Itraconazole
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1992
- First approval year
- 1992
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Itraconazole
- Molecular weight
- 705.65
- Structure (SMILES)
- CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O
- fungitraxx
- Fungitraxx
- itraconazole
- Itraconazole
- itraconazole component of suba
- Itraconazole component of suba-
- sporanox
- Sporanox
- sporanox i v
- Sporanox i.v.
- sporanox pulse
- Sporanox-pulse
- (±)-1-SEC-BUTYL-4-(P-(4-(P-(((2R*,4S*)-2-(2,4-DICHLOROPHENYL)-2-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-1,3-DIOXOLAN-4-YL)METHOXY)PHENYL)-1-PIPERAZINYL)PHENYL)-.DELTA.(SUP 2)-1,2,4-TRIAZOLIN-5-ONE
- 1 sec butyl 4 p 4 p 2r 4s 2 2 4 dichlorophenyl 2 1h 1 2 4 triazol 1 ylmethyl 1 3 dioxolan 4 yl methoxy phenyl 1 piperazinyl phenyl delta sup 2 1 2 4 triazolin 5 one
- 200 mg itraconazole
- 200 mg Itraconazole
- candistat
- Candistat
- canditral
- Canditral
- cladosal 100
- Cladosal 100
- fungitraxx
- Fungitraxx
- itrac
- Itrac
- itraconazol
- Itraconazol
- itraconazole
- Itraconazole
- Itraconazole (200 mg)
- Itraconazole (300 mg)
- ITRACONAZOLE (EMA EPAR: VETERINARY)
- Itraconazole (ITZ)
- itraconazole (Part 4)
- Itraconazole (Sporanox)
- ITRACONAZOLE [EP IMPURITY]
And 79 more, listed on the interactive page.
- ATC classification codes
- J02AC02
Sources for recorded values
- CAS registry numbers
- 84625-61-6
- ChEMBL ID
- CHEMBL64391
- InChIKey
- VHVPQPYKVGDNFY-UHFFFAOYSA-N
- RxNorm IDs (RxCUI)
- 28031
- FDA ingredient codes (UNII)
- 304NUG5GF4
- 3793
- 55283
- Applicant
- JANSSEN PHARMS
- Approval date
- 11 Sept 1992
- Application number
- NDA020083
- Patents
- 6
- Designations
- 4
- Earliest recorded loss of exclusivity
- 21 Jun 2033
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- itraconazole
- Type
- Synthetic organic
- Drug name stem
- -conazole
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
Mechanisms of action
- Mechanism
- Cytochrome P450 51 inhibitor
- Action type
- Inhibitor
- Target
- Lanosterol 14-alpha demethylase
- Protein identifier
- P10613
Open Targets mechanisms
- Mechanism
- Cytochrome P450 51 inhibitor
- Action type
- Inhibitor
- Target
- Lanosterol 14-alpha demethylase
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- ERG11
- Protein identifier
- P10613
- Organism
- Candida albicans (strain SC5314 / ATCC MYA-2876)
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Pulmonary Disease, Chronic Obstructive
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000341
- Subject identifier
- D029424
- Condition
- Crohn Disease
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000384
- Subject identifier
- D003424
- Condition
- Glioblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Infections
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000544
- Subject identifier
- D007239
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Polycystic Ovary Syndrome
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000660
- Subject identifier
- D011085
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Bacterial Infections
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000771
- Subject identifier
- D001424
- Condition
- Celiac Disease
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001060
- Subject identifier
- D002446
- Condition
- Malaria
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001068
- Subject identifier
- D008288
- Condition
- Obesity
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001073
- Subject identifier
- D009765
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Melanoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002617
- Subject identifier
- D008545
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Heart Failure
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003144
- Subject identifier
- D006333
- Condition
- Inflammatory Bowel Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003767
- Subject identifier
- D015212
- Condition
- Lung Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003818
- Subject identifier
- D008171
- Condition
- Pain
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003843
- Subject identifier
- D010146
- Condition
- Renal Insufficiency, Chronic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003884
- Subject identifier
- D051436
- Condition
- Carcinoma, Basal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004193
- Subject identifier
- D002280
- Condition
- Hepatitis B, Chronic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0004197
- Subject identifier
- D019694
- Condition
- Hepatitis C, Chronic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0004220
- Subject identifier
- D019698
And 44 more, listed on the interactive page.
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000660
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000764
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000771
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001060
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001073
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001075
- Condition identifier
- EFO_0002617
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003144
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003818
- Condition identifier
- EFO_0003884
- Highest recorded phase
- 1
- Condition identifier
- EFO_0004193
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004197
- Highest recorded phase
- 1
- Condition identifier
- EFO_0004234
- Highest recorded phase
- 1
- Condition identifier
- EFO_0004826
- Highest recorded phase
- 1
- Condition identifier
- EFO_0007140
- Highest recorded phase
- 3
- Condition identifier
- EFO_0007157
- Condition identifier
- EFO_0007174
- Condition identifier
- EFO_0007211
- Highest recorded phase
- 2
- Condition identifier
- EFO_0007265
- Highest recorded phase
- 2
- Condition identifier
- EFO_0007278
- Highest recorded phase
- 2
- Condition identifier
- EFO_0007310
And 76 more, listed on the interactive page.
Warnings
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
Open Targets warnings
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Country
- United States
- Event
- adrenal insufficiency
- Reports
- 35
- Reporting signal score
- 52.7303
- Event
- aspergillus infection
- Reports
- 31
- Reporting signal score
- 68.6959
- Event
- bronchopulmonary aspergillosis
- Reports
- 41
- Reporting signal score
- 93.7213
- Event
- cardiac failure
- Reports
- 93
- Reporting signal score
- 91.6577
- Event
- cardiotoxicity
- Reports
- 56
- Reporting signal score
- 122.442
- Event
- cushing's syndrome
- Reports
- 45
- Reporting signal score
- 112.151
- Event
- drug interaction
- Reports
- 479
- Reporting signal score
- 677.938
- Event
- drug resistance
- Reports
- 86
- Reporting signal score
- 131.058
- Event
- electrocardiogram qt prolonged
- Reports
- 74
- Reporting signal score
- 71.9923
- Event
- hepatic function abnormal
- Reports
- 83
- Reporting signal score
- 98.6403
- Event
- histoplasmosis
- Reports
- 30
- Reporting signal score
- 88.8457
- Event
- histoplasmosis disseminated
- Reports
- 32
- Reporting signal score
- 105.6
- Event
- hypokalaemia
- Reports
- 83
- Reporting signal score
- 78.898
- Event
- ileus paralytic
- Reports
- 39
- Reporting signal score
- 94.0089
- Event
- myopathy
- Reports
- 36
- Reporting signal score
- 57.0359
- Event
- neuropathy peripheral
- Reports
- 89
- Reporting signal score
- 50.7581
- Event
- oedema
- Reports
- 97
- Reporting signal score
- 106.919
- Event
- oedema peripheral
- Reports
- 111
- Reporting signal score
- 57.643
- Event
- pain
- Reports
- 17
- Reporting signal score
- 47.6455
- Event
- pathogen resistance
- Reports
- 46
- Reporting signal score
- 87.373
- Event
- pleural effusion
- Reports
- 68
- Reporting signal score
- 46.7783
- Event
- pseudohyponatraemia
- Reports
- 17
- Reporting signal score
- 82.3689
- Event
- rhabdomyolysis
- Reports
- 68
- Reporting signal score
- 50.806
- Event
- symmetrical drug-related intertriginous and flexural exanthema
- Reports
- 38
- Reporting signal score
- 159.742
- Event
- systemic mycosis
- Reports
- 22
- Reporting signal score
- 84.1425
- NCT00000992
- NCT00002159
- NCT00004811
- NCT00784368
- NCT00001280
- NCT00289991
- NCT00794703
- NCT01198236
- NCT03572049
- NCT03923010
- NCT04035187
- NCT04166669
- NCT00003883
- NCT01409018
- NCT03346837
- NCT05573724
- NCT06165822
- NCT00012467
- NCT00045942
- NCT05048615
- NCT00356915
- NCT00791219
- NCT05578950
- NCT06485505
- NCT00588016
And 104 more, listed on the interactive page.
- Dose
- 200 mg
- Route
- Oral
- How often
- Once daily
- Swallow whole
- Take with a full meal
- Hydrogen bond acceptors
- 12
- Hydrogen bond donors
- 0
- Polar surface area
- 104.7
- Calculated partition coefficient (ALogP)
- 5.58
- Calculated partition coefficient (XLogP)
- 5.7
- Prodrug
- No
- Chirality
- Racemic
- Inorganic
- No
- Rule-of-five violations
- 3
- Rotatable bonds
- 11
- Heavy atoms
- 49
- Molecular formula
- C35H38Cl2N8O4
- Monoisotopic mass
- 704.2393071
- Natural product
- Yes
- 13668-463
- 16571-245
- 16714-743
- 31722-006
- 46708-204
- 50268-450
- 50458-290
- 51862-462
- 60687-299
- 65162-087
- 65162-630
- 67877-454
- 69339-159
- 10147-1700
- Recorded assays
- 4,960
- Active assays
- 284
- Confirmatory
- Other
- Screening
- Antifungal Agents
- 14-alpha Demethylase Inhibitors
- Cytochrome P-450 CYP3A Inhibitors
These details could not be displayed.
Related records
Trials (561)
- A 2-Part Study to Assess Potential Metabolism-Based Drug-Drug Interactions of E2006 When Coadministered With Itraconazole, Rifampin, Midazolam, or Bupropion
- A 3-Part, Open-Label, Drug-Drug Interaction Study of Concomitant Administration of E2609 With Itraconazole, Rifampin, Digoxin, or Donepezil
- A Bioequivalence Study of the Fixed Dose Combination Tablets of Canagliflozin and Metformin Extended Release (XR) With Respect to the Individual Components
- A Bioequivalence Study of the Fixed Dose Combination Tablets of Canagliflozin and Metformin Extended Release (XR) With Respect to the Individual Components in Healthy Fed Participants
- A Clinical Drug-Drug Interaction (DDI) Study With Omaveloxolone
- A Clinical Study of MK-8527 in Healthy Participants (MK-8527-021)
- A Clinical Study of the Interactions Between Azvudine Tablets (FNC) and Itraconazole Capsules (ICZ)
- A Clinical Study to Evaluate the Pharmacokinetics of Lozanoc and Sporanox in Korean Healthy Male Volunteers
- A Clinical Study to Test if an Investigational Treatment Called BNT326 is Safe and Potentially Beneficial When Used Alone or in Combination With Other Investigational Treatments Such as BNT327, for People With Advanced Malignant Tumors
- A Clinical Trial in Healthy Participants to Learn How Itraconazole Affects MK-2828 Levels and How MK-2828 Affects Midazolam Levels (MK-2828-007)
- A Clinical Trial to Evaluate JAB-21822 Drug-drug Interactions in Healthy Subjects
- A Clinical Trial to Evaluate the Effect of Itraconazole and Rifampicin on ABSK021
- A Clinical Trial to Evaluate the Effects of Itraconazole or Rifampicin on the Pharmacokinetics of VC004 Capsules in Healthy Adult Subjects
- A Cross-over Study to Evaluate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics (PK) of GSK525762 in Healthy Female Subjects of Non Child Bearing Potential
- A Drug Interaction Study of ACH-0145228
- A Drug Interaction Study of GDC-0032 Co-administered With Rifampin or Itraconazole in Healthy Volunteers
- A Drug-Drug Interaction (DDI) Study of ADC189 With Itraconazole in Healthy, Adult Subjects
- A Drug-Drug Interaction (DDI) Study of HDM1002 With Rifampicin and Itraconazole in Healthy Subjects
- A Drug-Drug Interaction Study Between GDC-0853 and Midazolam, Itraconazole, Rosuvastatin, and Simvastatin
- A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib
Approved for (7)
- Aspergillosis
- Blastomycosis
- Candidiasis
- Fungal infectious disease
- Lung disorder
- Tinea infection
- Tinea unguium
In development for (59)
- Acute myeloid leukemia Phase 2
- Allergic bronchopulmonary aspergillosis Phase 3
- Alzheimer disease Phase 1
- Amyotrophic lateral sclerosis Phase 1
- Anti-neutrophil antibody associated vasculitis Phase 1
- Asthma Phase 1
- Bacterial infectious disease Phase 1
- Basal cell carcinoma Phase 2
- Bronchiectasis Phase 3
- Burn Phase 2
- Cancer Phase 3
- Celiac disease Phase 1
- Chronic hepatitis B virus infection Phase 1
- Chronic hepatitis C virus infection Phase 1
- Chronic kidney disease Phase 1
- Chronic obstructive pulmonary disease Phase 1
- Coccidioidomycosis Phase 2
- COVID-19 Phase 1
- Crohn disease Phase 2
- Cryptococcal meningitis Phase 2
Other linked conditions (4)
- Dermatophytosis of scalp or beard
- Meningitis
- Neutropenia
- Ovarian carcinoma