itraconazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
systemic antifungal agents, miconazole derivatives 1513 84625-61-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • itraconazole
  • canditral
  • itrizole
  • oriconazole
  • traconal
  • triasporin
  • R-51211
A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
  • Molecular weight: 705.64
  • Formula: C35H38Cl2N8O4
  • CLOGP: 6.84
  • LIPINSKI: 3
  • HAC: 12
  • HDO: 0
  • TPSA: 100.79
  • ALOGS: -4.86
  • ROTB: 11
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O
0.20 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.03 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 14.17 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 55 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 7.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 25 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.387 High 0.85
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.410 High 0.85
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 5.689 10^-6 cm/s High 0.85
dh-clint Dog hepatocyte intrinsic clearance 5.200 uL/min/10^6 cells High 0.85
dppb Dog plasma protein binding (% unbound) 0.100 % High 0.85
fcs-ppb Fetal calf serum protein binding (% unbound) 0.550 % High 0.85
herg hERG pIC50 5.218 pIC50 High 0.85
hh-clint Human hepatocyte intrinsic clearance 7.656 uL/min/10^6 cells High 0.85
hlm-clint Human liver microsomal intrinsic clearance 46.132 uL/min/mg protein High 0.85
hppb Human plasma protein binding (% unbound) 0.240 % High 0.85
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,EGFR,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIM2,PRKDC,STK33,TEK 24
kinase-selectivity-class AXL,EIF2AK3,GRK2 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.824 High 0.85
mh-clint Mouse hepatocyte intrinsic clearance 13.677 High 0.85
mppb Mouse plasma protein binding (% unbound) 0.140 High 0.85
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 10.889 High 0.85
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 0.290 % High 0.85
rh-clint Rat hepatocyte intrinsic clearance 10.544 uL/min/10^6 cells High 0.85
rh-fuinc Rat hepatocyte fraction unbound in incubation 0.850 % High 0.85
rppb Rat plasma protein binding (% unbound) 0.170 % High 0.85
solubility-dd Solubility at pH 7.4 in DMSO 0.780 uM High 0.85

Approvals:

DateAgencyCompanyOrphan
Sept. 11, 1992 FDA JANSSEN PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 524.92 16.83 393 13665 276060 90338329
Aspergillus infection 185.53 16.83 68 13990 10755 90603634
Bronchopulmonary aspergillosis 178.45 16.83 67 13991 11331 90603058
Febrile neutropenia 139.32 16.83 146 13912 158203 90456186
Pseudoaldosteronism 115.43 16.83 20 14038 128 90614261
Pseudohyponatraemia 103.21 16.83 16 14042 44 90614345
Drug resistance 102.47 16.83 62 13996 30387 90584002
Rhabdomyolysis 99.19 16.83 74 13984 51182 90563207
Symmetrical drug-related intertriginous and flexural exanthema 82.68 16.83 21 14037 958 90613431
Hepatic function abnormal 78.95 16.83 62 13996 46226 90568163
Neutrophil count decreased 73.88 16.83 72 13986 71460 90542929
Myopathy 71.35 16.83 37 14021 13481 90600908
Cytomegalovirus test positive 66.89 16.83 24 14034 3567 90610822
Cytomegalovirus infection 66.70 16.83 45 14013 26557 90587832
Labelled drug-drug interaction medication error 63.17 16.83 35 14023 14547 90599842
Hypokalaemia 62.88 16.83 89 13969 131027 90483362
Platelet count decreased 62.80 16.83 91 13967 136878 90477511
Sepsis 62.29 16.83 105 13953 179709 90434680
Pathogen resistance 60.14 16.83 28 14030 8087 90606302
Mycotic endophthalmitis 59.65 16.83 12 14046 186 90614203
Acute myeloid leukaemia 59.25 16.83 38 14020 20602 90593787
Septic shock 59.05 16.83 69 13989 84091 90530298
Adrenal insufficiency 57.42 16.83 43 14015 29878 90584511
Adrenal suppression 53.60 16.83 15 14043 994 90613395
Drug level increased 53.50 16.83 40 14018 27722 90586667
Pain 52.02 16.83 47 14011 996294 89618095
Neutropenia 51.41 16.83 110 13948 224794 90389595
Acute graft versus host disease 50.49 16.83 22 14036 5446 90608943
Skin candida 49.59 16.83 16 14042 1725 90612664
Disseminated aspergillosis 48.73 16.83 12 14046 482 90613907
Neutropenic sepsis 48.66 16.83 32 14026 18098 90596291
Transplant rejection 48.19 16.83 28 14030 12730 90601659
Abdominal discomfort 46.23 16.83 9 14049 477319 90137070
Ileus paralytic 45.46 16.83 20 14038 5065 90609324
Electrocardiogram QT prolonged 45.24 16.83 56 14002 72400 90541989
Pneumonia fungal 45.20 16.83 22 14036 7009 90607380
Swelling 42.52 16.83 7 14051 419051 90195338
Fungal infection 42.28 16.83 42 14016 42619 90571770
Cerebral aspergillosis 42.06 16.83 11 14047 564 90613825
Joint swelling 41.92 16.83 13 14045 503287 90111102
Fungal endocarditis 41.75 16.83 10 14048 357 90614032
Systemic lupus erythematosus 41.67 16.83 4 14054 361892 90252497
Histoplasmosis disseminated 41.41 16.83 15 14043 2290 90612099
Trichosporon infection 41.37 16.83 10 14048 371 90614018
Corneal perforation 41.36 16.83 11 14047 602 90613787
Cytomegalovirus viraemia 40.71 16.83 21 14037 7565 90606824
Mucormycosis 40.66 16.83 17 14041 3804 90610585
Cardiotoxicity 40.40 16.83 24 14034 11365 90603024
Thrombotic microangiopathy 40.35 16.83 27 14031 15716 90598673
Pleural effusion 39.55 16.83 66 13992 111925 90502464
Immune reconstitution inflammatory syndrome associated tuberculosis 38.62 16.83 10 14048 493 90613896
Contraindicated product prescribed 38.54 16.83 13 14045 1609 90612780
White blood cell count decreased 38.47 16.83 82 13976 167027 90447362
Scedosporium infection 38.11 16.83 11 14047 815 90613574
Toxic epidermal necrolysis 37.87 16.83 35 14023 32493 90581896
Arthropathy 37.42 16.83 6 14052 366236 90248153
Acute graft versus host disease in skin 37.08 16.83 17 14041 4739 90609650
Multiple organ dysfunction syndrome 36.67 16.83 49 14009 68287 90546102
Thrombocytopenia 36.58 16.83 92 13966 208633 90405756
Lung transplant rejection 35.60 16.83 11 14047 1030 90613359
Respiratory failure 34.33 16.83 64 13994 118354 90496035
Posterior reversible encephalopathy syndrome 33.99 16.83 28 14030 22311 90592078
Infusion related reaction 32.54 16.83 12 14046 416768 90197621
Eye infection fungal 32.31 16.83 7 14051 158 90614231
Human herpesvirus 6 infection reactivation 31.75 16.83 9 14049 625 90613764
Disseminated varicella zoster vaccine virus infection 31.41 16.83 6 14052 70 90614319
Pneumonia 31.23 16.83 187 13871 637872 89976517
Pericarditis 31.05 16.83 3 14055 270148 90344241
Candida infection 30.95 16.83 32 14026 34025 90580364
Rheumatoid arthritis 30.83 16.83 9 14049 362605 90251784
Exposure during pregnancy 30.79 16.83 94 13964 238316 90376073
Pyrexia 30.08 16.83 190 13868 660295 89954094
Pseudomonas infection 29.94 16.83 22 14036 14843 90599546
Polyglandular disorder 29.87 16.83 7 14051 227 90614162
Pulmonary nocardiosis 29.71 16.83 9 14049 789 90613600
Liver function test abnormal 29.67 16.83 38 14020 50807 90563582
Diabetes mellitus 29.55 16.83 43 14015 64832 90549557
Torticollis 29.31 16.83 12 14046 2546 90611843
Staphylococcal sepsis 28.74 16.83 18 14040 9365 90605024
Disseminated intravascular coagulation 28.67 16.83 25 14033 21513 90592876
Blood lactate dehydrogenase increased 28.45 16.83 27 14031 25905 90588484
Anaemia 28.31 16.83 119 13939 352683 90261706
Mobility decreased 28.25 16.83 3 14055 250731 90363658
Immunosuppressant drug level increased 28.16 16.83 14 14044 4666 90609723
Fatigue 28.11 16.83 89 13969 1153934 89460455
Systemic mycosis 27.65 16.83 10 14048 1520 90612869
Therapeutic product effect decreased 27.34 16.83 5 14053 277566 90336823
Infective pulmonary exacerbation of cystic fibrosis 27.23 16.83 18 14040 10261 90604128
Klebsiella infection 27.21 16.83 18 14040 10279 90604110
Discomfort 26.90 16.83 5 14053 274330 90340059
Erythema multiforme 26.66 16.83 19 14039 12227 90602162
Cardiac failure 26.66 16.83 55 14003 109441 90504948
Graft versus host disease 25.89 16.83 16 14042 8128 90606261
Musculoskeletal stiffness 25.87 16.83 7 14051 296525 90317864
Product dispensing issue 25.03 16.83 7 14051 463 90613926
Acute myeloid leukaemia recurrent 24.77 16.83 10 14048 2047 90612342
Mucosal inflammation 24.53 16.83 37 14021 57588 90556801
Varicella zoster virus infection 24.53 16.83 12 14046 3865 90610524
Cystic fibrosis 24.34 16.83 12 14046 3929 90610460
Blast cell count increased 24.21 16.83 7 14051 522 90613867
Hypersensitivity 24.17 16.83 21 14037 454656 90159733
Haematoma 24.08 16.83 30 14028 39018 90575371
Anaemia folate deficiency 23.99 16.83 7 14051 539 90613850
Drug hypersensitivity 23.95 16.83 22 14036 463587 90150802
Labelled drug-drug interaction issue 23.87 16.83 10 14048 2248 90612141
Drug reaction with eosinophilia and systemic symptoms 23.46 16.83 31 14027 42727 90571662
Candida test positive 23.40 16.83 8 14050 1031 90613358
Duodenal atresia 23.32 16.83 3 14055 0 90614389
Renal failure 23.20 16.83 58 14000 130949 90483440
Disseminated sporotrichosis 23.03 16.83 4 14054 26 90614363
Duplicate therapy error 22.99 16.83 5 14053 115 90614274
Pancreatitis haemorrhagic 22.80 16.83 7 14051 642 90613747
Galactorrhoea 22.41 16.83 12 14046 4660 90609729
Coccidioidomycosis 22.32 16.83 8 14050 1185 90613204
Implant site hypersensitivity 22.30 16.83 4 14054 32 90614357
Blood prolactin increased 22.24 16.83 11 14047 3626 90610763
Plasmapheresis 22.24 16.83 6 14052 347 90614042
Stevens-Johnson syndrome 22.13 16.83 25 14033 29351 90585038
Fibromyalgia 21.93 16.83 3 14055 206266 90408123
Cardiac valve vegetation 21.81 16.83 6 14052 373 90614016
Cholestatic liver injury 21.79 16.83 11 14047 3786 90610603
Cross sensitivity reaction 21.61 16.83 10 14048 2847 90611542
Leukopenia 21.54 16.83 48 14010 100662 90513727
Streptococcal bacteraemia 20.69 16.83 9 14049 2218 90612171
Injury 20.67 16.83 3 14055 197346 90417043
Moraxella infection 20.49 16.83 6 14052 468 90613921
Immune reconstitution inflammatory syndrome 20.33 16.83 13 14045 7006 90607383
Endocrine disorder 20.10 16.83 7 14051 953 90613436
Hypoparathyroidism 19.82 16.83 7 14051 994 90613395
Liver disorder 19.72 16.83 52 14006 121217 90493172
Alopecia 19.63 16.83 29 14029 495042 90119347
Alanine aminotransferase increased 19.51 16.83 51 14007 118287 90496102
Respiratory distress 19.48 16.83 27 14031 38919 90575470
Trichophytosis 19.27 16.83 4 14054 73 90614316
Renal impairment 19.01 16.83 47 14011 105374 90509015
Chronic hepatitis 18.90 16.83 7 14051 1138 90613251
Cutaneous nocardiosis 18.87 16.83 4 14054 81 90614308
Cushing's syndrome 18.75 16.83 6 14052 630 90613759
Peripheral swelling 18.62 16.83 22 14036 413084 90201305
Cystitis haemorrhagic 17.96 16.83 11 14047 5502 90608887
Culture stool positive 17.90 16.83 5 14053 329 90614060
Impaired healing 17.83 16.83 7 14051 234192 90380197
Ecchymosis 17.82 16.83 15 14043 12308 90602081
Dizziness 17.63 16.83 41 14017 589243 90025146
Engraft failure 17.30 16.83 5 14053 372 90614017
Secondary adrenocortical insufficiency 17.18 16.83 8 14050 2310 90612079
Heart transplant rejection 17.08 16.83 6 14052 838 90613551
Torsade de pointes 17.02 16.83 16 14042 15166 90599223
General physical health deterioration 17.00 16.83 18 14040 355097 90259292

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 326.31 14.96 470 17089 266529 42337247
Aspergillus infection 124.69 14.96 79 17480 15758 42588018
Drug resistance 122.11 14.96 106 17453 34142 42569634
Bronchopulmonary aspergillosis 112.32 14.96 80 17479 19349 42584427
Fungal infection 95.52 14.96 73 17486 19649 42584127
Pathogen resistance 92.33 14.96 58 17501 11392 42592384
Phaeohyphomycosis 81.88 14.96 27 17532 1157 42602619
Drug ineffective 81.10 14.96 488 17071 629709 41974067
Parathyroid gland enlargement 80.45 14.96 18 17541 167 42603609
Upper respiratory fungal infection 79.60 14.96 18 17541 176 42603600
Febrile neutropenia 78.05 14.96 209 17350 185494 42418282
Apparent mineralocorticoid excess 77.62 14.96 15 17544 61 42603715
Cardiotoxicity 76.31 14.96 44 17515 7401 42596375
Disseminated intravascular coagulation 73.12 14.96 69 17490 24725 42579051
Neutrophil count decreased 70.17 14.96 107 17452 63308 42540468
Drug level increased 69.90 14.96 69 17490 26131 42577645
Platelet count decreased 60.22 14.96 158 17401 138423 42465353
Forced expiratory volume 58.86 14.96 13 17546 113 42603663
Renal impairment 57.73 14.96 135 17424 110093 42493683
Cytomegalovirus test positive 53.74 14.96 29 17530 4290 42599486
Symmetrical drug-related intertriginous and flexural exanthema 52.90 14.96 18 17541 850 42602926
Adrenal insufficiency 48.92 14.96 49 17510 18875 42584901
Hepatic function abnormal 48.75 14.96 81 17478 51486 42552290
Mycobacterial infection 48.06 14.96 23 17536 2645 42601131
Bradyarrhythmia 44.98 14.96 22 17537 2653 42601123
Bronchial disorder 44.54 14.96 18 17541 1380 42602396
Cytomegalovirus infection 42.22 14.96 59 17500 32247 42571529
Hypokalaemia 42.15 14.96 92 17467 71629 42532147
Pseudoaldosteronism 41.90 14.96 10 17549 126 42603650
Bronchiectasis 41.76 14.96 44 17515 17975 42585801
Cutaneous vasculitis 41.37 14.96 29 17530 6831 42596945
Lip squamous cell carcinoma 40.73 14.96 10 17549 143 42603633
Acute myeloid leukaemia recurrent 39.34 14.96 22 17537 3490 42600286
Sinus congestion 38.62 14.96 28 17531 6952 42596824
Fluorosis 37.88 14.96 8 17551 55 42603721
Histoplasmosis disseminated 37.58 14.96 18 17541 2073 42601703
Tendon disorder 37.33 14.96 21 17538 3368 42600408
Blood lactate dehydrogenase increased 36.14 14.96 49 17510 26032 42577744
White blood cell count decreased 35.45 14.96 113 17446 110283 42493493
Hyperbilirubinaemia 35.24 14.96 43 17516 20592 42583184
Granulomatous rosacea 35.04 14.96 9 17550 156 42603620
Fatigue 34.31 14.96 81 17478 435560 42168216
Secretion discharge 34.21 14.96 27 17532 7608 42596168
Bronchopulmonary aspergillosis allergic 33.85 14.96 22 17537 4576 42599200
Obliterative bronchiolitis 33.84 14.96 15 17544 1446 42602330
Hyperventilation 33.12 14.96 19 17540 3163 42600613
Myopathy 30.82 14.96 33 17526 13728 42590048
Pyrexia 30.55 14.96 271 17288 393771 42210005
Pseudomonas infection 30.19 14.96 35 17524 15888 42587888
Death 30.09 14.96 97 17462 471088 42132688
Pneumonia fungal 29.96 14.96 27 17532 9119 42594657
Product dose omission issue 28.48 14.96 14 17545 154351 42449425
Ileus paralytic 27.91 14.96 24 17535 7617 42596159
Philadelphia positive acute lymphocytic leukaemia 26.98 14.96 6 17553 54 42603722
Haemoptysis 26.86 14.96 59 17500 46108 42557668
Neutrophil Pelger-Huet anomaly present 26.38 14.96 8 17551 260 42603516
Immunosuppressant drug level increased 25.67 14.96 23 17536 7708 42596068
Acute myeloid leukaemia 25.22 14.96 38 17521 22218 42581558
Fall 25.18 14.96 36 17523 234484 42369292
Lung transplant rejection 25.06 14.96 11 17548 1036 42602740
Cardiovascular insufficiency 24.80 14.96 13 17546 1813 42601963
Lymphadenopathy 24.56 14.96 47 17512 33318 42570458
Acute graft versus host disease 24.47 14.96 23 17536 8192 42595584
Folliculitis 23.50 14.96 19 17540 5539 42598237
Drug abuse 23.47 14.96 7 17552 104764 42499012
Liver disorder 23.44 14.96 51 17508 39593 42564183
Ocular surface squamous neoplasia 23.35 14.96 5 17554 37 42603739
Pneumonia 22.94 14.96 270 17289 421879 42181897
Treatment failure 22.79 14.96 67 17492 62557 42541219
Cerebrovascular accident 22.67 14.96 6 17553 97154 42506622
Histoplasmosis 22.23 14.96 12 17547 1775 42602001
Obstructive airways disorder 22.20 14.96 38 17521 24721 42579055
Graft versus host disease 22.17 14.96 27 17532 12898 42590878
Ubiquinone decreased 21.64 14.96 4 17555 12 42603764
Choriomeningitis lymphocytic 21.32 14.96 6 17553 149 42603627
Hypothalamic pituitary adrenal axis suppression 21.31 14.96 7 17552 296 42603480
Transplant rejection 21.09 14.96 27 17532 13561 42590215
Asthma-chronic obstructive pulmonary disease overlap syndrome 20.89 14.96 11 17548 1548 42602228
Acute graft versus host disease in skin 20.62 14.96 20 17539 7404 42596372
Sputum increased 20.55 14.96 14 17545 3149 42600627
Condition aggravated 20.49 14.96 180 17379 260574 42343202
CARD9 deficiency 20.02 14.96 4 17555 20 42603756
Alternaria infection 19.96 14.96 8 17551 600 42603176
Respiratory disorder 19.94 14.96 34 17525 22051 42581725
Pain 19.64 14.96 45 17514 244803 42358973
Trichosporon infection 19.59 14.96 9 17550 943 42602833
Blood alkaline phosphatase abnormal 19.54 14.96 8 17551 634 42603142
Epstein-Barr virus infection 19.50 14.96 22 17537 9696 42594080
Septic shock 19.40 14.96 82 17477 91590 42512186
Differentiation syndrome 19.34 14.96 11 17548 1802 42601974
Neutropenia 19.07 14.96 144 17415 199287 42404489
Cystitis haemorrhagic 18.98 14.96 19 17540 7310 42596466
Post transplant lymphoproliferative disorder 18.90 14.96 21 17538 9099 42594677
Blood immunoglobulin E increased 18.83 14.96 14 17545 3611 42600165
Hyperhidrosis 18.61 14.96 7 17552 90505 42513271
Bronchial polyp 18.31 14.96 3 17556 3 42603773
Myositis 17.73 14.96 26 17533 14840 42588936
Haemophagocytic lymphohistiocytosis 17.71 14.96 29 17530 18193 42585583
Dizziness 17.52 14.96 49 17510 249205 42354571
Squamous cell carcinoma of the oral cavity 17.34 14.96 6 17553 298 42603478
Overdose 17.31 14.96 11 17548 105253 42498523
Polyomavirus-associated nephropathy 17.26 14.96 16 17543 5599 42598177
Pneumonia cytomegaloviral 17.22 14.96 14 17545 4112 42599664
Immune reconstitution inflammatory syndrome 17.09 14.96 21 17538 10122 42593654
Feeling abnormal 16.88 14.96 4 17555 69782 42533994
Labelled drug-drug interaction medication error 16.80 14.96 26 17533 15556 42588220
Cytomegalovirus viraemia 16.71 14.96 21 17538 10356 42593420
Pulmonary haemorrhage 16.68 14.96 22 17537 11375 42592401
Pulmonary embolism 16.47 14.96 15 17544 119597 42484179
Sepsis 16.37 14.96 139 17420 199195 42404581
Weight decreased 16.04 14.96 39 17520 207909 42395867
Pneumaturia 15.99 14.96 4 17555 62 42603714
Acute graft versus host disease in liver 15.98 14.96 10 17549 1948 42601828
Back pain 15.97 14.96 21 17538 141755 42462021
Neurotoxicity 15.81 14.96 32 17527 23619 42580157
Drug level changed 15.68 14.96 6 17553 398 42603378
Acute graft versus host disease in intestine 15.64 14.96 13 17546 3938 42599838
Contraindicated product prescribed 15.63 14.96 7 17552 692 42603084
Oedema 15.56 14.96 52 17507 51949 42551827
Aspartate aminotransferase increased 15.53 14.96 68 17491 77095 42526681
Drug hypersensitivity 15.51 14.96 11 17548 99378 42504398
Therapeutic product effect incomplete 15.43 14.96 64 17495 70875 42532901
Corneal epithelium defect 15.42 14.96 6 17553 416 42603360
Candida infection 15.36 14.96 30 17529 21580 42582196
Aspergilloma 14.98 14.96 6 17553 449 42603327

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 811.31 14.29 810 27880 499373 110061236
Bronchopulmonary aspergillosis 273.25 14.29 140 28550 29723 110530886
Aspergillus infection 266.46 14.29 131 28559 25485 110535124
Drug resistance 216.47 14.29 151 28539 56223 110504386
Pathogen resistance 173.76 14.29 87 28603 17585 110543024
Febrile neutropenia 170.18 14.29 299 28391 316468 110244141
Pseudoaldosteronism 146.24 14.29 30 28660 296 110560313
Symmetrical drug-related intertriginous and flexural exanthema 132.05 14.29 39 28651 1858 110558751
Drug level increased 127.75 14.29 103 28587 47616 110512993
Ileus paralytic 124.95 14.29 61 28629 11676 110548933
Drug ineffective 118.94 14.29 735 27955 1519805 109040804
Neutrophil count decreased 117.89 14.29 151 28539 120790 110439819
Cardiotoxicity 117.49 14.29 66 28624 16815 110543794
Fungal infection 111.92 14.29 98 28592 50708 110509901
Platelet count decreased 107.77 14.29 205 28485 230238 110330371
Phaeohyphomycosis 105.30 14.29 32 28658 1682 110558927
Myopathy 100.81 14.29 69 28621 24891 110535718
Adrenal insufficiency 91.82 14.29 81 28609 42309 110518300
Hepatic function abnormal 90.97 14.29 114 28576 89181 110471428
Apparent mineralocorticoid excess 90.39 14.29 16 28674 64 110560545
Hypokalaemia 88.62 14.29 165 28525 182283 110378326
Parathyroid gland enlargement 85.63 14.29 18 28672 202 110560407
Cytomegalovirus test positive 82.26 14.29 39 28651 6997 110553612
Cytomegalovirus infection 79.98 14.29 84 28606 54360 110506249
Disseminated intravascular coagulation 77.88 14.29 73 28617 41213 110519396
Renal impairment 76.44 14.29 158 28532 188287 110372322
Pseudohyponatraemia 75.13 14.29 16 28674 192 110560417
Upper respiratory fungal infection 73.75 14.29 18 28672 409 110560200
Labelled drug-drug interaction medication error 73.68 14.29 61 28629 29241 110531368
Pain 72.28 14.29 85 28605 954870 109605739
Pneumonia fungal 72.23 14.29 46 28644 14708 110545901
Rhabdomyolysis 71.54 14.29 119 28571 120282 110440327
Fatigue 67.31 14.29 134 28556 1215824 109344785
Septic shock 66.15 14.29 134 28556 157394 110403215
Transplant rejection 65.67 14.29 53 28637 24514 110536095
Acute myeloid leukaemia 65.47 14.29 64 28626 38046 110522563
White blood cell count decreased 60.94 14.29 163 28527 229227 110331382
Forced expiratory volume 60.64 14.29 12 28678 97 110560512
Histoplasmosis disseminated 59.44 14.29 26 28664 3873 110556736
Acute myeloid leukaemia recurrent 58.60 14.29 28 28662 5111 110555498
Lung transplant rejection 57.96 14.29 21 28669 1910 110558699
Blood lactate dehydrogenase increased 57.40 14.29 64 28626 44270 110516339
Granulomatous rosacea 57.28 14.29 13 28677 213 110560396
Adrenal suppression 56.78 14.29 20 28670 1676 110558933
Abdominal discomfort 56.64 14.29 16 28674 393842 110166767
Arthropathy 56.16 14.29 5 28685 287517 110273092
Drug hypersensitivity 54.20 14.29 25 28665 454065 110106544
Pseudomonas infection 53.98 14.29 50 28640 27803 110532806
Rheumatoid arthritis 53.96 14.29 7 28683 299606 110261003
Trichosporon infection 53.93 14.29 18 28672 1282 110559327
Systemic lupus erythematosus 53.78 14.29 3 28687 254335 110306274
Bradyarrhythmia 53.58 14.29 26 28664 4908 110555701
Immunosuppressant drug level increased 53.56 14.29 35 28655 11689 110548920
Joint swelling 53.45 14.29 24 28666 442821 110117788
Pleural effusion 53.09 14.29 132 28558 177577 110383032
Neurotoxicity 53.05 14.29 60 28630 42147 110518462
Fungal endocarditis 53.04 14.29 16 28674 820 110559789
Swelling 52.87 14.29 13 28677 351028 110209581
Bronchiectasis 51.28 14.29 55 28635 36438 110524171
Contraindicated product prescribed 50.90 14.29 20 28670 2273 110558336
Completed suicide 50.82 14.29 3 28687 242378 110318231
Sepsis 50.57 14.29 193 28497 327153 110233456
Infusion related reaction 50.33 14.29 18 28672 381144 110179465
Mycobacterial infection 50.16 14.29 24 28666 4393 110556216
Pneumonia 49.31 14.29 392 28298 876322 109684287
Musculoskeletal stiffness 49.30 14.29 7 28683 279815 110280794
Wound 48.85 14.29 3 28687 234434 110326175
Mycotic endophthalmitis 48.50 14.29 13 28677 433 110560176
Respiratory failure 48.35 14.29 144 28546 215188 110345421
Bronchopulmonary aspergillosis allergic 48.17 14.29 29 28661 8397 110552212
Bronchial disorder 47.21 14.29 20 28670 2756 110557853
Skin candida 47.14 14.29 19 28671 2309 110558300
Pyrexia 44.82 14.29 391 28299 897874 109662735
Acute graft versus host disease in skin 44.09 14.29 30 28660 10710 110549899
Graft versus host disease 42.86 14.29 37 28653 18769 110541840
Cytomegalovirus viraemia 42.63 14.29 36 28654 17728 110542881
Fluorosis 41.50 14.29 10 28680 215 110560394
Acute graft versus host disease 41.41 14.29 31 28659 12850 110547759
Immune reconstitution inflammatory syndrome 41.25 14.29 34 28656 16192 110544417
Neutropenia 40.99 14.29 199 28491 374421 110186188
Hyperbilirubinaemia 40.95 14.29 45 28645 30626 110529983
Cardiac failure 39.79 14.29 123 28567 187503 110373106
Mucormycosis 39.67 14.29 28 28662 10600 110550009
Blast cell count increased 38.90 14.29 15 28675 1622 110558987
Dizziness 38.45 14.29 77 28613 698116 109862493
Headache 37.81 14.29 111 28579 882266 109678343
Lip squamous cell carcinoma 37.75 14.29 10 28680 318 110560291
Candida infection 37.70 14.29 54 28636 47955 110512654
Pericarditis 37.40 14.29 6 28684 219108 110341501
Peripheral swelling 37.39 14.29 30 28660 404004 110156605
Multiple organ dysfunction syndrome 36.49 14.29 104 28586 151606 110409003
Fall 36.36 14.29 63 28627 603419 109957190
Electrocardiogram QT prolonged 35.81 14.29 84 28606 108876 110451733
Obliterative bronchiolitis 35.62 14.29 18 28672 3705 110556904
Drug level decreased 35.37 14.29 33 28657 18515 110542094
Myositis 35.36 14.29 42 28648 31074 110529535
Haemoptysis 35.19 14.29 65 28625 71289 110489320
Discomfort 34.22 14.29 7 28683 214700 110345909
Cystitis haemorrhagic 34.04 14.29 27 28663 12182 110548427
Cerebral aspergillosis 33.95 14.29 15 28675 2287 110558322
Candida pneumonia 33.78 14.29 12 28678 1031 110559578
Sputum increased 33.41 14.29 20 28670 5731 110554878
Therapeutic product effect decreased 33.17 14.29 11 28679 244305 110316304
Scedosporium infection 33.01 14.29 15 28675 2443 110558166
Neuropathy peripheral 31.27 14.29 110 28580 179167 110381442
Tendon disorder 31.20 14.29 22 28668 8315 110552294
Corneal perforation 30.96 14.29 11 28679 945 110559664
Alanine aminotransferase increased 30.55 14.29 111 28579 183662 110376947
Liver function test abnormal 30.53 14.29 60 28630 68890 110491719
Histoplasmosis 30.39 14.29 15 28675 2938 110557671
Alternaria infection 30.35 14.29 11 28679 1001 110559608
Haemophagocytic lymphohistiocytosis 30.08 14.29 39 28651 31520 110529089
Injury 29.92 14.29 5 28685 177260 110383349
Product dose omission issue 29.62 14.29 24 28666 321758 110238851
Systemic mycosis 29.47 14.29 16 28674 3813 110556796
Aspergilloma 28.97 14.29 10 28680 789 110559820
Disseminated varicella zoster vaccine virus infection 28.68 14.29 7 28683 159 110560450
Acute graft versus host disease in intestine 28.65 14.29 18 28672 5621 110554988
Hypersensitivity 28.33 14.29 38 28652 403960 110156649
Post transplant lymphoproliferative disorder 28.28 14.29 27 28663 15586 110545023
Philadelphia positive acute lymphocytic leukaemia 28.25 14.29 6 28684 71 110560538
Ocular surface squamous neoplasia 27.68 14.29 5 28685 23 110560586
Infective pulmonary exacerbation of cystic fibrosis 27.62 14.29 26 28664 14745 110545864
Pneumonia cytomegaloviral 27.54 14.29 19 28671 6935 110553674
Eye infection fungal 27.31 14.29 9 28681 616 110559993
Arthralgia 27.29 14.29 107 28583 779525 109781084
Dry mouth 27.14 14.29 9 28681 199939 110360670
Neutrophil Pelger-Huet anomaly present 26.92 14.29 8 28682 389 110560220
Cutaneous vasculitis 26.91 14.29 24 28666 12705 110547904
Disseminated aspergillosis 26.72 14.29 13 28677 2467 110558142
Migraine 26.53 14.29 6 28684 171646 110388963
Nocardiosis 26.28 14.29 19 28671 7467 110553142
Immune reconstitution inflammatory syndrome associated tuberculosis 26.27 14.29 10 28680 1044 110559565
Contusion 26.08 14.29 14 28676 233347 110327262
Muscle injury 26.05 14.29 3 28687 140804 110419805
Injection site pain 25.98 14.29 7 28683 177915 110382694
Polyglandular disorder 25.95 14.29 7 28683 239 110560370
Secretion discharge 25.81 14.29 29 28661 20215 110540394
Staphylococcal sepsis 25.75 14.29 27 28663 17427 110543182
Mobility decreased 25.44 14.29 15 28675 237407 110323202
Osteoarthritis 25.18 14.29 8 28682 182615 110377994
Irritable bowel syndrome 24.87 14.29 6 28684 164209 110396400
Endophthalmitis 24.76 14.29 19 28671 8168 110552441
Drug level below therapeutic 24.66 14.29 22 28668 11651 110548958
Cushingoid 24.60 14.29 22 28668 11690 110548919
Lower respiratory tract infection fungal 24.53 14.29 9 28681 848 110559761
Pneumonia bacterial 24.33 14.29 32 28658 26229 110534380
Pulmonary alveolar haemorrhage 24.23 14.29 28 28662 20122 110540487
Differentiation syndrome 24.21 14.29 13 28677 3031 110557578
Blood immunoglobulin E increased 24.03 14.29 18 28672 7464 110553145
Corneal epithelium defect 23.99 14.29 9 28681 903 110559706
Alopecia 23.90 14.29 36 28654 364717 110195892
Arthritis 23.72 14.29 7 28683 167579 110393030
Blood creatine phosphokinase increased 23.64 14.29 56 28634 73021 110487588
Aspartate aminotransferase increased 23.60 14.29 93 28597 159843 110400766
Bursitis 23.46 14.29 3 28687 129915 110430694
Hyperventilation 23.27 14.29 19 28671 8928 110551681
Cardiovascular insufficiency 23.27 14.29 13 28677 3275 110557334
Tumour lysis syndrome 23.24 14.29 34 28656 30767 110529842
Impaired healing 23.18 14.29 11 28679 196706 110363903
Choriomeningitis lymphocytic 22.99 14.29 6 28684 180 110560429
Disseminated sporotrichosis 22.97 14.29 5 28685 67 110560542
Lymphadenopathy 22.95 14.29 51 28639 63784 110496825
Thrombocytopenia 22.91 14.29 162 28528 348723 110211886
Hyperhidrosis 22.81 14.29 10 28680 187288 110373321
Hypothalamic pituitary adrenal axis suppression 22.67 14.29 8 28682 674 110559935
Human herpesvirus 6 infection reactivation 22.12 14.29 9 28681 1120 110559489
Liver disorder 22.04 14.29 84 28606 142159 110418450
Varicella zoster virus infection 21.99 14.29 16 28674 6352 110554257
CARD9 deficiency 21.87 14.29 4 28686 20 110560589
Memory impairment 21.74 14.29 12 28678 196932 110363677
Pulmonary haemorrhage 21.72 14.29 24 28666 16432 110544177
Anaemia 21.66 14.29 227 28463 546859 110013750
Ill-defined disorder 21.39 14.29 7 28683 156846 110403763
Trichophytosis 21.27 14.29 7 28683 477 110560132
Lung infiltration 21.27 14.29 29 28661 24599 110536010
Acute lymphocytic leukaemia 21.08 14.29 15 28675 5750 110554859
Jaundice 20.93 14.29 47 28643 59189 110501420
Torticollis 20.81 14.29 12 28678 3209 110557400
Confusional state 20.73 14.29 58 28632 468622 110091987
Implant site hypersensitivity 20.60 14.29 4 28686 29 110560580
Ubiquinone decreased 20.60 14.29 4 28686 29 110560580
Polyomavirus-associated nephropathy 20.46 14.29 17 28673 8184 110552425
Musculoskeletal pain 20.42 14.29 11 28679 183012 110377597
Thrombotic microangiopathy 20.31 14.29 31 28659 29118 110531491
Cushing's syndrome 20.25 14.29 8 28682 922 110559687
Myelosuppression 20.13 14.29 62 28628 94278 110466331
Atypical mycobacterial infection 19.93 14.29 11 28679 2707 110557902
Fusarium infection 19.73 14.29 11 28679 2760 110557849
Secondary adrenocortical insufficiency 19.68 14.29 13 28677 4421 110556188
Nasopharyngitis 19.59 14.29 46 28644 394315 110166294
Psoriasis 19.53 14.29 6 28684 139987 110420622
Klebsiella infection 19.50 14.29 25 28665 19984 110540625
Cardiac valve vegetation 19.39 14.29 8 28682 1032 110559577
Sinus congestion 19.29 14.29 31 28659 30428 110530181
Cross sensitivity reaction 19.25 14.29 14 28676 5553 110555056
Pulmonary cavitation 19.23 14.29 10 28680 2184 110558425
Product dispensing issue 19.21 14.29 7 28683 647 110559962
Ileus 19.08 14.29 31 28659 30698 110529911
Obstructive airways disorder 19.04 14.29 39 28651 46110 110514499
Contraindicated product administered 18.81 14.29 22 28668 248245 110312364
Anaemia folate deficiency 18.74 14.29 7 28683 694 110559915
Splenic infection fungal 18.73 14.29 5 28685 164 110560445
Acute graft versus host disease in liver 18.55 14.29 10 28680 2349 110558260
Chronic granulomatous disease 18.49 14.29 4 28686 52 110560557
Pain in extremity 18.22 14.29 65 28625 487053 110073556
Pneumaturia 18.21 14.29 4 28686 56 110560553
Anterior chamber inflammation 18.05 14.29 7 28683 768 110559841
Fungal skin infection 18.03 14.29 15 28675 7234 110553375
Back pain 17.86 14.29 44 28646 370952 110189657
Urticaria 17.66 14.29 35 28655 318822 110241787
Periostitis 17.64 14.29 7 28683 816 110559793
Epstein-Barr virus infection 17.61 14.29 23 28667 18715 110541894
Pulmonary nocardiosis 17.54 14.29 10 28680 2619 110557990
Candida test positive 17.35 14.29 8 28682 1347 110559262
Bone marrow failure 17.29 14.29 43 28647 57805 110502804
Condition aggravated 17.27 14.29 277 28413 734559 109826050
Burkholderia cepacia complex infection 17.27 14.29 6 28684 483 110560126
Pneumonia klebsiella 17.07 14.29 14 28676 6618 110553991
Forced expiratory volume decreased 17.01 14.29 19 28671 13157 110547452
Disease progression 17.00 14.29 115 28575 243919 110316690
Disease recurrence 16.93 14.29 44 28646 60740 110499869
Inappropriate antidiuretic hormone secretion 16.89 14.29 31 28659 33820 110526789
Maternal exposure during pregnancy 16.84 14.29 25 28665 254858 110305751
Cortisol decreased 16.83 14.29 10 28680 2826 110557783
Gait disturbance 16.77 14.29 29 28661 278179 110282430
Intentional product use issue 16.69 14.29 24 28666 247882 110312727
Cystic fibrosis 16.59 14.29 12 28678 4719 110555890
Chronic graft versus host disease 16.46 14.29 16 28674 9441 110551168
Overdose 16.37 14.29 22 28668 233772 110326837
Fungal sepsis 16.25 14.29 9 28681 2228 110558381
Pancreatitis haemorrhagic 16.22 14.29 7 28683 1009 110559600
Paracoccidioides infection 16.14 14.29 4 28686 97 110560512
Cerebrovascular accident 16.09 14.29 14 28676 181270 110379339
Pancytopenia 15.95 14.29 101 28589 209512 110351097
Septic embolus 15.93 14.29 9 28681 2317 110558292
Drug level changed 15.88 14.29 6 28684 614 110559995
Labelled drug-drug interaction issue 15.76 14.29 11 28679 4090 110556519
General physical health deterioration 15.74 14.29 57 28633 425238 110135371
Galactorrhoea 15.63 14.29 11 28679 4144 110556465
Endocrine disorder 15.54 14.29 7 28683 1117 110559492
BK virus infection 15.40 14.29 18 28672 13088 110547521
Blood bilirubin increased 15.35 14.29 49 28641 75923 110484686
Chronic hepatitis 15.31 14.29 8 28682 1764 110558845
Oedema 15.26 14.29 100 28590 209876 110350733
Pseudomonal sepsis 15.18 14.29 15 28675 9031 110551578
Bacterial sepsis 15.15 14.29 16 28674 10410 110550199
Neutropenic sepsis 15.14 14.29 28 28662 30718 110529891
Depression 14.98 14.29 38 28652 317297 110243312
Cytomegalovirus infection reactivation 14.95 14.29 21 28669 18312 110542297
Squamous cell carcinoma of the oral cavity 14.86 14.29 6 28684 732 110559877
Nephropathy toxic 14.78 14.29 26 28664 27452 110533157
Myelodysplastic syndrome 14.67 14.29 31 28659 37453 110523156
Blood alkaline phosphatase abnormal 14.64 14.29 7 28683 1280 110559329
Neuropsychiatric symptoms 14.63 14.29 7 28683 1281 110559328
Moraxella infection 14.62 14.29 6 28684 764 110559845
Blood alkaline phosphatase increased 14.56 14.29 46 28644 70889 110489720
Drug ineffective for unapproved indication 14.52 14.29 59 28631 102779 110457830
Asthenia 14.47 14.29 112 28578 688887 109871722
Graft versus host disease in skin 14.43 14.29 14 28676 8240 110552369
Ecchymosis 14.34 14.29 20 28670 17318 110543291

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J02AC02 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOTICS FOR SYSTEMIC USE
ANTIMYCOTICS FOR SYSTEMIC USE
Triazole and tetrazole derivatives
FDA CS M0002083 Azoles
FDA EPC N0000175487 Azole Antifungal
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:38068 antimalarial
CHEBI has role CHEBI:50183 P450 inhibitor
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:64951 anti-HBV agent
CHEBI has role CHEBI:65023 anti-asthmatic agent
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:74518 anti-obesity agent
CHEBI has role CHEBI:77748 EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor
CHEBI has role CHEBI:140921 Hedgehog signaling pathway inhibitor
CHEBI has role CHEBI:233423 antifibrotic agent
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006727 Hormone Antagonists
MeSH PA D058888 14-alpha Demethylase Inhibitors
MeSH PA D065088 Steroid Synthesis Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D065692 Cytochrome P-450 CYP3A Inhibitors

Related Drugs by ATC class:

J02AC Triazole and tetrazole derivatives 5 drugs
fluconazoleisavuconazoniumoteseconazoleposaconazolevoriconazole

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Invasive pulmonary aspergillosis indication 3214003
Histoplasmosis indication 12962009 DOID:1731
Candidiasis of the esophagus indication 20639004 DOID:13146
Fusarium infection indication 64250002
Aspergillosis indication 65553006 DOID:13564
Blastomycosis indication 69996000 DOID:12663
Disseminated candidiasis indication 70572005
Onychomycosis of fingernails indication 403058003
Onychomycosis of toenails indication 403059006
Candidemia indication 432261003
Fungal Infection due to Scedosporium Apiospermum indication
Fungal Infection due to Fusarium Solani indication
Oropharyngeal Candidiasis indication
Coccidioidomycosis off-label use 60826002 DOID:13450
Chromoblastomycosis off-label use 187079000
Infection due to Penicillium marneffei off-label use 372936000
Onychomycosis due to dermatophyte off-label use 402134005
Heart valve disorder contraindication 368009 DOID:4079
Hypocalcemia contraindication 5291005
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Hearing loss contraindication 15188001
Torsades de pointes contraindication 31722008
Hypokalemia contraindication 43339004
Ventricular arrhythmia contraindication 44103008
Achlorhydria contraindication 47481007
Chronic heart failure contraindication 48447003
Hypochlorhydria contraindication 55961006
Heart failure contraindication 84114007 DOID:6000
Cardiomyopathy contraindication 85898001 DOID:0050700
Kidney disease contraindication 90708001 DOID:557
Prolonged QT interval contraindication 111975006
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Drug-induced hepatitis contraindication 235876009
Edema contraindication 267038008
Pregnancy, function contraindication 289908002
Peripheral nerve disease contraindication 302226006
Visual impairment contraindication 397540003
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Poor metabolizer due to cytochrome p450 CYP2C19 variant contraindication 424500005
Congenital long QT syndrome contraindication 442917000




🐶 Veterinary Drug Use

SpeciesUseRelation
Cats Dermatophytosis caused by Microsporum canis Indication

🐶 Veterinary products

ProductApplicantIngredients
Itrafungol Virbac AH Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.12 Basic
pKa2 5.0 Basic
pKa3 3.04 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
200MG ONMEL SEBELA IRELAND LTD N022484 April 29, 2010 DISCN TABLET ORAL 8486456 Oct. 3, 2028 ONYCHOMYCOSIS OF THE TOENAIL CAUSED BY TRICOPHYTON RUBRUM OR TRICHOPHYTON MENTAGROPHYTES, ONCE DAILY USE FOR 12 CONSECUTIVE WEEKS
65MG TOLSURA MAYNE PHARMA N208901 Dec. 11, 2018 RX CAPSULE ORAL 10463740 June 21, 2033 TREATMENT OF FUNGAL INFECTIONS, INCLUDING BLASTOMYCOSIS, HISTOPLASMOSIS, AND ASPERGILLOSIS
65MG TOLSURA MAYNE PHARMA N208901 Dec. 11, 2018 RX CAPSULE ORAL 9713642 June 21, 2033 TREATMENT OF FUNGAL INFECTIONS, INCLUDING BLASTOMYCOSIS, HISTOPLASMOSIS, AND ASPERGILLOSIS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Cytochrome P450 3A4 Enzyme IC50 6.05 DRUG MATRIX
ATP-binding cassette sub-family G member 2 Transporter IC50 5.70 CHEMBL
Vasopressin V2 receptor GPCR IC50 6.10 CHEMBL
Tyrosine-protein kinase Fyn Kinase IC50 5.41 DRUG MATRIX
Lanosterol 14-alpha demethylase Enzyme IC50 5.44 CHEMBL
C-C chemokine receptor type 4 GPCR IC50 6.70 CHEMBL
C-X-C chemokine receptor type 1 GPCR IC50 7 CHEMBL
Beta-2 adrenergic receptor GPCR Ki 6.30 CHEMBL
7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase Enzyme IC50 5.33 CHEMBL
Lanosterol 14-alpha demethylase Enzyme INHIBITOR MIC 9.25 WOMBAT-PK CHEMBL
Cruzipain Enzyme IC50 5.52 CHEMBL
14-alpha sterol demethylase Cyp51A Enzyme Kd 6 CHEMBL
14-alpha sterol demethylase Enzyme Kd 7.51 CHEMBL

External reference:

IDSource
4020560 VUID
N0000148264 NUI
D00350 KEGG_DRUG
4020560 VANDF
C0064113 UMLSCUI
CHEBI:6076 CHEBI
1YN PDB_CHEM_ID
CHEMBL64391 ChEMBL_ID
CHEMBL1711 ChEMBL_ID
D017964 MESH_DESCRIPTOR_UI
DB01167 DRUGBANK_ID
11426 IUPHAR_LIGAND_ID
5387 INN_ID
304NUG5GF4 UNII
55283 PUBCHEM_CID
28031 RXNORM
4940 MMSL
64593 MMSL
d00102 MMSL
003915 NDDF
387532006 SNOMEDCT_US
96038009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 10147-1700 CAPSULE 100 mg ORAL NDA 30 sections
Itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 13668-463 CAPSULE 100 mg ORAL ANDA 14 sections
Itraconazole Human Prescription Drug Label 1 16571-245 CAPSULE 100 mg ORAL ANDA 22 sections
Itraconazole Human Prescription Drug Label 1 16714-743 CAPSULE, COATED PELLETS 100 mg ORAL ANDA 21 sections
Itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 31722-006 SOLUTION 10 mg ORAL ANDA 14 sections
ITRACONAZOLE Human Prescription Drug Label 1 46708-204 CAPSULE 100 mg ORAL ANDA 22 sections
Itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 50268-450 CAPSULE 100 mg ORAL ANDA 13 sections
SPORANOX HUMAN PRESCRIPTION DRUG LABEL 1 50458-290 CAPSULE 100 mg ORAL NDA 29 sections
Tolsura HUMAN PRESCRIPTION DRUG LABEL 1 51862-462 CAPSULE, GELATIN COATED 65 mg ORAL NDA 34 sections
Itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 60687-299 CAPSULE 100 mg ORAL ANDA 24 sections
ITRACONAZOLE Human Prescription Drug Label 1 62332-204 CAPSULE 100 mg ORAL ANDA 22 sections
Itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 65162-087 SOLUTION 10 mg ORAL ANDA 22 sections
Itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 65162-630 CAPSULE 100 mg ORAL ANDA 13 sections
Itraconazole Human Prescription Drug Label 1 67877-454 CAPSULE, COATED PELLETS 100 mg ORAL ANDA 21 sections
itraconazole HUMAN PRESCRIPTION DRUG LABEL 1 68151-2718 CAPSULE 100 mg ORAL NDA 27 sections
Itraconazole Oral HUMAN PRESCRIPTION DRUG LABEL 1 69339-159 SOLUTION 10 mg ORAL ANDA 26 sections
CICLOPIROX 3% / ITRACONAZOLE 5% / UREA 20% HUMAN PRESCRIPTION DRUG LABEL 3 72934-2044 CREAM 5 g TOPICAL unapproved drug other 4 sections
FLUCONAZOLE 4% / IBUPROFEN 2% / ITRACONAZOLE 1% / TERBINAFINE HCL 4% HUMAN PRESCRIPTION DRUG LABEL 4 72934-4176 SOLUTION 1 g TOPICAL unapproved drug other 4 sections