0005952 |
| bronchiolitis obliterans syndrome | 3 | MONDO:0015265 | EFO:0007183 |
| seborrheic dermatitis | 3 | MONDO:0006608 | EFO:1000764 |
| membranous glomerulonephritis | 3 | MONDO:0005376 | EFO:0004254 |
| kidney failure | 3 | MONDO:0001106 | EFO:1002048 |
| skin neoplasm | 3 | MONDO:0002531 | MONDO:0002898 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| acute pancreatitis | 3 | MONDO:0006515 | EFO:1000652 |
| type 1 diabetes mellitus | 3 | MONDO:0005147 | MONDO:0005147 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| myelodysplastic syndrome | 2 | MONDO:0018881 | EFO:0000198 |
| acute lymphoblastic leukemia | 2 | MONDO:0004967 | EFO:0000220 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| chronic myeloid leukemia | 2 | MONDO:0011996 | EFO:0000339 |
| Crohn disease | 2 | MONDO:0005011 | EFO:0000384 |
| diabetes mellitus | 2 | MONDO:0005015 | EFO:0000400 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| leukemia | 2 | MONDO:0005059 | EFO:0000565 |
| lymphoma | 2 | MONDO:0005062 | EFO:0000574 |
| neoplasm | 2 | MONDO:0005070 | EFO:0000616 |
| neuroblastoma | 2 | MONDO:0005072 | EFO:0000621 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| systemic sclerosis | 2 | MONDO:0005100 | EFO:0000717 |
| pulmonary arterial hypertension | 2 | MONDO:0015924 | EFO:0001361 |
| age-related macular degeneration | 2 | MONDO:0005150 | EFO:0001365 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| liver disorder | 2 | MONDO:0005154 | EFO:0001421 |
| encephalomyelitis | 2 | MONDO:0005156 | EFO:0001423 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| primary myelofibrosis | 2 | MONDO:0009692 | EFO:0002430 |
| hepatitis C virus infection | 2 | MONDO:0005231 | EFO:0003047 |
| lung disorder | 2 | MONDO:0005275 | EFO:0003818 |
| cutaneous lupus erythematosus | 2 | MONDO:0005282 | EFO:0003834 |
| colitis | 2 | MONDO:0005292 | EFO:0003872 |
| IgA glomerulonephritis | 2 | MONDO:0005342 | EFO:0004194 |
| chronic hepatitis C virus infection | 2 | MONDO:0005354 | EFO:0004220 |
| focal segmental glomerulosclerosis | 2 | MONDO:0100313 | EFO:0004236 |
| autoimmune hepatitis | 2 | MONDO:0016264 | EFO:0005676 |
| aplastic anemia | 2 | MONDO:0015909 | EFO:0006927 |
| atopic conjunctivitis | 2 | MONDO:0005642 | EFO:0007141 |
| juvenile myelomonocytic leukemia | 2 | MONDO:0011908 | EFO:1000309 |
| vulvar lichen sclerosus | 2 | MONDO:0006491 | EFO:1000623 |
| epidermolysis bullosa | 2 | MONDO:0006541 | EFO:1000690 |
| Sezary syndrome | 2 | MONDO:0017844 | EFO:1000785 |
| mycosis fungoides | 2 | MONDO:0009691 | EFO:1001051 |
| mantle cell lymphoma | 2 | MONDO:0018876 | EFO:1001469 |
| peripheral T-cell lymphoma, not otherwise specified | 2 | MONDO:0004964 | EFO:0000211 |
| angioimmunoblastic T-cell lymphoma | 2 | MONDO:0004977 | EFO:0000255 |
| Burkitt lymphoma | 2 | MONDO:0007243 | EFO:0000309 |
| acquired polycythemia vera | 2 | MONDO:0009891 | EFO:0002429 |
| anaplastic large cell lymphoma | 2 | MONDO:0020325 | EFO:0003032 |
| lichen planus, oral | 2 | MONDO:0043923 | EFO:0008517 |
| Waldenstrom macroglobulinemia | 2 | MONDO:0100280 | EFO:0009441 |
| Langerhans cell histiocytosis | 2 | MONDO:0018310 | EFO:1000318 |
| chronic myelomonocytic leukemia | 2 | MONDO:0020311 | EFO:1001779 |
| myeloproliferative neoplasm | 2 | MONDO:0020076 | EFO:0002428 |
| kidney cancer | 2 | MONDO:0002367 | MONDO:0002367 |
| follicular lymphoma | 2 | MONDO:0018906 | MONDO:0018906 |
| nasal cavity and paranasal sinus lethal midline granuloma | 2 | MONDO:0006828 | MONDO:0019472 |
| hematopoietic and lymphoid system neoplasm | 2 | MONDO:0002334 | MONDO:0044881 |
| autoimmune thrombocytopenic purpura | 2 | MONDO:0008558 | EFO:0007160 |
| minimal change disease | 2 | MONDO:0006835 | EFO:1001020 |
| myelodysplastic/myeloproliferative disease | 2 | MONDO:0020077 | MONDO:0020077 |
| MALT lymphoma | 2 | MONDO:0007650 | EFO:0000191 |
| ischemia reperfusion injury | 2 | MONDO:0005203 | EFO:0002687 |
| amyotrophic lateral sclerosis | 2 | MONDO:0004976 | MONDO:0004976 |
| asthma | 2 | MONDO:0004979 | MONDO:0004979 |
| multiple sclerosis | 2 | MONDO:0005301 | MONDO:0005301 |
| Wiskott-Aldrich syndrome | 2 | MONDO:0010518 | MONDO:0010518 |
| sickle cell disease | 2 | MONDO:0011382 | MONDO:0011382 |
| Diamond-Blackfan anemia | 2 | MONDO:0015253 | MONDO:0015253 |
| severe combined immunodeficiency | 2 | MONDO:0015974 | MONDO:0015974 |
| lymphedema | 2 | MONDO:0019297 | MONDO:0019297 |
| Sjogren syndrome | 2 | MONDO:0010030 | EFO:0000699 |
| skin disorder | 2 | MONDO:0005093 | EFO:0000701 |
| hemoglobinuria | 2 | MONDO:0003656 | MONDO:0100244 |
| plasma cell neoplasm | 2 | MONDO:0004959 | EFO:0000200 |
| liver failure | 2 | MONDO:0100192 | MONDO:0100192 |
| reproductive system disorder | 1 | MONDO:0005039 | EFO:0000512 |
| venous thromboembolism | 1 | MONDO:0005399 | EFO:0004286 |
| plasma cell leukemia | 1 | MONDO:0018689 | EFO:0006475 |
| aspergillosis | 1 | MONDO:0005657 | EFO:0007157 |
| acute kidney tubular necrosis | 1 | MONDO:0006637 | EFO:1000794 |
| scleroderma | 1 | MONDO:0019340 | EFO:1001993 |
| beta thalassemia | 1 | MONDO:0019402 | Orphanet:848 |
| vasculitis | 1 | MONDO:0018882 | EFO:0006803 |
| blast phase chronic myelogenous leukemia, BCR-ABL1 positive | 1 | MONDO:0006115 | EFO:1000131 |
| respiratory syncytial virus infectious disease | 1 | MONDO:0001577 | EFO:1001413 |
| hematologic disorder | 1 | MONDO:0005570 | EFO:0005803 |
| alopecia | 1 | MONDO:0004907 | MONDO:0004907 |
| DiGeorge syndrome | 1 | MONDO:0008564 | MONDO:0018923 |
| alopecia areata | 1 | MONDO:0005340 | EFO:0004192 |
| lymphoid leukemia | 1 | MONDO:0005402 | EFO:0004289 |
| myeloid leukemia | 1 | MONDO:0004643 | MONDO:0004643 |
| neuroepithelial neoplasm | 0 | MONDO:0021193 | MONDO:0021193 |
20 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 891.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 292 |
| PHASE4 | 213 |
| PHASE3 | 118 |
| Not specified | 94 |
| PHASE1 | 84 |
| PHASE1/PHASE2 | 55 |
| PHASE2/PHASE3 | 24 |
| EARLY_PHASE1 | 11 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02081755 | PHASE4 | ENROLLING_BY_INVITATION | Safety and Efficacy of Everolimus Treatment in Liver Transplantation for Liver Cancer |
| NCT03266393 | PHASE4 | ACTIVE_NOT_RECRUITING | Envarsus XR® in Adolescent Renal Transplant Recipients |
| NCT04720326 | PHASE4 | ACTIVE_NOT_RECRUITING | Bioavailability and Practicability of Envarsus Versus Advagraf in Liver Transplant Recipients |
| NCT05089604 | PHASE4 | RECRUITING | Tacrolimus Associated Tremors in Liver Transplantation: Immediate-Release Versus Extended-Release Formulations |
| NCT05242315 | PHASE4 | RECRUITING | Extended-Release Tacrolimus Following Liver Transplantation |
| NCT05655273 | PHASE4 | ENROLLING_BY_INVITATION | Conversion of Maintenance Prograf to Envarsus in Liver Transplant Recipients |
| NCT05916781 | PHASE4 | RECRUITING | Effectiveness of Mycophenolate Mofetil Combined With Tacrolimus for Steroid Tapering in Systemic Lupus Erythematosus |
| NCT06147648 | PHASE4 | NOT_YET_RECRUITING | Early Conversion of Prolonged-release Tacrolimus in Liver Transplantation. |
| NCT06203470 | PHASE4 | NOT_YET_RECRUITING | Botox Versus Tacrolimus in Psoriasis Vulgaris |
| NCT06268769 | PHASE4 | RECRUITING | Tacrolimus C:D Ratio Measured in Renal Transplant Recipients Treated With Once-daily Prolonged-release Drugs |
| NCT06529536 | PHASE4 | RECRUITING | Utilising Genotype Informed Bayesian Dosing of Tacrolimus in Children Post Solid Organ Transplantation. |
| NCT06701825 | PHASE4 | RECRUITING | Effectiveness and Cost-effectiveness of a Pre-emptive Genotyping Strategy in Patients Receiving Tacrolimus |
| NCT07352566 | PHASE4 | NOT_YET_RECRUITING | Utilization of a Microdevice for Psoriasis and Atopic Dermatitis |
| NCT07437534 | PHASE4 | NOT_YET_RECRUITING | Comparative Evaluation of the Safety and Effectiveness of Crisaborole Ointment (2%) Versus Tacrolimus Ointment (0.1%) for the Topical Treatment of Atopic Dermatitis |
| NCT00087581 | PHASE4 | COMPLETED | Study of Therapeutic Monitoring of Mycophenolate Mofetil (MMF/CellCept) After Kidney Transplantation |
| NCT00106392 | PHASE4 | COMPLETED | A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy |
| NCT00113269 | PHASE4 | COMPLETED | Safety/Efficacy of Induction Agents With Tacrolimus, MMF, and Rapid Steroid Withdrawal in Renal Transplant Recipients |
| NCT00118742 | PHASE4 | COMPLETED | Liver Spare the Nephron (STN) Study - A Study of CellCept (Mycophenolate Mofetil) and Sirolimus in Recipients of a Liver Transplant |
| NCT00125307 | PHASE4 | COMPLETED | Tacrolimus for the Treatment of Systemic Lupus Erythematosus With Membranous Nephritis |
| NCT00133172 | PHASE4 | TERMINATED | Effect of Rapid Steroid Withdrawal on Subclinical Markers of Rejection |
| NCT00149994 | PHASE4 | COMPLETED | Cyclosporine A C-2h Monitoring Versus Tacrolimus C-0h Monitoring in de Novo Liver Transplant Recipients |
| NCT00160966 | PHASE4 | COMPLETED | Impact of Immunosuppressive Regimens on Polyomavirus-related Transplant Nephropathy |
| NCT00163657 | PHASE4 | COMPLETED | Study of Liver Transplant For End-Stage Liver Disease Caused By Chronic Hepatitis C Infection |
| NCT00166712 | PHASE4 | TERMINATED | A Trial of Two Steroid-Free Approaches Toward Mycophenolate Mofetil-Based Monotherapy Immunosuppression |
| NCT00166816 | PHASE4 | UNKNOWN | The Pharmacokinetics of Sirolimus When Combined With Cyclosporine or Tacrolimus in Renal Transplant Patients |
| NCT00166829 | PHASE4 | UNKNOWN | The Effect of Sirolimus on the Pharmacokinetics of Tacrolimus |
| NCT00166842 | PHASE4 | UNKNOWN | Sirolimus Blood Concentrations on Conversion From Oral Solution to Tablets |
| NCT00171496 | PHASE4 | COMPLETED | Evaluation of Cyclosporine Microemulsion and Tacrolimus on the Rate of New Onset Diabetes Mellitus in Kidney Transplantation Recipients |
| NCT00177138 | PHASE4 | TERMINATED | Use of Campath for Induction and Maintenance Therapy in Pancreas After Kidney Transplantation |
| NCT00182559 | PHASE4 | COMPLETED | The Vienna Prograf and Endothelial Progenitor Cell Study |
| NCT00195429 | PHASE4 | COMPLETED | A Study Comparing the Withdrawal of Steroids or Tacrolimus in Kidney Transplant Recipients |
| NCT00195988 | PHASE4 | COMPLETED | Comparison of Immunosuppression Protocols After LTx in Children |
| NCT00204191 | PHASE4 | UNKNOWN | Comparison of the Two Immunosuppressive Regimens Based on Tacrolimus and Cyclosporine Following Kidney Transplantation |
| NCT00223015 | PHASE4 | COMPLETED | Investigation of the Steady State Pharmacokinetics of Tacrolimus, Mycophenolate Mofetil and Fluvastatin After Renal Transplantation |
| NCT00229138 | PHASE4 | COMPLETED | Efficacy and Safety of Enteric-Coated Mycophenolate Sodium (EC-MPS) in Kidney Transplant Recipients |
| NCT00252655 | PHASE4 | UNKNOWN | Use of Sirolimus vs. Tacrolimus For African-American Renal Transplant Recipients |
| NCT00260208 | PHASE4 | TERMINATED | Liver Fibrosis in Patients Transplanted for Hepatitis C Receiving Either Cyclosporine Microemulsion or Tacrolimus |
| NCT00261820 | PHASE4 | COMPLETED | Study Comparing Two Immunosuppressive Regimens in De Novo Renal Allograft Recipients |
| NCT00275535 | PHASE4 | COMPLETED | The Comparison of Tacrolimus and Sirolimus Immunosuppression Based Drug Regimens in Kidney Transplant Recipients |
| NCT00290069 | PHASE4 | UNKNOWN | Renal Function Optimization With Mycophenolate Mofetil (MMF) Immunosuppressor Regimes (ALHAMBRA) |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
PharmGKB dosing guidelines (3) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):
| Guideline | Source | Gene(s) | Dosing | Recommendation |
|---|---|---|---|---|
| Annotation of DPWG Guideline for tacrolimus and CYP3A5 | DPWG | CYP3A5 | yes | yes |
| Annotation of CPIC Guideline for tacrolimus and CYP3A5 | CPIC | CYP3A5 | yes | yes |
| Annotation of RNPGx Guideline for tacrolimus and CYP3A4, CYP3A5 | RNPGx | CYP3A4;CYP3A5 | yes | yes |
PharmGKB also curates 82 clinical and 1,127 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
23 molecules share ≥1 primary target. Top 23 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CANNABIDIOL | ChEMBL + PubChem | Phase 4 (approved) | TRPM8 |
| CAPSAICIN | ChEMBL + PubChem | Phase 4 (approved) | TRPM8 |
| CLOTRIMAZOLE | ChEMBL + PubChem | Phase 4 (approved) | TRPM8 |
| DRONABINOL | ChEMBL + PubChem | Phase 4 (approved) | TRPM8 |
| ECONAZOLE | ChEMBL + PubChem | Phase 4 (approved) | TRPM8 |
| CYCLOSPORINE | ChEMBL | Phase 4 (approved) | FKBP1A |
| MENTHOL | ChEMBL | Phase 4 (approved) | TRPM8 |
| SIROLIMUS | ChEMBL | Phase 4 (approved) | FKBP1A |
| THIABENDAZOLE | ChEMBL | Phase 4 (approved) | FKBP1A |
| ICILLIN | ChEMBL | Phase 3 | TRPM8 |
| LEVOMENTHOL | ChEMBL | Phase 3 | TRPM8 |
| ACOLTREMON | ChEMBL | Phase 2 | TRPM8 |
| BIRICODAR | ChEMBL | Phase 2 | FKBP1A |
| CANNABIDIVARIN | ChEMBL | Phase 2 | TRPM8 |
| CANNABIGEROL | ChEMBL | Phase 2 | TRPM8 |
| CYCLOHEXIMIDE | ChEMBL | Phase 2 | FKBP1A |
| ELISMETREP | ChEMBL | Phase 2 | TRPM8 |
| SB-705498 | ChEMBL | Phase 2 | TRPM8 |
| TETRAHYDROCANNABIVARIN | ChEMBL | Phase 2 | TRPM8 |
| eucalyptol | PubChem | Approved | TRPM8 |
| Eugenol | PubChem | Approved | TRPM8 |
| menthol, unspecified form | PubChem | Approved | TRPM8 |
| Serotonin | PubChem | Approved | TRPM8 |
Related Atlas pages
- Genes: FKBP1A, TRPM8
- Diseases: hepatocellular carcinoma, Hodgkins lymphoma, atopic eczema, infertility disorder, injury, psoriasis, rheumatoid arthritis, ulcerative colitis, kidney disorder, heart disorder, chronic kidney disease, vitiligo, nephrotic syndrome, graft versus host disease, myasthenia gravis, lupus nephritis, non-Hodgkin lymphoma, bronchiolitis obliterans syndrome, seborrheic dermatitis, membranous glomerulonephritis, kidney failure, skin neoplasm, severe acute respiratory syndrome, acute pancreatitis, type 1 diabetes mellitus
- Drugs: Cannabidiol, Capsaicin, Clotrimazole, Dronabinol, Econazole, Cyclosporine, Menthol, Sirolimus, Thiabendazole, Icillin, eucalyptol, Serotonin