hydroxyitraconazole profile

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]

ID Source	ID
PubMed CID	108222
SCHEMBL ID	8507377
MeSH ID	M0225215

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)-

Excerpt	Reference	Relevance
" The coadministration of rifampin resulted in a 18 fold decrease of the Cmax of itraconazole [from 113."	( [Pharmacokinetic interaction between itraconazole and rifampin in Yucatan miniature pigs]. Cavalier, A; Elkhaili, H; Jehl, F; Kaltenbach, G; Levêque, D; Monteil, H; Peter, JD; Salmon, J; Salmon, Y, 1996)	0.29
" Pharmacokinetic parameters determined at days 1 and 14 (the area under the concentration-time curve from 0 to 10 h, the maximum concentration of drug in plasma [Cmax], and the time to Cmax) were comparable in both groups."	( Pharmacokinetics of itraconazole (oral solution) in two groups of human immunodeficiency virus-infected adults with oral candidiasis. Ajana, F; Bazin, C; Chwetzoff, E; Datry, A; Le Moing, JP; Levron, JC; Reynes, J, 1997)	0.3
" At steady state, mean bioavailabilities were 29% and 17% higher, respectively, in the fasted state; terminal half-life was similar under fasted and fed conditions (mean 39."	( Food interaction and steady-state pharmacokinetics of itraconazole oral solution in healthy volunteers. Barone, JA; Bierman, RH; Colaizzi, JL; Guarnieri, J; Hassell, AE; Jessen, L; Moskovitz, BL, )	0.13
" Plasma cortisol concentrations were determined as a pharmacodynamic index."	( Effect of itraconazole on the pharmacokinetics of prednisolone and methylprednisolone and cortisol secretion in healthy subjects. Archer, VC; Chosidow, O; Diquet, B; Lebrun-Vignes, B; Levron, JC; Puech, AJ; Warot, D, 2001)	0.31
" The pharmacokinetic interaction between methylprednisolone and itraconazole is probably related to inhibition of hepatic CYP3A4 activity by itraconazole."	( Effect of itraconazole on the pharmacokinetics of prednisolone and methylprednisolone and cortisol secretion in healthy subjects. Archer, VC; Chosidow, O; Diquet, B; Lebrun-Vignes, B; Levron, JC; Puech, AJ; Warot, D, 2001)	0.31
"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 who were using itraconazole as an addition to their antiretroviral therapy."	( Population pharmacokinetics of itraconazole in Thai HIV-1-infected persons. Beijnen, JH; Chuenyam, T; Huitema, AD; Koks, CH; Kroon, ED; Lange, JM; Sparidans, RW, 2003)	0.52
"We determined the steady-state intrapulmonary pharmacokinetic and pharmacodynamic parameters of orally administered itraconazole (ITRA), 200 mg every 12 h (twice a day [b."	( Intrapulmonary pharmacokinetics and pharmacodynamics of itraconazole and 14-hydroxyitraconazole at steady state. Conte, JE; Golden, JA; Kipps, J; McIver, M; Zurlinden, E, 2004)	0.55
"The objective of the study was to characterise the population pharmacokinetic properties of itraconazole and its active metabolite hydroxy-itraconazole in a representative paediatric population of cystic fibrosis and bone marrow transplant (BMT) patients and to identify patient characteristics influencing the pharmacokinetics of itraconazole."	( Population pharmacokinetics of itraconazole and its active metabolite hydroxy-itraconazole in paediatric cystic fibrosis and bone marrow transplant patients. Bell, SC; Charles, BG; Friberg, LE; Hennig, S; Miller, H; Wainwright, CE, 2006)	0.33
"The developed population pharmacokinetic model adequately described the pharmacokinetics of itraconazole and its active metabolite, hydroxy-itraconazole, in paediatric patients with either cystic fibrosis or undergoing BMT."	( Population pharmacokinetics of itraconazole and its active metabolite hydroxy-itraconazole in paediatric cystic fibrosis and bone marrow transplant patients. Bell, SC; Charles, BG; Friberg, LE; Hennig, S; Miller, H; Wainwright, CE, 2006)	0.33
"Itraconazole is a potent inhibitor of cytochrome P450 (CYP) 3A with an elimination half-life of more than 30 hours."	( Pharmacokinetic modeling of the dosing interval dependency for the interaction between itraconazole and triazolam. Ohtani, H; Sawada, Y; Toi, A; Tsujimoto, M, 2010)	0.36
"We developed a pharmacokinetic model based on the assumption that both itraconazole and hydroxyitraconazole competitively and reversibly inhibit the first-pass metabolism and systemic elimination of triazolam."	( Pharmacokinetic modeling of the dosing interval dependency for the interaction between itraconazole and triazolam. Ohtani, H; Sawada, Y; Toi, A; Tsujimoto, M, 2010)	0.58
" This study aimed to develop a population pharmacokinetic model for itraconazole and the active metabolite hydroxyitraconazole, in particular, quantifying the effects of food and formulation on oral absorption."	( Population pharmacokinetic modeling of itraconazole and hydroxyitraconazole for oral SUBA-itraconazole and sporanox capsule formulations in healthy subjects in fed and fasted states. Abuhelwa, AY; Foster, DJ; Hayes, D; Mudge, S; Upton, RN, 2015)	0.88

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

Excerpt	Reference	Relevance
" Variable interpatient bioavailability and detrimental drug interactions with p450 enzyme-inducing agents are well documented."	( Bioassay for serum itraconazole concentrations using hydroxyitraconazole standards. Denning, DW; Law, D; Moore, CB, 1994)	0.54
" In conclusion, the oral solution of itraconazole generates effective levels in plasma and saliva in HIV-infected patients; its relative bioavailability is not modified by the stage of HIV infection."	( Pharmacokinetics of itraconazole (oral solution) in two groups of human immunodeficiency virus-infected adults with oral candidiasis. Ajana, F; Bazin, C; Chwetzoff, E; Datry, A; Le Moing, JP; Levron, JC; Reynes, J, 1997)	0.3
" The oral bioavailability of the solubilizer hydroxypropyl-beta-cyclodextrin was less than 1% in the majority of the patients."	( Repeated-dose pharmacokinetics of an oral solution of itraconazole in infants and children. Cornu, G; De Beule, K; de Repentigny, L; Jacqmin, P; Leclerc, JM; Ratelle, J; Sokal, EM, 1998)	0.3
"To evaluate the effect of food on the bioavailability of itraconazole (ITR) hydroxypropyl-beta-cyclodextrin (HP-beta-CD) solution under multiple-dose to steady-state conditions, and to determine the pharmacokinetics of ITR solution at steady state."	( Food interaction and steady-state pharmacokinetics of itraconazole oral solution in healthy volunteers. Barone, JA; Bierman, RH; Colaizzi, JL; Guarnieri, J; Hassell, AE; Jessen, L; Moskovitz, BL, )	0.13
"The bioavailability of ITR and OH-ITR is enhanced when ITR oral solution is given in the fasted state; this was true for both single and multiple dosing to steady state."	( Food interaction and steady-state pharmacokinetics of itraconazole oral solution in healthy volunteers. Barone, JA; Bierman, RH; Colaizzi, JL; Guarnieri, J; Hassell, AE; Jessen, L; Moskovitz, BL, )	0.13
"The extensive interindividual variability in oral bioavailability of itraconazole prompted an assessment of the bioequivalence of two formulations marketed in Brazil, namely, Sporanox (reference) and Traconal (test)."	( Limited-sampling strategy models for itraconazole and hydroxy-itraconazole based on data from a bioequivalence study. Bozza, FA; Ponte, CG; Struchiner, CJ; Suarez-Kurtz, G; Vicente, FL, 1999)	0.3
" The ultimate goals were to determine the relative bioavailability between the two oral formulations (capsules vs oral solution) and to optimise dosing regimens in these patients."	( Population pharmacokinetics of itraconazole and its active metabolite hydroxy-itraconazole in paediatric cystic fibrosis and bone marrow transplant patients. Bell, SC; Charles, BG; Friberg, LE; Hennig, S; Miller, H; Wainwright, CE, 2006)	0.33
" However, the oral bioavailability of both compounds varies widely, and dose-serum concentration relationships are poorly defined for these analytes."	( Measurement of posaconazole, itraconazole, and hydroxyitraconazole in plasma/serum by high-performance liquid chromatography with fluorescence detection. Buckner, SL; Ceesay, MM; Flanagan, RJ; Morgan, PE; Pagliuca, A, 2011)	0.63
" The relative bioavailability of SUBA-itraconazole compared to that of Sporanox was 173% and was 21% less variable between subjects."	( Population pharmacokinetic modeling of itraconazole and hydroxyitraconazole for oral SUBA-itraconazole and sporanox capsule formulations in healthy subjects in fed and fasted states. Abuhelwa, AY; Foster, DJ; Hayes, D; Mudge, S; Upton, RN, 2015)	0.66
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Consequently an individual itraconazole adjusting dosage is necessary to ensure adequate clinical antifungal activity."	( Determination of itraconazole and its active metabolite in plasma by column liquid chromatography. Cheymol, G; Descamps, P; Lebot, M; Levy, M; Poirier, JM, 1994)	0.29
" The pits received daily during three weeks oral itraconazole at a dosage of 200 mg at the beginning of the meal, then during the next two weeks oral itraconazole combined with an intravenous administration of rifampin at a dosage of 10 mg/kg/day."	( [Pharmacokinetic interaction between itraconazole and rifampin in Yucatan miniature pigs]. Cavalier, A; Elkhaili, H; Jehl, F; Kaltenbach, G; Levêque, D; Monteil, H; Peter, JD; Salmon, J; Salmon, Y, 1996)	0.29
") treatment was directly followed by repeated administrations of an oral solution of itraconazole at a dosage of either 200 mg once daily or 200 mg twice daily (b."	( Concentrations in plasma and safety of 7 days of intravenous itraconazole followed by 2 weeks of oral itraconazole solution in patients in intensive care units. Colardyn, F; De Beule, K; Decruyenaere, J; Groen, K; Jaqmin, P; Van Peer, A; Vandewoude, K; Vogelaers, D; Woestenborghs, R, 1997)	0.3
" The patients were treated with itraconazole at a dosage of 5 mg/kg of body weight once daily for 2 weeks."	( Repeated-dose pharmacokinetics of an oral solution of itraconazole in infants and children. Cornu, G; De Beule, K; de Repentigny, L; Jacqmin, P; Leclerc, JM; Ratelle, J; Sokal, EM, 1998)	0.3
"The bioavailability of ITR and OH-ITR is enhanced when ITR oral solution is given in the fasted state; this was true for both single and multiple dosing to steady state."	( Food interaction and steady-state pharmacokinetics of itraconazole oral solution in healthy volunteers. Barone, JA; Bierman, RH; Colaizzi, JL; Guarnieri, J; Hassell, AE; Jessen, L; Moskovitz, BL, )	0.13
" The dosage of itraconazole was reduced when it was used in combination with lopinavir/ritonavir."	( 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
" Two hours after dosing they received another 240 ml of the beverage."	( Influence of grapefruit juice on the systemic availability of itraconazole oral solution in healthy adult volunteers. Fincher, TK; Franks, AM; Gubbins, PO; Gurley, BJ; McConnell, SA; Penzak, SR; Saccente, M; Williams, DK, 2004)	0.32
" The ultimate goals were to determine the relative bioavailability between the two oral formulations (capsules vs oral solution) and to optimise dosing regimens in these patients."	( Population pharmacokinetics of itraconazole and its active metabolite hydroxy-itraconazole in paediatric cystic fibrosis and bone marrow transplant patients. Bell, SC; Charles, BG; Friberg, LE; Hennig, S; Miller, H; Wainwright, CE, 2006)	0.33
" Building on this data, a final steady-state trial was performed with the use of a 7 mg/kg oral dosage twice a day of commercial capsules given in fish to a group of 15 penguins."	( Evaluation of oral itraconazole administration in captive Humboldt penguins (Spheniscus humboldti). Abou-Madi, N; Bunting, EM; Cox, S; Fox, H; Kollias, GV; Martin-Jimenez, T, 2009)	0.35
" Although separating their dosages by 24 hours has been shown to reduce the interaction, an appropriate dosage interval remains to be determined."	( Pharmacokinetic modeling of the dosing interval dependency for the interaction between itraconazole and triazolam. Ohtani, H; Sawada, Y; Toi, A; Tsujimoto, M, 2010)	0.36
" Subsequently, we simulated the plasma concentration profiles of triazolam administered after itraconazole therapy with various dosing intervals."	( Pharmacokinetic modeling of the dosing interval dependency for the interaction between itraconazole and triazolam. Ohtani, H; Sawada, Y; Toi, A; Tsujimoto, M, 2010)	0.36
"The model could explain and simulate the interaction between itraconazole-triazolam using a variety of dosage intervals between the administrations."	( Pharmacokinetic modeling of the dosing interval dependency for the interaction between itraconazole and triazolam. Ohtani, H; Sawada, Y; Toi, A; Tsujimoto, M, 2010)	0.36

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]

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]

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]

Trial Outcomes

Trial	Outcome
NCT00356915 (4) [back to overview]	Clinical and Mycological Cure of Target Toenail
NCT00356915 (4) [back to overview]	Clinical Improvement Compared to Placebo
NCT00356915 (4) [back to overview]	Clinical Improvement of the Target Toenail
NCT00356915 (4) [back to overview]	Complete Cure - Itraconazole Tablets Compared to Itraconazole Capsules
NCT00791219 (7) [back to overview]	"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Clinical Cure at the End of Study Visit (Week 12)"
NCT00791219 (7) [back to overview]	"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Clinical Cure at the End of Study Visit (Week 24)"
NCT00791219 (7) [back to overview]	"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Mycological Cure at the End of Study Visit (Week 12)"
NCT00791219 (7) [back to overview]	"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Mycological Cure at the End of Study Visit (Week 24)"
NCT00791219 (7) [back to overview]	"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Therapeutic Cure at the End of Study Visit (Week 24)"
NCT00791219 (7) [back to overview]	"The Proportion of Patients in Each Treatment Group Who Are Considered a Therapeutic Cure at the End of Treatment Visit (Week 12) 12)."
NCT00791219 (7) [back to overview]	Superiority of Test Treatment Over Placebo for Mycological Cure
NCT00887458 (2) [back to overview]	To Determine the Proportion of Men With ≥ 50% PSA Reduction From Baseline.
NCT00887458 (2) [back to overview]	To Determine the Proportion of Patients With Metastatic CRPC Who do Not Have Prostate Specific Antigen (PSA) Progression After 24 Weeks of Therapy With One of Two Dose-levels of Itraconazole: 200 mg or 600 mg Daily.
NCT03572049 (5) [back to overview]	Comparison of Plasma Itraconazole Levels and Hydroxyitraconazole Levels at Day 14
NCT03572049 (5) [back to overview]	Comparison of Plasma Itraconazole Levels and Hydroxyitraconazole Levels at Day 42
NCT03572049 (5) [back to overview]	Frequency of Treatment Related Adverse Events Days 1-42
NCT03572049 (5) [back to overview]	Resolution of Signs and Symptoms of Invasive Fungal Infection on Day 42
NCT03572049 (5) [back to overview]	The Number of Days of Hospitalization at Day 180
NCT04035187 (2) [back to overview]	AUC
NCT04035187 (2) [back to overview]	Cmax

Clinical and Mycological Cure of Target Toenail

"This study was designed to evaluate the superiority of itraconazole tablets to placebo tablets.~Clinical Cure was defined as an IGA score of 0 for the target toenail; Mycological Cure was defined as a negative potassium hydroxide (KOH) exam and a negative culture for dermatophytes of the target toenail." (NCT00356915)
Timeframe: 1 year

Intervention	Percentage of participants (Number)
Itraconazole Tablets	22.3
Placebo Tablets	1

Intervention	Percentage of participants (Number)
Itraconazole Tablets	22.3
Itraconazole Capsules	21.7
Placebo Tablets	1.0

Intervention	ng*hr/mL (Mean)
Fast Tablet	1624.8
Medium Tablet	1365.5
Slow Tablet	1282.2
Oral Solution	1848.7

Intervention	ng/mL (Mean)
Fast Tablet	174.3
Medium Tablet	108.5
Slow Tablet	121.3
Oral Solution	266.7

Substance	Relationship Strength	Studies	Trials	Classes	Roles
benzyl alcohol Benzyl Alcohol: A colorless liquid with a sharp burning taste and slight odor. It is used as a local anesthetic and to reduce pain associated with LIDOCAINE injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutic aid, and in perfumery and flavoring.. hydroxytoluene : Any member of the class of toluenes carrying one or more hydroxy substituents.. benzyl alcohol : An aromatic alcohol that consists of benzene bearing a single hydroxymethyl substituent.. aromatic alcohol : Any alcohol in which the alcoholic hydroxy group is attached to a carbon which is itself bonded to an aromatic ring.. aromatic primary alcohol : Any primary alcohol in which the alcoholic hydroxy group is attached to a carbon which is itself bonded to an aromatic ring.	2.03	1	0	benzyl alcohols	antioxidant; fragrance; metabolite; solvent
methanol Methanol: A colorless, flammable liquid used in the manufacture of FORMALDEHYDE and ACETIC ACID, in chemical synthesis, antifreeze, and as a solvent. Ingestion of methanol is toxic and may cause blindness.. primary alcohol : A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.. methanol : The primary alcohol that is the simplest aliphatic alcohol, comprising a methyl and an alcohol group.	2.49	2	0	alkyl alcohol; one-carbon compound; primary alcohol; volatile organic compound	amphiprotic solvent; Escherichia coli metabolite; fuel; human metabolite; mouse metabolite; Mycoplasma genitalium metabolite
phenytoin [no description available]	8.37	1	1	imidazolidine-2,4-dione	anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent
cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.	2.01	1	0	aliphatic sulfide; guanidines; imidazoles; nitrile	adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor
fexofenadine fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.	3.51	1	1	piperidines; tertiary amine	anti-allergic agent; H1-receptor antagonist
fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.	9.39	4	1	conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug	environmental contaminant; P450 inhibitor; xenobiotic
losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position	3.51	1	1	biphenylyltetrazole; imidazoles	angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist
miconazole Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion.. 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group.. miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.	3.45	1	1	dichlorobenzene; ether; imidazoles
terfenadine Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.	3.51	1	1	diarylmethane
triazolam Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.	2.05	1	0	triazolobenzodiazepine	sedative
ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist	3.46	1	1	carbamate ester; indoles; N-sulfonylcarboxamide	anti-asthmatic agent; leukotriene antagonist
prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.	3.39	1	1	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic
chloroform Chloroform: A commonly used laboratory solvent. It was previously used as an anesthetic, but was banned from use in the U.S. due to its suspected carcinogenicity.. chloroform : A one-carbon compound that is methane in which three of the hydrogens are replaced by chlorines.	3.41	1	1	chloromethanes; one-carbon compound	carcinogenic agent; central nervous system drug; inhalation anaesthetic; non-polar solvent; refrigerant
methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.	3.39	1	1	6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic
n-heptane Heptanes: Seven-carbon alkanes with the formula C7H16.. heptane : A straight-chain alkane with seven carbon atoms. It has been found in Jeffrey pine (Pinus jeffreyi).	3.41	1	1	alkane; volatile organic compound	non-polar solvent; plant metabolite
itraconazole Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.	12.66	81	28	aromatic ether; conazole antifungal drug; cyclic ketal; dichlorobenzene; dioxolane; N-arylpiperazine; triazole antifungal drug; triazoles	EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; Hedgehog signaling pathway inhibitor; P450 inhibitor
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	6	9	1	1,2,3-triazole
voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.	3.59	8	0	conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug	P450 inhibitor
lopinavir [no description available]	2.02	1	0	amphetamines; dicarboxylic acid diamide	anticoronaviral agent; antiviral drug; HIV protease inhibitor
exp3174 losartan carboxylic acid: structure given in first source. losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid.	3.51	1	1	biphenylyltetrazole; imidazoles; organochlorine compound	metabolite
moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.	3.4	1	1	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug
naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.	2.08	1	0	methoxynaphthalene; monocarboxylic acid	antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic
anidulafungin Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis.	7.05	1	0	antibiotic antifungal drug; azamacrocycle; echinocandin; heterodetic cyclic peptide; semisynthetic derivative
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	2.02	1	0	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
betadex beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.	6.48	6	3	cyclodextrin
tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.	7.41	1	0	macrolide lactam	bacterial metabolite; immunosuppressive agent
cerivastatin cerivastatin: cerivastatin is the ((E)-(+))-isomer; structure given in first source. cerivastatin : (3R,5S)-3,5-dihydroxyhept-6-enoic acid in which the (7E)-hydrogen is substituted by a 4-(4-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl group. Formerly used (as its sodium salt) to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.	3.38	1	1	dihydroxy monocarboxylic acid; pyridines; statin (synthetic)
posaconazole [no description available]	5.79	7	1	aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles	trypanocidal drug
l 743,872 [no description available]	2.05	1	0
micafungin Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy.	2.13	1	0	antibiotic antifungal drug; echinocandin	antiinfective agent
digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.	7	1	0	cardenolide glycoside; steroid saponin	anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope
amphotericin b Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.	7.43	2	0	antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic	antiamoebic agent; antiprotozoal drug; bacterial metabolite
fumarates Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)	3.45	1	1	butenedioate; C4-dicarboxylate	human metabolite; metabolite; Saccharomyces cerevisiae metabolite
aliskiren aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.	3.45	1	1	monocarboxylic acid amide; monomethoxybenzene	antihypertensive agent
ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.	3.45	1	1	ascorbic acid; vitamin C	coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent
cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).	7.41	1	0
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	1.99	1	0	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor
pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.	2.02	1	0

Condition	Relationship Strength	Studies	Trials
Congenital Zika Syndrome [description not available]	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.44	2	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1	0
Aspergilloses, Bronchopulmonary [description not available]	3.98	2	1
Pulmonary Aspergillosis Infections of the respiratory tract with fungi of the genus ASPERGILLUS.	3.98	2	1
Carcinoma, Non-Small Cell Lung [description not available]	3.64	1	1
Angiogenesis, Pathologic [description not available]	3.64	1	1
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	3.64	1	1
Hematologic Malignancies [description not available]	4.09	3	1
Fungal Diseases [description not available]	6.12	6	2
Chemotherapy-Induced Febrile Neutropenia FEVER accompanied by a significant reduction in NEUTROPHIL count associated with CHEMOTHERAPY.	2.1	1	0
Mycoses Diseases caused by FUNGI.	6.12	6	2
Hematologic Neoplasms Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.	4.09	3	1
Aspergillus Infection [description not available]	2.71	3	0
Aspergillosis Infections with fungi of the genus ASPERGILLUS.	2.71	3	0
Alloxan Diabetes [description not available]	2.05	1	0
Allergic Bronchopulmonary Mycosis [description not available]	4.37	1	1
Neutropenia A decrease in the number of NEUTROPHILS found in the blood.	4.37	1	1
Moniliasis, Oral [description not available]	4.64	3	2
HIV Coinfection [description not available]	4.09	3	1
Candidiasis, Oral Infection of the mucous membranes of the mouth by a fungus of the genus CANDIDA. (Dorland, 27th ed)	4.64	3	2
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	4.09	3	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	3.62	9	0
Histoplasma capsulatum Infection [description not available]	2.02	1	0
AIDS-Related Opportunistic Infections Opportunistic infections found in patients who test positive for human immunodeficiency virus (HIV). The most common include PNEUMOCYSTIS PNEUMONIA, Kaposi's sarcoma, cryptosporidiosis, herpes simplex, toxoplasmosis, cryptococcosis, and infections with Mycobacterium avium complex, Microsporidium, and Cytomegalovirus.	4.08	3	1
Histoplasmosis Infection resulting from exposure to the fungus HISTOPLASMA. It is worldwide in distribution and particularly common in the central and eastern states, especially areas around the Ohio and Mississippi River valleys.	2.02	1	0
Allergic Bronchopulmonary Aspergilloses [description not available]	2.03	1	0
Cystic Fibrosis of Pancreas [description not available]	3.82	2	1
Aspergillosis, Allergic Bronchopulmonary Hypersensitivity reaction (ALLERGIC REACTION) to fungus ASPERGILLUS in an individual with long-standing BRONCHIAL ASTHMA. It is characterized by pulmonary infiltrates, EOSINOPHILIA, elevated serum IMMUNOGLOBULIN E, and skin reactivity to Aspergillus antigen.	2.03	1	0
Cystic Fibrosis An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.	3.82	2	1
Extravascular Hemolysis [description not available]	2.03	1	0
Hemolysis The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.	2.03	1	0
Nail Fungus [description not available]	3.42	1	1
Hand Dermatosis [description not available]	3.42	1	1
Hand Dermatoses Skin diseases involving the HANDS.	3.42	1	1
Onychomycosis A fungal infection of the nail, usually caused by DERMATOPHYTES; YEASTS; or nondermatophyte MOLDS.	3.42	1	1
Leucocythaemia [description not available]	2.39	2	0
Leukemia A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)	2.39	2	0
Acute Kidney Failure [description not available]	1.98	1	0
Acute Kidney Injury Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.	1.98	1	0
Acquired Immune Deficiency Syndrome [description not available]	4.06	3	1
Acquired Immunodeficiency Syndrome An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.	4.06	3	1
Agranulocytosis A decrease in the number of GRANULOCYTES; (BASOPHILS; EOSINOPHILS; and NEUTROPHILS).	3.37	1	1
Opportunistic Infections An infection caused by an organism which becomes pathogenic under certain conditions, e.g., during immunosuppression.	1.99	1	0
Chronic Illness [description not available]	2	1	0
Fungal Meningitis [description not available]	2	1	0
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2	1	0
Acute Myelogenous Leukemia [description not available]	2	1	0
Discitis Inflammation of an INTERVERTEBRAL DISC or disk space which may lead to disk erosion. Until recently, discitis has been defined as a nonbacterial inflammation and has been attributed to aseptic processes (e.g., chemical reaction to an injected substance). However, recent studies provide evidence that infection may be the initial cause, but perhaps not the promoter, of most cases of discitis. Discitis has been diagnosed in patients following discography, myelography, lumbar puncture, paravertebral injection, and obstetrical epidural anesthesia. Discitis following chemonucleolysis (especially with chymopapain) is attributed to chemical reaction by some and to introduction of microorganisms by others.	2	1	0
Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.	2	1	0

hydroxyitraconazole

Description

Cross-References

Synonyms (24)

Research Excerpts

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Bioassays (5)

Research

Studies (84)

Market Indicators

Research Demand Index: 21.39

Study Types

Clinical Trials (26)

Trial Overview

Trial Outcomes

Clinical and Mycological Cure of Target Toenail

Clinical Improvement Compared to Placebo

Clinical Improvement of the Target Toenail

Complete Cure - Itraconazole Tablets Compared to Itraconazole Capsules

"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Clinical Cure at the End of Study Visit (Week 12)"

"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Clinical Cure at the End of Study Visit (Week 24)"

"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Mycological Cure at the End of Study Visit (Week 12)"

"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Mycological Cure at the End of Study Visit (Week 24)"

"Non-inferiority Will be Determined by Evaluating the Difference Between the Proportion of Patients in the Test and Reference Treatment Groups Who Are Considered a Therapeutic Cure at the End of Study Visit (Week 24)"

"The Proportion of Patients in Each Treatment Group Who Are Considered a Therapeutic Cure at the End of Treatment Visit (Week 12) 12)."

Superiority of Test Treatment Over Placebo for Mycological Cure

To Determine the Proportion of Men With ≥ 50% PSA Reduction From Baseline.

To Determine the Proportion of Patients With Metastatic CRPC Who do Not Have Prostate Specific Antigen (PSA) Progression After 24 Weeks of Therapy With One of Two Dose-levels of Itraconazole: 200 mg or 600 mg Daily.

Comparison of Plasma Itraconazole Levels and Hydroxyitraconazole Levels at Day 14

Comparison of Plasma Itraconazole Levels and Hydroxyitraconazole Levels at Day 42

Frequency of Treatment Related Adverse Events Days 1-42

Resolution of Signs and Symptoms of Invasive Fungal Infection on Day 42

The Number of Days of Hospitalization at Day 180

AUC

Cmax

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