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Details

Stereochemistry MIXED
Molecular Formula C35H38Cl2N8O4
Molecular Weight 705.633
Optical Activity ( + / - )
Defined Stereocenters 2 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ITRACONAZOLE

SMILES

CCC(C)N1N=CN(C1=O)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(OC[C@H]5CO[C@@](CN6C=NC=N6)(O5)C7=C(Cl)C=C(Cl)C=C7)C=C4

InChI

InChIKey=VHVPQPYKVGDNFY-ZPGVKDDISA-N
InChI=1S/C35H38Cl2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3/t25?,31-,35-/m0/s1

HIDE SMILES / InChI

Molecular Formula C35H38Cl2N8O4
Molecular Weight 705.633
Charge 0
Count
Stereochemistry EPIMERIC
Additional Stereochemistry No
Defined Stereocenters 2 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

SPORANOX is the brand name for itraconazole, an azole antifungal agent. Itraconazole is a 1:1:1:1 racemic mixture of four diastereomers (two enantiomeric pairs), each possessing three chiral centers. In vitro studies have demonstrated that itraconazole inhibits the cytochrome P450-dependent synthesis of ergosterol, which is a vital component of fungal cell membranes. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Itraconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis. SPORANOX capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: Blastomycosis, pulmonary and extrapulmonary; Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, nonmeningeal histoplasmosis, and Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy. SPORANOX is also indicated for the treatment of the following fungal infections in non-immunocompromised patients: Onychomycosis of the toenail, with or without fingernail involvement, due to dermatophytes (tinea unguium), and Onychomycosis of the fingernail due to dermatophytes (tinea unguium). Itraconazole is mainly metabolized through CYP3A4. Other drugs that either share this metabolic pathway or modify CYP3A4 activity may influence the pharmacokinetics of itraconazole. Similarly, itraconazole may modify the pharmacokinetics of other drugs that share this metabolic pathway. Itraconazole is a potent CYP3A4 inhibitor and a P-glycoprotein inhibitor. When using concomitant medication, it is recommended that the corresponding label be consulted for information on the route of metabolism and the possible need to adjust dosages.

CNS Activity

Curator's Comment: Limited ability to cross the blood-brain barrier https://books.google.ru/books?id=Qd_nCAAAQBAJ&pg=PA198&lpg=PA198&dq=ITRACONAZOLE+cross+blood-brain+barrier&source=bl&ots=gExVhzS3wQ&sig=M2Vea-eTPaedoDjCOCqfNT-Ftu0&hl=ru&sa=X&ved=0ahUKEwi21cbW4PbPAhVGuhoKHXGhDk44ChDoAQgbMAA#v=onepage&q=ITRACONAZOLE%20cross%20blood-brain%20barrier&f=false

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
SPORANOX

Approved Use

SPORANOX® (itraconazole) Capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: Blastomycosis, pulmonary and extrapulmonary Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, non-meningeal histoplasmosis, and Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy. Specimens for fungal cultures and other relevant laboratory studies (wet mount, histopathology, serology) should be obtained before therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, antiinfective therapy should be adjusted accordingly. SPORANOX® Capsules are also indicated for the treatment of the following fungal infections in non-immunocompromised patients: Onychomycosis of the toenail, with or without fingernail involvement, due to dermatophytes (tinea unguium), and Onychomycosis of the fingernail due to dermatophytes (tinea unguium). Prior to initiating treatment, appropriate nail specimens for laboratory testing (KOH preparation, fungal culture, or nail biopsy) should be obtained to confirm the diagnosis of onychomycosis. (See CLINICAL PHARMACOLOGY: Special Populations, CONTRAINDICATIONS, WARNINGS, and ADVERSE REACTIONS: Post-marketing Experience for more information.) Description of Clinical Studies Blastomycosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=73 combined) in patients with normal or abnormal immune status. The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 6 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of blastomycosis compared with the natural history of untreated cases. Histoplasmosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=34 combined) in patients with normal or abnormal immune status (not including HIV-infected patients). The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 12 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of histoplasmosis, compared with the natural history of untreated cases. Histoplasmosis in HIV-infected patients Data from a small number of HIV-infected patients suggested that the response rate of histoplasmosis in HIV-infected patients is similar to that of non-HIV-infected patients. The clinical course of histoplasmosis in HIV-infected patients is more severe and usually requires maintenance therapy to prevent relapse. Aspergillosis Analyses were conducted on data from an open-label, single-patient-use protocol designed to make itraconazole available in the U.S. for patients who either failed or were intolerant of amphotericin B therapy (N=190). The findings were corroborated by two smaller open-label studies (N=31 combined) in the same patient population. Most adult patients were treated with a daily dose of 200 to 400 mg, with a median duration of 3 months. Results of these studies demonstrated substantial evidence of effectiveness of itraconazole as a second-line therapy for the treatment of aspergillosis compared with the natural history of the disease in patients who either failed or were intolerant of amphotericin B therapy. Onychomycosis of the toenail Analyses were conducted on data from three double-blind, placebo-controlled studies (N=214 total; 110 given SPORANOX® Capsules) in which patients with onychomycosis of the toenails received 200 mg of SPORANOX® Capsules once daily for 12 consecutive weeks. Results of these studies demonstrated mycologic cure, defined as simultaneous occurrence of negative KOH plus negative culture, in 54% of patients. Thirty-five percent (35%) of patients were considered an overall success (mycologic cure plus clear or minimal nail involvement with significantly decreased signs) and 14% of patients demonstrated mycologic cure plus clinical cure (clearance of all signs, with or without residual nail deformity). The mean time to overall success was approximately 10 months. Twenty-one percent (21%) of the overall success group had a relapse (worsening of the global score or conversion of KOH or culture from negative to positive). Onychomycosis of the fingernail Analyses were conducted on data from a double-blind, placebo-controlled study (N=73 total; 37 given SPORANOX® Capsules) in which patients with onychomycosis of the fingernails received a 1-week course (pulse) of 200 mg of SPORANOX® Capsules b.i.d., followed by a 3-week period without SPORANOX®, which was followed by a second 1-week pulse of 200 mg of SPORANOX® Capsules b.i.d. Results demonstrated mycologic cure in 61% of patients. Fifty-six percent (56%) of patients were considered an overall success and 47% of patients demonstrated mycologic cure plus clinical cure. The mean time to overall success was approximately 5 months. None of the patients who achieved overall success relapsed.

Launch Date

1992
Curative
SPORANOX

Approved Use

SPORANOX® (itraconazole) Capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: Blastomycosis, pulmonary and extrapulmonary Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, non-meningeal histoplasmosis, and Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy. Specimens for fungal cultures and other relevant laboratory studies (wet mount, histopathology, serology) should be obtained before therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, antiinfective therapy should be adjusted accordingly. SPORANOX® Capsules are also indicated for the treatment of the following fungal infections in non-immunocompromised patients: Onychomycosis of the toenail, with or without fingernail involvement, due to dermatophytes (tinea unguium), and Onychomycosis of the fingernail due to dermatophytes (tinea unguium). Prior to initiating treatment, appropriate nail specimens for laboratory testing (KOH preparation, fungal culture, or nail biopsy) should be obtained to confirm the diagnosis of onychomycosis. (See CLINICAL PHARMACOLOGY: Special Populations, CONTRAINDICATIONS, WARNINGS, and ADVERSE REACTIONS: Post-marketing Experience for more information.) Description of Clinical Studies Blastomycosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=73 combined) in patients with normal or abnormal immune status. The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 6 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of blastomycosis compared with the natural history of untreated cases. Histoplasmosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=34 combined) in patients with normal or abnormal immune status (not including HIV-infected patients). The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 12 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of histoplasmosis, compared with the natural history of untreated cases. Histoplasmosis in HIV-infected patients Data from a small number of HIV-infected patients suggested that the response rate of histoplasmosis in HIV-infected patients is similar to that of non-HIV-infected patients. The clinical course of histoplasmosis in HIV-infected patients is more severe and usually requires maintenance therapy to prevent relapse. Aspergillosis Analyses were conducted on data from an open-label, single-patient-use protocol designed to make itraconazole available in the U.S. for patients who either failed or were intolerant of amphotericin B therapy (N=190). The findings were corroborated by two smaller open-label studies (N=31 combined) in the same patient population. Most adult patients were treated with a daily dose of 200 to 400 mg, with a median duration of 3 months. Results of these studies demonstrated substantial evidence of effectiveness of itraconazole as a second-line therapy for the treatment of aspergillosis compared with the natural history of the disease in patients who either failed or were intolerant of amphotericin B therapy. Onychomycosis of the toenail Analyses were conducted on data from three double-blind, placebo-controlled studies (N=214 total; 110 given SPORANOX® Capsules) in which patients with onychomycosis of the toenails received 200 mg of SPORANOX® Capsules once daily for 12 consecutive weeks. Results of these studies demonstrated mycologic cure, defined as simultaneous occurrence of negative KOH plus negative culture, in 54% of patients. Thirty-five percent (35%) of patients were considered an overall success (mycologic cure plus clear or minimal nail involvement with significantly decreased signs) and 14% of patients demonstrated mycologic cure plus clinical cure (clearance of all signs, with or without residual nail deformity). The mean time to overall success was approximately 10 months. Twenty-one percent (21%) of the overall success group had a relapse (worsening of the global score or conversion of KOH or culture from negative to positive). Onychomycosis of the fingernail Analyses were conducted on data from a double-blind, placebo-controlled study (N=73 total; 37 given SPORANOX® Capsules) in which patients with onychomycosis of the fingernails received a 1-week course (pulse) of 200 mg of SPORANOX® Capsules b.i.d., followed by a 3-week period without SPORANOX®, which was followed by a second 1-week pulse of 200 mg of SPORANOX® Capsules b.i.d. Results demonstrated mycologic cure in 61% of patients. Fifty-six percent (56%) of patients were considered an overall success and 47% of patients demonstrated mycologic cure plus clinical cure. The mean time to overall success was approximately 5 months. None of the patients who achieved overall success relapsed.

Launch Date

1992
Curative
SPORANOX

Approved Use

SPORANOX® (itraconazole) Capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: Blastomycosis, pulmonary and extrapulmonary Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, non-meningeal histoplasmosis, and Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy. Specimens for fungal cultures and other relevant laboratory studies (wet mount, histopathology, serology) should be obtained before therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, antiinfective therapy should be adjusted accordingly. SPORANOX® Capsules are also indicated for the treatment of the following fungal infections in non-immunocompromised patients: Onychomycosis of the toenail, with or without fingernail involvement, due to dermatophytes (tinea unguium), and Onychomycosis of the fingernail due to dermatophytes (tinea unguium). Prior to initiating treatment, appropriate nail specimens for laboratory testing (KOH preparation, fungal culture, or nail biopsy) should be obtained to confirm the diagnosis of onychomycosis. (See CLINICAL PHARMACOLOGY: Special Populations, CONTRAINDICATIONS, WARNINGS, and ADVERSE REACTIONS: Post-marketing Experience for more information.) Description of Clinical Studies Blastomycosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=73 combined) in patients with normal or abnormal immune status. The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 6 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of blastomycosis compared with the natural history of untreated cases. Histoplasmosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=34 combined) in patients with normal or abnormal immune status (not including HIV-infected patients). The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 12 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of histoplasmosis, compared with the natural history of untreated cases. Histoplasmosis in HIV-infected patients Data from a small number of HIV-infected patients suggested that the response rate of histoplasmosis in HIV-infected patients is similar to that of non-HIV-infected patients. The clinical course of histoplasmosis in HIV-infected patients is more severe and usually requires maintenance therapy to prevent relapse. Aspergillosis Analyses were conducted on data from an open-label, single-patient-use protocol designed to make itraconazole available in the U.S. for patients who either failed or were intolerant of amphotericin B therapy (N=190). The findings were corroborated by two smaller open-label studies (N=31 combined) in the same patient population. Most adult patients were treated with a daily dose of 200 to 400 mg, with a median duration of 3 months. Results of these studies demonstrated substantial evidence of effectiveness of itraconazole as a second-line therapy for the treatment of aspergillosis compared with the natural history of the disease in patients who either failed or were intolerant of amphotericin B therapy. Onychomycosis of the toenail Analyses were conducted on data from three double-blind, placebo-controlled studies (N=214 total; 110 given SPORANOX® Capsules) in which patients with onychomycosis of the toenails received 200 mg of SPORANOX® Capsules once daily for 12 consecutive weeks. Results of these studies demonstrated mycologic cure, defined as simultaneous occurrence of negative KOH plus negative culture, in 54% of patients. Thirty-five percent (35%) of patients were considered an overall success (mycologic cure plus clear or minimal nail involvement with significantly decreased signs) and 14% of patients demonstrated mycologic cure plus clinical cure (clearance of all signs, with or without residual nail deformity). The mean time to overall success was approximately 10 months. Twenty-one percent (21%) of the overall success group had a relapse (worsening of the global score or conversion of KOH or culture from negative to positive). Onychomycosis of the fingernail Analyses were conducted on data from a double-blind, placebo-controlled study (N=73 total; 37 given SPORANOX® Capsules) in which patients with onychomycosis of the fingernails received a 1-week course (pulse) of 200 mg of SPORANOX® Capsules b.i.d., followed by a 3-week period without SPORANOX®, which was followed by a second 1-week pulse of 200 mg of SPORANOX® Capsules b.i.d. Results demonstrated mycologic cure in 61% of patients. Fifty-six percent (56%) of patients were considered an overall success and 47% of patients demonstrated mycologic cure plus clinical cure. The mean time to overall success was approximately 5 months. None of the patients who achieved overall success relapsed.

Launch Date

1992
Curative
SPORANOX

Approved Use

SPORANOX® (itraconazole) Capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: Blastomycosis, pulmonary and extrapulmonary Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, non-meningeal histoplasmosis, and Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy. Specimens for fungal cultures and other relevant laboratory studies (wet mount, histopathology, serology) should be obtained before therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, antiinfective therapy should be adjusted accordingly. SPORANOX® Capsules are also indicated for the treatment of the following fungal infections in non-immunocompromised patients: Onychomycosis of the toenail, with or without fingernail involvement, due to dermatophytes (tinea unguium), and Onychomycosis of the fingernail due to dermatophytes (tinea unguium). Prior to initiating treatment, appropriate nail specimens for laboratory testing (KOH preparation, fungal culture, or nail biopsy) should be obtained to confirm the diagnosis of onychomycosis. (See CLINICAL PHARMACOLOGY: Special Populations, CONTRAINDICATIONS, WARNINGS, and ADVERSE REACTIONS: Post-marketing Experience for more information.) Description of Clinical Studies Blastomycosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=73 combined) in patients with normal or abnormal immune status. The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 6 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of blastomycosis compared with the natural history of untreated cases. Histoplasmosis Analyses were conducted on data from two open-label, non-concurrently controlled studies (N=34 combined) in patients with normal or abnormal immune status (not including HIV-infected patients). The median dose was 200 mg/day. A response for most signs and symptoms was observed within the first 2 weeks, and all signs and symptoms cleared between 3 and 12 months. Results of these two studies demonstrated substantial evidence of the effectiveness of itraconazole for the treatment of histoplasmosis, compared with the natural history of untreated cases. Histoplasmosis in HIV-infected patients Data from a small number of HIV-infected patients suggested that the response rate of histoplasmosis in HIV-infected patients is similar to that of non-HIV-infected patients. The clinical course of histoplasmosis in HIV-infected patients is more severe and usually requires maintenance therapy to prevent relapse. Aspergillosis Analyses were conducted on data from an open-label, single-patient-use protocol designed to make itraconazole available in the U.S. for patients who either failed or were intolerant of amphotericin B therapy (N=190). The findings were corroborated by two smaller open-label studies (N=31 combined) in the same patient population. Most adult patients were treated with a daily dose of 200 to 400 mg, with a median duration of 3 months. Results of these studies demonstrated substantial evidence of effectiveness of itraconazole as a second-line therapy for the treatment of aspergillosis compared with the natural history of the disease in patients who either failed or were intolerant of amphotericin B therapy. Onychomycosis of the toenail Analyses were conducted on data from three double-blind, placebo-controlled studies (N=214 total; 110 given SPORANOX® Capsules) in which patients with onychomycosis of the toenails received 200 mg of SPORANOX® Capsules once daily for 12 consecutive weeks. Results of these studies demonstrated mycologic cure, defined as simultaneous occurrence of negative KOH plus negative culture, in 54% of patients. Thirty-five percent (35%) of patients were considered an overall success (mycologic cure plus clear or minimal nail involvement with significantly decreased signs) and 14% of patients demonstrated mycologic cure plus clinical cure (clearance of all signs, with or without residual nail deformity). The mean time to overall success was approximately 10 months. Twenty-one percent (21%) of the overall success group had a relapse (worsening of the global score or conversion of KOH or culture from negative to positive). Onychomycosis of the fingernail Analyses were conducted on data from a double-blind, placebo-controlled study (N=73 total; 37 given SPORANOX® Capsules) in which patients with onychomycosis of the fingernails received a 1-week course (pulse) of 200 mg of SPORANOX® Capsules b.i.d., followed by a 3-week period without SPORANOX®, which was followed by a second 1-week pulse of 200 mg of SPORANOX® Capsules b.i.d. Results demonstrated mycologic cure in 61% of patients. Fifty-six percent (56%) of patients were considered an overall success and 47% of patients demonstrated mycologic cure plus clinical cure. The mean time to overall success was approximately 5 months. None of the patients who achieved overall success relapsed.

Launch Date

1992
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
658.1 ng/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
116.8 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
213 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
162 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
332 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
974.2 ng/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
221.7 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
264 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
9046.81 ng × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
905.09 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3.34 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
2.27 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7.05 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
19054.95 ng × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
2538.33 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
4.58 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
36.84 h
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
36.84 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
20.06 h
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
20.06 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.2%
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
0.2%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
0.2%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
0.2%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.5%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
0.5%
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
0.5%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
0.5%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROXYITRACONAZOLE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
2.5 mg/kg single, intravenous
Dose: 2.5 mg/kg
Route: intravenous
Route: single
Dose: 2.5 mg/kg
Sources:
unhealthy, 0.5 - 16 years
n = 33
Health Status: unhealthy
Condition: risk for fungal infection
Age Group: 0.5 - 16 years
Sex: M+F
Population Size: 33
Sources:
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Co-administed with::
hydroxypropyl-beta-cyclodextrin(0.1 g/kg)
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Other AEs: Depression...
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Other AEs: Nausea, Diarrhea...
Other AEs:
Nausea (11%)
Diarrhea (11%)
Vomiting (7%)
Abdominal pain (6%)
Constipation (2%)
Fever (7%)
Chest pain (3%)
Pain (2%)
Fatigue (2%)
Coughing (4%)
Dyspnea (2%)
Pneumonia (2%)
Sinusitis (2%)
Sputum increased (2%)
Rash (4%)
Sweating increased (3%)
Skin and subcutaneous tissue disorders (2%)
Headache (4%)
Dizziness (2%)
Pneumocystis carinii infection (2%)
Sources:
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: tinea
Age Group: adult
Sex: unknown
Sources:
AEs

AEs

AESignificanceDosePopulation
Depression 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Co-administed with::
hydroxypropyl-beta-cyclodextrin(0.1 g/kg)
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Diarrhea 11%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Nausea 11%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Constipation 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Dizziness 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Dyspnea 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Fatigue 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Pain 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Pneumocystis carinii infection 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Pneumonia 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Sinusitis 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Skin and subcutaneous tissue disorders 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Sputum increased 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Chest pain 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Sweating increased 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Coughing 4%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Headache 4%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Rash 4%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Abdominal pain 6%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Fever 7%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Vomiting 7%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 350
Health Status: unhealthy
Condition: HIV and oropharyngeal or esophageal candidiasis
Age Group: adult
Sex: unknown
Population Size: 350
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
strong [IC50 0.0004 uM]
strong [IC50 0.007 uM]
strong [IC50 0.0326 uM]
yes (co-administration study)
strong [IC50 2 uM]
strong [IC50 2 uM]
strong [IC50 2 uM]
weak (co-administration study)
Comment: Itraconazole increased the mean area under the plasma concentration-time curve [AUC (0-9)] of morphine by 29% (P=0.002), its AUC (0-48) by 22% (P=0.013) and its peak plasma concentration by 28%
strong [Ki 0.0144 uM]
yes [IC50 >10 uM]
yes [IC50 >10 uM]
yes
Drug as victim
PubMed

PubMed

TitleDatePubMed
Severe cholestasis related to intraconazole for the treatment of onychomycosis.
1999 Dec
[Itraconazole-induced hypokalemia in a patient with pulmonary aspergilloma].
1999 Jan
Randomized double-blind comparison of short-term itraconazole and terbinafine therapy for toenail onychomycosis.
1999 May
In vitro antifungal activity of BMS-207147 and itraconazole against yeast strains that are non-susceptible to fluconazole.
1999 Oct
[New antifungal drugs. Present and future].
1999 Sep
In vitro and in vivo activities of SCH 56592 (posaconazole), a new triazole antifungal agent, against Aspergillus and Candida.
2000 Aug
In vitro activities of a new lipopeptide antifungal agent, FK463, against a variety of clinically important fungi.
2000 Jan
Synergy between 6-amino-2-n-pentylthiobenzothiazole and ergosterol biosynthesis-inhibiting antimycotics against Candida albicans in vitro.
2000 Jul
In vitro antifungal activity of a novel lipopeptide antifungal agent, FK463, against various fungal pathogens.
2000 Oct
Clinical activity of the new triazole drug voriconazole (UK 109, 496) against disseminated hepatosplenic aspergillosis in a patient with relapsed leukemia.
2001
Penicillium marneffei: types and drug susceptibility.
2001
Hydrocortisone, prednisolone and dexamethasone act on Aspergillus fumigatus in vitro susceptibility to itraconazole.
2001
Clinical experience with itraconazole in systemic fungal infections.
2001
Pharmacology of itraconazole.
2001
Current management of fungal infections.
2001
Effect of clarithromycin and itraconazole on the pharmacokinetics of ropivacaine.
2001 Apr
Subcutaneous phaeohyphomycotic cysts caused by Exophiala jeanselmei in a lung transplant patient.
2001 Apr
Enhanced cyclosporine-itraconazole interaction with cola in lung transplant recipients.
2001 Apr
Phaeohyphomycosis due to Cladosporium cladosporioides.
2001 Feb
Successful treatment of Paecilomyces lilacinus endophthalmitis after foreign body trauma to the cornea.
2001 Jan
Systemic antifungal therapy.
2001 Jan
Clinical aspects of chronic granulomatous disease.
2001 Jan
Long-term follow-up study of onychomycosis: cure rate and dropout rate with oral antifungal treatments.
2001 Mar
Oral antifungals as prophylaxis in haematological malignancy.
2001 Mar
Malassezia pachydermatis fungaemia in a neonatal intensive care unit.
2001 Mar
Impending rupture in an aortic arch aneurysm by Candida infection.
2001 Mar
Efficacy of maintenance therapy with topical boric acid in comparison with oral itraconazole in the treatment of recurrent vulvovaginal candidiasis.
2001 Mar
Itraconazole-enhanced vincristine neurotoxicity in a child with acute lymphoblastic leukemia.
2001 Mar
Blastomycosis of the petrous apex.
2001 Mar
Acquired itraconazole resistance in Aspergillus fumigatus.
2001 Mar
Single-blind, randomized, prospective study on terbinafine and itraconazole for treatment of dermatophyte toenail onychomycosis in the elderly.
2001 Mar
Quantitation of itraconazole in rat heparinized plasma by liquid chromatography-mass spectrometry.
2001 Mar 5
Patents

Sample Use Guides

Blastomycosis and Histoplasmosis: The recommended dose is 200 mg once daily (2 capsules). If there is no obvious improvement, or there is evidence of progressive fungal disease, the dose should be increased in 100-mg increments to a maximum of 400 mg daily. Doses above 200 mg/day should be given in two divided doses. Aspergillosis: A daily dose of 200 to 400 mg is recommended. Treatment in Life-Threatening Situations: In life-threatening situations, a loading dose should be used. Although clinical studies did not provide for a loading dose, it is recommended, based on pharmacokinetic data, that a loading dose of 200 mg (2 capsules) three times daily (600 mg/day) be given for the first 3 days of treatment. Onychomycosis: Toenails with or without fingernail involvement: The recommended dose is 200 mg (2 capsules) once daily for 12 consecutive weeks. Onychomycosis: Fingernails only: The recommended dosing regimen is 2 treatment pulses, each consisting of 200 mg (2 capsules) b.i.d. (400 mg/day) for 1 week.
Route of Administration: Oral
The growth inhibition effects of different concentrations of itraconazole ITC (2, 6, 15 µmol/L) was detected by CCK8 assay in KG1α and primary adult acute leukemia cells. Different concentrations of ITC for 7, 14 and 21 days were applied for observing the effect on colony formation. After 48 h treatments with 6 µmol/L ITC the morphological changes of cells were observed by Wright staining.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:06:52 GMT 2023
Edited
by admin
on Fri Dec 15 16:06:52 GMT 2023
Record UNII
304NUG5GF4
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ITRACONAZOLE
EP   INCI   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
INCI   USAN   INN  
Official Name English
SUBA-ITRACONAZOLE COMPONENT ITRACONAZOLE
Common Name English
ITRACONAZOLE [USAN]
Common Name English
ITRACONAZOLE [INCI]
Common Name English
SPORANOX
Brand Name English
ORUNGAL
Brand Name English
ITRALEK
Brand Name English
ITRACONAZOLE (EMA EPAR: VETERINARY)
Common Name English
ITRACONAZOLE [ORANGE BOOK]
Common Name English
FUNGITRAXX
Brand Name English
CANDISTAT
Brand Name English
3H-1,2,4-TRIAZOL-3-ONE, 4-(4-(4-(4-((2-(2,4-DICHLOROPHENYL)-2-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-1,3-DIOXOLAN-4-YL)METHOXY)PHENYL)-1-PIPERAZINYL)PHENYL)-2,4-DIHYDRO-2-(1-METHYLPROPYL)-
Systematic Name English
SPORAMELT
Brand Name English
ITRACONAZOLE [MART.]
Common Name English
SEMPERA
Brand Name English
ITRIZOLE
Brand Name English
SPORONOX
Brand Name English
SPHERAZOLE CR
Brand Name English
NSC-759239
Code English
ITRACONAZOLE [EP IMPURITY]
Common Name English
ITRACONAZOLE [EP MONOGRAPH]
Common Name English
ITRACONAZOLE [VANDF]
Common Name English
CLADOSAL 100
Brand Name English
TRACONAL
Brand Name English
ITRACONAZOLE [USP-RS]
Common Name English
ITRACONAZOLE [JAN]
Common Name English
R 51,211
Code English
R-51211
Code English
(±)-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
Common Name English
ITRACONAZOLE COMPONENT OF SUBA-ITRACONAZOLE
Common Name English
SPHERAZOLE IR
Brand Name English
itraconazole [INN]
Common Name English
TRIASPORIN
Brand Name English
ITRACONAZOLE [USP MONOGRAPH]
Common Name English
Itraconazole [WHO-DD]
Common Name English
CANDITRAL
Brand Name English
ITRACONAZOLE [GREEN BOOK]
Common Name English
ITRAC
Brand Name English
ITRACONAZOLE [MI]
Common Name English
Classification Tree Code System Code
WHO-VATC QJ02AC02
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
NCI_THESAURUS C514
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
EMA VETERINARY ASSESSMENT REPORTS FUNGITRAXX (AUTHORISED)
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
FDA ORPHAN DRUG 781320
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
FDA ORPHAN DRUG 509515
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
WHO-ATC J02AC02
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
NDF-RT N0000008217
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
LIVERTOX NBK548273
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
EU-Orphan Drug EU/3/17/1901
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
FDA ORPHAN DRUG 257308
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
FDA ORPHAN DRUG 473715
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
NDF-RT N0000175487
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
Code System Code Type Description
SMS_ID
100000091697
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
MERCK INDEX
m6562
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY Merck Index
CAS
84604-65-9
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
ALTERNATIVE
DRUG CENTRAL
1513
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
CHEBI
6076
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
NDF-RT
N0000185503
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY P-Glycoprotein Inhibitors [MoA]
ChEMBL
CHEMBL22587
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
FDA UNII
304NUG5GF4
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
PUBCHEM
55283
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
NCI_THESAURUS
C1138
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
LACTMED
Itraconazole
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
CAS
84625-61-6
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
HSDB
7839
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
DAILYMED
304NUG5GF4
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
RS_ITEM_NUM
1354251
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
WIKIPEDIA
ITRACONAZOLE
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
NSC
759239
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
USAN
U-56
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
RXCUI
28031
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY RxNorm
INN
5387
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
EVMPD
SUB08353MIG
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
DRUG BANK
DB01167
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
EPA CompTox
DTXSID3023180
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
MESH
D017964
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY
NDF-RT
N0000182141
Created by admin on Fri Dec 15 16:06:52 GMT 2023 , Edited by admin on Fri Dec 15 16:06:52 GMT 2023
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
Related Record Type Details
TARGET ORGANISM->INHIBITOR
TRANSPORTER -> SUBSTRATE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
USP
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
STRONG
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
EP
TARGET ORGANISM->INHIBITOR
TARGET ORGANISM->INHIBITOR
SALT/SOLVATE -> PARENT
Related Record Type Details
METABOLITE ACTIVE -> PARENT
MAJOR
METABOLITE ACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
Sum of impurities C and D: not more than 0.3 percent peak area.
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
sum of impurities C and D: not more than 0.3 percent peak area
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC