Page last updated: 2024-12-07
hydroxyitraconazole
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
hydroxyitraconazole: a hydroxylated metabolite of itraconazole; likely contributes importantly to the in vivo activity attributed to itraconazole [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 108222 |
SCHEMBL ID | 8507377 |
MeSH ID | M0225215 |
Synonyms (24)
Synonym |
---|
hydroxyitraconazole |
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-(2-hydroxy-1-methylpropyl)-3h-1,2,4-triazol-3-one |
FT-0669698 |
4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-(3-hydroxybutan-2-yl)-1,2,4-triazol-3-one |
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)-, monohydroxy deriv. |
112559-91-8 |
r 63373 |
hydroxy itraconazole |
SCHEMBL8507377 |
HY-12772 |
AKOS025394152 |
itraconazole metabolite hydroxy itraconazole |
NCGC00485971-01 |
4-(4-{4-[4-({2-(2,4-dichlorophenyl)-2-[(1h-1,2,4-triazol-1-yl)methyl]-1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-(3-hydroxybutan-2-yl)-2,4-dihydro-3h-1,2,4-triazol-3-one |
DTXSID00920835 |
4-(4-(4-(4-((2-((1h-1,2,4-triazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-(3-hydroxybutan-2-yl)-2,4-dihydro-3h-1,2,4-triazol-3-one |
hydroxy itraconazole;r-63373 |
148626-66-8 |
BCP08597 |
hydroxyitraconazole; r 63373; r-63373; r63373;itraconazole metabolite hydroxy itraconazole |
4-[4-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2r,3r)-3-hydroxybutan-2-yl]-1,2,4-triazol-3-one |
F85153 |
A894570 |
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-(2-hydroxy-1-methylpropyl)- |
Research Excerpts
Pharmacokinetics
The authors describe the development of a population pharmacokinetic model using NONMEM for itraconazole and its active metabolite hydroxyitraconAZole in a Thai cohort of HIV-infected patients.
Compound-Compound Interactions
Excerpt | Reference | Relevance |
---|---|---|
"We describe a drug-drug interaction between coformulated lopinavir/ritonavir and itraconazole in a patient infected with human immunodeficiency virus type 1 who had disseminated histoplasmosis." | ( Drug-drug interaction between itraconazole and the antiretroviral drug lopinavir/ritonavir in an HIV-1-infected patient with disseminated histoplasmosis. Beijnen, JH; Crommentuyn, KM; Huitema, AD; Mulder, JW; Schellens, JH; Sparidans, RW, 2004) | 0.32 |
Bioavailability
Dosage Studied
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Bioassays (5)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (84)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 22 (26.19) | 18.2507 |
2000's | 35 (41.67) | 29.6817 |
2010's | 20 (23.81) | 24.3611 |
2020's | 7 (8.33) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 21.39
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.39) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 29 (33.33%) | 5.53% |
Reviews | 1 (1.15%) | 6.00% |
Case Studies | 2 (2.30%) | 4.05% |
Observational | 1 (1.15%) | 0.25% |
Other | 54 (62.07%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Clinical Trials (26)
Trial Overview
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Phase III Randomized, Evaluator-Blind, Parallel Group Study of the Safety and Efficacy of Itraconazole Tablets, Itraconazole Capsules and Placebo in the Treatment of Onychomycosis of the Toenail. [NCT00356915] | Phase 3 | 1,381 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
A Phase I, Open-label, Single-center Study to Assess the Effect of the CYP3A4 Inhibitor Itraconazole and the CYP2C19 Inhibitor Fluconazole on the Pharmacokinetics of a 25 mg Single Oral Dose of Selumetinib (AZD6244; ARRY-142866) ( Hyd-Sulfate) in Healthy [NCT02093728] | Phase 1 | 26 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
A Phase 1, Open-Label, Fixed-Sequence 2-Period Study To Investigate The Effect Of Multiple Doses Of Itraconazole On The Single Dose Pharmacokinetics of Palbociclib (PD-0332991) In Healthy Volunteers [NCT02131298] | Phase 1 | 12 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
An Open Labe Study to Evaluate the Drug-Drug Interaction of Itraconazole, Rifampicin and Midazolam With SIM0417/Ritonavir in Healthy Adult Chinese Participants [NCT05665647] | Phase 1 | 36 participants (Actual) | Interventional | 2022-12-29 | Completed | ||
Risk of QT-prolongation and Torsade de Pointes in Patients Treated With Acute Medication in a University Hospital [NCT02068170] | 178 participants (Actual) | Observational | 2014-02-28 | Completed | |||
Interventional, Open-label, One-sequence Crossover Study to Evaluate the Effect of Multiple Doses of Itraconazole (Inhibitor of CYP3A4/5) on the Multiple Dose Pharmacokinetics of Lu AE58054 in Healthy Subjects [NCT02122692] | Phase 1 | 20 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
A Phase I Study to Assess the Effect of Itraconazole and Rifampicin on Pharmacokinetics Profile of BPI-7711 in Chinese Healthy Volunteers [NCT04135833] | Phase 1 | 31 participants (Actual) | Interventional | 2019-12-12 | Completed | ||
Interventional, Open-label, One-sequence Crossover Study Evaluating the Effect of Multiple Doses of Itraconazole (Inhibitor of CYP3A4/5) on the Pharmacokinetics, Safety and Tolerability of Lu AF35700 in Healthy Young Men and Women [NCT03103646] | Phase 1 | 22 participants (Actual) | Interventional | 2017-03-28 | Completed | ||
A Phase 1, Open Label, Two Period, Fixed Sequence, Parallel Group Study To Estimate The Effects Of Multiple Dose Administration Of Itraconazole On The Single Dose Pharmacokinetics Of Conjugated Estrogens/Bazedoxifene In Non Obese (Bmi <30 Kg/m2) And Obese [NCT02100553] | Phase 1 | 24 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
SUBA-itraconazole Versus Conventional Itraconazole in the Treatment of Endemic Mycoses: a Multi-center, Open-label Comparative Trial [NCT03572049] | Phase 2/Phase 3 | 88 participants (Actual) | Interventional | 2018-09-17 | Completed | ||
Efficacy and Safety of Terbinafine and Itraconazole Monotherapy in Conventional and Increased Doses and in Combination in Dermatophytosis [NCT05881980] | Phase 2/Phase 3 | 150 participants (Anticipated) | Interventional | 2023-05-31 | Not yet recruiting | ||
Clinical Evaluation of a Formulated Nanoemulsion for Topical Application [NCT04110834] | Phase 2 | 30 participants (Actual) | Interventional | 2018-02-15 | Completed | ||
Evaluation of the Response of Itraconazole and Terbinafine Therapy in Subjects With Crohn's Disease Not Responding Adequately to Current Therapy [NCT05049525] | Phase 2 | 68 participants (Anticipated) | Interventional | 2022-02-22 | Recruiting | ||
Pharmacokinetics of Itraconazole in Pediatric Cancer Patients [NCT01409018] | Phase 1 | 6 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Phase 1 Study of the Effects of Itraconazole on the Pharmacokinetics of ALKS 5461 in Healthy Volunteers [NCT02272764] | Phase 1 | 24 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
Steady-State Comparative Bioavailability Study in Patients Requiring Anti-Fungal Prophylaxis Comparing Twice a Day Dosing of Lozanoc® (Mayne) Regardless of Food With Sporanox® (Janssen) Under Fed Conditions [NCT02621905] | Phase 4 | 40 participants (Actual) | Interventional | 2015-11-30 | Completed | ||
A Randomized Controlled Trial to Compare Oral Itraconazole Versus Combination of Systemic Glucorticoids and Oral Itraconazole in Chronic Pulmonary and Allergic Bronchopulmonary Aspergillosis Overlap Syndrome [NCT05444946] | 104 participants (Anticipated) | Interventional | 2022-06-15 | Recruiting | |||
Effect of Itraconazole on the Pharmacokinetics of Apatinib in Chinese Healthy Volunteers [NCT02836171] | Phase 1 | 20 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
Prediction of Itraconazole Oral Absorption From In Vitro Dissolution [NCT04035187] | Phase 4 | 17 participants (Actual) | Interventional | 2020-02-10 | Completed | ||
A Randomized, Double Blind, Multiple-site, Placebo-Controlled Study, Comparing the Efficacy and Safety of SUBA™-Itraconazole Capsules Compared to SPORANOX® (Itraconazole) Capsules in the Treatment of Onychomycosis of the Toenail [NCT00791219] | Phase 2 | 175 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
A Single-center, Open, Self-controlled Design Clinical Study to Evaluate the Pharmacokinetic Effects of Rifampicin or Itraconazole on Single-dose Laolotinib Mesylate Capsules in Healthy Subjects [NCT05057949] | Phase 1 | 32 participants (Anticipated) | Interventional | 2021-11-24 | Active, not recruiting | ||
A 4-Part Phase 1 Study to Evaluate the Effect of GDC-0853 on the Pharmacokinetics of Midazolam, Rosuvastatin, and Simvastatin and the Effect of Itraconazole on the Pharmacokinetics of GDC-0853 [NCT03174041] | Phase 1 | 63 participants (Actual) | Interventional | 2017-04-18 | Completed | ||
A Randomized Phase II Clinical Trial of Two Dose-levels of Itraconazole in Patients With Metastatic Castration-resistant Prostate Cancer [NCT00887458] | Phase 2 | 46 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Itraconazole Repurposing to Reduce Residual Cancer Risk in Patients With High-risk Barrett's Esophagus After Ablation [NCT05609253] | Phase 1 | 10 participants (Anticipated) | Interventional | 2022-09-14 | Recruiting | ||
A Randomized Phase II Study of SUBATM-itraconazole With Cisplatin/Gemcitabine in Patients With Previously Untreated Metastatic Squamous Non-Small Cell Lung Cancer. [NCT01752023] | Phase 2 | 3 participants (Actual) | Interventional | 2013-03-31 | Terminated(stopped due to Low Accrual) | ||
Phase 1, 3-Part, Open-Label Study to Assess Safety, Tolerability and PK of Single and Multiple Doses of PUR1900 in Healthy Subjects and Crossover Study of Single Doses of PUR1900 and Sporanox in Adult Subjects With Mild to Moderate Asthma [NCT03479411] | Phase 1 | 58 participants (Actual) | Interventional | 2018-02-09 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |