Page last updated: 2024-12-05

itraconazole

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Itraconazole is a triazole antifungal medication. It works by interfering with the production of ergosterol, a vital component of fungal cell membranes. This disrupts the fungal cell wall, leading to cell death. It is used to treat a variety of fungal infections, including blastomycosis, histoplasmosis, coccidioidomycosis, paracoccidioidomycosis, aspergillosis, and candidiasis. Itraconazole is also used to prevent fungal infections in people with weakened immune systems. The synthesis of itraconazole involves a multi-step process starting from a commercially available starting material. The drug is orally administered and is well absorbed. Its importance lies in its broad spectrum of activity against various fungal pathogens, making it a valuable therapeutic option for treating severe fungal infections. Itraconazole is extensively studied due to its clinical efficacy, safety profile, and potential for new applications in treating other fungal infections and even certain types of cancer.'

Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID55283
CHEMBL ID22587
CHEBI ID6076
SCHEMBL ID23934
MeSH IDM0027131
PubMed CID3793
CHEMBL ID64391
CHEBI ID94366
SCHEMBL ID95627
SCHEMBL ID16984893
MeSH IDM0027131

Synonyms (188)

Synonym
AC-542
AB01274818-01
AKOS015842738
itraconazole & nyotran(liposomal nystatin)
itraconazole & nyotran
CHEBI:6076 ,
onmel
2-(butan-2-yl)-4-{4-[4-(4-{[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-2,4-dihydro-3h-1,2,4-triazol-3-one
4-(4-{4-[4-({[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl}oxy)phenyl]piperazin-1-yl}phenyl)-2-(1-methylpropyl)-2,4-dihydro-3h-1,2,4-triazol-3-one
sporanox
oriconazole
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)-
itraconazol [spanish]
r51211
itcz
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-sec-butyl-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-pipera-zinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)
itz ,
itraconazole
sporanox(tm)
DB01167
itraconazole (jp17/usp)
itrizole (tn)
sporanox (tn)
D00350
intraconazole
chembl22587
bdbm50127138
2-butan-2-yl-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]-1,2,4-triazol-3-one
304nug5gf4 ,
cis-itraconazole
pharmakon1600-01505756
nsc-759239
nsc759239
tox21_110854
dtxcid903180
cas-84625-61-6
dtxsid3023180 ,
itraconazolum
itraconazol
AKOS015961385
NCGC00274068-02
S2476
itraconazole [mart.]
itraconazole [green book]
(+/-)-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
itraconazole [orange book]
itraconazole [vandf]
itraconazole (ema epar: veterinary)
itraconazole [who-dd]
fungitraxx
itraconazole [usp-rs]
itraconazole [ep monograph]
itraconazole [inci]
itraconazole [mi]
itraconazole [usp monograph]
itraconazole [usan]
suba-itraconazole component itraconazole
itraconazole [inn]
itraconazole component of suba-itraconazole
cladosal 100
itraconazole [ep impurity]
itraconazole [jan]
HY-17514
SCHEMBL23934
tox21_110854_1
NCGC00274068-01
KS-1268
1-(butan-2-yl)-4-{4-[4-(4-{[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-4,5-dihydro-1h-1,2,4-triazol-5-one
MLS006011958
smr001827898
4-(4-(4-(4-(((2r,4s)-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-(sec-butyl)-2,4-dihydro-3h-1,2,4-triazol-3-one
AB01274818_02
AB01274818_03
itraconazole 2.0 mg/ml in dimethyl sulfoxide
SBI-0206914.P001
NCGC00274068-07
873066-43-4
SW219756-1
Q411229
Z1544404944
itraconazole (sporanox) ,
BRD-A23067620-001-01-7
EN300-122640
1-(butan-2-yl)-4-{4-[4-(4-{[(2r,4s)-2-(2,4-dichlorophenyl)-2-[(1h-1,2,4-triazol-1-yl)methyl]-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-4,5-dihydro-1h-1,2,4-triazol-5-one
AMY922
CCG-270391
A933954
gtpl11426
itraconazolo
itraconazole oral
3h-1,2,4-triazol-3-one, 4-
itraconazole (ep impurity)
itraconazole (usp monograph)
itraconazole (usp-rs)
itraconazole (mart.)
tolsura
lozanoc
itraconazole (ep monograph)
j02ac02
itrafungol
MLS001148245
HMS3393K14
AB00383031-14
itraconazolum [latin]
sempera
orungal
itrizole
r-51211
r 51211
MLS000759472
NCGC00089812-03
MLS000863291 ,
smr000058959
MLS000028582
HMS2051K14
HMS2090M20
I0732
AKOS000280875
2-butan-2-yl-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]-1,2,4-triazol-3-one
NCGC00018268-03
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)-1-(sec-butyl)-1h-1,2,4-triazol-5(4h)-one
NCGC00018268-02
spherazole cr
sporonox
candistat
itrac
canditral
triasporin
r 51,211
traconal
spherazole ir
sporamelt
itralek
MLS001424065
HMS2235M11
CCG-100876
FT-0601621
HMS3370P13
CCG-220567
DL-427
SCHEMBL95627
AKOS022171690
NC00126
CHEMBL64391
itrazole
itraconazole, antibiotic for culture media use only
Q-201261
bdbm50011478
OPERA_ID_902
STL450986
2-(butan-2-yl)-4-{4-[4-(4-{[2-(2,4-dichlorophenyl)-2-(1h-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-2,4-dihydro-3h-1,2,4-triazol-3-one
1217512-35-0
SCHEMBL16984893
itraconazole, united states pharmacopeia (usp) reference standard
2-butan-2-yl-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-1,2,4-triazol-3-one
CHEBI:94366
itraconazole, >=98% (tlc)
itraconazole, european pharmacopoeia (ep) reference standard
(+/-)-cis-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)-3h-1,2,4-triazol-3-one
itraconazole, pharmaceutical secondary standard; certified reference material
itraconazole for system suitability, european pharmacopoeia (ep) reference standard
J-015921
SR-01000003153-5
SR-01000003153-6
trans itraconazole
sr-01000003153
itraconzaole
HMS3713B16
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-(sec-butyl)-2,4-dihydro-3h-1,2,4-triazol-3-one
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)-1-sec-butyl-1h-1,2,4-triazol-5(4h)-one
Q27166205
2049588-24-9
1-(butan-2-yl)-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}-4,5-dihydro-1h-1,2,4-triazol-5-one
mfcd00941396
itraconazole,(s)
BCP28497
FT-0670576
O11835
NCGC00018268-05
NCGC00018268-06
nsc754771
nsc-754771
EN300-246240
SY057462
BI164594
CS-0242228
Z2194031989

Research Excerpts

Overview

Itraconazole (ITZ) is an FDA-approved member of the triazole class of antifungal agents. The drug was recently found to possess potent antiangiogenic activity and anti-hedgehog (Hh) pathway activity.

ExcerptReferenceRelevance
"Itraconazole is an antifungal drug that was recently found to possess potent antiangiogenic activity and anti-hedgehog (Hh) pathway activity. "( Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling.
Aftab, BT; Head, S; Liu, JO; Nacev, BA; Rudin, CM; Shi, W, 2011
)
3.25
"Itraconazole (ITZ) is an FDA-approved member of the triazole class of antifungal agents. "( Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
Chan, KA; DeBerardinis, AM; Hadden, MK; Pace, JR; Raccuia, DS; Sail, V; Tacheva-Grigorova, SK; Tran, R; Wechsler-Reya, RJ, 2016
)
2.12

Toxicity

Itraconazole is safe and effective at a dose of 5 mg/kg per day in a short duration of therapy for superficial fungal infections and 10 mg/ kg per day for systemic fungal infection in infants. Clinicians should be aware of pseudohyperaldosteronism as a possiblity.

ExcerptReferenceRelevance
" Two itraconazole patients stopped medication due to an adverse event, compared to four patients in the griseofulvin group."( Efficacy and safety of itraconazole in the long-term treatment of onychomycosis.
Blomqvist, K; Brandt, H; Havu, V; Hollmen, A; Kohtamäki, K; Lehtonen, L; Piepponen, T; Turjanmaa, K, 1992
)
0.28
" This is, however, a species-specific phenomenon which leads to secondary events at toxic doses, especially in long-term toxicity studies."( Safety aspects of oral antifungal agents.
Coussement, W; De Coster, R; Lampo, A; Marsboom, R; Van Cauteren, H; Vandenberghe, J; Vanparys, P, 1990
)
0.28
" Adverse reactions possibly due to itraconazole were seen in 74 patients (39%)."( Adverse events associated with itraconazole in 189 patients on chronic therapy.
Denning, DW; Haq, Y; Stevens, DA; Tucker, RM, 1990
)
0.28
" This species-specific phenomenon leads at toxic dose levels to secondary events, especially in the long-term toxicity studies."( Toxicological profile and safety evaluation of antifungal azole derivatives.
Coussement, W; De Coster, R; Lampo, A; Marsboom, R; Van Cauteren, H; Vandenberghe, J; Vanparys, P, 1989
)
0.28
"Itraconazole pulse therapy was efficient and safe for the treatment of onychomycosis caused by dermatophytes, although a much higher daily dosage than the known continuous administration was used."( Efficacy and safety of itraconazole pulse therapy: Brazilian multicentric study on toenail onychomycosis caused by dermatophytes.
Campbell, I; Gontijo, B; Marques, SA; Ramos-e-Silva, M; Veloso, ST; Zaitz, C, 1998
)
0.3
" During treatment, adverse events were recorded in 7 patients in the itraconazole group and 2 patients in the placebo group."( Efficacy and safety of short-term itraconazole in tinea pedis: a double-blind, randomized, placebo-controlled trial.
Avnstorp, C; Heremans, A; Nilsson, J; Svejgaard, E; Wanscher, B, 1998
)
0.3
" Most adverse events occurred infrequently; major changes in liver function tests were not noted."( Safety and efficacy of intermittent therapy with itraconazole in finger- and toenail onychomycosis: a multicentre trial.
Abeck, D; Haneke, E; Ring, J, 1998
)
0.3
" A possible adverse drug interaction with itraconazole and amphotericin B is postulated based on the mechanism of action of each drug."( Hepatotoxicity possibly caused by amphotericin B.
Gill, J; Ralph, ED; Sharpe, MD; Sprenger, HR, 1999
)
0.3
"Amphotericin B therapy can be associated with many adverse effects, but reports of hepatotoxicity are rare."( Hepatotoxicity possibly caused by amphotericin B.
Gill, J; Ralph, ED; Sharpe, MD; Sprenger, HR, 1999
)
0.3
" Adverse events were reported in 4 of the 27 itraconazole subjects; no adverse events were reported in the 25 palliative treatment subjects."( The safety of itraconazole in the diabetic population.
Albreski, DA; Gross, EG, 1999
)
0.3
" From clinical trials including a total of 189 diabetic patients treated with itraconazole for various infections (mainly systemic infections and vaginal candidiasis), only one itraconazole-related adverse event was recorded; this was a case of aggravated diabetes in a renal transplant recipient who was also receiving cyclosporine."( Safety of itraconazole in diabetic patients.
De Doncker, P; Gupta, AK; Marynissen, G; Verspeelt, J, 1999
)
0.3
"A 1-week intermittent itraconazole dosing regimen is a safe and effective treatment for onychomycosis."( Therapeutic efficacy and safety of one-week intermittent therapy with itraconazole for onychomycosis in a Chinese patient population.
Li, RY; Wang, AP; Wang, DL; Wang, R, 1999
)
0.3
" In addition, itraconazole is safe to use in diabetic patients with dermatomycosis or onychomycosis."( Continuous itraconazole treatment for onychomycosis and dermatomycosis: an overview of safety.
Doncker, PD; Gupta, A; Jacko, ML; Moskovitz, BL; Nolting, SK,
)
0.13
" Adverse events are generally mild and transient."( Update on the safety of itraconazole pulse therapy in onychomycosis and dermatomycoses.
Gupta, A; Lambert, J; Revuz, J; Shear, N,
)
0.13
" As expected in the patient population studied, all patients experienced some adverse events (mainly gastrointestinal)."( Pharmacokinetics and safety of a 7-day administration of intravenous itraconazole followed by a 14-day administration of itraconazole oral solution in patients with hematologic malignancy.
Boogaerts, MA; Bosly, A; Cleeren, M; De Beule, K; Maertens, J; Michaux, JM; Van Der Geest, R; Van Hoof, A; Wostenborghs, R, 2001
)
0.31
"The extent and consistency of adverse effects documented in this study support the recommendation that concurrent administration of vincristine and itraconazole should be avoided."( Potentiation of vincristine toxicity by itraconazole in children with lymphoid malignancies.
Breatnach, F; Butler, K; Kamaluddin, M; McNally, P; O'Dell, E; O'Marcaigh, A; O'Meara, A; Scanlon, P; Webb, D, 2001
)
0.31
" The most common adverse events are gastrointestinal upset, headache, and transient skin reaction."( Hepatic safety of itraconazole.
Baran, R; Chwetzoff, E; Del Rosso, J; Gupta, AK,
)
0.13
"To determine rates of drug-induced, rare, serious adverse events affecting the liver, kidneys, skin, or blood, occurring within 45 days of completing a prescription or refill for itraconazole or fluconazole."( Itraconazole and fluconazole and certain rare, serious adverse events.
Bradbury, BD; Jick, SS, 2002
)
0.31
"Itraconazole and fluconazole do not commonly cause rare, serious adverse events affecting the liver, kidneys, skin, or blood."( Itraconazole and fluconazole and certain rare, serious adverse events.
Bradbury, BD; Jick, SS, 2002
)
0.31
"6%) discontinued treatment prematurely due to study drug-related adverse events."( Safety, pharmacokinetics, and pharmacodynamics of cyclodextrin itraconazole in pediatric patients with oropharyngeal candidiasis.
Chiou, CC; Dad, L; Groll, AH; Mickiene, D; Piscitelli, SC; Roden, M; Townley, E; Walsh, TJ; Wood, L, 2002
)
0.31
" The oral solution also produces good rates of efficacy, but may be associated with a somewhat higher potential for gastrointestinal adverse events than the capsules."( Efficacy and safety of itraconazole use in children.
Cooper, EA; Ginter, G; Gupta, AK, 2003
)
0.32
" Measurements included incidence of fungal colonization, superficial or systemic fungal infections requiring systemic therapy, adverse events, and mortality rate."( Efficacy and safety of itraconazole prophylaxis for fungal infections after orthotopic liver transplantation: a prospective, randomized, double-blind study.
David Colby, W; Ghent, C; Grant, D; Horbay, GL; McDougal, J; Sharpe, MD, 2003
)
0.32
" Adverse events were reported by 97% and 100% of the intraconazole and placebo groups, respectively, and one itraconazole and six placebo-group patients died within the study period."( Efficacy and safety of itraconazole prophylaxis for fungal infections after orthotopic liver transplantation: a prospective, randomized, double-blind study.
David Colby, W; Ghent, C; Grant, D; Horbay, GL; McDougal, J; Sharpe, MD, 2003
)
0.32
" Safety was assessed from biochemistry and haematology data and reported adverse events."( Pharmacokinetics and safety of itraconazole in patients with cystic fibrosis.
Brownlee, KG; Conway, SP; Cunliffe, H; Etherington, C; Peckham, DG; Whitehead, A, 2004
)
0.32
" Adverse events were reported by 53% of subjects."( Pharmacokinetics and safety of itraconazole in patients with cystic fibrosis.
Brownlee, KG; Conway, SP; Cunliffe, H; Etherington, C; Peckham, DG; Whitehead, A, 2004
)
0.32
" The dosage regimen was safe and well tolerated."( Pharmacokinetics and safety of itraconazole in patients with cystic fibrosis.
Brownlee, KG; Conway, SP; Cunliffe, H; Etherington, C; Peckham, DG; Whitehead, A, 2004
)
0.32
" The frequency of adverse incident of A, B, C groups were 22."( [Study on the compliance and safety of the oral antifungal agents for the treatment of onychomycosis].
Dai, XY; Hu, Y; Hua, HK; Qi, J; Sun, H; Wei, L; Yang, LJ; Zheng, Y, 2005
)
0.33
" When treating onychomycosis with oral itraconazole, the results seemed to be just as safe as when using terbinafine."( [Study on the compliance and safety of the oral antifungal agents for the treatment of onychomycosis].
Dai, XY; Hu, Y; Hua, HK; Qi, J; Sun, H; Wei, L; Yang, LJ; Zheng, Y, 2005
)
0.33
" The relationship between liver adverse reaction and itraconazole treatment was evaluated."( [Hepatic safety of itraconazole intravenous solution in treatment of invasive fungal infection].
Chen, S; Huang, YX; Lu, Q; Shi, GF; Weng, XH; Yang, FF; Zhang, WH; Zhang, YX; Zhu, LP, 2006
)
0.33
" However, only in 2 patients with mild liver function test abnormality the liver adverse reaction could be associated with itraconazole treatment."( [Hepatic safety of itraconazole intravenous solution in treatment of invasive fungal infection].
Chen, S; Huang, YX; Lu, Q; Shi, GF; Weng, XH; Yang, FF; Zhang, WH; Zhang, YX; Zhu, LP, 2006
)
0.33
" The most common adverse events were hypokalemia (13."( Clinical study on the efficacy and safety of intravenous itraconazole infusion for the treatment of invasive fungal infection in china.
Glasmacher, A; Hahn-Ast, C; Han, M; He, L; Li, R; Liang, D; Liao, W; Liekwok, WA; Shen, Z; Wang, A; Wu, S; Zhang, Y, 2006
)
0.33
" Permanent discontinuation of study medication due to any adverse event was the primary safety parameter."( Safety and efficacy of itraconazole compared to amphotericin B as empirical antifungal therapy for neutropenic fever in patients with haematological malignancy.
Aulitzky, WE; Bammer, S; Binder, C; Böhme, A; Egerer, G; Ehninger, G; Glasmacher, A; Sandherr, M; Schuler, U; Schwerdtfeger, R; Silling, G; Wandt, H, 2007
)
0.34
"Significantly fewer itraconazole patients discontinued treatment due to any adverse event (22."( Safety and efficacy of itraconazole compared to amphotericin B as empirical antifungal therapy for neutropenic fever in patients with haematological malignancy.
Aulitzky, WE; Bammer, S; Binder, C; Böhme, A; Egerer, G; Ehninger, G; Glasmacher, A; Sandherr, M; Schuler, U; Schwerdtfeger, R; Silling, G; Wandt, H, 2007
)
0.34
" This study confirms the role of itraconazole as a useful and safe agent in empirical antifungal therapy of febrile neutropenic cancer patients."( Safety and efficacy of itraconazole compared to amphotericin B as empirical antifungal therapy for neutropenic fever in patients with haematological malignancy.
Aulitzky, WE; Bammer, S; Binder, C; Böhme, A; Egerer, G; Ehninger, G; Glasmacher, A; Sandherr, M; Schuler, U; Schwerdtfeger, R; Silling, G; Wandt, H, 2007
)
0.34
" Study end-points were proven invasive fungal infection (IFI), survival, adverse reactions and graft-vs."( Intravenous and oral sequential itraconazole antifungal prophylaxis in paediatric stem cell transplantation recipients: a pilot study for evaluation of safety and efficacy.
Beilken, A; Grigull, L; Kuehlke, O; Linderkamp, C; Sander, A; Schmid, H; Schuster, FR; Seidemann, K; Sykora, KW; Welte, K, 2007
)
0.34
"We estimated the absolute risks of treatment termination and incidence of adverse liver outcomes among all commonly used oral antifungal treatments for superficial dermatophytosis and onychomycosis."( The safety of oral antifungal treatments for superficial dermatophytosis and onychomycosis: a meta-analysis.
Chan, AK; Chang, CH; Kurth, T; Orav, JE; Young-Xu, Y, 2007
)
0.34
"Oral antifungal therapy against superficial dermatophytosis and onychomycosis, including intermittent and continuous terbinafine, itraconazole, and fluconazole, was associated with a low incidence of adverse events in an immunocompetent population."( The safety of oral antifungal treatments for superficial dermatophytosis and onychomycosis: a meta-analysis.
Chan, AK; Chang, CH; Kurth, T; Orav, JE; Young-Xu, Y, 2007
)
0.34
" Four patients discontinued ITCZ therapy because of adverse effects following the administration of 200 mg/day or 400 mg/day."( [Correlations between drug plasma concentration and adverse effects in patients treated with itraconazole for pulmonary aspergilloma].
Hashiguchi, K; Higashiyama, Y; Kohno, S; Maesaki, S; Miyazaki, H; Miyazaki, Y; Sasaki, E; Tashiro, T; Tomiyama, Y; Tomono, K, 1999
)
0.3
" Clinical efficacy and adverse reaction were record."( [Clinical efficacy and safety of itraconazole injection/oral solution sequential therapy for treatment of invasive fungal infection in intensive care unit].
Qui, HB, 2008
)
0.35
" (4) No severe adverse reaction was found."( [Clinical efficacy and safety of itraconazole injection/oral solution sequential therapy for treatment of invasive fungal infection in intensive care unit].
Qui, HB, 2008
)
0.35
"Itraconazole injection/oral sequential therapy is an effective and safe antibiotic for the treatment of IFI in ICU."( [Clinical efficacy and safety of itraconazole injection/oral solution sequential therapy for treatment of invasive fungal infection in intensive care unit].
Qui, HB, 2008
)
0.35
" Adverse effects were found in 58 patients (8."( [A retrospective study of efficacy and safety of itraconazole for treatment of invasive fungal infection in hematologic diseases].
Huang, XJ; Ji, Y, 2008
)
0.35
"Itraconazole is an effective and safe antifungal agent for patients with hematological disease or undergoing HSCT and is suitable for empirical antifungal therapy."( [A retrospective study of efficacy and safety of itraconazole for treatment of invasive fungal infection in hematologic diseases].
Huang, XJ; Ji, Y, 2008
)
0.35
" Mild adverse reactions were observed in 6 patients (8."( Efficacy and safety of intravenous itraconazole as empirical antifungal therapy for persistent fever in neutropenic patients with hematological malignancies in Japan.
Aoyama, Y; Hagihara, K; Hayashi, Y; Hino, M; Hirose, A; Koh, H; Kumura, T; Nakane, T; Nakao, Y; Nishiki Kosaka, S; Ohta, K; Okamoto, S; Sakamoto, E; Takeoka, Y; Terada, Y; Umemoto, Y; Yamamura, R, 2009
)
0.35
" Drug discontinuation because of adverse events occurred in 15 patients (21%) receiving voriconazole and six (11%) receiving itraconazole (P=0."( Efficacy and safety of intravenous voriconazole and intravenous itraconazole for antifungal prophylaxis in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome.
Alvarado, G; Blamble, D; Cortes, J; Faderl, S; Hernandez, M; Kantarjian, H; Koller, C; Mattiuzzi, GN; Pierce, S; Verstovsek, S; Xiao, L, 2011
)
0.37
" Even if combined with coronary artery disease and/or cor pulmonale, the elderly patients who have chronic pulmonary diseases were safe when using the itraconazole injection in 14 days."( [The clinical efficacy and cardiac safety of itraconazole injection in treatment of acute pulmonary invasive fungal infection in chronic pulmonary diseases in the elderly].
Gao, SL; Jia, W; Li, GH; Li, YC; Zhang, DR; Zhao, XY; Zhou, YL; Zhu, YQ, 2010
)
0.36
" It is an effective and safe alternative treatment for cutaneous sporotrichosis, which can also lower the cost by decreasing the number of capsules."( Efficacy and safety of itraconazole pulses vs. continuous regimen in cutaneous sporotrichosis.
Cai, Q; Huo, SS; Li, SS; Liu, YY; Song, Y; Yao, L; Zhong, SX; Zhou, JF, 2011
)
0.37
" Clinical efficacy and adverse events were recorded."( [The clinical efficacy and safety of itraconazole injection in treatment of invasive fungal infection in intensive care unit].
, 2010
)
0.36
"Itraconazole injection was an effective and safe drug for the treatment of IFI in ICU."( [The clinical efficacy and safety of itraconazole injection in treatment of invasive fungal infection in intensive care unit].
, 2010
)
0.36
" The aim of this article is to review the metabolism of these two drugs, to analyze the published cases with severe triazole-enhanced vincristine neurotoxicity, to discuss the pathophysiological mechanisms of this adverse effect, and to contribute in understanding the differences in triazole-vincristine interaction severity."( Risk of azole-enhanced vincristine neurotoxicity in pediatric patients with hematological malignancies: old problem - new dilemma.
Pana, ZD; Roilides, E, 2011
)
0.37
" Drug-related adverse events occurred in 18."( Efficacy and safety of intravenous itraconazole followed by oral itraconazole solution in the treatment of invasive pulmonary mycosis.
Zhang, YY; Zhou, X, 2011
)
0.37
"This study showed that in patients with invasive pulmonary mycosis, intravenous itraconazole followed by oral itraconazole solution therapy was safe and effective."( Efficacy and safety of intravenous itraconazole followed by oral itraconazole solution in the treatment of invasive pulmonary mycosis.
Zhang, YY; Zhou, X, 2011
)
0.37
" Other adverse effects were reported but did not lead to the discontinuation of treatment, as follows: hepatic dysfunction, two patients; hypokalemia, nine patients."( [An open, noncomparative multicenter study of the efficacy and safety of itraconazole injections and high dose capsules in chronic pulmonary aspergillosis].
Fujii, H; Hayashi, M; Kaneda, T; Kaneko, M; Karino, T; Kida, Y; Suzuki, Y; Tada, K; Tomii, K; Tomioka, H, 2011
)
0.37
" The incidence of adverse events was 22."( Efficacy and safety of itraconazole as empirical antifungal therapy in febrile neutropenic patients with hematologic malignancies: an open-lable, multicenter, observational trial in a Chinese cohort.
Cheng, S; Huang, XJ; Jin, J; Shen, ZX; Zhou, JF; Zou, P, 2011
)
0.37
" Adverse events occurred in 6 of the 17 patients (35."( The clinical efficacy and safety of micafungin-itraconazole combination therapy in patients with pulmonary aspergilloma.
Fujita, M; Harada, E; Ikegame, S; Kajiki, A; Matsumoto, T; Nakanishi, Y; Ouchi, H; Tao, Y; Uchino, J; Watanabe, K, 2012
)
0.38
" Adverse effects occurred in 9 of 60 patients (15."( Clinical efficacy and safety of intravenous itraconazole in the management of invasive candidiasis in patients of surgery and critical care.
Aikawa, N; Fujishima, S; Mikamo, H; Oda, S; Takesue, Y, 2012
)
0.38
" Significant differences in incidence of withdrawal due to an adverse event (4."( Multicenter, randomized, open-label study comparing the efficacy and safety of micafungin versus itraconazole for prophylaxis of invasive fungal infections in patients undergoing hematopoietic stem cell transplant.
Chen, H; Chen, X; Han, M; Hu, J; Huang, H; Huang, X; Lai, Y; Liu, T; Wang, J; Wu, D; Zhu, H; Zou, P, 2012
)
0.38
" Adverse events such as liver dysfunction and heart failure were observed in 9 of the 24 patients."( Efficacy and safety of short- and long-term treatment of itraconazole on chronic necrotizing pulmonary aspergillosis in multicenter study.
Ando, T; Kamei, K; Kurashima, A; Niki, Y; Oritsu, M; Yamamoto, T; Yoshida, K, 2012
)
0.38
"To investigate spontaneous reporting relationships between representative antifungal agents and congestive heart failure (CHF)-related adverse events (AE) we performed multiple disproportionality analyses of the US FDA AERS database."( A quantitative analysis of the spontaneous reporting of congestive heart failure-related adverse events with systemic anti-fungal drugs.
Hauben, M; Hung, EY, 2013
)
0.39
"Tricyclic antidepressants, not influencing the P450 3A4 activity, are safe in combination with drugs of other groups used in the treatment of comorbid patients."( [Preclinical investigation of pharmaceuticals impact against cytochrome P450 activity and prognosis of substrate affinity as means for providing substrate therapy safety].
Baĭchorov, IKh; Fomin, EV; Shikh, EV; Sizova, ZhM, 2013
)
0.39
"Itraconazole injection was an effective and safe agent in targeted and diagnostic- driven antifungal therapy for immunocompromised or neutropenic febrile patients with hematological malignancies."( [Efficacy and safety of intravenous itraconazole in different antifungal strategies for patients undergoing intensive chemotherapy or hematopoietic stem cell transplantation].
Huang, X; Ji, Y; Xu, L, 2014
)
0.4
"21 adult asthmatics with SAFS (n = 11) and ABPA (n = 10) who had either failed itraconazole (n = 8), voriconazole proceeded by itraconazole (n = 5) or developed adverse events (AEs) to either agent (n = 7) were treated with 10mg of NAB (Fungizone) twice daily."( Efficacy and safety of nebulised amphotericin B (NAB) in severe asthma with fungal sensitisation (SAFS) and allergic bronchopulmonary aspergillosis (ABPA).
Chishimba, L; Denning, DW; Langridge, P; Niven, RM; Powell, G, 2015
)
0.42
"Combination of itraconazole and SSKI is an effective treatment modality for RFC with relatively faster onset of action, low relapse rates, and minimal adverse effects."( A prospective case series evaluating efficacy and safety of combination of itraconazole and potassium iodide in rhinofacial conidiobolomycosis.
Dogra, S; Gupta, M; Kaur, RJ; Manhas, A; Narang, T; Saikia, UN, 2016
)
0.43
" Grade 3 adverse events including hyperbilirubinemia (2 vs."( Efficacy and safety of micafungin versus intravenous itraconazole as empirical antifungal therapy for febrile neutropenic patients with hematological malignancies: a randomized, controlled, prospective, multicenter study.
Choi, CW; Jang, JH; Jeong, SH; Kim, DY; Kim, JS; Kim, SH; Mun, YC; Park, JS, 2016
)
0.43
"Itraconazole is safe and effective at a dose of 5 mg/kg per day in a short duration of therapy for superficial fungal infections and 10 mg/kg per day for systemic fungal infections in infants."( Efficacy and safety of itraconazole use in infants.
Chen, S; Feng, XW; Lama, J; Ran, X; Ran, YP; Sun, KY, 2016
)
0.43
" Adverse events occurred in 53 subjects (33 in the miconazole group and 20 in the itraconazole group)."( The Efficacy and Safety of Miconazole Nitrate Mucoadhesive Tablets versus Itraconazole Capsules in the Treatment of Oral Candidiasis: An Open-Label, Randomized, Multicenter Trial.
Chou, L; Guan, X; Han, Y; Hua, H; Lin, M; Liu, X; Liu, Y; Wang, Q; Wang, W; Yan, Z; Zhang, H; Zhu, S; Zhu, X, 2016
)
0.43
" Physicians should be cautious about thrombocytopenic purpura occurring as a rare and serious adverse event of miconazole nitrate."( The Efficacy and Safety of Miconazole Nitrate Mucoadhesive Tablets versus Itraconazole Capsules in the Treatment of Oral Candidiasis: An Open-Label, Randomized, Multicenter Trial.
Chou, L; Guan, X; Han, Y; Hua, H; Lin, M; Liu, X; Liu, Y; Wang, Q; Wang, W; Yan, Z; Zhang, H; Zhu, S; Zhu, X, 2016
)
0.43
" In addition to commonly described adverse effects, there have been few reports of heart failure with its use."( Cardiotoxicity with Itraconazole.
Paul, V; Rawal, H, 2017
)
0.46
" However, addition of emulsifiers to stabilize the formulation may cause toxic effects."( Cytotoxicity screening of emulsifiers for pulmonary application of lipid nanoparticles.
Corzo, C; Fröhlich, E; Öhlinger, K; Salar-Behzadi, S; Steiner, V, 2019
)
0.51
"The tested emulsifiers showed overall low cytotoxicity with less pronounced adverse effects in human cells than in murine macrophages."( Cytotoxicity screening of emulsifiers for pulmonary application of lipid nanoparticles.
Corzo, C; Fröhlich, E; Öhlinger, K; Salar-Behzadi, S; Steiner, V, 2019
)
0.51
" Being human cells, they appear more suitable for the screening of adverse effects in human lungs."( Cytotoxicity screening of emulsifiers for pulmonary application of lipid nanoparticles.
Corzo, C; Fröhlich, E; Öhlinger, K; Salar-Behzadi, S; Steiner, V, 2019
)
0.51
"Oral itraconazole has variable pharmacokinetics and risks of adverse events associated with high plasma exposure."( A phase 1/1b study of PUR1900, an inhaled formulation of itraconazole, in healthy volunteers and asthmatics to study safety, tolerability and pharmacokinetics.
Bedwell, P; Connor, L; Curran, AK; Hava, DL; Henderson, D; Johnson, P; Kane, K; Khan, N; Kramer, S; Layton, G; McKenzie, L; Perry, J; Roach, J; Singh, D; Swann, C; Tan, L, 2020
)
0.56
"None of the adverse events considered as at least possibly related to study treatment were moderate or severe, and none were classed as serious."( A phase 1/1b study of PUR1900, an inhaled formulation of itraconazole, in healthy volunteers and asthmatics to study safety, tolerability and pharmacokinetics.
Bedwell, P; Connor, L; Curran, AK; Hava, DL; Henderson, D; Johnson, P; Kane, K; Khan, N; Kramer, S; Layton, G; McKenzie, L; Perry, J; Roach, J; Singh, D; Swann, C; Tan, L, 2020
)
0.56
"PUR1900 was safe and well-tolerated under the study conditions."( A phase 1/1b study of PUR1900, an inhaled formulation of itraconazole, in healthy volunteers and asthmatics to study safety, tolerability and pharmacokinetics.
Bedwell, P; Connor, L; Curran, AK; Hava, DL; Henderson, D; Johnson, P; Kane, K; Khan, N; Kramer, S; Layton, G; McKenzie, L; Perry, J; Roach, J; Singh, D; Swann, C; Tan, L, 2020
)
0.56
"This systematic review and network meta-analysis compared the efficacy (as per mycological cure) and adverse event rates of three oral antifungal medications in the treatment of dermatophyte toenail onychomycosis, namely terbinafine, itraconazole and fluconazole."( The efficacy and safety of pulse vs. continuous therapy for dermatophyte toenail onychomycosis.
Bamimore, MA; Foley, KA; Gupta, AK; Piguet, V; Shear, NH; Stec, N, 2020
)
0.56
" There were no significant differences in the likelihood of adverse events between any continuous and pulse regimens of terbinafine, itraconazole and fluconazole."( The efficacy and safety of pulse vs. continuous therapy for dermatophyte toenail onychomycosis.
Bamimore, MA; Foley, KA; Gupta, AK; Piguet, V; Shear, NH; Stec, N, 2020
)
0.56
" Our results indicate that in the treatment of dermatophyte toenail onychomycosis, the continuous and pulse regimens for terbinafine and itraconazole have similar efficacies and rates of adverse events."( The efficacy and safety of pulse vs. continuous therapy for dermatophyte toenail onychomycosis.
Bamimore, MA; Foley, KA; Gupta, AK; Piguet, V; Shear, NH; Stec, N, 2020
)
0.56
"To classify the most common adverse reactions with the oral onychomycosis medications terbinafine, itraconazole, and off-label fluconazole."( Retrospective analysis of adverse events with systemic onychomycosis medications reported to the United States Food and Drug Administration.
Lipner, SR; Wang, Y, 2021
)
0.62
"The United States Food and Drug Administration Adverse Event Reporting (FAERS) database was analyzed for common adverse reactions with terbinafine, itraconazole, and off-label fluconazole."( Retrospective analysis of adverse events with systemic onychomycosis medications reported to the United States Food and Drug Administration.
Lipner, SR; Wang, Y, 2021
)
0.62
"The most common adverse reaction with terbinafine was taste disturbance and the most common adverse events with itraconazole and fluconazole were drug interactions."( Retrospective analysis of adverse events with systemic onychomycosis medications reported to the United States Food and Drug Administration.
Lipner, SR; Wang, Y, 2021
)
0.62
"Patients should be counseled that taste disturbance with terbinafine is the most common adverse event."( Retrospective analysis of adverse events with systemic onychomycosis medications reported to the United States Food and Drug Administration.
Lipner, SR; Wang, Y, 2021
)
0.62
"The aim of the study was to determine whether it is safe to stop secondary prophylaxis in patients with talaromycosis after immune reconstitution with a sustained increase in CD4 count to ≥ 100 cells/µL after antiretroviral therapy (ART)."( Is stopping secondary prophylaxis safe in HIV-positive talaromycosis patients? Experience from Myanmar.
Ashley, E; Aung, Y; Deed, X; Hlaing, M; Mclean, A; Smithuis, F; Tun, N; Wilkins, E, 2020
)
0.56
" Clinicians should be aware of pseudohyperaldosteronism as a possible adverse effect of itraconazole, and we recommend monitoring potassium levels and blood pressure in all patients receiving this drug over a longer period of time."( Pseudohyperaldosteroism during itraconazole treatment: a hitherto neglected clinically significant side effect.
Brandi, SL; Eldrup, E; Feltoft, CL; Serup, J, 2021
)
0.62
" PK parameters, dose proportionality, adverse events and taste assessments (taste strips; dysgeusia questionnaire) were evaluated."( First-in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics.
Baumann, S; Chang, X; Friedrich, C; Gashaw, I; Hummel, T; Klein, S; Thuß, U, 2022
)
0.72
"The PK profile, particularly the long half-life, and favourable tolerability with no taste-related adverse events, supports the further development of eliapixant in disorders with underlying P2X3 receptor-mediated neuronal hypersensitisation."( First-in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics.
Baumann, S; Chang, X; Friedrich, C; Gashaw, I; Hummel, T; Klein, S; Thuß, U, 2022
)
0.72
"This study concluded that the test drugs (IHA and HK) were safe and effective in the treatment of PV."( Evaluation of the efficacy and safety of Unani Formulations in Pityriasis Versicolor: A randomized controlled trial.
Fatima, SH; Ismail, BA; Minhajuddin, A; Nawab, M; Rasheed Naikodi, MA, 2022
)
0.72
" The primary endpoint was clinical cure at the end-of-treatment period [visit 4 (V4)] while secondary endpoints were clinical remission rates, partial remission rates, mycological cure, clinical relapse, and adverse events (AEs)."( Efficacy and safety of miconazole muco-adhesive tablet versus itraconazole in oropharyngeal candidiasis: A randomized, multi-centered, double-blind, phase 3 trial.
Chai, H; Chen, Q; Duan, N; Fan, Y; Fei, W; Guan, X; Hua, H; Jia, C; Jiang, L; Kong, H; Liu, J; Liu, Q; Lu, H; Lun, W; Luo, Z; Shen, X; Tang, G; Wang, H; Wang, W; Wang, Y; Xu, J; Yan, Z; Zhang, T; Zhao, J; Zhou, H, 2022
)
0.72
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

Itraconazole significantly increased the Cmax of zopiclone from 49 to 63 ng. Despite some pharmacokinetic differences, formulation-specific dosages do not appear to be necessary.

ExcerptReferenceRelevance
" Based on the pharmacokinetic profile, 100 mg itraconazole daily was then compared with 500 mg ultramicronized griseofulvin daily using a fixed treatment schedule of 15 days in tinea corporis and/or cruris and 30 days in tinea pedis and/or manus."( Itraconazole compared with griseofulvin in the treatment of tinea corporis/cruris and tinea pedis/manus: an interpretation of the clinical results of all completed double-blind studies with respect to the pharmacokinetic profile.
Cauwenbergh, G; De Doncker, P; Janssen, PA; Lachapelle, JM; Tennstedt, D, 1992
)
0.28
" and median Cmax were 412 +/- 227 ng/mL and 375 ng/mL respectively and for ITRA-PEG (n = 5), 315 +/- 177 ng/mL and 327 ng/mL."( Comparison of the multiple dose pharmacokinetics of two formulations of itraconazole during remission induction for acute myeloblastic leukaemia.
Bradford, CR; Copplestone, JA; Prentice, AG; Warnock, DW, 1991
)
0.28
"Orally active antifungals have different physicochemical and pharmacokinetic properties."( Pharmacokinetics of oral antifungals and their clinical implications.
Cauwenbergh, G; Heykants, J; Lavrijsen, K; Meuldermans, W; Van Peer, A; Woestenborghs, R, 1990
)
0.28
"Itraconazole is an orally active triazole antifungal drug which has demonstrated a broad spectrum of activity and a favourable pharmacokinetic profile."( Itraconazole. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in superficial and systemic mycoses.
Clissold, SP; Grant, SM, 1989
)
0.28
" The pharmacokinetics of itraconazole in man are characterized by a good oral absorption, an extensive tissue distribution with tissue concentrations many times higher than in plasma, a relatively long elimination half-life of about one day and a biotransformation into a large number of metabolites."( The clinical pharmacokinetics of itraconazole: an overview.
Cauwenbergh, G; Heykants, J; Lavrijsen, K; Meuldermans, W; Van Cutsem, J; Van de Velde, V; Van Peer, A; Van Rooy, P; Woestenborghs, R, 1989
)
0.28
" All data support dose-dependent pharmacokinetic behavior for itraconazole."( Pharmacokinetics of itraconazole following oral administration to normal volunteers.
Fetchick, R; Graybill, JR; Hardin, TC; Kuhn, JG; Rinaldi, MG; Woestenborghs, R, 1988
)
0.27
" With fluconazole the pharmacokinetic parameters after food were essentially the same for the 2 races."( Comparative pharmacokinetics of fluconazole and of itraconazole in Japanese and in German subjects.
Albrecht, M; Laufen, H; Wildfeuer, A; Yeates, RA; Zimmermann, T, 1995
)
0.29
"05; ANOVA) in the pharmacokinetic parameters of fluconazole (AUC, Cmax, Tmax) were found during the three days of the trial."( Administration of the antimycotic agents fluconazole and itraconazole to leukaemia patients: a comparative pharmacokinetic study.
Lazo de la Vega, S; Pfaff, G; Volkow, P; Yeates, RA, 1994
)
0.29
" Half-life of itraconazole ranges between 17 to 21 h and 99."( Itraconazole: pharmacokinetics and indications.
Arechavala, AI; Negroni, R, 1993
)
0.29
" Single-dose terfenadine administration (120 mg) was accompanied by pharmacokinetic profiles and serial determination of the QTc interval for 12 hours."( Itraconazole affects single-dose terfenadine pharmacokinetics and cardiac repolarization pharmacodynamics.
Cantilena, LR; Honig, PK; Hull, R; Smith, JE; Wortham, DC; Zamani, K, 1993
)
0.29
"Blood samples were obtained for pharmacokinetic analyses immediately before dosing and at regular intervals up to 96 hours after each dose."( Effect of food on the pharmacokinetics of a new hydroxypropyl-beta-cyclodextrin formulation of itraconazole.
Cauwenbergh, GF; De Beule, KL; Heykants, JJ; Van de Velde, VJ; Van Peer, AP; Van Rooy, P; Woestenborghs, RJ,
)
0.13
" The mean times to peak concentration for both the parent compound and its metabolite were significantly shorter under fasting than under nonfasting conditions."( Effect of food on the pharmacokinetics of a new hydroxypropyl-beta-cyclodextrin formulation of itraconazole.
Cauwenbergh, GF; De Beule, KL; Heykants, JJ; Van de Velde, VJ; Van Peer, AP; Van Rooy, P; Woestenborghs, RJ,
)
0.13
" 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
"Itraconazole significantly increased the Cmax of zopiclone from 49 to 63 ng."( Effect of itraconazole on the pharmacokinetics and pharmacodynamics of zopiclone.
Jalava, KM; Neuvonen, PJ; Olkkola, KT, 1996
)
0.29
"Itraconazole has a statistically significant pharmacokinetic interaction with zopiclone but this is only of limited clinical importance, at least in young adults."( Effect of itraconazole on the pharmacokinetics and pharmacodynamics of zopiclone.
Jalava, KM; Neuvonen, PJ; Olkkola, KT, 1996
)
0.29
"Itraconazole treatment did not significantly change the peak concentration of astemizole (0."( Influence of itraconazole on the pharmacokinetics and electrocardiographic effects of astemizole.
Lefebvre, RA; Van Peer, A; Woestenborghs, R, 1997
)
0.3
"Since ceftriaxone and itraconazole are highly protein bound, are excreted via a biliary pathway, and are in vitro modulators of the efflux pump P glycoprotein, a pharmacokinetic interaction between these antimicrobial agents can be hypothesized."( Pharmacokinetic interaction between itraconazole and ceftriaxone in Yucatan miniature pigs.
Cavalier, A; Elkhaïli, H; Geisert, J; Jehl, F; Levêque, D; Monteil, H; Nobelis, P; Peter, JD; Salmon, J; Salmon, Y, 1997
)
0.3
" 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
" The increases in digoxin Cmax and T(1/2) by itraconazole were not statistically significant."( Itraconazole decreases renal clearance of digoxin.
Jalava, KM; Neuvonen, PJ; Partanen, 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
" The pharmacokinetic and pharmacologic properties provide the basis of their activity and are related to their efficacy and safety in dermatophyte infections."( Pharmacokinetics and pharmacology of terbinafine and itraconazole.
Leyden, J, 1998
)
0.3
" With concomitant omeprazole treatment, the mean AUC0-24 and Cmax of itraconazole were significantly reduced by 64% and 66%, respectively."( Effect of omeprazole on the pharmacokinetics of itraconazole.
Jaruratanasirikul, S; Sriwiriyajan, S, 1998
)
0.3
" Plasma concentrations of itraconazole were measured by HPLC, and pharmacokinetic parameters; Cmax, Tmax, T1/2, AUC, and AUC corrected by human body surface area: AUC/S, were calculated."( Effect of grapefruit juice on pharmacokinetics of itraconazole in healthy subjects.
Hidaka, T; Ishizuka, T; Kawakami, M; Matsuki, Y; Nakamura, H; Suzuki, K, 1998
)
0.3
"Grapefruit juice had no effect on any pharmacokinetic parameter of itraconazole."( Effect of grapefruit juice on pharmacokinetics of itraconazole in healthy subjects.
Hidaka, T; Ishizuka, T; Kawakami, M; Matsuki, Y; Nakamura, H; Suzuki, K, 1998
)
0.3
"Coadministration of grapefruit juice did not affect any pharmacokinetic parameter of itraconazole while that of orange juice decreased the parameters of T1/2, AUC, and AUC/S of the drug."( Effect of grapefruit juice on pharmacokinetics of itraconazole in healthy subjects.
Hidaka, T; Ishizuka, T; Kawakami, M; Matsuki, Y; Nakamura, H; Suzuki, K, 1998
)
0.3
" The mean values of Cmin ITRA and OH-ITRA, respectively, were 287 +/- 109 ng/ml and 629 +/- 227 ng/ml at day -1 and 378 +/- 147 ng/ml and 725 +/- 242 ng/ml at day +1."( Pharmacokinetics of itraconazole oral solution in allogeneic bone marrow transplant patients receiving total body irradiation.
Belhabri, A; Chwetzoff, E; Fiere, D; Kranzhöfer, N; Le Moing, JP; Levron, JC; Michallet, M; Persat, F; Piens, MA; Prat, C, 1998
)
0.3
"The effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin, two inhibitors of HMG-CoA reductase with different pharmacokinetic properties, were studied."( Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin.
Kantola, T; Kivistö, KT; Neuvonen, PJ, 1998
)
0.3
" Itraconazole had no significant effects on the pharmacokinetic parameters of levosimendan."( The CYP3A4 inhibitor intraconazole does not affect the pharmacokinetics of a new calcium-sensitizing drug levosimendan.
Antila, S; Honkanen, T; Lehtonen, L; Neuvonen, PJ, 1998
)
0.3
"10 ml/min per kg) and prolonged the elimination half-life (15."( Effect of itraconazole on the single oral dose pharmacokinetics and pharmacodynamics of alprazolam.
Furukori, H; Kaneko, S; Kondo, T; Nagasaki, T; Ohkubo, T; Otani, K; Sugawara, K; Yasui, N, 1998
)
0.3
"05) and the Cmax by 57% (P<0."( Interactions of buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of buspirone.
Kivistö, KT; Lamberg, TS; Neuvonen, PJ, 1999
)
0.3
" Based on these results, the pharmacokinetic interaction between DGX and ITZ may be due not only to a reduction in the renal clearance but also to a reduction in the metabolic clearance of DGX by ITZ."( Effect of itraconazole on the pharmacokinetics of digoxin in guinea pigs.
Hibino, J; Iga, T; Kotaki, H; Nishihara, K; Sawada, Y, 1999
)
0.3
" The Medline electronic database from 1966 through 1998 was used to identify clinical studies of the pharmacokinetic effect of drugs on these three benzodiazepines."( Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam, and triazolam.
Balian, JD; Flockhart, DA; Yuan, R, 1999
)
0.3
"Concomitant administration of diclofenac reduced the partial clearance of quinidine by N-oxidation by 27%, while no effect was found for other pharmacokinetic parameters of quinidine."( Effect of diclofenac, disulfiram, itraconazole, grapefruit juice and erythromycin on the pharmacokinetics of quinidine.
Brosen, K; Damkier, P; Hansen, LL, 1999
)
0.3
"05), while it had no significant effect on other pharmacokinetic variables of the enantiomers."( Effect of itraconazole on the pharmacokinetics of bupivacaine enantiomers in healthy volunteers.
Neuvonen, PJ; Olkkola, KT; Palkama, VJ, 1999
)
0.3
"The objective of this study was to evaluate the pharmacodynamic activity of fluconazole, itraconazole, and amphotericin B against Candida albicans."( Pharmacodynamics of fluconazole, itraconazole, and amphotericin B against Candida albicans.
Burgess, DS; Hardin, TC; Hastings, RW; Rinaldi, MG; Summers, KK, 2000
)
0.31
"The reversal effect of itraconazole on P-glycoprotein (P-gp)-mediated resistance of vinblastine, daunorubicin and doxorubicin was analyzed from a cellular pharmacokinetic point of view, namely by [3H]azidopine photoaffinity labeling, intracellular accumulation and transcellular transport experiments."( Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
Komada, F; Nishiguchi, K; Okumura, K; Sakaeda, T; Takara, K; Tanigawara, Y, 1999
)
0.3
" Pharmacokinetic parameters [AUC(0-infinity), AUC(0-tn), peak concentration (Cmax), time to reach Cmax (tmax), and half-life (t1/2)] were determined for parent statins and major metabolites."( Itraconazole alters the pharmacokinetics of atorvastatin to a greater extent than either cerivastatin or pravastatin.
Agarwal, V; Lasseter, KC; Lettieri, J; Mazzu, AL; Shamblen, EC; Sundaresen, P, 2000
)
0.31
" However, itraconazole dramatically increased atorvastatin AUC (150%), Cmax (38%), and t1/2 (30%) (P < ."( Itraconazole alters the pharmacokinetics of atorvastatin to a greater extent than either cerivastatin or pravastatin.
Agarwal, V; Lasseter, KC; Lettieri, J; Mazzu, AL; Shamblen, EC; Sundaresen, P, 2000
)
0.31
" There were no significant changes in the pharmacokinetic parameters of the parent ropivacaine after ingestion of clarithromycin or itraconazole."( Effect of clarithromycin and itraconazole on the pharmacokinetics of ropivacaine.
Ahonen, J; Jokinen, MJ; Neuvonen, PJ; Olkkola, KT, 2001
)
0.31
" 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
" Pharmacokinetic sampling was performed after the first dose and for up to 120 h after the last dose, and antifungal efficacy was evaluated by standardized scoring of the oropharynx."( Safety, pharmacokinetics, and pharmacodynamics of cyclodextrin itraconazole in pediatric patients with oropharyngeal candidiasis.
Chiou, CC; Dad, L; Groll, AH; Mickiene, D; Piscitelli, SC; Roden, M; Townley, E; Walsh, TJ; Wood, L, 2002
)
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
)
0.32
" Pharmacokinetic parameters were calculated by a non-compartmental model."( Pharmacokinetics of lower doses of saquinavir soft-gel caps (800 and 1200 mg twice daily) boosted with itraconazole in HIV-1-positive patients.
Burger, D; Cardiello, PG; Cooper, DA; Hoetelmans, R; Lange, JM; Mahanontharit, A; Phanuphak, P; Ruxrungtham, K; Samor, T, 2003
)
0.32
" The time course of the pharmacodynamic effects of bromazepam on the central nervous system was assessed using a subjective rating of sedation, continuous number addition test and electroencephalography up to 21."( The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers.
Kotegawa, T; Kuwatani, K; Nakano, S; Oda, M; Ohtani, Y; Tsutsumi, K, 2003
)
0.32
" The mean (+/-SD) values of area under the plasma concentration-time curve and elimination half-life for placebo versus itraconazole were 1328+/-330 ng h/ml versus 1445+/-419 ng h/ml and 32."( The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers.
Kotegawa, T; Kuwatani, K; Nakano, S; Oda, M; Ohtani, Y; Tsutsumi, K, 2003
)
0.32
" Hence, the method is suitable for use in pharmacokinetic and bioavailability studies of itraconazole."( Liquid chromatographic method for the determination of plasma itraconazole and its hydroxy metabolite in pharmacokinetic/bioavailability studies.
Nisar, UR; Wong, JW; Yuen, KH, 2003
)
0.32
" We determined the extent of the pharmacokinetic interaction between cyclosporine and itraconazole oral solution in renal transplant recipients and the effect on daily drug costs."( Beneficial pharmacokinetic interaction between cyclosporine and itraconazole in renal transplant recipients.
Capitano, B; Florea, NR; Hull, D; Leitz, GJ; Nicolau, DP; Nightingale, CH, 2003
)
0.32
" Once at steady state, blood samples were collected over 12 hours for pharmacokinetic evaluation of cyclosporine, itraconazole, and hydroxy-itraconazole."( Beneficial pharmacokinetic interaction between cyclosporine and itraconazole in renal transplant recipients.
Capitano, B; Florea, NR; Hull, D; Leitz, GJ; Nicolau, DP; Nightingale, CH, 2003
)
0.32
" The aim of this study was to elucidate clinical effectiveness and pharmacokinetic profiles of a 6-month continuous itraconazole treatment at a daily dose of 100 mg."( Clinical and pharmacokinetic studies of continuous itraconazole for the treatment of onychomycosis.
Aragane, Y; Kawada, A; Tezuka, T, 2004
)
0.32
" Dialysis had no effect on the half-life and clearance of ITC or OH-ITC."( Pharmacokinetics of intravenous itraconazole in stable hemodialysis patients.
Finkel, KW; Leitz, GJ; Mohr, JF; Ostrosky-Zeichner, L; Rex, JH; Rodriguez, JR, 2004
)
0.32
" The pharmacokinetic profile of intravenous midazolam was characterized before and after itraconazole administration (200 mg once daily for 4 days) and also after rifampin (INN, rifampicin) pretreatment (600 mg once daily for 10 days), with a washout period of 2 weeks in between."( Effect of the CYP3A5 genotype on the pharmacokinetics of intravenous midazolam during inhibited and induced metabolic states.
Cho, JY; Chung, JY; Hong, KS; Jang, IJ; Kim, JR; Lim, HS; Liu, KH; Oh, DS; Shin, JG; Shin, SG; Yi, SY; Yu, KS, 2004
)
0.32
"The pharmacokinetic profiles of midazolam and of its hydroxy metabolites did not show differences between the genotype groups under basal and induced metabolic conditions."( Effect of the CYP3A5 genotype on the pharmacokinetics of intravenous midazolam during inhibited and induced metabolic states.
Cho, JY; Chung, JY; Hong, KS; Jang, IJ; Kim, JR; Lim, HS; Liu, KH; Oh, DS; Shin, JG; Shin, SG; Yi, SY; Yu, KS, 2004
)
0.32
"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
)
0.32
" No statistically significant differences were observed in any of the pharmacokinetic parameters; peak concentrations, concentration peak times or elimination half-lives of lidocaine or monoethylglycinexylidide."( Effect of itraconazole on the pharmacokinetics of inhaled lidocaine.
Isohanni, MH; Neuvonen, PJ; Olkkola, KT, 2004
)
0.32
" Studies compared the multiple-dose pharmacokinetic interaction profiles of pravastatin, simvastatin, and atorvastatin when coadministered with 4 inhibitors of cytochrome P450-3A4 isoenzymes in healthy subjects."( Comparative pharmacokinetic interaction profiles of pravastatin, simvastatin, and atorvastatin when coadministered with cytochrome P450 inhibitors.
Jacobson, TA, 2004
)
0.32
"1 ng ml h(-1)), and prolonged the elimination half-life (4."( Effect of itraconazole on the pharmacokinetics and pharmacodynamics of a single oral dose of brotizolam.
Kaneko, S; Kondo, T; Ohkubo, T; Osanai, T; Yasui, N, 2004
)
0.32
"To determine whether coadministration of the cytochrome P450 3A4 (CYP3A4) inhibitors itraconazole or grapefruit juice will modify the pharmacokinetic profile of telithromycin, and to assess the safety of telithromycin."( Effects of itraconazole or grapefruit juice on the pharmacokinetics of telithromycin.
Bhargava, VO; Leroy, B; Montay, G; Shi, J, 2005
)
0.33
"Standard pharmacokinetic and safety measurements were performed."( Effects of itraconazole or grapefruit juice on the pharmacokinetics of telithromycin.
Bhargava, VO; Leroy, B; Montay, G; Shi, J, 2005
)
0.33
" The pharmacokinetic parameters of ARIPIPRAZOLE and its main metabolite OPC-14857 were determined."( Influence of itraconazole co-administration and CYP2D6 genotype on the pharmacokinetics of the new antipsychotic ARIPIPRAZOLE.
Azuma, J; Fukuda, T; Inaba, A; Koue, T; Kubo, M; Maune, H; Takeda, H, 2005
)
0.33
"A population pharmacokinetic analysis of cyclosporine (CsA) was performed, and the influence of covariates on CsA oral clearance and relative bioavailability was investigated."( Population pharmacokinetics of cyclosporine in cardiopulmonary transplant recipients.
Akhlaghi, F; Baheti, G; Rosenbaum, SE; Trull, AK, 2005
)
0.33
" Consequently, we have used a previously published decision-making algorithm to determine whether clinical pharmacokinetic monitoring of itraconazole is warranted."( Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients.
Buchkowsky, SS; Ensom, MH; Partovi, N, 2005
)
0.33
" The first study evaluated in vivo release of ITZ from subcutaneously injected controlled-release gel formulations and the second study compared pharmacokinetic parameters for two ITZ oral suspensions."( Studies on itraconazole delivery and pharmacokinetics in mallard ducks (Anas platyrhynchos).
Clemons, KV; Clifford, A; Craigmill, AL; Ina, JH; Laizure, SC; Nugent-Deal, JP; Stevens, DA; Sun, Y; Tell, LA; Woods, L, 2005
)
0.33
"In the placebo phase, pharmacokinetic parameters of fexofenadine showed no statistically significant difference between 2 MDR1 haplotypes; the area under the curve from time 0 to infinity (AUC(0-infinity)) of fexofenadine in the T/T and G/C groups was 5194."( Effect of itraconazole on the pharmacokinetics and pharmacodynamics of fexofenadine in relation to the MDR1 genetic polymorphism.
Cha, IJ; Choi, YG; Hong, WS; Lee, SS; Nguyen, PM; Shin, JG; Shon, JH; Yoon, YR, 2005
)
0.33
" Based on these findings, three clinical studies were carried out to investigate pharmacokinetic drug interactions in vivo with gefitinib."( Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol.
Laight, A; Leadbetter, J; McKillop, D; Ranson, M; Smith, RP; Swaisland, HC; Wild, MJ, 2005
)
0.33
" Data were analyzed by compartmental and noncompartmental pharmacokinetic methods."( Pharmacokinetics and tissue distribution of itraconazole after oral and intravenous administration to horses.
Davis, JL; Papich, MG; Salmon, JH, 2005
)
0.33
"94 L/kg) and a long half-life (11."( Pharmacokinetics and tissue distribution of itraconazole after oral and intravenous administration to horses.
Davis, JL; Papich, MG; Salmon, JH, 2005
)
0.33
" Itraconazole had no statistically significant effect on any of the pharmacokinetic or pharmacodynamic variables of atenolol."( Effect of itraconazole on the pharmacokinetics of atenolol.
Backman, JT; Lilja, JJ; Neuvonen, PJ, 2005
)
0.33
"A single-institution, open-label prospective pharmacokinetic evaluation of the interaction between intravenous itraconazole and intravenous cyclosporin A and tacrolimus was conducted in allogeneic hematopoietic stem cell transplant recipients."( Pharmacokinetic evaluation of the drug interaction between intravenous itraconazole and intravenous tacrolimus or intravenous cyclosporin A in allogeneic hematopoietic stem cell transplant recipients.
Boyette, RM; Leather, H; Tian, L; Wingard, JR, 2006
)
0.33
" The pharmacokinetics of haloperidol and its pharmacodynamic effects measured for QTc prolongation and neurologic side effects were evaluated after a single dose of 5 mg haloperidol following a pretreatment of placebo or itraconazole at 200 mg/d for 10 days in a randomized crossover manner."( Combined effects of itraconazole and CYP2D6*10 genetic polymorphism on the pharmacokinetics and pharmacodynamics of haloperidol in healthy subjects.
Cha, IJ; Jung, HJ; Kim, KA; Park, JY; Shim, JC; Shin, JG; Shon, JH; Yoon, YR, 2006
)
0.33
" Elimination half-life and renal clearance in the itraconazole phase were not altered significantly compared with those in the control phase."( Effects of itraconazole and diltiazem on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein.
Shimizu, M; Sugawara, K; Tateishi, T; Uno, T, 2006
)
0.33
" Although the elimination half-life and the renal clearance of fexofenadine remained relatively constant, a single administration of itraconazole with fexofenadine significantly increased mean area under the plasma concentration-time curve (AUC(0-infinity)) of fexofenadine (1701/3554, 4308, and 4107 ng h/ml for control; 50 mg, 100 mg, and 200 mg of itraconazole, respectively)."( Lack of dose-dependent effects of itraconazole on the pharmacokinetic interaction with fexofenadine.
Shimizu, M; Sugawara, K; Tateishi, T; Uno, T, 2006
)
0.33
"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
"The primary objective of the study was to estimate the population pharmacokinetic parameters for itraconazole and hydroxy-itraconazole, in particular, the relative oral bioavailability of the capsule compared with solution in adult cystic fibrosis patients, in order to develop new dosing guidelines."( A d-optimal designed population pharmacokinetic study of oral itraconazole in adult cystic fibrosis patients.
Bell, SC; Charles, BG; Duffull, SB; France, M; Hennig, S; Miller, H; Wainwright, CE; Waterhouse, TH, 2007
)
0.34
" The pharmacokinetic profiles of ITZ-PM for itraconazole and its major metabolite, hydroxy-itraconazole, were comparable to those of the cyclodextrin formulations (Sporanox(R) Injection and Oral Solution) in rats and dogs."( A mixed polymeric micellar formulation of itraconazole: Characteristics, toxicity and pharmacokinetics.
Hwang, SJ; Kim, BO; Kim, SO; Seo, MH; Shim, M; Yi, Y; Yoon, HJ, 2007
)
0.34
" Although elimination half-life differed significantly (16."( Effect of itraconazole on pharmacokinetics of paroxetine: the role of gut transporters.
Inoue, Y; Kaneko, S; Niioka, T; Saito, M; Sato, Y; Yasui-Furukori, N, 2007
)
0.34
" Nevirapine pharmacokinetic studies were carried out starting with the seventh dose of nevirapine in the nevirapine regimen (on days 7-10 or 28-31) and the combination regimen (on days 49-52)."( Pharmacokinetic study of the interaction between itraconazole and nevirapine.
Jaruratanasirikul, S; Sriwiriyajan, S, 2007
)
0.34
"There was no significant difference in nevirapine pharmacokinetic parameters between the nevirapine and combination regimens."( Pharmacokinetic study of the interaction between itraconazole and nevirapine.
Jaruratanasirikul, S; Sriwiriyajan, S, 2007
)
0.34
" In this study, we aim to predict the effect of the CYP3A4 inhibitors, itraconazole (ITZ) and its primary metabolite, hydroxyitraconazole (OH-ITZ) on the pharmacokinetics of the anesthetic, midazolam (MDZ) and its metabolites, 1' hydroxymidazolam (1OH-MDZ) and 1' hydroxymidazolam glucuronide (1OH-MDZ-Glu) using mechanistic whole body physiologically-based pharmacokinetic simulation models."( Dynamically simulating the interaction of midazolam and the CYP3A4 inhibitor itraconazole using individual coupled whole-body physiologically-based pharmacokinetic (WB-PBPK) models.
Edginton, AN; Jang, IJ; Niederalt, C; Sevestre, M; Vossen, M; Willmann, S, 2007
)
0.34
" The terminal half-life of itraconazole was 524 min."( Pharmacokinetics, blood partition, and tissue distribution of itraconazole.
Lee, JH; Lee, MG; Shin, JH, 2004
)
0.32
" This study suggests that an important pharmacokinetic interaction between CIP and KTC or ITC is likely to occur when either of the two antifungal drugs is administered concomitantly with CIP."( Pharmacokinetic interaction of ketoconazole and itraconazole with ciprofloxacin.
Abou-Auda, HS; Al-Humayyd, MS; Mustafa, AA, 2008
)
0.35
"The population pharmacokinetic parameters of aripiprazole in healthy Japanese males were estimated using a nonlinear mixed effects model (NONMEM) program."( Nonlinear mixed effects model analysis of the pharmacokinetics of aripiprazole in healthy Japanese males.
Azuma, J; Fukuda, T; Funaki, T; Hashimoto, Y; Kayano, Y; Koue, T; Kubo, M; Takaai, M, 2007
)
0.34
"Although administration of antifungal agents, such as itraconazole (ITC) solution, for prophylaxis is the most promising strategy for the treatment of haematological malignancies, little is known about the population pharmacokinetic (PK) parameters."( Population pharmacokinetics of itraconazole solution used as prophylaxis for febrile neutropenia.
Fujimoto, Y; Horiike, S; Kanbayashi, Y; Matsumoto, Y; Nomura, K; Okamoto, K; Shimazaki, C; Shimizu, D; Shimura, K; Takagi, T; Taniwaki, M, 2008
)
0.35
"Therapeutic drug monitoring of any pharmacologic agent should be considered when there is both significant pharmacokinetic variability and strong, clinically relevant, exposure-effect relationships."( Therapeutic drug monitoring of antifungals: pharmacokinetic and pharmacodynamic considerations.
Andes, D; Smith, J, 2008
)
0.35
" Large interindividual variations were observed in area under the concentration curve values among patients."( Effects of cyclosporine a on single-dose pharmacokinetics of intravenous itraconazole in patients with hematologic malignancies.
Beijnen, JH; Bosch, TM; Huijgens, PC; Kessels, LW; Timmers, GJ; Veldkamp, AI; Wilhelm, AJ, 2008
)
0.35
"The pharmacokinetic parameters of atorvastatin were measured after intravenous (2 mg/kg) and intragastric (10 mg/kg) administration of atorvastatin in rats, which were pretreated with cyclosporin A (5, 10, and 20 mg/kg) or itraconazole (5, 10, and 20 mg/kg)."( Effects of cyclosporin A and itraconazole on the pharmacokinetics of atorvastatin in rats.
Chen, XJ; Dong, J; Sun, YB; Wang, GJ; Wang, L; Yu, X, 2008
)
0.35
"A rapid and highly sensitive liquid chromatography/electrospray ionization tandem mass spectrometric method (LC/ESI-MS/MS) for itraconazole determination in human plasma was validated and applied to pharmacokinetic and bioequivalence study in humans."( A sensitive validated LC-MS/MS method for quantification of itraconazole in human plasma for pharmacokinetic and bioequivalence study in 24 Korean volunteers.
Kang, JS; Kim, DS; Lee, MH; Park, JH; Park, YS; Rhim, SY; Shaw, LM, 2009
)
0.35
" It has been reported that physicochemical characteristics of these compounds are disparate, leading to different pharmacokinetic profiles."( Comparison of the oral pharmacokinetics of fluconazole and itraconazole in Mexicans.
Carrasco-Portugal, Mdel C; Flores-Murrieta, FJ; Landa, C, 2008
)
0.35
" Blood concentrations of everolimus were measured up to 240 min, and pharmacokinetic parameters were calculated."( Effect of itraconazole on the pharmacokinetics of everolimus administered by different routes in rats.
Inui, K; Katsura, T; Masuda, S; Sato, E; Yano, I; Yokomasu, A, 2009
)
0.35
" This article reviews the pharmacokinetic differences between fexofenadine enantiomers in humans and summarizes the previous reports that co-administration of P-glycoprotein inhibitors has altered the stereoselective pharmacokinetics of fexofenadine enantiomers."( Clinical pharmacokinetics of fexofenadine enantiomers.
Miura, M; Uno, T, 2010
)
0.36
" The most appropriate method for data analysis might be a semi-mechanistic population pharmacokinetic modelling approach."( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole.
Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010
)
0.36
" First, pharmacokinetic models of itraconazole and tesofensine were developed in parallel."( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole.
Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010
)
0.36
"This analysis presents a semi-mechanistic population pharmacokinetic approach that may be useful for the evaluation of DDI studies."( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole.
Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010
)
0.36
" Plasma concentrations of oxycodone and its oxidative metabolites were measured for 48 h, and pharmacodynamic effects were evaluated."( Effects of itraconazole on the pharmacokinetics and pharmacodynamics of intravenously and orally administered oxycodone.
Grönlund, J; Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Saari, TI, 2010
)
0.36
" Most of the pharmacokinetic changes in oral oxycodone were seen in the elimination phase, with modest effects by itraconazole on its peak concentration, which was increased by 45% (P=0."( Effects of itraconazole on the pharmacokinetics and pharmacodynamics of intravenously and orally administered oxycodone.
Grönlund, J; Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Saari, TI, 2010
)
0.36
"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
)
0.36
" Thus, we investigated whether a pharmacokinetic interaction occurs between the anti-fungal agent itraconazole and the anti-glycaemic drug metformin, as both drugs are commonly administered together to diabetic patients and are metabolized via hepatic CYP3A subfamily in rats."( Pharmacokinetic interaction between itraconazole and metformin in rats: competitive inhibition of metabolism of each drug by each other via hepatic and intestinal CYP3A1/2.
Choi, YH; Lee, BK; Lee, MG; Lee, U, 2010
)
0.36
" Drug concentrations were analyzed using standard pharmacokinetic methods."( Effects of compounding on pharmacokinetics of itraconazole in black-footed penguins (Spheniscus demersus).
Mitchell, MA; Papich, MG; Russell, G; Smith, JA, 2010
)
0.36
" Plasma concentrations of oxycodone and its oxidative metabolites were measured over 48 hours, and pharmacokinetic and pharmacodynamic parameters subsequently evaluated."( Effect of inhibition of cytochrome P450 enzymes 2D6 and 3A4 on the pharmacokinetics of intravenous oxycodone: a randomized, three-phase, crossover, placebo-controlled study.
Grönlund, J; Hagelberg, NM; Laine, K; Neuvonen, PJ; Olkkola, KT; Saari, TI, 2011
)
0.37
"To investigate the pharmacokinetic interaction between ciprofloxacin and itraconazole in healthy male volunteers."( Pharmacokinetic interactions between ciprofloxacin and itraconazole in healthy male volunteers.
Mahatthanatrakul, W; Ridtitid, W; Samaeng, M; Sriwiriyajan, S; Wongnawa, M, 2011
)
0.37
"Ten healthy male volunteers were assigned into a 2-sequence, 3-period pharmacokinetic interaction study."( Pharmacokinetic interactions between ciprofloxacin and itraconazole in healthy male volunteers.
Mahatthanatrakul, W; Ridtitid, W; Samaeng, M; Sriwiriyajan, S; Wongnawa, M, 2011
)
0.37
" The half-life and CL of itraconazole were not changed significantly."( Pharmacokinetic interactions between ciprofloxacin and itraconazole in healthy male volunteers.
Mahatthanatrakul, W; Ridtitid, W; Samaeng, M; Sriwiriyajan, S; Wongnawa, M, 2011
)
0.37
" Pharmacokinetic parameters were determined using non-compartmental methods."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
0.37
"To set up a population pharmacokinetic (PPK) model of cyclosporine A (CsA) in Chinese allogeneic hematopoietic stem cell transplantation (allo-HSCT) patients to provide reference for individualized medication in clinical practice."( Population pharmacokinetics of cyclosporine A based on NONMEM in Chinese allogeneic hematopoietic stem cell transplantation recipients.
Cheng, XL; Gao, Y; Li, ZD; Zhou, H, 2012
)
0.38
"The pharmacokinetic variability of hydroxy-itraconazole (OH-ITZ), an active metabolite of itraconazole (ITZ), is not fully known."( Hydroxy-itraconazole pharmacokinetics is similar to that of itraconazole in immunocompromised patients receiving oral solution of itraconazole.
Kawakami, J; Mino, Y; Naito, T; Watanabe, T; Yagi, T; Yamada, H; Yamada, T, 2013
)
0.39
"The pharmacokinetic variability of OH-ITZ was associated with saturated metabolism to keto-ITZ, serum concentration of albumin, and renal function in immunocompromised patients."( Hydroxy-itraconazole pharmacokinetics is similar to that of itraconazole in immunocompromised patients receiving oral solution of itraconazole.
Kawakami, J; Mino, Y; Naito, T; Watanabe, T; Yagi, T; Yamada, H; Yamada, T, 2013
)
0.39
"5mg/kg for pharmacokinetic profile (lung and plasma concentration) determination in ICR CD-1 mice."( Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention.
Amighi, K; Duret, C; Merlos, R; Sebti, T; Vanderbist, F; Wauthoz, N, 2014
)
0.4
" Systolic and diastolic blood pressures and pulse rate were periodically recorded after nadolol administration as pharmacodynamic parameters."( Pharmacokinetic and pharmacodynamic interaction of nadolol with itraconazole, rifampicin and grapefruit juice in healthy volunteers.
Fukushima, T; Kimura, J; Misaka, S; Miyazaki, N; Ono, T; Shikama, Y; Yatabe, MS, 2013
)
0.39
" When co-administered with voriconazole, pharmacokinetic parameters of imatinib were not significantly altered except for a 36."( Differential effects of ketoconazole, itraconazole and voriconazole on the pharmacokinetics of imatinib and its main metabolite GCP74588 in rat.
Han, A; Hu, G; Kan, X; Lin, G; Qiu, X; Wang, C; Wang, Z; Xu, T, 2014
)
0.4
"A new approach for calculation of sample size in pediatric clinical pharmacokinetic studies was suggested based on desired precision for a pharmacokinetic parameter of interest."( Precision criteria to derive sample size when designing pediatric pharmacokinetic studies: which measure of variability should be used?
Aarons, L; Johnson, TN; Ogungbenro, K; Rostami-Hodjegan, A; Salem, F; Vajjah, P, 2014
)
0.4
" Correlation of pharmacokinetic and pharmacodynamic (PK-PD) parameters with the in vivo bactericidal action of antimicrobial agents has progressed markedly in recent years."( Population pharmacokinetics of itraconazole in Japanese patients with invasive fungal peritonitis.
Hagihara, M; Hamada, Y; Mikamo, H; Yamagishi, Y, 2013
)
0.39
" For the pharmacokinetic analysis, average concentrations of high variability drug-itraconazole were used before (BO) and after sampling intervals optimization (AO)."( Sampling intervals verification in pharmacokinetics studies.
Bujalska-Zadrożny, M; Grabowski, T; Jaroszewski, JJ; Sasinowska-Motyl, M, 2014
)
0.4
" Terbinafine increased the peak concentration (C max) of tramadol by 53 % (P < 0."( Effects of terbinafine and itraconazole on the pharmacokinetics of orally administered tramadol.
Backman, JT; Hagelberg, NM; Laine, K; Neuvonen, PJ; Olkkola, KT; Saari, TI; Saarikoski, T; Scheinin, M, 2015
)
0.42
"After IV administration, the major pharmacokinetic parameters were as follows (mean ± SD): terminal elimination half-life (T1/2λz ) 15."( Pharmacokinetics and bioavailability of itraconazole oral solution in cats.
Cao, C; Li, W; Liang, C; Shan, Q; Wang, J; Zeng, Z; Zhang, X; Zhong, J, 2016
)
0.43
" Empirical antifungal efficacy was assessed retrospectively in 159 transplantations, and a full pharmacokinetic study was prospectively conducted in six of these patients."( Successful empirical antifungal therapy of intravenous itraconazole with pharmacokinetic evidence in pediatric cancer patients undergoing hematopoietic stem cell transplantation.
Ahn, HS; Jang, IJ; Jang, MK; Kang, HJ; Kim, H; Kim, MS; Kim, SJ; Lee, JW; Park, JD; Park, KD; Shin, D; Shin, HY; Song, ES; Yu, KS, 2015
)
0.42
" The purpose of the present study is to develop a physiologically based pharmacokinetic (PBPK) model for atorvastatin and its two primary metabolites, 2-hydroxy-atorvastatin acid and atorvastatin lactone, using in vitro and in vivo data."( Physiologically based pharmacokinetic modeling of disposition and drug-drug interactions for atorvastatin and its metabolites.
Zhang, T, 2015
)
0.42
" 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
)
0.42
" A physiologically based pharmacokinetic model was developed to describe DDIs between domperidone and three different inhibitors of CYP3A4."( A physiologically based pharmacokinetic modeling approach to predict drug-drug interactions between domperidone and inhibitors of CYP3A4.
Ravenstijn, P; Sensenhauser, C; Snoeys, J; Templeton, I, 2016
)
0.43
"Physiologically based pharmacokinetic (PBPK) modeling for itraconazole has been challenging due to highly variable in vitro d ata used for 'bottom-up' model building."( Development of a Physiologically Based Pharmacokinetic Model for Itraconazole Pharmacokinetics and Drug-Drug Interaction Prediction.
Budha, N; Chen, Y; Hop, CE; Jin, JY; Kenny, JR; Lu, T; Ma, F; Mao, J; Wong, H, 2016
)
0.43
" The key parameters that govern the pharmacokinetic profile, including non-linear clearance (i."( Development of a Physiologically Based Pharmacokinetic Model for Itraconazole Pharmacokinetics and Drug-Drug Interaction Prediction.
Budha, N; Chen, Y; Hop, CE; Jin, JY; Kenny, JR; Lu, T; Ma, F; Mao, J; Wong, H, 2016
)
0.43
" The resulting interaction between these CYP3A4 substrates can be utilized clinically as a pharmacokinetic booster for prolonging saquinavir dosing regimen and/or decreasing saquinavir dose requirement in HIV/AIDS patients."( A semi-mechanistic pharmacokinetic model of saquinavir combined with itraconazole in HIV-1-positive patients.
Jenjob, A; Lohitnavy, M; Methaneethorn, J; Pankaew, A; Phuphuak, K; Sriarwut, T, 2015
)
0.42
" Even though pharmacokinetic data regarding such interaction are available, they cannot be used for quantitative prediction."( Pharmacokinetic model for the inhibition of simvastatin metabolism by itraconazole.
Chan-Im, D; Chiang-Ngernthanyakool, R; Lohitnavy, M; Methaneethorn, J; Phaohorm, S; Tongpeng, W, 2015
)
0.42
"Published data involving pharmacokinetic of simvastatin, itraconazole, and pharmacokinetic interaction between simvastatin and itraconazole were selected from PubMed search."( Pharmacokinetic model for the inhibition of simvastatin metabolism by itraconazole.
Chan-Im, D; Chiang-Ngernthanyakool, R; Lohitnavy, M; Methaneethorn, J; Phaohorm, S; Tongpeng, W, 2015
)
0.42
"IVIVC was developed based on fed/fasted pharmacokinetic data from randomized cross-over trials, in vitro dissolution studies, and prior information about typical and between subject variability of GI pH and transit times."( Population In Vitro-In Vivo Correlation Model Linking Gastrointestinal Transit Time, pH, and Pharmacokinetics: Itraconazole as a Model Drug.
Abuhelwa, AY; Foster, DJ; Hayes, D; Mudge, S; Upton, RN, 2016
)
0.43
" Pharmacokinetic profiles for fasted itraconazole periods were described based on the in vitro dissolution model, in vivo disposition model, and the prior information on GI pH and transit times."( Population In Vitro-In Vivo Correlation Model Linking Gastrointestinal Transit Time, pH, and Pharmacokinetics: Itraconazole as a Model Drug.
Abuhelwa, AY; Foster, DJ; Hayes, D; Mudge, S; Upton, RN, 2016
)
0.43
"The results of this study suggest that vismodegib can be administered with acid-reducing agents and P-gp and CYP inhibitors without the risk of a clinically meaningful pharmacokinetic drug-drug interaction."( A clinical drug-drug interaction study to evaluate the effect of a proton-pump inhibitor, a combined P-glycoprotein/cytochrome 450 enzyme (CYP)3A4 inhibitor, and a CYP2C9 inhibitor on the pharmacokinetics of vismodegib.
Chandra, P; Colburn, D; Dresser, MJ; Graham, RA; Hop, CE; Malhi, V; Williams, SJ, 2016
)
0.43
" The aim of this study was to investigate the influence of itraconazole (ITCZ) on tacrolimus absorption, distribution and metabolism by developing a semi-physiological pharmacokinetic model of tacrolimus in mice."( Use of a semi-physiological pharmacokinetic model to investigate the influence of itraconazole on tacrolimus absorption, distribution and metabolism in mice.
Bi, KS; Chen, XH; Lu, XF; Zhan, J; Zhou, Y, 2017
)
0.46
"Rat is commonly used for pharmacokinetic screening during pharmaceutical lead optimization."( Single jugular vein cannulated rats may not be suitable for intravenous pharmacokinetic screening of high logP compounds.
Gaud, N; Holenarsipur, VK; Kole, P; Kumar, A; Mandlekar, S; Matta, M; Sridhar, S, 2017
)
0.46
"Therapeutic drug monitoring (TDM) may be required to achieve optimal clinical outcomes in the setting of significant pharmacokinetic variability, a situation that applies to a number of anti-mould therapies."( Therapeutic drug monitoring for invasive mould infections and disease: pharmacokinetic and pharmacodynamic considerations.
Hope, WW; Stott, KE, 2017
)
0.46
" Pharmacokinetic parameters were determined with compartmental analysis."( Pharmacokinetics and Relative Bioavailability of Orally Administered Innovator-Formulated Itraconazole Capsules and Solution in Healthy Dogs.
Hasbach, AE; Langlois, DK; Papich, MG; Rosser, EJ, 2017
)
0.46
" Despite some pharmacokinetic differences between itraconazole capsule and solution, formulation-specific dosages do not appear to be necessary."( Pharmacokinetics and Relative Bioavailability of Orally Administered Innovator-Formulated Itraconazole Capsules and Solution in Healthy Dogs.
Hasbach, AE; Langlois, DK; Papich, MG; Rosser, EJ, 2017
)
0.46
"001% bath, itraconazole exceeded the MIC and declined with a disappearance half-life that markedly varied (14."( THE PHARMACOKINETICS OF TOPICAL ITRACONAZOLE IN PANAMANIAN GOLDEN FROGS (ATELOPUS ZETEKI).
Barrett, K; Boothe, D; Bronson, E; Rifkin, A; Visser, M, 2017
)
0.46
" Dissolution tests by pH transition and pharmacokinetic study using male Sprague Dawley rats were conducted."( Characterization and pharmacokinetic study of itraconazole solid dispersions prepared by solvent-controlled precipitation and spray-dry methods.
Choi, HG; Choi, S; Kang, W; Kim, DW; Kim, KS; Kim, M; Kim, Y; Lee, ES; Lee, JW; Lim, C; Oh, KT; Sim, T, 2017
)
0.46
"In recent years, physiologically based PharmacoKinetic (PBPK) modeling has received growing interest as a useful tool for the assessment of drug pharmacokinetics."( Prediction of drug-drug interactions using physiologically-based pharmacokinetic models of CYP450 modulators included in Simcyp software.
Daali, Y; Desmeules, JA; Marsousi, N; Rudaz, S, 2018
)
0.48
"The accuracy of physiologically based pharmacokinetic (PBPK) model prediction in children, especially those younger than 2 years old, has not been systematically evaluated."( Predictive Performance of Physiologically Based Pharmacokinetic (PBPK) Modeling of Drugs Extensively Metabolized by Major Cytochrome P450s in Children.
Al-Huniti, N; Bui, KH; Cheung, SYA; Johnson, TN; Li, J; Xu, H; Zhou, D; Zhou, W, 2018
)
0.48
"The aim of this study was to develop a population in vitro-in vivo pharmacokinetic model that simultaneously describe the absorption and accumulation kinetics of itraconazole (ICZ) and hydroxy-itraconazole (HICZ) in healthy subjects."( Population in vitro-in vivo pharmacokinetic model of first-pass metabolism: itraconazole and hydroxy-itraconazole.
Abuhelwa, AY; Foster, DJR; Mudge, S; Upton, RN, 2018
)
0.48
" Physiologically based pharmacokinetic (PBPK) modeling was conducted using a population-based simulator."( Physiologically Based Pharmacokinetic Modeling to Evaluate the Systemic Exposure of Gefitinib in CYP2D6 Ultrarapid Metabolizers and Extensive Metabolizers.
Al-Huniti, N; Chen, Y; Masson, E; Tang, W; Zhou, D; Zhou, W, 2018
)
0.48
"16-fold increase of AUC of avatrombopag, prolonged terminal elimination phase half-life (from 19."( Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs.
Aluri, J; Boyd, P; Chang, MK; Ferry, J; Lai, WG; Nomoto, M; Rege, B; Schuck, E; Siu, YA; Yasuda, S; Zamora, CA, 2018
)
0.48
" The objective of the present study was to develop a physiologically-based pharmacokinetic (PBPK) model for BMS-823778 and use the model to predict PK and drug-drug interaction (DDI) in virtual populations with multiple polymorphic genes."( Physiologically-based pharmacokinetic modelling of a CYP2C19 substrate, BMS-823778, utilizing pharmacogenetic data.
Gong, J; Humphreys, WG; Iacono, L; Iyer, RA; Zheng, M, 2018
)
0.48
"Physiologically based pharmacokinetic (PBPK) modeling for itraconazole using a bottom-up approach is challenging, not only due to complex saturable pharmacokinetics (PK) and the presence of three metabolites exhibiting CYP3A4 inhibition, but also because of discrepancies in reported in vitro data."( Physiologically Based Pharmacokinetic Model of Itraconazole and Two of Its Metabolites to Improve the Predictions and the Mechanistic Understanding of CYP3A4 Drug-Drug Interactions.
Ericsson, H; Janzén, D; Kanebratt, KP; Lennernäs, H; Lundahl, A; Prieto Garcia, L, 2018
)
0.48
" Risdiplam exhibited linear PK over the dose range with a multi-phasic decline with a mean terminal half-life of 40-69 h."( A phase 1 healthy male volunteer single escalating dose study of the pharmacokinetics and pharmacodynamics of risdiplam (RG7916, RO7034067), a SMN2 splicing modifier.
Al Kotbi, N; Bergauer, T; Cleary, Y; Czech, C; Frances, N; Günther, A; Heinig, K; Jaber, B; Jordan, P; Khwaja, O; Kletzl, H; Marquet, A; Müller, L; Parkar, N; Poirier, A; Ratni, H; Sturm, S, 2019
)
0.51
"An in vitro-in vivo (IVIV) pharmacokinetic model of itraconazole and hydroxyitraconazole was developed including data from an omeprazole interaction study with SUBA itraconazole."( Mechanistic Assessment of the Effect of Omeprazole on the In Vivo Pharmacokinetics of Itraconazole in Healthy Volunteers.
Abuhelwa, AY; Foster, DJR; Mudge, S; Upton, RN, 2019
)
0.51
" The physiologically based pharmacokinetic (PBPK) models were developed to investigate the influence of different triazoles on tamoxifen pharmacokinetics in this paper."( Predicting the Effects of Different Triazole Antifungal Agents on the Pharmacokinetics of Tamoxifen.
Chen, L; Li, M; Li, N; Qi, F; Wang, N; Zhu, L, 2019
)
0.51
"We previously verified a physiologically based pharmacokinetic (PBPK) model for mirabegron in healthy subjects using the Simcyp Simulator by incorporating data on the inhibitory effect on cytochrome P450 (CYP) 2D6 and a multi-elimination pathway mediated by CYP3A4, uridine 5'-diphosphate-glucuronosyltransferase (UGT) 2B7 and butyrylcholinesterase (BChE)."( Application of a physiologically based pharmacokinetic model for the prediction of mirabegron plasma concentrations in a population with severe renal impairment.
Konishi, K; Minematsu, T; Nagasaka, Y; Tabata, K, 2019
)
0.51
" This work by an International Consortium for Innovation and Quality in Pharmaceutical Development working group (WG) is to develop and verify a mechanistic ITZ physiologically-based pharmacokinetic model and provide recommendations for optimal DDI study design based on model simulations."( Recommendations for the Design of Clinical Drug-Drug Interaction Studies With Itraconazole Using a Mechanistic Physiologically-Based Pharmacokinetic Model.
Cabalu, TD; Callegari, E; Chen, Y; Einolf, H; Hall, SD; Liu, L; Parrott, N; Peters, SA; Schuck, E; Sharma, P; Tracey, H; Upreti, VV; Zheng, M; Zhu, AZX, 2019
)
0.51
" The pharmacokinetic profile of PUR1900 suggests the potential to improve upon the efficacy and safety profile observed with oral itraconazole."( A phase 1/1b study of PUR1900, an inhaled formulation of itraconazole, in healthy volunteers and asthmatics to study safety, tolerability and pharmacokinetics.
Bedwell, P; Connor, L; Curran, AK; Hava, DL; Henderson, D; Johnson, P; Kane, K; Khan, N; Kramer, S; Layton, G; McKenzie, L; Perry, J; Roach, J; Singh, D; Swann, C; Tan, L, 2020
)
0.56
"A multicenter-based population pharmacokinetic model of ciclosporin was established."( Multicenter-Based Population Pharmacokinetic Analysis of Ciclosporin in Hematopoietic Stem Cell Transplantation Patients.
Ding, XL; Liu, LN; Miao, LY; Tian, JX; Xue, L; Yan, HH; Zhang, JJ; Zhang, WJ; Zhang, WW, 2019
)
0.51
" A physiologically based pharmacokinetic (PBPK) model incorporating the metabolites was developed to predict the effect of other strong and moderate CYP3A4 inhibitors and inducers."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
" Pharmacokinetic parameters were calculated using noncompartmental analysis, and safety was assessed."( Effects of itraconazole and rifampicin on the single-dose pharmacokinetics of the nonsteroidal mineralocorticoid receptor blocker esaxerenone in healthy Japanese subjects.
Irie, S; Ishizuka, H; Ishizuka, T; Kato, M; Kirigaya, Y; Nakatsu, T; Nishikawa, Y; Shimizu, T; Shiramoto, M; Uchimaru, H, 2020
)
0.56
" Values for total clearance of compounds from plasma should be one of the most important pharmacokinetic parameters for predictions."( Predicted values for human total clearance of a variety of typical compounds with differently humanized-liver mouse plasma data.
Ito, S; Iwamoto, K; Kamimura, H; Mizunaga, M; Nakayama, K; Negoro, T; Nishiwaki, M; Nomura, Y; Suemizu, H; Yamazaki, H; Yoneda, N, 2020
)
0.56
" To enable administering safe doses of molibresib to healthy volunteers, this 2-part randomized, open-label, crossover drug-drug interaction trial was conducted as an adaptive design study using physiologically based pharmacokinetic (PBPK) modeling and simulation to predict the lowest doses of molibresib that could be safely administered alone (10 mg) or with itraconazole and rifampicin (strong inhibitors and inducers of CYP3A and P-gp, respectively)."( An Adaptive Physiologically Based Pharmacokinetic-Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers.
Collins, G; Ferron-Brady, G; Kremer, BE; Patel, A; Riddell, K; Schramek, D; Zhou, Y, 2021
)
0.62
"Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)."( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia.
Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020
)
0.56
" We report on how 2 acumapimod clinical DDI studies and a physiologically-based pharmacokinetic (PBPK) model assessing how co-administration of a weak (azithromycin) and strong (itraconazole) CYP3A4 inhibitor affected acumapimod systemic exposure, informed decision making and supported concomitant use of CYP3A4 and P-gp inhibitors."( A Physiologically Based Pharmacokinetic Model to Predict Potential Drug-Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor.
Agyemang, A; Farrell, C; Moore, W; Parkin, J, 2021
)
0.62
" It has been reported that sunitinib was mainly metabolized by CYP3A but its pharmacokinetic interactions have not been revealed."( Effects of CYP3A inhibitors ketoconazole, voriconazole, and itraconazole on the pharmacokinetics of sunitinib and its main metabolite in rats.
Chen, RJ; Cheng, C; Cui, X; Huang, CK; Sun, W; Wang, J; Wang, Y; Wang, Z, 2021
)
0.62
" We investigated whether the single-dose pharmacokinetic (PK) profile of pamiparib is altered by coadministration of a strong CYP3A inducer (rifampin) or a strong CYP3A inhibitor (itraconazole) in patients with solid tumors."( The pharmacokinetics of pamiparib in the presence of a strong CYP3A inhibitor (itraconazole) and strong CYP3A inducer (rifampin) in patients with solid tumors: an open-label, parallel-group phase 1 study.
Andreu-Vieyra, C; Bulat, I; Lin, C; Maglakelidze, M; Mu, S; Sahasranaman, S; Skarbova, V; Skrzypczyk-Ostaszewicz, A, 2021
)
0.62
" A physiologically based pharmacokinetic (PBPK) model was constructed to predict plasma concentration-time profiles of selumetinib, and to evaluate the impact of coadministering moderate cytochrome P450 (CYP) 3A4/2C19 inhibitors/inducers."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
0.62
" Physiologically based pharmacokinetic (PBPK) modelling was performed to predict the drug-drug interaction (DDI) effect of cytochrome P450 (CYP)3A modulators on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment."( Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment.
Igawa, Y; Ishizuka, H; Ishizuka, T; Shimizu, T; Watanabe, A; Yamada, M, 2022
)
0.72
"As one of the key components in model-informed drug discovery and development, physiologically-based pharmacokinetic (PBPK) modeling linked with in vitro-to-in vivo extrapolation (IVIVE) is widely applied to quantitatively predict drug-drug interactions (DDIs) on drug-metabolizing enzymes and transporters."( Physiologically-based pharmacokinetic modeling to evaluate in vitro-to-in vivo extrapolation for intestinal P-glycoprotein inhibition.
De Zwart, L; Evers, R; Yamazaki, S, 2022
)
0.72
"A new UPLC-MS/MS technique for the determination of ripretinib in beagle dog plasma was developed, and the pharmacokinetic effects of voriconazole and itraconazole on ripretinib in beagle dogs were studied."( The Pharmacokinetic Effect of Itraconazole and Voriconazole on Ripretinib in Beagle Dogs by UPLC-MS/MS Technique.
Geng, XN; Gou, KF; Qiu, XJ; Su, YD; Wang, HJ; Zhou, CY, 2021
)
0.62
" The concentration of ripretinib was detected, and the pharmacokinetic parameters of ripretinib were calculated."( The Pharmacokinetic Effect of Itraconazole and Voriconazole on Ripretinib in Beagle Dogs by UPLC-MS/MS Technique.
Geng, XN; Gou, KF; Qiu, XJ; Su, YD; Wang, HJ; Zhou, CY, 2021
)
0.62
" To predict the potential influence of different triazoles (voriconazole, fluconazole, and itraconazole) on the pharmacokinetics of crizotinib by modeling and simulation the physiologically based pharmacokinetic models were established and validated in virtual cancer subjects through Simcyp software based on the essential physicochemical properties and pharmacokinetic data collected."( Use of Modeling and Simulation to Predict the Influence of Triazole Antifungal Agents on the Pharmacokinetics of Crizotinib.
Chen, L; Chen, W; Li, L, 2022
)
0.72
"Eliapixant had a long half-life (23."( First-in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics.
Baumann, S; Chang, X; Friedrich, C; Gashaw, I; Hummel, T; Klein, S; Thuß, U, 2022
)
0.72
" As SHR2554 is mainly metabolized by CYP3A4, it is helpful to conduct research on the effects of itraconazole, a strong inhibitor of CYP3A4-metabolizing enzymes, on the pharmacokinetic characteristics and safety of SHR2554."( Study on pharmacokinetic interactions between SHR2554 and itraconazole in healthy subjects: A single-center, open-label phase I trial.
Cui, C; Deng, K; Huang, J; Wang, H; Xiang, Y; Yang, G; Yang, S; Yang, X; Zou, C; Zou, Y, 2023
)
0.91
"We conducted a single-center, open-label pharmacokinetic study of itraconazole on SHR2554 in 18 healthy Chinese subjects."( Study on pharmacokinetic interactions between SHR2554 and itraconazole in healthy subjects: A single-center, open-label phase I trial.
Cui, C; Deng, K; Huang, J; Wang, H; Xiang, Y; Yang, G; Yang, S; Yang, X; Zou, C; Zou, Y, 2023
)
0.91
" Here, we investigate the pharmacokinetic drug-drug interaction potential of trilaciclib."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
0.72
" Population pharmacokinetic modeling showed no significant effect of trilaciclib on topotecan clearance."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
0.72
"A phase I open-label study assessed the effect of multiple oral doses of a potent CYP3A4 inhibitor (itraconazole) and inducer (rifampicin) on the pharmacokinetic profile of a single oral dose of senaparib, a novel, highly potent poly-(ADP-ribose) polymerase 1/2 inhibitor and CYP3A4 substrate, in Chinese healthy male volunteers (HMV)."( Effect of a strong CYP3A4 inhibitor and inducer on the pharmacokinetics of senaparib (IMP4297) in healthy volunteers: A drug-drug interaction study.
Cai, SX; Hsieh, CY; Hu, X; Li, X; Liu, L; Liu, P; Liu, W; Shi, H; Xu, P; Xu, S; Zhang, H; Zhang, M; Zhang, Y, 2023
)
0.91
" To consider an adult physiologically-based pharmacokinetic (PBPK) model for pediatric scaling, we assessed in vitro-derived cytochrome P450 (CYP) and uridine 5'-diphospho-glucuronosyltransferase (UGT) enzyme contributions to CBD clearance in human."( Verifying in vitro-determined enzyme contributions to cannabidiol clearance for exposure predictions in human through physiologically-based pharmacokinetic modeling.
Beers, JL; Edginton, AN; Jackson, KD; Yeung, CHT, 2023
)
0.91
" Full pharmacokinetic curves were obtained on Days 7 and 14."( Repurposing antifungals: population pharmacokinetics of itraconazole and hydroxy-itraconazole following administration of a nanocrystal formulation.
Blijlevens, N; Brüggemann, RJM; Donnelly, JP; Jansen, AME; Ter Heine, R, 2023
)
0.91
"This study provides information on the pharmacokinetic properties of the itraconazole NCF useful for development of this formulation."( Repurposing antifungals: population pharmacokinetics of itraconazole and hydroxy-itraconazole following administration of a nanocrystal formulation.
Blijlevens, N; Brüggemann, RJM; Donnelly, JP; Jansen, AME; Ter Heine, R, 2023
)
0.91
" This study aimed to evaluate the utility of physiologically-based pharmacokinetic (PBPK) modeling in the prediction of gastric pH-mediated drug exposure by using itraconazole, a weak base, as a case."( Prediction of gastric pH-mediated drug exposure using physiologically-based pharmacokinetic modeling: A case study of itraconazole.
Lee, S; Yang, E; Yu, KS, 2023
)
0.91
" Pharmacokinetic parameters were calculated using non-compartmental analysis."( Effect of CYP3A4 induction and inhibition on the pharmacokinetics of SHR0302 in healthy subjects.
Feng, S; Fu, M; Gao, X; Li, X; Li, Y; Lin, H; Shen, K; Yu, G; Zhang, P; Zhang, Z, 2023
)
0.91
" This project used physiologically based pharmacokinetic (PBPK) modeling to assess the DDI potential of inhaled PUR1900, using midazolam as a "victim drug."( Evaluation of the Potential for Drug-Drug Interactions with Inhaled Itraconazole Using Physiologically Based Pharmacokinetic Modelling, Based on Phase 1 Clinical Data.
Bergagnini-Kolev, M; Curran, AK; Kane, K; Templeton, IE, 2023
)
0.91
" Clinical pharmacokinetic drug-drug interaction (DDI) of ocedurenone with CYP3A inhibitor and inducer were investigated in healthy volunteers."( Pharmacokinetics and Drug-Drug Interaction of Ocedurenone (KBP-5074) in vitro and in vivo.
Liu, J; McCabe, J; Tan, X; Wang, P; Yang, F; Zhang, J, 2023
)
0.91
"The reversal effect of itraconazole on P-glycoprotein (P-gp)-mediated resistance of vinblastine, daunorubicin and doxorubicin was analyzed from a cellular pharmacokinetic point of view, namely by [3H]azidopine photoaffinity labeling, intracellular accumulation and transcellular transport experiments."( Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
Komada, F; Nishiguchi, K; Okumura, K; Sakaeda, T; Takara, K; Tanigawara, Y, 1999
)
0.86
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" This can be rationalized based on the interplay of the effects of lipophilicity on individual parameter values in pharmacokinetic equations."( Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
Geissler, WM; Madeira, M; Martin, IJ; Miller, RR; Raab, CE; Wood, HB, 2020
)
0.56

Compound-Compound Interactions

We studied the activities of the combination of CAS and SMX against 31 Aspergillus isolates. We compared them with that of SMX combined with amphotericin B (AMB) or itraconazole. Cytarabine metabolism was significantly decreased when combined with caspofungin or ItC.

ExcerptReferenceRelevance
"Cilofungin, a lipopeptide antifungal agent, was tested for in vitro activity alone and in combination with ketoconazole, itraconazole, flucytosine and amphotericin B against 102 clinical isolates of Candida species."( In vitro comparison of cilofungin alone and in combination with other antifungal agents against clinical isolates of Candida species.
Cobbs, CG; Dismukes, WE; Lank, KM; Smith, KR, 1991
)
0.28
"A randomized trial of amphotericin B (AB) alone and in combination with oral itraconazole (IZ) is carried out in two groups of 10 mucocutaneous leishmaniasis patients from Bolivia and Peru."( A randomized trial of amphotericin B alone or in combination with itraconazole in the treatment of mucocutaneous leishmaniasis.
Cardenas, F; Dedet, JP; Mendoza, C; Paredes, V; Rodriguez, LV,
)
0.13
"Ten expressed human CYPs and human liver microsomes were used in the experiments for the identification of enzymes responsible for zonisamide metabolism and for the prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data, respectively."( Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data.
Kitada, M; Kiuchi, M; Nakamura, H; Nakasa, H; Ohmori, S; Ono, S; Tsutsui, M, 1998
)
0.3
"We demonstrated that: (1) zonisamide is metabolized by recombinant CYP3A4, CYP2C19 and CYP3A5, (2) the metabolism is inhibited to a variable extent by known CYP3A4/5 substrates and/or inhibitors in human liver microsomes, and (3) in vitro-in vivo predictive calculations suggest that several compounds demonstrating CYP3A4-affinity might cause in vivo drug-drug interactions with zonisamide."( Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data.
Kitada, M; Kiuchi, M; Nakamura, H; Nakasa, H; Ohmori, S; Ono, S; Tsutsui, M, 1998
)
0.3
" We investigated the antifungal activities of nikkomycin Z alone and in combination with fluconazole and itraconazole."( In vitro antifungal activity of nikkomycin Z in combination with fluconazole or itraconazole.
Li, RK; Rinaldi, MG, 1999
)
0.3
" In addition, special attention is needed for the detection of adverse drug reactions resulting from possible drug-drug interactions."( Signalling possible drug-drug interactions in a spontaneous reporting system: delay of withdrawal bleeding during concomitant use of oral contraceptives and itraconazole.
Egberts, AC; Leufkens, HG; Meyboom, RH; Van Puijenbroek, EP, 1999
)
0.3
" This approach might be a promising tool for the development of procedures for automated detection of possible drug-drug interactions in spontaneous reporting systems."( Signalling possible drug-drug interactions in a spontaneous reporting system: delay of withdrawal bleeding during concomitant use of oral contraceptives and itraconazole.
Egberts, AC; Leufkens, HG; Meyboom, RH; Van Puijenbroek, EP, 1999
)
0.3
" In contrast, there are no drug-drug contraindications with terbinafine."( Drug interactions of the newer oral antifungal agents.
Katz, HI, 1999
)
0.3
" A physiologically-based pharmacokinetic model was used to predict the maximum in vivo drug-drug interaction."( Inhibition of in vitro metabolism of simvastatin by itraconazole in humans and prediction of in vivo drug-drug interactions.
Ikeda, T; Inoue, S; Ishigam, M; Ito, K; Iwabuchi, H; Komai, T; Kondo, T; Sugiyama, Y; Takasaki, W; Uchiyama, M, 2001
)
0.31
"The objectives of this review are to discuss the role of cytochrome P450 (CYP450) isoforms in drug metabolism, to explain differences in metabolism among the HMG-CoA reductase inhibitors (HMGs, statins), to review drug-drug and drug-food interaction studies dealing with the HMGs, to present case reports dealing with HMG-related myopathy, to discuss major clinical implications of these case reports and to express an opinion of use of HMGs in clinical practice."( The role of cytochrome P450-mediated drug-drug interactions in determining the safety of statins.
Bottorff, M; Worz, CR, 2001
)
0.31
" These results showed that the encapsulated, enteric-coated bead formulation of didanosine can be concomitantly administered with drugs, such as the azole antifungal agents, whose bioavailability may be influenced by interaction with antacids."( Absence of clinically relevant drug interactions following simultaneous administration of didanosine-encapsulated, enteric-coated bead formulation with either itraconazole or fluconazole.
Damle, B; Hess, H; Kaul, S; Knupp, C, 2002
)
0.31
" The method was applied to drug-drug interaction study of TZ with itraconazole (ITZ)."( Semi-micro column HPLC of triazolam in rat plasma and brain microdialysate and its application to drug interaction study with itraconazole.
Al-Dirbashi, OY; Kaddoumi, A; Nakashima, K; Nakashima, MN; Yamamoto, K, 2003
)
0.32
" Amphotericin B was combined with flucytosine and ciprofloxacin, whereas itraconazole was combined with ciprofloxacin, levofloxacin, lomefloxacin and sulfadiazine."( In vitro activity of amphotericin B and itraconazole in combination with flucytosine, sulfadiazine and quinolones against Exophiala spinifera.
Afeltra, J; de Hoog, GS; Rijs, AJ; Verweij, PE; Vitale, RG, 2003
)
0.32
"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
" Cytarabine metabolism was significantly decreased when combined with caspofungin or itraconazole."( In vitro evaluation of cytochrome P450-mediated drug interactions between cytarabine, idarubicin, itraconazole and caspofungin.
Colburn, DE; Giles, FJ; Oladovich, D; Smith, JA, 2004
)
0.32
" We studied the activities of the combination of CAS and SMX against 31 Aspergillus isolates and compared them with that of SMX combined with amphotericin B (AMB) or itraconazole (ITC)."( In vitro activity of caspofungin combined with sulfamethoxazole against clinical isolates of Aspergillus spp.
Osherov, N; Shadkchan, Y; Shalit, I; Yekutiel, A, 2004
)
0.32
"To evaluate and compare the in vitro antifungal properties of lufenuron and nikkomycin Z against isolates of Coccidioides immitis and Aspergillus fumigatus when used singly and in combination with the azole antifungal agent itraconazole."( Comparison of susceptibility of fungal isolates to lufenuron and nikkomycin Z alone or in combination with itraconazole.
Davidson, AP; Hector, RF; Johnson, SM, 2005
)
0.33
"This article reviews the in vitro metabolic and the in vivo pharmacokinetic drug-drug interactions with antifungal drugs, including fluconazole, itraconazole, micafungin, miconazole, and voriconazole."( [Drug-drug interaction of antifungal drugs].
Niwa, T; Shiraga, T; Takagi, A, 2005
)
0.33
" Consequently, azoles interact with a vast array of compounds."( Drug-drug interactions of antifungal agents and implications for patient care.
Amsden, JR; Gubbins, PO, 2005
)
0.33
"Rhinotomy with removal of the flap combined with one-hour infusion of 2 per cent enilconazole and oral itraconazole resulted in satisfactory outcome in dogs with severe or recurrent aspergillosis."( Surgical treatment of canine nasal aspergillosis by rhinotomy combined with enilconazole infusion and oral itraconazole.
Claeys, S; Clercx, C; Hamaide, A; Lefebvre, JB; Schuller, S, 2006
)
0.33
"This study was aimed to investigate the clinical features and therapy of Ph(+) acute lymphoblastic leukemia (Ph(+)ALL) combined with invasive aspergillosis."( [Ph+ acute lymphoblastic leukemia combined with lung and brain invasive aspergillosis].
Huang, M; Liu, WL; Ran, D; Sun, HY; Zhang, YC; Zhou, JF, 2006
)
0.33
" A potentially drug-drug interaction (DDI) occurred when the use of concomitant drugs were recorded within +/-30 days from the date of the first azoles prescription."( Co-prescriptions with itraconazole and fluconazole as a signal for possible risk of drug-drug interactions: a four-year analysis from Italian general practice.
Caputi, AP; Cricelli, C; Galatti, L; Greco, A; Mazzaglia, G; Nicoletti, G; Schito, GC; Sessa, E; Spina, E, 2007
)
0.34
"Although there is a presumed drug-drug interaction between itraconazole and nonnucleoside reverse-transcriptase inhibitors, the medical literature lacks such documentation."( Drug-drug interaction between itraconazole and efavirenz in a patient with AIDS and disseminated histoplasmosis.
Andrade, RA; Hamill, RJ; Koo, HL, 2007
)
0.34
"We describe drug-drug interactions (DDIs) encountered with antifungals in clinical practice."( Drug-drug interactions with systemic antifungals in clinical practice.
Abouelfath, A; Depont, F; Dupon, M; Dutronc, H; Galpérine, T; Giauque, E; Hébert, G; Moore, N; Ragnaud, JM; Valentino, R; Vargas, F, 2007
)
0.34
" All treatment episodes with antifungal agent were examined and all prescribed concomitant medication identified for potential drug-drug interactions (PDDI)-serious events occurring during treatment were adjudicated for clinical DDI."( Drug-drug interactions with systemic antifungals in clinical practice.
Abouelfath, A; Depont, F; Dupon, M; Dutronc, H; Galpérine, T; Giauque, E; Hébert, G; Moore, N; Ragnaud, JM; Valentino, R; Vargas, F, 2007
)
0.34
" In conclusion, posaconazole salvage therapy demonstrated greater efficacy and safety than HD-LPD/AMB alone or in combination with caspofungin in the salvage therapy of invasive aspergillosis in hematologic malignancy."( Novel antifungal agents as salvage therapy for invasive aspergillosis in patients with hematologic malignancies: posaconazole compared with high-dose lipid formulations of amphotericin B alone or in combination with caspofungin.
Afif, C; Boktour, M; Hachem, RY; Hanna, HA; Jiang, Y; Kontoyiannis, DP; Raad, II; Torres, HA, 2008
)
0.35
" Collections of individual case safety reports (ICSRs) related to suspected ADR incidents in clinical practice have proven to be very useful in post-marketing surveillance for pairwise drug--ADR associations, but have yet to reach their full potential for drug-drug interaction surveillance."( A statistical methodology for drug-drug interaction surveillance.
Bate, A; Edwards, IR; Norén, GN; Sundberg, R, 2008
)
0.35
"The vitro antifungal activity of retigeric acid B (RAB), a pentacyclic triterpenoid from the lichen species Lobaria kurokawae, was evaluated alone and in combination with fluconazole, ketoconazole, and itraconazole against Candida albicans using checkerboard microdilution and time-killing tests."( In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
Cheng, A; Lou, H; Sun, L; Sun, S; Wu, X; Zhang, Y, 2009
)
0.35
"For compounds with a long elimination half-life, the evaluation of a drug-drug interaction (DDI) study can be challenging."( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole.
Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010
)
0.36
"In vitro investigation of pharmacokinetic drug-drug interactions (DDIs) has officially been part of the regulatory pathway for new drugs in the USA since the publication of an FDA guidance on the subject in 1997."( The nasty surprise of a complex drug-drug interaction.
Bode, C, 2010
)
0.36
"To further explore the mechanism underlying the interaction between repaglinide and gemfibrozil, alone or in combination with itraconazole."( Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism.
Chen, W; Gan, J; Gao, L; Hong, Y; Humphreys, WG; Li, W; Rodrigues, AD; Shen, H; Tang, Y; Tian, Y; Zhang, H; Zhang, Y, 2010
)
0.36
"Exposure to vandetanib, as assessed by AUC(504) in healthy subjects, was reduced by around 40% when a single dose was given in combination with the potent CYP3A4 inducer rifampicin."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
0.37
" Due to the difference in the IC50 values for CYP3A4 and CYP3A5, nonconcordant expression of CYP3A4 and CYP3A5 protein can significantly affect the observed magnitude of CYP3A-mediated drug-drug interactions in humans."( Effect of CYP3A5 expression on the inhibition of CYP3A-catalyzed drug metabolism: impact on modeling CYP3A-mediated drug-drug interactions.
Chang, SY; Grubb, MF; Isoherranen, N; Peng, CC; Rodrigues, AD; Shirasaka, Y; Thummel, KE, 2013
)
0.39
" Finally, observed/predicted drug-drug interactions between antiretrovirals and antifungals are summarized along with clinical recommendations."( Clinically relevant drug-drug interactions between antiretrovirals and antifungals.
Mitra, AK; Pal, D; Patel, M; Paturi, DK; Vadlapatla, RK, 2014
)
0.4
" Posaconazole is contraindicated in combination with either efavirenz or fosamprenavir."( Clinically relevant drug-drug interactions between antiretrovirals and antifungals.
Mitra, AK; Pal, D; Patel, M; Paturi, DK; Vadlapatla, RK, 2014
)
0.4
" We treated one case of chromoblastomycosis by photodynamic therapy (PDT) of 5-aminolevulinic acid (ALA) irradiation combined with terbinafine 250 mg a day."( Photodynamic therapy combined with terbinafine against chromoblastomycosis and the effect of PDT on Fonsecaea monophora in vitro.
Hamblin, MR; Hu, Y; Huang, X; Lu, S; Mylonakis, E; Xi, L; Zhang, J, 2015
)
0.42
"Ketoconazole has been widely used as a strong cytochrome P450 (CYP) 3A (CYP3A) inhibitor in drug-drug interaction (DDI) studies."( Best practices for the use of itraconazole as a replacement for ketoconazole in drug-drug interaction studies.
Bello, A; Dresser, MJ; Heald, D; Komjathy, SF; Liu, L; O'Mara, E; Robertson, SM; Rogge, M; Stoch, SA, 2016
)
0.43
" The model was used to predict the pharmacokinetic profiles and drug-drug interaction (DDI) effect for atorvastatin and its metabolites in different DDI scenarios."( Physiologically based pharmacokinetic modeling of disposition and drug-drug interactions for atorvastatin and its metabolites.
Zhang, T, 2015
)
0.42
"Domperidone is a dopamine receptor antagonist and a substrate of CYP3A4, hence there is a potential for CYP3A inhibition-based drug-drug interactions (DDI)."( A physiologically based pharmacokinetic modeling approach to predict drug-drug interactions between domperidone and inhibitors of CYP3A4.
Ravenstijn, P; Sensenhauser, C; Snoeys, J; Templeton, I, 2016
)
0.43
" Under-prediction of pharmacokinetics and drug-drug interactions (DDIs) following multiple doses of itraconazole has limited the use of PBPK model simulation to aid an itraconazole clinical DDI study design."( Development of a Physiologically Based Pharmacokinetic Model for Itraconazole Pharmacokinetics and Drug-Drug Interaction Prediction.
Budha, N; Chen, Y; Hop, CE; Jin, JY; Kenny, JR; Lu, T; Ma, F; Mao, J; Wong, H, 2016
)
0.43
"The mechanism of drug-drug interaction between saquinavir, a protease inhibitor used effectively for HIV/AIDS treatment, and itraconazole, an azole antifungal agent, is hypothesized to involve competitive inhibition at CYP3A4 enzyme, an important drug metabolizing enzyme in humans."( A semi-mechanistic pharmacokinetic model of saquinavir combined with itraconazole in HIV-1-positive patients.
Jenjob, A; Lohitnavy, M; Methaneethorn, J; Pankaew, A; Phuphuak, K; Sriarwut, T, 2015
)
0.42
"The majority of hospitalized patients receiving mold-active triazoles are at risk of drug-drug interactions (DDIs)."( Drug-Drug Interaction Associated with Mold-Active Triazoles among Hospitalized Patients.
Andes, D; Azie, N; Franks, B; Harrington, R; Kelley, C; Khandelwal, N; Kristy, R; Lee, E; Spalding, J; Tan, RD; Wu, EQ; Yang, H, 2016
)
0.43
" Preclinical studies of GTx-024 supported the evaluation of several potential drug-drug interactions in a clinical setting."( Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin.
Coss, CC; Dalton, JT; Jones, A, 2016
)
0.43
"The results of this study suggest that vismodegib can be administered with acid-reducing agents and P-gp and CYP inhibitors without the risk of a clinically meaningful pharmacokinetic drug-drug interaction."( A clinical drug-drug interaction study to evaluate the effect of a proton-pump inhibitor, a combined P-glycoprotein/cytochrome 450 enzyme (CYP)3A4 inhibitor, and a CYP2C9 inhibitor on the pharmacokinetics of vismodegib.
Chandra, P; Colburn, D; Dresser, MJ; Graham, RA; Hop, CE; Malhi, V; Williams, SJ, 2016
)
0.43
" In this study, we examined the efficacy of laser treatment using self-controlled study programs involving a long-pulsed Nd:YAG 1064-nm laser combined with oral medication."( Self-controlled Study of Onychomycosis Treated with Long-pulsed Nd:YAG 1064-nm Laser Combined with Itraconazole.
Li, Y; Xu, J; Zhao, JY; Zhuo, FL, 2016
)
0.43
" Muscle biopsy was compatible with statin-associated rhabdomyolysis, probably caused by a drug-drug interaction between simvastatin and itraconazole."( Statin-associated rhabdomyolysis triggered by drug-drug interaction with itraconazole.
Damkier, P; Dybro, AM; Hellfritzsch, M; Rasmussen, TB, 2016
)
0.43
"The antifungal activity of tacrolimus in combination with antifungal agents against different fungal species has been previously reported."( Antifungal activities of tacrolimus in combination with antifungal agents against fluconazole-susceptible and fluconazole-resistant Trichosporon asahii isolates.
Alves, SH; Azevedo, MI; Denardi, LB; Kubiça, TF; Oliveira, V; Santurio, JM; Severo, LC,
)
0.13
"To investigate the antitumor effect of arsenic trioxide (ATO) combined with itraconazole (ITRA) on human multiple myeloma NCI-H929 cells by synergistically inhibiting Hedgehog (HH) signaling pathway."( [Synergistic Inhibitory Effect of Arsenic Trioxide Combined with Itraconazole on Hedgehog Pathway of Multiple Myeloma NCI-H929 Cells].
Che, FF; Cheng, J; Huang, XB; Shi, Y; Wang, CS; Wang, XD, 2016
)
0.43
"ATO combined with ITRA significantly inhibited NCI-H929 cell proliferation as compared with a single administration."( [Synergistic Inhibitory Effect of Arsenic Trioxide Combined with Itraconazole on Hedgehog Pathway of Multiple Myeloma NCI-H929 Cells].
Che, FF; Cheng, J; Huang, XB; Shi, Y; Wang, CS; Wang, XD, 2016
)
0.43
"ATO combined with ITRA can more strongly suppress the growth of multiple myeloma NCI-H929 cells, as compared with a single administration."( [Synergistic Inhibitory Effect of Arsenic Trioxide Combined with Itraconazole on Hedgehog Pathway of Multiple Myeloma NCI-H929 Cells].
Che, FF; Cheng, J; Huang, XB; Shi, Y; Wang, CS; Wang, XD, 2016
)
0.43
"The efficacy and safety of amorolfine 5% nail lacquer in combination with systemic antifungal agents in the treatment of the onychomycosis were evaluated."( Efficacy and tolerability of amorolfine 5% nail lacquer in combination with systemic antifungal agents for onychomycosis: A meta-analysis and systematic review.
Feng, X; Ran, Y; Xiong, X, 2017
)
0.46
" Menthol in combination with itraconazole or nystatin exhibited the synergistic effects against all species of Candida tested."( Synergistic anticandidal activity of menthol in combination with itraconazole and nystatin against clinical Candida glabrata and Candida krusei isolates.
Khosravi, AR; Sharifzadeh, A; Shokri, H; Tari, PS, 2017
)
0.46
"In this study, impact of a polymorphism of CYP2C19 on drug-drug interaction (DDI) was examined for etizolam."( Notable Drug-Drug Interaction Between Etizolam and Itraconazole in Poor Metabolizers of Cytochrome P450 2C19.
Furihata, K; Hisaka, A; Iwatsubo, T; Kusayama, S; Mori, A; Moritoyo, T; Motohashi, K; Ogoe, K; Suzuki, H; Yamamoto, T, 2017
)
0.46
"To explore the effect of arsenic trioxide combined with itraconazole on proliferation and apoptosis of KG1a cells and its potential mechanism."( [Synergistic Killing Effects of Arsenic Trioxide Combined with Itraconazole on KG1a Cells].
Fan, JX; Guo, KY; Li, YM; Wu, JW; Xiao, WT; Ye, YB; Zeng, YJ; Zhen, R, 2017
)
0.46
"Arsenic trioxide combined with itraconazole can inhibit the KG1a cell proliferation and induce apoptosis, which may be related with the inhibition of Hh signaling pathway and upregulation of both Caspase-3 and BAX protein expression, and provided experimental data of arsenic trioxide combined with itraconazole for the treatment of refractory AML."( [Synergistic Killing Effects of Arsenic Trioxide Combined with Itraconazole on KG1a Cells].
Fan, JX; Guo, KY; Li, YM; Wu, JW; Xiao, WT; Ye, YB; Zeng, YJ; Zhen, R, 2017
)
0.46
" It has been demonstrated to be informative and helpful to quantify the modification in drug exposure due to specific physio-pathological conditions, age, genetic polymorphisms, ethnicity and particularly drug-drug interactions (DDIs)."( Prediction of drug-drug interactions using physiologically-based pharmacokinetic models of CYP450 modulators included in Simcyp software.
Daali, Y; Desmeules, JA; Marsousi, N; Rudaz, S, 2018
)
0.48
" We assessed three drug-drug interactions of avatrombopag as a victim with dual or selective CYP2C9/3A inhibitors and inducers."( Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs.
Aluri, J; Boyd, P; Chang, MK; Ferry, J; Lai, WG; Nomoto, M; Rege, B; Schuck, E; Siu, YA; Yasuda, S; Zamora, CA, 2018
)
0.48
" Herein, we aimed to evaluate the effect of ITC in combination with the mAb-anti-Ly6G in an experimental model of pulmonary PCM."( Itraconazole in combination with neutrophil depletion reduces the expression of genes related to pulmonary fibrosis in an experimental model of paracoccidioidomycosis.
Arango, JC; González, A; Pino-Tamayo, PA; Puerta-Arias, JD; Salazar-Peláez, LM, 2018
)
0.48
" A combination of in vitro data, clinical pharmacokinetic data, and drug-drug interaction (DDI) data of osimertinib in oncology patients were used to develop the physiologically based pharmacokinetic (PBPK) model and verify the DDI data of osimertinib."( Development, Verification, and Prediction of Osimertinib Drug-Drug Interactions Using PBPK Modeling Approach to Inform Drug Label.
Ballard, P; Pilla Reddy, V; Sharma, P; Vishwanathan, K; Walker, M, 2018
)
0.48
"9-ms 1064-nm Nd:YAG laser alone or combined with itraconazole for treatment of toenail onychomycosis."( [Effect of 0.9-ms 1064-nm Nd:YAG laser combined with itraconazole for treatment of toenail onychomycosis].
Han, X; Hu, YQ; Hu, YX; Hunag, SY; Liu, KX; Lu, Y; Mao, ZH; Wu, Z; Yang, YM; Zhong, ZM; Zhou, ST; Zhou, XY, 2018
)
0.48
" The patients in group A were treated with laser alone, and those in group B were treated with laser combined with itraconazole."( [Effect of 0.9-ms 1064-nm Nd:YAG laser combined with itraconazole for treatment of toenail onychomycosis].
Han, X; Hu, YQ; Hu, YX; Hunag, SY; Liu, KX; Lu, Y; Mao, ZH; Wu, Z; Yang, YM; Zhong, ZM; Zhou, ST; Zhou, XY, 2018
)
0.48
" Given the scarcity of options for sporotrichosis treatment and the promising activity of diphenyl diselenide (PhSe)2 against a diversity of fungal pathogens, this study aimed to evaluate the in vitro susceptibility of Sporothrix brasiliensis to (PhSe)2 alone and in combination with itraconazole (ITC)."( Antifungal activity of diphenyl diselenide alone and in combination with itraconazole against Sporothrix brasiliensis.
Klafke, GB; Mattei, AS; Mendes, JF; Poester, VR; Ramis, IB; Sanchotene, KO; Xavier, MO, 2019
)
0.51
" The overall objective of this study is to provide a comprehensive mechanistic PBPK model for itraconazole in order to increase the confidence in its drug-drug interaction (DDI) predictions."( Physiologically Based Pharmacokinetic Model of Itraconazole and Two of Its Metabolites to Improve the Predictions and the Mechanistic Understanding of CYP3A4 Drug-Drug Interactions.
Ericsson, H; Janzén, D; Kanebratt, KP; Lennernäs, H; Lundahl, A; Prieto Garcia, L, 2018
)
0.48
" Using drugs with potential to be repurposed, combined with 5-fluorouracil, the aim of this project was to investigate whether this combination led to therapeutic benefits, comparing with the isolated drugs."( Study of New Therapeutic Strategies to Combat Breast Cancer Using Drug Combinations.
Correia, A; Gärtner, F; Silva, D; Vale, N; Vilanova, M, 2018
)
0.48
"Regulatory agencies currently recommend itraconazole (ITZ) as a strong cytochrome P450 3A (CYP3A) inhibitor for clinical drug-drug interaction (DDI) studies."( Recommendations for the Design of Clinical Drug-Drug Interaction Studies With Itraconazole Using a Mechanistic Physiologically-Based Pharmacokinetic Model.
Cabalu, TD; Callegari, E; Chen, Y; Einolf, H; Hall, SD; Liu, L; Parrott, N; Peters, SA; Schuck, E; Sharma, P; Tracey, H; Upreti, VV; Zheng, M; Zhu, AZX, 2019
)
0.51
" Accordingly, the drug-drug interaction (DDI) potential of darolutamide was investigated in both nonclinical and clinical studies."( Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies.
Bairlein, M; Denner, K; Fricke, R; Gieschen, H; Graudenz, K; Korjamo, T; Koskinen, M; Prien, O; von Bühler, CJ; Wilkinson, G; Zurth, C, 2019
)
0.51
"We treated 5 refractory and complex cases of chromoblastomycosis with 5-aminolevulinic acid photodynamic therapy (ALA-PDT) combined with oral antifungal drugs."( Photodynamic therapy combined with antifungal drugs against chromoblastomycosis and the effect of ALA-PDT on Fonsecaea in vitro.
Chen, X; Hu, Y; Liu, K; Lu, Y; Mao, Z; Qi, X; Sun, H; Wu, Z; Yang, Y; Zhou, X, 2019
)
0.51
"These results provide the basis for the development of a new therapeutic approach, and ALA-PDT combined with oral antifungal drugs constitutes a promising alternative method for the treatment of refractory and complex cases of chromoblastomycosis."( Photodynamic therapy combined with antifungal drugs against chromoblastomycosis and the effect of ALA-PDT on Fonsecaea in vitro.
Chen, X; Hu, Y; Liu, K; Lu, Y; Mao, Z; Qi, X; Sun, H; Wu, Z; Yang, Y; Zhou, X, 2019
)
0.51
" An integrated in silico, in vitro, and clinical approach including a clinical drug interaction study as well as a bespoke physiologically based pharmacokinetic (PBPK) model was used to assess the drug-drug interaction (DDI) risk."( Drug Interactions for Low-Dose Inhaled Nemiralisib: A Case Study Integrating Modeling, In Vitro, and Clinical Investigations.
Cahn, AP; Georgiou, A; Harrell, AW; Hessel, EM; Marotti, M; Patel, A; Riddell, K; Taskar, KS; Taylor, M; Tracey, H; Wilson, R, 2020
)
0.56
"Cyclodextrins are widely used pharmaceutical excipients, particularly for insoluble compounds dosed orally, such as the oral solution of itraconazole, which is frequently used in clinical drug-drug interaction studies to inhibit cytochrome P450 3A."( Understanding the Effect of Hydroxypropyl-β-Cyclodextrin on Fenebrutinib Absorption in an Itraconazole-Fenebrutinib Drug-Drug Interaction Study.
Chen, JZ; Chen, Y; Chiang, PC; Chinn, LW; Durk, MR; Jones, NS; Liu, J; Mao, C; Nagapudi, K; Plise, EG; Wong, S, 2020
)
0.56
"In this study, we aimed to develop and validate a sensitive and simple ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the quantification of gilteritinib in plasma and to investigate whether CYP3A4 inhibitors (fluconazole and itraconazole) could influence the pharmacokinetics of gilteritinib from a drug-drug interaction study in rats."( An LC-MS/MS Bioanalytical Assay for the Determination of Gilteritinib in Rat Plasma and Application to a Drug-Drug Interaction Study.
Chen, D; Chen, Z; Wang, Q; Ye, XY, 2020
)
0.56
" The validated UPLC-MS/MS method was successfully applied to a drug-drug interaction study between gilteritinib and CYP3A4 inhibitors (fluconazole and itraconazole) in rats."( An LC-MS/MS Bioanalytical Assay for the Determination of Gilteritinib in Rat Plasma and Application to a Drug-Drug Interaction Study.
Chen, D; Chen, Z; Wang, Q; Ye, XY, 2020
)
0.56
" Consequently, the potential of iberdomide as a victim of drug-drug interactions (DDI) was evaluated in a clinical study with healthy subjects."( Evaluation of iberdomide and cytochrome p450 drug-drug interaction potential in vitro and in a phase 1 study in healthy subjects.
Atsriku, C; Gaudy, A; Liu, L; MacGorman, K; Palmisano, M; Surapaneni, S; Xue, Y; Ye, Y, 2021
)
0.62
"6 mg) and when administered with the CYP3A and P-gp inhibitor itraconazole (200 mg twice daily on day 1 and 200 once daily on days 2 through 9)."( Evaluation of iberdomide and cytochrome p450 drug-drug interaction potential in vitro and in a phase 1 study in healthy subjects.
Atsriku, C; Gaudy, A; Liu, L; MacGorman, K; Palmisano, M; Surapaneni, S; Xue, Y; Ye, Y, 2021
)
0.62
"Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)."( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia.
Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020
)
0.56
" Concerns about drug-drug interactions (DDIs) have meant patients receiving drugs that inhibit CYP3A4 were ineligible for acumapimod trials."( A Physiologically Based Pharmacokinetic Model to Predict Potential Drug-Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor.
Agyemang, A; Farrell, C; Moore, W; Parkin, J, 2021
)
0.62
"This drug-drug interaction study determined whether the metabolism and distribution of the Polo-like kinase 1 inhibitor, volasertib, is affected by co-administration of the P-glycoprotein and cytochrome P-450 3A4 inhibitor, itraconazole."( Potential Drug-Drug Interactions with Combination Volasertib + Itraconazole: A Phase I, Fixed-sequence Study in Patients with Solid Tumors.
Chizhikov, E; Fritsch, H; Lang, I; Liptai, B; Liu, D; Taube, T, 2020
)
0.56
" Due to its widespread use and CYP3A4-mediated metabolism, there is concern regarding drug-drug interactions (DDIs), particularly a suboptimal LNG exposure when co-administered with CYP3A4 inducers, potentially leading to unintended pregnancies."( Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling.
Chaturvedula, A; Cicali, B; Cristofoletti, R; Hoechel, J; Lingineni, K; Schmidt, S; Vozmediano, V; Wendl, T; Wiesinger, H, 2021
)
0.62
"To assess the pharmacokinetic of itraconazole capsule formulation and its active metabolite, hydroxyitraconazole, in adults with HIV diagnosed with talaromycosis in an endemic area, and to evaluate the drug-drug interaction between itraconazole/hydroxyitraconazole (ITC/OH-ITC) and efavirenz."( Drug-drug interaction between itraconazole capsule and efavirenz in adults with HIV for talaromycosis treatment.
Chaiwarith, R; Chindamporn, A; Cressey, TR; Kaewpoowat, Q; Sirisanthana, T; Worasilchai, N; Yasri, S, 2021
)
0.62
" The clinical impact of this drug-drug interaction on talaromycosis treatment or prophylaxis in the era of potent ART needs further evaluation."( Drug-drug interaction between itraconazole capsule and efavirenz in adults with HIV for talaromycosis treatment.
Chaiwarith, R; Chindamporn, A; Cressey, TR; Kaewpoowat, Q; Sirisanthana, T; Worasilchai, N; Yasri, S, 2021
)
0.62
" In vitro experiments proved that terbinafine combined with itraconazole achieves better antifungal effects."( Terbinafine Hydrochloride Combined With Itraconazole for Fungal Skin Diseases: A Randomized Controlled Trial.
Chen, C; Lai, H; Liao, W; Liu, S; Zhang, D,
)
0.13
"Terbinafine combined with itraconazole achieves better therapeutic effects in fungal skin diseases."( Terbinafine Hydrochloride Combined With Itraconazole for Fungal Skin Diseases: A Randomized Controlled Trial.
Chen, C; Lai, H; Liao, W; Liu, S; Zhang, D,
)
0.13
" The current study aims to understand the drug-drug interaction (DDI) risk of milademetan as a CYP3A substrate during its early clinical development."( Model-based assessments of CYP3A-mediated drug-drug interaction risk of milademetan.
Abutarif, M; Hong, Y; Ishizuka, H; Ishizuka, T; LaCreta, F; Lee, M; Tachibana, M; Watanabe, A, 2021
)
0.62
" This model was built based on physiochemical data and clinical in vivo drug-drug interaction (DDI) studies with itraconazole and fluconazole, and verified against data from an in vivo rifampicin DDI study and an absolute bioavailability study."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
0.62
"We investigated savolitinib pharmacokinetics (PK) when administered alone or in combination with rifampicin, itraconazole or famotidine, and investigated midazolam PK when administered with or without savolitinib in healthy males."( Clinical evaluation of the potential drug-drug interactions of savolitinib: Interaction with rifampicin, itraconazole, famotidine or midazolam.
Burke, W; Cantarini, M; Frewer, P; Goldwater, R; Han, D; Hara, I; Li, Y; Ren, S; Scarfe, G; Schalkwijk, S; Vishwanathan, K, 2022
)
0.72
" Photodynamic therapy combined with oral itraconazole was administered, and the patient recovered in a short time."( Photodynamic therapy combined with itraconazole against a case of cutaneous blastomycosis.
Cheng, QH; Ding, W; He, Y; Huang, XQ; Lei, X; Wu, JJ; Zhang, XJ, 2021
)
0.62
" As such, this 2-part clinical drug-drug interaction study was conducted to assess the effect of itraconazole (a strong CYP3A4 inhibitor), rifampicin (a strong CYP3A4 inducer), rabeprazole, and omeprazole (both proton pump inhibitors) on the pharmacokinetics of belumosudil."( A Phase 1 Pharmacokinetic Drug Interaction Study of Belumosudil Coadministered With CYP3A4 Inhibitors and Inducers and Proton Pump Inhibitors.
Alabanza, A; Lohmer, L; Patel, J; Schueller, O; Singh, N; Willson, A, 2022
)
0.72
" albicans isolates and to evaluate the inhibitory activity of eucalyptol on Candida biofilm, alone and in combination with antifungal agents."( Anti-biofilm properties of eucalyptol in combination with antifungals against Candida albicans isolates in patients with hematological malignancy.
Abolghasemi, S; Falahati, M; Farahyar, S; Ghasemi, R; Keymaram, M; Khalandi, H; Lotfali, E; Mahmoudi, S; Raiesi, O; Sadeghi, F; Shamsaei, S, 2022
)
0.72
" Here, we investigate the pharmacokinetic drug-drug interaction potential of trilaciclib."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
0.72
"Overall, the drug-drug interaction and safety profiles of trilaciclib in these studies support its continued use in patients with extensive-stage small-cell lung cancer."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
0.72
" Understanding potential drug-drug interactions (DDIs) informs proper dosing when co-administering tucatinib with other therapies."( Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers.
Abdulrasool, LI; Endres, CJ; Lee, A; Mayor, JG; Rustia, EL; Sun, H; Topletz-Erickson, A; Walker, L, 2022
)
0.72
" Here, we report the results from 2 drug-drug interaction studies."( Drug-Drug Interaction Studies to Evaluate the Effect of Inhibition of UGT1A1 and CYP3A4 and Induction of CYP3A4 on the Pharmacokinetics of Tropifexor in Healthy Subjects.
Chen, J; Gu, J; Hackling, M; Prince, W; Shah, B; Stringer, R; Woessner, R; Zhang, Y, 2022
)
0.72
" It is metabolized via cytochrome P450 (CYP) 3A, but little is known about the drug-drug interactions of JNJ-56136379 when combined with drugs that inhibit or are metabolized by CYP3A."( Drug-Drug Interactions With the Hepatitis B Virus Capsid Assembly Modulator JNJ-56136379 (Bersacapavir).
Biermer, M; Biewenga, J; Hillewaert, V; Kakuda, TN; Nangosyah, J; Palmer, M; Rasschaert, F; Snoeys, J; Talloen, W; Vandenbossche, J; Yogaratnam, J, 2022
)
0.72
" Based on nonclinical in vitro characterization of gepotidacin metabolism, two phase I studies were conducted in healthy participants to investigate clinical drug-drug interactions (DDIs)."( Clinical assessment of gepotidacin (GSK2140944) as a victim and perpetrator of drug-drug interactions via CYP3A metabolism and transporters.
Barth, A; Brimhall, DB; Dumont, EF; Nguyen, D; Perry, CR; Shabbir, S; Srinivasan, M; Swift, B; Thomas, S; Zamek-Gliszczynski, MJ, 2023
)
0.91
" Considering the possibility of combination therapy in patients with NSCLC, we investigated the drug-drug interaction (DDI) potential of SH-1028 both in vitro and in clinical trials."( Drug-drug interaction potential of SH-1028, a third-generation EGFR-TKI: in vitro and clinical trials.
Ding, J; Ding, Y; He, C; Li, X; Liu, B; Liu, Y; Shan, R; Wang, Y; Wang, Z; Xie, J; Xu, Y; Zhou, H; Zhu, M, 2023
)
0.91
" Phase I studies investigated the drug-drug interactions of futibatinib with itraconazole (a dual P-gp and strong CYP3A inhibitor), rifampin (a dual P-gp and strong CYP3A inducer), or midazolam (a sensitive CYP3A substrate) in healthy adult participants."( Evaluation of the Cytochrome P450 3A and P-glycoprotein Drug-Drug Interaction Potential of Futibatinib.
Benhadji, KA; Gao, L; He, Y; Hunt, A; Mina, M; Sonnichsen, D; Takenaka, T; Yamamiya, I, 2023
)
0.91
"Itraconazole is a potent inhibitor of cytochrome P450 3A4 (CYP3A4), associated with numerous drug-drug interactions (DDI)."( Evaluation of the Potential for Drug-Drug Interactions with Inhaled Itraconazole Using Physiologically Based Pharmacokinetic Modelling, Based on Phase 1 Clinical Data.
Bergagnini-Kolev, M; Curran, AK; Kane, K; Templeton, IE, 2023
)
0.91
" Clinical pharmacokinetic drug-drug interaction (DDI) of ocedurenone with CYP3A inhibitor and inducer were investigated in healthy volunteers."( Pharmacokinetics and Drug-Drug Interaction of Ocedurenone (KBP-5074) in vitro and in vivo.
Liu, J; McCabe, J; Tan, X; Wang, P; Yang, F; Zhang, J, 2023
)
0.91
" This study is aimed to evaluate the in vitro activity of doxycycline combined with antifungal therapy against dominant Mucorales pathogens."( In vitro combination with doxycycline plus antifungals against clinical Mucorales pathogens.
Liang, G; Liu, W; Pathakumari, B; Song, G; Zhang, M; Zheng, H, 2023
)
0.91
"The vitro antifungal activity of retigeric acid B (RAB), a pentacyclic triterpenoid from the lichen species Lobaria kurokawae, was evaluated alone and in combination with fluconazole, ketoconazole, and itraconazole against Candida albicans using checkerboard microdilution and time-killing tests."( In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
Cheng, A; Lou, H; Sun, L; Sun, S; Wu, X; Zhang, Y, 2009
)
0.54
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38

Bioavailability

The aim of this study is to compare the bioavailability of two itraconazole (CAS 84625-61-6) capsule formulations. The drug has extremely poor solubility and its bioavailability is affected by food.

ExcerptReferenceRelevance
" 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
)
0.29
" The bioavailability (90% confidence intervals) of itraconazole relative to that after the full meal, was 54% (41-77%) on an empty stomach and 86% (65-102%) after a light meal."( Influence of concomitant food intake on the oral absorption of two triazole antifungal agents, itraconazole and fluconazole.
Laufen, H; Pfaff, G; Wildfeuer, A; Yeates, RA; Zimmermann, T, 1994
)
0.29
" This itraconazole-cyclodextrin solution was well absorbed and was effective in the treatment of experimental invasive aspergillosis; it demonstrates the potential of this class of agents in improving therapy for invasive aspergillosis."( Efficacy of itraconazole solution in a rabbit model of invasive aspergillosis.
Fothergill, AW; Patterson, TF; Rinaldi, MG, 1993
)
0.29
" The improved effectiveness of these agents is probably related to their rapid penetration into the nails and prolonged bioavailability at the site of infection."( New approaches to the treatment of onychomycosis.
De Doncker, P; Roseeuw, D, 1993
)
0.29
"Our findings suggest that the higher bioavailability of this new formulation of itraconazole may be of benefit in seriously ill patients who are not able to ingest adequate quantities of food."( Effect of food on the pharmacokinetics of a new hydroxypropyl-beta-cyclodextrin formulation of itraconazole.
Cauwenbergh, GF; De Beule, KL; Heykants, JJ; Van de Velde, VJ; Van Peer, AP; Van Rooy, P; Woestenborghs, RJ,
)
0.13
" In addition, a comparative evaluation of the oral bioavailability of itraconazole was made in volunteers after intake of Funazol and Sporanox."( Paradoxical response to itraconazole treatment in a patient with onychomycosis caused by Microsporum gypseum.
Arrese, JE; De Doncker, P; Jacqmin, P; Pierard, GE; Pierard-Franchimont, G; Van de Velde, V, 1995
)
0.29
" The systemic bioavailability of desmethylastemizole was also increased."( Influence of itraconazole on the pharmacokinetics and electrocardiographic effects of astemizole.
Lefebvre, RA; Van Peer, A; Woestenborghs, R, 1997
)
0.3
"Thirty-three healthy individuals participated in an open-label, randomized, three-way crossover study designed to compared the bioavailability of a single 200-mg oral dose of itraconazole when administered alone or after treatment with ranitidine, both with and without coadministration of a cola beverage."( Effect of a cola beverage on the bioavailability of itraconazole in the presence of H2 blockers.
Klausner, M; Lange, D; Pavao, JH; Wu, J, 1997
)
0.3
"To determine the disposition of itraconazole in cats after single IV and oral dosing (as a solution or capsule) and multiple oral (capsule) dosing, and to establish bioavailability after oral administration of the solution."( Itraconazole disposition after single oral and intravenous and multiple oral dosing in healthy cats.
Boothe, DM; Calvin, J; Dvorak, J; Herring, I; Way, N, 1997
)
0.3
"864 micrograms/ml, MRT was 48 +/- 17 hours, and bioavailability was 78."( Itraconazole disposition after single oral and intravenous and multiple oral dosing in healthy cats.
Boothe, DM; Calvin, J; Dvorak, J; Herring, I; Way, N, 1997
)
0.3
"Oxybutynin has low oral bioavailability due to an extensive presystemic metabolism."( Itraconazole moderately increases serum concentrations of oxybutynin but does not affect those of the active metabolite.
Aranko, K; Juhakoski, A; Lukkari, E; Neuvonen, PJ, 1997
)
0.3
"The oral bioavailability of buspirone is very low as a result of extensive first-pass metabolism."( Plasma buspirone concentrations are greatly increased by erythromycin and itraconazole.
Kantola, T; Kivistö, KT; Lamberg, TS; Neuvonen, PJ, 1997
)
0.3
" 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 bioavailability of fluconazole is much less varied although validation of compliance is a situation where obtaining serum concentrations may provide additional information."( Therapeutic drug monitoring of systemic antifungal therapy.
Gore, SJ; Graybill, JR; Hardin, TC; Summers, KK, 1997
)
0.3
"The bioavailability of itraconazole from an extemporaneously prepared suspension was compared with its bioavailability from the commercially available capsules."( Relative bioavailability of itraconazole from an extemporaneously prepared suspension and from the marketed capsules.
Bowman, JL; Buice, RG; Christensen, KJ; Gubbins, PO; Gurley, BJ, 1998
)
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
"Omeprazole affects itraconazole kinetics, leading to a reduction in bioavailability and Cmax."( Effect of omeprazole on the pharmacokinetics of itraconazole.
Jaruratanasirikul, S; Sriwiriyajan, S, 1998
)
0.3
" Itraconazole has recently undergone reformulation as a solution, which gives significant added advantages in bioavailability and increases the practical applications."( Itraconazole: managing mycotic complications in immunocompromised patients.
Graybill, JR, 1998
)
0.3
" This work shows a good bioavailability of itraconazole oral solution during the early phase after allogeneic BMT, but more data are needed for the late phases."( Pharmacokinetics of itraconazole oral solution in allogeneic bone marrow transplant patients receiving total body irradiation.
Belhabri, A; Chwetzoff, E; Fiere, D; Kranzhöfer, N; Le Moing, JP; Levron, JC; Michallet, M; Persat, F; Piens, MA; Prat, C, 1998
)
0.3
" Ten (50%) patients in the itraconazole group were taking concomitant medications that could potentially affect the bioavailability of itraconazole."( Safety and efficacy of single-dose fluconazole compared with a 7-day regimen of itraconazole in the treatment of AIDS-related oropharyngeal candidiasis.
Clumeck, N; De Vroey, C; De Wit, S; O'Doherty, E,
)
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
"Lignocaine is metabolized by cytochrome P450 3A4 enzyme (CYP3A4), and has a moderate to high extraction ratio resulting in oral bioavailability of 30%."( Effect of erythromycin and itraconazole on the pharmacokinetics of oral lignocaine.
Isohanni, MH; Neuvonen, PJ; Olkkola, KT, 1999
)
0.3
" Therapeutic itraconazole monitoring by plasma concentrations measurement is justified by its dose-dependent pharmacokinetics, drug interactions, and frequent bioavailability modifications observed in immunocompromised patients."( [Prevention of aspergillosis with itraconazole in neutropenic patients: importance of drug monitoring].
Cheymol, G; Poirier, JM, 1999
)
0.3
" Itraconazole has a broader spectrum of activity but the capsules give erratic bioavailability in neutropenic patients."( A randomized controlled trial of itraconazole versus fluconazole for the prevention of fungal infections in patients with haematological malignancies. U.K. Multicentre Antifungal Prophylaxis Study Group.
Morgenstern, GR; Prentice, AG; Prentice, HG; Ropner, JE; Schey, SA; Warnock, DW, 1999
)
0.3
" Since the bioavailability of itraconazole is reduced in these patients, a satisfactory dosing regimen remains to be defined."( Itraconazole trough concentrations in antifungal prophylaxis with six different dosing regimens using hydroxypropyl-beta-cyclodextrin oral solution or coated-pellet capsules.
Glasmacher, A; Hahn, C; Marklein, G; Molitor, E; Sauerbruch, T; Schmidt-Wolf, IG, 1999
)
0.3
"The role of itraconazole in anti-fungal prophylaxis has been limited by the low bioavailability of the capsule formulation but the bioavailability of the oral solution is much improved."( Antifungal prophylaxis with itraconazole oral solution in neutropenic patients.
Kibbler, CC, 1999
)
0.3
" When given orally, its absorption was low, with a mean absolute bioavailability of 16."( Absorption, first-pass metabolism, and disposition of itraconazole in rats.
Jun, H; Kang, E; Lee, KC; Lee, KH; Shin, BS; Yoo, SD, 2000
)
0.31
" Fluconazole and itraconazole are widely used in chemoprophylaxis because of their favourable oral bioavailability and safety profiles."( Current management of fungal infections.
Meis, JF; Verweij, PE, 2001
)
0.31
" The enhanced absorption and bioavailability of itraconazole from these new formulations make them ideal for the treatment of systemic fungal infections in a wide range of patient populations."( Pharmacology of itraconazole.
De Beule, K; Van Gestel, J, 2001
)
0.31
" The recent development of an itraconazole oral solution and an intravenous itraconazole solution has increased the options for the use of this drug and increased the oral bioavailability in a variety of at-risk patients."( Clinical experience with itraconazole in systemic fungal infections.
Boogaerts, M; Maertens, J, 2001
)
0.31
" These formulations have improved the solubility of itraconazole, leading to enhanced absorption and bioavailability compared with the original capsule formulation, without having an impact on the tolerability profile of itraconazole."( Itraconazole oral solution and intravenous formulations: a review of pharmacokinetics and pharmacodynamics.
de Beule, K; van der Geest, R; Willems, L, 2001
)
0.31
" Itraconazole-cyclodextrin is well absorbed even in the presence of chemotherapy-induced neutropenia."( The use of itraconazole as prophylaxis against invasive fungal infection in blood and marrow transplant recipients.
Boyle, BM; McCann, SR, 2000
)
0.31
"This open-label, two-way crossover study was undertaken to determine whether the enteric formulation of didanosine influences the pharmacokinetics of itraconazole or fluconazole, two agents frequently used to treat fungal infections that occur with HIV infection, and whose bioavailability may be influenced by changes in gastric pH."( Absence of clinically relevant drug interactions following simultaneous administration of didanosine-encapsulated, enteric-coated bead formulation with either itraconazole or fluconazole.
Damle, B; Hess, H; Kaul, S; Knupp, C, 2002
)
0.31
" This formulation has a higher bioavailability and leads to higher local concentrations in the oral cavity which are advantages over the solid capsule formulation."( Itraconazole solution: summary of pharmacokinetic features and review of activity in the treatment of fluconazole-resistant oral candidosis in HIV-infected persons.
Beijnen, JH; Bult, A; Koks, CH; Meenhorst, PL, 2002
)
0.31
"Oral itraconazole solution has adequate bioavailability in liver transplant recipients for effective antifungal prophylaxis."( Randomized controlled trial of oral itraconazole solution versus intravenous/oral fluconazole for prevention of fungal infections in liver transplant recipients.
Busuttil, RW; Winston, DJ, 2002
)
0.31
" General considerations that may be associated with recurrent infections are, a genetic predisposition and suboptimal bioavailability of drug, resulting in insufficient concentration at the target site."( Onychomycosis: strategies to improve efficacy and reduce recurrence.
Baran, R; Gupta, AK; Summerbell, R, 2002
)
0.31
" The results suggest that cocrystals of drug molecules have the possibility of achieving the higher oral bioavailability common for amorphous forms of water-insoluble drugs while maintaining the long-term chemical and physical stability that crystal forms provide."( Crystal engineering of novel cocrystals of a triazole drug with 1,4-dicarboxylic acids.
Almarsson, O; Guzmán, HR; MacPhee, JM; Morissette, SL; Moulton, B; Peterson, ML; Remenar, JF, 2003
)
0.32
" Hence, the method is suitable for use in pharmacokinetic and bioavailability studies of itraconazole."( Liquid chromatographic method for the determination of plasma itraconazole and its hydroxy metabolite in pharmacokinetic/bioavailability studies.
Nisar, UR; Wong, JW; Yuen, KH, 2003
)
0.32
" The extent of absolute oral bioavailability (F) was 34."( Dose-dependent pharmacokinetics of itraconazole after intravenous or oral administration to rats: intestinal first-pass effect.
Choi, KY; Kim, YC; Lee, MG; Shin, JH, 2004
)
0.32
" Two of the first nine patients, in whom bioavailability was compromised due to significant vomiting and/or diarrhoea, died of probable or proven invasive aspergillus."( A pilot study of targeted itraconazole prophylaxis in patients with graft-versus-host disease at high risk of invasive mould infections following allogeneic stem cell transplantation.
Brown, M; Grigg, AP; Roberts, AW; Slavin, MA; Szer, J, 2004
)
0.32
" The mean bioavailability of itraconazole was comparable after administration of the HPMC solid dispersion, compared to Sporanox, while it was lower after administration of the Eudragit E100 or Eudragit E100-PVPVA64 dispersions."( Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion.
Bouche, MP; Brewster, ME; Daems, T; de Hoon, J; Depre, M; Peeters, J; Prinsen, P; Six, K; Van den Mooter, G; Van Hecken, A; Verreck, G, 2005
)
0.33
"The findings are in line with the hypothesis that the determination of the bioavailability of highly variable CYP3A substrates might be improved by simultaneous non-interfering phenotyping."( Simultaneous itraconazole bioequivalence assessment and CYP3A phenotyping in South American subjects.
Bellocq, B; del Campo, MJ; Estevez-Carrizo, FE; Leal, C; Ruiz, S; Siri, MT, 2005
)
0.33
"A population pharmacokinetic analysis of cyclosporine (CsA) was performed, and the influence of covariates on CsA oral clearance and relative bioavailability was investigated."( Population pharmacokinetics of cyclosporine in cardiopulmonary transplant recipients.
Akhlaghi, F; Baheti, G; Rosenbaum, SE; Trull, AK, 2005
)
0.33
"The objective of this study was to elucidate the feasibility to improve the solubility and bioavailability of poorly water-soluble itraconazole via solid dispersions by using supercritical fluid (SCF)."( Preparation and characterization of solid dispersions of itraconazole by using aerosol solvent extraction system for improvement in drug solubility and bioavailability.
Hwang, SJ; Jun, SW; Kim, MS; Lee, S; Nam, K; Park, JS; Woo, JS, 2005
)
0.33
" Bioavailability after administration of capsules relative to solution was 33."( Pharmacokinetics and tissue distribution of itraconazole after oral and intravenous administration to horses.
Davis, JL; Papich, MG; Salmon, JH, 2005
)
0.33
" These results demonstrate that the SEDDS of itraconazole composed of Transcutol, Pluronic L64 and tocopherol acetate greatly enhanced the bioavailability of itraconazole after the dose, particularly not influenced by food intake or not."( A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption.
Hong, JY; Kim, CK; Kim, JK; Park, JS; Song, YK, 2006
)
0.33
" BCS class II compounds are poorly soluble but highly permeable, exhibiting bioavailability that is limited by dissolution."( Cryogenic liquids, nanoparticles, and microencapsulation.
Chen, X; Hu, J; Johnston, KP; McConville, JT; Overhoff, KA; Purvis, T; Rogers, TL; Sinswat, P; Vaughn, JM; Williams, RO, 2006
)
0.33
" The bioavailability of the liquid formulation was significantly lower when the solution was given by a feeding tube."( Itraconazole prophylaxis in pediatric cancer patients receiving conventional chemotherapy or autologous stem cell transplants.
Besuden, M; Bode, U; Fleischhack, G; Glasmacher, A; Hasan, C; Kreutzberg, S; Lampe, D; Simon, A; Vezmar, S, 2007
)
0.34
" 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
"The objectives of this retrospective study were to examine the relationship between the bioavailability of itraconazole and the type of food consumed and to determine the effects of food consumption on the pharmacokinetic parameters following a single oral dose of itraconazole in healthy volunteers."( Comparative analysis of the effects of rice and bread meals on bioavailability of itraconazole using NONMEM in healthy volunteers.
Baek, MS; Choi, BK; Kwon, KI; Park, IS; Yun, HY, 2006
)
0.33
"The primary objective of the study was to estimate the population pharmacokinetic parameters for itraconazole and hydroxy-itraconazole, in particular, the relative oral bioavailability of the capsule compared with solution in adult cystic fibrosis patients, in order to develop new dosing guidelines."( A d-optimal designed population pharmacokinetic study of oral itraconazole in adult cystic fibrosis patients.
Bell, SC; Charles, BG; Duffull, SB; France, M; Hennig, S; Miller, H; Wainwright, CE; Waterhouse, TH, 2007
)
0.34
" The relative bioavailability for itraconazole capsules was 82% compared with the solution."( A d-optimal designed population pharmacokinetic study of oral itraconazole in adult cystic fibrosis patients.
Bell, SC; Charles, BG; Duffull, SB; France, M; Hennig, S; Miller, H; Wainwright, CE; Waterhouse, TH, 2007
)
0.34
" It was anticipated that the semisolid dosage forms would be industrially applicable to improving the bioavailability of poorly water-soluble drugs."( Characterization of itraconazole semisolid dosage forms prepared by hot melt technique.
Ji, CW; Lee, BJ; Park, ES; Sah, H; Shim, SY, 2006
)
0.33
" The present study demonstrated that the bioavailability of paroxetine was increased by itraconazole, suggesting a possible involvement of P-glycoprotein in the pharmacokinetics of paroxetine."( Effect of itraconazole on pharmacokinetics of paroxetine: the role of gut transporters.
Inoue, Y; Kaneko, S; Niioka, T; Saito, M; Sato, Y; Yasui-Furukori, N, 2007
)
0.34
" Due to the biopharmaceutical differences of SES in terms of efficient solubilization, easy dispersibility and higher lymphatic transport, the in vivo bioavailability of SES was about twice greater than that of SD in rats."( In vitro and in vivo comparative study of itraconazole bioavailability when formulated in highly soluble self-emulsifying system and in solid dispersion.
Lee, BJ; Park, MJ; Ren, S, 2007
)
0.34
"The main objective of this study was to improve the inclusion formation between itraconazole and beta-cyclodextrin and thus enhance dissolution amount and bioavailability characteristics of itraconazole."( Enhancement of dissolution amount and in vivo bioavailability of itraconazole by complexation with beta-cyclodextrin using supercritical carbon dioxide.
Al-Marzouqi, AH; Hamza, AA; Hassan, HA; Jobe, B; Ramadan, GA, 2007
)
0.34
" When administered as oral solutions, the itraconazole:HBenBCD formulation provided higher oral bioavailability than the Sporanox oral solution."( Pharmacokinetics of itraconazole after intravenous and oral dosing of itraconazole-cyclodextrin formulations.
Buchanan, CM; Buchanan, NL; Edgar, KJ; Klein, S; Little, JL; Ramsey, MG; Ruble, KM; Wacher, VJ; Wempe, MF, 2007
)
0.34
" After loading itraconazole into OMS, its oral bioavailability was compared with the crystalline drug and the marketed product Sporanox in rabbits and dogs."( Increasing the oral bioavailability of the poorly water soluble drug itraconazole with ordered mesoporous silica.
Aerts, CA; Annaert, P; Augustijns, P; Jammaer, JA; Martens, JA; Mellaerts, R; Mols, R; Van den Mooter, G; Van Humbeeck, J, 2008
)
0.35
" This study was designed to compare the oral bioavailability and food-effect of SMEDDS of itraconazole (ITRA-GSMP capsule containing 50mg itraconazole) to that of the currently marketed formulation (Sporanox capsule containing 100mg itraconazole)."( Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers.
Hong, JY; Kim, CK; Lim, SJ; Song, YK; Woo, JS, 2008
)
0.35
" Although itraconazole co-administration is known to increase the bioavailability of a racemic mixture of fexofenadine, little is known about the stereoselective inhibition of P-gp activity by itraconazole."( The different effects of itraconazole on the pharmacokinetics of fexofenadine enantiomers.
Miura, M; Suzuki, T; Tateishi, T; Uno, T, 2008
)
0.35
" Clearance, volume of distribution and the absorption rate constant were 12."( Population pharmacokinetics of itraconazole solution used as prophylaxis for febrile neutropenia.
Fujimoto, Y; Horiike, S; Kanbayashi, Y; Matsumoto, Y; Nomura, K; Okamoto, K; Shimazaki, C; Shimizu, D; Shimura, K; Takagi, T; Taniwaki, M, 2008
)
0.35
"2, w/w) yielded improved bioavailability in mice."( High bioavailability from nebulized itraconazole nanoparticle dispersions with biocompatible stabilizers.
Johnston, KP; McConville, JT; Miller, DA; Tam, J; Williams, RO; Yang, W; Zhou, J, 2008
)
0.35
" The effect of medium composition on the intrinsic dissolution rate of itraconazole was evaluated as this drug has extremely poor solubility and its bioavailability is affected by food."( In vitro evaluation of the dissolution behaviour of itraconazole in bio-relevant media.
Dyas, AM; Ford, JL; Ghazal, HS; Hutcheon, GA, 2009
)
0.35
" However, the efficacy and bioavailability of these drugs have been limited by their poor aqueous solubility and dissolution rate."( Physicochemical properties of antifungal drug-cyclodextrin complexes prepared by supercritical carbon dioxide and by conventional techniques.
Adem, A; Al-Marzouqi, AH; Elwy, HM; Shehadi, I, 2009
)
0.35
"8 by minimizing undissolved excess surface area may be expected to be beneficial for raising bioavailability by gastrointestinal delivery."( Highly supersaturated solutions from dissolution of amorphous itraconazole microparticles at pH 6.8.
Johnston, KP; Matteucci, ME; Miller, MA; Paguio, JC; Williams, RO,
)
0.13
"Amorphous engineered particle compositions of itraconazole (ITZ) and potential concentration enhancing polymers, cellulose acetate phthalate (CAP) and polyvinyl acetate phthalate (PVAP), were produced by ultra-rapid freezing to investigate the effect of these polymers on the bioavailability of ITZ solid dispersions."( Amorphous compositions using concentration enhancing polymers for improved bioavailability of itraconazole.
DiNunzio, JC; McGinity, JW; Miller, DA; Williams, RO; Yang, W,
)
0.13
" These results suggest that oral solution itraconazole significantly interacts with calcineurin inhibitors with a wide interindividual variability in allogeneic HSCT recipients, which could partly be explained by the variable bioavailability of oral solution itraconazole."( Drug interaction between oral solution itraconazole and calcineurin inhibitors in allogeneic hematopoietic stem cell transplantation recipients: an association with bioavailability of oral solution itraconazole.
Aisa, Y; Ikeda, Y; Kato, J; Mori, T; Nakamura, Y; Okamoto, S, 2009
)
0.35
" Oral bioavailability was determined using a Sprague-Dawley rat model."( Fusion processing of itraconazole solid dispersions by kinetisol dispersing: a comparative study to hot melt extrusion.
Brough, C; DiNunzio, JC; McGinity, JW; Miller, DA; Williams, RO, 2010
)
0.36
" Oral bioavailability of the 30/70 dispersion was, although lower compared to the marketed Sporanox formulation, significantly enhanced compared to the crystalline drug."( Itraconazole/TPGS/Aerosil200 solid dispersions: characterization, physical stability and in vivo performance.
Augustijns, P; Froyen, L; Houthoofd, K; Martens, JA; Mols, R; Van den Mooter, G; Van Eerdenbrugh, B; Van Humbeeck, J; Van Speybroeck, M, 2009
)
0.35
"001), with an enormous reduction in the oral bioavailability of ebastine and significantly reduced histamine-induced skin reactions."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
0.36
"The effect of supersaturation on bioavailability of inhaled nebulized aerosols is compared for amorphous versus crystalline nanoparticulate dispersions."( Comparison of bioavailability of amorphous versus crystalline itraconazole nanoparticles via pulmonary administration in rats.
Johnston, KP; Williams, RO; Yang, W, 2010
)
0.36
" To enhance the oral bioavailability of such compounds, pharmaceutical formulations target the creation of a supersaturated solution."( Growth of itraconazole nanofibers in supersaturated simulated intestinal fluid.
Aerts, A; Augustijns, P; Caremans, TP; Martens, JA; Mellaerts, R; Van den Mooter, G; Vermant, J, 2010
)
0.36
" Oral bioavailability of lead formulations was also assessed in animal models."( Production of advanced solid dispersions for enhanced bioavailability of itraconazole using KinetiSol Dispersing.
Brough, C; DiNunzio, JC; Hughey, JR; McGinity, JW; Miller, DA; Williams, RO, 2010
)
0.36
" Co-administration of Icz with CsA resulted in significant increases of oral bioavailability of CsA."( Effects of multiple oral dosing of itraconazole on the pharmacokinetics of cyclosporine in cats.
Kamishina, H; Katayama, M; Katayama, R, 2010
)
0.36
"The purpose of this study is to compare the bioavailability of two itraconazole (CAS 84625-61-6) capsule formulations."( Bioequivalence study of two formulations of 100 mg capsule of itraconazole. Quantification by tandem mass spectrometry.
Donaduzzi, CM; dos Santos, MB; Favreto, WA; Manfio, JL; Pugens, AM; Weich, A, 2010
)
0.36
" A simple formulation of 1:2 (w/w) ITZ/HPMC-P dispersion in a capsule was compared to crystalline ITZ in a capsule in a dog bioavailability study, with the dispersion being significantly more bioavailable."( A solid-state approach to enable early development compounds: selection and animal bioavailability studies of an itraconazole amorphous solid dispersion.
Byrn, S; Campbell, C; Engers, D; Gent, P; Hossack, S; Ivanisevic, I; Jimenez-Novoa, J; Newman, A; Templeton, A; Teng, J; Thomson, J, 2010
)
0.36
" The dissolution, bioavailability in rats and stability of solid dispersions were evaluated."( Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability.
Balakrishnan, P; Choi, HG; Lee, MK; Oh, DH; Park, YJ; Xuan, JJ; Yang, HJ; Yeo, WH; Yong, CS, 2010
)
0.36
"This system is envisioned to increase bioavailability of ITZ by improving aqueous dispersibility and increasing antifungal penetration, thereby increasing antifungal activity of the entrapped drug."( Itraconazole-loaded poly(lactic-co-glycolic) acid nanoparticles for improved antifungal activity.
Damann, K; Leonardi, C; Patel, NR; Sabliov, CM, 2010
)
0.36
" Therefore, SDs obtained by MW technique using vitamin E TPGS as carrier provide a promising way to increase the dissolution rate and solubility of poorly bioavailable drugs."( Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology.
De Zordi, N; Macchiavelli, S; Moneghini, M; Princivalle, F; Solinas, D, 2010
)
0.36
"Nanosizing techniques are important tools for improving the bioavailability of water insoluble drugs."( Nanosuspensions of poorly soluble drugs: preparation and development by wet milling.
Hirvonen, J; Kiesvaara, J; Laaksonen, T; Laru, J; Liu, P; Peltonen, L; Rong, X; van Veen, B, 2011
)
0.37
"The objective of this study was to enhance the oral bioavailability of itraconazole (ITZ) with dried drug nanosuspensions."( Potent dried drug nanosuspensions for oral bioavailability enhancement of poorly soluble drugs with pH-dependent solubility.
Chen, H; Mou, D; Wan, J; Xu, H; Yang, X, 2011
)
0.37
" In particular, the analogues 30d, 30c, 31c, and 36d exhibited much higher solubility and bioavailability than that of itraconazole."( Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
Cao, X; He, H; Liu, X; Liu, Y; Liu, Z; Yang, Y, 2011
)
0.37
"Rapid flocculation of nanoparticle dispersions of a poorly water soluble drug, itraconazole (Itz), was utilized to produce amorphous powders with desirable dissolution properties for high bioavailability in rats."( Flocculated amorphous itraconazole nanoparticles for enhanced in vitro supersaturation and in vivo bioavailability.
DiNunzio, J; Johnston, KP; Ludher, BS; Matteucci, ME; Miller, MA; Williams, RO, 2012
)
0.38
" 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
)
0.37
" Fluconazole and voriconazole are well absorbed and exhibit high oral bioavailability, whereas the oral bioavailability of itraconazole and posaconazole is lower and more variable."( Triazole antifungal agents in invasive fungal infections: a comparative review.
Lass-Flörl, C, 2011
)
0.37
"The poor solubility of itraconazole (ITR) results in its variable oral absorption and bioavailability and has also proven to be a major setback in developing an efficient oral delivery system."( Preparation and cyclodextrin assisted dissolution rate enhancement of itraconazolium dinitrate salt.
Bansal, G; Jana, AK; Kumar, N; Kumar, S, 2013
)
0.39
"The objective of the present study was to enhance solubility and bioavailability of itraconazole by a combined use of membrane emulsification and spray drying solidification technique."( Enhanced solubility and oral bioavailability of itraconazole by combining membrane emulsification and spray drying technique.
Choi, HG; Choi, YK; Kim, JO; Kim, JW; Marasini, N; Poudel, BK; Yang, KY; Yong, CS, 2012
)
0.38
" This study shows the utility of an itraconazole-succinic acid cocrystal for improving itraconazole bioavailability while also demonstrating the potential for CO(2) to replace traditional liquid antisolvents in cocrystal preparation, thus making cocrystal production more environmentally benign and scale-up more feasible."( Formation of itraconazole-succinic acid cocrystals by gas antisolvent cocrystallization.
Gupta, RB; Ober, CA, 2012
)
0.38
" The PBPK modelling predicted that the bioavailability of itraconazole is likely to be increased after oral administration of ternary complex formulations, especially when itraconazole is formulated as a ternary complex comprising HP-β-CD or HBen-β-CD and Soluplus®."( Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: itraconazole.
Buchanan, CM; Dressman, JB; Klein, S; Taupitz, T, 2013
)
0.39
"Miconazole and itraconazole possess adequate membrane permeability, but only slight water solubility, which limits their bioavailability and antifungal effect."( Formulation and drying of miconazole and itraconazole nanosuspensions.
Cerdeira, AM; Gander, B; Mazzotti, M, 2013
)
0.39
" PL increased the systemic bioavailability of ITZ (determined by the AUCplasma to AUClung ratio) as a consequence of their wetting and absorption enhancement effect."( Pharmacokinetic evaluation in mice of amorphous itraconazole-based dry powder formulations for inhalation with high bioavailability and extended lung retention.
Amighi, K; Duret, C; Merlos, R; Sebti, T; Vanderbist, F; Wauthoz, N, 2014
)
0.4
" The relative bioavailability values with their 95% confidence limit were calculated to be 98."( Increased dissolution and oral absorption of itraconazole/Soluplus extrudate compared with itraconazole nanosuspension.
Lin, X; Luo, Q; Tang, X; Tian, B; Yang, S; Yu, H; Zhang, K; Zhang, Y, 2013
)
0.39
" While newer antifungal agents are now available, itraconazole is an orally bioavailable agent with broad-spectrum antifungal activity."( Itraconazole: an update on pharmacology and clinical use for treatment of invasive and allergic fungal infections.
Hope, WW; Lestner, J, 2013
)
0.39
" The low aqueous solubility hinders their clinical translations due to low bioavailability and dissolution-limited absorption of orally-administered drugs."( A nanosystem for water-insoluble drugs prepared by a new technology, nanoparticulation using a solid lipid and supercritical fluid.
Kim, KS; Lee, ES; Oh, KT; Oh, YT; Park, JW; Youn, YS; Yun, JM, 2013
)
0.39
" The SEDDS based on PEGylated bile acids provide a controlled release system with significant improvement of the bioavailability of itraconazole in rats, as demonstrated by the pharmacokinetic studies."( PEGylated bile acids for use in drug delivery systems: enhanced solubility and bioavailability of itraconazole.
Hildgen, P; Le Dévédec, F; Leclair, G; Strandman, S; Zhu, XX, 2013
)
0.39
" Due to the suppression of gastric acid secretion, they can significantly alter the intragastric pH conditions and are thus likely to affect the bioavailability of coadministered drugs requiring an acidic gastric environment for dissolution and subsequent absorption."( Mechanistic understanding of the effect of PPIs and acidic carbonated beverages on the oral absorption of itraconazole based on absorption modeling with appropriate in vitro data.
Fotaki, N; Klein, S, 2013
)
0.39
" The SNESD-loaded tablet displayed significantly increased oral bioavailability in healthy human volunteers compared with the reference Sporanox® capsule."( Formulation and in vivo human bioavailability of dissolving tablets containing a self-nanoemulsifying itraconazole solid dispersion without precipitation in simulated gastrointestinal fluid.
Choe, JS; Lee, BJ; Oh, KT; Piao, ZZ; Rhee, YS, 2014
)
0.4
"In order to investigate the influence of drug physicochemical properties on bioavailability of water insoluble drug nanosuspensions, five drug nanosuspensions were prepared using high pressure homogenization."( Influence of drug physicochemical properties on absorption of water insoluble drug nanosuspensions.
Cheng, J; Cun, D; Fang, L; Li, W; Liu, J; Quan, P; Xiang, R; Zhang, Y, 2014
)
0.4
" The in vivo study showed that the NS formulation has a similar systemic bioavailability to Sporanox® while providing a sustained plasma level (> 100 ng/mL) for up to 24 hours after intravenous administration."( Development of PLGA-based itraconazole injectable nanospheres for sustained release.
Bian, X; Hsiao, CH; John, J; Liang, D; Liang, S; Wei, X; Xie, H, 2013
)
0.39
"Our newly developed PLGA-ITZ-NS has shown great sustained release and comparable bioavailability with Sporanox®, therefore having the potential to be an alternative injectable formulation of ITZ."( Development of PLGA-based itraconazole injectable nanospheres for sustained release.
Bian, X; Hsiao, CH; John, J; Liang, D; Liang, S; Wei, X; Xie, H, 2013
)
0.39
"The aim of the study is to increase the bioavailability of itraconazole (ITRA) using nanosized cocrystals prepared via wet milling of ITRA in combination with dicarboxylic acids."( Formulation of itraconazole nanococrystals and evaluation of their bioavailability in dogs.
Adriaensens, P; Carleer, R; De Beer, T; De Smet, L; Remon, JP; Saerens, L; Van Bocxlaer, J; Vervaet, C, 2014
)
0.4
" The objective of this study was to formulate solid oral nanocrystal delivery systems of itraconazole, and thus enhance the oral bioavailability of the very poorly soluble drug."( Nanocrystal-based per-oral itraconazole delivery: superior in vitro dissolution enhancement versus Sporanox® is not realized in in vivo drug absorption.
Häkkinen, MR; Hirvonen, J; Ilkka, J; Järvinen, K; Kiesvaara, J; Kovalainen, M; Laaksonen, T; Laru, J; Oksala, O; Peltonen, L; Rönkkö, S; Sarnes, A, 2014
)
0.4
"Amorphous drug nanoparticles have recently emerged as a promising bioavailability enhancement strategy of poorly soluble drugs attributed to the high supersaturation solubility generated by the amorphous state and fast dissolution afforded by the nanoparticles."( Amorphization strategy affects the stability and supersaturation profile of amorphous drug nanoparticles.
Cheow, WS; Hadinoto, K; Kiew, TY; Yang, Y, 2014
)
0.4
" In conclusion, the nanosuspension approach is feasible to improve the oral absorption of a BCS Class II drug in a tablet formulation and capable of achieving oral bioavailability equivalent to other well established oral absorption enhancement method."( Spray drying of a poorly water-soluble drug nanosuspension for tablet preparation: formulation and process optimization with bioavailability evaluation.
Li, LC; Mao, S; Ni, R; Sun, W; Zhang, X, 2015
)
0.42
" It has a nephrotoxic effect and low bioavailability in patients who suffer from renal insufficiency, and its poor solubility in water makes ITR largely unavailable."( Bioadhesive tablets containing cyclodextrin complex of itraconazole for the treatment of vaginal candidiasis.
Açma, A; Aksu, B; Cevher, E; Mülazımoğlu, L; Sinani, G; Zloh, M, 2014
)
0.4
"Itraconazole (ITR) is an antifungal drug with a limited bioavailability due to its poor aqueous solubility."( Heat induced evaporative antisolvent nanoprecipitation (HIEAN) of itraconazole.
Mugheirbi, NA; Paluch, KJ; Tajber, L, 2014
)
0.4
" In vitro dissolution and in vivo bioavailability studies of the nano-amorphous powders were performed."( Nano-amorphous spray dried powder to improve oral bioavailability of itraconazole.
Burgess, DJ; Kumar, S; Shen, J, 2014
)
0.4
"The objectives of the present study were to formulate and optimize different sized liquid and solid nanocrystalline formulations and evaluate their in vitro and in vivo performance to determine the effect of particle size on the oral bioavailability of solid nanocrystalline formulations."( In Vitro and In Vivo Performance of Different Sized Spray-Dried Crystalline Itraconazole.
Burgess, DJ; Jog, R; Kumar, S; Sadrieh, N; Shen, J; Zolnik, B, 2015
)
0.42
" The recent approval of a solid oral tablet formulation of posaconazole with improved bioavailability and once-daily dosing has significantly improved the clinical utility of this agent."( Optimizing azole antifungal therapy in the prophylaxis and treatment of fungal infections.
Dolton, MJ; McLachlan, AJ, 2014
)
0.4
"The tunable particle size, surface charge, and favourable encapsulation efficiency with a sustained drug release profile of PLHNs suggesting that it could be promising system envisioned to increase the bioavailability by improving intestinal permeability through lymphatic uptake, M cell of payer's patch or paracellular pathway which was proven by confocal microscopy."( Formulation and optimization of itraconazole polymeric lipid hybrid nanoparticles (Lipomer) using Box Behnken design.
Dalwadi, C; Gajra, B; Patel, R, 2015
)
0.42
" In conclusion, ITZ-loaded-TPP NPs significantly improved ITZ bioavailability by increasing its aqueous dispersibility and extending the duration of drug release, thereby improving the antifungal efficacy of the ITZ agent."( Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles.
Chen, H; Hu, B; Hu, Y; Li, S; Qiu, L; Wu, X; Zheng, Y, 2015
)
0.42
" The capsular preparation often does not allow for accurate dosing, the oral solution is difficult to administer and poorly tolerated, and the bioavailability of compounded formulations has been shown to be poor in other species."( Alternate-day dosing of itraconazole in healthy adult cats.
Dirikolu, L; Kubier, A; Middleton, SM; Mitchell, MA; Papich, MG; Rubin, SI, 2016
)
0.43
"The aim of this study was to describe the pharmacokinetics and bioavailability of itraconazole (ITR) oral solution in healthy cats."( Pharmacokinetics and bioavailability of itraconazole oral solution in cats.
Cao, C; Li, W; Liang, C; Shan, Q; Wang, J; Zeng, Z; Zhang, X; Zhong, J, 2016
)
0.43
" The absolute bioavailability of ITR oral solution after oral administration was 52."( Pharmacokinetics and bioavailability of itraconazole oral solution in cats.
Cao, C; Li, W; Liang, C; Shan, Q; Wang, J; Zeng, Z; Zhang, X; Zhong, J, 2016
)
0.43
" In vivo pharmacokinetic showed significant enhancement in C max and AUC0-t with relative bioavailability of 225%."( Formulation Development of Spherical Crystal Agglomerates of Itraconazole for Preparation of Directly Compressible Tablets with Enhanced Bioavailability.
Desai, J; Fadke, J; Thakkar, H, 2015
)
0.42
"This research aimed to develop a supercritical fluid (SCF) technique for preparing a particulate form of itraconazole (ITZ) with good dissolution and bioavailability characteristics."( Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs.
Daintree, LS; Ding, S; Han, J; Ledger, DM; Qi, J; Wang, B; Wu, W; Yin, X; Zhao, W, 2015
)
0.42
"For the solubility and bioavailability of poorly soluble active pharmaceutical ingredients (APIs) to be improved, the transformation of crystalline APIs to the amorphous state has often been shown to be advantageous."( Predicting the Solubility Advantage of Amorphous Pharmaceuticals: A Novel Thermodynamic Approach.
Ji, Y; Paus, R; Sadowski, G; Vahle, L, 2015
)
0.42
" Moreover calcitriol strongly synergizes with itraconazole (ITZ) in Smo inhibition, which did not result from elevated calcitriol bioavailability due to ITZ-mediated 24-hydroxylase inhibition but rather from a direct interaction of the compounds at the level of Smo."( A Functional and Putative Physiological Role of Calcitriol in Patched1/Smoothened Interaction.
Adamski, J; Dittmann, K; Hahn, H; Linder, B; Uhmann, A; Weber, S, 2015
)
0.42
" 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
)
0.42
"Itraconazole (ITR), an antifungal agent has poor bioavailability due to low aqueous solubility."( Formulation and evaluation of Itraconazole nanoemulsion for enhanced oral bioavailability.
Dhande, RD; Khunt, A; Patel, AA; Thakkar, HP, 2015
)
0.42
" Due to the unique attributes of the KinetiSol® dispersing (KSD) technology, PVAL has been enabled for this application and it is the aim of this paper to investigate various grades for improvement of the solubility and bioavailability of poorly water soluble active pharmaceutical ingredients."( Use of Polyvinyl Alcohol as a Solubility-Enhancing Polymer for Poorly Water Soluble Drug Delivery (Part 1).
Brough, C; Keen, JM; Kucera, SA; Lubda, D; Miller, DA; Williams, RO, 2016
)
0.43
" Our previous study revealed that the 88% hydrolyzed grade of PVAL was optimal for itraconazole (ITZ) amorphous compositions with regard to solid-state properties, non-sink dissolution performance, and bioavailability enhancement."( Use of Polyvinyl Alcohol as a Solubility Enhancing Polymer for Poorly Water-Soluble Drug Delivery (Part 2).
Brough, C; Ellenberger, D; Lubda, D; Miller, DA; Williams, RO, 2016
)
0.43
"A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug."( Biodegradable Porous Starch Spheres as a Novel Carrier for Enhancement of Dissolution Rate and Oral Bioavailability of Itraconazole.
Ali, MT; Amin, P; Fule, R; Moravkar, K; Pawar, J; Sathaye, S; Seervi, M, 2017
)
0.46
" A proof of concept study showed that the optimized method is applicable to test the bioavailability of drug formulations containing ITZ."( Sampling only ten microliters of whole blood for the quantification of poorly soluble drugs: Itraconazole as case study.
Evrard, B; Fillet, M; Kok, MGM; Nys, G; Thiry, J, 2017
)
0.46
" When compared to the single cannulation approach, clearance, volume of distribution and bioavailability determined by dual cannulation were 39%, 60% and 38% higher for itraconazole, and 46%, 34% and 42% higher for amiodarone, respectively."( Single jugular vein cannulated rats may not be suitable for intravenous pharmacokinetic screening of high logP compounds.
Gaud, N; Holenarsipur, VK; Kole, P; Kumar, A; Mandlekar, S; Matta, M; Sridhar, S, 2017
)
0.46
" Ethylcellulose (EC) coated and uncoated minitablets prepared with the 30% drug load dispersion were delivered orally to rats and exhibited sustained release characteristics, with overall bioavailability greater for the uncoated minitablets compared to the EC-coated minitablets, similar to the rank order observed in our in vitro dissolution experiments."( Mucoadhesive amorphous solid dispersions for sustained release of poorly water soluble drugs.
LaFountaine, JS; McGinity, JW; Miller, DA; Prasad, LK; Williams, RO, 2017
)
0.46
" When Sporanox and itraconazole/AFFINISOL High Productivity HPMCAS SDDs were dosed in rats, the maximum absorption rate for each formulation rank-ordered with membrane flux in vitro."( Impact of Drug-Rich Colloids of Itraconazole and HPMCAS on Membrane Flux in Vitro and Oral Bioavailability in Rats.
Brodeur, TJ; Friesen, DT; Goodwin, AK; Grass, ME; Morgen, MM; Stewart, AM; Vodak, DT, 2017
)
0.46
" However, marked differences in bioavailability have been reported in other species."( Pharmacokinetics and Relative Bioavailability of Orally Administered Innovator-Formulated Itraconazole Capsules and Solution in Healthy Dogs.
Hasbach, AE; Langlois, DK; Papich, MG; Rosser, EJ, 2017
)
0.46
"The mean relative bioavailability of the capsule was 85% that of the solution, but drug absorption was variable, and overall drug concentrations were similar between formulations."( Pharmacokinetics and Relative Bioavailability of Orally Administered Innovator-Formulated Itraconazole Capsules and Solution in Healthy Dogs.
Hasbach, AE; Langlois, DK; Papich, MG; Rosser, EJ, 2017
)
0.46
" Its variable and unpredictable oral bioavailability make it difficult to determine the optimal dosing regimen."( Pharmacokinetic evaluation of oral itraconazole for antifungal prophylaxis in children.
Allegra, S; Carcieri, C; Cusato, J; D'Avolio, A; De Francia, S; De Nicolò, A; Di Perri, G; Fatiguso, G; Favata, F; Pirro, E, 2017
)
0.46
"Solid dispersion formulations have attracted attention to improve solubility and bioavailability of water-insoluble drugs."( Characterization and pharmacokinetic study of itraconazole solid dispersions prepared by solvent-controlled precipitation and spray-dry methods.
Choi, HG; Choi, S; Kang, W; Kim, DW; Kim, KS; Kim, M; Kim, Y; Lee, ES; Lee, JW; Lim, C; Oh, KT; Sim, T, 2017
)
0.46
" After the oral administration of crystalline ITZ to high-fat meal-fed rats, the oral bioavailability of ITZ was 14-fold higher than that in fasted rats."( Avoidance of food effect on oral absorption profile of itraconazole by self-micellizing solid dispersion approach.
Kobayashi, K; Kojo, Y; Matsunaga, S; Onoue, S; Sato, H; Seto, Y; Suzuki, H, 2017
)
0.46
"Itraconazole is a fungicide drug which has low bioavailability due to its poor water solubility."( Application of hydroxypropyl methylcellulose as a protective agent against magnesium stearate induced crystallization of amorphous itraconazole.
Balogh, A; Démuth, B; Farkas, A; Galata, DL; Hirsch, E; Marosi, G; Mensch, J; Nagy, B; Nagy, ZK; Pataki, H; Szabó, E; Verreck, G; Vigh, T, 2018
)
0.48
" A newer formulation of oral itraconazole with improved bioavailability was commenced."( Treatment of disseminated histoplasmosis in advanced HIV using itraconazole with increased bioavailability.
Cronin, K; Mangalore, RP; McMahon, JH; Moso, MA; Young, K, 2018
)
0.48
" Areas covered: A detailed analysis of the manufacturing process of itraconazole with emphasis on pelletization and parameters affecting the dissolution and bioavailability is presented."( Parameters that determine dissolution and efficacy of itraconazole and its relevance to recalcitrant dermatophytoses.
Gupta, A; Khurana, A; Sardana, K, 2019
)
0.51
" These findings may be useful for improving the bioavailability of several drugs by effective absorption from the upper small intestine, with floating gastric retention system."( Fabrication of Zero-Order Sustained-Release Floating Tablets via Fused Depositing Modeling 3D Printer.
Ishikawa, T; Itai, S; Iwao, Y; Kimura, SI; Kondo, H, 2019
)
0.51
"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
"The oral bioavailability of ibrutinib is low and variable, mainly due to extensive first-pass metabolism by cytochrome P450 (CYP) 3A4."( Itraconazole Increases Ibrutinib Exposure 10-Fold and Reduces Interindividual Variation-A Potentially Beneficial Drug-Drug Interaction.
Backman, JT; Elonen, E; Neuvonen, M; Neuvonen, PJ; Niemi, M; Olkkola, AM; Tapaninen, T; Tornio, A, 2020
)
0.56
" ITR has an unpredictable bioavailability and quality variation among brands is known to affect clinical outcome."( An exploratory pilot analysis of the optimal pellet number in 100 mg of itraconazole capsule to maximize the surface area to satisfy the Noyes-Whitney equation.
Khurana, A; Panesar, S; Sardana, K; Singh, A, 2021
)
0.62
"0 L and the bioavailability (F) was 81."( Multicenter-Based Population Pharmacokinetic Analysis of Ciclosporin in Hematopoietic Stem Cell Transplantation Patients.
Ding, XL; Liu, LN; Miao, LY; Tian, JX; Xue, L; Yan, HH; Zhang, JJ; Zhang, WJ; Zhang, WW, 2019
)
0.51
" An absolute bioavailability study informed the hepatic and gastric availability."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
" Since ITZ is only weakly soluble in water, its bioavailability is limited."( Cholesterol Reduces Partitioning of Antifungal Drug Itraconazole into Lipid Bilayers.
Bunker, A; Dzieciuch-Rojek, M; Kepczynski, M; Poojari, C; Róg, T; Zak, A, 2020
)
0.56
"Molibresib (GSK525762), an orally bioavailable small molecule with 2 major equipotent active metabolites, is being developed for the treatment of cancers."( An Adaptive Physiologically Based Pharmacokinetic-Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers.
Collins, G; Ferron-Brady, G; Kremer, BE; Patel, A; Riddell, K; Schramek, D; Zhou, Y, 2021
)
0.62
" A formulation of 'SUper BioAvailability itraconazole' (SUBA-itraconazole; Lozanoc®) has been developed, with adult studies demonstrating rapid and reliable attainment of therapeutic levels, yet paediatric data are lacking."( Clinical experience with SUBA-itraconazole at a tertiary paediatric hospital.
Abbotsford, J; Blyth, CC; Bowen, AC; Foley, DA; Goff, Z; Yeoh, DK, 2021
)
0.62
"Spray dried dispersions (SDDs) have the potential to dramatically improve the oral bioavailability of drugs with poor water solubility."( The effects of spray drying, HPMCAS grade, and compression speed on the compaction properties of itraconazole-HPMCAS spray dried dispersions.
Alayoubi, A; Ashraf, M; Das, S; Feng, X; Hoag, SW; Honick, M; Muller, FX; Polli, JE; Zidan, A, 2020
)
0.56
"Nadolol is a hydrophilic and nonselective β-adrenoceptor blocker with a bioavailability of 30%, relatively longer half-life, negligible metabolism, and predominant renal excretion."( Urinary Excretion of Nadolol as a Possible In Vivo Probe for Drug Interactions Involving P-Glycoprotein.
Kuroda, J; Misaka, S; Shimazaki, S; Shimomura, K, 2021
)
0.62
" The current standard treatment by systemic administration is limited by inadequate local bioavailability and systemic toxic effects."( Inhaled Antifungal Agents for the Treatment and Prophylaxis of Pulmonary Mycoses.
Lam, JKW; Liao, Q, 2021
)
0.62
" Our center has recently changed from posaconazole to a highly bioavailable formulation of itraconazole (SUBA®-itraconazole) at substantially reduced cost, but safety and toxicity require further assessment."( A novel highly bio-available itraconazole formulation (SUBA®-Itraconazole) for anti-fungal prophylaxis in lung transplant recipients.
Boan, P; Lavender, M; Musk, M; Whitmore, TJ; Wrobel, J; Yaw, M, 2021
)
0.62
" This model was built based on physiochemical data and clinical in vivo drug-drug interaction (DDI) studies with itraconazole and fluconazole, and verified against data from an in vivo rifampicin DDI study and an absolute bioavailability study."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
0.62
" Itraconazole, a broad-spectrum tri azole antifungal agent, is poorly absorbed in the intestines after oral absorption and makes it difficult to achieve a stable serum drug concentration."( Efficacy of Intravenous Itraconazole Versus Liposomal Amphotericin B as Empirical Antifungal Therapy in Hematological Malignancy with Persistent Fever and Neutropenia: Study Protocol for a Multicenter, Prospective, Randomized Non-inferiority Trial.
Hidaka, M; Kaneko, Y; Miyazaki, Y; Nagai, H; Saito, AM; Sawamura, M; Tanaka, S; Uike, N; Yoshida, I; Yoshida, S, 2021
)
0.62
" The comparison of the in vitro data with published in vivo data revealed that the model successfully predicted the effect of food intake as well as of modified gastric pH conditions on the bioavailability of itraconazole from this formulation."( Application of tiny-TIM as a mechanistic tool to investigate the in vitro performance of different itraconazole formulations under physiologically relevant conditions.
Fischer, PL; Koziolek, M; Lenz, V; López Mármol, Á; Sauer, K; Schwöbel, D; Wahl, A, 2022
)
0.72
" We report a case of a woman in fifties with post-COVID-19 respiratory failure who successfully underwent lung transplantation, followed by improved bioavailability of ITCZ tablets when given with acidic lemon beverages."( Improved absorption of itraconazole tablet by co-administration with lemon beverages in a lung transplant recipient: A case report.
Date, H; Katada, Y; Matsumura, K; Nagao, M; Nakagawa, S; Ohsumi, A; Sugimoto, M; Terada, T; Umemura, K; Yonezawa, A, 2022
)
0.72
"Solubility and dissolution rate are essential for the oral absorption and bioavailability of poorly soluble drugs."( Combination of co-crystal and nanocrystal techniques to improve the solubility and dissolution rate of poorly soluble drugs.
Bodmeier, R; Huang, Z; Staufenbiel, S, 2022
)
0.72
" There is a scarcity of studies on the bioavailability of various itraconazole brands available in the market."( Correlation of plasma levels of itraconazole with treatment response at 4 weeks in chronic dermatophytosis: Results of a randomised controlled trial.
Bhalavi, H; Dogra, S; Mehta, H; Narang, T; Rudramurthy, SM; Sachdeva, N; Shafiq, N; Shaw, D, 2023
)
0.91
" Plasma levels of the three drugs were however similar, indicating that factors other than serum bioavailability are at play in determining response of chronic dermatophyte infections to oral itraconazole."( Correlation of plasma levels of itraconazole with treatment response at 4 weeks in chronic dermatophytosis: Results of a randomised controlled trial.
Bhalavi, H; Dogra, S; Mehta, H; Narang, T; Rudramurthy, SM; Sachdeva, N; Shafiq, N; Shaw, D, 2023
)
0.91
"The current study aimed to improve the processability and oral bioavailability of itraconazole (ITZ) via spherical agglomeration."( Processability and Oral Bioavailability Improvement of Itraconazole by Particle Engineering Technique.
Kapalatiya, H; Patel, D; Singh, AD; Wairkar, S, 2022
)
0.72
" In this work, AmB and ITR have been formulated within granules to elicit an enhanced pharmacological effect, while enhancing the oral bioavailability of AmB."( Can amphotericin B and itraconazole be co-delivered orally? Tailoring oral fixed-dose combination coated granules for systemic mycoses.
Bolás-Fernández, F; Chamorro-Sancho, MJ; Fernández-García, R; Healy, AM; Jiménez-Cebrián, A; O'Connell, P; Paloma Ballesteros, M; Raposo, R; Serrano, DR; Slowing, K; Walsh, D, 2023
)
0.91
"Solubility of the drug is an important property of the drug as it affects the release, absorption, dissolution rate and ultimately bioavailability of the drug."( Comparative assessment of solubility enhancement of itroconazole by solid dispersion and co-crystallization technique: Investigation of simultaneous effect of media composition on drug dissolution.
Barethiya, V; Dixit, G; Hiradeve, S; Kale, S; Karodadeo, GR; Kohale, N; Kumar, V; Lahane, A; Rajbhar, K; Rarokar, NR; Thakre, V, 2023
)
0.91
"Along with the increasing demand for candidate-enabling formulations comes the need for appropriate in vitro bioavailability forecasting."( In vitro dissolution/permeation tools for amorphous solid dispersions bioavailability forecasting I: Experimental design for PermeaLoop™.
Bauer-Brandl, A; Brandl, M; Henriques, J; Nunes, PD; Paiva, AM; Pinto, JF, 2023
)
0.91
"Esaxerenone was estimated to have high bioavailability (85."( Population pharmacokinetics of esaxerenone, a novel non-steroidal mineralocorticoid receptor blocker, in patients with essential hypertension, patients with diabetic nephropathy, and healthy volunteers.
Fukae, M; Ishizuka, H; Kastrissios, H; Shimizu, T; Wada, R; Yoshihara, K, 2023
)
0.91
" Super bioavailability (SUBA) itraconazole was initially not tolerated."( [Recurrent tinea corporis generalisata due to Terbinafine-resistant Trichophyton rubrum strain : Long-term treatment with super bioavailability itraconazole].
Burmester, A; Ebert, A; Monod, M; Nenoff, P; Schaller, M; Stahl, M; Uhrlaß, S, 2023
)
0.91
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" In particular, the analogues 30d, 30c, 31c, and 36d exhibited much higher solubility and bioavailability than that of itraconazole."( Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
Cao, X; He, H; Liu, X; Liu, Y; Liu, Z; Yang, Y, 2011
)
0.84
" Moreover, pharmacokinetic studies in SD rats showed that A33 exhibited favourable pharmacokinetic properties, with a bioavailability of 77."( Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
Cheng, M; Su, X; Sun, N; Sun, Y; Tian, L; Yin, W; Zhang, C; Zhao, D; Zhao, L; Zhao, S; Zheng, Y, 2021
)
0.62
" Moreover, pharmacokinetic studies in SD rats showed that compound 22a exhibited pharmacokinetic properties with a bioavailability of 15."( Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
Cheng, M; Cui, H; Jiang, H; Liu, L; Su, X; Sun, Y; Wu, T; Yin, W; Zhang, Y; Zhao, D; Zhao, L, 2022
)
0.72

Dosage Studied

The poorly water-soluble compound, itraconazole (ITZ), was selected for the development of an immediate-release oral dosage form. The study was to assess the feasibility of a multicompartmental in vitro dissolution apparatus, gastrointestinal simulator.

ExcerptRelevanceReference
" Cure of the toenails was observed in 79% of the patients treated with the 200 mg dosage and in 26% of those treated with 100 mg at 6 months after therapy."( Posttreatment itraconazole levels in the nail. New implications for treatment in onychomycosis.
Cauwenbergh, G; De Doncker, P; Heykants, J; Roseeuw, D; Van Cutsem, J; Van de Velde, V; Willems, J; Willemsen, M; Woestenborghs, R, 1992
)
0.28
" The proper duration and dosage and the combination of antifungal drugs have not been clearly defined."( [Primary Aspergillus endocarditis. Apropos of a case and review of the international literature].
Cajot, MA; Gosselin, B; Goullard, L; Koussa, A; Marquette, F; Pol, A; Roux, JP; Soots, G; Warembourg, H, 1992
)
0.28
" In this open non-comparative clinical trial, itraconazole was given orally in the dosage of 100 mg per day for 14 consecutive days."( Treatment of dermatophytosis with new systemic antifungal agent, itraconazole.
Noppakun, N; Phuphaibool, K, 1992
)
0.28
" Liposomal Amphotericin B allowing higher dosage by lower toxicity appears effective as salvage treatment especially in aspergillosis which also responds to Itraconazole available as oral formulation so far."( Antifungal treatment strategy in leukemia patients.
Büchner, T; Roos, N, 1992
)
0.28
" In vivo, subchronic intraperitoneal dosing with 40 mg/kg ketoconazole or itraconazole to mice had no effect on the antibody response to SRBC as measured by the number of splenic IgM and IgG plaque-forming cells and did not significantly affect the DTH response to oxazolone."( Lack of immunosuppression by ketoconazole and itraconazole.
Aerts, F; Cools, M; Van Wauwe, J, 1992
)
0.28
" Patients were classified in terms of severity and received itraconazole at the dosage of 200 to 400 mg per day until previously described criteria of cure have been reached."( Itraconazole in the treatment of chromoblastomycosis due to Fonsecaea pedrosoi.
Bordignon, GF; Cauwenbergh, G; Fillus, JN; Lameira, RP; Purim, KS; Queiroz-Telles, F; Van Cutsem, J, 1992
)
0.28
" The trial also aimed at a possible improvement of the therapy of toxoplasmosis in regard to safety and dosing easiness."( [Itraconazole action on Toxoplasma gondii].
Amato Neto, V; Braz, LM; Camargo, ME; Jamra, LM,
)
0.13
" However, 600 mg/day may be approaching the upper limits of acceptable dosing for long-term treatment."( High-dose itraconazole in the treatment of severe mycoses.
Dunn, JF; Fetchick, RJ; Graybill, JR; Hardin, TC; Rinaldi, MG; Sharkey, PK, 1991
)
0.28
" In those treated for two months or longer, the mean total serum IgE level fell from 2,462 U/ml (CI, 752 to 4,202 U/ml) to 502 U/ml (CI, 123 to 880 U/ml) during each course, and the mean daily steroid dosage was decreased to a mean of 24 mg/day (CI, 11 to 37 mg/day)."( Adjunctive therapy of allergic bronchopulmonary aspergillosis with itraconazole.
Denning, DW; Lewiston, NJ; Stevens, DA; Van Wye, JE, 1991
)
0.28
" However, the wide variation within and between patients suggests that an ITRA-PEL dosage of 400 mg/day may ensure earlier and more consistent therapeutic levels."( Comparison of the multiple dose pharmacokinetics of two formulations of itraconazole during remission induction for acute myeloblastic leukaemia.
Bradford, CR; Copplestone, JA; Prentice, AG; Warnock, DW, 1991
)
0.28
" The concentrations of itraconazole that reversed drug resistance are comparable to the plasma levels achieved by therapeutic dosage used in the treatment of fungal infections."( Reversal of daunorubicin resistance in P388/ADR cells by itraconazole.
Gollapudi, S; Gupta, S; Kim, J, 1991
)
0.28
" The same results could not be achieved with the same concentration or dosage of either ketoconazole or fluconazole."( Oral and parenteral treatment with itraconazole in various superficial and systemic experimental fungal infections. Comparisons with other antifungals and combination therapy.
Van Cutsem, J, 1990
)
0.28
" The feasibility of one-day therapy was assessed in a clinical study in which three different dosage regimens were compared in a total of 552 patients with acute vulvovaginal candidosis: 200 mg twice daily for one day; 200 mg once daily for two days; and 200 mg once daily for three days."( Itraconazole: a single-day oral treatment for acute vulvovaginal candidosis.
Wesel, S, 1990
)
0.28
" The fixed schedules indicated by pharmacokinetics and clinical studies are one 100 mg capsule daily for 15 days in cases of tinea corporis and tinea cruris and the same dosage for 30 days in cases of tinea pedis and tinea manuum."( Itraconazole in common dermatophyte infections of the skin: fixed treatment schedules.
Bonifaz, A; Saul, A, 1990
)
0.28
" In order to prevent a mycotic infection in these immunocompromised patients, itraconazole, a new broad-spectrum antimycotic drug of the azole group, was given in an oral dosage of 100 mg day-1 (mean duration of prophylactic treatment 24 months)."( Prophylaxis of fungal infections with itraconazole in immunocompromised cancer patients.
König, HJ; Mühldorfer, SM, 1990
)
0.28
" Treatment of invasive aspergillosis required a higher dosage (about 5 mg/kg) and prolonged administration."( Experience with itraconazole in cryptococcosis and aspergillosis.
Almaviva, M; Cristina, S; De Maria, R; Ferrazzi, P; Fiocchi, R; Langer, M; Negri, C; Scoccia, S; Tortorano, AM; Viviani, MA, 1989
)
0.28
"We have studied the influence of food and dose (50, 100, 200 mg) on the oral systemic availability of the broad spectrum antifungal itraconazole and the pharmacokinetics after repeated dosing of 100 mg in six healthy volunteers."( The effects of food and dose on the oral systemic availability of itraconazole in healthy subjects.
Gasparini, R; Gauwenbergh, G; Heykants, J; Van Peer, A; Woestenborghs, R, 1989
)
0.28
" There is a clear need to obtain quick information on itraconazole plasma levels in order to adapt dosage during prophylactic treatment in immunocompromised patients."( Antifungal prophylaxis with itraconazole in prolonged neutropenia: correlation with plasma levels.
Boogaerts, MA; De Beule, K; Demuynck, H; Verbist, L; Verhoef, GE; Zachee, P, 1989
)
0.28
" Two dosage regimens were tested--200 mg twice a day for 1 day and 200 mg twice a day for 2 days."( Itraconazole in the treatment of acute vaginal candidiasis.
Barnard, PG; Bloch, B; Burger, GD; Meyer, JS; Parkes, JR; Smythe, E, 1988
)
0.27
" This study could not demonstrate any significant effect of renal dysfunction and hemodialysis or continuous ambulatory peritoneal dialysis treatment upon the pharmacokinetics of itraconazole, and firm conclusions concerning dosing in such patients should await confirmation of our data in a larger patient population."( Itraconazole pharmacokinetics in patients with renal dysfunction.
Boelaert, J; Daneels, R; De Beule, K; Heykants, J; Matthys, E; Schurgers, M; van Peer, A; Woestenborghs, R, 1988
)
0.27
"Male Wistar rats were dosed with miconazole, ketoconazole and itraconazole by gastric intubation once daily for up to 7 days."( Induction potential of antifungals containing an imidazole or triazole moiety. Miconazole and ketoconazole, but not itraconazole are able to induce hepatic drug metabolizing enzymes of male rats at high doses.
Heykants, J; Lavrijsen, K; Meuldermans, W; Thijs, D; Van Houdt, J, 1986
)
0.27
" The pharmacologic profiles, mechanisms of action, pharmacokinetics, clinical indications for use, dosage recommendations, side effects, and drug interactions for these agents are presented."( The pharmacology of agents used in the treatment of pulmonary mycoses.
Borgers, M; Cauwenbergh, G; Vanden Bossche, H, 1986
)
0.27
" It appears that a dosage of 50 mg of itraconazole daily is not adequate for the treatment of these mycoses."( Itraconazole in the treatment of superficial mycoses: an open trial of 40 cases.
Arias, I; Bonifáz, A; Saúl, A,
)
0.13
" Since the larger dosage induces a faster response, it should be evaluated further."( Itraconazole in the treatment of dermatophytoses: a comparison of two daily dosages.
Borghys, A; De Veylder, H; Degreef, H; Duprez, K; Mariën, K; Verhoeve, L,
)
0.13
" The dosage was 100 mg daily for four to six weeks."( Itraconazole in the treatment of tinea corporis: a pilot study.
Nuijten, ST; Schuller, JL,
)
0.13
" The difference between these rates was not significant, but the groups were small and the difference in dosage may ultimately be meaningful in terms of rates of cure."( Itraconazole in pityriasis versicolor.
Estrada, RA,
)
0.13
" The sexual partners of one-half of the women were treated with the same dosage of itraconazole; the other men received placebo."( Itraconazole in the treatment of vaginal candidosis and the effect of treatment of the sexual partner.
Calderón-Márquez, JJ,
)
0.13
" Almost 50% were women with vaginal candidosis; a dosage of 200 mg per day for three days appeared to be optimal for their treatment."( Itraconazole in the treatment of human mycoses: review of three years of clinical experience.
Cauwenbergh, G; De Dier, AM; De Doncker, P; Goyvaerts, H; Schuermans, V; Stoops, K,
)
0.13
" Itraconazole was administered at a daily dosage of 50 mg for six months in the majority of these cases."( Oral treatment of paracoccidioidomycosis and histoplasmosis with itraconazole in humans.
Galimberti, RL; Koren, F; Negroni, R; Palmieri, O; Tiraboschi, IN,
)
0.13
" Dosage was 100-200 mg per day, and duration of treatment was based on response."( Itraconazole for deep mycoses: preliminary experience in Mexico.
De Ovando, F; Lavalle, P; Reynoso, S; Suchil, P,
)
0.13
" We used the Michaelis-Menten model for calculating dosing rates under steady-state conditions."( [Therapeutic drug monitoring of itraconazole--a report of experiences].
Kreutzberg, S; Lampe, D; Prümke, HJ, 1994
)
0.29
" With oral itraconazole at a dosage of 100 mg d(-1) for 15 months (total dose 45."( Successful treatment of chromoblastomycosis with itraconazole.
Yu, R,
)
0.13
" In all cases, increasing the itraconazole dosage increased its prophylactic efficacy."( Prophylaxis of Candida and Aspergillus infections with oral administration of itraconazole.
Van Cutsem, J,
)
0.13
" Well-defined dose-response curves reflecting impairment of mitochondrial function by the antifungal agents were obtained."( Susceptibility testing of Candida albicans and Aspergillus species by a simple microtiter menadione-augmented 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay.
Bhakdi, S; Jahn, B; Martin, E; Stueben, A, 1995
)
0.29
" Thus serum concentrations of itraconazole suitable for antifungal prophylaxis can be attained in neutropenic patients, with the administration of an oral solution in a dosage of 5 mg/kg as either an od or bd schedule, following pre-autograft high-dose cytotoxic chemotherapy."( Multiple dose pharmacokinetics of an oral solution of itraconazole in autologous bone marrow transplant recipients.
Johnson, SA; Oliver, DA; Phillips, MJ; Prentice, AG; Warnock, DW, 1994
)
0.29
" Amphotericin B is often considered as the gold standard treatment despite its high toxicity particularly with high dosage (1-1."( [Curative treatment of invasive aspergillosis].
Dupont, B, 1994
)
0.29
" 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
" Itraconazole was given at a dosage of 200-400 mg day-1 for periods ranging from 14 to 488 days."( Itraconazole in the treatment of aspergillosis: a study of 16 cases.
Ambroise-Thomas, P; Brion, JP; Bru, JP; Delormas, P; Goût, JP; Lebeau, B; Michallet, M; Pelloux, H; Pinel, C; Pison, C,
)
0.13
"Nail surfaces of toe-nail fragments were analysed by optical profilometry in patients treated with two different dosages of itraconazole: 200 mg continuous dosing for 12 weeks, or a pulse-dose regimen of 1 week per month of 400 mg itraconazole daily for 3-4 months."( Acquired nail beading in patients receiving itraconazole--an indicator of faster nail growth? A study using optical profilometry.
Doncker, PD; Pierard, GE, 1994
)
0.29
" Twelve healthy male volunteers received each of 4 dosing regimens: 200 mg itraconazole alone, 200 mg itraconazole and famotidine, 100 mg fluconazole alone, and 100 mg fluconazole and famotidine."( Short report: the absorption of fluconazole and itraconazole under conditions of low intragastric acidity.
Hudson, M; Lim, SG; Pounder, RE; Sawyerr, AM; Sercombe, J, 1993
)
0.29
" Delayed-type hypersensitivity (DTH) reaction to SRBC, phagocyte activity and circulating leukocytes also were significantly decreased in mice dosed at 40 and 80 mg/kg ICZ."( The effects of itraconazole on the immune responses in ICR mice.
Ahn, YK; Kim, JH, 1994
)
0.29
" In the treatment of allergic bronchopulmonary aspergillosis, itraconazole has been reported to prompt a reduction in corticosteroid dosage in selected patients."( Treatment of aspergillosis with itraconazole.
Hardin, TC; Jennings, TS, 1993
)
0.29
" Consistent therapy with itraconazole (Sempera) dosed at 3 mg/kg body weight per day over a period of 4 weeks led to a permanent cure."( [Trichophyton soudanense as the pathogen of tinea corporis et capitis].
Bröcker, EB; Ebert, J; Schwinn, A; Wever, S, 1995
)
0.29
" Shorter, higher dosage itraconazole treatment regimens (200 or 400 mg/day for 1 week) are also beneficial in dermatomycoses."( Itraconazole. A reappraisal of its pharmacological properties and therapeutic use in the management of superficial fungal infections.
Bryson, HM; Goa, KL; Haria, M, 1996
)
0.29
"Blood samples were obtained for pharmacokinetic analyses immediately before dosing and at regular intervals up to 96 hours after each dose."( Effect of food on the pharmacokinetics of a new hydroxypropyl-beta-cyclodextrin formulation of itraconazole.
Cauwenbergh, GF; De Beule, KL; Heykants, JJ; Van de Velde, VJ; Van Peer, AP; Van Rooy, P; Woestenborghs, RJ,
)
0.13
" The fact that the solution was also well tolerated and was not associated with clinically significant changes in any laboratory value further underscores the potential utility of this dosing form."( Effect of food on the pharmacokinetics of a new hydroxypropyl-beta-cyclodextrin formulation of itraconazole.
Cauwenbergh, GF; De Beule, KL; Heykants, JJ; Van de Velde, VJ; Van Peer, AP; Van Rooy, P; Woestenborghs, RJ,
)
0.13
" 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
" The dependence of this interaction on the time interval of their ingestion and the possibility of avoiding the interaction by a correct daily dosing was studied."( The effect of ingestion time interval on the interaction between itraconazole and triazolam.
Neuvonen, PJ; Olkkola, KT; Varhe, A, 1996
)
0.29
" A sensitivity analysis assessing alternative dosing regimens and a rank order stability analysis investigating the effects of length of treatment, success rates, relapse rates, and drug acquisition costs on overall results were also conducted."( Pharmacoeconomic analysis of oral therapies for onychomycosis: a US model.
Marchetti, A; McGhan, WF; Neugut, AI; Piech, CT; Smith, BT,
)
0.13
" More studies should be performed to determine the most appropriate dosage and the optimal duration of itraconazole treatment in children."( Disseminated histoplasmosis in children: the role of itraconazole therapy.
Arango, M; Espinal, D; Franco, L; Gómez, I; Restrepo, A; Tobón, AM; Trujillo, H, 1996
)
0.29
" One patient was given a lower dosage of 100 mg, one capsule daily."( Itraconazole therapy for onychomycosis: case reports.
Kirshbaum, BA, 1996
)
0.29
" These observations suggest that itraconazole intermittent dosing is a highly effective therapy for the treatment of onychomycosis caused by dermatophyte organisms, because it provides a high cure rate after only a short course of therapy."( Treatment of onychomycosis and tinea pedis with intermittent itraconazole therapy.
Del Rosso, JQ, 1996
)
0.29
" Firstly, the purpose of the study, the comparator drugs, their dosage regimens and the time frame of the analysis were defined."( Economic evaluation of antifungal agents in the treatment of toenail onychomycosis in Germany.
De Doncker, P; Dubois, DJ; Eggleston, A; Gupta, AK; Haneke, E; Tormans, G; Van Doorslaer, EK; Van Rossem, K, 1996
)
0.29
" Complete healing was achieved after re-treatment with itraconazole for 20 weeks at the same dosage in combination with topical amorolfine and local hyperthermia."( [Diagnosis, clinical aspects and therapy of early chromoblastomycosis in a case example].
de Hoog, GS; Gründer, K; Köhn, FM; Mayser, P; Qadripur, S; Schill, WB, 1996
)
0.29
"We treated 36 patients with this drug given as continuous dosing (100 or 200 mg/ day) for 6 to 20 weeks or as a 1-week pulse dosing (200 mg twice daily for 1 week per month) for two to four pulses."( Itraconazole therapy is effective for pedal onychomycosis caused by some nondermatophyte molds and in mixed infection with dermatophytes and molds: a multicenter study with 36 patients.
Baran, RL; De Doncker, PR; Decroix, J; Degreef, HJ; Gupta, AK; Havu, V; Piérard, GE; Roseeuw, DI; Rosen, T; Scher, RK, 1997
)
0.3
"Our purpose was to compare the effectiveness and tolerability of intermittent dosing of itraconazole ("pulse therapy") with placebo in fingernail onychomycosis."( A multicenter, placebo-controlled, double-blind study of intermittent therapy with itraconazole for the treatment of onychomycosis of the fingernail.
Aly, R; Daniel, CR; DeVillez, R; Elewski, BE; Jacko, M; Moskovitz, BL; Odom, RB; Oleka, N; Scher, RK; Zaias, N, 1997
)
0.3
" To assess plasma and tissues concentrations after oral dosing in reptiles, a 23."( Itraconazole plasma and tissue concentrations in the spiny lizard (Sceloporus sp.) following once-daily dosing.
Alvarado, TP; Bennett, CL; Gamble, KC, 1997
)
0.3
"To determine the disposition of itraconazole in cats after single IV and oral dosing (as a solution or capsule) and multiple oral (capsule) dosing, and to establish bioavailability after oral administration of the solution."( Itraconazole disposition after single oral and intravenous and multiple oral dosing in healthy cats.
Boothe, DM; Calvin, J; Dvorak, J; Herring, I; Way, N, 1997
)
0.3
" For the multiple oral dosing study, MRT (at last dose: 81."( Itraconazole disposition after single oral and intravenous and multiple oral dosing in healthy cats.
Boothe, DM; Calvin, J; Dvorak, J; Herring, I; Way, N, 1997
)
0.3
"The oral itraconazole solution is preferred to capsules; a 24-hour dosing interval should be sufficient; 10 mg/kg given daily should generate therapeutic concentrations in most cats; steady-state concentrations may take up to 3 weeks to achieve; and cats appear to tolerate itraconazole well."( Itraconazole disposition after single oral and intravenous and multiple oral dosing in healthy cats.
Boothe, DM; Calvin, J; Dvorak, J; Herring, I; Way, N, 1997
)
0.3
" Increased duration and/or dosage improved the efficacy of nikkomycin Z, with 10 days of each dose curing 50 to 90% of the animals."( Efficacy of nikkomycin Z against experimental pulmonary blastomycosis.
Clemons, KV; Stevens, DA, 1997
)
0.3
"For tinea pedis and manuum, the recommended dosage is itraconazole 200 mg twice daily for 1 week (n = 220)."( Itraconazole pulse therapy for onychomycosis and dermatomycoses: an overview.
Doncker, PD; Gupta, AK; Heremans, A; Marynissen, G; Stoffels, P, 1997
)
0.3
") 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
" ITZ treatment was continued again at the same dosage for 3 months until the antigen titer was negative (< 8)."( A case of feline cryptococcosis treated with itraconazole.
Hasegawa, A; Kano, R; Nakamura, Y; Tsujimoto, H; Watari, T, 1997
)
0.3
" After 14 days, each subject was given the dosage form that he or she did not previously receive, and testing was repeated."( Relative bioavailability of itraconazole from an extemporaneously prepared suspension and from the marketed capsules.
Bowman, JL; Buice, RG; Christensen, KJ; Gubbins, PO; Gurley, BJ, 1998
)
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
" Concomitant use of potent inhibitors of CYP3A with simvastatin should be avoided or its dosage should be greatly reduced."( Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole.
Kantola, T; Kivistö, KT; Neuvonen, PJ, 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
" This has proved an effective and safe regimen which requires only 50% of the medication used for continuous dosing schedules."( Itraconazole in the treatment of onychomycosis: a double-blind comparison with miconazole.
De Doncker, P; Haneke, E; Heremans, A; Tajerbashi, M, 1998
)
0.3
" In addition, the short treatment times (< 3 months) and intermittent dosing schedules are likely to enhance compliance and reduce the costs of therapy."( Onychomycosis: pathogenesis, diagnosis, and management.
Elewski, BE, 1998
)
0.3
"Itraconazole, even at a small dosage of 100 mg daily, greatly elevated plasma concentrations of lovastatin and its active metabolite, lovastatin acid."( Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin.
Kantola, T; Kivistö, KT; Neuvonen, PJ, 1998
)
0.3
" During the 1-week pulse of active therapy, itraconazole (5 mg/kg/day) was dosed as follows: more than 40 kg, 200 mg per day (two capsules per day); 20 to 40 kg, 100 mg per day (one capsule per day); and 10 to 19 kg, 50 mg per day (one half of a capsule per day)."( Treatment of tinea capitis with itraconazole capsule pulse therapy.
Adam, P; Alexis, M; De Doncker, P; Gupta, AK; Hofstader, SL; Raboobee, N; Solomon, R; Summerbell, RC, 1998
)
0.3
" For patients administered concomitant cyclosporine, ketoconazole, and diltiazem, the dosage of cyclosporine, if it is administered alone, should be 20% to achieve the same blood concentrations."( Effect of metabolic inhibitors on cyclosporine pharmacokinetics using a population approach.
McLachlan, AJ; Tett, SE, 1998
)
0.3
"The efficacy and safety of an intermittent itraconazole dosing regimen was investigated in 354 patients with toenail onychomycosis, from 98 dermatology centres."( An intermittent itraconazole 1-week dosing regimen for the treatment of toenail onychomycosis in dermatological practice.
De Doncker, P; Ginter, G,
)
0.13
" The dosage regimen was 3 mg/kg per day given once daily in a fasting state with each pulse lasting 1 week."( Itraconazole oral solution for the treatment of tinea capitis.
Adam, P; Gupta, AK; Solomon, RS, 1998
)
0.3
" Five cats treated at the highest dosage of itraconazole vomited or became anorectic."( Efficacy of oral administration of itraconazole to cats with dermatophytosis caused by Microsporum canis.
Mancianti, F; Pedonese, F; Zullino, C, 1998
)
0.3
"Itraconazole pulse therapy was efficient and safe for the treatment of onychomycosis caused by dermatophytes, although a much higher daily dosage than the known continuous administration was used."( Efficacy and safety of itraconazole pulse therapy: Brazilian multicentric study on toenail onychomycosis caused by dermatophytes.
Campbell, I; Gontijo, B; Marques, SA; Ramos-e-Silva, M; Veloso, ST; Zaitz, C, 1998
)
0.3
" This information would then be useful in determining the efficacy of itraconazole administered by means of intermittent pulse dosing in the treatment of tinea capitis."( Itraconazole pulse therapy is effective in the treatment of Majocchi's granuloma: a clinical and pharmacokinetic evaluation and implications for possible effectiveness in tinea capitis.
De Doncker, P; Groen, K; Gupta, AK; Woestenborghs, R, 1998
)
0.3
" Zolpidem-induced benzodiazepine agonist effects (increased electrocardiographic beta activity, digit-symbol substitution test impairment, and delayed recall) during the first 4 hours after dosage were enhanced by ketoconazole but not by itraconazole or fluconazole."( Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole, and fluconazole.
Counihan, M; Durol, AL; Graf, JA; Greenblatt, DJ; Harmatz, JS; Mertzanis, P; Roth-Schechter, B; Shader, RI; von Moltke, LL, 1998
)
0.3
" Oral steroid dosing requirements and acute episodes of ABPA for days with vs days without itraconazole were compared."( Allergic bronchopulmonary aspergillosis in cystic fibrosis: role of atopy and response to itraconazole.
Esrig, S; Moss, RB; Nepomuceno, IB, 1999
)
0.3
" Short course and pulse dosing are particularly exciting options that may decrease cost and lower the risk of adverse side effects."( The evolving role of itraconazole, fluconazole and terbinafine in the treatment of tinea capitis.
Friedlander, SF, 1999
)
0.3
" The recent move to once-daily dosing means that criteria for therapeutic drug monitoring need to be redefined."( The therapeutic monitoring of antimicrobial agents.
Barclay, ML; Begg, EJ; Kirkpatrick, CJ, 1999
)
0.3
" First, the purpose of the study, the comparator drugs and their dosage regimens were defined."( Pharmacoeconomic analysis of oral antifungal therapies used to treat dermatophyte onychomycosis of the toenails. A US analysis.
Gupta, AK, 1998
)
0.3
"The purpose of this study was to compare the efficacy of different dosage regimens in the management of onychomycosis with itraconazole and to determine the results of a further 1-week intermittent pulse treatment in non-cured patients."( A comparison among four regimens of itraconazole treatment in onychomycosis.
Chen, J; Liao, W; Wen, H; Wu, J; Yao, Z, 1999
)
0.3
"To evaluate the efficacy and safety of a 1-week intermittent itraconazole dosing schedule for onychomycosis."( Therapeutic efficacy and safety of one-week intermittent therapy with itraconazole for onychomycosis in a Chinese patient population.
Li, RY; Wang, AP; Wang, DL; Wang, R, 1999
)
0.3
"A 1-week intermittent itraconazole dosing regimen is a safe and effective treatment for onychomycosis."( Therapeutic efficacy and safety of one-week intermittent therapy with itraconazole for onychomycosis in a Chinese patient population.
Li, RY; Wang, AP; Wang, DL; Wang, R, 1999
)
0.3
"In this open, randomized, parallel-group, the efficacy and safety of itraconazole pulse therapy (1 week 400 mg daily, 3 months) was evaluated in comparison with continuous terbinafine dosing (250 mg daily, 3 months) for the treatment of toenail onychomycosis."( Itraconazole pulse therapy vs continuous terbinafine dosing for toenail onychomycosis.
Kejda, J, 1999
)
0.3
" The itraconazole was given once daily in a fasting state at a dosage of 3 mg/kg/day as a pulse lasting 1 week."( Itraconazole oral solution for the treatment of tinea capitis using the pulse regimen.
Adam, P; Aly, R; Gupta, AK; Soloman, R, 1999
)
0.3
" Itraconazole was given from the start of chemotherapy in one of six different dosing regimens."( Fungal surveillance cultures during antifungal prophylaxis with itraconazole in neutropenic patients with acute leukaemia.
Glasmacher, A; Hahn, C; Marklein, G; Molitor, E; Sauerbruch, T; Schmidt-Wolf, IG, 1999
)
0.3
" All three benzodiazepines were susceptible to drug interactions, but oral dosing of midazolam and triazolam resulted in greater alterations in the pharmacokinetic parameters than alprazolam due to their larger presystemic extraction."( Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam, and triazolam.
Balian, JD; Flockhart, DA; Yuan, R, 1999
)
0.3
" Forty patients were randomly assigned to receive either itraconazole cyclodextrin solution or itraconazole capsules, both at a dosage of 100 mg bd for 15 days."( Serum itraconazole concentrations and clinical responses in Candida-associated denture stomatitis patients treated with itraconazole solution and itraconazole capsules.
Bagg, J; Cross, LJ; Oliver, D; Warnock, D, 2000
)
0.31
"A tablet dosage form containing solid dispersions of itraconazole (Asd tablets) was prepared by using the spray-drying and wet granulation methods."( Bioavailability of itraconazole in rats and rabbits after administration of tablets containing solid dispersion particles.
Jun, H; Jung, JY; Kang, E; Lee, KH; Lee, SH; Park, JW; Yoo, SD, 2000
)
0.31
" Since the bioavailability of itraconazole is reduced in these patients, a satisfactory dosing regimen remains to be defined."( Itraconazole trough concentrations in antifungal prophylaxis with six different dosing regimens using hydroxypropyl-beta-cyclodextrin oral solution or coated-pellet capsules.
Glasmacher, A; Hahn, C; Marklein, G; Molitor, E; Sauerbruch, T; Schmidt-Wolf, IG, 1999
)
0.3
" The optimal dosage and end point of treatment need to be ascertained after a larger study."( Itraconazole pulse therapy in chromoblastomycosis.
Kumarasinghe, MP; Kumarasinghe, SP,
)
0.13
"The boosted oral antifungal treatment (BOAT) is introduced as a novel approach improving the efficacy of oral treatment with the itraconazole pulse dosing regimen."( The boosted oral antifungal treatment for onychomycosis beyond the regular itraconazole pulse dosing regimen.
Arrese, JE; Piérard, GE; Piérard-Franchimont, C, 2000
)
0.31
" One patient treated with the lowest dosage for the shortest term had a recurrence after 1 month and needed a second 30-day course of itraconazole at a higher dosage."( Improved outcome of pulmonary aspergillosis in heart transplant recipients with early diagnosis and itraconazole treatment.
Andreana, A; Cione, P; Cotrufo, M; Cuccurullo, S; De Vivo, F; Maiello, C; Marra, C; Mormone, G; Sarnataro, G; Tripodi, MF; Utili, R; Zampino, R, 2000
)
0.31
" When problems are known to arise, they can often be overcome or minimised by varying the dosage regimens, or by drug monitoring."( The implications and management of drug interactions with itraconazole, fluconazole and terbinafine.
Drake, L; Gupta, AK; Lambert, J; Shear, N; Yaniv, R, 2000
)
0.31
" The 2-, 6-, and 20-mg/kg dosages of POC maintained plasma drug levels above the MICs for the entire 24-h dosing interval."( Antifungal activity and pharmacokinetics of posaconazole (SCH 56592) in treatment and prevention of experimental invasive pulmonary aspergillosis: correlation with galactomannan antigenemia.
Avila, N; Bacher, J; Candelario, M; Field-Ridley, A; Groll, AH; Petraitiene, R; Petraitis, V; Piscitelli, S; Sein, T; Walsh, TJ, 2001
)
0.31
" A newly recognized phenomenon known as the post-antifungal effect implies that antifungals, even at sub-therapeutic concentrations, may suppress the virulent attributes of yeasts, especially intra-orally where topical drug levels fluctuate dramatically during dosing intervals."( Antimycotic agents in oral candidosis: an overview: 2. Treatment of oral candidosis.
Ellepola, AN; Samaranayake, LP, 2000
)
0.31
" The patient failed to respond to treatment with a conventional dosage of a lipid formulation of amphotericin B (lifoAmB; 5 mg/kg/day) given alone or in combination with itraconazole, and he responded only to an aggressive strategy that included a very high dosage of lifoAmB (15 mg/kg/day) given in combination with itraconazole as well as a rapid reduction in immunosuppression."( Progressive disseminated aspergillosis in a bone marrow transplant recipient: response with a high-dose lipid formulation of amphotericin B.
Andersson, BS; Kontoyiannis, DP; Lewis, RE; Raad, II, 2001
)
0.31
" Intermittent pulse dosing with itraconazole is as safe and effective as short-term continuous therapy but more economical and convenient."( Treating onychomycosis.
Bassler, M; Rodgers, P, 2001
)
0.31
" The CSA dosing interval over time was significantly prolonged in group 2 compared to group 1 or the control group (p< or =0."( Enhanced cyclosporine-itraconazole interaction with cola in lung transplant recipients.
Gordon, SM; Haug , MT; Maurer, JR; Mehta, AC; Qu, A; Schilz, RJ; Shermock, KM; Wimberley, SL, 2001
)
0.31
"ICZ capsules administered in a fed state with a cola resulted in greater random levels of ICZ, a decrease in cost/d of CSA, and a prolongation of CSA dosing interval."( Enhanced cyclosporine-itraconazole interaction with cola in lung transplant recipients.
Gordon, SM; Haug , MT; Maurer, JR; Mehta, AC; Qu, A; Schilz, RJ; Shermock, KM; Wimberley, SL, 2001
)
0.31
" The area under the curve (AUC) of simvastatin after concomitant dosing with itraconazole was predicted to increase ca."( Inhibition of in vitro metabolism of simvastatin by itraconazole in humans and prediction of in vivo drug-drug interactions.
Ikeda, T; Inoue, S; Ishigam, M; Ito, K; Iwabuchi, H; Komai, T; Kondo, T; Sugiyama, Y; Takasaki, W; Uchiyama, M, 2001
)
0.31
" Ternary polyoxyethylene [21] stearyl ether/ oil and water form liquid crystalline system cream, which has a potential as dosage form for 1% itraconazole as topical dermal drug delivery."( Formulation and evaluation of itraconazole via liquid crystal for topical delivery system.
Nesseem, DI, 2001
)
0.31
" Prophylactic measures to avoid fungal contamination must be performed during hospitalization; patients should be taught how to avoid contamination, not only during the first period after transplantation, when high dosage immunosuppressive drugs are given, but also later when a normal lifestyle is resumed."( Fungal skin infections in organ transplant recipients.
Mantovani, L; Virgili, A; Zampino, MR, 2002
)
0.31
" Use of prednisone was discontinued, the dosage of methotrexate was decreased, and use of oral itraconazole 400 mg/day was instituted."( Disseminated cutaneous sporotrichosis treated with itraconazole.
Bell, K; Rosen, T; Stalkup, JR, 2002
)
0.31
"2 years), at a dosage of 400 mg daily for 1 week a month for 6 months."( Systemic itraconazole in the yellow nail syndrome.
Iorizzo, M; Piraccini, BM; Tosti, A, 2002
)
0.31
"To avoid severe myopathy, cyclosporine levels should be monitored sooner than weekly intervals and statins should be discontinued or their dosage should be reduced, as long as azoles need to be prescribed in transplant recipients."( Itraconazole-induced rhabdomyolysis and acute renal failure in a heart transplant recipient treated with simvastatin and cyclosporine.
Alivizatos, PA; Chilidou, D; Manginas, A; Vlahakos, DV; Zamanika, C, 2002
)
0.31
" These agents differ in their dosing regimen, efficacy, adverse events profile, potential for drug interaction, and cost."( Economic analysis of oral and topical therapies for onychomycosis of the toenails and fingernails.
Amaya, K; Arikian, S; Casciano, J; Doyle, J; Haspel, M; Kahler, K; Shear, N, 2003
)
0.32
" If the combination is considered necessary, repaglinide dosage should be greatly reduced and blood glucose concentrations carefully monitored."( Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics and pharmacodynamics of repaglinide: potentially hazardous interaction between gemfibrozil and repaglinide.
Backman, JT; Neuvonen, M; Neuvonen, PJ; Niemi, M, 2003
)
0.32
" These studies suggested that an HPbetaCD-based, emulsified wax cream formulation was a useful and effective dosage form for treating vaginal candidiasis."( A mucoadhesive, cyclodextrin-based vaginal cream formulation of itraconazole.
Brewster, ME; De Proost, E; Delaet, U; Francois, M; Peeters, J; Putteman, P; Snoeckx, E; Wouters, F, 2003
)
0.32
"The application of electrostatic spinning to pharmaceutical applications resulted in dosage forms with useful and controllable dissolution properties."( Preparation and characterization of nanofibers containing amorphous drug dispersions generated by electrostatic spinning.
Brewster, ME; Chun, I; Peeters, J; Rosenblatt, J; Verreck, G, 2003
)
0.32
" Five Kemp's ridley sea turtles (Lepidochelys kempi) receiving itraconazole at several dosages in a rehabilitation program had blood collected within 24 hr to estimate dosing frequency."( Steady-state plasma concentrations of itraconazole after oral administration in Kemp's ridley sea turtles, Lepidochelys kempi.
Hunter, RP; Manire, CA; Pennick, GJ; Rhinehart, HL; Rinaldi, MG; Sutton, DA, 2003
)
0.32
"Current dosing regimens for itraconazole are effective, safe, and versatile for use in superficial fungal infections in children, particularly tinea capitis."( Efficacy and safety of itraconazole use in children.
Cooper, EA; Ginter, G; Gupta, AK, 2003
)
0.32
" Posttransplantation, renal transplant recipients received itraconazole solution 200 mg twice daily and cyclosporine, dosed to achieve target concentrations."( Beneficial pharmacokinetic interaction between cyclosporine and itraconazole in renal transplant recipients.
Capitano, B; Florea, NR; Hull, D; Leitz, GJ; Nicolau, DP; Nightingale, CH, 2003
)
0.32
" Tacrolimus levels and dosage requirements were compared before and during azole therapy."( Tacrolimus dosage requirements after initiation of azole antifungal therapy in pediatric thoracic organ transplantation.
Boyle, GJ; Gandhi, S; Kurland, G; Law, YM; Mahnke, CB; Michaels, M; Miller, SA; Pigula, FA; Sutton, RM; Venkataramanan, R; Webber, SA, 2003
)
0.32
" Studies included in this meta-analysis required a standard accepted dosage regimen, treatment duration and follow-up period."( Cumulative meta-analysis of systemic antifungal agents for the treatment of onychomycosis.
Gupta, AK; Johnson, AM; Ryder, JE, 2004
)
0.32
" The dosage regimen was safe and well tolerated."( Pharmacokinetics and safety of itraconazole in patients with cystic fibrosis.
Brownlee, KG; Conway, SP; Cunliffe, H; Etherington, C; Peckham, DG; Whitehead, A, 2004
)
0.32
" 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
" In all children, the dosage of itraconazole was adjusted according to body weight, with 5 mg/kg/day given in a continuous regimen either as a capsule (116 patients) or an oral suspension (47 patients)."( Itraconazole in the treatment of tinea capitis caused by Microsporum canis: experience in a large cohort.
Ginter-Hanselmayer, G; Gupta, A; Smolle, J,
)
0.13
" Each patient received a daily dosage of 400 mg of itraconazole for a minimum of 3 months."( Itraconazole in the treatment of New World mucocutaneous leishmaniasis.
Armijos, RX; Calvopina, M; Cooper, PJ; Davidson, RN; Guevara, AG; Hashiguchi, Y, 2004
)
0.32
" The clinical implication of this study is that no lidocaine dosage adjustments are necessary if it is used to prepare the airway prior to endoscopic procedures or intubation in patients using itraconazole or other inhibitors of CYP3A4."( Effect of itraconazole on the pharmacokinetics of inhaled lidocaine.
Isohanni, MH; Neuvonen, PJ; Olkkola, KT, 2004
)
0.32
" These data highlight the species-specific differences in antifungal pharmacodynamics between mold-active agents that could be relevant for the development of in vitro susceptibility breakpoints and antifungal dosing in vivo."( In vitro pharmacodynamics of amphotericin B, itraconazole, and voriconazole against Aspergillus, Fusarium, and Scedosporium spp.
Klepser, ME; Lewis, RE; Wiederhold, NP, 2005
)
0.33
" Although the symptoms worsened when the prednisone dosage was gradually reduced, her growth retardation and increased weight decided us to stop prednisone treatment."( [Allergic bronchopulmonary aspergillosis in asthma and cystic fibrosis].
Dompeling, E; Hendriks, JJ; Jöbsis, Q; van Hoorn, JH, 2005
)
0.33
" Clinical studies have suggested minimum bioavailable dosage and minimum trough blood levels for effective prophylaxis against systemic fungal infection."( Making sense of itraconazole pharmacokinetics.
Glasmacher, A; Prentice, AG, 2005
)
0.33
" Exposure to gefitinib is increased by coadministration with CYP3A4 inhibitors, but since gefitinib is known to have a good tolerability profile, a dosage reduction is not recommended."( Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol.
Laight, A; Leadbetter, J; McKillop, D; Ranson, M; Smith, RP; Swaisland, HC; Wild, MJ, 2005
)
0.33
" Thus, this system may provide a useful dosage form for oral water-insoluble drug without food effect."( A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption.
Hong, JY; Kim, CK; Kim, JK; Park, JS; Song, YK, 2006
)
0.33
" Tacrolimus levels and dosage requirements were compared during and after itraconazole therapy."( Itraconazole prophylaxis in lung transplant recipients receiving tacrolimus (FK 506): efficacy and drug interaction.
Bakal, I; Kramer, MR; Ollech, A; Ollech, JE; Sahar, G; Saute, M; Shitrit, D, 2005
)
0.33
"Both oral itraconazole and terbinafine are effective in the treatment of onychomycosis when administered in the pulse dosage form."( An open randomized comparative study of oral itraconazole pulse and terbinafine pulse in the treatment of onychomycosis.
Mishra, K; Mishra, M; Panda, P; Sengupta, S; Tripathy, S,
)
0.13
" Plasma concentrations of perospirone and ID-15036 up to 10 hours after perospirone dosing were measured by high-performance liquid chromatography (HPLC)."( Effects of itraconazole and tandospirone on the pharmacokinetics of perospirone.
Koyama, T; Kusumi, I; Masui, T; Takahashi, Y, 2006
)
0.33
" After several regimen changes, the patient received oral itraconazole 200 mg every 12 hours and sirolimus at a dosage of 7 mg/day on days 76-80 and 5 mg/day on days 81 and 82."( Sirolimus-itraconazole interaction in a hematopoietic stem cell transplant recipient.
Abidi, MH; Dieterle, N; Garnick, JJ; Ibrahim, RB; Peres, E; Said, A, 2006
)
0.33
"The objective of this study was to determine and compare the lung and serum concentrations in mice following oral and pulmonary dosing of amorphous nanoparticulate itraconazole (ITZ) compositions as well as the Sporanox oral solution (itraconazole/Janssen)."( Single dose and multiple dose studies of itraconazole nanoparticles.
Burgess, D; Johnston, KP; McConville, JT; Peters, JI; Talbert, RL; Vaughn, JM; Williams, RO, 2006
)
0.33
"To study the efficacy of the 1-pulse dosing regimen of two generic products of itraconazole (Itracon and Itra) in comparison with the innovative product (Sporal) for the treatment of tinea pedis."( A comparison of the efficacy between two itraconazole generic products and the innovative itraconazole in the treatment of tinea pedis.
Chaichalotornkul, J; Hoharitanon, S; Sindhupak, W, 2005
)
0.33
" A separate dosing uniformity study was also performed to qualify use of the chamber."( Targeted high lung concentrations of itraconazole using nebulized dispersions in a murine model.
Burgess, DS; Frei, BL; Johnston, KP; McConville, JT; Overhoff, KA; Peters, JI; Sinswat, P; Talbert, RL; Vaughn, JM; Williams, RO, 2006
)
0.33
" Rats were pretreated with PB (75 mg/kg for 4 days) prior to itraconazole or fluconazole dosing (20 and 200 mg/kg for 4 days)."( Involvement of phenobarbital and SKF 525A in the hepatotoxicity of antifungal drugs itraconazole and fluconazole in rats.
Ahmad Bustamam, A; Hasiah, AH; Israf, DA; Khairi, HM; Somchit, N; Sulaiman, MR; Wong, CW; Zuraini, A, 2006
)
0.33
" Orally dosed itraconazole (ITZ) compositions, formed by SFL, produce higher serum levels of the drug compared to the commercial product, Sporanox oral solution."( Cryogenic liquids, nanoparticles, and microencapsulation.
Chen, X; Hu, J; Johnston, KP; McConville, JT; Overhoff, KA; Purvis, T; Rogers, TL; Sinswat, P; Vaughn, JM; Williams, RO, 2006
)
0.33
" The minimal inhibitory concentration (MIC) values calculated from dose-response curves on agar diffusion-test (Kadłubowski's method), were also examined by analysing the variation (mean x +/- standard error, median Me, mode Mo, Min-Max)."( [Susceptibility to itraconazole and miconazole of fungi strains isolated from the vaginal ontocenosis].
Horwatt-Bozyczko, E; Kołtuńska, M; Kurnatowska, A, 2001
)
0.31
" 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
"The primary objective of the study was to estimate the population pharmacokinetic parameters for itraconazole and hydroxy-itraconazole, in particular, the relative oral bioavailability of the capsule compared with solution in adult cystic fibrosis patients, in order to develop new dosing guidelines."( A d-optimal designed population pharmacokinetic study of oral itraconazole in adult cystic fibrosis patients.
Bell, SC; Charles, BG; Duffull, SB; France, M; Hennig, S; Miller, H; Wainwright, CE; Waterhouse, TH, 2007
)
0.34
" Simulations from the final model showed that a dosing schedule of 500 mg twice daily for both formulations provided the highest chance of target success."( A d-optimal designed population pharmacokinetic study of oral itraconazole in adult cystic fibrosis patients.
Bell, SC; Charles, BG; Duffull, SB; France, M; Hennig, S; Miller, H; Wainwright, CE; Waterhouse, TH, 2007
)
0.34
" From oral dosing of rats, it was determined that the two extrudate formulations performed similarly in vivo as confirmed by their statistically equivalent AUC values."( Hot-melt extrusion for enhanced delivery of drug particles.
McConville, JT; McGinity, JW; Miller, DA; Williams, RO; Yang, W, 2007
)
0.34
"The objective of this study was to formulate itraconazole semisolid dosage forms and characterize their physicochemical properties."( Characterization of itraconazole semisolid dosage forms prepared by hot melt technique.
Ji, CW; Lee, BJ; Park, ES; Sah, H; Shim, SY, 2006
)
0.33
" ITZ-IV at daily doses of 10, 20, or 40 mg/kg was as effective as the intraperitoneal administration of amphotericin B (AMPH) at a dosage of 1 mg/kg daily in improving survival."( Efficacy of intravenous itraconazole against invasive pulmonary aspergillosis in neutropenic mice.
Abe, S; Ishibashi, H; Ono, Y; Otani, H; Tansho, S; Torii, S; Yamaguchi, H, 2006
)
0.33
" However, a higher daily dosage of itraconazole might have an inhibitory effect."( Pharmacokinetic study of the interaction between itraconazole and nevirapine.
Jaruratanasirikul, S; Sriwiriyajan, S, 2007
)
0.34
" After repeated dosing for 1 week, both SES and SD increased the areas of Peyer's patch region in intestinal tissues but no distinct histopathological damage of the intestine was observed except the hepatocytes."( In vitro and in vivo comparative study of itraconazole bioavailability when formulated in highly soluble self-emulsifying system and in solid dispersion.
Lee, BJ; Park, MJ; Ren, S, 2007
)
0.34
"The goal of this research was to evaluate an intravenous itraconazole nanosuspension dosage form, relative to a solution formulation, in the rat."( Itraconazole IV nanosuspension enhances efficacy through altered pharmacokinetics in the rat.
Barker, K; Cook, C; Gass, J; Glosson, J; Kipp, J; Papadopoulos, P; Rabinow, B; Sun, CS; White, R; Wielgos, T; Wong, J; Wood, K, 2007
)
0.34
" No food effects were observed with the itraconazole:HBenBCD solid dosage forms."( Pharmacokinetics of itraconazole after intravenous and oral dosing of itraconazole-cyclodextrin formulations.
Buchanan, CM; Buchanan, NL; Edgar, KJ; Klein, S; Little, JL; Ramsey, MG; Ruble, KM; Wacher, VJ; Wempe, MF, 2007
)
0.34
" Treatment arms with the same regimen in terms of drug, type (continuous or intermittent), and dosage were combined to estimate the risk of an outcome of interest."( The safety of oral antifungal treatments for superficial dermatophytosis and onychomycosis: a meta-analysis.
Chan, AK; Chang, CH; Kurth, T; Orav, JE; Young-Xu, Y, 2007
)
0.34
" Eight healthy volunteers received Sporanox or ITRA-GSMP capsule in the fasted state or after a high-fat diet on four separate dosing occasions with a 2-week washout period."( Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers.
Hong, JY; Kim, CK; Lim, SJ; Song, YK; Woo, JS, 2008
)
0.35
" Nineteen patients were treated with itraconazole 200 mg once daily for 12 weeks, and 17 patients were treated with terbinafine for 12 weeks in a dosage according to their body weight, respectively."( Onychomycosis: a new emerging infectious disease in childhood population and adolescents. Report on treatment experience with terbinafine and itraconazole in 36 patients.
Ginter-Hanselmayer, G; Smolle, J; Weger, W, 2008
)
0.35
" The solid dosage form Sporanox again failed to achieve a similar extent of absorption enhancement (0."( Ordered mesoporous silica induces pH-independent supersaturation of the basic low solubility compound itraconazole resulting in enhanced transepithelial transport.
Annaert, P; Augustijns, P; Kayaert, P; Martens, JA; Mellaerts, R; Mols, R; Van den Mooter, G; Van Humbeeck, J, 2008
)
0.35
" In order to prepare an effective solid dosage form for a nanosuspension, it is imperative that the spray-dried nanoparticles should go back to their original particle size when reconstituted in an aqueous system."( Conversion of nanosuspensions into dry powders by spray drying: a case study.
Chaubal, MV; Popescu, C, 2008
)
0.35
" Upon addition to water, ITZ formed a colloidal dispersion suitable for nebulization, which demonstrated optimal aerodynamic properties for deep lung delivery and high lung and systemic levels when dosed to mice."( High bioavailability from nebulized itraconazole nanoparticle dispersions with biocompatible stabilizers.
Johnston, KP; McConville, JT; Miller, DA; Tam, J; Williams, RO; Yang, W; Zhou, J, 2008
)
0.35
" The influence of solubilizers on the aqueous solubility of the itraconazole, ketoconazole and miconazole was investigated in order to enhance their solubility for a possible parenteral dosage form."( Aqueous solvent system for the solubilization of azole compounds.
Antal, I; Klebovich, I; Kovács, K; Ludányi, K; Stampf, G, 2009
)
0.35
" Posaconazole and itraconazole were the most active in vitro with MICs falling well below the achievable serum levels typically observed with standard dosing regimens."( Antifungal susceptibility testing of Exophiala spp.: a head-to-head comparison of amphotericin B, itraconazole, posaconazole and voriconazole.
Fothergill, AW; Rinaldi, MG; Sutton, DA, 2009
)
0.35
" Our data suggests that survival and microbiological response depend more on drug dosing than on the trailing phenotype of the isolates."( Lack of correlation of 24- vs. 48-h itraconazole minimum inhibitory concentrations with microbiological and survival outcomes in a guinea pig model of disseminated candidiasis.
Chen, E; Leitz, GJ; Odabasi, Z; Ostrosky-Zeichner, L; Paetznick, VL; Rex, JH; Rodriguez, JR, 2010
)
0.36
" Based on these distinctions, it is important to carry out local studies in order to establish dosage regimens according the characteristics of each population."( Comparison of the oral pharmacokinetics of fluconazole and itraconazole in Mexicans.
Carrasco-Portugal, Mdel C; Flores-Murrieta, FJ; Landa, C, 2008
)
0.35
" We found that the current dosage regimen of IV-ITZ (200 mg/day) was appropriate to obtain therapeutic trough concentrations for neutropenic patients in Korea."( Population pharmacokinetics of intravenous itraconazole in patients with persistent neutropenic fever.
Chae, H; Choi, JH; Choi, SM; Kim, S; Lee, DG; Park, SH; Shin, WS; Yim, DS; Yoo, JH, 2009
)
0.35
" 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
" One study used daily dosing and the rest used once-weekly dosing."( Efficacy of fluconazole for the treatment of onychomycosis.
Brown, SJ, 2009
)
0.35
" However, fluconazole may be preferred in patients unable to tolerate other oral antifungal agents due to the dosing regimen, adverse effect profile, and drug interactions."( Efficacy of fluconazole for the treatment of onychomycosis.
Brown, SJ, 2009
)
0.35
" The antihistamine response after ebastine dosing would be decreased following rifampin pretreatments."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
0.36
"In this case, dosing recommendations of itraconazole 200 mg daily with lopinavir/ritonavir were appropriate."( Drug-drug interaction between itraconazole and the protease inhibitor lopinavir/ritonavir.
Hills-Nieminen, C; Houston, S; Hughes, CA; Shafran, SD, 2009
)
0.35
"The dose of itraconazole was reduced to 200 mg daily as recommended by current guidelines, and therapeutic drug monitoring of both itraconazole and lopinavir concentrations confirmed that no further dosage adjustments were necessary."( Drug-drug interaction between itraconazole and the protease inhibitor lopinavir/ritonavir.
Hills-Nieminen, C; Houston, S; Hughes, CA; Shafran, SD, 2009
)
0.35
" In the persistently neutropenic model with A1163, aminocandin, CAS and micafungin (2-10mg/kg) were all effective at prolonging survival, with some impact on reducing culture burdens, even with alternate-day dosing (4mg/kg)."( Activity of aminocandin (IP960; HMR3270) compared with amphotericin B, itraconazole, caspofungin and micafungin in neutropenic murine models of disseminated infection caused by itraconazole-susceptible and -resistant strains of Aspergillus fumigatus.
Denning, DW; Morrissey, G; Sharp, A; Warn, PA, 2010
)
0.36
" Single-dose 24-h pharmacokinetic studies were conducted in Sprague-Dawley rats following inhalation of the nebulized colloidal dispersions (equivalent to 20mgITZ/mL dispersion in 5mL) in a nose-only dosing apparatus."( Comparison of bioavailability of amorphous versus crystalline itraconazole nanoparticles via pulmonary administration in rats.
Johnston, KP; Williams, RO; Yang, W, 2010
)
0.36
" The aim of the presently reported study was the evaluation of the antimycotic action of two azole compounds--miconazole and itraconazole (Janssen) against 205 Candida strains isolated from the various biological specimens of two groups of patients--hospitalized (group 1) and examined in outpatient clinic (group 2); differentiation of species and codes of these strains; analysis of dose-response curves and parameters of polygons of the azoles minimal inhibitory concentrations (MIC)."( [Susceptibility to miconazole and itraconazole of Candida strains isolated from hospitalized and outpatient clinic patients].
Kurnatowska, AK; Kwaśniewska, J, 2009
)
0.35
" Conscious dogs, instrumented with a high-fidelity pressure transducer in the left ventricle, were placed in a sling for dosing and cardiac monitoring."( Nanosuspension formulation of itraconazole eliminates the negative inotropic effect of SPORANOX in dogs.
Cook, C; Gass, J; McKee, J; Rabinow, B, 2010
)
0.36
" In this study, the effect of multiple dosing of Icz on the pharmacokinetics of CsA in three healthy cats was investigated."( Effects of multiple oral dosing of itraconazole on the pharmacokinetics of cyclosporine in cats.
Kamishina, H; Katayama, M; Katayama, R, 2010
)
0.36
" 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
" The complex was formulated as a capsule dosage form and drug release was evaluated."( Comparative study of itraconazole-cyclodextrin inclusion complex and its commercial product.
Ahmed, SM; Alanazi, FK; Alhamed, SS; Alsarra, IA; Bosela, AA; Mowafy, HA; Neau, SH, 2010
)
0.36
" The present retrospective pharmacokinetic-pharmacodynamic (PK-PD) analysis was designed to find any factors affecting clinical outcome of ITCZ treatment, and was performed to evaluate the appropriateness of the current dosage regimen in ICU patients."( Pharmacokinetic-pharmacodynamic study of itraconazole in patients with fungal infections in intensive care units.
Hagihara, M; Hasegawa, T; Kasai, H; Kato, T; Mikamo, H; Umemura, T, 2011
)
0.37
" Plasma clearance of the commercial itraconazole solution was more rapid than the clearance published for other species, possibly warranting more frequent dosing in black-footed penguins."( Effects of compounding on pharmacokinetics of itraconazole in black-footed penguins (Spheniscus demersus).
Mitchell, MA; Papich, MG; Russell, G; Smith, JA, 2010
)
0.36
" Therefore, when administering ITCZ-OS, which is more rapidly absorbed in the digestive tract compared to its conventional dosage forms, to patients with blood disease, the blood concentration of ITCZ should be measured to maintain its efficacy and safety."( Clinical significance of measuring the blood concentration of itraconazole oral solution in the field of hematology.
Kawano, K; Kobayashi, H; Nakagawa, S; Ohta, S; Shimoeda, S; Yamato, S, 2010
)
0.36
" Tacrolimus levels and dosage requirements were compared during and after azole therapy."( Voriconazole and itraconazole in lung transplant recipients receiving tacrolimus (FK 506): efficacy and drug interaction.
Amital, A; Fuks, L; Kramer, MR; Shitrit, D,
)
0.13
" In contrast, the other three strains resistant to 8 mg/L itraconazole in vitro were refractory to the therapy, even at the highest itraconazole dosage (40 mg/kg)."( Correlation of in vitro activity and in vivo efficacy of itraconazole intravenous and oral solubilized formulations by testing Candida strains with various itraconazole susceptibilities in a murine invasive infection.
Shimogawara, K; Uchida, K; Yamaguchi, H, 2011
)
0.37
" The dosage of itraconazole should be reduced and its therapeutic outcome should be monitored closely when these two agents are concomitantly administered."( Pharmacokinetic interactions between ciprofloxacin and itraconazole in healthy male volunteers.
Mahatthanatrakul, W; Ridtitid, W; Samaeng, M; Sriwiriyajan, S; Wongnawa, M, 2011
)
0.37
" Anidulafungin is unique in that it possesses no clinically relevant drug interactions and does not require dosage adjustment in renal or hepatic impairment."( Anidulafungin: when and how? The clinician's view.
George, J; Reboli, AC, 2012
)
0.38
" The findings suggest that the dosage of S-ketamine should be reduced in patients receiving ticlopidine."( Exposure to oral S-ketamine is unaffected by itraconazole but greatly increased by ticlopidine.
Hagelberg, NM; Laine, K; Neuvonen, PJ; Olkkola, KT; Peltoniemi, MA; Reponen, P; Saari, TI; Turpeinen, M, 2011
)
0.37
" Suggestions for dosing regimens and laboratory monitoring are given."( Systemic drugs in patients with skin diseases.
Byekova, Y; Elewski, B; Hughey, L, 2011
)
0.37
"In this study, the potential of wet granulation of ordered mesoporous silica (OMS) material was evaluated to assess the risk of premature drug release during processing and to improve the bulk powder flow properties and compactibility for the development of an immediate release oral dosage form."( Risk assessment of premature drug release during wet granulation of ordered mesoporous silica loaded with poorly soluble compounds itraconazole, fenofibrate, naproxen, and ibuprofen.
Backhuijs, F; Martens, JA; Van den Mooter, G; Vialpando, M, 2012
)
0.38
" Response rates to griseofulvin are similar to rates seen in the 1970s, but require higher dosing and conversion to crushed tablets in partial responders."( Treatment outcomes for tinea capitis in a skin of color population.
Alexis, A; Bhanusali, D; Coley, M; Silverberg, JI; Silverberg, NB, 2012
)
0.38
" Serum concentrations were lower, with a maximum concentration of 104ng/ml at 4h after dosing and a terminal half-life of 10."( Inhalable highly concentrated itraconazole nanosuspension for the treatment of bronchopulmonary aspergillosis.
Rundfeldt, C; Scherliess, H; Steckel, H; Wlaź, P; Wyska, E, 2013
)
0.39
" According to the close drug monitoring, all 10 patients experienced supratherapeutic levels of CsA even with a preemptive CsA dosage reduction and prompt dose adjustment."( Adverse drug interactions as a high-risk factor for lethal post-transplant complications in Chinese population.
Chen, RL; Chen, ZZ; Fu, DH; Hu, JD; Li, J; Luo, XF; Qiu, HQ; Wu, XM; Yang, T; Yuan, XH; Zheng, XY,
)
0.13
" Additional therapy with itraconazole leads to the decrease of total IgE to the limits recommended for proper omalizumab dosing (30-1500 kUA/l)."( Itraconazole as 'bridge therapy' to anti-IgE in a patient with severe asthma with fungal sensitisation.
Badiu, I; Bussolino, C; Pizzimenti, S; Rolla, G, 2013
)
0.39
"The influence of dosing regimens on the recurrence rates of onychomycosis has not been investigated."( Recurrences of dermatophyte toenail onychomycosis during long-term follow-up after successful treatments with mono- and combined therapy of terbinafine and itraconazole.
Cooper, EA; Gupta, AK; Paquet, M,
)
0.13
"To compare recurrence rates for toenail dermatophyte onychomycosis between four dosing regimens."( Recurrences of dermatophyte toenail onychomycosis during long-term follow-up after successful treatments with mono- and combined therapy of terbinafine and itraconazole.
Cooper, EA; Gupta, AK; Paquet, M,
)
0.13
" Itraconazole (ITRA) is an antifungal commonly used in birds, but administration requires repeated oral dosing and the safety margin is narrow."( A model for treating avian aspergillosis: serum and lung tissue kinetics for Japanese quail (Coturnix japonica) following single and multiple aerosol exposures of a nanoparticulate itraconazole suspension.
Jeżewska-Witkowska, G; Rundfeldt, C; Steckel, H; Witkowski, A; Wlaź, P; Wyska, E, 2013
)
0.39
"This paper presents the chemometrically assisted optimization and validation of the RP-HPLC method intended for the quantitative analysis of itraconazole and its impurities in pharmaceutical dosage forms."( Chemometrically assissted optimization and validation of RP-HPLC method for the analysis of itraconazole and its impurities.
Ivanović, D; Jančić Stojanović, B; Jovanović, M; Kasagić, I; Malenović, A; Rakić, T, 2013
)
0.39
"Itraconazole, approved for treatment of toenail fungal infection onychomycosis, provides antifungal activity at a dosage requiring once-daily (QD) administration of 2 100-mg capsules for 12 weeks."( Randomized, placebo-controlled, phase 3 study of itraconazole for the treatment of onychomycosis.
Bulger, L; Maddin, S; Quiring, J, 2013
)
0.39
"This phase 3, randomized, placebo-controlled trial investigated the noninferiority of 1 itraconazole 200-mg tablet to 2 itraconazole 100-mg capsules dosed QD for 12 weeks, with a 40-week follow-up period."( Randomized, placebo-controlled, phase 3 study of itraconazole for the treatment of onychomycosis.
Bulger, L; Maddin, S; Quiring, J, 2013
)
0.39
" Itraconazole (ITZ) was selected as the model compound for the development of an oral dosage form for enhanced release."( Agglomeration of mesoporous silica by melt and steam granulation. part II: screening of steam granulation process variables using a factorial design.
Albertini, B; Martens, JA; Passerini, N; Rombaut, P; Van Den Mooter, G; Vander Heyden, Y; Vialpando, M, 2013
)
0.39
" The poorly water-soluble compound, itraconazole (ITZ), was selected for the development of an immediate-release oral dosage form."( Agglomeration of mesoporous silica by melt and steam granulation. Part I: a comparison between disordered and ordered mesoporous silica.
Albertini, B; Bergers, D; Martens, JA; Passerini, N; Rombaut, P; Van Den Mooter, G; Vialpando, M, 2013
)
0.39
" However, the optimal dosage of antifungal agents based on PK-PD properties has not been clearly established."( Population pharmacokinetics of itraconazole in Japanese patients with invasive fungal peritonitis.
Hagihara, M; Hamada, Y; Mikamo, H; Yamagishi, Y, 2013
)
0.39
"The aims of the present study were to prepare new dual-mode floating gastroretentive tablets (DF-GRT) containing itraconazole (ITR) and to evaluate influence of the dosage forms on pharmacokinetic parameters of ITR."( Preparation and evaluation of dual-mode floating gastroretentive tablets containing itraconazole.
Ha, JM; Kim, JY; Park, CW; Park, ES; Rhee, YS, 2014
)
0.4
"The mean 6β-hydroxycortisol/cortisol ratio was reduced by 68% from baseline (P < 0·05) after the 1st pulse dosing, but the inhibitory effect appeared to be resolved before the next pulse dosing and at 3 months post-treatment."( Longitudinal monitoring of CYP3A activity in patients receiving 3 cycles of itraconazole pulse therapy for onychomycosis.
Atsuda, K; Echizen, H; Inamoto, N; Kubo, H; Machida, M; Ono, N; Saito, H; Shibata, S; Shinozaki, K; Takahashi, H; Wada, N, 2014
)
0.4
" Nanocrystal suspensions were prepared by a rapid wet milling technique, after which the suspensions were transformed into solid dosage forms by both freeze drying and granulating."( Nanocrystal-based per-oral itraconazole delivery: superior in vitro dissolution enhancement versus Sporanox® is not realized in in vivo drug absorption.
Häkkinen, MR; Hirvonen, J; Ilkka, J; Järvinen, K; Kiesvaara, J; Kovalainen, M; Laaksonen, T; Laru, J; Oksala, O; Peltonen, L; Rönkkö, S; Sarnes, A, 2014
)
0.4
" The most widely used chemotherapeutic treatment is itraconazole, although the dosage commonly used can be harmful to some individuals and species."( Reduced itraconazole concentration and durations are successful in treating Batrachochytrium dendrobatidis infection in amphibians.
Brannelly, LA, 2014
)
0.4
" The dosage of anti-F."( Association of IgG immunoglobulin and subclasses level with the severity of chromoblastomycosis due to Fonsecaea pedrosoi and therapeutic response to itraconazole.
Azevedo, CD; Azevedo, FS; Bouillet, LE; Bruña-Romero, O; Marques, SG; Nascimento, FR; Pinto, MC; Silva, LA; Stoianoff, MA, 2014
)
0.4
" Limited published information exists regarding tacrolimus dosing when transitioning from voriconazole to itraconazole."( Tacrolimus dosage requirements in lung transplant recipients receiving antifungal prophylaxis with voriconazole followed by itraconazole: a preliminary prospective study.
Enderby, CY; Heckman, MG; Keller, CA; Thomas, CS, 2014
)
0.4
"Tacrolimus dosage adjustments were not necessary when converting from voriconazole to itraconazole."( Tacrolimus dosage requirements in lung transplant recipients receiving antifungal prophylaxis with voriconazole followed by itraconazole: a preliminary prospective study.
Enderby, CY; Heckman, MG; Keller, CA; Thomas, CS, 2014
)
0.4
" Recent advances in our knowledge of azole exposure-response relationships, therapeutic drug monitoring and individualized dosing strategies are reviewed as follows."( Optimizing azole antifungal therapy in the prophylaxis and treatment of fungal infections.
Dolton, MJ; McLachlan, AJ, 2014
)
0.4
" The recent approval of a solid oral tablet formulation of posaconazole with improved bioavailability and once-daily dosing has significantly improved the clinical utility of this agent."( Optimizing azole antifungal therapy in the prophylaxis and treatment of fungal infections.
Dolton, MJ; McLachlan, AJ, 2014
)
0.4
" Plasma concentrations of triazoles and their major metabolites at 12h after dosing were determined."( Impact of inflammation and concomitant glucocorticoid administration on plasma concentration of triazole antifungals in immunocompromised patients.
Kawakami, J; Mino, Y; Naito, T; Yamada, T, 2015
)
0.42
"The main goal of the current work was to investigate the possible use of flexographic printing for the conversion of nanosuspensions into solid dosage forms."( Fabrication of drug-loaded edible carrier substrates from nanosuspensions by flexographic printing.
Genina, N; Kolakovic, R; Laaksonen, T; Määttänen, A; Palo, M; Peltonen, J; Salonen, J; Sandler, N, 2015
)
0.42
" The most successful treatment option for eumycetomas offers itraconazole in a dosage of 200 mg twice daily."( Eumycetoma and actinomycetoma--an update on causative agents, epidemiology, pathogenesis, diagnostics and therapy.
Fahal, AH; Nenoff, P; Reinel, D; Schöfer, H; van de Sande, WW, 2015
)
0.42
" Interestingly although not approved as a treatment option, Itraconazole was effective in the seven cases it was used to treat cryptococcosis, with a dosage range of 100-400 mg/d and duration from 3 to 6 months."( Systemic Review of Published Reports on Primary Cutaneous Cryptococcosis in Immunocompetent Patients.
Chen, J; Du, L; Gu, J; Liao, W; Yang, Y; Zhu, Y, 2015
)
0.42
"The current available formulations of itraconazole are not ideal for dosing in cats."( Alternate-day dosing of itraconazole in healthy adult cats.
Dirikolu, L; Kubier, A; Middleton, SM; Mitchell, MA; Papich, MG; Rubin, SI, 2016
)
0.43
"The aim of this article is to investigate the role of amphiphilic block copolymer-based polymeric micelles of itraconazole for the management of fungal keratitis to overcome the limitations of the conventional dosage form."( Zero order delivery of itraconazole via polymeric micelles incorporated in situ ocular gel for the management of fungal keratitis.
Jaiswal, M; Kumar, M; Pathak, K, 2015
)
0.42
" A dose-response curve was generated for itraconazole and clarithromycin (maximal concentration 100 μM) and compared to that of Zosuquidar, a highly specific known P-gp inhibitor."( Itraconazole and clarithromycin inhibit P-glycoprotein activity in primary human sinonasal epithelial cells.
Bleier, BS; Han, X; Hoang, JD; Lam, A; Singleton, A, 2015
)
0.42
"Both itraconazole and clarithromycin demonstrated a dose-response curve for P-gp inhibition similar to that of Zosuquidar."( Itraconazole and clarithromycin inhibit P-glycoprotein activity in primary human sinonasal epithelial cells.
Bleier, BS; Han, X; Hoang, JD; Lam, A; Singleton, A, 2015
)
0.42
"The objective of the present work was to formulate tablet dosage form of itraconazole with enhanced bioavailability."( Formulation Development of Spherical Crystal Agglomerates of Itraconazole for Preparation of Directly Compressible Tablets with Enhanced Bioavailability.
Desai, J; Fadke, J; Thakkar, H, 2015
)
0.42
" Various factors considered in the recommendations include the choice of itraconazole dosage form, administration in the fasted or fed state, the dose and duration of itraconazole administration, the timing of substrate and itraconazole coadministration, and measurement of itraconazole and metabolite plasma concentrations, among others."( Best practices for the use of itraconazole as a replacement for ketoconazole in drug-drug interaction studies.
Bello, A; Dresser, MJ; Heald, D; Komjathy, SF; Liu, L; O'Mara, E; Robertson, SM; Rogge, M; Stoch, SA, 2016
)
0.43
" The activities of the benznidazole/itraconazole combinations were compared with the results from those receiving the same dosage of each individual drug."( Benznidazole/Itraconazole Combination Treatment Enhances Anti-Trypanosoma cruzi Activity in Experimental Chagas Disease.
Assíria Fontes Martins, T; Bahia, MT; Caldas, IS; Caldas, S; da Silva do Nascimento, ÁF; de Andrade, IM; de Figueiredo Diniz, L; Mazzeti, AL; Ribeiro, I, 2015
)
0.42
" We further formulated the amorphous solid dispersions into tablet dosage forms and evaluated their performance in a bio-relevant dissolution media."( Effect of hydrophilic additives on the dissolution and pharmacokinetic properties of itraconazole-enteric polymer hot-melt extruded amorphous solid dispersions.
Lang, B; Liu, S; McGinity, JW; Williams, RO, 2016
)
0.43
" The aim of this study was to establish the optimal dosage and administration of immunosuppressants and antifungal agents."( [Optimization of Immunosuppression and the Prevention of Fungal Infection in Autoimmune Diseases].
Mino, Y, 2015
)
0.42
" The resulting interaction between these CYP3A4 substrates can be utilized clinically as a pharmacokinetic booster for prolonging saquinavir dosing regimen and/or decreasing saquinavir dose requirement in HIV/AIDS patients."( A semi-mechanistic pharmacokinetic model of saquinavir combined with itraconazole in HIV-1-positive patients.
Jenjob, A; Lohitnavy, M; Methaneethorn, J; Pankaew, A; Phuphuak, K; Sriarwut, T, 2015
)
0.42
" Model application can be of advantage for dosing adjustment to avoid serious adverse effects resulted from concomitant use of both drugs."( Pharmacokinetic model for the inhibition of simvastatin metabolism by itraconazole.
Chan-Im, D; Chiang-Ngernthanyakool, R; Lohitnavy, M; Methaneethorn, J; Phaohorm, S; Tongpeng, W, 2015
)
0.42
" Continuous dosing may be required to fully inhibit the HH pathway and achieve clinical response."( Effects of Combined Treatment With Arsenic Trioxide and Itraconazole in Patients With Refractory Metastatic Basal Cell Carcinoma.
Ally, MS; Atwood, SX; Bailey-Healy, I; Beachy, PA; Chang, AL; Colevas, AD; Kim, J; Oro, A; Ransohoff, K; Rezaee, M; Sarin, K; Tang, JY, 2016
)
0.43
" In short, the quantification of BNZ and ITZ by analysis of mixtures had shown to be efficient and cost-effective alternative for determination of these drugs in a pharmaceutical dosage form."( Simultaneous determination of benznidazole and itraconazole using spectrophotometry applied to the analysis of mixture: A tool for quality control in the development of formulations.
Cunha-Filho, MS; Infante, CM; Pinho, LA; Sá-Barreto, LC, 2016
)
0.43
"The purpose of this study was to assess the feasibility of a multicompartmental in vitro dissolution apparatus, gastrointestinal simulator (GIS), in assessing the drug dissolution of 2 commercially available oral dosage forms for itraconazole (ICZ)."( The Evaluation of In Vitro Drug Dissolution of Commercially Available Oral Dosage Forms for Itraconazole in Gastrointestinal Simulator With Biorelevant Media.
Amidon, GE; Amidon, GL; Matsui, K; Tsume, Y, 2016
)
0.43
" The objective of the present study was to better understand the best choice of rodent model for evaluating the pharmacokinetic and efficacy of this orally administered modified release ITZ dosage form against invasive Aspergillus fumigatus."( Modified release itraconazole amorphous solid dispersion to treat Aspergillus fumigatus: importance of the animal model selection.
Huang, S; Kirkpatrick, WR; Maincent, JP; Najvar, LK; Patterson, TF; Peters, JI; Wiederhold, NP; Williams, RO, 2017
)
0.46
" In patients whose blood concentration decreases after the switch, the development of GVHD should be monitored and tacrolimus dosage should be readjusted to maintain an appropriate blood concentration."( Analysis of the variable factors influencing tacrolimus blood concentration during the switch from continuous intravenous infusion to oral administration after allogeneic hematopoietic stem cell transplantation.
Akashi, K; Ikesue, H; Masuda, S; Matsukawa, K; Miyamoto, T; Shiratsuchi, M; Suetsugu, K; Tsuchiya, Y; Uchida, M; Watanabe, H; Yamamoto-Taguchi, N, 2017
)
0.46
" Based on the in vitro and in vivo results, further investigations in larger animals are a logical next step where fluid volumes, pH, and transit times are more favorable for the evaluated dosage forms."( Mucoadhesive amorphous solid dispersions for sustained release of poorly water soluble drugs.
LaFountaine, JS; McGinity, JW; Miller, DA; Prasad, LK; Williams, RO, 2017
)
0.46
" The delivery of TDM as a future standard of care will require real-time measurement of drug concentrations at the bedside and algorithms for dosage adjustment."( Therapeutic drug monitoring for invasive mould infections and disease: pharmacokinetic and pharmacodynamic considerations.
Hope, WW; Stott, KE, 2017
)
0.46
"There is more research required to broaden the knowledge on the downstream processing of nanosuspensions into solid oral dosage forms, especially for coated nanosuspensions onto beads as carriers."( Downstream drug product processing of itraconazole nanosuspension: Factors influencing drug particle size and dissolution from nanosuspension-layered beads.
Low, A; Möschwitzer, JP; Parmentier, J; Tan, EH, 2017
)
0.46
" When Sporanox and itraconazole/AFFINISOL High Productivity HPMCAS SDDs were dosed in rats, the maximum absorption rate for each formulation rank-ordered with membrane flux in vitro."( Impact of Drug-Rich Colloids of Itraconazole and HPMCAS on Membrane Flux in Vitro and Oral Bioavailability in Rats.
Brodeur, TJ; Friesen, DT; Goodwin, AK; Grass, ME; Morgen, MM; Stewart, AM; Vodak, DT, 2017
)
0.46
" Its variable and unpredictable oral bioavailability make it difficult to determine the optimal dosing regimen."( Pharmacokinetic evaluation of oral itraconazole for antifungal prophylaxis in children.
Allegra, S; Carcieri, C; Cusato, J; D'Avolio, A; De Francia, S; De Nicolò, A; Di Perri, G; Fatiguso, G; Favata, F; Pirro, E, 2017
)
0.46
"There has been limited research done on the downstream processing of nanosuspensions into solid oral dosage forms."( Downstream drug product processing of itraconazole nanosuspension: Factors influencing tablet material properties and dissolution of compacted nanosuspension-layered sugar beads.
Low, A; Möschwitzer, JP; Parmentier, J; Tan, EH, 2017
)
0.46
" SMSD technology could be an efficacious dosage option for the consistent oral absorption and clinical outcomes of ITZ."( Avoidance of food effect on oral absorption profile of itraconazole by self-micellizing solid dispersion approach.
Kobayashi, K; Kojo, Y; Matsunaga, S; Onoue, S; Sato, H; Seto, Y; Suzuki, H, 2017
)
0.46
" Using an in vivo estimation of the pharmacodynamic target and a previously published pharmacokinetic model, the probability of target attainment (PTA) was determined for a range of isavuconazole MICs using three dosing regimens (I, 200 mg once daily; II, 300 mg once daily; and III, 400 mg once daily)."( Isavuconazole susceptibility of clinical Aspergillus fumigatus isolates and feasibility of isavuconazole dose escalation to treat isolates with elevated MICs.
Brüggemann, RJM; Buil, JB; Meis, JF; Melchers, WJG; Mouton, JW; Verweij, PE; Wasmann, RE; Zoll, J, 2018
)
0.48
" The PTA for isolates with an isavuconazole MIC of 1 mg/L was 92%-99% for 90% effective concentration (EC90) for the three dosing regimens."( Isavuconazole susceptibility of clinical Aspergillus fumigatus isolates and feasibility of isavuconazole dose escalation to treat isolates with elevated MICs.
Brüggemann, RJM; Buil, JB; Meis, JF; Melchers, WJG; Mouton, JW; Verweij, PE; Wasmann, RE; Zoll, J, 2018
)
0.48
"The formulation factors relevant to developing immediate and controlled release dosage forms containing poorly soluble drugs dispersed in amorphous systems are poorly understood."( Development of Itraconazole Tablets Containing Viscous KinetiSol Solid Dispersions: In Vitro and In Vivo Analysis in Dogs.
Hughey, JR; Keen, JM; LaFountaine, JS; McGinity, JW; Miller, DA, 2018
)
0.48
"The poor attainment of target levels with current recommended dosing in children <12 years of age suggests that higher empiric doses are needed in this age group."( Itraconazole Dosing and Drug Monitoring at a Tertiary Children's Hospital.
Boast, A; Cranswick, N; Curtis, N; Gwee, A; Leong, YH, 2019
)
0.51
"Current dosing regimens of reported drugs are effective and safe for use in tinea capitis in children."( Tinea capitis in children: a systematic review of management.
Friedlander, SF; Gupta, AK; Mays, RR; Piguet, V; Piraccini, BM; Shear, NH; Tosti, A; Versteeg, SG, 2018
)
0.48
" To evaluate the efficacy and safety of different cycles of itraconazole pulse therapy, determine the optimal dosage and number of cycles for onychomycosis."( An exploration of the optimum dosage and number of cycles of itraconazole pulse therapy for severe onychomycosis.
Li, X; Shi, Y; Tao, Y; Xu, H; Yu, J; Zhang, L, 2018
)
0.48
" Performance of the model was validated using prespecified acceptance criteria against different dosing regimens, formulations for 29 PK, and DDI studies with midazolam and other CYP3A4 substrates."( Physiologically Based Pharmacokinetic Model of Itraconazole and Two of Its Metabolites to Improve the Predictions and the Mechanistic Understanding of CYP3A4 Drug-Drug Interactions.
Ericsson, H; Janzén, D; Kanebratt, KP; Lennernäs, H; Lundahl, A; Prieto Garcia, L, 2018
)
0.48
" Such thermodynamic based solubility data of ITRA will be of immense help in solubilization, synthesis, process development, preformualtion, and dosage form development in pharmaceuticals."( Solubilization and determination of solution thermodynamic properties of itraconazole in different solvents at different temperatures.
Jagdale, SK; Nawale, RB, 2019
)
0.51
"Using patient-derived glioblastoma stem cell (GSC) cultures from 15 GBM patients, we described stem cell properties of individual cultures, determined the dose-response relationships of the drugs in the CUSP9, and assessed the efficacy the CUSP9 combination with TMZ in concentrations clinically achievable."( The efficacy of a coordinated pharmacological blockade in glioblastoma stem cells with nine repurposed drugs using the CUSP9 strategy.
Grieg, Z; Langmoen, IA; Sandberg, CJ; Skaga, E; Skaga, IØ; Vik-Mo, EO, 2019
)
0.51
"4 mg/lb], PO, q 24 h, with or without a loading dosage protocol) and itraconazole (approx 10 mg/kg [4."( Investigation of a combination of amiodarone and itraconazole for treatment of American trypanosomiasis (Chagas disease) in dogs.
Benaím, G; Estep, JS; Luis Concepción, J; Madigan, R; Majoy, S; Márquez, ME; Mogollón-Mendoza, AC; Paniz-Mondolfi, AE; Pérez Alvarez, A; Ritter, K; Rodriguez-Morales, AJ; Silva, SC; Zao, CL, 2019
)
0.51
"Solid dosage forms of amorphous solid dispersions (ASDs) have rarely been assessed for their crushability, although it might possibly be a more frequent practice than thought to facilitate oral administration in several clinical conditions (e."( The influence of crushing amorphous solid dispersion dosage forms on the in-vitro dissolution kinetics.
Appeltans, B; Pas, T; Van den Mooter, G; Verbert, S, 2020
)
0.56
"These results provided a new perspective for designing topical dosage forms for the treatment of onychomycosis."( Effect of monoterpenes on ex vivo transungual delivery of itraconazole for the management of onychomycosis.
Abdollahi, D; Afshar, M; Jafariazar, Z, 2020
)
0.56
" The current PBPK model, which considers changes in unbound potency-adjusted active species, can be used to inform dosing recommendations when abemaciclib is coadministered with CYP3A4 perpetrators."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
0.56
"Cyclodextrins are widely used pharmaceutical excipients, particularly for insoluble compounds dosed orally, such as the oral solution of itraconazole, which is frequently used in clinical drug-drug interaction studies to inhibit cytochrome P450 3A."( Understanding the Effect of Hydroxypropyl-β-Cyclodextrin on Fenebrutinib Absorption in an Itraconazole-Fenebrutinib Drug-Drug Interaction Study.
Chen, JZ; Chen, Y; Chiang, PC; Chinn, LW; Durk, MR; Jones, NS; Liu, J; Mao, C; Nagapudi, K; Plise, EG; Wong, S, 2020
)
0.56
" ECG data were collected on multiple days during repeat dosing treatment regimens, thereby allowing the capture of QT data across a wide range of drug concentrations in each study participant and encompassing both "therapeutic" and "supra-therapeutic" exposures."( PKPD and cardiac single cell modeling of a DDI study with a CYP3A4 substrate and itraconazole to quantify the effects on QT interval duration.
Bentley, D; Derks, M; Diack, C; Jaminion, F; Wandel, C; Wang, K, 2020
)
0.56
"The administration of conventional dosage forms of itraconazole (ITZ) for cutaneous candidiasis treatment is limited by its poor aqueous solubility and the deep location ofCandida albicans(CA) in this disease."( Dissolving microneedle-mediated dermal delivery of itraconazole nanocrystals for improved treatment of cutaneous candidiasis.
Anjani, QK; Donnelly, RF; Paredes, AJ; Permana, AD; Utomo, E; Volpe-Zanutto, F, 2020
)
0.56
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; Bedel, J; Bedlack, R; Bermúdez de Castro, JM; Berry, JD; Berthier, C; Bhattacharya, D; Biadgo, B; Bianco, G; Bianco, M; Bibi, S; Bigliardi, AP; Billheimer, D; Birnie, DH; Biswas, K; Blair, HC; Bognetti, P; Bolan, PJ; Bolla, JR; Bolze, A; Bonnaillie, P; Borlimi, R; Bórquez, J; Bottari, NB; Boulleys-Nana, JR; Brighetti, G; Brodeur, GM; Budnyak, T; Budnyk, S; Bukirwa, VD; Bulman, DM; Burm, R; Busman-Sahay, K; Butcher, TW; Cai, C; Cai, H; Cai, L; Cairati, M; Calvano, CD; Camacho-Ordóñez, A; Camela, E; Cameron, T; Campbell, BS; Cansian, RL; Cao, Y; Caporale, AS; Carciofi, AC; Cardozo, V; Carè, J; Carlos, AF; Carozza, R; Carroll, CJW; Carsetti, A; Carubelli, V; Casarotta, E; Casas, M; Caselli, G; Castillo-Lora, J; Cataldi, TRI; Cavalcante, ELB; Cavaleiro, A; Cayci, Z; Cebrián-Tarancón, C; Cedrone, E; Cella, D; Cereda, C; Ceretti, A; Ceroni, M; Cha, YH; Chai, X; Chang, EF; Chang, TS; Chanteux, H; Chao, M; Chaplin, BP; Chaturvedi, S; Chaturvedi, V; Chaudhary, DK; Chen, A; Chen, C; Chen, HY; Chen, J; Chen, JJ; Chen, K; Chen, L; Chen, Q; Chen, R; Chen, SY; Chen, TY; Chen, WM; Chen, X; Chen, Y; Cheng, G; Cheng, GJ; Cheng, J; Cheng, YH; Cheon, HG; Chew, KW; Chhoker, S; Chiu, WN; Choi, ES; Choi, MJ; Choi, SD; Chokshi, S; Chorny, M; Chu, KI; Chu, WJ; Church, AL; Cirrincione, A; Clamp, AR; Cleff, MB; Cohen, M; Coleman, RL; Collins, SL; Colombo, N; Conduit, N; Cong, WL; Connelly, MA; Connor, J; Cooley, K; Correa Ramos Leal, I; Cose, S; Costantino, C; Cottrell, M; Cui, L; Cundall, J; Cutaia, C; Cutler, CW; Cuypers, ML; da Silva Júnior, FMR; Dahal, RH; Damiani, E; Damtie, D; Dan-Li, W; Dang, Z; Dasa, SSK; Davin, A; Davis, DR; de Andrade, CM; de Jong, PL; de Oliveira, D; de Paula Dorigam, JC; Dean, A; Deepa, M; Delatour, C; Dell'Aiera, S; Delley, MF; den Boer, RB; Deng, L; Deng, Q; Depner, RM; Derdau, V; Derici, U; DeSantis, AJ; Desmarini, D; Diffo-Sonkoue, L; Divizia, M; Djenabou, A; Djordjevic, JT; Dobrovolskaia, MA; Domizi, R; Donati, A; Dong, Y; Dos Santos, M; Dos Santos, MP; Douglas, RG; Duarte, PF; Dullaart, RPF; Duscha, BD; Edwards, LA; Edwards, TE; Eichenwald, EC; El-Baba, TJ; Elashiry, M; Elashiry, MM; Elashry, SH; Elliott, A; Elsayed, R; Emerson, MS; Emmanuel, YO; Emory, TH; Endale-Mangamba, LM; Enten, GA; Estefanía-Fernández, K; Estes, JD; Estrada-Mena, FJ; Evans, S; Ezra, L; Faria de, RO; Farraj, AK; Favre, C; Feng, B; Feng, J; Feng, L; Feng, W; Feng, X; Feng, Z; Fernandes, CLF; Fernández-Cuadros, ME; Fernie, AR; Ferrari, D; Florindo, PR; Fong, PC; Fontes, EPB; Fontinha, D; Fornari, VJ; Fox, NP; Fu, Q; Fujitaka, Y; Fukuhara, K; Fumeaux, T; Fuqua, C; Fustinoni, S; Gabbanelli, V; Gaikwad, S; Gall, ET; Galli, A; Gancedo, MA; Gandhi, MM; Gao, D; Gao, K; Gao, M; Gao, Q; Gao, X; Gao, Y; Gaponenko, V; Garber, A; Garcia, EM; García-Campos, C; García-Donas, J; García-Pérez, AL; Gasparri, F; Ge, C; Ge, D; Ge, JB; Ge, X; George, I; George, LA; Germani, G; Ghassemi Tabrizi, S; Gibon, Y; Gillent, E; Gillies, RS; Gilmour, MI; Goble, S; Goh, JC; Goiri, F; Goldfinger, LE; Golian, M; Gómez, MA; Gonçalves, J; Góngora-García, OR; Gonul, I; González, MA; Govers, TM; Grant, PC; Gray, EH; Gray, JE; Green, MS; Greenwald, I; Gregory, MJ; Gretzke, D; Griffin-Nolan, RJ; Griffith, DC; Gruppen, EG; Guaita, A; Guan, P; Guan, X; Guerci, P; Guerrero, DT; Guo, M; Guo, P; Guo, R; Guo, X; Gupta, J; Guz, G; Hajizadeh, N; Hamada, H; Haman-Wabi, AB; Han, TT; Hannan, N; Hao, S; Harjola, VP; Harmon, M; Hartmann, MSM; Hartwig, JF; Hasani, M; Hawthorne, WJ; Haykal-Coates, N; Hazari, MS; He, DL; He, P; He, SG; Héau, C; Hebbar Kannur, K; Helvaci, O; Heuberger, DM; Hidalgo, F; Hilty, MP; Hirata, K; Hirsch, A; Hoffman, AM; Hoffmann, JF; Holloway, RW; Holmes, RK; Hong, S; Hongisto, M; Hopf, NB; Hörlein, R; Hoshino, N; Hou, Y; Hoven, NF; Hsieh, YY; Hsu, CT; Hu, CW; Hu, JH; Hu, MY; Hu, Y; Hu, Z; Huang, C; Huang, D; Huang, DQ; Huang, L; Huang, Q; Huang, R; Huang, S; Huang, SC; Huang, W; Huang, Y; Huffman, KM; Hung, CH; Hung, CT; Huurman, R; Hwang, SM; Hyun, S; Ibrahim, AM; Iddi-Faical, A; Immordino, P; Isla, MI; Jacquemond, V; Jacques, T; Jankowska, E; Jansen, JA; Jäntti, T; Jaque-Fernandez, F; Jarvis, GA; Jatt, LP; Jeon, JW; Jeong, SH; Jhunjhunwala, R; Ji, F; Jia, X; Jia, Y; Jian-Bo, Z; Jiang, GD; Jiang, L; Jiang, W; Jiang, WD; Jiang, Z; Jiménez-Hoyos, CA; Jin, S; Jobling, MG; John, CM; John, T; Johnson, CB; Jones, KI; Jones, WS; Joseph, OO; Ju, C; Judeinstein, P; Junges, A; Junnarkar, M; Jurkko, R; Kaleka, CC; Kamath, AV; Kang, X; Kantsadi, AL; Kapoor, M; Karim, Z; Kashuba, ADM; Kassa, E; Kasztura, M; Kataja, A; Katoh, T; Kaufman, JS; Kaupp, M; Kehinde, O; Kehrenberg, C; Kemper, N; Kerr, CW; Khan, AU; Khan, MF; Khan, ZUH; Khojasteh, SC; Kilburn, S; Kim, CG; Kim, DU; Kim, DY; Kim, HJ; Kim, J; Kim, OH; Kim, YH; King, C; Klein, A; Klingler, L; Knapp, AK; Ko, TK; Kodavanti, UP; Kolla, V; Kong, L; Kong, RY; Kong, X; Kore, S; Kortz, U; Korucu, B; Kovacs, A; Krahnert, I; Kraus, WE; Kuang, SY; Kuehn-Hajder, JE; Kurz, M; Kuśtrowski, P; Kwak, YD; Kyttaris, VC; Laga, SM; Laguerre, A; Laloo, A; Langaro, MC; Langham, MC; Lao, X; Larocca, MC; Lassus, J; Lattimer, TA; Lazar, S; Le, MH; Leal, DB; Leal, M; Leary, A; Ledermann, JA; Lee, JF; Lee, MV; Lee, NH; Leeds, CM; Leeds, JS; Lefrandt, JD; Leicht, AS; Leonard, M; Lev, S; Levy, K; Li, B; Li, C; Li, CM; Li, DH; Li, H; Li, J; Li, L; Li, LJ; Li, N; Li, P; Li, T; Li, X; Li, XH; Li, XQ; Li, XX; Li, Y; Li, Z; Li, ZY; Liao, YF; Lin, CC; Lin, MH; Lin, Y; Ling, Y; Links, TP; Lira-Romero, E; Liu, C; Liu, D; Liu, H; Liu, J; Liu, L; Liu, LP; Liu, M; Liu, T; Liu, W; Liu, X; Liu, XH; Liu, Y; Liuwantara, D; Ljumanovic, N; Lobo, L; Lokhande, K; Lopes, A; Lopes, RMRM; López-Gutiérrez, JC; López-Muñoz, MJ; López-Santamaría, M; Lorenzo, C; Lorusso, D; Losito, I; Lu, C; Lu, H; Lu, HZ; Lu, SH; Lu, SN; Lu, Y; Lu, ZY; Luboga, F; Luo, JJ; Luo, KL; Luo, Y; Lutomski, CA; Lv, W; M Piedade, MF; Ma, J; Ma, JQ; Ma, JX; Ma, N; Ma, P; Ma, S; Maciel, M; Madureira, M; Maganaris, C; Maginn, EJ; Mahnashi, MH; Maierhofer, M; Majetschak, M; Malla, TR; Maloney, L; Mann, DL; Mansuri, A; Marelli, E; Margulis, CJ; Marrella, A; Martin, BL; Martín-Francés, L; Martínez de Pinillos, M; Martínez-Navarro, EM; Martinez-Quintanilla Jimenez, D; Martínez-Velasco, A; Martínez-Villaseñor, L; Martinón-Torres, M; Martins, BA; Massongo, M; Mathew, AP; Mathews, D; Matsui, J; Matsumoto, KI; Mau, T; Maves, RC; Mayclin, SJ; Mayer, JM; Maynard, ND; Mayr, T; Mboowa, MG; McEvoy, MP; McIntyre, RC; McKay, JA; McPhail, MJW; McVeigh, AL; Mebazaa, A; Medici, V; Medina, DN; Mehmood, T; Mei-Li, C; Melku, M; Meloncelli, S; Mendes, GC; Mendoza-Velásquez, C; Mercadante, R; Mercado, MI; Merenda, MEZ; Meunier, J; Mi, SL; Michels, M; Mijatovic, V; Mikhailov, V; Milheiro, SA; Miller, DC; Ming, F; Mitsuishi, M; Miyashita, T; Mo, J; Mo, S; Modesto-Mata, M; Moeller, S; Monte, A; Monteiro, L; Montomoli, J; Moore, EE; Moore, HB; Moore, PK; Mor, MK; Moratalla-López, N; Moratilla Lapeña, L; Moreira, R; Moreno, MA; Mörk, AC; Morton, M; Mosier, JM; Mou, LH; Mougharbel, AS; Muccillo-Baisch, AL; Muñoz-Serrano, AJ; Mustafa, B; Nair, GM; Nakanishi, I; Nakanjako, D; Naraparaju, K; Nawani, N; Neffati, R; Neil, EC; Neilipovitz, D; Neira-Borrajo, I; Nelson, MT; Nery, PB; Nese, M; Nguyen, F; Nguyen, MH; Niazy, AA; Nicolaï, J; Nogueira, F; Norbäck, D; Novaretti, JV; O'Donnell, T; O'Dowd, A; O'Malley, DM; Oaknin, A; Ogata, K; Ohkubo, K; Ojha, M; Olaleye, MT; Olawande, B; Olomo, EJ; Ong, EWY; Ono, A; Onwumere, J; Ortiz Bibriesca, DM; Ou, X; Oza, AM; Ozturk, K; Özütemiz, C; Palacio-Pastrana, C; Palaparthi, A; Palevsky, PM; Pan, K; Pantanetti, S; Papachristou, DJ; Pariani, A; Parikh, CR; Parissis, J; Paroul, N; Parry, S; Patel, N; Patel, SM; Patel, VC; Pawar, S; Pefura-Yone, EW; Peixoto Andrade, BCO; Pelepenko, LE; Peña-Lora, D; Peng, S; Pérez-Moro, OS; Perez-Ortiz, AC; Perry, LM; Peter, CM; Phillips, NJ; Phillips, P; Pia Tek, J; Piner, LW; Pinto, EA; Pinto, SN; Piyachaturawat, P; Poka-Mayap, V; Polledri, E; Poloni, TE; Ponessa, G; Poole, ST; Post, AK; Potter, TM; Pressly, BB; Prouty, MG; Prudêncio, M; Pulkki, K; Pupier, C; Qian, H; Qian, ZP; Qiu, Y; Qu, G; Rahimi, S; Rahman, AU; Ramadan, H; Ramanna, S; Ramirez, I; Randolph, GJ; Rasheed, A; Rault, J; Raviprakash, V; Reale, E; Redpath, C; Rema, V; Remucal, CK; Remy, D; Ren, T; Ribeiro, LB; Riboli, G; Richards, J; Rieger, V; Rieusset, J; Riva, A; Rivabella Maknis, T; Robbins, JL; Robinson, CV; Roche-Campo, F; Rodriguez, R; Rodríguez-de-Cía, J; Rollenhagen, JE; Rosen, EP; Rub, D; Rubin, N; Rubin, NT; Ruurda, JP; Saad, O; Sabell, T; Saber, SE; Sabet, M; Sadek, MM; Saejio, A; Salinas, RM; Saliu, IO; Sande, D; Sang, D; Sangenito, LS; Santos, ALSD; Sarmiento Caldas, MC; Sassaroli, S; Sassi, V; Sato, J; Sauaia, A; Saunders, K; Saunders, PR; Savarino, SJ; Scambia, G; Scanlon, N; Schetinger, MR; Schinkel, AFL; Schladweiler, MC; Schofield, CJ; Schuepbach, RA; Schulz, J; Schwartz, N; Scorcella, C; Seeley, J; Seemann, F; Seinige, D; Sengoku, T; Seravalli, J; Sgromo, B; Shaheen, MY; Shan, L; Shanmugam, S; Shao, H; Sharma, S; Shaw, KJ; Shen, BQ; Shen, CH; Shen, P; Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
" Plasma concentrations of ITZ and OH-ITZ at 12 h after dosing were determined at steady state."( Associations between plasma hydroxylated metabolite of itraconazole and serum creatinine in patients with a hematopoietic or immune-related disorder.
Imoto, Y; Kawakami, J; Miyadera, Y; Naito, T; Ono, T, 2021
)
0.62
" Although the clinical practices of nebulised parenteral amphotericin B and voriconazole formulations (off-label use) are reported to show promising therapeutic effects with few adverse effects, there is no consensus about the dosage regimen (e."( Inhaled Antifungal Agents for the Treatment and Prophylaxis of Pulmonary Mycoses.
Lam, JKW; Liao, Q, 2021
)
0.62
" According to our study, resveratrol can reduce the dosage to 1/64 of ketoconazole as well as itraconazole."( The synergistic antifungal activity of resveratrol with azoles against Candida albicans.
Gao, L; Song, F; Wan, Y; Wang, J; Wang, L; Zhang, L; Zhang, X, 2021
)
0.62
"7 mg/L were achieved on empiric dosing in 49% and 68% respectively."( A novel highly bio-available itraconazole formulation (SUBA®-Itraconazole) for anti-fungal prophylaxis in lung transplant recipients.
Boan, P; Lavender, M; Musk, M; Whitmore, TJ; Wrobel, J; Yaw, M, 2021
)
0.62
" The model was also used to extrapolate pharmacokinetic exposures from older children with different body surface area to guide dosing in younger children."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
0.62
" The model was also verified by the observed pharmacokinetics after multiple oral dosing and by the effect of hepatic impairment on esaxerenone pharmacokinetics."( Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment.
Igawa, Y; Ishizuka, H; Ishizuka, T; Shimizu, T; Watanabe, A; Yamada, M, 2022
)
0.72
" We have summarized the most appropriate dosing regimens of posaconazole, fosravuconazole, voriconazole, and oteseconazole (VT-1161) to treat onychomycosis and superficial fungal infections."( Review of the alternative therapies for onychomycosis and superficial fungal infections: posaconazole, fosravuconazole, voriconazole, oteseconazole.
Gupta, AK; Talukder, M; Venkataraman, M, 2022
)
0.72
" In clinic, adverse drug reactions and toxicity related to crizotinib should be carefully monitored, and therapeutic drug monitoring for crizotinib is recommended to guide dosing and optimize treatment when coadministered with voriconazole, fluconazole, or itraconazole."( Use of Modeling and Simulation to Predict the Influence of Triazole Antifungal Agents on the Pharmacokinetics of Crizotinib.
Chen, L; Chen, W; Li, L, 2022
)
0.72
" When a 200-mg single oral dose of belumosudil was coadministered with both rabeprazole and omeprazole, parent and metabolite exposures were largely reduced, suggesting that belumosudil dosage should be increased when given with PPIs."( A Phase 1 Pharmacokinetic Drug Interaction Study of Belumosudil Coadministered With CYP3A4 Inhibitors and Inducers and Proton Pump Inhibitors.
Alabanza, A; Lohmer, L; Patel, J; Schueller, O; Singh, N; Willson, A, 2022
)
0.72
"Limited research has been performed on the downstream processing of nano-co-crystal suspensions into solid oral dosage forms."( Incorporation of itraconazole nano-co-crystals into multiparticulate oral dosage forms.
Bodmeier, R; Huang, Z; Staufenbiel, S, 2022
)
0.72
" Understanding potential drug-drug interactions (DDIs) informs proper dosing when co-administering tucatinib with other therapies."( Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers.
Abdulrasool, LI; Endres, CJ; Lee, A; Mayor, JG; Rustia, EL; Sun, H; Topletz-Erickson, A; Walker, L, 2022
)
0.72
" However, the dosage of venetoclax is fixed, irrespective of body surface area (BSA) or weight."( Utility of therapeutic drug monitoring of venetoclax in acute myeloid leukemia.
Kobayashi, M; Kosugi, N; Suzaki, K; Yasu, T, 2022
)
0.72
" Most responders did not follow the strategies of voriconazole dosage based on CYP2C19 genotyping."( A survey to describe common practices on antifungal monitoring among Spanish clinicians.
Gómez-López, A; Martín-Gómez, MT; Salavert Lletí, M, 2023
)
0.91
" Interestingly, a substantial reduction in plasma itraconazole concentration was observed during TPE, which was attributed to an insufficient delay between the dosing of itraconazole and TPE initiation."( Effect of Therapeutic Plasma Exchange on Itraconazole Pharmacokinetics: A Case Study.
Girgis, L; Kocic, D; Marriott, DJE; Reuter, SE; Seah, V; Sreeharan, T; Stocker, SL, 2023
)
0.91
" The dog was initially treated with oral itraconazole at a dosage of 10 mg/kg once daily."( Cutaneous protothecosis in a dog successfully treated with oral itraconazole in pulse dosing.
Bacher, LH; Baldasso, G; de Farias, MR; Gmyterco, VC; Jagielski, T; Ribeiro, MG, 2023
)
0.91
"This report highlights the refractoriness of skin infections by Prototheca wickerhamii with therapies proposed in the literature and suggests a new treatment option with oral itraconazole in pulse dosing for long-term disease control successfully performed in a dog with skin lesions."( Cutaneous protothecosis in a dog successfully treated with oral itraconazole in pulse dosing.
Bacher, LH; Baldasso, G; de Farias, MR; Gmyterco, VC; Jagielski, T; Ribeiro, MG, 2023
)
0.91
" These present studies provided valuable information that helps inform SHR0302 dosing instructions and concomitant medication precautions."( Effect of CYP3A4 induction and inhibition on the pharmacokinetics of SHR0302 in healthy subjects.
Feng, S; Fu, M; Gao, X; Li, X; Li, Y; Lin, H; Shen, K; Yu, G; Zhang, P; Zhang, Z, 2023
)
0.91
" We found that an agent's dosage was associated with its efficacy; for example, the 1-year odds of mycological cure with terbinafine 250 mg daily for 24 weeks (SUCRA = 92."( Relative impact of traditional vs. newer oral antifungals for dermatophyte toenail onychomycosis: a network meta-analysis study.
Bamimore, MA; Gupta, AK; Venkataraman, M, 2023
)
0.91
"14); however, a statistically significant difference was noted for OD dosing over BD dosing in achieving clinical cure rates (p<0."( Efficacy of Super-Bioavailable Itraconazole and Conventional Itraconazole at Different Dosing Regimens in Glabrous Tinea Infection - A Randomized Clinical Trial.
Barkate, H; Bhushan, S; Chakraborty, D; Choudhary, A; Das, A; De, A; Dhoot, D; Doshi, Y; Gadkari, R; Gonsalves, N; J, D; Kamat, S; Lahiri, K; Mahadkar, N; Saraswat, A; Sarda, A; Shah, B; Shenoy, MM; Yadav, S, 2023
)
0.91
" over the 12-h dosing interval and for 24 h following the last dose."( Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
Conte, JE; Golden, JA; Krishna, G; Little, E; McIver, M; Zurlinden, E, 2009
)
0.35
" Increasing the standard dosing regimen may have some effect and may be clinically useful if no alternatives are available."( Efficacy of posaconazole against three clinical Aspergillus fumigatus isolates with mutations in the cyp51A gene.
Brüggemann, RJ; Mavridou, E; Melchers, WJ; Mouton, JW; Verweij, PE, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
P450 inhibitorAn enzyme inhibitor that interferes with the activity of cytochrome P450 involved in catalysis of organic substances.
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitorAn EC 3.6.3.* (acid anhydride hydrolase catalysing transmembrane movement of substances) inhibitor that interferes with the action of xenobiotic-transporting ATPase (EC 3.6.3.44).
Hedgehog signaling pathway inhibitorAny pathway inhibitor that inhibits the Hedgehog signalling pathway.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (9)

ClassDescription
triazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.
dioxolane
N-arylpiperazine
dichlorobenzeneAny member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.
cyclic ketalA ketal in the molecule of which the ketal carbon and one or both oxygen atoms thereon are members of a ring.
conazole antifungal drugAny conazole antifungal agent that has been used for the treatment of fungal infections in animals or humans.
triazole antifungal drugAny triazole antifungal agent that has been used for the treatment of fungal infections in humans or animals.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
piperazines
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (75)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency6.00703.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency1.43340.006038.004119,952.5996AID1159521; AID1159523
Fumarate hydrataseHomo sapiens (human)Potency29.56590.00308.794948.0869AID1347053
GALC proteinHomo sapiens (human)Potency0.631028.183828.183828.1838AID1159614
GLI family zinc finger 3Homo sapiens (human)Potency1.50590.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency5.63190.000221.22318,912.5098AID1259243; AID1259247
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency2.98490.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency2.49260.001022.650876.6163AID1224838; AID1224893
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.69180.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.83330.001310.157742.8575AID1259252
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency1.59160.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency2.39140.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency4.57280.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency8.41200.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency2.98490.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency5.56790.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743075; AID743079; AID743080; AID743091
GVesicular stomatitis virusPotency10.96400.01238.964839.8107AID1645842
polyproteinZika virusPotency29.56590.00308.794948.0869AID1347053
activating transcription factor 6Homo sapiens (human)Potency7.56240.143427.612159.8106AID1159516
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency6.007019.739145.978464.9432AID1159509
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency3.78270.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency5.95530.042027.378961.6448AID743210
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency2.07550.000627.21521,122.0200AID743202; AID743219
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency3.75780.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency10.96400.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.96400.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency10.59090.002319.595674.0614AID651631
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency3.75780.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.96400.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.96400.01238.964839.8107AID1645842
Chain A, Beta-lactamaseEscherichia coli K-12Potency6.30960.044717.8581100.0000AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency7.94330.631035.7641100.0000AID504339
TDP1 proteinHomo sapiens (human)Potency2.45190.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency1.97320.180013.557439.8107AID1460
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency2.51190.00137.762544.6684AID914; AID915
67.9K proteinVaccinia virusPotency14.12540.00018.4406100.0000AID720580
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency19.95260.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency2.90930.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.58490.035520.977089.1251AID504332
beta-2 adrenergic receptorHomo sapiens (human)Potency15.84890.00586.026332.6427AID492947
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency2.05960.00419.984825.9290AID504444
mitogen-activated protein kinase 1Homo sapiens (human)Potency14.12540.039816.784239.8107AID1454
gemininHomo sapiens (human)Potency4.84700.004611.374133.4983AID624296; AID624297
DNA polymerase kappa isoform 1Homo sapiens (human)Potency44.66840.031622.3146100.0000AID588579
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency7.89970.005612.367736.1254AID624032; AID624044
lamin isoform A-delta10Homo sapiens (human)Potency4.46680.891312.067628.1838AID1487
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency4.46680.316212.765731.6228AID881
Alpha-synucleinHomo sapiens (human)Potency2.23870.56239.398525.1189AID652106
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency4.46680.00638.235039.8107AID881
TAR DNA-binding protein 43Homo sapiens (human)Potency28.18381.778316.208135.4813AID652104
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)18.00000.11007.190310.0000AID1443980; AID1473738
Tyrosine-protein kinase FynHomo sapiens (human)IC50 (µMol)3.89000.00021.67898.6800AID625185
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)0.70000.06404.012610.0000AID150754; AID681128
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)1.66600.00022.318510.0000AID150752; AID150755; AID679463; AID681122; AID681127
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.42560.00011.753610.0000AID1180169; AID1783793; AID54923; AID625251
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)0.20000.20004.713010.0000AID150753; AID681119
C-X-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)8.50380.00102.022710.0000AID729310; AID729311; AID729312
CruzipainTrypanosoma cruziIC50 (µMol)101.50000.00022.04508.0000AID484274; AID484275
Vasopressin V2 receptorHomo sapiens (human)IC50 (µMol)6.39880.00001.12137.0000AID729307; AID729308; AID729309
C-C chemokine receptor type 4Homo sapiens (human)IC50 (µMol)5.76200.20004.542410.0000AID729298; AID729313; AID729314; AID729315
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)40.00000.00091.901410.0000AID1138338
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50 (µMol)3.60000.05001.43904.0000AID322753
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)2.00000.00401.966610.0000AID1873196
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 144Mycobacterium tuberculosis CDC1551Kd30.20000.36002.59905.3000AID1799791
Steroid C26-monooxygenaseMycobacterium tuberculosis CDC1551Kd30.20000.10002.59676.1000AID1799791
Steroid C26-monooxygenaseMycobacterium tuberculosis CDC1551Kd30.20000.36002.59905.3000AID1799791
Sterol 14-alpha demethylaseAspergillus fumigatus Af293Kd1.01001.01003.03004.7900AID575747
14-alpha sterol demethylase Aspergillus fumigatusKd0.03100.03100.84824.0300AID575755
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC500.19500.19503.667918.6960AID540270
HSP40, subfamily A [Plasmodium falciparum 3D7]Plasmodium falciparum 3D7AbsAC1000_uM0.12900.12904.116911.3160AID540271
heat shock protein 90, putativePlasmodium falciparum 3D7AC500.19500.19504.992098.5000AID540268
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (450)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
response to singlet oxygenTyrosine-protein kinase FynHomo sapiens (human)
neuron migrationTyrosine-protein kinase FynHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusTyrosine-protein kinase FynHomo sapiens (human)
heart processTyrosine-protein kinase FynHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
calcium ion transportTyrosine-protein kinase FynHomo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
axon guidanceTyrosine-protein kinase FynHomo sapiens (human)
learningTyrosine-protein kinase FynHomo sapiens (human)
feeding behaviorTyrosine-protein kinase FynHomo sapiens (human)
regulation of cell shapeTyrosine-protein kinase FynHomo sapiens (human)
gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of hydrogen peroxide biosynthetic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of neuron projection developmentTyrosine-protein kinase FynHomo sapiens (human)
protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
forebrain developmentTyrosine-protein kinase FynHomo sapiens (human)
T cell costimulationTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase FynHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusTyrosine-protein kinase FynHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase FynHomo sapiens (human)
response to ethanolTyrosine-protein kinase FynHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
dendrite morphogenesisTyrosine-protein kinase FynHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
activated T cell proliferationTyrosine-protein kinase FynHomo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase FynHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase FynHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTyrosine-protein kinase FynHomo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase FynHomo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein targeting to membraneTyrosine-protein kinase FynHomo sapiens (human)
dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase FynHomo sapiens (human)
regulation of glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to L-glutamateTyrosine-protein kinase FynHomo sapiens (human)
cellular response to glycineTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to membraneTyrosine-protein kinase FynHomo sapiens (human)
regulation of calcium ion import across plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activityTyrosine-protein kinase FynHomo sapiens (human)
innate immune responseTyrosine-protein kinase FynHomo sapiens (human)
cell differentiationTyrosine-protein kinase FynHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
dendritic cell chemotaxisC-X-C chemokine receptor type 1Homo sapiens (human)
cell surface receptor signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
receptor internalizationC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8-mediated signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
chemokine-mediated signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 1Homo sapiens (human)
immune responseC-X-C chemokine receptor type 1Homo sapiens (human)
neutrophil chemotaxisC-X-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 1Homo sapiens (human)
positive regulation of systemic arterial blood pressureVasopressin V2 receptorHomo sapiens (human)
renal water retentionVasopressin V2 receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVasopressin V2 receptorHomo sapiens (human)
activation of adenylate cyclase activityVasopressin V2 receptorHomo sapiens (human)
hemostasisVasopressin V2 receptorHomo sapiens (human)
positive regulation of cell population proliferationVasopressin V2 receptorHomo sapiens (human)
negative regulation of cell population proliferationVasopressin V2 receptorHomo sapiens (human)
positive regulation of gene expressionVasopressin V2 receptorHomo sapiens (human)
telencephalon developmentVasopressin V2 receptorHomo sapiens (human)
response to cytokineVasopressin V2 receptorHomo sapiens (human)
positive regulation of intracellular signal transductionVasopressin V2 receptorHomo sapiens (human)
cellular response to hormone stimulusVasopressin V2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionVasopressin V2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayVasopressin V2 receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinVasopressin V2 receptorHomo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
tolerance inductionC-C chemokine receptor type 4Homo sapiens (human)
chemotaxisC-C chemokine receptor type 4Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 4Homo sapiens (human)
response to bacteriumC-C chemokine receptor type 4Homo sapiens (human)
homeostasis of number of cellsC-C chemokine receptor type 4Homo sapiens (human)
positive regulation of positive chemotaxisC-C chemokine receptor type 4Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 4Homo sapiens (human)
interneuron migrationC-C chemokine receptor type 4Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 4Homo sapiens (human)
immune responseC-C chemokine receptor type 4Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 4Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
steroid biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
cholesterol biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol metabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein catabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein secretionLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of amyloid-beta clearanceLanosterol 14-alpha demethylaseHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (158)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
protein bindingTyrosine-protein kinase FynHomo sapiens (human)
ATP bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase FynHomo sapiens (human)
enzyme bindingTyrosine-protein kinase FynHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
identical protein bindingTyrosine-protein kinase FynHomo sapiens (human)
alpha-tubulin bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase FynHomo sapiens (human)
transmembrane transporter bindingTyrosine-protein kinase FynHomo sapiens (human)
metal ion bindingTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
tau protein bindingTyrosine-protein kinase FynHomo sapiens (human)
tau-protein kinase activityTyrosine-protein kinase FynHomo sapiens (human)
growth factor receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
scaffold protein bindingTyrosine-protein kinase FynHomo sapiens (human)
disordered domain specific bindingTyrosine-protein kinase FynHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Mus musculus (house mouse)
interleukin-8 receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
chemokine receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8 bindingC-X-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 1Homo sapiens (human)
vasopressin receptor activityVasopressin V2 receptorHomo sapiens (human)
protein bindingVasopressin V2 receptorHomo sapiens (human)
peptide bindingVasopressin V2 receptorHomo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
chemokine receptor activityC-C chemokine receptor type 4Homo sapiens (human)
protein bindingC-C chemokine receptor type 4Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 4Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 4Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
iron ion bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol 14-demethylase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
heme bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenLanosterol 14-alpha demethylaseHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (84)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
nucleusTyrosine-protein kinase FynHomo sapiens (human)
mitochondrionTyrosine-protein kinase FynHomo sapiens (human)
endosomeTyrosine-protein kinase FynHomo sapiens (human)
cytosolTyrosine-protein kinase FynHomo sapiens (human)
actin filamentTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
postsynaptic densityTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
perikaryonTyrosine-protein kinase FynHomo sapiens (human)
cell bodyTyrosine-protein kinase FynHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase FynHomo sapiens (human)
perinuclear endoplasmic reticulumTyrosine-protein kinase FynHomo sapiens (human)
glial cell projectionTyrosine-protein kinase FynHomo sapiens (human)
Schaffer collateral - CA1 synapseTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Mus musculus (house mouse)
plasma membraneC-X-C chemokine receptor type 1Homo sapiens (human)
secretory granule membraneC-X-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 1Homo sapiens (human)
endosomeVasopressin V2 receptorHomo sapiens (human)
endoplasmic reticulumVasopressin V2 receptorHomo sapiens (human)
Golgi apparatusVasopressin V2 receptorHomo sapiens (human)
plasma membraneVasopressin V2 receptorHomo sapiens (human)
membraneVasopressin V2 receptorHomo sapiens (human)
endocytic vesicleVasopressin V2 receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneVasopressin V2 receptorHomo sapiens (human)
perinuclear region of cytoplasmVasopressin V2 receptorHomo sapiens (human)
plasma membraneVasopressin V2 receptorHomo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
plasma membraneC-C chemokine receptor type 4Homo sapiens (human)
neuronal cell bodyC-C chemokine receptor type 4Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 4Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
endoplasmic reticulum membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2253)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1799791Binding Assay from Article 10.1074/jbc.M110.164293: \\Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen.\\2010The Journal of biological chemistry, Dec-03, Volume: 285, Issue:49
Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID371226Antimicrobial activity against Candida albicans ATCC 24433 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID581866Antifungal activity against Candida albicans isolated from HSCT recipient 301 with acute or chronic GVHD mouth after 114 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1076027Antifungal activity against Candida sp. clinical isolate 12341 derived from urine by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID555576Antimicrobial activity against Candida pelliculosa by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555614Antimicrobial activity against Aspergillus glaucus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID467286Antifungal activity against Candida tropicalis by serial dilution method after 24 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of highly potent novel antifungal azoles by structure-based rational design.
AID606218Antifungal activity against Fonsecaea compacta by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID584394Antifungal activity against 8 days cultured Candida krusei isolated from neutropenic subject with AML or MDS pharynx after 12 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1157297Antifungal activity against Microsporum gypseum Cmccfmza assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID555620Antimicrobial activity against Fusarium verticillioides by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID554716Antimicrobial activity against Candida krusei NZCDC 90.147 after 48 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID581898Antifungal activity against Candida glabrata isolated from HSCT recipient 002 with acute or chronic GVHD mouth after 116 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID582253Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS prior to initiation of fluconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID525542Antimicrobial activity against Fonsecaea pedrosoi isolates after 72 hrs by CLSI M38-A2 protocol method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
AID563412Antifungal activity against Aspergillus tubingensis isolate CM-3654 obtained from blood culture after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID563413Antifungal activity against Aspergillus tubingensis isolate CM-4000 after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID515014Antifungal activity against Candida kefyr by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID532162Antifungal activity against Candida glabrata by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID531249Antifungal activity against Candida tropicalis assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID1473925AUC in human at 200 mg, po QD for 1 to 2 weeks after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID249331Minimum inhibitory concentration against Microsporum species (n=38)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID1413326Antifungal activity against Candida pseudotropicalis YOGI2018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID1872520Antifungal activity against Cryptococcus neoformans TIMM 1855 by 96-well microplate method2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID1604175Antileishmanial activity against Leishmania amazonensis MHOM/BR/75/Josefa intracellular amastigotes infected in CF-1 macrophages assessed as reduction in parasite viability after 72 hrs by optical microscopic method2019European journal of medicinal chemistry, Dec-01, Volume: 183Multi-target drugs active against leishmaniasis: A paradigm of drug repurposing.
AID725869Antifungal activity against Rhizomucor pusillus RHMI1 after 48 hrs by broth microdilution test2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID323599Antifungal activity against Candida sp. bloodstream isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates.
AID424635Antimicrobial activity against azole-resistant Candida albicans isolate CA16 cotreated with calcineurin signaling inhibitor Tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1357638Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID1204554Antifungal activity against Candida albicans Strain 24 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID545670Ratio of intracellular to extracellular drug uptake in alveolar macrophages of New Zealand white rabbit infected with Mycobacterium bovis at 1 ug/ml2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Intracellular concentrations of posaconazole in different compartments of peripheral blood.
AID1067048Antifungal activity against Candida albicans SC5314 after 24 hrs by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID527135Antifungal activity against Trichophyton rubrum LMGO 4218 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID1872498Antifungal activity against Candida albicans2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID555579Antimicrobial activity against Candida intermedia by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID341560AUC (0 to 24 hrs) in children of >6-12 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID518602Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID405051Antifungal activity against Sporothrix schenckii PGAC0016 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1689212Antifungal activity against fluconazole-resistant Candida auris 381 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID555618Antimicrobial activity against Fusarium proliferatum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1157293Antifungal activity against Candida glabrata 537 assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID1254070Antibacterial activity against Streptococcus mutans 3065 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID29344Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1419495Antifungal activity against ITC and FLC-susceptible Candida albicans ATCC MYA-2876 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID532146Antifungal activity against Rhizopus oryzae2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID555622Antimicrobial activity against Paecilomyces lilacinus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1413331Antifungal activity against resistant Candida albicans ATCC 641242018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID519450Antimicrobial activity against Aspergillus fumigatus ATCC 2004305 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID555569Antimicrobial activity against Candida glabrata by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1598000Antifungal activity against Microsporum gypseum after 7 days by NCCLS protocol based method2019European journal of medicinal chemistry, May-15, Volume: 170Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
AID525140Antifungal activity against Fusarium moniliforme clade 2 by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID1877280Antifungal activity against Candida albicans CPCC400616 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID283337Antifungal activity against Rhizopus spp after 48 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID584593Antifungal activity against 56 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 172 days after 114 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID468519Antifungal activity against Candida albicans ATCC 10231 after 24 to 72 hrs by NCCLS method2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Synthesis and antimicrobial activities of 3-O-alkyl analogues of (+)-catechin: improvement of stability and proposed action mechanism.
AID581901Antifungal activity against Candida glabrata isolated from HSCT recipient 497 with acute or chronic GVHD mouth receiving antifungal drug after 114 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID609309Antifungal activity against Aspergillus flavus JLC 40437 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID575479Antifungal activity against 10'7 CFU/ml Candida albicans B2630 infected in vulvovaginitis rat model assessed as fungal burden at 5 mg/kg administered tropically twice daily measured after 3 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID432803Antifungal activity against Sporothrix albicans after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID532561Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 0.5 ug/ml (Rvb = 0.144%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID555807Antimicrobial activity against Rhizopus oryzae by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555809Antimicrobial activity against Cunninghamella bertholletiae by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID480477Antifungal activity against Candida krusei after 24 hrs by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID519064Antifungal activity against Candida parapsilosis assessed as resistant isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID547564Antifungal activity against Candida tropicalis after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID555571Antimicrobial activity against Candida guilliermondii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1674374Half life in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID1411888Antifungal activity against Candida krusei ATCC 14243 by M27-A3 guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID48960Tested in vitro for the minimum inhibitory concentration (MIC) against Candida albicans ATCC 645502002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Synthesis of Sordaricin analogues as potent antifungal agents against Candida albicans.
AID1609928Antifungal activity against Candida glabrata assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID1419498Antifungal activity against ITC and FLC-resistant Candida albicans ATCC 1237 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID542417Antimicrobial activity against Aspergillus terreus clinical isolate after 48 hrs by EUCAST test2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activities of various antifungal drugs against Aspergillus terreus: Global assessment using the methodology of the European committee on antimicrobial susceptibility testing.
AID1204522Antifungal activity against Candida lipolytica by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID584392Antifungal activity against 19 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth after 17 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1413328Antifungal activity against Candida rugosa 95-9672018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID555628Antimicrobial activity against Fusarium equiseti by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID245443Minimum inhibitory concentration against Candida albicans V-01-191 evaluated by in vitro agar diffusion and microbroth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID1493827Antifungal activity against Candida albicans SC5314 after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID341547Clearance in children of >6-12 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID584397Antifungal activity against 14 days cultured Candida krusei isolated from neutropenic subject with AML or MDS pharynx after 12 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID532323Antifungal activity against Candida guilliermondii by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID582231Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS receiving posaconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID680076TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling in membranes from MDR1-expressing LLC-PK1 cells1999Biological & pharmaceutical bulletin, Dec, Volume: 22, Issue:12
Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
AID1917560Induction of apoptosis in human A549 cells assessed as viable cells at 30 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 98.2%)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID563387Antifungal activity against Aspergillus niger isolate CM-3236 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID245680In vitro minimal inhibitory concentration against Candida albicans with percentage of resistant strains %R = 25 (MIC > 64 ug/mL) at a range of 0.062-0.25 ug/mL2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antifungal agents. 11. N-substituted derivatives of 1-[(aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole: synthesis, anti-Candida activity, and QSAR studies.
AID736604Antifungal activity against caspofungin-resistant Candida glabrata R assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID518597Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, Q88H mutant gene and by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID542418Antimicrobial activity against Aspergillus terreus environmental isolate after 48 hrs by EUCAST test2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activities of various antifungal drugs against Aspergillus terreus: Global assessment using the methodology of the European committee on antimicrobial susceptibility testing.
AID484274Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-1002010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID519466Antimicrobial activity against Cryptococcus neoformans var. grubii obtained from AIDS patient by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID322855Antifungal activity against azole-resistant Aspergillus fumigatus V27/28-CM3273 isolate from patient by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID1493833Antifungal activity against Microsporum gypseum Cmccfmza after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID323594Antifungal activity against Candida albicans bloodstream isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates.
AID555615Antimicrobial activity against Aspergillus spp. by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID609303Antifungal activity against Candida krusei JLC 30386 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID1595046Antifungal activity against Candida parapsilosis ATCC 22019 assessed as reduction in fungal cell growth incubated for 48 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID555568Antimicrobial activity against Candida tropicalis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555797Antimicrobial activity against Alternaria alternata by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID582797Antifungal activity against Candida albicans isolate 14 by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID405064Antifungal activity against Sporothrix schenckii P3287 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID468517Antifungal activity against Candida krusei IFO 1664 after 24 to 72 hrs by NCCLS method2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Synthesis and antimicrobial activities of 3-O-alkyl analogues of (+)-catechin: improvement of stability and proposed action mechanism.
AID532158Antifungal activity against Curvularia lunata2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID531471Antimicrobial activity against azole-resistant Aspergillus fumigatus harboring Tandem repeat-L98H (TR) mutation in cyp51A gene after 48 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Epidemiological cutoffs and cross-resistance to azole drugs in Aspergillus fumigatus.
AID564271Antifungal activity against Candida albicans isolate 177 after 48 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID405009Antifungal activity against Sporothrix schenckii P0019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID406952Antifungal activity against Candida albicans ATCC 10261 at 35 degC after 48 to 96 hrs by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID419079Antifungal activity against Candida albicans ATCC 645502009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID549310Antifungal activity against Rhizopus oryzae after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID555799Antimicrobial activity against Exophiala dermatitidis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID581873Antifungal activity against Candida glabrata isolated from neutropenic subject 1187 with AML or MDS stool receiving antifungal drug after 22 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID563582Metabolic stability in healthy human plasma assessed as compound recovery at 3 mg/kg QD2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Development, validation, and routine application of a high-performance liquid chromatography method coupled with a single mass detector for quantification of itraconazole, voriconazole, and posaconazole in human plasma.
AID532338Antifungal activity against Rhizopus oryzae by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID532545Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 assessed as accumulation of lanosterol at 8 ug/ml (Rvb = 17+/- 1.22 %)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID547546Antifungal activity against Cryptococcus gattii after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID563608Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as ergosterol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID406950Antifungal activity against Candida parapsilosis ATCC 22019 at 35 degC after 48 hrs by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID1309056Antifungal activity against Aspergillus flavus ATCC MYA-3631 after 48 hrs by CLSI M38-A2 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID555607Antimicrobial activity against Aspergillus nidulans by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1872522Antifungal activity against Aspergillus flavus SANK 18497 by 96-well microplate method2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID283339Antifungal activity against Syncephalastrum spp after 48 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID678776TP_TRANSPORTER: increase in brain concentration in mdr1a(-/-) mouse1998Antimicrobial agents and chemotherapy, Jul, Volume: 42, Issue:7
P-glycoprotein-mediated transport of itraconazole across the blood-brain barrier.
AID484276Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1877282Antifungal activity against Cryptococcus neoformans CGMCC 2.3161 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID535620Antifungal activity against Candida tropicalis T26 blood stream isolate harboring Fks1p LLTLSLRDP mutant protein2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies.
AID555611Antimicrobial activity against Aspergillus ustus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID341558AUC (0 to 24 hrs) in infants of 0.6-2 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID531234Antifungal activity against Candida albicans after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID392422Antifungal activity against Aspergillus fumigatus AF980032009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and structure-activity relationships of 2-phenyl-1-[(pyridinyl- and piperidinylmethyl)amino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID609891Antifungal activity against Candida tropicalis by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID1059366Antifungal activity against Candida albicans after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID555595Antimicrobial activity against Trichosporon jirovecii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555802Antimicrobial activity against Cladosporium spp. by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID532126Antifungal activity against Candida glabrata2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID609314AUC (0 to t) in rat at 10 mg/kg, po administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID546076Antifungal activity against Candida rugosa isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID555818Antifungal activity against cdr1/cdr1 deficient Candida albicans STY19 after 48 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID1889407Cardiotoxicity in zebrafish embryos assessed as pericardial edema at 0.25 uM treated at 6 hpf and measured at 120 hpf by stereomicroscopic analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis.
AID551209Antifungal activity against Trichophyton rubrum by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID563415Antifungal activity against Aspergillus foetidus isolate CM-4002 after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID519433Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4420 obtained from nail of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID249335Minimum inhibitory concentration against Trichophyton tonsurans (n=18)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID284106Antifungal activity against Candida neoformans IM 031631 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID582254Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS receiving fluconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1634359Antifungal activity against Cryptococcus neoformans cgmcc 2.3161 assessed as inhibition of visible microbe growth by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.
AID405099Antimicrobial activity against Rhizomucor sp. after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID555798Antimicrobial activity against Alternaria infectoria by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID565554Antifungal activity against Rhizopus microsporus UTHSC 04-3294 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID1204548Antifungal activity against Candida albicans Strain 18 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID555823Ratio of MIC50 for Candida albicans 5674 to MIC50 for cdr1/cdr1/cdr2/cdr2 deficient Candida albicans STY312009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID584414Antifungal activity against 16 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 31 days after 28 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1265815Antifungal activity against azole-resistant Candida albicans ATCC 64124 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID555601Antimicrobial activity against Trichosporon mycotoxinivorans by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID566883Antifungal activity against Aspergillus fumigates by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID547568Antifungal activity against Candida dubliniensis after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID480478Antifungal activity against Cryptococcus neoformans after 72 hrs by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID1067045Antifungal activity against Aspergillus fumigatus by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID294853Antifungal activity against Trichophyton rubrum after 7 days by microbroth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID125941In vitro evaluation of minimum inhibitory concentration against Microsporum canis 471995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID1743171Antifungal activity against Epidermophyton floccosum2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID701472Antifungal activity against Candida spp2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID1595048Antifungal activity against Candida albicans assessed as reduction in fungal cell growth incubated for 48 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID341569AUC (0 to 24 hrs) in human at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID547566Antifungal activity against Candida parapsilosis after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID519047Antifungal activity against Candida krusei after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID1634361Antifungal activity against Aspergillus fumigatus cgmcc 3.7795 assessed as inhibition of visible microbe growth by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.
AID532157Antifungal activity against Sporothrix schenckii2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1546100Antimicrobial activity against Escherichia coli after 24 hrs by agar disk diffusion method2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID555566Antimicrobial activity against Candida albicans by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID546075Antifungal activity against Candida guilliermondii isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID1204547Antifungal activity against Candida albicans Strain 17 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID518609Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, M172V, L358L, E427K, C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID285855Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.12 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID555592Antimicrobial activity against Trichosporon inkin by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID415954Antimicrobial activity against Microsporum gypseum by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID405016Antifungal activity against Sporothrix schenckii P25013 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID492161Antimicrobial activity against Candida albicans ATCC 66029 at 100 ug/well after 24 hrs at 30 degC by agar diffusion assay2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cellular localization of clathridimine, an antimicrobial 2-aminoimidazole alkaloid produced by the Mediterranean calcareous sponge Clathrina clathrus.
AID1061739Antimicrobial activity against Candida glabrata by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID302122Antifungal activity against fluconazole-resistant Candida albicans 0511655 after 24 hrs2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and antifungal activities of novel 2-aminotetralin derivatives.
AID322543Antifungal activity against Trichophyton mentagrophytes after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID563397Antifungal activity against Aspergillus niger isolate CM-4213 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID341577AUC (0 to 24 hrs) in children of >6-12 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID555801Antimicrobial activity against Hortaea werneckii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID480480Antifungal activity against Aspergillus fumigatus after 7 days by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID484275Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-1002010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID575480Antifungal activity against azole-resistant Aspergillus fumigatus isolate R13 harboring Cyp51A TR/L98H mutant gene assessed as inhibition of fungal growth at 4 mg/l relative to control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID525544Antimicrobial activity against Fonsecaea nubica isolates after 72 hrs by CLSI M38-A2 protocol method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
AID701459Antifungal activity against Trichophyton rubrum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID1076023Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID1689214Antifungal activity against fluconazole-resistant Candida auris 384 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1411889Antifungal activity against Candida glabrata ATCC 34138 by M27-A3 guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID1872499Antifungal activity against Candida tropicalis2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID531236Antifungal activity against Candida parapsilosis after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID602933Antifungal activity against Aspergillus fumigatus by broth microdilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID1898159Antifungal activity against Candida albicans 12#
AID322549Antifungal activity against Microsporum canis after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID518596Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, S52T mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1817557Antifungal activity against Aspergillus fumigatus ATCC 204305 assessed as inhibition of fungal growth incubated for 24 hrs by broth microdilution method2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Identification of Thiazoyl Guanidine Derivatives as Novel Antifungal Agents Inhibiting Ergosterol Biosynthesis for Treatment of Invasive Fungal Infections.
AID322552Antifungal activity against Microsporum sp. after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID284105Antifungal activity against Candida neoformans IM 972751 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID1783793Inhibition of CYP3A4 in human liver microsome using Nifedipine as a substrate incubated for 10 mins in the presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID278905Antifungal activity against Scedosporium apiospermum isolates at 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Prevalence and susceptibility testing of new species of pseudallescheria and scedosporium in a collection of clinical mold isolates.
AID525601Antibacterial activity against Fluconazole resistant Candida albicans DSY3706 containing tac1delta/delta ERG11-1/ERG11-1 genotype by EUCAST standards based broth microdilution method sCandida albicans DSY2942010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID531239Antifungal activity against Candida lusitaniae after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID532954Antifungal activity against Candida albicans isolate V4 with CAI genotype by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
AID1557075Antifungal activity against Candida albicans ATCC 90028 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID283330Antifungal activity against Cunninghamella spp after 24 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID420660Antifungal activity against Candida albicans ATCC 76615 after 24 hrs by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID563406Antifungal activity against Aspergillus tubingensis isolate CM-4005 after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID509111Antifungal activity against 2 x 10'5 CFU Fonsecaea monophora CBS 117236 infected in OF1 mouse assessed as increase in mouse survival at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID563414Antifungal activity against Aspergillus tubingensis isolate CM-4001 after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID581872Antifungal activity against Candida glabrata isolated from neutropenic subject 1187 with AML or MDS stool after 22 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID525597Antibacterial activity against Fluconazole resistant Candida albicans DSY3752 containing (TAC1-5/TAC1-5 ERG11-1/ERG11-1) genotype by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID1783769Antifungal activity against Candida tropicalis GIM2.183 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID555586Antimicrobial activity against Saccharomyces cerevisiae by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID50136Minimum concentration required to inhibit the growth of Candida kefyr2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID1204549Antifungal activity against Candida albicans Strain 19 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID564266Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as obtusifoliol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID283329Antifungal activity against Absidia spp after 48 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID519464Antimicrobial activity against Cryptococcus neoformans var. grubii by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID729315Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID547545Antifungal activity against Cryptococcus neoformans after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID729305Inhibition of vasopressin V2 receptor (unknown origin) assessed as change in intracellular calcium levels incubated with compound treated with Tween-80 by fluorometric analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID575455Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as decreased fungal load in kidney at 50 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated con2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID405019Antifungal activity against Sporothrix schenckii P20825 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID406951Antifungal activity against Candida albicans ATCC 10261 at 35 degC after 48 hrs by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID532552Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 1 ug/ml (Rvb = 0.157%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID518404Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A M220V mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID440319Antifungal activity against Aspergillus niger isolated from patient sputum after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID1783066Antifungal activity against fluconazole-sensitive Candida albicans 0304103 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID558028Antifungal activity against voriconalzole-resistant Aspergillus fumigatus isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Avian Aspergillus fumigatus strains resistant to both itraconazole and voriconazole.
AID1658274Thermodynamic solubility in 0.001N HCl by HPLC analysis
AID1556211Antifungal activity against Candida tropicalis CGMCC 2.3739 assessed as inhibition of visible microbial growth by NCCLS protocol based method2019European journal of medicinal chemistry, Sep-01, Volume: 177Design, synthesis, and structure-activity relationship studies of l-amino alcohol derivatives as broad-spectrum antifungal agents.
AID45502In vivo Evaluation of minimum inhibitory concentration against Candida albicans 4061995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID1071689Cytotoxicity against human PBMC assessed as cell viability after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Antifungal ether diglycosides from Matayba guianensis Aublet.
AID549323Antifungal activity against Rhizomucor variabilis after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID519054Antifungal activity against Penicillium marneffei after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID555577Antimicrobial activity against Candida coliculosa by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID532143Antifungal activity against Absidia corymbifera2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID341554Cmax in human at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID532160Antifungal activity against Rhinocladiella aquaspersa2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID537735Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID575493Antifungal activity against azole-resistant Aspergillus fumigatus isolate T22 harboring Cyp51A TR/L98H mutation assessed as inhibition of fungal growth at 4 mg/l relative to control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID575458Antifungal activity against 5 x 10'6 CFU/ml Trichophyton mentagrophytes B70554 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID37717In vitro evaluation of minimum inhibitory concentration against Aspergillus niger 181995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID555813Antimicrobial activity against Exophiala jeanselmei by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID527137Antifungal activity against Trichophyton rubrum LMGO 08 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID546069Antifungal activity against Candida krusei isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID294851Antifungal activity against Cryptococcus neoformans ATCC BLS108 after 72 hrs by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID525141Antifungal activity against Fusarium moniliforme clade 3 by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID508312Antifungal activity against Aspergillus fumigatus isolate V28-77 harboring M220I mutation in Cyp51A protein by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Efficacy of posaconazole against three clinical Aspergillus fumigatus isolates with mutations in the cyp51A gene.
AID1204539Antifungal activity against Candida albicans Strain 9 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID531254Antifungal activity against Candida albicans assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID39704In vitro evaluation of minimum inhibitory concentration against Aspergillus fumigatus 331995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID436738Antifungal activity against multidrug-resistant Candida albicans after 24 hrs by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID371229Antimicrobial activity against Candida albicans ATCC 64550 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID1524622Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID555590Antimicrobial activity against Trichosporon asahii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID432799Antifungal activity against Sporothrix brasiliensis after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID1223574Inhibition of CYP3A4.16 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID1754263Antifungal activity against Cryptococcus neoformans ATCC 32609 by microplate reader assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41A new sulfated triterpene glycoside from the sea cucumber Colochirus quadrangularis, and evaluation of its antifungal, antitumor and immunomodulatory activities.
AID527133Antifungal activity against Microsporum canis LMGO 22 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1898170Antifungal activity against Candida tropicalis ATCC750
AID1076028Antifungal activity against Candida sp. clinical isolate 300 derived from urine by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID150753Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID262546Antifungal activity against Candida albicans2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID341561AUC (0 to 24 hrs) in adolescents of >12-16 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID531253Antifungal activity against Candida lusitaniae assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID554714Antimicrobial activity against Candida krusei NZCDC 89.102 after 48 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID563395Antifungal activity against Aspergillus niger isolate CM-3672 obtained from cutaneous layer of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1689210Antifungal activity against Candida albicans ATCC 10231 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1076031Antifungal activity against Candida albicans ATCC 66027 by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID532347Antifungal activity against Fusarium solani by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID518613Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A L252L mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID747171Antimicrobial activity against Candida tropicalis ATCC 750 by broth dilution method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Synthesis and antimicrobial activity of novel amphiphilic aromatic amino alcohols.
AID581878Antifungal activity against Candida glabrata isolated from HSCT recipient 186 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID753510Antidermatophytic activity against Epidermophyton floccosum isolate after 7 days by broth microdilution method2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity.
AID584403Antifungal activity against 1 day cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 25 days after 3 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID725871Antifungal activity against Scedosporium sp. SCSP1 after 48 hrs by broth microdilution test2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID1413325Antifungal activity against Cryptococcus neoformans 94-25862018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID551211Antifungal activity against Microsporum gypseum by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID440320Antifungal activity against Aspergillus niger isolated from patient nasal swab after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID1770938Antifungal activity against Candida albicans CPCC400616 assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID555587Antimicrobial activity against Yarrowia lipolytica by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555600Antimicrobial activity against Trichosporon domesticum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1301916Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 10 mins by LC/MS/MS analysis2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID519439Antimicrobial activity against Neosartorya hiratsukae isolate CNM-CM-3303 obtained from skin of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID563419Antifungal activity against Aspergillus tubingensis isolate CM-4899 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID37564Antifungal activity against Aspergillus nidulans CABI 0160037 strain2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Distamycin analogues with enhanced lipophilicity: synthesis and antimicrobial activity.
AID531247Antifungal activity against Candida albicans assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID531470Antimicrobial activity against azole-resistant Aspergillus fumigatus harboring M220V, M220K, M220T and M220I mutation in cyp51A gene after 48 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Epidemiological cutoffs and cross-resistance to azole drugs in Aspergillus fumigatus.
AID1155872Antifungal activity against Candida albicans assessed as growth inhibition after 24 hrs by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID532042Antifungal activity against Lichtheimia ramosa clinical isolate after 48 hrs by EUCAST method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
AID1138338Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
AID555795Antimicrobial activity against Scedosporium apiospermum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID37585Antifungal activity against Aspergillus niger IMI17454 strain.2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Distamycin analogues with enhanced lipophilicity: synthesis and antimicrobial activity.
AID555817Antifungal activity against cdr2/cdr2 deficient Candida albicans STY7 after 48 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID555584Antimicrobial activity against Candida zeylanoides by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID515008Antifungal activity against Candida albicans SC5314 after 24 hrs by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID420665Antifungal activity against Candida krusei by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID555619Antimicrobial activity against Fusarium oxysporum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1783067Antifungal activity against fluconazole-sensitive Candida albicans 7781 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1770932Fungicidal activity against Candida albicans ATCC SC5314 assessed as inhibition of visible fungal growth measured after 48 hrs2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID361270Binding affinity to recombinant CYP3A4 expressed in Escherichia coli assessed as spectral dissociation constant by spectrophotometric equilibrium binding titration method2007The Journal of biological chemistry, Mar-02, Volume: 282, Issue:9
Multiple sequential steps involved in the binding of inhibitors to cytochrome P450 3A4.
AID549326Antifungal activity against Actinomucor spp. after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID1689221Antifungal activity against Cryptococcus neoformans NR41298 assessed as reduction in fungal growth incubated for 48 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID532556Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 4 ug/ml (Rvb = 0.144%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID249314In vitro concentration causing 50% inhibition of Candida albicans with percentage of resistant strains %R = 25 (MIC > 64 ug/mL) at a range of 0.062-0.25 ug/mL2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antifungal agents. 11. N-substituted derivatives of 1-[(aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole: synthesis, anti-Candida activity, and QSAR studies.
AID1783775Antifungal activity against Candida albicans GIM2.194 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1284002Antifungal activity against Mucor hiemalis ATCC 8690 by M38-A protocol-based microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID1301923Antiproliferative activity against HUVEC assessed as inhibition of VEGF induced cell proliferation using methyl-[3H]thymidine after 36 hrs2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID518610Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, M172V, N248T, D255E, E427K mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID532342Antifungal activity against Cunninghamella species by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID606217Antifungal activity against Trichophyton rubrum after 7 days by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID1557083Antifungal activity against Candida guilliermondii T-47 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID405010Antifungal activity against Sporothrix schenckii P0019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID284100Antifungal activity against Candida neoformans IM 983040 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID415951Antimicrobial activity against Candida parapsilosis by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID606214Antifungal activity against Candida tropicalis by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID405011Antifungal activity against Sporothrix schenckii P0019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID533028Antifungal activity against Aspergillus fumigatus ATCC 9197 grown as planktonic cell on CFBE41o cell after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Aspergillus fumigatus forms biofilms with reduced antifungal drug susceptibility on bronchial epithelial cells.
AID584389Antifungal activity against 1 day cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth after 17 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID522129Antimicrobial activity against wild type Candida glabrata TG11 by colorimetric microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Roles of calcineurin and Crz1 in antifungal susceptibility and virulence of Candida glabrata.
AID1872496Antifungal activity against Candida parapsilosis2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID1872507In vivo antifungal activity against Candida albicans infected in CDF1 mouse treated po or iv 2 hrs after infection twice daily for 2 days measured on day 102022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID424631Antimicrobial activity against azole-susceptible Candida albicans isolate CA14 co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID584418Antifungal activity against 62 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 143 days after 116 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID559692Antimicrobial activity against Mycocladus corymbiferus after 24 hrs by broth microdilution checkerboard procedure2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro interactions between antifungals and immunosuppressive drugs against zygomycetes.
AID294854Antifungal activity against Fonsecaea compacta after 7 days by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID48819Tested in vitro for the minimum inhibitory concentration (MIC) against Candida tropicalis ATCC7502002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Synthesis of Sordaricin analogues as potent antifungal agents against Candida albicans.
AID285869Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 1 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID204351Minimum concentration required to inhibit the growth of Sporothrix schenck ii2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID554720Antimicrobial activity against Saccharomyces cerevisiae isolate AD overexpressing Candida krusei ERG11C after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID520618Antifungal activity against Candida parapsilosis by microdilution AFST-EUCAST method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Prevalence and susceptibility profile of Candida metapsilosis and Candida orthopsilosis: results from population-based surveillance of candidemia in Spain.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1204523Antifungal activity against Candida pseudotropicalis by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID341579Cmax in adolescents of >12-16 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID531464Antifungal activity against Candida parapsilosis assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID582232Antifungal activity against Candida krusei isolated from neutropenic subjects with AML or MDS prior to initiation of posaconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID729313Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID555612Antimicrobial activity against Aspergillus niveus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1284001Antifungal activity against Rhizopus oryzae ATCC 10329 by M38-A protocol-based microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID405075Antifungal activity against Sporothrix schenckii isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID314996Antifungal activity against Aspergillus fumigatus AF980032008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.
AID525591Antibacterial activity against Fluconazole resistant Candida albicans DSY296 overexpressing multidrug transporter gene CDR1 and CDR2 and containing ERG11 G464S mutation by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID610070Antifungal activity against Candida parapsilosis JLC 30275 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID525592Antibacterial activity against Fluconazole resistant Candida albicans DSY3083 containing tac1delta/delta genotype by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID1357632Antifungal activity against Candida krusei ATCC 20298 after 48 hrs by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID554933Increase in ERG11 mRNA expression in Candida krusei B2399 at 2 times MIC concentration after 1 hr by hot-phenol extraction based Northern blotting2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID1076029Antifungal activity against Candida sp. clinical isolate 178 derived from high vaginal swabs by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID341548Apparent volume of distribution in children of >6-12 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1549141Antifungal activity against azole-sensitive Cryptococcus neoformans H99 after 72 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID1898177Antifungal activity against Candida auris BS12372
AID572692Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP51 at pH7.52009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae.
AID1820637Antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal growth by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-15, Volume: 228Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.
AID1204531Antifungal activity against Candida albicans Strain 1 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID419076Antifungal activity against Aspergillus fumigatus SANK 105692009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID531238Antifungal activity against Candida krusei after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID249333Minimum inhibitory concentration against Trichophyton species (n=80)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID527145Antifungal activity against Cryptococcus gattii LMGO L1 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID44970Antifungal activity against Candida albicans NCPF 3179 strain; na = not active2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Distamycin analogues with enhanced lipophilicity: synthesis and antimicrobial activity.
AID508311Antifungal activity against Aspergillus fumigatus isolate AZN 8196 harboring wild type Cyp51A protein by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Efficacy of posaconazole against three clinical Aspergillus fumigatus isolates with mutations in the cyp51A gene.
AID1817568Antifungal activity against pan-azole resistant Aspergillus fumigatus SR47013 harbouring Cyp51A Y121F mutant assessed as inhibition of fungal growth incubated for 24 hrs by broth microdilution method2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Identification of Thiazoyl Guanidine Derivatives as Novel Antifungal Agents Inhibiting Ergosterol Biosynthesis for Treatment of Invasive Fungal Infections.
AID729309Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID322547Antifungal activity against Trichophyton sp. after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID371235Antimicrobial activity against Aspergillus fumigatus ATCC 6430 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID319757Antimicrobial activity against Fonsecaea compacta isolates2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID322857Antifungal activity against azole-resistant Aspergillus fumigatus V34/75-CM3276 isolate from patient with hyper-immunoglobulin E syndrome by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID405059Antifungal activity against Sporothrix schenckii P14036 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID340965Antifungal activity against sKloeckera apiculata isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID519430Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4370 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID582250Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS receiving fluconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID319754Antimicrobial activity against Aspergillus fumigatus isolates2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID48248Compound was tested for inherent antifungal geometric minimum inhibitory concentration (GMMIC) against Candida albicans and Candida tropicalis in serial dilution from 64 to 0.0313 ug/mL2002Bioorganic & medicinal chemistry letters, Jul-08, Volume: 12, Issue:13
Synthesis and antifungal activity of the 2,2,5-tetrahydrofuran regioisomers of SCH 51048.
AID1419505Antifungal activity against Aspergillus terreus ATCC MYA-3633 incubated for 48 hrs by CLSI M38-A2 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID736601Antifungal activity against fluconazole-resistant Candida glabrata isolate 6258 assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID575375Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as decreased fungal load in brain at 25 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated cont2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID575376Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as decreased fungal load in kidney at 25 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated con2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID555803Antimicrobial activity against Cladophialophora bantiana by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID419073Antifungal activity against Candida glabrata ATCC 900302009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID1917556Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID285868Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.5 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID319751Antimicrobial activity against Cryptococcus parapsilosis isolates2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID323069Antifungal activity against Cryptococcus neoformans IM 042074 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID575366Antifungal activity against Cunninghamella bertholletiae UTSCH 05-2275 infected in diabetic OF1 mouse assessed as decreased fungal load in lung at 50 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID424626Antimicrobial activity against azole-resistant Candida albicans isolate CA135 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID610068Antifungal activity against Candida albicans JLC 31374 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID1419494Antifungal activity against Candida albicans ATCC 64124 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID729307Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID285866Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.12 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID532152Antifungal activity against Scedosporium apiospermum2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID532388Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 4 ug/ml (Rvb = 0.157%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID547569Antifungal activity against Candida guilliermondii after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID322548Antifungal activity against Epidermophyton floccosum after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID519052Antifungal activity against Fusarium sp. after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID440326Antifungal activity against Aspergillus flavus isolated from patient sputum after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID566888Antifungal activity against Cladophialophora carrionii by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID1917558Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 30 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.316%)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID1284000Antifungal activity against Trichosporon cutaneum ATCC 28592 by M38-A protocol-based microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID405092Antimicrobial activity against Rhizopus sp. after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID532350Antifungal activity against Curvularia lunata by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID535617Antifungal activity against Candida tropicalis T7 blood stream isolate2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies.
AID532159Antifungal activity against Bipolaris australiensis2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID532137Antifungal activity against Geotrichum candidum2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID340951Antifungal activity against Candida albicans isolates from animals by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID1413330Antifungal activity against Candida albicans ATCC 102312018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID531233Antifungal activity against Candida tropicalis after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID566884Antifungal activity against Aspergillus flavus by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID1783063Antifungal activity against fluconazole-resistant Candida tropicalis 3890 assessed as inhibition of fungal growth incubated for 48 hrs by two-fold serial microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID549312Antifungal activity against Mucor circinelloides after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID26380Dissociation constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID582242Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD prior to initiation of fluconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID768336Antifungal activity against Aspergillus flavus ATCC 204304 after 48 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID584416Antifungal activity against 1 day cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 143 days after 116 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405101Antimicrobial activity against Cunninghamella sp. after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID532145Antifungal activity against Rhizopus microsporus var. oligosporus2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID48959Tested in vitro for the minimum inhibitory concentration (MIC) against Candida albicans ATCC 244332002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Synthesis of Sordaricin analogues as potent antifungal agents against Candida albicans.
AID559694Antimicrobial activity against Rhizopus microsporus after 24 hrs by broth microdilution checkerboard procedure2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro interactions between antifungals and immunosuppressive drugs against zygomycetes.
AID609313Tmax in rat at 10 mg/kg, po administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID424632Antimicrobial activity against azole-susceptible Candida albicans isolate CA129 co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1491242Antifungal activity against Candida albicans ATCC SC5314 by broth microdilution method2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
AID575367Antifungal activity against Cunninghamella bertholletiae UTSCH 05-2275 infected in diabetic OF1 mouse assessed as decreased fungal load in kidney at 50 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated contro2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID285852Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.015 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID518608Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, M172V, L358L, E427K, C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID546070Antifungal activity against Candida parapsilosis isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID1301921Antiangiogenic activity against HUVEC assessed as inhibition of total tube junctions at 1 uM after 16 hrs by inverted microscopy2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID1877283Antifungal activity against Candida parapsilosis GIM2.190 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID425136Antimicrobial activity against azole-susceptible Candida albicans isolate CA14 assessed as log reduction in colony count at 1 ug/ml co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by XTT assay2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID278901Antifungal activity against Scedosporium aurantiacum corneal isolate CNM-CM-2923 at 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Prevalence and susceptibility testing of new species of pseudallescheria and scedosporium in a collection of clinical mold isolates.
AID582239Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD prior to initiation of fluconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID176380Efficacy against Candida albicans CY3003 on day 14th after peroral administration in rat2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
AID371231Antimicrobial activity against Candida glabrata ATCC 90030 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID319756Antimicrobial activity against Microsporum gypseum isolates2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID1411893Antifungal activity against Trichosporon cutaneum ATCC 28592 by M38-A guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID555598Antimicrobial activity against Rhodotorula glutinis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID484387Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 2.5 uM by dynamic light scattering assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID555575Antimicrobial activity against Candida famata by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID322859Antifungal activity against azole-resistant Aspergillus fumigatus V34/77-CM3278 isolate from patient with hyper-immunoglobulin E syndrome by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID294850Antifungal activity against Candida tropicalis after 7 days by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID405048Antifungal activity against Sporothrix schenckii P26187 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID525543Antimicrobial activity against Fonsecaea monophora isolates after 72 hrs by CLSI M38-A2 protocol method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
AID340963Antifungal activity against Cryptococcus neoformans ATCC 90112 by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID1141106Antimicrobial activity against Candida albicans ATCC 537Y after 48 hrs by two-fold broth microdilution method2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Exploring 5-nitrofuran derivatives against nosocomial pathogens: synthesis, antimicrobial activity and chemometric analysis.
AID535619Antifungal activity against Candida tropicalis T19 blood stream isolate harboring Fks1p FLTLS/PLRDP mutant protein2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies.
AID575476Antifungal activity against 10'7 CFU/ml Candida albicans B2630 infected in vulvovaginitis rat model assessed as fungal burden at 10 mg/kg, po SID2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID1595071Antifungal activity against Aspergillus flavus NCIM 524 assessed as reduction in fungal cell growth incubated for 3 to 4 days by disk diffusion method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID1770936Anti-biofilm activity in Candida albicans CPCC400616 assessed as inhibition of biofilm formation incubated for 3 hrs by XTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID415950Antimicrobial activity against Cryptococcus neoformans by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID532153Antifungal activity against Penicillium marneffei2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID603347Antifungal activity against Microsporum gypseum clinical isolate by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID633997Antifungal activity against Saccharomyces cerevisiae ATCC 24657 assessed as growth inhibition at 90.7 uM after 24 hrs by spectrophotometric bioassay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID575464Antifungal activity against 5 x 10'6 CFU/ml Candida glabrata B63155 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID546072Antifungal activity against Candida glabrata isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID532156Antifungal activity against Fusarium oxysporum2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID405068Antifungal activity against Candida krusei ATCC 6258 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID519440Antimicrobial activity against Neosartorya hiratsukae isolate CNM-CM-3305 obtained from skin of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID509390Antifungal activity against 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected in po dosed OF1 mouse assessed as reduction in fungal load in lung at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID532328Antifungal activity against Trichosporon asahii by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID509120Antifungal activity against 2 x 10'5 CFU Fonsecaea monophora CBS 117236 infected in po dosed OF1 mouse assessed as reduction in fungal load in spleen at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID510637Antifungal activity against Trichophyton rubrum ATCC 28188 after 24 hrs by AFSTEUCAST assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and biological evaluation of (+)-labdadienedial, derivatives and precursors from (+)-sclareolide.
AID555581Antimicrobial activity against Candida metapsilosis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1411887Antifungal activity against Candida utilis ATCC 9226 by M27-A3 guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID575205Antifungal activity against Cunninghamella echinulata UTHSC 03-3725 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID322544Antifungal activity against Trichophyton tonsurans after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID283206Antimicrobial activity against polyene-resistant Candida glabrata 21229 isolate by E-test2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth.
AID557813Antifungal activity against Aspergillus fumigatus isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Avian Aspergillus fumigatus strains resistant to both itraconazole and voriconazole.
AID484291Colloidal aggregation in phosphate buffer at 50 uM by transmission electron microscopy in presence of 0.5% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID533026Antifungal activity against Aspergillus fumigatus ATCC 9197 grown as planktonic cell on 16HBE cell after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Aspergillus fumigatus forms biofilms with reduced antifungal drug susceptibility on bronchial epithelial cells.
AID518598Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, N125I mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID555602Antimicrobial activity against Trichosporon spp. by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID620355Antifungal activity against Geotrichum candidum RCMB 052006 at 30 ug/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives.
AID1204557Antifungal activity against Candida albicans Strain 27 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID584400Antifungal activity against 35 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 165 days after 138 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID424627Antimicrobial activity against azole-resistant Candida albicans isolate CA137 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID519449Antimicrobial activity against Aspergillus viridinutans isolate CNM-CM-4518 obtained from nail of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1204553Antifungal activity against Candida albicans Strain 23 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID249384In vitro concentration causing 90% inhibition of Candida albicans with percentage of resistant strains %R = 25 (MIC > 64 ug/mL) at a range of 0.062-0.25 ug/mL2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Antifungal agents. 11. N-substituted derivatives of 1-[(aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole: synthesis, anti-Candida activity, and QSAR studies.
AID527136Antifungal activity against Trichophyton rubrum LMGO 06 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID424633Antimicrobial activity against azole-resistant Candida albicans isolate CA10 co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1511963Inhibition of Hedgehog signaling pathway in Sufu-deficient mouse MEF cells assessed as decrease in Gli1 mRNA expression by q-PCR analysis relative to control2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Truncated Itraconazole Analogues Exhibiting Potent Anti-Hedgehog Activity and Improved Drug-like Properties.
AID246930Effective dose was measured in guinea pig infected with Microsporum canis on 21st day2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID549049Antifungal activity against Candida albicans CA132 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID341557Half life in human at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1595073Antifungal activity against Penicillium marneffei assessed as reduction in fungal cell growth incubated for 3 to 4 days by disk diffusion method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID581893Antifungal activity against Candida albicans isolated from HSCT recipient 042 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID584386Antifungal activity against 29 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS pharynx after 48 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID322551Antifungal activity against Microsporum cookei after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID582240Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD prior to initiation of fluconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID736603Antifungal activity against voriconazole-resistant Candida glabrata clinical isolate 724 assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID49980Minimum concentration required to inhibit the growth of Candida glabrata2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID609322Clearance in rat at 10 mg/kg, iv administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID566891Antifungal activity against Exophiala xenobiotica by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID555583Antimicrobial activity against Candida pintolopesii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID565550Antifungal activity against Rhizopus microsporus IHEM 13311 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID575470Cmax in plasma of guinea pig infected with 10'6 CFU Microsporum canis B68128 at 20 mg/kg, po administered 2 hrs before infection for 5 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID1911626Antifungal activity against Aspergillus fumigatus AF293 assessed as fungal growth inhibition by broth microdilution assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Development of Lipo-γ-AA Peptides as Potent Antifungal Agents.
AID1180169Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design and optimization of highly-selective fungal CYP51 inhibitors.
AID555811Antimicrobial activity against Rhizomucor spp.by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID519469Antimicrobial activity against Cryptococcus albidus by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID518603Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing wild type cyp51A gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID575204Antifungal activity against Cunninghamella bertholletiae UTHSC 06-1945 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID555580Antimicrobial activity against Candida inconspicua by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID531252Antifungal activity against Candida krusei assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID565075Antimicrobial activity against Blastoschizomyces capitatus by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Case of fatal Blastoschizomyces capitatus infection occurring in a patient receiving empiric micafungin therapy.
AID415953Antimicrobial activity against Trichophyton rubrum by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID602931Antifungal activity against Cryptococcus neoformans BLS108 after 72 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID405074Antifungal activity against Aspergillus flavus ATCC 204304 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID729311Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID555627Antimicrobial activity against Hormographiella aspergillata by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1351937Ratio of MIC for Candida albicans ATCC 90028 in presence of ergosterol to MIC for Candida albicans ATCC 90028 in absence of ergosterol2018European journal of medicinal chemistry, Feb-10, Volume: 145New 1,5 and 2,5-disubstituted tetrazoles-dependent activity towards surface barrier of Candida albicans.
AID1898171Antifungal activity against Candida krusei 463
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID436740Antifungal activity against Candida albicans after 24 hrs by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID532955Antifungal activity against Candida albicans isolate V5 with CAI genotype by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
AID1059363Antifungal activity against Candida krusei after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID285854Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.06 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID532352Antifungal activity against Rhinocladiella aquaspersa by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID555800Antimicrobial activity against Aureobasidium pullulans by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID119043The compound was tested in vivo for anti-candida activity in mice model 2 (dose 1 mg/kg, fluconazole-treated group); not tested1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID73614In vitro antifungal activity against 6 filamentous fungi1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID1877317Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 4 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID532154Antifungal activity against Penicillium species2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID519283Antifungal activity against Candida krusei ATCC 6258 by WIDERYST method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts.
AID1301917Inhibition of hedgehog pathway in mouse MERP MB cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by qPCR method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID555630Antimicrobial activity against Hormographiella verticillata by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID532128Antifungal activity against Candida krusei2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID582800Antifungal activity against Candida albicans isolate 488 harboring ERG3 H243N, T330A, A351V and ERG11 D225G, E266D, E391G, V488I mutant genes by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID648414Antifungal activity against recultured Trichophyton mentagrophytes by serial plate dilution method2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID532550Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID1783771Antifungal activity against Candida albicans SC5314 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID1898174Antifungal activity against Candida krusei 467
AID563390Antifungal activity against Aspergillus tubingensis isolate CM-3507 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID582228Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS prior to initiation of posaconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1911625Antifungal activity against Mucor racemosus R715 assessed as fungal growth inhibition by broth microdilution assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Development of Lipo-γ-AA Peptides as Potent Antifungal Agents.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1413336Antifungal activity against sensitive Candida parapsilosis2018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID1546102Antimicrobial activity against Klebsiella pneumoniae after 24 hrs by agar disk diffusion method2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID555330Antimicrobial activity against Candida krusei ATCC 6258 by EUCAST broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID323597Antifungal activity against Candida parapsilosis bloodstream isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates.
AID532952Antifungal activity against Candida albicans isolate V2 with CAI genotype by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
AID1609924Antifungal activity against fluconazole-resistant Candida albicans CaR assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID1392807Antifungal activity against Candida albicans ATCC SC5314 after 24 hrs by serial dilution method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
AID1609927Antifungal activity against Candida tropicalis GIM 2.183 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID584601Antifungal activity against 16 days cultured Candida krusei isolated from neutropenic subject with AML or MDS pharynx receiving antifungal therapy for 19 days after 6 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID565556Antifungal activity against Rhizopus microsporus UTHSC 01-983 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID555603Antimicrobial activity against Aspergillus fumigatus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1204527Antifungal activity against Mucor hiemalis ATCC 8690 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1223578Ratio of Ki for CYP3A4.16 (unknown origin) to Ki for CYP3A4.1 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID524737Antimicrobial activity against Fusarium solani after 48 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Species distribution and in vitro antifungal susceptibility patterns of 75 clinical isolates of Fusarium spp. from northern Italy.
AID1415218Anti-angiogenic activity against HUVEC after 24 hrs by scintillation counting based [3H]-thymidine incorporation assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Novel Tetrazole-Containing Analogues of Itraconazole as Potent Antiangiogenic Agents with Reduced Cytochrome P450 3A4 Inhibition.
AID520619Antifungal activity against Candida orthopsilosis by microdilution AFST-EUCAST method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Prevalence and susceptibility profile of Candida metapsilosis and Candida orthopsilosis: results from population-based surveillance of candidemia in Spain.
AID1419496Antifungal activity against ITC and FLC-resistant Candida albicans ATCC MYA-90819 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID1674373Fraction unbound in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID424621Antimicrobial activity against azole-susceptible Candida albicans isolate CA14 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID582230Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS prior to initiation of posaconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID584419Antifungal activity against 85 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 143 days after 116 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID446450Antifungal activity against Aspergillus fumigatus AF980032009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.
AID581895Antifungal activity against Candida albicans isolated from HSCT recipient 928 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1917554Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID1917566Induction of mitochondrial membrane potential loss in human A549 cells assessed as assessed as proportion of MMP decreased cells at 30 uM and measured after 24 hrs by JC-1 staining based flow cytometry assay (Rvb = 7.50%)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID555609Antimicrobial activity against Aspergillus versicolor by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1309047Antifungal activity against Candida albicans ATCC 64124 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1901385Antifungal activity against Candida albicans assessed as inhibition of fungal growth measured after 48 hrs in presence of exogenous ergosterol by M27-A3 based broth microdilution2022European journal of medicinal chemistry, Feb-15, Volume: 230Tetrazole derivatives bearing benzodiazepine moiety-synthesis and action mode against virulence of Candida albicans.
AID532528Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 2 ug/ml (Rvb = 0.157%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID555133Antimicrobial activity against Candida glabrata by EUCAST broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID425156Antimicrobial activity against azole-resistant Candida albicans isolate CA10 assessed as log reduction in colony count at 1 ug/ml co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by time killing test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID609315AUC (0 to t) in rat at 10 mg/kg, iv administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID405111Antimicrobial activity against Absidia corymbifera assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID1059354Antifungal activity against Candida tropicalis clinical isolate after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID563394Antifungal activity against Aspergillus niger isolate CM-3641 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID565555Antifungal activity against Rhizopus microsporus UTHSC 07-371 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID118899In vivo antifungal activity against murine candidosis model after peroral administration with 1 mg/kg for 5 days.(percent protection for 100% mortality with untreated group); not tested1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol.
AID634076Fungistatic activity against Saccharomyces cerevisiae ATCC 24657 assessed as cell proliferation at 90.7 uM after 24 hrs by agar plate bioassay relative to control2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID563411Antifungal activity against Aspergillus niger isolate CM-3551 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1061741Antimicrobial activity against Candida parapsilosis by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID529668Antimicrobial activity against Paecilomyces lilacinus by microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Susceptibility testing and molecular classification of Paecilomyces spp.
AID554719Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Candida albicans ERG11A after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID322858Antifungal activity against azole-resistant Aspergillus fumigatus V34/76-CM3277 isolate from patient with hyper-immunoglobulin E syndrome by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID519049Antifungal activity against Candida tropicalis after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID546074Antifungal activity against Candida dubliniensis isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID609306Antifungal activity against Aspergillus fumigatus JLC 30506 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID547567Antifungal activity against Candida krusei after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID1076034Antifungal activity against Candida tropicalis ATCC 66029 by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID532327Antifungal activity against Trichosporon inkin by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID581864Antifungal activity against 29 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool after 48 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID262550Antifungal activity against Aspergillus fumigatus2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID285875Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID565397Antifungal activity against Rhizopus microsporus FMR 3542 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID214273Minimum concentration required to inhibit the growth of Trichophyton mentagrophytes2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID283232Reduction of fungal burden in Coccidioides immitis Silveira infected po dosed CD1 mouse brain, spinal cord, lung, kidney administered twice daily after 3 days of infection measured after 5 days relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID581904Antifungal activity against Candida glabrata isolated from HSCT recipient 491 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID531241Antifungal activity against Candida glabrata assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID278904Antifungal activity against Scedosporium aurantiacum bronchial aspirate isolate CNM-CM-4183 at 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Prevalence and susceptibility testing of new species of pseudallescheria and scedosporium in a collection of clinical mold isolates.
AID581903Antifungal activity against Candida glabrata isolated from HSCT recipient 807 with acute or chronic GVHD mouth receiving antifungal drug after 114 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID48806Minimum inhibitory concentration of compound for antifungal activity against Candida tropicalis2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID283202Susceptibility of polyene-resistant Candida glabrata 21229 isolate at 8 ug by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth.
AID736606Antifungal activity against fluconazole-resistant Candida albicans clinical isolate 5.O.A assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID549328Antifungal activity against Apophysomyces spp. after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID1061740Antimicrobial activity against Cryptococcus neoformans after 72 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID405113Antimicrobial activity against Apophysomyces elegans assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID519053Antifungal activity against Paecilomyces variotii after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID322542Antifungal activity against Trichophyton rubrum after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID118760In vivo antifungal activity against murine candidosis model after peroral administration with 0.5 mg/kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol.
AID582249Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS prior to initiation of fluconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID525598Antibacterial activity against Fluconazole resistant Candida albicans DSY296 overexpressing multidrug transporter gene CDR1 and CDR2 and containing ERG11 G464S mutation by EUCAST standards based broth microdilution method relative to wildtype sCandida alb2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID519055Antifungal activity against Penicillium sp. after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID323598Antifungal activity against Candida tropicalis bloodstream isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates.
AID527144Antifungal activity against Candida krusei LMGO 174 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID609896Antifungal activity against Aspergillus fumigatus by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID1609931Antifungal activity against fluconazole-resistant Candida albicans 632 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID532127Antifungal activity against Candida parapsilosis2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID519060Antifungal activity against Candida tropicalis assessed as susceptible isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID581869Antifungal activity against Candida glabrata isolated from neutropenic subject 1102 with AML or MDS stool receiving antifungal drug after 26 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1301922Inhibition of hedgehog pathway in mouse Shh-Light2 cells after 46 hrs by luciferase reporter gene assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID582217Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD receiving posaconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID467288Antifungal activity against Trichophyton rubrum by serial dilution method after 7 days2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of highly potent novel antifungal azoles by structure-based rational design.
AID519467Antimicrobial activity against Cryptococcus neoformans var. grubii obtained from non-AIDS patient by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID341563Cmax in infants of 0.6-2 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1420568Inhibition of Smo-mediated hedgehog signaling pathway in mouse Light2 cells in Shh conditioned medium after 48 hrs by Gli-Renilla luciferase reporter gene assay2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Current trends in Hedgehog signaling pathway inhibition by small molecules.
AID522127Antimicrobial activity against Candida glabrata TG172 containing deltacrz1 mutant by colorimetric microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Roles of calcineurin and Crz1 in antifungal susceptibility and virulence of Candida glabrata.
AID1180173Antifungal activity against Trichophyton rubrum by broth macrodilution method2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design and optimization of highly-selective fungal CYP51 inhibitors.
AID1911624Antifungal activity against Mucor racemosus MZ140 assessed as fungal growth inhibition by broth microdilution assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Development of Lipo-γ-AA Peptides as Potent Antifungal Agents.
AID521787Antifungal activity against Candida albicans after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID519465Antimicrobial activity against Cryptococcus neoformans var. grubii clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID405031Antifungal activity against Sporothrix schenckii P24223 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID545165Antimicrobial activity against Candida albicans isolate C after 48 hrs by EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing.
AID19468Partition coefficient (logP)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID582251Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS prior to initiation of fluconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID467287Antifungal activity against Cryptococcus neoformans by serial dilution method after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of highly potent novel antifungal azoles by structure-based rational design.
AID285863Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.015 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID527132Antifungal activity against Microsporum gypseum LMGO 533 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID519065Antifungal activity against Candida tropicalis assessed as resistant isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID572693Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP51 in presence of 0.5 M NaCl at pH7.52009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1595047Antifungal activity against Candida krusei assessed as reduction in fungal cell growth incubated for 48 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID405021Antifungal activity against Sporothrix schenckii P30019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID405045Antifungal activity against Sporothrix schenckii SSA29 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID284101Antifungal activity against Candida neoformans IM 972724 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID531250Antifungal activity against Candida parapsilosis assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID532134Antifungal activity against Cryptococcus neoformans var. gattii2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID549321Antifungal activity against Rhizomucor pusillus after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID283335Antifungal activity against Rhizomucor spp after 48 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID581891Antifungal activity against Candida albicans isolated from HSCT recipient 462 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID563398Antifungal activity against Aspergillus tubingensis isolate CM-4264 obtained from blood culture after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID582218Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD prior to initiation of posaconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID665067Antifungal activity against Candida albicans after 24 hrs by serial dilution method2012European journal of medicinal chemistry, Jul, Volume: 53Design, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains.
AID48962Tested in vitro for the minimum inhibitory concentration (MIC) against Candida albicans TIMM31642002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Synthesis of Sordaricin analogues as potent antifungal agents against Candida albicans.
AID518606Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, L358L, E427K, C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID679612TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM, Itraconazole: 100 uM) in MDR1-expressing LLC-PK1 cells1999Biological & pharmaceutical bulletin, Dec, Volume: 22, Issue:12
Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
AID555866Antimicrobial activity against Beauveria bassiana by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID549319Antifungal activity against Rhizopus microsporus after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID546079Antifungal activity against Candida lipolytica isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID176382Efficacy against Candida tropicalis CY5042 on day 14th after peroral administration in rat2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
AID1265816Antifungal activity against azole-susceptible Candida albicans ATCC MYA-2876 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID555608Antimicrobial activity against Aspergillus sydowii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID575495Antifungal activity against azole-susceptible Aspergillus fumigatus isolate CM-237 by EUCAST microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID602930Antifungal activity against Candida kefyr by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID283331Antifungal activity against Cunninghamella spp after 48 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1898164Antifungal activity against Candida albicans 20#
AID341134Antifungal activity against Saccharomycopsis guttulata isolates from feeding stuff by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID563388Antifungal activity against Aspergillus niger isolate CM-3257 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID150756Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1204519Antifungal activity against Candida albicans ATCC 10231 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1877279Antifungal activity against Candida albicans ATCC SC5314 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID566877Antifungal activity against Candida albicans by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID1204544Antifungal activity against Candida albicans Strain 14 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID546068Antifungal activity against Candida albicans isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID1898165Antifungal activity against Candida albicans 28#
AID541567AUC (0 to 24 hrs) in healthy human alveolar cell at 200 mg, po every 12 hrs for 5 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
AID249332Minimum inhibitory concentration against Trichophyton rubrum (n=14)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID554709Antimicrobial activity against Candida krusei NZCDC 89.221 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID245478Minimum inhibitory concentration against Aspergillus fumigatus LSI-11 evaluated by in vitro agar diffusion and microbroth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID416040Fungicidal activity against tebuconazole-nonadapted wild type Colletotrichum graminicola CgM2 assessed as inhibition of radial growth rate at 23 degC in darkness2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Treatment of a clinically relevant plant-pathogenic fungus with an agricultural azole causes cross-resistance to medical azoles and potentiates caspofungin efficacy.
AID531251Antifungal activity against Candida guilliermondii assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID405049Antifungal activity against Sporothrix schenckii P26187 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID119044The compound was tested in vivo for anti-candida activity in mice model 2 (dose 1 mg/kg, untreated group); not tested1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID518400Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A G54W mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID532046Antifungal activity against Lichtheimia ornata clinical isolate after 48 hrs by EUCAST method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
AID519429Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4330 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID125957In vitro evaluation of minimum inhibitory concentration against Microsporum gypseum 221995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID527140Antifungal activity against Candida albicans LMGO 102 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID532125Antifungal activity against Candida albicans2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID532322Antifungal activity against Candida tropicalis by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID283231Reduction of fungal burden in Coccidioides immitis Silveira infected CD1 mouse brain, spinal cord and lungs administered after 3 days of infection at 25 mg/kg, po bid after 12 days relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID405066Antifungal activity against Candida krusei ATCC 6258 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID546073Antifungal activity against Candida tropicalis isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID1594793Antifungal activity against Histoplasma capsulatum G217B after 10 to 14 days by microscopic method2019Journal of natural products, 06-28, Volume: 82, Issue:6
Secondary Metabolites of Onygenales Fungi Exemplified by Aioliomyces pyridodomos.
AID555567Antimicrobial activity against Candida parapsilosis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID554715Antimicrobial activity against Candida krusei NZCDC 89.221 after 48 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID555135Antimicrobial activity against Candida albicans by EUCAST broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID1754264Antifungal activity against clinical strain Candida tropicalis by microplate reader assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41A new sulfated triterpene glycoside from the sea cucumber Colochirus quadrangularis, and evaluation of its antifungal, antitumor and immunomodulatory activities.
AID1484674Antileishmanial activity against wild type Leishmania major LV39 Rho/SU/59/P promastigote forms after 48 hrs2017European journal of medicinal chemistry, Jul-28, Volume: 135An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy.
AID341581AUC (0 to 24 hrs) in adolescents of >12-16 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID563611Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as ergosta 5,7-dienol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID549329Antifungal activity against Apophysomyces spp. after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID555597Antimicrobial activity against Ustilago spp by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID527141Antifungal activity against Candida parapsilosis ATCC 22019 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID405095Antimicrobial activity against Rhizopus microsporus var. rhizopodiformis after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID283328Antifungal activity against Absidia spp after 24 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID566890Antifungal activity against Exophiala oligosperma by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID609304Antifungal activity against Cryptococcus neoformans JLC 50122 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID575068Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as increase in mouse survival rate at 20 mg/kg, po qd administered 1 day after infection for 7 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID525599Antibacterial activity against Fluconazole resistant Candida albicans DSY3083 containing tac1delta/delta genotype by EUCAST standards based broth microdilution method sCandida albicans DSY2942010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID509548Antagonist activity at hedgehog receptor2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Modulators of the hedgehog signaling pathway.
AID214268In vitro evaluation of minimum inhibitory concentration against Trichophyton mentagrophytes 231995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID606219Antifungal activity against Microsporum gypseum after 7 days by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID1204542Antifungal activity against Candida albicans Strain 12 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID532548Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 assessed as accumulation of ergosterol at 8 ug/ml (Rvb = 57+/- 1.00 %)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID419072Antifungal activity against fluconazole-resistant Candida albicans TIMM31642009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID283234Antifungal activity against Coccidioides immitis by broth macrodilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID563399Antifungal activity against Aspergillus tubingensis isolate CM-4296 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1254068Antibacterial activity against Staphylococcus aureus 209 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID725876Antifungal activity against Aspergillus fumigatus ASFU7 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID725872Antifungal activity against Aspergillus fumigatus ASFU23 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID564270Antifungal activity against Candida albicans isolate 14 after 48 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID289592Antifungal activity against Trichophyton mentagrophytes by serial plate dilution method2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Synthesis of some bioactive 2-bromo-5-methoxy-N'-[4-(aryl)-1,3-thiazol-2-yl]benzohydrazide derivatives.
AID1330312Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity at 100 uM preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID582234Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS prior to initiation of posaconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID519468Antimicrobial activity against Cryptococcus gattii by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID583000Antimicrobial activity against Saccharomyces cerevisiae YUG37 transformed with plasmid carrying cyp51A gene in reverse orientation without doxycycline-regulatable promoter by broth dilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Complementation of a Saccharomyces cerevisiae ERG11/CYP51 (sterol 14α-demethylase) doxycycline-regulated mutant and screening of the azole sensitivity of Aspergillus fumigatus isoenzymes CYP51A and CYP51B.
AID582226Antifungal activity against Candida krusei isolated from HSCT recipients with acute or chronic GVHD prior to initiation of posaconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID150754Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID531237Antifungal activity against Candida guilliermondii after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID323070Antifungal activity against Cryptococcus neoformans IM 983036 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID609890Antifungal activity against Candida albicans Y0109 by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID1301913Inhibition of hedgehog pathway in mouse ASZ cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by qPCR method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID1175555Antimicrobial activity against Aspergillus niger SNB-AF1 after 24 hrs2015Journal of natural products, Jan-23, Volume: 78, Issue:1
Antibacterial ilicicolinic acids C and D and ilicicolinal from Neonectria discophora SNB-CN63 isolated from a termite nest.
AID634072Antifungal activity against Saccharomyces cerevisiae ATCC 24657 assessed as growth at 90.7 uM after 48 hrs by agar plate bioassay relative to control2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID525602Antibacterial activity against Fluconazole resistant Candida albicans DSY3606 containing tac1delta/delta ERG11-1/ERG11-1 (TAC1-5) genotype by EUCAST standards based broth microdilution method sCandida albicans DSY2942010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID249329Minimum inhibitory concentration against Candida species (n=24)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID521969Antibacterial activity against Fluconazole resistant Candida albicans DSY3608 containing tac1delta/delta ERG11-1/ERG11-1 (TAC1-1) genotype by EUCAST standards based broth microdilution method sCandida albicans DSY2942010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID582238Antifungal activity against Candida krusei isolated from neutropenic subjects with AML or MDS prior to initiation of posaconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID531244Antifungal activity against Candida guilliermondii assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID603259Antifungal activity against Candida albicans ATCC Y0109 after 24 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID50131In vitro evaluation of minimum inhibitory concentration against Candida guilliermondii 261995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID622012Inhibition of VEGFR2 glycosylation in human HUVEC cells at 2 uM after 24 hrs by Western blot analysis2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling.
AID532335Antifungal activity against Absidia corymbifera by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID436741Antifungal activity against Cryptococcus neoformans after 72 hrs by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID543973Half life in human at 15 mg, po pretreated with itraconazole at 200 mg, po qd for 4 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Voriconazole increases while itraconazole decreases plasma meloxicam concentrations.
AID405055Antifungal activity against Sporothrix schenckii PJRC002 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1689222Antifungal activity against Cryptococcus neoformans NR41300 assessed as reduction in fungal growth incubated for 48 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID405012Antifungal activity against Sporothrix schenckii PSSA81 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID525541Antimicrobial activity against Fonsecaea isolates after 72 hrs by CLSI M38-A2 protocol method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
AID1783777Antifungal activity against Candida parapsilosis GIM2.190 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID549325Antifungal activity against Cunninghamella spp. after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID1557082Antifungal activity against Candida parapsilosis ATCC 22019 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID405093Antimicrobial activity against Rhizopus arrhizus after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID1493829Antifungal activity against Candida glabrata 537 after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID554722Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Saccharomyces cerevisiae ERG11 to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID532320Antifungal activity against Candida krusei by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID610067Antifungal activity against Candida albicans JLC 30364 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID554721Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Candida krusei ERG11g after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID1059364Antifungal activity against Candida parapsilosis after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID603260Antifungal activity against Candida parapsilosis clinical isolate by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID563613Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as 14 -Methylergosta-8,24(28)-dien-3beta,6alpha-diol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID1309057Antifungal activity against Aspergillus nidulans ATCC 38163 after 48 hrs by CLSI M38-A2 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1557079Antifungal activity against Candida glabrata ATCC 2001 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID1898179Antifungal activity against Candida auris D12
AID1689226Antifungal activity against Aspergillus fumigatus NR 35303 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1223571Inhibition of CYP3A4.1 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID322863Antifungal activity against azole-resistant Aspergillus fumigatus V48/27-CM3936 isolate from patient with acute myeloid leukemia by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID341565AUC (0 to 24 hrs) in infants of 0.6-2 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1917561Antiproliferative activity against human A549 cells assessed as inhibition of clone formation at 10 uM incubated for 1 day followed by culture in new medium for 7 days by crystal violet staining based assay relative to control2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID37739Compound was tested for inherent antifungal geometric minimum inhibitory concentration (GMMIC) against Aspergillus in serial dilution from 64 to 0.0313 ug/mL2002Bioorganic & medicinal chemistry letters, Jul-08, Volume: 12, Issue:13
Synthesis and antifungal activity of the 2,2,5-tetrahydrofuran regioisomers of SCH 51048.
AID1357636Antifungal activity against Cryptococcus neoformans ATCC 24067 after 72 hrs by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID582799Antifungal activity against Candida albicans isolate 12 harboring ERG3 W332R mutant gene by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID1898168Antifungal activity against Candida parapsilosis 700
AID1413329Antifungal activity against Candida tropicalis 95-412018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID729308Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID581899Antifungal activity against Candida glabrata isolated from HSCT recipient 002 with acute or chronic GVHD mouth receiving antifungal drug after 116 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID584600Antifungal activity against 16 days cultured Candida krusei isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 19 days after 6 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID609311Solubility of the compound in water at pH 7.42011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID582219Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD receiving posaconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID582224Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD prior to initiation of posaconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID497819Antifungal activity against Fusarium sp. clinical isolates after 48 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of thimerosal against ocular pathogenic fungi.
AID1917555Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID564272Antifungal activity against Candida albicans isolate 108 harboring erg11 and erg5 double mutant after 48 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID584401Antifungal activity against 60 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 75 days after 33 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID436739Antifungal activity against Candida tropicalis after 24 hrs by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID622013Ratio of itraconazole IC50 to compound IC50 for antiproliferative activity against mouse Ptch+/- p53-/- medulloblastoma cells isolated from allografts in nude Harlan mouse after 96 hrs2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling.
AID341580Tmax in adolescents of >12-16 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID405109Antimicrobial activity against Rhizomucor sp. assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID546078Antifungal activity against Candida kefyr isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID245449Minimum inhibitory concentration against Candida glabrata ATCC 90030 evaluated by in vitro agar diffusion and microbroth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID634074Fungistatic activity against Saccharomyces cerevisiae ATCC 24657 assessed as cell proliferation at 90.7 uM after 24 hrs by spectrophotometric bioassay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID432800Antifungal activity against Sporothrix schenckii after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID1877315Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 4 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID519470Antimicrobial activity against Cryptococcus albidosimilis by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
AID582227Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD receiving fluconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID531872Antifungal activity against Scedosporium apiospermum isolated from voriconazole treated scedosporiosis patient by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Treatment of scedosporiosis with voriconazole: clinical experience with 107 patients.
AID283332Antifungal activity against Mucor spp after 24 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID432801Antifungal activity against Sporothrix globosa after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID753515Antidermatophytic activity against Trichophyton mentagrophytes var. erinacei NCPF 375 after 7 days by broth microdilution method2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity.
AID532332Antifungal activity against Aspergillus flavus by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID584588Antifungal activity against -2 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 168 days after 113 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID249266Minimum inhibitory concentration against Microsporum species (n=38)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID555599Antimicrobial activity against Cryptococcus laurentii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID519051Antifungal activity against Curvularia species after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID532527Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 16 ug/ml (Rvb = 0.157%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID648418Antifungal activity against Aspergillus fumigatus NCIM 902 by serial plate dilution method2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID323073Antifungal activity against Cryptococcus neoformans IM 031631 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID424625Antimicrobial activity against azole-resistant Candida albicans isolate CA16 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1059350Fungicidal activity against Candida albicans clinical isolate by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID1877304Antibiofilm activity against FLC-resistant Candida albicans CPCC400616 assessed as assessed as inhibition of biofilm formation measured at 3 hrs by XTT reduction assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID575496Antifungal activity against Aspergillus niger isolate2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID323074Antifungal activity against Cryptococcus neoformans IM 031706 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID341572Tmax in children of >2-6 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1428258Antifungal activity against Syncephalastrum racemosum 005004 assessed as zone of inhibition at 30 ug/ml2017European journal of medicinal chemistry, Jan-27, Volume: 126An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
AID1411890Antifungal activity against Candida parapsilosis ATCC 22019 by M27-A3 guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID555134Antimicrobial activity against Candida glabrata by CLSI M27-A2 broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID532341Antifungal activity against Mucor species by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID563417Antifungal activity against Aspergillus tubingensis isolate CM-4352 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID565401Antifungal activity against Rhizopus microsporus IHEM 9503 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID1898176Antifungal activity against Candida auris 791
AID515010Antifungal activity against Cryptococcus neoformans after 72 hrs by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID582225Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD receiving posaconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID532147Antifungal activity against Rhizopus species2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID322865Antifungal activity against azole-resistant Aspergillus fumigatus V49/77-CM4050 isolate from patient with acute myeloid leukemia by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID555591Antimicrobial activity against Rhodotorula mucilaginosa by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1411894Antifungal activity against Rhizopus oryzae ATCC 10329by M38-A guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID509098Antifungal activity against Fonsecaea monophora CBS 269.372010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID549044Antifungal activity against Candida albicans CA1 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID532560Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 1 ug/ml (Rvb = 0.144%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID543974Tmax in human at 15 mg, po pretreated with itraconazole at 200 mg, po qd for 4 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Voriconazole increases while itraconazole decreases plasma meloxicam concentrations.
AID323595Antifungal activity against Candida glabrata bloodstream isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates.
AID603346Antifungal activity against Fonsecaea compacta clinical isolate by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID405023Antifungal activity against Sporothrix schenckii P30019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID555621Antimicrobial activity against Paecilomyces variotii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID532140Antifungal activity against Aspergillus flavus2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID549316Antifungal activity against Cunninghamella bertholletiae after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID302758Solubility by shake flask method2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Poorly soluble marketed drugs display solvation limited solubility.
AID322861Antifungal activity against azole-resistant Aspergillus fumigatus V41/26-CM3820 isolate from patient with pulmonary fibrosis by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID701455Antifungal activity against Cryptococcus neoformans2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID747169Antimicrobial activity against Candida glabrata ATCC 18804 by broth dilution method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Synthesis and antimicrobial activity of novel amphiphilic aromatic amino alcohols.
AID405022Antifungal activity against Sporothrix schenckii P30019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID405077Antifungal activity against Sporothrix schenckii isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID582802Antifungal activity against Candida albicans isolate 1008 harboring ERG3 K97E, L193P, V237A, A351V, A353T and ERG11 E266D mutant genes by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID405038Antifungal activity against Sporothrix schenckii P24255 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID341553Half life in adolescents of >12-16 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID340953Antifungal activity against Candida glabrata isolates from feeding stuffs by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID546080Antifungal activity against Candida pulcherrima isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID563612Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as 14 -Methylergosta-8,24(28)-dien-3beta,6alpha-diol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID1904357Antifungal activity against Candida albicans CPCC400616 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID1164090Antifungal activity against Candida albicans ATCC 18804 by broth microdilution method2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents.
AID1743167Antifungal activity against Trichophyton gypseum2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID424628Antimicrobial activity against azole-susceptible Candida albicans isolate CA5 co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID610071Antifungal activity against Candida krusei JLC 30366 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID619761Antifungal activity against Candida albicans RCMB 052002 at 30 mg/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Design and synthesis of some new thiophene, thienopyrimidine and thienothiadiazine derivatives of antipyrine as potential antimicrobial agents.
AID1820640Antifungal activity against Cryptococcus neoformans GIM 2.209 assessed as inhibition of fungal growth by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-15, Volume: 228Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.
AID549052Antifungal activity against Candida albicans CA137 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID1204520Antifungal activity against Candida tropicalis ATCC 13803 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1917553Inhibition of hedgehog signalling pathway in human A549 cells assessed as reduction in Gli gene expression incubated for 24 hrs by qPCR analysis2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID510636Antifungal activity against Trichophyton mentagrophytes ATCC 24198 after 24 hrs by AFSTEUCAST assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and biological evaluation of (+)-labdadienedial, derivatives and precursors from (+)-sclareolide.
AID406959Antifungal activity against dermatophytes at 28 degC after 7 days by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID555624Antimicrobial activity against Scopulariopsis brevicaulis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1059349Fungicidal activity against Candida tropicalis clinical isolate by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID1301914Antiproliferative activity against HUVEC assessed as inhibition of VEGF induced cell proliferation after 72 hrs by MTS assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID555804Antimicrobial activity against Scytalidium hyalinum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1204543Antifungal activity against Candida albicans Strain 13 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID555810Antimicrobial activity against Rhizopus microsporus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID415955Antimicrobial activity against Aspergillus fumigatus by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID1589575Substrate activity at BCRP in human Caco2 cells assessed as efflux ratio by LC-MS/MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID527138Antifungal activity against Trichophyton mentagrophytes LMGO 1931 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID655584Antifungal activity against Candida tropicalis by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID1223573Inhibition of CYP3A4.7 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID519423Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-3134 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID531235Antifungal activity against Candida glabrata after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID531874Antifungal activity against Scedosporium prolificans isolated from voriconazole treated scedosporiosis patient by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Treatment of scedosporiosis with voriconazole: clinical experience with 107 patients.
AID1428256Antifungal activity against Aspergillus fumigatus RCMB 002006 assessed as zone of inhibition at 30 ug/ml2017European journal of medicinal chemistry, Jan-27, Volume: 126An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
AID575751Antimicrobial activity against sterol 14-alpha demethylase isoenzyme B-deficient Aspergillus fumigatus CEA102010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
AID341582Half life in adolescents of >12-16 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID555629Antimicrobial activity against Fusarium reticulatum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID582216Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD prior to initiation of posaconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID49633Minimum concentration required to inhibit the growth of Candida albicans 22000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID602929Antifungal activity against Candida parapsilosis by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID1689211Antifungal activity against fluconazole-resistant Candida albicans NR29448 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1204551Antifungal activity against Candida albicans Strain 21 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID582246Antifungal activity against Candida krusei isolated from HSCT recipients with acute or chronic GVHD receiving fluconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID531246Antifungal activity against Candida lusitaniae assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID1419502Antifungal activity against Candida parapsilosis ATCC 22019 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID436742Antifungal activity against Trichophyton rubrum after 7 days by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID341578Half life in children of >6-12 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID555625Antimicrobial activity against Trichoderma spp. by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1254074Antibacterial activity against Pseudomonas aeruginosa 2004 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1254071Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID582221Antifungal activity against Candida krusei isolated from HSCT recipients with acute or chronic GVHD receiving posaconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405107Antimicrobial activity against Mucor sp. after assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID284099Antifungal activity against Candida neoformans ATCC 32264 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID1477763Antifungal activity against drug resistant Candida albicans DF2672R after 24 hrs by two fold serial dilution method2017Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
Semisynthesis and Biological Evaluation of Xanthone Amphiphilics as Selective, Highly Potent Antifungal Agents to Combat Fungal Resistance.
AID1689217Antifungal activity against Candida parapsilosis ATCC 22019 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID176376Efficacy against Aspergillosis fumigatus CY1003 on day 14th after peroral administration in rat2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
AID665072Antifungal activity against Trichophyton rubrum by serial dilution method2012European journal of medicinal chemistry, Jul, Volume: 53Design, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains.
AID565552Antifungal activity against Rhizopus microsporus UTHSC R-3466 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID545671Ratio of intracellular to extracellular drug uptake in RBC of New Zealand white rabbit infected with Mycobacterium bovis at 1 ug/ml2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Intracellular concentrations of posaconazole in different compartments of peripheral blood.
AID1589583Permeability of the compound after 5 hrs by PAMPA2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID1872506In vivo antifungal activity against Candida albicans infected in CDF1 mouse treated po or iv immediately after infection measured on day 72022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID1609926Antifungal activity against Candida albicans GIM 2.194 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID555593Antimicrobial activity against Trichosporon ovoides by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555596Antimicrobial activity against Cryptococcus albidus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1164092Antifungal activity against Candida glabrata ATCC 90030 by broth microdilution method2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents.
AID1549138Antifungal activity against azole-resistant Candida albicans 7781 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID519422Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-1290 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID524736Antimicrobial activity against Fusarium verticillioides after 48 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Species distribution and in vitro antifungal susceptibility patterns of 75 clinical isolates of Fusarium spp. from northern Italy.
AID532537Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as accumulation of ergosterol at 8 ug/ml (Rvb = 54+/- 0.82 %)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID547353Antifungal activity against Candida lusitaniae after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID214430Minimum inhibitory concentration of compound for antifungal activity against Trichophyton rubrum2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID701462Antifungal activity against Candida parapsilosis2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID655581Antifungal activity against Candida albicans Y0109 after 24 hrs by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID1754262Antifungal activity against Candida albicans ATCC 76615 by microplate reader assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41A new sulfated triterpene glycoside from the sea cucumber Colochirus quadrangularis, and evaluation of its antifungal, antitumor and immunomodulatory activities.
AID619767Antifungal activity against Syncephalastrum racemosum RCMB 052003 at 30 mg/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Design and synthesis of some new thiophene, thienopyrimidine and thienothiadiazine derivatives of antipyrine as potential antimicrobial agents.
AID753514Antidermatophytic activity against Trichophyton mentagrophytes var. erinacei isolate after 7 days by broth microdilution method2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity.
AID1309051Antifungal activity against Candida albicans ATCC MYA-1237 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1076022Cytotoxicity against human HT1080 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID405067Antifungal activity against Candida krusei ATCC 6258 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1674377Unbound AUC at steady state in human administered as single dose2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID549047Antifungal activity against Candida albicans CA4 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID1904362Antifungal activity against Candida krusei GIM 2.1 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID442519Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by microbroth dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID340959Antifungal activity against Candida parapsilosis ATCC 22013 by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID581879Antifungal activity against Candida glabrata isolated from HSCT recipient 186 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID415948Antimicrobial activity against Candida krusei by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID581870Antifungal activity against Candida glabrata isolated from neutropenic subject 1318 with AML or MDS stool after 36 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID554727Inhibition of Candida krusei ABC1 expressed in Saccharomyces cerevisiae isolate ADdelta at 0.36 nM2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID509122Antifungal activity against 2 x 10'5 CFU Fonsecaea monophora CBS 117236 infected in po dosed OF1 mouse assessed as reduction in fungal load in brain at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID519436Antimicrobial activity against Aspergillus fumisynnematus isolate CNM-CM-4063 obtained from bronchoalveolar aspirate of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID519427Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-3583 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID214426Minimum concentration required to inhibit the growth of Trichophyton rubrum2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID519046Antifungal activity against Candida glabrata after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID725870Antifungal activity against Rhizomucor pusillus RHPU1 after 48 hrs by broth microdilution test2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID533030Antifungal activity against Aspergillus fumigatus ATCC 9197 grown as planktonic cell on polystyrene after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Aspergillus fumigatus forms biofilms with reduced antifungal drug susceptibility on bronchial epithelial cells.
AID1076030Antifungal activity against Candida sp. clinical isolate 11972 derived from high vaginal swabs by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID283226Effect on fungal burdens in Coccidioides immitis Silveira infected CD1 mouse brain administered after 3 days of infection at 50 mg/kg, po bid after 12 days2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID532330Antifungal activity against Aspergillus fumigatus by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1689828Antifungal activity against Fusarium sp. assessed as reduction in microbial growth after 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID341562AUC (0 to 24 hrs) in human at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1556210Antifungal activity against Cryptococcus neoformans CGMCC 2.3161 assessed as inhibition of visible microbial growth by NCCLS protocol based method2019European journal of medicinal chemistry, Sep-01, Volume: 177Design, synthesis, and structure-activity relationship studies of l-amino alcohol derivatives as broad-spectrum antifungal agents.
AID622014Inhibition of hedgehog signaling pathway in mouse Ptch+/- p53-/- medulloblastoma cells assessed as inhibition of receptor-mediated Gli1 transcriptional activity at antiproliferative IC90 concentration after 24 hrs by RT-PCR analysis relative to control2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling.
AID1689219Antifungal activity against Candida krusei CAB 396420 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1484676Antileishmanial activity against Leishmania major LV39 Rho/SU/59/P promastigote forms harboring C14DM null mutant after 48 hrs2017European journal of medicinal chemistry, Jul-28, Volume: 135An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy.
AID55045Minimum concentration required to inhibit the growth of Cryptococcus neoformans2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID565404Antifungal activity against Rhizopus microsporus IHEM 5234 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID406960Antifungal activity against dermatophytes at 35 degC after 48 to 96 hrs by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID341566Half life in infants of 0.6-2 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1415219Inhibition of human liver microsome CYP3A4 at 1 uM expressed in baculosomes using fluorogenic-DBOMF as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by fluorescence based assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Novel Tetrazole-Containing Analogues of Itraconazole as Potent Antiangiogenic Agents with Reduced Cytochrome P450 3A4 Inhibition.
AID554708Antimicrobial activity against Candida krusei NZCDC 89.102 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID532044Antifungal activity against Lichtheimia corymbifera clinical isolate after 48 hrs by EUCAST method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
AID546071Antifungal activity against Clavispora lusitaniae isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID729312Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID1204534Antifungal activity against Candida albicans Strain 4 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID405025Antifungal activity against Sporothrix schenckii P14954 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID575207Antifungal activity against Cunninghamella echinulata FMR 10973 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID555613Antimicrobial activity against Aspergillus sclerotiorum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID541563Cmax in healthy human lung epithelial lining fluid assessed as hydroxyitraconazole at 200 mg, po every 12 hrs for 5 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
AID480476Antifungal activity against Candida parapsilosis after 24 hrs by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID1663762Antifungal activity against Paracoccidioides brasiliensis Pb182020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Synthesis and antifungal activity of new hybrids pyrimido[4,5-d]pyridazinone-N-acylhydrazones.
AID555582Antimicrobial activity against Candida orthopsilosis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555605Antimicrobial activity against Aspergillus flavus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1877314Cytotoxicity against human HEK293T cells assessed as inhibition of cell growth incubated for 4 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID1309054Antifungal activity against Candida krusei ATCC 6258 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1419503Antifungal activity against Aspergillus flavus ATCC MYA-3631 incubated for 48 hrs by CLSI M38-A2 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID519057Antifungal activity against Candida glabrata assessed as susceptible isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID1898167Antifungal activity against Candida parapsilosis 90018
AID371234Antimicrobial activity against Cryptococcus neoformans TIMM 1855 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID619763Antifungal activity against Aspergillus fumigatus RCMB 002003 at 30 mg/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Design and synthesis of some new thiophene, thienopyrimidine and thienothiadiazine derivatives of antipyrine as potential antimicrobial agents.
AID1689220Antifungal activity against Candida krusei ATCC 34135 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID405076Antifungal activity against Sporothrix schenckii isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1413327Antifungal activity against Candida lusitaniae 95-7672018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID555572Antimicrobial activity against Candida lusitaniae by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID584591Antifungal activity against 176 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 168 days after 113 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID575489Antifungal activity against azole-resistant Aspergillus fumigatus isolate T18 harboring Cyp51A TR/L98H mutation assessed as inhibition of fungal growth at 4 mg/l relative to control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID1428259Antifungal activity against Candida albicans RCMB 0005003 assessed as zone of inhibition at 30 ug/ml2017European journal of medicinal chemistry, Jan-27, Volume: 126An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
AID549046Antifungal activity against Candida albicans CA3 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID1059362Antifungal activity against Candida dubliniensis after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID467289Antifungal activity against Aspergillus fumigatus by serial dilution method after 7 days2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of highly potent novel antifungal azoles by structure-based rational design.
AID634073Antifungal activity against Saccharomyces cerevisiae ATCC 24657 assessed as growth at 90.7 uM after 48 hrs by spectrophotometric bioassay relative to control2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID555578Antimicrobial activity against Candida norvegensis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1334850Anti-fungal activity against Aspergillus fumigatus CGMCC 3.7795 by broth microdilution method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
AID1604174Antileishmanial activity against Leishmania amazonensis MHOM/BR/75/Josefa promastigotes assessed as reduction in parasite viability after 72 hrs by Neubauer chamber counting method2019European journal of medicinal chemistry, Dec-01, Volume: 183Multi-target drugs active against leishmaniasis: A paradigm of drug repurposing.
AID519050Antifungal activity against Aspergillus sp. after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID55176Minimum inhibitory concentration of compound for antifungal activity against Cryptococcus neoformans2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID1357637Antifungal activity against Paracoccidioides brasiliensis Pb18 after 7 days by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID584410Antifungal activity against -3 days cultured Candida tropicalis isolated from neutropenic subject with AML or MDS pharynx receiving antifungal therapy for 45 days after 24 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID679901TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) (Vinblastine: 0.1 uM, Itraconazole: 100 uM) in MDR1-expressing LLC-PK1 cells1999Biological & pharmaceutical bulletin, Dec, Volume: 22, Issue:12
Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
AID341743Toxicity in human at risk for fungal infection assessed as occurrence of adverse events at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1783070Antifungal activity against fluconazole-sensitive Candida albicans 9770 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1689225Antifungal activity against Cryptococcus gattii NR43209 assessed as reduction in fungal growth incubated for 48 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID532041Antifungal activity against Lichtheimia ramosa clinical isolate after 24 hrs by EUCAST method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
AID1556208Antifungal activity against Candida albicans CPCC 400523 assessed as inhibition of visible microbial growth by NCCLS protocol based method2019European journal of medicinal chemistry, Sep-01, Volume: 177Design, synthesis, and structure-activity relationship studies of l-amino alcohol derivatives as broad-spectrum antifungal agents.
AID575755Binding affinity to Aspergillus fumigatus AF293 sterol 14-alpha demethylase isoenzyme B expressed in Escherichia coli assessed as tight binding affinity constant2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
AID563410Antifungal activity against Aspergillus tubingensis isolate CM-3177 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1419493Antifungal activity against Candida albicans ATCC 10231 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID515009Antifungal activity against Candida albicans Y0109 after 24 hrs by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID563391Antifungal activity against Aspergillus tubingensis isolate CM-3585 after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1204559Antifungal activity against Candida albicans Strain 29 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1128929Antifungal activity against Aspergillus fumigatus assessed as total growth inhibition by micro-broth dilution method2014European journal of medicinal chemistry, Apr-09, Volume: 76Imidazolylchromanones containing non-benzylic oxime ethers: synthesis and molecular modeling study of new azole antifungals selective against Cryptococcus gattii.
AID278903Antifungal activity against Scedosporium aurantiacum ear swab isolate CNM-CM-2846 at 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Prevalence and susceptibility testing of new species of pseudallescheria and scedosporium in a collection of clinical mold isolates.
AID532333Antifungal activity against Aspergillus niger by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1689824Antifungal activity against Aspergillus fumigatus ASFU77 assessed as reduction in microbial growth after 48 hrs by resazurin staining based spectrofluorometric method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID1076025Antifungal activity against Candida sp. clinical isolate 12810 derived from blood by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID519549Antimicrobial activity against Aspergillus fumisynnematus isolate CNM-CM-2280 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID405096Antimicrobial activity against Mucor sp. after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID532558Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 8 ug/ml (Rvb = 0.144%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID602932Antifungal activity against Trichophyton rubrum by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID1415222Binding affinity to NPC1 in HUVEC assessed as increase in cholesterol accumulation in late endosome/lysosome at 0.2 uM after 14 hrs by filipin staining-based confocal microscopy2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Novel Tetrazole-Containing Analogues of Itraconazole as Potent Antiangiogenic Agents with Reduced Cytochrome P450 3A4 Inhibition.
AID424630Antimicrobial activity against azole-susceptible Candida albicans isolate CA12 co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID581905Antifungal activity against Candida glabrata isolated from HSCT recipient 491 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1820639Antifungal activity against Candida tropicalis GIM 2.183 assessed as inhibition of fungal growth by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-15, Volume: 228Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.
AID563400Antifungal activity against Aspergillus niger isolate CM-4316 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID531463Antifungal activity against Candida tropicalis assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID555610Antimicrobial activity against Aspergillus ochraceus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID468520Antifungal activity against Candida tropicalis IFO 10241 after 24 to 72 hrs by NCCLS method2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Synthesis and antimicrobial activities of 3-O-alkyl analogues of (+)-catechin: improvement of stability and proposed action mechanism.
AID1597998Antifungal activity against Cryptococcus neoformans after 72 hrs by NCCLS protocol based method2019European journal of medicinal chemistry, May-15, Volume: 170Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
AID581867Antifungal activity against Candida albicans isolated from HSCT recipient 301 with acute or chronic GVHD mouth receiving antifungal drug after 114 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1204550Antifungal activity against Candida albicans Strain 20 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1334851Anti-fungal activity against Candida tropicalis CGMCC 2.3739 by broth microdilution method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
AID283338Antifungal activity against Syncephalastrum spp after 24 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID1204533Antifungal activity against Candida albicans Strain 3 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID405037Antifungal activity against Sporothrix schenckii P24255 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1061743Antimicrobial activity against Candida albicans Y0109 after 24 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID278902Antifungal activity against Scedosporium aurantiacum sputum isolate CNM-CM-2631 at 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Prevalence and susceptibility testing of new species of pseudallescheria and scedosporium in a collection of clinical mold isolates.
AID1689224Antifungal activity against Cryptococcus gattii NR43210 assessed as reduction in fungal growth incubated for 48 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1743166Antifungal activity against Trichophyton rubrum2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID405102Antimicrobial activity against Apophysomyces elegans after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID484285Colloidal aggregation in fed state simulated intestinal fluid assessed as critical aggregation concentration by UV-visible spectrophotometry in presence of 3% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID753511Antidermatophytic activity against Epidermophyton floccosum RSKK 3027 after 7 days by broth microdilution method2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity.
AID681119TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID341570Half life in human at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1904360Antifungal activity against Candida parapsilosis GIM 2.190 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID1357631Antifungal activity against Candida albicans ATCC 18804 after 48 hrs by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID582243Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD receiving fluconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID581886Antifungal activity against Saccharomyces cerevisiae isolated from HSCT recipient 513 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1411891Antifungal activity against Mucor hiemalis ATCC 8690 by M38-A guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID1204535Antifungal activity against Candida albicans Strain 5 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID220225The compound was tested in vitro for antifungal activity against 10 yeasts.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol.
AID204352Minimum inhibitory concentration of compound for antifungal activity against Sporothrix schenck ii2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID1474172Antifungal activity against Candida tropicalis cgmcc 2.3739 by broth microdilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents.
AID549313Antifungal activity against Mucor circinelloides after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID1904358Antifungal activity against Candida tropicalis CGMCC 2.3739 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID555796Antimicrobial activity against Scedosporium prolificans by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1059357Fungicidal activity against Candida krusei by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID575483Antifungal activity against azole-resistant Aspergillus fumigatus isolate T11 harboring Cyp51A TR/L98H mutant gene assessed as inhibition of fungal growth at 4 mg/l relative to control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID484289Binding affinity to beta-lactamase AmpC at 200 uM after 30 mins by SDS-PAGE2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID581882Antifungal activity against Candida glabrata isolated from HSCT recipient 975 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID545674Ratio of cellular uptake in alveolar macrophages to plasma of healthy human at 10 doses of 200 mg/kg, twice daily2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Intracellular concentrations of posaconazole in different compartments of peripheral blood.
AID582222Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD prior to initiation of posaconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID609895Antifungal activity against Trichophyton rubrum by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID1413332Antifungal activity against sensitive Candida albicans MYA-28762018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID1392810Antifungal activity against Candida tropicalis cgmcc 2.3739 after 24 hrs by serial dilution method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
AID468518Antifungal activity against Candida lusitaniae ATCC 42720 after 24 to 72 hrs by NCCLS method2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Synthesis and antimicrobial activities of 3-O-alkyl analogues of (+)-catechin: improvement of stability and proposed action mechanism.
AID736599Antifungal activity against anidulafungin-resistant Candida parapsilosis isolate 22019 assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID440321Antifungal activity against Aspergillus fumigatus isolated from patient sputum after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID582255Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS prior to initiation of fluconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1856367Antifungal activity against Aspergillus fumigatus ATCC 46645 assessed as inhibition of conidial and mycelial growth incubated for 5 days by CLSI protocol based microbroth dilution method
AID555812Antimicrobial activity against Saksenaea vasiformis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID405018Antifungal activity against Sporothrix schenckii P20825 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID249339Minimum inhibitory concentration against Epidermophyton floccosum (n=12)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID405098Antimicrobial activity against Mucor circinelloides after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID581862Antifungal activity against Candida krusei isolated from neutropenic subjects with AML or MDS receiving fluconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405053Antifungal activity against Sporothrix schenckii PGAC0016 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID549318Antifungal activity against Rhizopus microsporus after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID581865Antifungal activity against Candida albicans isolated from HSCT recipient 262 with acute or chronic GVHD mouth receiving antifungal drug after 115 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1428257Antifungal activity against Geotrichum candidum 052008 assessed as zone of inhibition at 30 ug/ml2017European journal of medicinal chemistry, Jan-27, Volume: 126An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
AID575471Tmax in guinea pig infected with 10'6 CFU Microsporum canis B68128 at 20 mg/kg, po administered 2 hrs before infection for 5 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID555623Antimicrobial activity against Acremonium sp.by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1770943Antifungal activity against Candida krusei GIM2.1 assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID555617Antimicrobial activity against Fusarium solani by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID532139Antifungal activity against Aspergillus terreus2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID582229Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS receiving posaconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID729306Inhibition of vasopressin V2 receptor (unknown origin) assessed as change in intracellular calcium levels treated with centrifuged compound solution by fluorometric analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID405020Antifungal activity against Sporothrix schenckii P20825 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID519048Antifungal activity against Candida parapsilosis after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID518604Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID518605Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, E427K, C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID551212Antifungal activity against Aspergillus fumigatus by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID405100Antimicrobial activity against Absidia corymbifera after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID283334Antifungal activity against Rhizomucor spp after 24 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID302124Antifungal activity against fluconazole-resistant Candida albicans 18 after 24 hrs2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and antifungal activities of novel 2-aminotetralin derivatives.
AID1820638Antifungal activity against Candida albicans GIM 2.194 assessed as inhibition of fungal growth by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-15, Volume: 228Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.
AID1634358Antifungal activity against Candida albicans CPCC 400523 assessed as inhibition of visible microbe growth by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.
AID555604Antimicrobial activity against Aspergillus terreus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID533029Antifungal activity against Aspergillus fumigatus ATCC 9197 grown as biofilm on polystyrene after 24 to 48 hrs by XTT assay2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Aspergillus fumigatus forms biofilms with reduced antifungal drug susceptibility on bronchial epithelial cells.
AID283336Antifungal activity against Rhizopus spp after 24 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID535618Antifungal activity against Candida tropicalis T3 blood stream isolate harboring Fks1p FLTLS/PLRDP mutant protein2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies.
AID555574Antimicrobial activity against Candida rugosa by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID323596Antifungal activity against Candida krusei bloodstream isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates.
AID555570Antimicrobial activity against Candida krusei by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555806Antimicrobial activity against Mycocladus corymbiferus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID575194Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in diabetic OF1 mouse assessed as increase in mouse survival rate at 25 mg/kg, po bid administered 1 day after infection for 7 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID555588Antimicrobial activity against Galactomyces geotrichum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID581875Antifungal activity against Candida glabrata isolated from neutropenic subject 1497 with AML or MDS pharynx receiving antifungal drug after 61 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID582233Antifungal activity against Candida krusei isolated from neutropenic subjects with AML or MDS receiving posaconazole by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1204540Antifungal activity against Candida albicans Strain 10 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID525600Antibacterial activity against Fluconazole resistant Candida albicans DSY3604 containing tac1delta/delta ERG11-1/ERG11-5 genotype by EUCAST standards based broth microdilution method sCandida albicans DSY2942010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID262549Antifungal activity against Cryptococcus neoformans2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID554712Antimicrobial activity against Candida krusei IFO0011 after 48 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID531096Binding affinity to Candida albicans CYP56 by spectrophotometry2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
CYP56 (Dit2p) in Candida albicans: characterization and investigation of its role in growth and antifungal drug susceptibility.
AID555815Antifungal activity against tac1/tac1 deficient Candida albicans SZY31 after 48 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID581880Antifungal activity against Candida glabrata isolated from HSCT recipient 474 with acute or chronic GVHD mouth after 124 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID555616Antimicrobial activity against Penicillium spp. by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID555585Antimicrobial activity against Dipodascus capitatus by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1524623Antibacterial activity against Streptococcus mutans 3289 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID681126TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID319755Antimicrobial activity against Trichophyton rubrum isolates2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID519431Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4387 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID533027Antifungal activity against Aspergillus fumigatus ATCC 9197 grown as biofilm on CFBE41o cell after 24 to 48 hrs by XTT assay2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Aspergillus fumigatus forms biofilms with reduced antifungal drug susceptibility on bronchial epithelial cells.
AID340962Antifungal activity against sCandida stellata isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID1597999Antifungal activity against Trichophyton rubrum after 7 days by NCCLS protocol based method2019European journal of medicinal chemistry, May-15, Volume: 170Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
AID340966Antifungal activity against Rhodotorula sp. isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID1595044Antifungal activity against Cryptococcus neoformans LA314 assessed as reduction in fungal cell growth incubated for 48 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID509110Antifungal activity against 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected in OF1 mouse assessed as increase in mouse survival at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID566880Antifungal activity against Candida krusei by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID416041Fungicidal activity against tebuconazole-adapted wild type Colletotrichum graminicola CgM2 assessed as inhibition of radial growth rate at 23 degC in darkness2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Treatment of a clinically relevant plant-pathogenic fungus with an agricultural azole causes cross-resistance to medical azoles and potentiates caspofungin efficacy.
AID211473In vitro evaluation of minimum inhibitory concentration against Torulopsis glabrata 781995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID1157291Antifungal activity against Candida albicans SC5314 assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID547565Antifungal activity against Candida glabrata after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID1067047Antifungal activity against Cryptococcus neoformans after 72 hrs by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID1419501Antifungal activity against Candida krusei ATCC 6258 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID555594Antimicrobial activity against Trichosporon dermatis by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1157292Antifungal activity against Candida parapsilosis 22019 assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID584402Antifungal activity against 88 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 75 days after 33 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1128930Antifungal activity against Exophiala dermatitidis assessed as total growth inhibition by micro-broth dilution method2014European journal of medicinal chemistry, Apr-09, Volume: 76Imidazolylchromanones containing non-benzylic oxime ethers: synthesis and molecular modeling study of new azole antifungals selective against Cryptococcus gattii.
AID302125Antifungal activity against fluconazole-resistant Candida albicans 25 after 24 hrs2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and antifungal activities of novel 2-aminotetralin derivatives.
AID518614Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A S400I mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1534780Inhibition of CYP3A4 in human liver microsomes by LC-MS/MS analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Development of posaconazole-based analogues as hedgehog signaling pathway inhibitors.
AID1901384Antifungal activity against Candida albicans assessed as inhibition of fungal growth measured after 48 hrs by M27-A3 based broth microdilution2022European journal of medicinal chemistry, Feb-15, Volume: 230Tetrazole derivatives bearing benzodiazepine moiety-synthesis and action mode against virulence of Candida albicans.
AID555821Ratio of MIC50 for Candida albicans 5674 to MIC50 for cdr1/cdr1 deficient Candida albicans STY192009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID532043Antifungal activity against Lichtheimia corymbifera clinical isolate after 24 hrs by EUCAST method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
AID284104Antifungal activity against Candida neoformans IM 00319 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID49636Minimum concentration required to inhibit the growth of Candida albicans 42000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID1254075Antibacterial activity against Salmonella typhimurium 2421 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1877284Antifungal activity against Candida glabrata clinical isolate assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID554951Inhibition of Candida krusei Abc1g expressed in Saccharomyces cerevisiae isolate ADdelta assessed as fractional inhibitory concentration index at 2.5 ug/ml after 48 hrs by checkerboard susceptibility assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID1484675Antileishmanial activity against Leishmania major LV39 Rho/SU/59/P promastigote forms harboring c14dm-/+C14DM mutant after 48 hrs2017European journal of medicinal chemistry, Jul-28, Volume: 135An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy.
AID47892In vitro evaluation of minimum inhibitory concentration against Candida parapsilosis 611995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID49988Tested in vitro for the minimum inhibitory concentration (MIC) against Candida glabrata ATCC 900302002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Synthesis of Sordaricin analogues as potent antifungal agents against Candida albicans.
AID1301919Antiangiogenic activity against HUVEC assessed as inhibition of total tube length at 1 uM after 16 hrs by inverted microscopy2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID405050Antifungal activity against Sporothrix schenckii P26187 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1770934Anti-biofilm activity in Candida albicans CPCC400616 assessed as inhibition of biofilm formation incubated for 18 hrs by XTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID1357634Antifungal activity against Candida tropicalis ATCC 750 after 48 hrs by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID532349Antifungal activity against Sporothrix schenckii by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID509396Drug level in 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected OF1 mouse serum at 50 mg/kg, po bid administered 1 day after infection measured on day 6 after 4 hrs of last treatment2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID549311Antifungal activity against Rhizopus oryzae after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID560241Antifungal activity against Candida albicans by checkerboard method in presence of itraconazole2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Curcumin modulates efflux mediated by yeast ABC multidrug transporters and is synergistic with antifungals.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID563615Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as lanosterol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID289590Antifungal activity against Penicillium marneffei by serial plate dilution method2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Synthesis of some bioactive 2-bromo-5-methoxy-N'-[4-(aryl)-1,3-thiazol-2-yl]benzohydrazide derivatives.
AID480475Antifungal activity against Candida tropicalis after 24 hrs by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID620357Antifungal activity against Syncephalastrum racemosum RCMB 005003 at 30 ug/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives.
AID532138Antifungal activity against Aspergillus fumigatus2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID575463Antifungal activity against 5 x 10'6 CFU/ml Candida albicans B2630 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID609308Antifungal activity against Aspergillus flavus JLC 30784 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID283333Antifungal activity against Mucor spp after 48 hrs2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
AID581888Antifungal activity against Candida albicans isolated from HSCT recipient 031 with acute or chronic GVHD mouth after 109 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405027Antifungal activity against Sporothrix schenckii MRSS4 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1067043Antifungal activity against Trichophyton rubrum by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID1334849Anti-fungal activity against Cryptococcus neoformans CGMCC 2.3161 by broth microdilution method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
AID340964Antifungal activity against Pichia anomala isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID519281Antifungal activity against Candida krusei ATCC 6258 by AFST-EUCAST method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts.
AID1330310Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release at 100 uM preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID1898175Antifungal activity against Candida glabrata ATCC2001
AID45503In vivo Evaluation of minimum inhibitory concentration against Candida albicans 601995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID1076024Cytotoxicity against human MCF10A cells after 48 hrs by WST1 assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID1783062Antifungal activity against fluconazole-resistant Candida tropicalis 5008 assessed as inhibition of fungal growth incubated for 48 hrs by two-fold serial microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID547563Antifungal activity against Candida albicans after 24 to 72 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antifungal activities of bis(alkylpyridinium)alkane compounds against pathogenic yeasts and molds.
AID584594Antifungal activity against 43 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 172 days after 114 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1157290Antifungal activity against Candida albicans Y0109 assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID555805Antimicrobial activity against Lecythophora hoffmannii by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID541565AUC (0 to 24 hrs) in healthy human plasma at 200 mg, po every 12 hrs for 5 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
AID531462Antifungal activity against Candida glabrata assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID531468Antimicrobial activity against azole-susceptible Aspergillus fumigatus after 48 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Epidemiological cutoffs and cross-resistance to azole drugs in Aspergillus fumigatus.
AID555631Antimicrobial activity against Chrysonilia sitophila by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID581860Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS receiving fluconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID322545Antifungal activity against Trichophyton soudanense after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID1392808Antifungal activity against Candida albicans CPCC 400523 after 24 hrs by serial dilution method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
AID518593Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, M172V, N248T, D255E, L358L, E427K and C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID285864Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.03 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID1392811Antifungal activity against Aspergillus fumigatus cgmcc 3.7795 after 7 days by serial dilution method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
AID527142Antifungal activity against Candida parapsilosis LMGO 05 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID249344Minimum inhibitory concentration against Trichophyton mentagrophytes (n=20)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID54923Inhibition of human cytochrome P450 3A42003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID532321Antifungal activity against Candida lusitaniae by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID322860Antifungal activity against azole-resistant Aspergillus fumigatus V34/78-CM3279 isolate from patient with hyper-immunoglobulin E syndrome by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID405058Antifungal activity against Sporothrix schenckii P14036 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID532551Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 8 ug/ml (Rvb = 0.157%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID1904361Antifungal activity against Candida glabrata clinical isolate assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID283230Prolongation of survival in po dosed CD1 mouse infected with Coccidioides immitis Silveira administered after 3 days of infection after 12 days relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID584390Antifungal activity against 14 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth after 17 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID420663Antifungal activity against Candida tropicalis by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID1157296Antifungal activity against Trichophyton rubrum Cmccftla assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID622011Ratio of itraconazole IC50 to compound IC50 for antiangiogenic activity in human HUVEC cells assessed as inhibition of cell proliferation2011Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling.
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1557080Antifungal activity against Candida glabrata 192 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID768345Antifungal activity against Candida parapsilosis ATCC 22019 after 24 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID341556Apparent volume of distribution in human at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1525382Inhibition of mouse Smo A1 mutant expressed in mouse Shh Light2 cells assessed as reduction in hedgehog pathway activation incubated for 30 hrs by luminescence assay2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Inhibiting Hedgehog: An Update on Pharmacological Compounds and Targeting Strategies.
AID467285Antifungal activity against Candida albicans by serial dilution method after 24 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of highly potent novel antifungal azoles by structure-based rational design.
AID510820Antifungal activity against Fusarium oxysporum ATCC 48112 after 24 hrs by AFSTEUCAST assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and biological evaluation of (+)-labdadienedial, derivatives and precursors from (+)-sclareolide.
AID1898160Antifungal activity against Candida albicans 25#
AID1770942Antifungal activity against Candida glabrata assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID532131Antifungal activity against Candida guilliermondii2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID519284Antifungal activity against Candida parapsilosis ATCC 22019 by AFST-EUCAST method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID405103Antimicrobial activity against Rhizopus sp. assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID563409Antifungal activity against Aspergillus tubingensis isolate CM-3125 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID575749Antimicrobial activity against sterol 14-alpha demethylase isoenzyme A-deficient Aspergillus fumigatus CEA102010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
AID323072Antifungal activity against Cryptococcus neoformans IM 972751 by microbroth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID341571Cmax in children of >2-6 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID564265Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as obtusifoliol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID249330Minimum inhibitory concentration against Aspergillus species (n=8)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID1820641Antifungal activity against Aspergillus fumigatus CGMCC 3.7795 assessed as inhibition of fungal growth by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-15, Volume: 228Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.
AID508314Antifungal activity against Aspergillus fumigatus isolate V59-73 harboring G54W mutation in Cyp51A protein by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Efficacy of posaconazole against three clinical Aspergillus fumigatus isolates with mutations in the cyp51A gene.
AID554723Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Candida albicans ERG11A to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID609893Antifungal activity against Candida kefyr by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID525596Antibacterial activity against Fluconazole resistant Candida albicans DSY3608 containing tac1delta/delta ERG11-1/ERG11-1 (TAC1-1) genotype by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID425157Antimicrobial activity against azole-resistant Candida albicans isolate CA10 assessed as log reduction in colony count at 1 ug/ml co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by XTT assay2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1770937Antifungal activity against Candida albicans ATCC SC5314 assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID341568Tmax in human at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID606213Antifungal activity against Candida parapsilosis ATCC 0306392 by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID634078Fungistatic activity against Saccharomyces cerevisiae ATCC 24657 assessed as cell growth at 90.7 uM after 48 hrs by spectrophotometric bioassay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID1265821Antifungal activity against Aspergillus nidulans ATCC 38163 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID50156In vitro evaluation of minimum inhibitory concentration against Candida krusei 701995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID584408Antifungal activity against 10 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 37 days after 9 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID283227Effect on fungal burdens in Coccidioides immitis Silveira infected CD1 mouse spinal cord administered after 3 days of infection at 50 mg/kg, po bid after 12 days2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID1658281Effect on VEGFR2 localization in human HUVEC cells assessed as accumulation of VEGFR2 in perinuclear region at 2 uM by DAPI staining based confocal micrscopy
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1877305Antibiofilm activity against FLC-resistant Candida albicans CPCC400616 assessed as assessed as inhibition of biofilm formation measured at 6 hrs by XTT reduction assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID532953Antifungal activity against Candida albicans isolate V3 with CAI genotype by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
AID1877316Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 4 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID289591Antifungal activity against Aspergillus flavus by serial plate dilution method2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Synthesis of some bioactive 2-bromo-5-methoxy-N'-[4-(aryl)-1,3-thiazol-2-yl]benzohydrazide derivatives.
AID532565Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID340960Antifungal activity against Candida rugosa isolates from feeding stuff by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID584415Antifungal activity against 31 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 31 days after 28 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1557076Antifungal activity against Candida albicans P-87 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID323067Antifungal activity against Cryptococcus neoformans IM 983040 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID584388Antifungal activity against 42 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool after 48 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID559693Antimicrobial activity against Mucor circinelloides after 24 hrs by broth microdilution checkerboard procedure2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro interactions between antifungals and immunosuppressive drugs against zygomycetes.
AID609319Half life in rat at 10 mg/kg, iv administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID294852Antifungal activity against Aspergillus fumigatus after 7 days by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID1872519Antifungal activity against Candida albicans SANK 51486 by 96-well microplate method2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID566879Antifungal activity against Candida glabrata by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID554707Antimicrobial activity against Candida krusei NZCDC 89.021 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID725874Antifungal activity against Aspergillus fumigatus ASFU20 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID563614Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as lanosterol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID648417Antifungal activity against Aspergillus flavus NCIM 524 at MIC after 3 to 4 days2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID1325032Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells at 5 uM measured after 10 hrs by FACS analysis2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists.
AID736600Antifungal activity against anidulafungin-resistant Candida parapsilosis ANF8 assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID1589582Inhibition of CYP3A4 (unknown origin) using midazolam as substrate by UPLC-MS/MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID555819Antifungal activity against cdr1/cdr1/cdr2/cdr2 deficient Candida albicans STY31 after 48 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID1783772Antifungal activity against Candida albicans CPCC400523 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID322864Antifungal activity against azole-resistant Aspergillus fumigatus V49/09-CM4023 isolate from patient with chronic obstructive pulmonary disease by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID371236Antimicrobial activity against Aspergillus fumigatus SANK 10569 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID249267Minimum inhibitory concentration against Trichophyton rubrum (n=14)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID119042Tested in vivo for anti-candida activity in mice model 1 (dose: 0.5 mg/kg, untreated group).1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID220226In vitro for antifungal activity against 10 yeasts1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1589580Half life in human liver microsomes at 1 uM by UPLC-MS/MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID405013Antifungal activity against Sporothrix schenckii PSSA81 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID283225Prolongation of survival in CD1 mouse infected with Coccidioides immitis Silveira administered after 3 days of infection at 50 mg/kg, po bid after 12 days relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID1534782Intrinsic clearance in human liver microsomes at 1 uM by LC-MS/MS analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Development of posaconazole-based analogues as hedgehog signaling pathway inhibitors.
AID584398Antifungal activity against 14 days cultured Candida krusei isolated from neutropenic subject with AML or MDS stool after 12 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405046Antifungal activity against Sporothrix schenckii SSA29 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID566881Antifungal activity against Candida guilliermondii by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID1223572Inhibition of CYP3A4.2 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID405070Antifungal activity against Candida parapsilosis ATCC 22019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID575466Antifungal activity against 5 x 10'6 CFU/ml Candida krusei B68404 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID1674369Volume of distribution at steady state in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID442520Antifungal activity against Candida parapsilosis ATCC 22019 after 48 hrs by microbroth dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID1301912Inhibition of hedgehog pathway in mouse C3H10T1/2 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by qPCR method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID1474171Antifungal activity against Aspergillus fumigatus cgmcc 3.7795 by broth microdilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents.
AID520620Antifungal activity against Candida metapsilosis by microdilution AFST-EUCAST method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Prevalence and susceptibility profile of Candida metapsilosis and Candida orthopsilosis: results from population-based surveillance of candidemia in Spain.
AID532345Antifungal activity against Penicillium marneffei by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID325035Antimicrobial activity against Candida albicans SC5314 after 24 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole.
AID406958Antifungal activity against fluconazole-sensitive Candida albicans Fe40 at 35 degC after 48 hrs by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID1917563Induction of intracellular reactive oxygen species production in human A549 cells assessed as increase in number ROS positive cells at 30 uM and measured after 24 hrs by H2DCFH-DA staining based flow cytometric analysis (Rvb=1.10%)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID319750Antimicrobial activity against Candida albicans ATCC 766152008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID531469Antimicrobial activity against azole-resistant Aspergillus fumigatus harboring G54V, G54E, G54R and G54W mutation in cyp51A gene after 48 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Epidemiological cutoffs and cross-resistance to azole drugs in Aspergillus fumigatus.
AID532325Antifungal activity against Cryptococcus neoformans var. neoformans by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1833887Inhibition of Naegleria fowleri CYP51 catalytic activity using [3-3H]sterol substrate measured after 1 hr by RP-HPLC analysis2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Relaxed Substrate Requirements of Sterol 14α-Demethylase from
AID554725Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Candida krusei ERG11g to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID262551Antifungal activity against Fonsecaea pedrosoi2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID582244Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD prior to initiation of fluconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1743172Antifungal activity against Microsporum canis2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID484281Colloidal aggregation in fed state simulated intestinal fluid at 100 uM by transmission electron microscopy in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID141791Minimum concentration required to inhibit the growth of Mucosporum canis2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID1059365Antifungal activity against Candida tropicalis after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID405072Antifungal activity against Aspergillus flavus ATCC 204304 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1557078Antifungal activity against Candida glabrata ATCC 66032 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID637165Antifungal activity against Saccharomyces cerevisiae ATCC 9763 at 12.5 mg/ml after 72 hrs by agar diffusion test2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and in vitro antimycobacterial activity of compounds derived from (R)- and (S)-2-amino-1-butanol - The crucial role of the configuration.
AID533025Antifungal activity against Aspergillus fumigatus ATCC 9197 grown as biofilm on 16HBE cell after 24 to 48 hrs by XTT assay2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Aspergillus fumigatus forms biofilms with reduced antifungal drug susceptibility on bronchial epithelial cells.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1223580Ratio of Ki for CYP3A4.2 (unknown origin) to Ki for CYP3A4.1 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID532129Antifungal activity against Candida lusitaniae2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID581885Antifungal activity against Candida glabrata isolated from HSCT recipient 270 with acute or chronic GVHD mouth receiving antifungal drug after 108 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405033Antifungal activity against Sporothrix schenckii PSCC1 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID532142Antifungal activity against Rhizomucor species2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1204545Antifungal activity against Candida albicans Strain 15 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1743170Antifungal activity against Trichophyton mentagrophytes var. interdigitale2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID606215Antifungal activity against Cryptococcus neoformans ATCC BLS108 after 72 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID582236Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS prior to initiation of posaconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID322862Antifungal activity against azole-resistant Aspergillus fumigatus V45/07-CM3819 isolate from patient with chronic granulomatous disease by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID575195Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in diabetic OF1 mouse assessed as increase in mouse survival rate at 50 mg/kg, po bid administered 1 day after infection for 7 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID701453Antifungal activity against Aspergillus fumigatus2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID681122TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID545672Ratio of intracellular to extracellular drug uptake in alveolar macrophages of New Zealand white rabbit infected with Mycobacterium bovis at 1 ug/ml in presence of 5% serum2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Intracellular concentrations of posaconazole in different compartments of peripheral blood.
AID405015Antifungal activity against Sporothrix schenckii P25013 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1872521Antifungal activity against Aspergillus fumigatus SANK 10569 by 96-well microplate method2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID405071Antifungal activity against Candida parapsilosis ATCC 22019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID284103Antifungal activity against Candida neoformans IM 983036 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID524739Antimicrobial activity against Fusarium oxysporum after 48 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Species distribution and in vitro antifungal susceptibility patterns of 75 clinical isolates of Fusarium spp. from northern Italy.
AID584417Antifungal activity against 12 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 143 days after 116 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID549320Antifungal activity against Rhizomucor pusillus after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID440325Antifungal activity against Aspergillus terreus isolated from patient bronchoalveolar lavage fluid after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID575374Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as decreased fungal load in lung at 25 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated contr2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID442522Antifungal activity against Microsporum gypseum NCPF 580 after 7 days by microbroth dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID555138Antimicrobial activity against Candida parapsilosis ATCC 22019 by EUCAST broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID1783770Antifungal activity against Cryptococcus neoformans GIM2.209 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID1059353Antifungal activity against Candida parapsilosis clinical isolate after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID665068Antifungal activity against Candida tropicalis after 24 hrs by serial dilution method2012European journal of medicinal chemistry, Jul, Volume: 53Design, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains.
AID1743168Antifungal activity against Trichophyton tonsurans2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID527146Antifungal activity against Trichophyton mentagrophytes LMGO 09 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID549322Antifungal activity against Rhizomucor variabilis after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID575461Antifungal activity against 5 x 10'6 CFU/ml Trichophyton quinckeanum B68683 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID1674367Clearance in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID555606Antimicrobial activity against Aspergillus niger by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1301911Inhibition of hedgehog pathway in mouse C3H10T1/2 cells assessed as Gli1 mRNA expression at 1 uM after 24 hrs by qPCR method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID584399Antifungal activity against 59 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 75 days after 33 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID283201Susceptibility of Candida glabrata 21231 isolate at 8 ug by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth.
AID555808Antimicrobial activity against Mucor spp.by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID1265817Antifungal activity against azole-resistant Candida albicans ATCC 90819 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID1493830Antifungal activity against Cryptococcus neoformans 32609 after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID549314Antifungal activity against Mycocladus corymbifer after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID1770961Cytotoxicity against human THLE-2 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID563407Antifungal activity against Aspergillus tubingensis isolate CM-4688 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID341575Cmax in children of >6-12 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID420664Antifungal activity against Trichophyton rubrum by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID519425Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-3537 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID745593Antifungal activity against Trichophyton rubrum SNB-TR1 assessed as growth inhibition after 5 days by CLSI microdilution method2013Journal of natural products, May-24, Volume: 76, Issue:5
Antifungal agents from Pseudallescheria boydii SNB-CN73 isolated from a Nasutitermes sp. termite.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1557086Antifungal activity against Candida albicans SN152 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID1265814Antifungal activity against azole-resistant Candida albicans ATCC 10231 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID1493831Antifungal activity against Aspergillus fumigatus 07544 after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID1898166Antifungal activity against Candida parapsilosis 660
AID1689822Antifungal activity against Aspergillus fumigatus ASFU76 assessed as reduction in microbial growth after 48 hrs by resazurin staining based spectrofluorometric method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID405044Antifungal activity against Sporothrix schenckii P1621 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1511962Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in recombinant mouse sonic hedgehog/oxysterol-induced Gli1 mRNA expression by q-PCR analysis2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Truncated Itraconazole Analogues Exhibiting Potent Anti-Hedgehog Activity and Improved Drug-like Properties.
AID564268Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant eburicol level after 2 hrs by gas chromatography2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID176374Efficacy against Aspergillosis fumigatus CF924390 on day 14th after peroral administration in rat2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
AID424629Antimicrobial activity against azole-susceptible Candida albicans isolate CA8 co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID532144Antifungal activity against Absidia species2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID531243Antifungal activity against Candida parapsilosis assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID284109Antifungal activity against Candida neoformans IM 052470 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID725873Antifungal activity against Aspergillus fumigatus ASFU19 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID341544Apparent volume of distribution in children of >2-6 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID563389Antifungal activity against Aspergillus niger isolate CM-3506 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID39835Minimum inhibitory concentration of compound for antifungal activity against Aspergillus fumigatus2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID609307Antifungal activity against Aspergillus fumigatus JLC 30883 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID559695Antimicrobial activity against Rhizomucor pusillus after 24 hrs by broth microdilution checkerboard procedure2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro interactions between antifungals and immunosuppressive drugs against zygomycetes.
AID572709Selectivity ratio of Kd for Mycobacterium smegmatis ATCC 700084 CYP164A2 in presence of 0.5 M NaCl to Kd for Mycobacterium smegmatis ATCC 700084 CYP164A22009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae.
AID1754265Antifungal activity against clinical strain Candida parapsilosis by microplate reader assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41A new sulfated triterpene glycoside from the sea cucumber Colochirus quadrangularis, and evaluation of its antifungal, antitumor and immunomodulatory activities.
AID49982Minimum inhibitory concentration of compound for antifungal activity against Candida glabrata2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID584395Antifungal activity against 8 days cultured Candida krusei isolated from neutropenic subject with AML or MDS stool after 12 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID681128TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID575499Antifungal activity against Aspergillus fumigatus isolates harboring Cyp51A TR/L98H mutation by EUCAST method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID1157294Antifungal activity against Cryptococcus neoformans 32609 assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID150755Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID341574Half life in children of >2-6 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID323068Antifungal activity against Cryptococcus neoformans IM 972724 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID1309058Antifungal activity against Aspergillus terreus ATCC MYA3633 after 48 hrs by CLSI M38-A2 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID555814Antifungal activity against azole-susceptible Candida albicans 5457 after 48 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID543971AUC (0 to 72 hrs) in human at 15 mg, po pretreated with itraconazole at 200 mg, po qd for 4 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Voriconazole increases while itraconazole decreases plasma meloxicam concentrations.
AID509099Antifungal activity against Fonsecaea monophora CBS 1172362010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID555816Antifungal activity against azole-resistant Candida albicans 5674 after 48 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID575460Antifungal activity against 5 x 10'6 CFU/ml Trichophyton rubrum J941704 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID532132Antifungal activity against Saccharomyces cerevisiae2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID341539Clearance in infants of 0.6-2 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID602927Antifungal activity against Candida albicans Y0109 after 24 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID581892Antifungal activity against Candida albicans isolated from HSCT recipient 042 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID603348Antifungal activity against Aspergillus fumigatus clinical isolate by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID551210Antifungal activity against Fusarium by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID419081Antifungal activity against Candida krusei ATCC 62582009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID518405Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A M220K mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID551206Antifungal activity against Cryptococcus neoformans ATCC BLS108 after 72 hrs by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID563405Antifungal activity against Aspergillus tubingensis isolate CM-4003 after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID284108Antifungal activity against Candida neoformans IM 961951 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID1067044Antifungal activity against Candida glabrata by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID665069Antifungal activity against Candida parapsilosis after 24 hrs by serial dilution method2012European journal of medicinal chemistry, Jul, Volume: 53Design, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains.
AID549315Antifungal activity against Mycocladus corymbifer after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1330317Antagonist activity at Cav2.2 in human SH-SY5Y cells assessed as inhibition of KCl/CaCl2-stimulated Ca2+ flux up to 100 uM after 30 mins in presence of nifedipine by Fuo-4 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID582245Antifungal activity against Candida glabrata isolated from HSCT recipients with acute or chronic GVHD receiving fluconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID531240Antifungal activity against Candida albicans assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID285858Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 1 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID1783065Antifungal activity against fluconazole-sensitive Candida albicans SC5314 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID509123Antifungal activity against 2 x 10'5 CFU Fonsecaea monophora CBS 117236 infected in po dosed OF1 mouse assessed as reduction in fungal load in lung at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID1059358Fungicidal activity against Candida parapsilosis by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID565403Antifungal activity against Rhizopus microsporus IHEM 4770 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID420662Antifungal activity against Candida parapsilosis by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID531465Antifungal activity against Candida guilliermondii assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID440322Antifungal activity against Aspergillus fumigatus isolated from patient bronchoalveolar lavage fluid after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID532950Antifungal activity against Candida albicans isolate O with CAI genotype by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
AID581863Antifungal activity against Candida albicans isolated from HSCT recipient 262 with acute or chronic GVHD mouth after 115 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID620354Antifungal activity against Aspergillus fumigatus RCMB 002003 at 30 ug/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID419077Antifungal activity against Aspergillus flavus SANK 184972009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID480479Antifungal activity against Trichophyton rubrum after 7 days by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID681127TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID340957Antifungal activity against Candida lambica isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID405039Antifungal activity against Sporothrix schenckii P10012 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID575498Antifungal activity against Aspergillus lentulus isolate2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID424622Antimicrobial activity against azole-susceptible Candida albicans isolate CA129 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID584387Antifungal activity against 36 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS pharynx after 48 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405024Antifungal activity against Sporothrix schenckii P14954 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1904356Antifungal activity against Candida albicans ATCC SC5314 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID610069Antifungal activity against Candida parapsilosis JLC 30365 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID406957Antifungal activity against fluconazole-resistant Candida albicans isolated from oropharyngeal or vaginal disease patient after 48 hrs by broth microdilution test2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.
AID584599Antifungal activity against 6 days cultured Candida krusei isolated from neutropenic subject with AML or MDS pharynx receiving antifungal therapy for 19 days after 6 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID609310Solubility of the compound in water at pH 1.22011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID566882Antifungal activity against Cryptococcus neoformans by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID285856Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.25 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID532151Antifungal activity against Scedosporium prolificans2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1595050Antifungal activity against Aspergillus niger assessed as reduction in fungal cell growth incubated for 72 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID405028Antifungal activity against Sporothrix schenckii MRSS4 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1301915Antiproliferative activity against mouse MERP MB cells assessed as cell growth inhibition using methyl-[3H]thymidine after 48 hrs by liquid scintillation spectrophotometry2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.
AID1770962Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID1223575Inhibition of CYP3A4.18 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID467290Antifungal activity against Microsporum gypseum by serial dilution method after 24 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of highly potent novel antifungal azoles by structure-based rational design.
AID619765Antifungal activity against Geotrichum candidum RCMB 052006 at 30 mg/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Design and synthesis of some new thiophene, thienopyrimidine and thienothiadiazine derivatives of antipyrine as potential antimicrobial agents.
AID150751Inhibition of P-glycoprotein using ATPase in MDR1 membranes2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1392809Antifungal activity against Cryptococcus neoformans cgmcc 2.3161 after 72 hrs by serial dilution method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
AID341552Apparent volume of distribution in adolescents of >12-16 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1059345Antifungal activity against Candida glabrata after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID1204529Antifungal activity against Trichosporon cutaneum ATCC 28592 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1419504Antifungal activity against Aspergillus nidulans ATCC 38163 incubated for 48 hrs by CLSI M38-A2 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID532155Antifungal activity against Fusarium solani2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID584391Antifungal activity against 16 days cultured Candida glabrata isolated from invasive fungal infected subject blood after 17 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID532951Antifungal activity against Candida albicans isolate V1 with CAI genotype by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
AID565398Antifungal activity against Rhizopus microsporus CBS 102277 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID531466Antifungal activity against Candida krusei assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID48233In vitro evaluation of minimum inhibitory concentration against Candida pseudotropicalis 131995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID519448Antimicrobial activity against Aspergillus viridinutans isolate CNM-CM-3147 obtained from oropharyngeal exudate of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1473927Ratio of drug concentration at steady state in human at 200 mg, po QD for 1 to 2 weeks after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1556209Antifungal activity against Candida albicans ATCC SC5314 assessed as inhibition of visible microbial growth by NCCLS protocol based method2019European journal of medicinal chemistry, Sep-01, Volume: 177Design, synthesis, and structure-activity relationship studies of l-amino alcohol derivatives as broad-spectrum antifungal agents.
AID1877285Antifungal activity against Candida krusei GIM2.1 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID655583Antifungal activity against Candida parapsilosis by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID1783774Antifungal activity against Aspergillus fumigatus CGMCC3.7795 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID283223Prolongation of survival in CD1 mouse infected with Coccidioides immitis Silveira administered after 3 days of infection at 10 mg/kg, po bid after 12 days relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID283228Effect on fungal burdens in Coccidioides immitis Silveira infected CD1 mouse lung administered after 3 days of infection at 50 mg/kg, po bid after 12 days2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID575208Antifungal activity against Cunninghamella echinulata UTHSC 01-2298 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID405026Antifungal activity against Sporothrix schenckii P14954 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID563396Antifungal activity against Aspergillus niger isolate CM-4004 obtained from after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID584404Antifungal activity against 3 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 25 days after 3 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID39829Minimum concentration required to inhibit the growth of Aspergillus fumigatus2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID285874Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID1689829Antifungal activity against Scedosporium apiospermum SCAP1 assessed as reduction in microbial growth after 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID532135Antifungal activity against Trichosporon inkin2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1059361Fungicidal activity against Candida albicans by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID1609925Antifungal activity against Candida albicans SC5314 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID747170Antimicrobial activity against Candida albicans ATCC 22019 by broth dilution method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Synthesis and antimicrobial activity of novel amphiphilic aromatic amino alcohols.
AID531467Antifungal activity against Candida lusitaniae assessed as susceptible dose-dependent isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID541559Cmax in healthy human plasma at 200 mg, po every 12 hrs for 5 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
AID1770935Anti-biofilm activity in Candida albicans CPCC400616 assessed as inhibition of biofilm formation incubated for 6 hrs by XTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID1849824Antifungal activity against Sporothrix schenckii assessed as fungal growth inhibition incubated for 48 hrs by CLSI-based broth microdilution assay2021European journal of medicinal chemistry, Jan-15, Volume: 210A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials.
AID419080Antifungal activity against Candida parapsilosis ATCC 900182009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID532348Antifungal activity against Fusarium oxysporum by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID582220Antifungal activity against Candida krusei isolated from HSCT recipients with acute or chronic GVHD prior to initiation of posaconazole therapy by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1204546Antifungal activity against Candida albicans Strain 16 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID551208Antifungal activity against Candida tropicalis by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID118897In vivo antifungal activity against murine candidosis model after peroral administration with 1 mg/kg for 5 days.(percent protection for 100% mortality with fluconazole-treated group.); not tested1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol.
AID319753Antimicrobial activity against Cryptococcus neoformans ATCC 326092008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID262548Antifungal activity against Candida tropicalis2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID555573Antimicrobial activity against Candida kefyr by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID532136Antifungal activity against Trichosporon asahii2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID246892Effective dose was measured in mice infected with Trichophyton mentagrophytes2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID565551Antifungal activity against Rhizopus microsporus IHEM 15210 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID440323Antifungal activity against Aspergillus versicolor isolated from patient sputum after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID566889Antifungal activity against Exophiala spinifera by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID245420Minimum inhibitory concentration against Candida albicans A261 evaluated by in vitro agar diffusion and micro-broth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID1770963Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID555626Antimicrobial activity against Phialemonium curvatum by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID325038Antimicrobial activity against Candida albicans P5 after 48 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole.
AID1898172Antifungal activity against Candida krusei 629
AID405276Antifungal activity against Sporothrix schenckii P3287 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID249263Minimum inhibitory concentration against Candida species (n=24)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID1646827Inhibition of Hedgehog signaling pathway in mouse ASZ001 cells assessed as decrease in Gli1 mRNA expression after 48 hrs by qRT-PCR analysis2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Inhibition of hedgehog signaling by stereochemically defined des-triazole itraconazole analogues.
AID527131Antifungal activity against Microsporum gypseum LMGO 10 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID415949Antimicrobial activity against Candida albicans by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID405036Antifungal activity against Sporothrix schenckii P24255 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID549048Antifungal activity against Candida albicans CA127 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID519286Antifungal activity against Candida parapsilosis ATCC 22019 by WIDERYST method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts.
AID522130Antimicrobial activity against Candida glabrata TG162 containing calcineurin deltacnb1 mutant by colorimetric microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Roles of calcineurin and Crz1 in antifungal susceptibility and virulence of Candida glabrata.
AID519444Antimicrobial activity against Neosartorya pseudofischeri isolate CNM-CM-3769 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID549050Antifungal activity against Candida albicans CA10 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID680505TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Doxorubicin: 0.1 uM, Itraconazole: 100 uM) in MDR1-expressing LLC-PK1 cells1999Biological & pharmaceutical bulletin, Dec, Volume: 22, Issue:12
Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
AID519428Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-3599 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID340958Antifungal activity against Candida norvegensis isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID48961Tested in vitro for the minimum inhibitory concentration (MIC) against Candida albicans SANK514862002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
Synthesis of Sordaricin analogues as potent antifungal agents against Candida albicans.
AID1917557Induction of apoptosis in human A549 cells assessed as necrotic cells at 30 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.084%)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID1155873Antifungal activity against Aspergillus fumigatus assessed as growth inhibition after 7 days by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID1609930Antifungal activity against fluconazole-resistant Candida albicans 17 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID609894Antifungal activity against Cryptococcus neoformans BLS108 by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID285867Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.25 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID1689825Antifungal activity against Rhizopus oryzae RHPOR1 assessed as reduction in microbial growth after 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID284102Antifungal activity against Candida neoformans IM 042074 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID1557088Antifungal activity against Candida glabrata 192 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID442523Antifungal activity against Trichophyton tonsurans NCPF 245 after 7 days by microbroth dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID559691Antimicrobial activity against Rhizopus oryzae after 24 hrs by broth microdilution checkerboard procedure2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro interactions between antifungals and immunosuppressive drugs against zygomycetes.
AID545330Antimicrobial activity against Candida albicans isolate C after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing.
AID341549Half life in children of >6-12 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID285857Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.5 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID565553Antifungal activity against Rhizopus microsporus UTHSC 03-1802 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID554950Inhibition of Candida krusei B2399 Abc1p assessed as fractional inhibitory concentration index at 2.5 ug/ml after 48 hrs by checkerboard susceptibility assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID1689239Antifungal activity against Candida albicans SS5314 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID519424Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-3364 obtained from bronchoalveolar lavage fluid of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID555136Antimicrobial activity against Candida albicans by CLSI M27-A2 broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID415952Antimicrobial activity against Candida tropicalis by micro-broth dilution method2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols.
AID729314Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID302123Antifungal activity against fluconazole-resistant Candida albicans 01010 after 24 hrs2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and antifungal activities of novel 2-aminotetralin derivatives.
AID1557081Antifungal activity against Candida parapsilosis ATCC 90018 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID1334848Anti-fungal activity against Candida albicans CPCC 400523 by broth microdilution method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
AID1898163Antifungal activity against Candida albicans 305
AID1898173Antifungal activity against Candida krusei 397
AID1204537Antifungal activity against Candida albicans Strain 7 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID515015Antifungal activity against Aspergillus fumigatus by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID555589Antimicrobial activity against Cryptococcus neoformans var. neoformans by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Activity profile in vitro of micafungin against Spanish clinical isolates of common and emerging species of yeasts and molds.
AID322854Antifungal activity against azole-resistant Aspergillus fumigatus V13/03-CM3272 isolate from patient with X-linked chronic granulomatous disease by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID1534783Kinetic solubility of compound in pH 7.4 PBS by LC-MS/MS analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Development of posaconazole-based analogues as hedgehog signaling pathway inhibitors.
AID48801Minimum concentration required to inhibit the growth of Candida tropicalis2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID531242Antifungal activity against Candida tropicalis assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID581902Antifungal activity against Candida glabrata isolated from HSCT recipient 807 with acute or chronic GVHD mouth after 114 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1493828Antifungal activity against Candida parapsilosis 22019 after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID670446Antifungal activity against Trichophyton rubrum incubated at 35 degC for 72 hrs by NCCLS based microbroth dilution method2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Synthesis and biological evaluation of vinyl ether-containing azole derivatives as inhibitors of Trichophyton rubrum.
AID1067042Antifungal activity against Microsporum gypseum by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID581868Antifungal activity against Candida glabrata isolated from neutropenic subject 1102 with AML or MDS stool after 26 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID141790Minimum inhibitory concentration of compound for antifungal activity against Mucosporam canis2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID420667Antifungal activity against Aspergillus fumigatus by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID285853Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.03 ug/ml by CLSI method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID1204541Antifungal activity against Candida albicans Strain 11 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1889406Hepatotoxicity in zebrafish embryos assessed as liver failure by measuring necrotic and decreased liver with non-resorbed yolk at 0.25 uM treated at 6 hpf and measured at 120 hpf by stereomicroscopic analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis.
AID283224Prolongation of survival in CD1 mouse infected with Coccidioides immitis Silveira administered after 3 days of infection at 25 mg/kg, po bid after 12 days relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID1164091Antifungal activity against Candida tropicalis ATCC 750 by broth microdilution method2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents.
AID197814In vitro evaluation of minimum inhibitory concentration against Rhodotorula rubra 161995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID49637Minimum inhibitory concentration of compound for antifungal activity against Candida albicans 42000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID442521Antifungal activity against Candida krusei ATCC 6258 after 48 hrs by microbroth dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID340955Antifungal activity against Candida krusei isolates from grapes and feeding stuffs by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID527143Antifungal activity against Candida glabrata LMGO 44 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID405014Antifungal activity against Sporothrix schenckii PSSA81 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID584413Antifungal activity against 9 days cultured Candida tropicalis isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 45 days after 24 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID575462Antifungal activity against 5 x 10'6 CFU/ml Candida albicans B59163 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1204532Antifungal activity against Candida albicans Strain 2 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID249269Minimum inhibitory concentration against Trichophyton species (n=80)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID1589576Inhibition of human ERG2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID1474168Antifungal activity against Candida albicans ATCC SC5314 by broth microdilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents.
AID582252Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS receiving fluconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID341543Clearance in children of >2-6 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID214279Minimum inhibitory concentration of compound for antifungal activity against Trichophyton mentagrophytes2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID245450Minimum inhibitory concentration against Candida tropicalis ATCC750 evaluated by in vitro agar diffusion and microbroth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID341541Half life in infants of 0.6-2 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID609305Antifungal activity against Cryptococcus neoformans JLC 50123 by broth microdilution method2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID424634Antimicrobial activity against azole-resistant Candida albicans isolate CA15 cotreated with calcineurin signaling inhibitor Tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID405052Antifungal activity against Sporothrix schenckii PGAC0016 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID584406Antifungal activity against 25 days cultured Candida glabrata isolated from invasive fungal infected subject blood receiving antifungal therapy for 25 days after 3 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID49630Minimum concentration required to inhibit the growth of Candida albicans 12000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID1770939Antifungal activity against Candida tropicalis CGMCC 2.3739 assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID582999Antimicrobial activity against Saccharomyces cerevisiae YUG37 transformed with plasmid carrying cyp51B gene with doxycycline-regulatable promoter by broth dilution method in presence of doxycycline2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Complementation of a Saccharomyces cerevisiae ERG11/CYP51 (sterol 14α-demethylase) doxycycline-regulated mutant and screening of the azole sensitivity of Aspergillus fumigatus isoenzymes CYP51A and CYP51B.
AID1689826Antifungal activity against Rhizopus oryzae RHPOR2 assessed as reduction in microbial growth after 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID551205Antifungal activity against Candida albicans ATCC Y0109 after 24 hrs by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID49634Minimum inhibitory concentration of compound for antifungal activity against Candida albicans 22000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID1155871Antifungal activity against Cryptococcus neoformans assessed as growth inhibition after 72 hrs by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID575465Antifungal activity against 5 x 10'6 CFU/ml Candida kefyr B46120 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID537734Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1204555Antifungal activity against Candida albicans Strain 25 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID480474Antifungal activity against Candida albicans after 24 hrs by serial dilution method2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives.
AID518600Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, A284A mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1877307Antibiofilm activity against FLC-resistant Candida albicans CPCC400616 assessed as assessed as inhibition of biofilm formation measured at 24 hrs by XTT reduction assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID405042Antifungal activity against Sporothrix schenckii P1621 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID572696Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP164A2 in presence of 0.5 M NaCl at pH7.52009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae.
AID582241Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD receiving fluconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1589579Kinetic solubility of the compound in PBS at pH 7.4 by by UPLC-MS/MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1204556Antifungal activity against Candida albicans Strain 26 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID245494Minimum inhibitory concentration against Candida parapsilosis ATCC 22019 evaluated by in vitro agar diffusion and micro-broth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID1419499Antifungal activity against ITC and FLC-resistant Candida albicans ATCC MYA-1003 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID582248Antifungal activity against Candida krusei isolated from HSCT recipients with acute or chronic GVHD receiving fluconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID745594Antifungal activity against Aspergillus fumigatus SNB-AF1 assessed as growth inhibition after 24 hrs by CLSI microdilution method2013Journal of natural products, May-24, Volume: 76, Issue:5
Antifungal agents from Pseudallescheria boydii SNB-CN73 isolated from a Nasutitermes sp. termite.
AID519061Antifungal activity against Candida albicans assessed as resistant isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID1743173Antifungal activity against Candida albicans2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID549045Antifungal activity against Candida albicans CA2 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID1309046Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1413324Antifungal activity against Cryptococcus neoformans H992018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID606216Antifungal activity against Aspergillus fumigatus after 7 days by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID1689216Antifungal activity against Candida glabrata ATCC MYA-2950 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID245429Minimum inhibitory concentration against Candida krusei ATCC 6528 evaluated by in vitro agar diffusion and micro-broth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID519435Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4428 obtained from skin of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1059359Fungicidal activity against Candida glabrata by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID518615Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing wild type cyp51A gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID701448Antifungal activity against Microsporum lauosum2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID584602Antifungal activity against 19 days cultured Candida krusei isolated from invasive fungal infected subject blood receiving antifungal therapy for 19 days after 6 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1265820Antifungal activity against azole-resistant Candida albicans MYA-1003 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID545329Antimicrobial activity against Candida albicans isolate R after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing.
AID582247Antifungal activity against Candida krusei isolated from HSCT recipients with acute or chronic GVHD prior to initiation of fluconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID509121Antifungal activity against 2 x 10'5 CFU Fonsecaea monophora CBS 117236 infected in po dosed OF1 mouse assessed as reduction in fungal load in kidney at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID565402Antifungal activity against Rhizopus microsporus IHEM 10123 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID609312Cmax in rat at 10 mg/kg, po administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID531248Antifungal activity against Candida glabrata assessed as resistant isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID563416Antifungal activity against Aspergillus niger isolate CM-4262 after 48 hrs by EUCAST broth dilution method Ophthalmic2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1546101Antimicrobial activity against Pseudomonas aeruginosa after 24 hrs by agar disk diffusion method2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID532346Antifungal activity against Penicillium species by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID546081Antifungal activity against Candida intermedia isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID582223Antifungal activity against Candida albicans isolated from HSCT recipients with acute or chronic GVHD receiving posaconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID436744Antifungal activity against Microsporum gypseum after 7 days by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID1254076Antifungal activity against Candida albicans 7535 by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID584409Antifungal activity against -3 days cultured Candida tropicalis isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 45 days after 24 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1872500Antifungal activity against Candida glabrata2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID1877306Antibiofilm activity against FLC-resistant Candida albicans CPCC400616 assessed as assessed as inhibition of biofilm formation measured at 18 hrs by XTT reduction assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID581897Antifungal activity against Candida glabrata isolated from neutropenic subject 1331 with AML or MDS pharynx receiving antifungal drug after 21 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID575206Antifungal activity against Cunninghamella echinulata FMR 10974 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID655582Antifungal activity against Cryptococcus neoformans after 72 hrs by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID118765In vivo antifungal activity against murine candidosis model after peroral administration with 0.5 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol.
AID563408Antifungal activity against Aspergillus foetidus isolate CM-5264 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1549136Antifungal activity against azole-sensitive Candida albicans SC5314 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID545675Ratio of cellular uptake in alveolar macrophages to plasma of healthy human at 14 doses of 400 mg/kg, twice daily2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Intracellular concentrations of posaconazole in different compartments of peripheral blood.
AID519447Antimicrobial activity against Neosartorya pseudofischeri isolate CNM-CM-3914 obtained from nail of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1067049Antifungal activity against Candida albicans Y0109 after 24 hrs by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID1493832Antifungal activity against Trichophyton rubrum Cmccftla after 24 hrs by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors.
AID1783064Antifungal activity against Cryptococcus neoformans H99 assessed as inhibition of fungal growth incubated for 72 hrs by two-fold serial microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID1357633Antifungal activity against Candida parapsilosis ATCC 22019 after 48 hrs by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID322753Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
AID1557077Antifungal activity against Candida albicans SN152 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID1309053Antifungal activity against Candida glabrata ATCC 2001 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID532150Antifungal activity against Cunninghamella species2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID283205Antimicrobial activity against Candida glabrata 21231 isolate by E-test2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth.
AID48793In vitro evaluation of minimum inhibitory concentration against Candida tropicalis 2.111995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID532559Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 2 ug/ml (Rvb = 0.144%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID515011Antifungal activity against Candida parapsilosis by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID564269Antifungal activity against Candida albicans isolate 6 after 48 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B.
AID531245Antifungal activity against Candida krusei assessed as susceptible isolates after 48 hrs by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
In vitro susceptibilities of invasive isolates of Candida species: rapid increase in rates of fluconazole susceptible-dose dependent Candida glabrata isolates.
AID1783773Antifungal activity against Cryptococcus neoformans CGMCC2.3161 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID322856Antifungal activity against azole-resistant Aspergillus fumigatus V28/78-CM3275 isolate from patient with acute myeloid leukemia by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID575477Antifungal activity against 10'7 CFU/ml Candida albicans B2630 infected in vulvovaginitis rat model assessed as fungal burden at 5 mg/kg, po SID2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID1265819Antifungal activity against azole-resistant Candida albicans MYA-1237 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID633996Antifungal activity against Saccharomyces cerevisiae ATCC 24657 assessed as growth inhibition at 90.7 uM after 24 hrs by agar plate bioassay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID436743Antifungal activity against Aspergillus fumigatus after 7 days by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID150752Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID581861Antifungal activity against Candida krusei isolated from neutropenic subjects with AML or MDS prior to initiation of fluconazole therapy assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID522126Antimicrobial activity against deltacrz1 mutant containing Candida glabrata TG173 complemented with CRZ1 gene by colorimetric microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Roles of calcineurin and Crz1 in antifungal susceptibility and virulence of Candida glabrata.
AID405097Antimicrobial activity against Absidia sp. after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID563402Antifungal activity against Aspergillus niger isolate CM-5095 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1157295Antifungal activity against Aspergillus fumigatus 07544 assessed as growth inhibition by automatic microplate reader analysis2014Journal of natural products, May-23, Volume: 77, Issue:5
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
AID1419500Antifungal activity against Candida glabrata ATCC 2001 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID519445Antimicrobial activity against Neosartorya pseudofischeri isolate CNM-CM-2270 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1204525Antifungal activity against Candida parapsilosis by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID584597Antifungal activity against 1 day cultured Candida krusei isolated from neutropenic subject with AML or MDS pharynx receiving antifungal therapy for 19 days after 6 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1309050Antifungal activity against Candida albicans ATCC MYA-2310 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID525142Antifungal activity against Fusarium thapsinum by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID1877286Antifungal activity against Aspergillus fumigatus CGMCC3.7795 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID1491244Antifungal activity against Candida tropicalis cgmcc 2.3739 by broth microdilution method2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
AID49631Minimum inhibitory concentration of compound for antifungal activity against Candida albicans 12000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID1770931Ratio of MFC for fungicidal activity against Candida albicans ATCC SC5314 to MIC for Antifungal activity against Candida albicans ATCC SC53142021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID405094Antimicrobial activity against Rhizopus microsporus var. rhizopodiformis after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID545151Antimicrobial activity against Candida albicans isolate R after 48 hrs by EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing.
AID341555Clearance in human at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID518401Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A G138C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1474170Antifungal activity against Cryptococcus neoformans cgmcc 2.3161 by broth microdilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents.
AID1917559Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 30 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 1.40%)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells.
AID575456Cytotoxicity against human MRC5 cells2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID509389Antifungal activity against 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected in po dosed OF1 mouse assessed as reduction in fungal load in brain at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID285865Antimicrobial susceptibility of Pichia anomala from nosocomial fungemia patient assessed as percent susceptible isolates at 0.06 ug/ml by EUCAST method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antifungal drug susceptibility profile of Pichia anomala isolates from patients presenting with nosocomial fungemia.
AID525595Antibacterial activity against Fluconazole resistant Candida albicans DSY3606 containing tac1delta/delta ERG11-1/ERG11-1 (TAC1-5) genotype by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID405110Antimicrobial activity against Absidia sp. assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID575377Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as decreased fungal load in lung at 50 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated contr2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID572695Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP164A2 at pH7.52009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae.
AID518599Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, Q141H mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID341576Tmax in children of >6-12 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID440324Antifungal activity against Aspergillus versicolor isolated from patient skin after 48 hrs by broth microdilution method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
AID584411Antifungal activity against 2 days cultured Candida tropicalis isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 45 days after 24 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID729310Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID532141Antifungal activity against Aspergillus niger2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID484287Aggregation-based binding affinity to beta-lactamase AmpC at 200 uM in fed state simulated intestinal fluid after 30 mins by silver staining in presence of 2% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1597996Antifungal activity against Candida albicans after 24 hrs by NCCLS protocol based method2019European journal of medicinal chemistry, May-15, Volume: 170Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
AID419071Antifungal activity against Candida albicans SANK 514862009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID405061Antifungal activity against Sporothrix schenckii P30915 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID48051Minimum inhibitory concentration of compound for antifungal activity against Candida parapsilosis2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID554705Antimicrobial activity against Candida krusei B2399 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID563392Antifungal activity against Aspergillus niger isolate CM-3586 obtained from catheter of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID532557Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 16 ug/ml (Rvb = 0.144%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID554710Antimicrobial activity against Candida krusei NZCDC 90.147 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID518607Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, M172V, L358L, C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID563418Antifungal activity against Aspergillus tubingensis isolate CM-4897 obtained from blood culture after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID1849833Antifungal activity against Sporothrix brasiliensis assessed as fungal growth inhibition incubated for 48 hrs by CLSI-based broth microdilution assay2021European journal of medicinal chemistry, Jan-15, Volume: 210A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials.
AID1534781Half life in human liver microsomes at 1 uM by LC-MS/MS analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Development of posaconazole-based analogues as hedgehog signaling pathway inhibitors.
AID575365Antifungal activity against Cunninghamella bertholletiae UTSCH 05-2275 infected in diabetic OF1 mouse assessed as decreased fungal load in brain at 50 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID554713Antimicrobial activity against Candida krusei NZCDC 89.021 after 48 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID1557087Antifungal activity against Candida glabrata ATCC 66032 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID546077Antifungal activity against Candida pelliculosa isolated from candidemia patient by AFST-EUCAST microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
A 10-year survey of antifungal susceptibility of candidemia isolates from intensive care unit patients in Greece.
AID555822Ratio of MIC50 for Candida albicans 5674 to MIC50 for cdr2/cdr2 deficient Candida albicans STY72009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance.
AID575478Antifungal activity against 10'7 CFU/ml Candida albicans B2630 infected in vulvovaginitis rat model assessed as fungal burden at 10 mg/kg administered tropically twice daily measured after 3 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID575457Antifungal activity against 5 x 10'6 CFU/ml Microsporum canis B68128 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID575201Antifungal activity against Cunninghamella bertholletiae FMR-9598 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID1589584Substrate activity at P-glycoprotein in human Caco2 cells assessed as efflux ratio by LC-MS/MS analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.
AID1309052Antifungal activity against Candida albicans ATCC MYA-1003 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1658277Inhibition of NPC1 in HUVEC cells assessed as accumulation of cholesterol in perinuclear structure at 0.2 uM incubated for 24 hrs by filipin staining based confocal microscopy analysis
AID284107Antifungal activity against Candida neoformans IM 031706 after 48 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and antifungal activity of (Z)-5-arylidenerhodanines.
AID1524625Antifungal activity against Candida albicans 7535 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID665070Antifungal activity against Cryptococcus neoformans after 72 hrs by serial dilution method2012European journal of medicinal chemistry, Jul, Volume: 53Design, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains.
AID581881Antifungal activity against Candida glabrata isolated from HSCT recipient 474 with acute or chronic GVHD mouth receiving antifungal drug after 124 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405035Antifungal activity against Sporothrix schenckii PSCC1 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1223576Ratio of Ki for CYP3A4.7 (unknown origin) to Ki for CYP3A4.1 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID249273Minimum inhibitory concentration against Trichophyton mentagrophytes (n=20)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID519059Antifungal activity against Candida parapsilosis assessed as susceptible isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID575754Antimicrobial activity against Aspergillus fumigatus AF2932010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
AID1204538Antifungal activity against Candida albicans Strain 8 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID532331Antifungal activity against Aspergillus terreus by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID549317Antifungal activity against Cunninghamella bertholletiae after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID405112Antimicrobial activity against Cunninghamella sp. assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1334864Inhibition of CYP3A4 in human liver microsomes assessed as reduction in nifedipine oxidation incubated for 10 mins2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID405060Antifungal activity against Sporothrix schenckii P30915 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID554706Antimicrobial activity against Candida krusei IFO0011 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID405062Antifungal activity against Sporothrix schenckii P30915 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID565399Antifungal activity against Rhizopus microsporus IHEM 18821 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID405017Antifungal activity against Sporothrix schenckii P25013 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1674376AUC at steady state in human administered as single dose2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID563403Antifungal activity against Aspergillus tubingensis isolate CM-3123 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID340950Antifungal activity against Candida albicans isolates from HIV infected patient during fluconazole therapy by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID518594Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, S297T, F495 mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1067046Antifungal activity against Candida parapsilosis by micro-broth dilution method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates.
AID1180168Antifungal activity against Candida albicans by broth macrodilution method2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design and optimization of highly-selective fungal CYP51 inhibitors.
AID1059355Antifungal activity against Candida albicans clinical isolate after 20 hrs by agar dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID768327Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID1254072Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID405041Antifungal activity against Sporothrix schenckii P10012 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID648419Antifungal activity against Aspergillus fumigatus NCIM 902 at MIC after 3 to 4 days2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID581884Antifungal activity against Candida glabrata isolated from HSCT recipient 270 with acute or chronic GVHD mouth after 108 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID545152Antimicrobial activity against Candida albicans isolate R after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing.
AID405054Antifungal activity against Sporothrix schenckii PJRC002 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1474169Antifungal activity against Candida albicans CPCC 400523 by broth microdilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents.
AID56597Compound was tested for inherent antifungal geometric minimum inhibitory concentration (GMMIC) against Dermatophytes in serial dilution from 64 to 0.0313 ug/mL2002Bioorganic & medicinal chemistry letters, Jul-08, Volume: 12, Issue:13
Synthesis and antifungal activity of the 2,2,5-tetrahydrofuran regioisomers of SCH 51048.
AID725875Antifungal activity against Aspergillus fumigatus ASFU17 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID714985Antifungal activity against Saccharomyces cerevisiae MYH 500 assessed as growth inhibition in presence of 30 mM sodium fluoride after 9 hrs2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Fluoride enhances the activity of fungicides that destabilize cell membranes.
AID249272Minimum inhibitory concentration against Epidermophyton floccosum (n=12)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID246926Effective dose was measured in guinea pig infected with Microsporum canis on 7th day2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID341564Tmax in infants of 0.6-2 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1689213Antifungal activity against fluconazole-resistant Candida auris 383 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID249271Minimum inhibitory concentration against Trichophyton tonsurans (n=18)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID655587Antifungal activity against Aspergillus fumigatus by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID405063Antifungal activity against Sporothrix schenckii P3287 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID753512Antidermatophytic activity against Microsporum gypseum isolate after 7 days by broth microdilution method2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID575454Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as decreased fungal load in brain at 50 mg/kg, po bid administered 1 day post infection measured after 4 to 5 days relative to untreated cont2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID341538Cmax in infants of 0.6-2 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID532531Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as accumulation of 14-alpha-methylergosta-8,24(28)-dien-3beta-6alpha-diol at 8 ug/ml2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID575497Antifungal activity against Aspergillus nidulans isolate2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID1071690Antifungal activity against Candida parapsilosis ATCC 22019 assessed as growth inhibition by microdliution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Antifungal ether diglycosides from Matayba guianensis Aublet.
AID1076033Antifungal activity against Candida parapsilosis ATCC 22019 by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID50296Minimum inhibitory concentration of compound for antifungal activity against Candida krusei2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID575203Antifungal activity against Cunninghamella bertholletiae UTHSC 03-2241 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID176378Efficacy against Candida albicans CY1002 on day 14th after peroral administration in rat2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
AID1609929Antifungal activity against Candida parapsilosis GIM 2.190 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID519441Antimicrobial activity against Neosartorya hiratsukae isolate CNM-CM-3764 obtained from oropharyngeal exudate of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID371232Antimicrobial activity against Candida krusei ATCC 6258 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID584589Antifungal activity against 15 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 168 days after 113 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1413335Antifungal activity against resistant Candida parapsilosis2018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID581874Antifungal activity against Candida glabrata isolated from neutropenic subject 1497 with AML or MDS pharynx after 61 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1155875Antifungal activity against Microsporum gypseum assessed as growth inhibition by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID432802Antifungal activity against Sporothrix mexicana after 72 hrs by microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro antifungal susceptibilities of five species of sporothrix.
AID1334847Anti-fungal activity against Candida albicans SC5314 by broth microdilution method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
AID1309049Antifungal activity against Candida albicans ATCC MYA-90819 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID563401Antifungal activity against Aspergillus tubingensis isolate CM-5094 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID575066Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as increase in mouse survival rate at 25 mg/kg, po bid administered 1 day after infection for 7 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID322852Antifungal activity against azole-resistant Aspergillus fumigatus M03/669-CM2627 isolate from patient by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID584590Antifungal activity against 43 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 168 days after 113 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID405032Antifungal activity against Sporothrix schenckii P24223 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1556212Antifungal activity against Aspergillus fumigatus CGMCC 3.7795 assessed as inhibition of visible microbial growth by NCCLS protocol based method2019European journal of medicinal chemistry, Sep-01, Volume: 177Design, synthesis, and structure-activity relationship studies of l-amino alcohol derivatives as broad-spectrum antifungal agents.
AID519058Antifungal activity against Candida krusei assessed as susceptible isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID768337Antifungal activity against Aspergillus fumigatus ATCC 204305 after 48 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID1204536Antifungal activity against Candida albicans Strain 6 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1586469Antifungal activity against Histoplasma capsulatum G217B after 10 to 14 days by microscopic method2018Journal of natural products, 12-28, Volume: 81, Issue:12
Onydecalins, Fungal Polyketides with Anti- Histoplasma and Anti-TRP Activity.
AID1511951Inhibition of Hedgehog signaling pathway in mouse ASZ001 cells assessed as decrease in Gli1 mRNA expression after 48 hrs by qRT-PCR analysis2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
Truncated Itraconazole Analogues Exhibiting Potent Anti-Hedgehog Activity and Improved Drug-like Properties.
AID584596Antifungal activity against 177 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 172 days after 114 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID532534Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as accumulation of lanosterol at 8 ug/ml (Rvb = 23+/- 1.08 %)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID1491245Antifungal activity against Aspergillus fumigatus GIM 3.524 by broth microdilution method2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
AID584587Antifungal activity against 111 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 143 days after 116 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID541566AUC (0 to 24 hrs) in healthy human lung epithelial lining fluid at 200 mg, po every 12 hrs for 5 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1872501Antifungal activity against Candida krusei2022European journal of medicinal chemistry, Mar-05, Volume: 231Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development.
AID45494In vitro evaluation of minimum inhibitory concentration against Candida albicans 761995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID405047Antifungal activity against Sporothrix schenckii SSA29 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID322550Antifungal activity against Microsporum gypseum after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID1524624Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1283997Antifungal activity against Candida albicans ATCC 10231 by M27-A3 protocol-based broth microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID1283998Antifungal activity against Candida tropicalis ATCC 13803 by M27-A3 protocol-based broth microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID1061738Antimicrobial activity against Trichophyton rubrum by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID1164093Antifungal activity against Candida parapsilosis ATCC 22019 by broth microdilution method2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents.
AID518601Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, L339L mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID747168Antimicrobial activity against Candida parapsilosis ATCC 90030 by broth dilution method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Synthesis and antimicrobial activity of novel amphiphilic aromatic amino alcohols.
AID537736Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1898178Antifungal activity against Candida auris 887
AID294855Antifungal activity against Microsporum gypseum after 7 days by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID714984Antifungal activity against Saccharomyces cerevisiae MYH 500 assessed as growth inhibition in presence of 80 mM sodium fluoride after 9 hrs2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Fluoride enhances the activity of fungicides that destabilize cell membranes.
AID584592Antifungal activity against -2 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 172 days after 114 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID525594Antibacterial activity against Fluconazole resistant Candida albicans DSY3706 containing tac1delta/delta ERG11-1/ERG11-1 genotype by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID1770933Anti-biofilm activity in Candida albicans CPCC400616 assessed as inhibition of biofilm formation incubated for 24 hrs by XTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID584598Antifungal activity against 6 days cultured Candida krusei isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 19 days after 6 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1557084Antifungal activity against Candida dubliniensis T-99 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID1783069Antifungal activity against fluconazole-sensitive Candida albicans 10061 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID405040Antifungal activity against Sporothrix schenckii P10012 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID581876Antifungal activity against Candida glabrata isolated from neutropenic subject 1491 with AML or MDS pharynx after 23 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID554717Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID582235Antifungal activity against Candida albicans isolated from neutropenic subjects with AML or MDS receiving posaconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1076026Antifungal activity against Candida sp. clinical isolate 12485 derived from urine by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID1597997Antifungal activity against Candida tropicalis after 24 hrs by NCCLS protocol based method2019European journal of medicinal chemistry, May-15, Volume: 170Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
AID609892Antifungal activity against Candida parapsilosis by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID50295Minimum concentration required to inhibit the growth of Candida krusei2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID1549139Antifungal activity against azole-resistant Candida albicans 4108 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID532161Antifungal activity against Candida albicans by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID655580Antifungal activity against Candida albicans SC5314 after 24 hrs by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID1689827Antifungal activity against Mucor circinelloides MURI1 assessed as reduction in microbial growth after 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID341567Cmax in human at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID524740Antimicrobial activity against Fusarium subglutinans after 48 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Species distribution and in vitro antifungal susceptibility patterns of 75 clinical isolates of Fusarium spp. from northern Italy.
AID1898169Antifungal activity against Candida tropicalis 112936
AID518595Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A L98H, F495I mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1076021Cytotoxicity against human A549 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID1689227Antifungal activity against Aspergillus fumigatus NR 35304 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID532130Antifungal activity against Candida tropicalis2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1059348Fungicidal activity against Candida parapsilosis clinical isolate by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID606212Antifungal activity against Candida albicans ATCC Y0109 after 24 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives.
AID1595045Antifungal activity against Candida glabrata assessed as reduction in fungal cell growth incubated for 48 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID532045Antifungal activity against Lichtheimia ornata clinical isolate after 24 hrs by EUCAST method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
AID725877Antifungal activity against Aspergillus fumigatus ASFU13 after 48 hrs by M38 method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
AID565400Antifungal activity against Rhizopus microsporus IHEM 13267 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation of in vitro activity, serum levels, and in vivo efficacy of posaconazole against Rhizopus microsporus in a murine disseminated infection.
AID602928Antifungal activity against Candida tropicalis by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID1254073Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID509388Antifungal activity against 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected in po dosed OF1 mouse assessed as reduction in fungal load in kidney at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID1413315Antifungal activity against Cryptococcus neoformans 90-262018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID307628Antifungal activity against Aspergillus fumigatus AF980003 by alamar blue assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety.
AID575459Antifungal activity against 5 x 10'6 CFU/ml Trichophyton rubrum B68183 by resazurin based fluorimetry assay2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID581894Antifungal activity against Candida albicans isolated from HSCT recipient 928 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1180174Selectivity index, ratio of IC50 for human hepatocytes CYP3A4 to MIC for Trichophyton rubrum2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Design and optimization of highly-selective fungal CYP51 inhibitors.
AID420666Antifungal activity against Microsporum gypseum by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID1911627Antifungal activity against Aspergillus fumigatus shjt40 assessed as fungal growth inhibition by broth microdilution assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Development of Lipo-γ-AA Peptides as Potent Antifungal Agents.
AID768339Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for Candida krusei ATCC 62582013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID581883Antifungal activity against Candida glabrata isolated from HSCT recipient 975 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1330316Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol-stimulated Ca2+ flux up to 100 uM after 30 mins by calcium-4 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID424619Antimicrobial activity against azole-susceptible Candida albicans isolate CA8 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1595074Antifungal activity against Trichophyton mentagrophytes assessed as reduction in fungal cell growth incubated for 3 to 4 days by disk diffusion method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID549327Antifungal activity against Actinomucor spp. after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID1689223Antifungal activity against Cryptococcus neoformans NR48770 assessed as reduction in fungal growth incubated for 48 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID584405Antifungal activity against 23 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 25 days after 3 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID323075Antifungal activity against Cryptococcus neoformans IM 961951 by micro-broth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID555137Antimicrobial activity against Candida parapsilosis ATCC 22019 by CLSI M27-A2 broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID532329Antifungal activity against Geotrichum candidum by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID609325Oral bioavailability in rat at 10 mg/kg, administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID736605Antifungal activity against azole-resistant Candida albicans clinical isolate 7.O.A assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID1419497Antifungal activity against ITC and FLC-susceptible Candida albicans ATCC MYA-2310 incubated for 48 hrs by modified CLSI M27-A3 protocol based method2017European journal of medicinal chemistry, Jun-16, Volume: 133Novel alkylated azoles as potent antifungals.
AID532553Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 0.5 ug/ml (Rvb = 0.157%)2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID341551Clearance in adolescents of >12-16 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID679463TP_TRANSPORTER: inhibition of Daunorubicin transport in G185 cells2002Antimicrobial agents and chemotherapy, Jan, Volume: 46, Issue:1
Interaction of common azole antifungals with P glycoprotein.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID543972Cmax in human at 15 mg, po pretreated with itraconazole at 200 mg, po qd for 4 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Voriconazole increases while itraconazole decreases plasma meloxicam concentrations.
AID537733Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID648413Antifungal activity against recultured Penicillium marneffei at MIC after 3 to 4 days2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID371237Antimicrobial activity against Aspergillus fumigatus SANK 18497 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID246929Effective dose was measured in guinea pig infected with Microsporum canis on 14th day2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID532351Antifungal activity against Bipolaris australiensis by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1609933Antifungal activity against fluconazole-resistant Candida albicans 904 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID1901374Toxicity in Galleria mellonella larvae assessed as melanization of larvae at 0.23 ug/ml measured every 24 hrs upto 5 days relative to control2022European journal of medicinal chemistry, Feb-15, Volume: 230Tetrazole derivatives bearing benzodiazepine moiety-synthesis and action mode against virulence of Candida albicans.
AID341133Antifungal activity against sSaccharomyces cerevisiae isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID1204558Antifungal activity against Candida albicans Strain 28 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID340952Antifungal activity against Candida albicans isolates by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID73613The compound was tested in vitro for antifungal activity against 6 filamentous fungi.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol.
AID522128Antimicrobial activity against calcineurin deltacnb1 mutant containing Candida glabrata TG163 complemented with CNB1 gene by colorimetric microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Roles of calcineurin and Crz1 in antifungal susceptibility and virulence of Candida glabrata.
AID341540Apparent volume of distribution in infants of 0.6-2 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID575752Antimicrobial activity against Aspergillus fumigatus CEA102010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
AID1549140Antifungal activity against azole-resistant Candida tropicalis 5008 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID341542Cmax in children of >2-6 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID518616Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A G54E mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID262552Antifungal activity against Trichophyton rubrum2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID1413333Antifungal activity against Candida albicans B-3112018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID1415220Antiangiogenic activity in HUVEC assessed as inhibition of tube formation at 5 uM after 24 hrs by matrigel assay relative to control2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Novel Tetrazole-Containing Analogues of Itraconazole as Potent Antiangiogenic Agents with Reduced Cytochrome P450 3A4 Inhibition.
AID519426Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-3538 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID428913Antifungal activity against Cryptococcus neoformans ATCC 24067 after 72 hrs by NCCLS M27A method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Voriconazole inhibits melanization in Cryptococcus neoformans.
AID1770940Antifungal activity against Cryptococcus neoformans CGMCC2.3161 assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID519446Antimicrobial activity against Neosartorya pseudofischeri isolate CNM-CM-4060 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1595072Antifungal activity against Aspergillus fumigatus NCIM 902 assessed as reduction in fungal cell growth incubated for 3 to 4 days by disk diffusion method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID554711Antimicrobial activity against Candida krusei B2399 after 48 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID551207Antifungal activity against Candida parapsilosis by broth microdilution method2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
New azoles with antifungal activity: Design, synthesis, and molecular docking.
AID1204530Antifungal activity against Rhizopus oryzae ATCC 10329 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID575487Antifungal activity against azole-susceptible Aspergillus fumigatus isolate CM-237 assessed as fungal growth at 4 mg/l relative to control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
AID1254069Antibacterial activity against Staphylococcus aureus 503 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID405057Antifungal activity against Sporothrix schenckii P14036 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID655586Antifungal activity against Trichophyton rubrum by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID519442Antimicrobial activity against Neosartorya hiratsukae isolate CNM-CM-3740 obtained from oropharyngeal exudate of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID1904363Antifungal activity against Aspergillus fumigatus CGMCC 3.7795 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID39390In vitro evaluation of minimum inhibitory concentration against Aspergillus flavus 191995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID581889Antifungal activity against Candida albicans isolated from HSCT recipient 031 with acute or chronic GVHD mouth receiving antifungal drug after 109 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1265818Antifungal activity against azole-susceptible Candida albicans ATCC MYA-2310 after 48 hrs by microbroth dilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles.
AID603345Antifungal activity against Trichophyton rubrum clinical isolate by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID563393Antifungal activity against Aspergillus niger isolate CM-3636 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID294848Antifungal activity against Candida albicans ATCC Y0109 after 24 hrs by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID1204524Antifungal activity against Candida krusei by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID549324Antifungal activity against Cunninghamella spp. after 24 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.
AID581896Antifungal activity against Candida glabrata isolated from neutropenic subject 1331 with AML or MDS pharynx after 21 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID371227Antimicrobial activity against Candida albicans SANK 51486 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID519062Antifungal activity against Candida glabrata assessed as resistant isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID603261Antifungal activity against Candida tropicalis clinical isolate by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID768324Antifungal activity against Candida parapsilosis ATCC 22019 at > MIC up to 24 hrs by time kill study2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID1059360Fungicidal activity against Candida tropicalis by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID566878Antifungal activity against Candida parapsilosis by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID681120TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID545673Ratio of intracellular to extracellular drug uptake in alveolar macrophages of New Zealand white rabbit infected with Mycobacterium bovis at 1 ug/ml in presence of 100% serum2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Intracellular concentrations of posaconazole in different compartments of peripheral blood.
AID554724Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Candida krusei ERG11C to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID609889Antifungal activity against Candida albicans SC5314 by micro-broth dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
AID1904359Antifungal activity against Cryptococcus neoformans CGMCC 2.3161 assessed as fungal growth inhibition by CLSI based serial microbroth dilution method2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
AID581887Antifungal activity against Saccharomyces cerevisiae isolated from HSCT recipient 513 with acute or chronic GVHD mouth receiving antifungal drug after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1674375Oral bioavailability in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID371228Antimicrobial activity against Candida albicans TIMM 3164 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID648412Antifungal activity against recultured Penicillium marneffei by serial plate dilution method2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID1413334Antifungal activity against Candida albicans 94-21812018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID581871Antifungal activity against Candida glabrata isolated from neutropenic subject 1318 with AML or MDS stool receiving antifungal drug after 36 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID549053Antifungal activity against Candida albicans CA138 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID262547Antifungal activity against Candida parapsilosis2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.
AID1076032Antifungal activity against Candida sp. clinical isolate 13184 derived from high vaginal swabs by microbroth dilution method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide.
AID655585Antifungal activity against Candida kefyr by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies.
AID1689218Antifungal activity against Candida parapsilosis CAB 502638 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID519432Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4415 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID519434Antimicrobial activity against Aspergillus lentulus isolate CNM-CM-4426 obtained from sputum of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID563420Antifungal activity against Aspergillus foetidus isolate CM-4995 obtained from prosthesis after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID508313Antifungal activity against Aspergillus fumigatus isolate V52-35 harboring TR L98H mutation in Cyp51A protein by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Efficacy of posaconazole against three clinical Aspergillus fumigatus isolates with mutations in the cyp51A gene.
AID1658273Inhibition of NPC1/VDAC1 in HUVEC cells assessed as reduction in cell proliferation pretreated for 24 hrs followed by [3H]thymidine incorporation by scintillation counter method
AID119038Tested in vivo for anti-candida activity in mice model 1 (dose:0.5 mg/kg, fluconazole-treated group)1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
AID582237Antifungal activity against Candida glabrata isolated from neutropenic subjects with AML or MDS receiving posaconazole assessed as maximum MIC by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1674368Unbound clearance in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID634087Antifungal activity against Candida albicans assessed as morphogenetic transformation after 3 hrs by phase-contrast microscopy2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.
AID555139Antimicrobial activity against Candida krusei ATCC 6258 by CLSI M27-A2 broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes.
AID436745Antifungal activity against Candida parapsilosis after 24 hrs by serial dilution method2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
New azoles with potent antifungal activity: design, synthesis and molecular docking.
AID340949Antifungal activity against Candida albicans isolates from HIV infected patient before fluconazole therapy by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID584595Antifungal activity against 176 days cultured Candida glabrata isolated from HSCT recipient with acute or chronic GVHD mouth receiving antifungal therapy for 172 days after 114 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID566887Antifungal activity against Aspergillus terreus by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID532148Antifungal activity against Mucor hiemalis2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1491241Antifungal activity against Candida albicans CPCC 400523 by broth microdilution method2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
AID424636Antimicrobial activity against azole-resistant Candida albicans isolate CA135 cotreated with calcineurin signaling inhibitor Tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID768342Antifungal activity against Candida krusei ATCC 6258 after 24 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antifungal activity of terpenyl-1,4-naphthoquinone and 1,4-anthracenedione derivatives.
AID545166Antimicrobial activity against Candida albicans isolate C after 48 hrs by microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing.
AID323071Antifungal activity against Cryptococcus neoformans IM 00319 by microbroth dilution method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
AID1689215Antifungal activity against Candida glabrata ATCC 66032 assessed as reduction in fungal growth incubated for 24 hrs by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID325037Antimicrobial activity against Candida albicans SC5314 after 48 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole.
AID405029Antifungal activity against Sporothrix schenckii MRSS4 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID603344Antifungal activity against Cryptococcus neoformans ATCC BLS108 after 72 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and molecular docking studies of novel triazole as antifungal agent.
AID701451Antifungal activity against Candida tropicalis2012Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
The biology and chemistry of antifungal agents: a review.
AID1898162Antifungal activity against Candida albicans 14#
AID602926Antifungal activity against Candida albicans SC5314 after 24 hrs by micro-broth dilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
AID1254067Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID405056Antifungal activity against Sporothrix schenckii PJRC002 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by ATB Fungus 2 method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1595049Antifungal activity against Candida tropicalis assessed as reduction in fungal cell growth incubated for 48 hrs by broth microdilution method2019European journal of medicinal chemistry, May-15, Volume: 170Tetrazole hybrids and their antifungal activities.
AID47895Minimum concentration required to inhibit the growth of Candida parapsilosis2000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity.
AID1634357Antifungal activity against Candida albicans ATCC SC5314 assessed as inhibition of visible microbe growth by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.
AID519443Antimicrobial activity against Neosartorya hiratsukae isolate CNM-CM-4328 obtained from cornea of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID532133Antifungal activity against Cryptococcus neoformans var. neoformans2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID584396Antifungal activity against 13 days cultured Candida krusei isolated from invasive fungal infected subject blood after 12 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID575747Binding affinity to Aspergillus fumigatus AF293 sterol 14-alpha demethylase isoenzyme A expressed in Escherichia coli2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
AID294849Antifungal activity against Candida parapsilosis ATCC 0306392 after 7 days by micro-broth dilution method2007European journal of medicinal chemistry, Sep, Volume: 42, Issue:9
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).
AID575202Antifungal activity against Cunninghamella bertholletiae UTHSC 04-2581 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID527134Antifungal activity against Microsporum canis LMGO 02 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID525590Antibacterial activity against azole-susceptible Candida albicans DSY294 by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID665071Antifungal activity against Candida krusei after 24 hrs by serial dilution method2012European journal of medicinal chemistry, Jul, Volume: 53Design, synthesis and structure-activity relationships of new triazole derivatives containing N-substituted phenoxypropylamino side chains.
AID419075Antifungal activity against Cryptococcus neoformans TIMM 18552009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID484389Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 20 uM by dynamic light scattering assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID420661Antifungal activity against Cryptococcus neoformans ATCC 32609 after 72 hrs by micro-broth dilution method2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID1204528Antifungal activity against Aspergillus fumigatus 16907 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID582801Antifungal activity against Candida albicans isolate 490 harboring ERG3 D147G, T330A, A351V and ERG11 F72S, T229A, E266D, N440S, V488I, R523G mutant genes by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID1674370Unbound volume of distribution at steady state in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
AID582796Antifungal activity against Candida albicans isolate 6 by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID510817Antifungal activity against Aspergillus fumigatus ATCC 204305 after 24 hrs by AFSTEUCAST assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and biological evaluation of (+)-labdadienedial, derivatives and precursors from (+)-sclareolide.
AID1634360Antifungal activity against Candida tropicalis cgmcc 2.3739 assessed as inhibition of visible microbe growth by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.
AID319752Antimicrobial activity against Candida tropicalis isolates2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
AID419074Antifungal activity against Candida tropicalis ATCC 7502009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID1357635Antifungal activity against Cryptococcus gattii ATCC 32608 after 72 hrs by microbroth dilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID1783068Antifungal activity against fluconazole-sensitive Candida albicans 4108 assessed as inhibition of fungal growth2021European journal of medicinal chemistry, Oct-05, Volume: 221Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections.
AID575200Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID1898161Antifungal activity against Candida albicans 162
AID581890Antifungal activity against Candida albicans isolated from HSCT recipient 462 with acute or chronic GVHD mouth after 112 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID1309055Antifungal activity against Candida parapsilosis ATCC 22019 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID1877281Antifungal activity against Candida tropicalis CGMCC 2.3739 assessed as fungal growth inhibition by NCCLS protocol based method2022European journal of medicinal chemistry, Jan-05, Volume: 227Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents.
AID419078Antifungal activity against Candida albicans ATCC 244332009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID341546Cmax in children of >6-12 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID563579Cmin in healthy human plasma before initiation of 3 mg/kg QD2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Development, validation, and routine application of a high-performance liquid chromatography method coupled with a single mass detector for quantification of itraconazole, voriconazole, and posaconazole in human plasma.
AID289593Antifungal activity against Aspergillus fumigatus by serial plate dilution method2007European journal of medicinal chemistry, Mar, Volume: 42, Issue:3
Synthesis of some bioactive 2-bromo-5-methoxy-N'-[4-(aryl)-1,3-thiazol-2-yl]benzohydrazide derivatives.
AID521970Antibacterial activity against Fluconazole resistant Candida albicans DSY3752 containing (TAC1-5/TAC1-5 ERG11-1/ERG11-1) genotype by EUCAST standards based broth microdilution method sCandida albicans DSY2942010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID519285Antifungal activity against Candida parapsilosis ATCC 22019 by CLSI M27-A2 microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts.
AID532149Antifungal activity against Mucor species2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID283229Effect on Coccidioides immitis Silveira infection in CD1 mouse brain, spinal cord and lungs administered after 3 days of infection at 50 mg/kg, po bid after 10 days2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Comparison of itraconazole and fluconazole treatments in a murine model of coccidioidal meningitis.
AID424637Antimicrobial activity against azole-resistant Candida albicans isolate CA137 cotreated with calcineurin signaling inhibitor Tacrolimus after 48 hrs by microdilution checkerboard technique2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1873196Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by liquid scintillation counter analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID1770941Antifungal activity against Candida parapsilosis GIM2.190 assessed as fungal growth inhibition by CLSI protocol based method2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
AID575067Antifungal activity against Cunninghamella bertholletiae UTHSC 05-2275 infected in neutropenic OF1 mouse assessed as increase in mouse survival rate at 50 mg/kg, po bid administered 1 day after infection for 7 days relative to untreated control2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro and in vivo antifungal susceptibilities of the Mucoralean fungus Cunninghamella.
AID1061742Antimicrobial activity against Candida albicans SC5314 after 24 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID1283999Antifungal activity against Aspergillus fumigatus ATCC 16907 by M38-A protocol-based broth microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID1061736Antimicrobial activity against Microsporum gypseum by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID584407Antifungal activity against 7 days cultured Candida glabrata isolated from neutropenic subject with AML or MDS stool receiving antifungal therapy for 37 days after 9 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID371230Antimicrobial activity against Candida parapsilosis ATCC 90018 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID581900Antifungal activity against Candida glabrata isolated from HSCT recipient 497 with acute or chronic GVHD mouth after 114 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID736602Antifungal activity against voriconazole-resistant Candida glabrata clinical isolate 730 assessed as growth inhibition after 24 to 48 hrs by CLSI microbroth dilution method2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives.
AID249264Minimum inhibitory concentration against Aspergillus species (n=8)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
AID648416Antifungal activity against Aspergillus flavus NCIM 524 by serial plate dilution method2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID214425In vitro evaluation of minimum inhibitory concentration against Trichophyton rubrum 901995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
AID484390Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering-based beads autocorrelation assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1534784Inhibition of human ERG expressed in CHO cells at 25 uM by electrophysiology assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Development of posaconazole-based analogues as hedgehog signaling pathway inhibitors.
AID518402Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A M220R mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1557085Antifungal activity against Candida albicans ATCC 90028 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.
AID1059356Fungicidal activity against Candida dubliniensis by micro dilution method2013European journal of medicinal chemistry, , Volume: 70Designing and synthesis of novel antimicrobial heterocyclic analogs of fatty acids.
AID584393Antifungal activity against 1 day cultured Candida albicans isolated from HSCT recipient with acute or chronic GVHD mouth after 2 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID325036Antimicrobial activity against Candida albicans P5 after 24 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole.
AID1546103Antimicrobial activity against Proteus mirabilis after 24 hrs by agar disk diffusion method2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID1175556Antimicrobial activity against Trichophyton rubrum SNB-TR1 after 5 days2015Journal of natural products, Jan-23, Volume: 78, Issue:1
Antibacterial ilicicolinic acids C and D and ilicicolinal from Neonectria discophora SNB-CN63 isolated from a termite nest.
AID519438Antimicrobial activity against Aspergillus fumisynnematus isolate CNM-CM-3227 obtained from bronchoalveolar lavage fluid of patient after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification.
AID566885Antifungal activity against Aspergillus niger by microdilution test2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and antifungal activity of some substituted phenothiazines and related compounds.
AID322853Antifungal activity against azole-resistant Aspergillus fumigatus V13/02-CM3271 isolate from patient with X-linked chronic granulomatous disease by broth microdilution susceptibility test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
A new Aspergillus fumigatus resistance mechanism conferring in vitro cross-resistance to azole antifungals involves a combination of cyp51A alterations.
AID1357639Cytotoxicity against human HEK293 cells assessed as cell viability at 250 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives.
AID405104Antimicrobial activity against Rhizopus arrhizus assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID340954Antifungal activity against Candida glabrata ATCC 90030 by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID424620Antimicrobial activity against azole-susceptible Candida albicans isolate CA12 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID532324Antifungal activity against Saccharomyces cerevisiae by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID341545Half life in children of >2-6 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID541561Cmax in healthy human alveolar cell at 200 mg, po every 12 hrs for 5 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects.
AID1128928Antifungal activity against Cryptococcus gattii assessed as total growth inhibition by micro-broth dilution method2014European journal of medicinal chemistry, Apr-09, Volume: 76Imidazolylchromanones containing non-benzylic oxime ethers: synthesis and molecular modeling study of new azole antifungals selective against Cryptococcus gattii.
AID1204521Antifungal activity against Candida utilis ATCC 9226 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID1155874Antifungal activity against Trichophyton rubrum assessed as growth inhibition by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID341559AUC (0 to 24 hrs) in children of >2-6 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID648415Antifungal activity against recultured Trichophyton mentagrophytes at MIC after 3 to 4 days2012European journal of medicinal chemistry, May, Volume: 51Facile synthesis, characterization and pharmacological activities of 3,6-disubstituted 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 5,6-dihydro-3,6-disubstituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
AID1549137Antifungal activity against azole-resistant Candida albicans 0304103 after 48 hrs by spectrophotometry-based serial microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.
AID424624Antimicrobial activity against azole-resistant Candida albicans isolate CA15 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1309048Antifungal activity against Candida albicans ATCC MYA-2876 after 48 hrs by CLSI M27-A3 method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.
AID519282Antifungal activity against Candida krusei ATCC 6258 by CLSI M27-A2 microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts.
AID515013Antifungal activity against Trichophyton rubrum by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID405106Antimicrobial activity against Rhizopus microsporus var. microsporus assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID1411892Antifungal activity against Aspergillus fumigatus ATCC 16907 by M38-A guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID529667Antimicrobial activity against Paecilomyces variotii by microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Susceptibility testing and molecular classification of Paecilomyces spp.
AID532541Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 assessed as accumulation of 14-alpha-methylergosta-8,24(28)-dien-3beta-6alpha-diol at 8 ug/ml2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.
AID581877Antifungal activity against Candida glabrata isolated from neutropenic subject 1491 with AML or MDS pharynx receiving antifungal drug after 23 days prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID525593Antibacterial activity against Fluconazole resistant Candida albicans DSY3604 containing tac1delta/delta ERG11-1/ERG11-5 genotype by EUCAST standards based broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic dissection of azole resistance mechanisms in Candida albicans and their validation in a mouse model of disseminated infection.
AID575472Half life in guinea pig infected with 10'6 CFU Microsporum canis B68128 at 20 mg/kg, po administered 2 hrs before infection for 5 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.
AID371233Antimicrobial activity against Candida tropicalis ATCC 750 by broth microdilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID515012Antifungal activity against Candida tropicalis by micro-broth dilution method2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase.
AID543975Fraction unbound in human at 15 mg, po pretreated with itraconazole at 200 mg, po qd for 4 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Voriconazole increases while itraconazole decreases plasma meloxicam concentrations.
AID1330315Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-stimulated Ca2+ flux up to 100 uM after 30 mins by calcium-4 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID554718Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Saccharomyces cerevisiae ERG11 after 48 hrs by liquid microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.
AID518611Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A F46Y, G89G, M172V, N248T, D255E, L358L, E427K, C454C mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID405069Antifungal activity against Candida parapsilosis ATCC 22019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID341550Cmax in adolescents of >12-16 yrs age at risk for fungal infection at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID532319Antifungal activity against Candida parapsilosis by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1061737Antimicrobial activity against Aspergillus fumigatus by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and evaluation of novel azoles as potent antifungal agents.
AID582998Antimicrobial activity against Saccharomyces cerevisiae YUG37 transformed with plasmid carrying cyp51A gene with doxycycline-regulatable promoter by broth dilution method in presence of doxycycline2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Complementation of a Saccharomyces cerevisiae ERG11/CYP51 (sterol 14α-demethylase) doxycycline-regulated mutant and screening of the azole sensitivity of Aspergillus fumigatus isoenzymes CYP51A and CYP51B.
AID419082Antifungal activity against Aspergillus fumigatus ATCC 264302009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID527139Antifungal activity against Candida albicans ATCC 10231 after 5 days microdilution technique2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Search for antifungal compounds from the wood of durable tropical trees.
AID1491243Antifungal activity against Cryptococcus neoformans cgmcc 2.3161 by broth microdilution method2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
AID405043Antifungal activity against Sporothrix schenckii P1621 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1283996Antifungal activity against Candida utilis ATCC 9226 by M27-A3 protocol-based broth microdilution method2016European journal of medicinal chemistry, Apr-13, Volume: 112Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.
AID340956Antifungal activity against Candida krusei ATCC 6258 by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID425135Antimicrobial activity against azole-susceptible Candida albicans isolate CA14 assessed as log reduction in colony count at 1 ug/ml co-treated with calcineurin signaling inhibitor tacrolimus after 48 hrs by time killing test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1473926Drug concentration at steady state in human at 200 mg, po QD for 1 to 2 weeks after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID620356Antifungal activity against Candida albicans RCMB 005002 at 30 ug/ml after 3 to 4 days by agar well diffusion method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives.
AID405073Antifungal activity against Aspergillus flavus ATCC 204304 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1325030Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells at 5 uM measured after 10 hrs by DAPI staining based fluorescence microscopic assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists.
AID1155869Antifungal activity against Candida parapsilosis assessed as growth inhibition after 24 hrs by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID1783776Antifungal activity against Candida krusei GIM2.1 assessed as inhibition of fungal growth by NCCLS protocol based method2021European journal of medicinal chemistry, Nov-15, Volume: 224Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
AID1609932Antifungal activity against fluconazole-resistant Candida albicans 901 assessed as reduction in fungal growth incubated for 24 hrs by serial dilution method
AID509401Drug level in 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected OF1 mouse brain at 50 mg/kg, po bid administered 1 day after infection measured on day 6 after 4 hrs of last treatment2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID1743169Antifungal activity against Trichophyton violaceum2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID532326Antifungal activity against Cryptococcus neoformans var. gattii by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID1204552Antifungal activity against Candida albicans Strain 22 by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID341573AUC (0 to 24 hrs) in children of >2-6 yrs age at risk for fungal infection assessed as hydroxyitraconazole level at 2.5 mg/kg, iv in 0.1 g/kg hydroxypropyl-beta-cyclodextrin administered as single dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-beta-cyclodextrin in infants, children, and adolescents.
AID1413339Antifungal activity against Aspergillus flavus2018MedChemComm, Jun-01, Volume: 9, Issue:6
Antifungal amphiphilic kanamycins: new life for an old drug.
AID729298Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL222013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
AID519056Antifungal activity against Candida albicans assessed as susceptible isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID524738Antimicrobial activity against Fusarium proliferatum after 48 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Species distribution and in vitro antifungal susceptibility patterns of 75 clinical isolates of Fusarium spp. from northern Italy.
AID532344Antifungal activity against Scedosporium apiospermum by EUCAST method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Activities of antifungal agents against yeasts and filamentous fungi: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID509387Antifungal activity against 1 x 10'6 CFU Fonsecaea monophora CBS 269.37 infected in po dosed OF1 mouse assessed as reduction in fungal load in spleen at 25 mg/kg, po bid administered 1 day after infection for 7 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
AID609318Half life in rat at 10 mg/kg, po administered as single dose2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.
AID549051Antifungal activity against Candida albicans CA135 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans.
AID1411886Antifungal activity against Candida tropicalis ATCC 13803 by M27-A3 guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID582798Antifungal activity against Candida albicans isolate 177 by broth dilution method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Identification and characterization of four azole-resistant erg3 mutants of Candida albicans.
AID424618Antimicrobial activity against azole-susceptible Candida albicans isolate CA5 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID518612Antimicrobial activity against itraconazole-susceptible Aspergillus fumigatus clinical isolate expressing cyp51A E130D mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID1155870Antifungal activity against Candida glabrata assessed as growth inhibition after 24 hrs by serial dilution method2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.
AID1128927Antifungal activity against Candida albicans assessed as total growth inhibition by micro-broth dilution method2014European journal of medicinal chemistry, Apr-09, Volume: 76Imidazolylchromanones containing non-benzylic oxime ethers: synthesis and molecular modeling study of new azole antifungals selective against Cryptococcus gattii.
AID405108Antimicrobial activity against Mucor circinelloides assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID322546Antifungal activity against Trichophyton violaceum after 7 days by broth microdilution test2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
AID405030Antifungal activity against Sporothrix schenckii P24223 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by modified NCCLS M38-A method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1689823Antifungal activity against Aspergillus fumigatus ASFU7 assessed as reduction in microbial growth after 48 hrs by resazurin staining based spectrofluorometric method2020European journal of medicinal chemistry, Mar-01, Volume: 189New azole antifungals with a fused triazinone scaffold.
AID405105Antimicrobial activity against Rhizopus microsporus var. rhizopodiformis assessed as percent of susceptible isolates after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
AID1204526Antifungal activity against Candida glabrata by broth microdilution method2015European journal of medicinal chemistry, Jun-05, Volume: 97A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity.
AID340961Antifungal activity against Candida albidus isolates from grapes by NCCLS M27-A2 method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
AID584412Antifungal activity against 2 days cultured Candida tropicalis isolated from neutropenic subject with AML or MDS pharynx receiving antifungal therapy for 45 days after 24 days of prophylaxis by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species.
AID50137Minimum inhibitory concentration of compound for antifungal activity against Candida kefyr2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization.
AID405034Antifungal activity against Sporothrix schenckii PSCC1 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods.
AID1411885Antifungal activity against Candida albicans ATCC 10231 by M27-A3 guideline based method2017MedChemComm, Dec-01, Volume: 8, Issue:12
Synthesis and antifungal activity of novel oxazolidin-2-one-linked 1,2,3-triazole derivatives.
AID753513Antidermatophytic activity against Microsporum gypseum NCPF 580 after 7 days by broth microdilution method2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Evaluation of bioactivities of chlorokojic acid derivatives against dermatophytes couplet with cytotoxicity.
AID442525Antifungal activity against Trichophyton mentagrophytes var. erinacei NCPF 375 after 7 days by microbroth dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID245421Minimum inhibitory concentration against Candida krusei 1766-1 evaluated by in vitro agar diffusion and micro-broth dilution assay 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
AID518403Antimicrobial activity against itraconazole-resistant Aspergillus fumigatus clinical isolate expressing cyp51A M220I mutant gene by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Azole resistance profile of amino acid changes in Aspergillus fumigatus CYP51A based on protein homology modeling.
AID563404Antifungal activity against Aspergillus tubingensis isolate CM-3810 obtained from respiratory tract infection of patient after 48 hrs by EUCAST broth dilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Species identification and antifungal susceptibility patterns of species belonging to Aspergillus section Nigri.
AID525139Antifungal activity against Fusarium moniliforme clade 1 by microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum.
AID519063Antifungal activity against Candida krusei assessed as resistant isolates after 48 hrs by broth microdilution2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
AID424623Antimicrobial activity against azole-resistant Candida albicans isolate CA10 after 48 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro interactions between tacrolimus and azoles against Candida albicans determined by different methods.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,069)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990150 (2.47)18.7374
1990's1328 (21.88)18.2507
2000's1907 (31.42)29.6817
2010's1973 (32.51)24.3611
2020's711 (11.72)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 110.55

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index110.55 (24.57)
Research Supply Index5.54 (2.92)
Research Growth Index5.87 (4.65)
Search Engine Demand Index204.45 (26.88)
Search Engine Supply Index2.05 (0.95)

This Compound (110.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials653 (10.14%)5.53%
Trials4 (1.61%)5.53%
Reviews748 (11.61%)6.00%
Reviews15 (6.02%)6.00%
Case Studies2,181 (33.87%)4.05%
Case Studies2 (0.80%)4.05%
Observational18 (0.28%)0.25%
Observational0 (0.00%)0.25%
Other2,840 (44.10%)84.16%
Other228 (91.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (352)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
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 31,381 participants (Actual)Interventional2006-07-31Completed
A First-in-Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single and Multiple Doses of BMS-986209 in Healthy Participants [NCT04154800]Phase 1114 participants (Actual)Interventional2019-12-06Completed
A RANDOMIZED CONTROLLED STUDY OF ITRACONAZOLE IN CHRONIC CAVITARY PULMONARY ASPERGILLOSIS [NCT01259336]Phase 431 participants (Actual)Interventional2010-07-31Completed
Prospective, Open-Label, Comparative, Multi-Center Study Of Voriconazole Compared To Itraconazole For The Primary Prophylaxis Of Invasive Fungal Infection (IFI) With Allogeneic Hematopoietic Stem Cell Transplants (HSCT) [NCT00289991]Phase 3489 participants (Actual)Interventional2006-03-31Completed
An Open-label, Single Group Study to Evaluate the Effect of Repeated Oral Administration of Itraconazole (ITZ) on the Single Oral Dose Pharmacokinetics of BAY1902607 in Healthy Male Participants [NCT03789890]Phase 114 participants (Actual)Interventional2019-01-08Completed
An Open-label Phase II (Proof of Concept (POC)) Trial of PKC412 Monotherapy in Participants With Acute Myeloid Leukemia (AML) and Participants With High Risk Myelodysplastic Syndrome (MDS) (CPKC412A2104 Core); An Open-label, Randomized Phase II POC Trial [NCT00045942]Phase 1/Phase 2144 participants (Actual)Interventional2002-01-30Completed
A Open-Label, Two-sequence Phase I Drug-drug Interaction Clinical Study to Investigate the Pharmacokinetics of ZSP1273 With Digoxin, Rosuvastatin,Itraconazole and Probenecid in Healthy Participants [NCT05954624]Phase 148 participants (Anticipated)Interventional2023-07-10Recruiting
A Phase II Trial to Evaluate the Effect of Itraconazole on Pathologic Complete Response Rates in Resectable Esophageal Cancer [NCT05563766]Phase 278 participants (Anticipated)Interventional2024-01-15Not yet recruiting
Therapeutic Efficacy Comparison of a Six-month Treatment by Itraconazole and Nebulised Ambisome® Versus Treatment by Itraconazole Alone in Non- or Mildly- Immunocompromised Patients With Chronic Pulmonary Aspergillosis: a Prospective, Randomized, Single B [NCT03656081]Phase 3224 participants (Anticipated)Interventional2018-12-19Recruiting
A Non-Randomized, Open Label, One Sequence, Two-Period Cross-Over Study to Investigate the Effect of CYP3A Inhibition on the Pharmacokinetics of RO7017773 in Healthy Participants [NCT03774576]Phase 114 participants (Actual)Interventional2018-12-17Completed
Itraconazole in the Management of Superficial Fungal Infections in India. A Pilot Study [NCT03923010]Phase 440 participants (Actual)Interventional2019-08-06Terminated(stopped due to Further recruitment not possible due to COVID 19 impact. Hence a decision to close study was taken by the sponsor in Aug 2020)
Relative Bioavailability of a Single Oral Dose of BI 730357 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, One-way Crossover Study) [NCT03782987]Phase 114 participants (Actual)Interventional2019-01-10Completed
Long-term Versus Short-term Sequential Therapy (Intravenous Itraconazole Followed by Oral Solution) of Itraconazole as Primary Prophylaxis in Patients Undergoing Allogeneic Stem Cell Transplantation [NCT01160952]Phase 2120 participants (Anticipated)Interventional2009-05-31Recruiting
Efficacy of Itraconazole as Secondary Prophylaxis in Patients Undergoing Allogeneic Stem Cell Transplantation or Chemotherapy With Prior Invasive Fungal Infection [NCT01198236]Phase 4150 participants (Actual)Interventional2008-07-31Completed
A Phase 1 Single Center Open-label, Non-randomized, Fixed Sequence Study in Healthy Volunteers to Assess the Pharmacokinetics (PK) of AZD9977 When Administered Alone and With Itraconazole [NCT03843060]Phase 114 participants (Actual)Interventional2019-02-22Completed
A Non-Randomized, Open-Label, Three-Part, Drug-Drug Interaction Study to Evaluate the Effects of Itraconazole, Rifampin, and Quinidine on the Pharmacokinetics and Safety of EDP-938 in Healthy Subjects [NCT03755778]Phase 172 participants (Actual)Interventional2018-11-29Completed
An Open-Label, Phase 1 Study in Healthy Volunteers to Evaluate the Drug-Drug Interaction Potential of CCX168 With Concomitant Medications [NCT06004947]Phase 132 participants (Actual)Interventional2016-01-14Completed
a Single-center, Open-label, Fixed Sequence Study in Healthy Chinese Subjects to Evaluate the Pharmacokinetic Effects of Itraconazole and Rifampicin on Oral Administration of a Single Dose of ABSK021 [NCT06089733]Phase 132 participants (Anticipated)Interventional2023-04-11Enrolling by invitation
A Randomized Phase II, Multi-center, Non-inferiority Clinical Trial for Efficacy and Safety of Micafungin Versus Intravenous Itraconazole as Empirical Antifungal Therapy for Febrile Neutropenic Patients With Hematological Diseases [NCT01344681]Phase 2153 participants (Actual)Interventional2011-06-30Completed
Effect of a Potent CYP3A and P-gp Inhibitor (Itraconazole) on Ipatasertib Pharmacokinetics in Healthy Subjects [NCT03222310]Phase 115 participants (Actual)Interventional2017-07-18Completed
A Phase 1 Combined Single and Multiple Ascending Oral Dose Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ASP6282 in Healthy Nonelderly and Elderly Male and Female Subjects, Including a Food Effect Cohort and Drug-drug [NCT02420782]Phase 1116 participants (Actual)Interventional2015-05-31Completed
A Single-Center, Non-Randomized, Open-Label, One-Sequence, Two-Period Within-Subject Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of Multiple Doses of Balovaptan in Healthy Volunteers [NCT03579719]Phase 115 participants (Actual)Interventional2018-07-10Completed
A Phase 1, 2-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effects of Itraconazole, Food, and pH, on the Single Dose Pharmacokinetics of BMS-986368 in Healthy Participants [NCT06170723]Phase 132 participants (Anticipated)Interventional2024-01-12Not yet recruiting
A Phase 1, Open-Label, Fixed-sequence, 5-part, Drug-drug Interaction Study of Tucatinib to Evaluate the Effects of CYP3A4 and CYP2C8 Inhibition and Induction on the Pharmacokinetics of Tucatinib and to Evaluate the Effects of Tucatinib on the Pharmacokine [NCT03723395]Phase 1116 participants (Actual)Interventional2018-09-17Completed
A PHASE 1 OPEN-LABEL, TWO-ARM,DRUG-DRUG INTERACTION STUDY TO EVALUATE THE EFFECT OF ITRACONAZOLE AND RIFAMPIN ON THE PHARMACOKINETICS OF TALAZOPARIB IN PATIENTS WITH ADVANCED SOLID TUMORS [NCT03077607]Phase 136 participants (Actual)Interventional2016-11-07Completed
A Single-Sequence, Open-Label, 2-Period, Crossover Trial to Evaluate the Effect of the Potent CYP3A4 Inhibitor Itraconazole on the Single-Dose Pharmacokinetics of Oral TAK-906 in Healthy Adult Subjects [NCT03161405]Phase 112 participants (Actual)Interventional2017-06-05Completed
A PHASE 1, OPEN-LABEL, FIXED SEQUENCE 2-PERIOD STUDY TO INVESTIGATE THE EFFECT OF MULTIPLE DOSES OF ITRACONAZOLE ON THE PHARMACOKINETICS OF A SINGLE DOSE OF PF-06651600 IN HEALTHY PARTICIPANTS [NCT03821493]Phase 112 participants (Actual)Interventional2019-02-21Completed
[NCT01321827]Phase 2/Phase 3100 participants (Actual)Interventional2011-04-30Completed
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 126 participants (Actual)Interventional2014-04-30Completed
Effect of Itraconazole on the Pharmacokinetics of a Single Oral Dose of BI 1584862 in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Design Study) [NCT06041438]Phase 114 participants (Actual)Interventional2023-09-29Completed
Study to Evaluate the Effect of Dose and Duration of Treatment of Itraconazole Administered as a Dry Powder for Inhalation (PUR1900) on Safety, Tolerability, and Potential Outcomes in Adult Patients With ABPA [NCT05667662]Phase 230 participants (Anticipated)Interventional2023-02-01Recruiting
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 112 participants (Actual)Interventional2014-05-31Completed
Open-Label, Single-Center, Single-arm, Fixed Sequence Study on the Effect of Itraconazole on the Pharmacokinetics of SHR1459 in Health Subjects [NCT04455100]Phase 120 participants (Actual)Interventional2020-07-17Completed
A Phase 1, Open-Label, 2-Period, Fixed Sequence Study to Estimate the Effect of Itraconazole on the Pharmacokinetics of PF-07817883 in Healthy Adults [NCT05822440]Phase 112 participants (Actual)Interventional2023-04-13Completed
A Phase 1, Fixed-Sequence, Two-Period, Open-Label Drug-Drug Interaction Study to Assess the Effect of an Inhibitor of Cytochrome P450 Isoenzyme 3A4 and Permeability Glycoprotein 1 on the Pharmacokinetics of TD-1211 [NCT01568411]Phase 120 participants (Actual)Interventional2012-04-30Completed
A Phase I, Open-label, Fixed Sequence, Two-period, Crossover, Drug-drug Interaction Study to Investigate the Interaction Potential of Itraconazole on the Pharmacokinetics of Ganaplacide and Lumefantrine Combination in Healthy Participants [NCT05084651]Phase 119 participants (Actual)Interventional2021-11-18Completed
An Adaptive, Part Open-label, Part Randomised Phase 1 Clinical Trial in Healthy Volunteers to Study Drug Interactions With RV521 Including Those Mediated by CYP3A4 and P-glycoprotein [NCT03782662]Phase 182 participants (Actual)Interventional2018-11-06Completed
An Open-label, Single-Sequence, 2-Treatment Period Study to Investigate the Effects of Cytochrome P450 3A4 Inhibition by Itraconazole on the Pharmacokinetics of BMS-986256 in Healthy Participants [NCT03950960]Phase 115 participants (Actual)Interventional2019-05-02Completed
A Phase 1, Open-label, Fixed-sequence Study To Estimate The Effects Of Multiple-dose Administration Of Itraconazole On The Steady-state Pharmacokinetics Of Pf-06649751 In Healthy Adult Subjects [NCT03121664]Phase 111 participants (Actual)Interventional2017-04-07Completed
A Phase 1, Single-Center, Open-Label, 2-Cohort, Fixed-Sequence, Drug-Drug Interaction Study to Assess the Pharmacokinetics of DC-806 When Orally Administered Alone, When Coadministered With Itraconazole, and When Coadministered With Carbamazepine in Healt [NCT05994807]Phase 133 participants (Actual)Interventional2023-08-08Completed
A Non-randomized, Open-label, Fixed-sequence Phase I Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of AZD5305 in Patients With Advanced Solid Malignancies [NCT05573724]Phase 116 participants (Actual)Interventional2022-11-07Active, not recruiting
A Phase 1, Open-Label, Fixed Sequence Study to Investigate the Effect of Coadministration of Itraconazole on the Pharmacokinetics of CRD-740 in Healthy Adult Subjects [NCT05437094]Phase 120 participants (Actual)Interventional2022-06-27Completed
A Phase 1, Open-label, Two-period, Fixed-sequence Study To Estimate The Effects Of Multiple-dose Administration Of Itraconazole On The Single-dose Pharmacokinetics Of Pf-06372865 In Healthy Adult Subjects [NCT02475746]Phase 10 participants (Actual)Interventional2015-07-31Withdrawn
A Phase I/II Study of Hydroxychloroquine and Itraconazole as Therapy for Men With Androgen Normalised Prostate Cancer [NCT03513211]Phase 1/Phase 212 participants (Actual)Interventional2018-08-23Completed
[NCT02470832]Phase 112 participants (Actual)Interventional2015-05-31Completed
A Study to Investigate the Potential Effects of Repeated Administration of Itraconazole on the Pharmacokinetics of JNJ-42847922 in Healthy Male Subjects [NCT02455856]Phase 116 participants (Actual)Interventional2015-05-18Completed
A Phase 1, Open-Label, Fixed Sequence Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of Debio 1450 in Healthy Subjects [NCT03209648]Phase 120 participants (Actual)Interventional2017-06-14Completed
Comparative Study of Systemic Antifungal Drugs Used in Treatment of Onychomycosis [NCT03171584]Phase 360 participants (Anticipated)Interventional2017-07-01Not yet recruiting
A Phase 1, Randomized, Parallel-Group, Open-Label Study to Evaluate the Effect of the Modulators of the Cytochrome P450 (CYP) 2C8 and/or 3A on the Single-Dose Pharmacokinetics of Ozanimod and CC112273 in Healthy Adult Subjects [NCT03624959]Phase 1100 participants (Actual)Interventional2018-06-20Completed
Phase I, Open-label, Single-sequence, Cross-over Study of the Effect of Multiple Doses of Itraconazole on Single-dose Tepotinib Pharmacokinetics in Healthy Participants [NCT05203822]Phase 118 participants (Actual)Interventional2022-01-21Completed
A Phase 1, Single-center, Open-label, 2-part, 2-treatment Period, 1-sequence, Cross-over, Drug-drug Interaction Study to Investigate the Effect of Erythromycin on SAR443820 (Part A) and the Effect of Itraconazole on SAR443820 (Part B) in Healthy Adult Par [NCT05797753]Phase 116 participants (Actual)Interventional2022-02-18Completed
The Effect of Itraconazole on the Clinical Outcomes of Patients With Advanced Non Small Cell Lung Cancer Receiving Platinum Based Chemotherapy [NCT03664115]Phase 260 participants (Anticipated)Interventional2018-07-02Recruiting
An Open-label, Fixed-sequence, Drug-drug Interaction Study in Healthy Subjects to Evaluate the Effect of Itraconazole, a Strong CYP3A4 Inhibitor and Potent P-gp Inhibitor on the Pharmacokinetics of GLPG3667 [NCT05272683]Phase 114 participants (Actual)Interventional2022-02-28Completed
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 136 participants (Actual)Interventional2022-12-29Completed
An Open-label, Randomized, 2-period, 2-sequence Study to Evaluate the Single-dose Pharmacokinetics of Milademetan When Administered Alone or Concomitantly With Itraconazole or Posaconazole in Healthy Subjects [NCT03614455]Early Phase 136 participants (Actual)Interventional2018-07-13Completed
Risk of QT-prolongation and Torsade de Pointes in Patients Treated With Acute Medication in a University Hospital [NCT02068170]178 participants (Actual)Observational2014-02-28Completed
Comparison of Efficacy of Double Dose Oral Terbinafine Versus Itraconazole in Treatment of Dermatophyte Infections of Skin - A Prospective, Randomized Controlled Trial [NCT04880980]Phase 3120 participants (Actual)Interventional2021-03-15Completed
A Phase 1,Parallel Assignment,Fixed-Sequence Study to Assess the Effect of Itraconazole, Rifampicin on the Pharmacokinetics of TPN171H in Healthy Subjects [NCT06090123]Phase 124 participants (Actual)Interventional2020-01-01Completed
A Phase 1/2a, Multicenter, Open-Label, First in Human Study to Assess the Safety, Tolerability, Pharmacokinetics, and Preliminary Antitumor Activity of DB-1303 in Patients With Advanced/Metastatic Solid Tumors [NCT05150691]Phase 1/Phase 2631 participants (Anticipated)Interventional2022-01-31Recruiting
Single-Ascending Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of LY3323795 in Healthy Subjects [NCT02989389]Phase 142 participants (Actual)Interventional2016-12-12Completed
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 120 participants (Actual)Interventional2014-03-31Completed
An Open-label Non-randomized, Phase 1 Study to Evaluate the Effect of (a) Itraconazole or Rifampin on the Pharmacokinetics of a Single Intravenous Dose of Copanlisib and (b) Copanlisib on Cardiovascular Safety in Subjects With Advanced Solid Tumors and No [NCT02253420]Phase 151 participants (Actual)Interventional2014-10-08Completed
An Open-label, 2-period, Single-sequence, Crossover Study to Evaluate the Effect of Multiple Oral Dosing of Itraconazole on BCT197 Systemic Exposure in Healthy Male Participants [NCT03498170]Phase 116 participants (Actual)Interventional2018-03-19Completed
An Open-label, 2-Period, Fixed-sequence, Phase 1 Study in Healthy Volunteers to Evaluate the Effect of Itraconazole, a Potent CYP3A Inhibitor, on the Pharmacokinetics of IW-1973 [NCT03499106]Phase 124 participants (Actual)Interventional2018-04-12Completed
A Study to Evaluate the Relative Bioavailability of Different Strengths of STI-1558 Capsules and the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and Inducer (Rifampin) on the Pharmacokinetics of STI-1558 in Healthy Volunteers [NCT05685719]Phase 137 participants (Actual)Interventional2023-01-04Completed
A Two Cohort, Open-Label, Fixed Sequence Study to Investigate the Effect of CYP3A4 Inhibition on the Single Dose Pharmacokinetics of ASTX660 and the Effect of a Single Dose of ASTX660 on the Pharmacokinetics of the CYP3A4 Substrate Midazolam [NCT04411030]Phase 136 participants (Actual)Interventional2020-05-20Completed
A Phase 1, Open-Label, Single-Sequence Crossover Study in Healthy Male Participants to Determine the Effect of an Inhibitor of Cytochrome P450 3A and P Glycoprotein on Exposure to Orvepitant [NCT03535662]Phase 116 participants (Actual)Interventional2018-06-08Completed
An Open-Label, Fixed-Sequence Study to Assess Effects of Clarithromycin on the Single-Dose Pharmacokinetics of JNJ-54861911 in Healthy Male Subjects [NCT02197884]Phase 113 participants (Actual)Interventional2014-07-31Completed
Phase Ib/II Study Evaluating Orteronel (Without Prednisone) Combined With Itraconazole In Men With Castration-Resistant Prostate Cancer (CRPC) [NCT02054793]Phase 1/Phase 20 participants (Actual)Interventional2014-06-30Withdrawn(stopped due to This study was never able to open due to lack of funding from the pharmaceutical company.)
Phase I Open Label, Drug-Drug Interaction, Study to Evaluate the Effect of Itraconazole and Phenytoin on the Pharmacokinetics of ASC41 in Healthy Volunteers and A Study to Evaluate the PK, Safety and Tolerability in Subjects With Non-alcoholic Fatty Liver [NCT04845646]Phase 124 participants (Actual)Interventional2021-03-16Completed
A Phase 1, Single-Center, Nonrandomized, Open-Label, 2-Part, Fixed-Sequence, Drug-Drug Interaction Study to Assess the Pharmacokinetics and Safety of AZD4205 When Orally Administered Alone, When Coadministered With Itraconazole, and When Coadministered Wi [NCT05486949]Phase 132 participants (Actual)Interventional2022-07-27Completed
An Open-Label, Pharmacokinetic Study to Evaluate the Pharmacokinetics and Relative Bioavailability of BIIB091 Formulations and to Assess the Impact of Food, a Proton Pump Inhibitor and CYP3A4 Inhibitor on BIIB091 Exposure Using the Selected Formulation in [NCT04564612]Phase 159 participants (Actual)Interventional2020-09-28Completed
A Two-Part Study to Evaluate the Effect of CYP3A4 Inhibition (Itraconazole-Part 1) and CYP1A2 Inhibition (Ciprofloxacin - Part 2) on the Single-Dose Pharmacokinetics of Pracinostat in Healthy Nonsmoking Subjects [NCT02118909]Phase 132 participants (Actual)Interventional2014-05-31Completed
The Possible Effect of Itraconazole as add-on Therapy to Paclitaxel and Carboplatin on the Treatment Outcome in Patients With Advanced Ovarian Cancer [NCT05591560]66 participants (Anticipated)Interventional2022-10-31Not yet recruiting
A Phase I, Open-Label, Randomized, Drug-Drug Interaction Study to Evaluate the Effect of Itraconazole and Voriconazole on the Single-Dose Pharmacokinetics of GLPG1690 in Healthy Male Subjects [NCT03515382]Phase 118 participants (Actual)Interventional2018-03-16Completed
A Randomized, Open-Label, Parallel Group, Drug-drug Interaction Study to Evaluate the Effect of Fluconazole and Itraconazole on the Pharmacokinetics of Erdafitinib in Healthy Adult Subjects [NCT03135106]Phase 154 participants (Actual)Interventional2017-04-14Completed
An Open-label, 2-cycle Clinical Study to Evaluate the Drug Interaction Between Itraconazole or Dextromethorphan and IBI351 in Healthy Subjects [NCT05699993]Phase 124 participants (Actual)Interventional2023-03-10Completed
[NCT01214941]Phase 412 participants (Actual)Interventional2010-09-30Completed
A Phase 1 Single Center Open-label, Non-randomized, Fixed Sequence Study in Healthy Volunteers to Assess the Pharmacokinetics (PK) of BV100 When Administered Alone and With Itraconazole [NCT05684718]Phase 116 participants (Actual)Interventional2023-02-01Completed
A Phase 1, Open-Label, Single-Sequence Crossover Study in Healthy Subjects to Determine the Effect of an Inhibitor of Cytochrome P450 3A on Exposure to Relacorilant and Its Main Metabolites [NCT03512548]Phase 152 participants (Actual)Interventional2018-04-10Completed
Evaluation of Antifungal Prophylaxis Against Invasive Fungal Infections During Corticosteroid Containing Therapy for Graft-versus-host Disease Following Allogeneic Hematopoietic Stem Cell Transplantation [NCT01282879]Phase 436 participants (Actual)Interventional2009-12-31Terminated(stopped due to In interim analysis, this study met the primary hypothesis.)
An Open-label, Fixed-sequence, Drug-drug Interaction Study to Evaluate the Effect of Itraconazole on the Pharmacokinetics of JNJ-56136379 in Healthy Adult Participants [NCT03945539]Phase 116 participants (Actual)Interventional2019-05-15Completed
A Phase 1, 3-arm, Open-label, Sequential Design Study to Investigate the Effect of Multiple Doses of Itraconazole, Gemfibrozil, or Carbamazepine on Single-dose Pharmacokinetics of BMS-986278 in Healthy Participants [NCT05932303]Phase 147 participants (Actual)Interventional2023-07-12Completed
A Phase 1 First in Human, Single and Multiple Ascending Dose and Food Effect and Drug-Drug Interaction in Healthy Subjects to Evaluate the Safety, Tolerability and Assessment of Pharmacokinetics of ABBV-903 [NCT05691699]Phase 1104 participants (Actual)Interventional2023-01-03Completed
Effects of CYP3A4 Inhibition by Itraconazole on the Pharmacokinetics of LY3200882 in Healthy Subjects [NCT03792139]Phase 123 participants (Actual)Interventional2019-01-08Completed
A Phase 1, Two-part, Open-label, Fixed-sequence Study to Evaluate the Effects of Multiple Doses of Itraconazole and Carbamazepine on the Single-dose Pharmacokinetics of LY3410738 in Healthy Adult Subjects [NCT05205447]Phase 127 participants (Actual)Interventional2022-01-05Terminated(stopped due to Data from part 2 no longer deemed necessary for this program.)
A Single-center, Open-label, Fixed-sequence Study to Investigate the Effect of Multiple-dose Itraconazole on the Pharmacokinetics of a Single Dose of 10 mg ACT-1004-1239 in Healthy Male Subjects [NCT05549531]Phase 116 participants (Actual)Interventional2022-10-01Completed
An Open-label, 2-Period, Fixed-sequence, Phase 1 Study in Healthy Volunteers to Evaluate the Effect of Itraconazole, a Potent CYP3A Inhibitor, on the Pharmacokinetics of Olinciguat (IW-1701) [NCT03892499]Phase 124 participants (Actual)Interventional2019-05-03Completed
A Phase 1, Open-Label Study to Evaluate the Effect of Itraconazole and Mefenamic Acid on the Single-Dose Pharmacokinetic Profile of Soticlestat in Healthy Participants [NCT05064449]Phase 128 participants (Actual)Interventional2021-10-14Completed
A Phase 1, Open-label, Fixed-sequence, 2-Panel Study to Assess the Effects of Itraconazole and Etravirine on the Single-dose Pharmacokinetics of JNJ-64417184 in Healthy Adult Subjects [NCT04208373]Phase 132 participants (Actual)Interventional2019-12-20Completed
An Open-Label, Fixed Sequence Study in Healthy Post Menopausal Female Subjects to Assess the Pharmacokinetics of Camizestrant (AZD9833) When Administered Alone and in Combination With Itraconazole [NCT05551897]Phase 114 participants (Actual)Interventional2022-10-04Completed
A Randomized Double-blind (Sponsor Unblind) Placebo Controlled Study in Healthy Subjects to Evaluate: Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Repeat Doses of GSK2881078, the Selective Androgen Receptor Modulator With an Open La [NCT02567773]Phase 1108 participants (Actual)Interventional2015-09-30Completed
A Single-Center, Randomized, Investigator/Subject-Blind, Adaptive Single-Ascending-Dose(SAD), Placebo-Controlled, Parallel Study to Investigate the Safety, Tolerability, Pharmacokinetics (Including the Effect of Food and the Effect of Itraconazole on the [NCT02633709]Phase 133 participants (Actual)Interventional2016-01-07Completed
A NON-RANDOMIZED, OPEN-LABEL, THREE-PART, DRUG-DRUG INTERACTION STUDY TO EVALUATE THE EFFECTS OF ITRACONAZOLE, CARBAMAZEPINE, AND QUINIDINE ON THE PHARMACOKINETICS AND SAFETY OF EDP-235 IN HEALTHY PARTICIPANTS [NCT05594602]Phase 136 participants (Actual)Interventional2022-10-06Completed
A Phase I Study to Assess the Effect of Itraconazole and Rifampicin on Pharmacokinetics Profile of BPI-7711 in Chinese Healthy Volunteers [NCT04135833]Phase 131 participants (Actual)Interventional2019-12-12Completed
A First-in-Human, Phase I, Double-blind, Placebo-controlled, Single and Multiple Ascending Oral Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of KRP-A218 in Healthy Subjects, Including Food-Effect and Drug-drug Interaction With Itr [NCT04908800]Phase 199 participants (Actual)Interventional2021-05-27Completed
A Phase I, Open-label Multi-dose Two-part Study to Characterize the Effects of a Strong CYP3A4 Inhibitor and a Strong CYP3A4 Inducer on the Steady-State Pharmacokinetics of Tazemetostat (EPZ-6438) in Subjects With Advanced Malignancies [NCT04537715]Phase 142 participants (Actual)Interventional2020-04-23Completed
Phase 1, Open-label, Fixed Sequence, 2-period Study To Investigate The Effect Of Multiple Doses Of Itraconazole On The Pharmacokinetics Of Single Dose Pf-06463922 In Healthy Volunteers In The Fasted Condition [NCT02838264]Phase 116 participants (Actual)Interventional2016-08-16Completed
A Phase I Study to Evaluate Drug-Drug Interaction of TQB3909 Tablets [NCT06165822]Phase 140 participants (Anticipated)Interventional2023-12-31Not yet recruiting
An Open-Label, Randomized, Parallel-Group Drug-Drug Interaction Study to Assess the Effect of Multiple Doses of Itraconazole or Gemfibrozil on the Pharmacokinetics of a Single Dose of JNJ-56021927 in Healthy Male Subjects [NCT02230033]Phase 145 participants (Actual)Interventional2014-09-30Completed
The Effect of Cytochrome P 450 3A4 Inhibition by Itraconazole on the Single Oral Dose Pharmacokinetics of Cilobradine (an Open-label, Randomised, Single-dose, Two-way Crossover Study) [NCT02264041]Phase 125 participants (Actual)Interventional2004-01-31Completed
A Phase I/II Trial Investigating the Tolerability, Toxicity and Efficacy of Tamoxifen and SUBA-Itraconazole in Patients With Platinum Resistant Recurrent Epithelial Ovarian Cancer [NCT05156892]Phase 144 participants (Anticipated)Interventional2022-09-04Recruiting
A Single-centre, Open, Single-dose, Self-control Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of Pyrotinib in Healthy Subjects [NCT04479891]Phase 118 participants (Actual)Interventional2019-09-18Completed
A Phase 1, One Sequence, Cross-over Pharmacokinetic Study to Assess the Interaction Between ASP1707 and Itraconazole, a CYP3A and P-gp Inhibitor in Healthy Female Subjects [NCT02175407]Phase 114 participants (Actual)Interventional2014-04-30Completed
A Phase 1, Single-center, Randomized, Double-blind, Double-dummy, Drug Interaction Study Between AVP-923 and Itraconazole, and Between AVP-786 and Itraconazole in Healthy Adult Subjects [NCT02402595]Phase 124 participants (Actual)Interventional2015-03-31Completed
A Randomized, Placebo Controlled, Double Blind, Single and Repeat Dose Escalation Phase 1 Study to Evaluate Safety, Tolerability, and Pharmacokinetics of GSK3915393 in Healthy Participants and Open Label Assessment of Coadministration of GSK3915393 With G [NCT04604795]Phase 165 participants (Actual)Interventional2020-11-04Completed
A Phase 1, Open-label, Parallel-group, Fixed-sequence Study to Investigate the Effect of the CYP3A Inducer Rifampin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of Pamiparib (BGB-290) in Cancer Patients [NCT03994211]Phase 125 participants (Actual)Interventional2019-05-29Completed
[NCT02055703]Phase 1195 participants (Actual)Interventional2014-01-31Completed
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 122 participants (Actual)Interventional2017-03-28Completed
A Three-part, Single-center, Open-label, Phase I Drug-drug Interaction Clinical Study to Investigate the Effect of Itraconazole, Gemfibrozil or Rifampicin on Pharmacokinetics of SKLB1028 in Healthy Subjects [NCT05069870]Phase 142 participants (Actual)Interventional2021-06-07Active, not recruiting
A Four-part, Single-center, Open-label, Phase I Clinical Study to Evaluate the Drug-drug Interactions (DDIs) Between GP681 and Rosuvastatin/Digoxin/Itraconazole/Oseltamivir in Chinese Healthy Volunteers [NCT05789342]Phase 154 participants (Actual)Interventional2023-02-15Completed
[NCT02085967]Phase 1106 participants (Actual)Interventional2014-02-28Completed
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 124 participants (Actual)Interventional2014-04-30Completed
An Open-Label, Multicenter Study to Assess the Potential Effects of Itraconazole (a Strong CYP3A4 Inhibitor) on the Pharmacokinetics of Lurbinectedin (PM01183) in Patients With Advanced Solid Tumors [NCT05063318]Phase 111 participants (Anticipated)Interventional2020-10-07Recruiting
A Pilot Study Investigating Antitumorigenic Potential of Topical Itraconazole in the Treatment of Basal Cell Carcinoma [NCT02120677]Early Phase 15 participants (Actual)Interventional2014-05-31Completed
An Open-label, Non-randomized, Phase I Study to Evaluate the Effect of Itraconazole on the Pharmacokinetics of a Single Oral Dose of Roniciclib in Patients With Advanced Solid Tumors [NCT02457351]Phase 114 participants (Actual)Interventional2015-07-31Completed
A Phase I, Two-part, Open-label Study to Evaluate the Pharmacokinetics of Rilapladib (SB-659032) and Its Metabolites, and to Determine the Effect of Repeat Dose Itraconazole on the Pharmacokinetics of Rilapladib in Healthy Volunteers [NCT02130661]Phase 10 participants (Actual)Interventional2017-10-31Withdrawn
SUBA-itraconazole Versus Conventional Itraconazole in the Treatment of Endemic Mycoses: a Multi-center, Open-label Comparative Trial [NCT03572049]Phase 2/Phase 388 participants (Actual)Interventional2018-09-17Completed
A Study to Investigate the Potential Effects of Repeated Administration of Itraconazole on the Pharmacokinetics of JNJ-42165279 in Healthy Male Subjects [NCT02065739]Phase 116 participants (Actual)Interventional2014-01-31Completed
An Open-label, Three-period, One-sequence Crossover Clinical Trial to Evaluate the Effects of Food or Proton Pump Inhibitor on the Pharmacokinetics of Itraconazole in Healthy Volunteers [NCT04942652]Phase 113 participants (Actual)Interventional2021-07-13Completed
A Phase I, Non-randomized, Open-label, Fixed-sequence Study to Investigate the Effect of a Probe CYP3A4 Inhibitor and Inducer on the Pharmacokinetics of BAY1841788 (ODM 201) in Healthy Male Volunteers [NCT03048110]Phase 115 participants (Actual)Interventional2017-02-15Completed
A Phase 1, Open-Label, 2-Cohort Study to Assess the Single Dose Pharmacokinetics of Two Formulations of TD-1473 and to Assess the Effect of a High-Fat Meal and Itraconazole on the Pharmacokinetics of TD-1473 in Healthy Subjects [NCT03555617]Phase 136 participants (Actual)Interventional2018-06-13Completed
A Phase 1 Study to Evaluate the Potential Drug Interactions Between ALXN2080 and Itraconazole, Fluconazole, and Carbamazepine in Healthy Adult Participants [NCT06173596]Phase 160 participants (Anticipated)Interventional2023-12-21Not yet recruiting
A Phase 1 First in Human Study Evaluating the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AMG 176 in Subjects With Relapsed or Refractory Multiple Myeloma and Subjects With Relapsed or Refractory Acute Myeloid Leukemia [NCT02675452]Phase 1142 participants (Actual)Interventional2016-06-13Active, not recruiting
A Single-center, Open-label, Drug-drug Interaction Study of SH-1028 Tablets in Healthy Subjects [NCT04808648]Phase 140 participants (Anticipated)Interventional2021-04-06Not yet recruiting
Safety, Tolerability and Pharmacokinetics of Single Rising Oral Doses and Multiple Oral Doses of BI 1323495 Versus Placebo in Healthy Male Japanese Subjects Genotyped as Poor and Extensive Metabolizers of UGT2B17 (Single-blind, Randomised, Placebo-control [NCT04619251]Phase 174 participants (Actual)Interventional2020-11-13Completed
A Phase 1 Study of the Effects of Itraconazole on the Pharmacokinetics of ALKS 5461 in Healthy Volunteers [NCT02272764]Phase 124 participants (Actual)Interventional2014-10-31Completed
A Phase I, Single-center, Open-label, Fixed-sequence Study of AB-106 in Chinese Healthy Adult Men Evaluated the Effects of Itraconazole and Rifampicin on AB-106 Pharmacokinetics [NCT05357820]Phase 156 participants (Actual)Interventional2021-07-19Completed
A Phase 1, Randomized, Double-blind, Placebo-controlled, Multiple-dose Escalation Study Evaluating the Safety, Pharmacokinetics, and Pharmacodynamics of VX-708 in Healthy Subjects [NCT05518734]Phase 164 participants (Actual)Interventional2022-09-17Completed
Interventional, Open-label, Interaction Study Investigating the Effects of Itraconazole (Inhibitor of CYP3A4/5) on the Pharmacokinetics and Safety and Tolerability of Lu AF11167 in Healthy Young Subjects [NCT02199431]Phase 120 participants (Actual)Interventional2014-07-31Completed
An Open-Label, 2-Period, Fixed Sequence Study to Determine the Effect of Multiple Oral Doses of Itraconazole on the Single Dose Pharmacokinetics of AG 120 in Healthy Adult Subjects [NCT02831972]Phase 122 participants (Actual)Interventional2016-06-30Completed
A Phase 1, First-in-human Study of Safety, Tolerability, and Pharmacokinetics of VX-828 [NCT06154447]Phase 1157 participants (Anticipated)Interventional2023-12-12Recruiting
Single- and Multiple-Ascending Dose, Safety, Tolerability, and Pharmacokinetic Study With LY3154885 in Healthy Subjects [NCT04014361]Phase 136 participants (Actual)Interventional2019-08-09Terminated(stopped due to HUAA study is terminated early due to a business decision.)
A PHASE 1, OPEN-LABEL, FIXED SEQUENCE 2-PERIOD STUDY TO INVESTIGATE THE EFFECT OF MULTIPLE DOSES OF ITRACONAZOLE ON THE PHARMACOKINETICS OF A SINGLE DOSE OF PF-06700841 IN HEALTHY PARTICIPANTS [NCT04090047]Phase 112 participants (Actual)Interventional2019-09-24Completed
A Phase 1, Open-Label, 4-Part, Drug-Drug Interaction Study With Omaveloxolone in Healthy Subjects [NCT04008186]Phase 161 participants (Actual)Interventional2019-06-14Completed
A Phase I Study to Evaluate Drug-Drug Interaction of TQ05105 Tablets [NCT06024915]Phase 140 participants (Anticipated)Interventional2023-09-30Not yet recruiting
A Phase 1, Open-label, Single-center Study to Evaluate the Effect of Cytochrome P450 (CYP) 3A Inhibition and Induction on the Pharmacokinetics of CC-220 in Healthy Subjects [NCT02820935]Phase 136 participants (Actual)Interventional2016-07-31Completed
An Open-Label Single-Sequence Study to Evaluate the Effect of Co-administration of Itraconazole or Diltiazem on the Single-Dose Pharmacokinetics of BMS-986177 in Healthy Subjects [NCT02807909]Phase 128 participants (Actual)Interventional2016-07-31Completed
Relative Bioavailability of a Single Oral Dose of BI 1323495 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, One-way Crossover Study) [NCT04011241]Phase 114 participants (Actual)Interventional2019-07-24Completed
Efficacy and Safety of Drug Combination Therapy of Isotretinoin and Some Antifungal Drugs as A Potential Aerosol Therapy for COVID-19 : An Innovative Therapeutic Approach [NCT04577378]Phase 245 participants (Anticipated)Interventional2020-10-20Not yet recruiting
An Open-Label, One-Sequence, Two-Period Study to Evaluate the Effects of Itraconazole on the Pharmacokinetics of DS-8500a in Healthy Subjects [NCT02790671]Phase 126 participants (Actual)Interventional2016-05-31Completed
A 3-Part, Phase 1 Study to Assess the Drug Interactions of BBT-877 and Midazolam, Itraconazole, and Esomeprazole in Healthy Adult Subjects [NCT04138836]Phase 148 participants (Actual)Interventional2019-09-17Completed
Efficacy and Safety of Terbinafine and Itraconazole Monotherapy in Conventional and Increased Doses and in Combination in Dermatophytosis [NCT05881980]Phase 2/Phase 3150 participants (Anticipated)Interventional2023-05-31Not yet recruiting
A Two-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effect of Multiple Doses of Itraconazole and Rifampin on the Single-Dose Pharmacokinetics of Mitapivat Sulfate (AG-348) in Healthy Adult Subjects [NCT03991312]Phase 128 participants (Actual)Interventional2019-06-20Completed
A Phase 1, Single Ascending Oral Dose Study to Assess the Safety, Tolerability and Pharmacokinetics of ASP3700 in Healthy Male Subjects, Including a Drug-drug Interaction Part With Itraconazole [NCT02155504]Phase 144 participants (Actual)Interventional2014-05-31Completed
A Randomized Controlled Trial to Compare Oral Itraconazole and Standard Care Versus Standard Care Alone in Patients With Non-cystic Fibrosis Related Bronchiectasis With Chronic Aspergillus Infection in Reducing Bronchiectasis Exacerbations [NCT06160713]Phase 380 participants (Anticipated)Interventional2023-12-01Recruiting
A Phase I, Open Label Study in Healthy Subjects to Evaluate the Effect of Itraconazole and Rifampicin Upon the Pharmacokinetics of a Single Oral Dose of Olorofim. [NCT04171739]Phase 124 participants (Actual)Interventional2019-11-18Completed
A Two-part, Phase I, Open-label, Multicenter, Two-period, One-sequence Study to Investigate the Effect of Itraconazole and Rifampin on the PK of Vemurafenib at Steady State [NCT02608034]Phase 132 participants (Anticipated)Interventional2016-05-26Completed
Comparison of Efficacy of Single Oral Dose Fluconazole and Itraconazole in Patients With Pityriasis Versicolor [NCT05862714]Phase 1164 participants (Actual)Interventional2022-03-01Completed
An Exploratory, Randomized, Double-blind, Placebo Controlled Study to Assess the Efficacy of Multiple Doses of Omalizumab in Cystic Fibrosis Complicated by Allergic Bronchopulmonary Aspergillosis (ABPA) [NCT00787917]Phase 414 participants (Actual)Interventional2008-11-30Terminated
An Open-Label, Single-Dose Study to Evaluate the Safety and Pharmacokinetics of DIC075V in Subjects With Mild or Moderate Chronic Renal Insufficiency and in Subjects With Mild Chronic Hepatic Impairment Compared to Healthy Adult Volunteers and a Randomize [NCT00805090]Phase 137 participants (Actual)Interventional2008-12-31Completed
Clinical Evaluation of a Formulated Nanoemulsion for Topical Application [NCT04110834]Phase 230 participants (Actual)Interventional2018-02-15Completed
Clinical Study to Evaluate the Efficacy of Prophylactic Itraconazole in High-Dose Chemotherapy and Autologous Hematopoietic Stem Cell Transplantation for Pediatric Solid Tumors [NCT00336531]Phase 4100 participants (Anticipated)Interventional2006-04-30Completed
A Phase 1, Open-label, Two-period, Fixed-sequence Study To Estimate The Effects Of Multiple-dose Administration Of Itraconazole On The Single-dose Pharmacokinetics Of Pf-06648671 In Healthy Adults [NCT02883114]Phase 112 participants (Actual)Interventional2016-09-30Completed
A Multi-center, Randomized, Open Label, Parallel Study to Evaluate and Compare the Efficacy and Safety of Mycamine® vs Itraconazole Oral Solution for Prophylaxis of Fungal Infections in Patients Undergoing a Hematopoietic Stem Cell Transplant [NCT00794703]Phase 3288 participants (Actual)Interventional2008-11-30Completed
A Randomized Controlled Trial to Compare the Clinical Outcomes With Six Months of Therapy With Oral Itraconazole Versus Oral Voriconazole for Management of Treatment naïve Subjects With Chronic Pulmonary Aspergillosis [NCT04824417]Phase 3100 participants (Anticipated)Interventional2021-03-01Recruiting
Evaluation of the Response of Itraconazole and Terbinafine Therapy in Subjects With Crohn's Disease Not Responding Adequately to Current Therapy [NCT05049525]Phase 268 participants (Anticipated)Interventional2022-02-22Recruiting
Study on the Pharmacokinetic Effects of Single-centered, Open, Single-arm, Fixed-sequence Itraconazole on SHR0302 Tablets in Healthy Subjects [NCT05404724]Phase 114 participants (Actual)Interventional2022-06-25Completed
An Open Label, Phase I Study to Assess the Effect of Itraconazole (CYP3A4 and P-gp Inhibitor) on the Pharmacokinetics of Anetumab Ravtansine and to Assess the ECG Effects, Safety and Immunogenicity of Anetumab Ravtansine Given as a Single Agent and Togeth [NCT02824042]Phase 163 participants (Actual)Interventional2016-09-07Completed
Randomized, Placebo-controlled, Double-blind, Parallel Group Study to Investigate the Safety, Tolerability and Pharmacokinetics of Increasing Single Oral Doses (10 - 1500 mg, Tablets) of BAY1817080 Including the Effect of Food and Itraconazole on the Rela [NCT02817100]Phase 188 participants (Actual)Interventional2016-07-22Completed
A 3-Part, Open-Label Study to Assess Pharmacokinetic Drug-Drug Interaction Between Avatrombopag When Co-Administered With Fluconazole (Moderate Inhibitor of CYP2C9 and CYP3A), Itraconazole (Strong CYP3A Inhibitor), or Rifampin (Strong CYP3A and Moderate C [NCT02809768]Phase 148 participants (Actual)Interventional2016-04-30Completed
A Case Study of the Effects of Topical Itraconazole on Pharmacodynamic Modulation of Hedgehog Target Gene Expression in Basal Cell Carcinomas in Patients [NCT02735356]Early Phase 19 participants (Actual)Interventional2016-05-05Completed
An Open-Label Study of the Effect of a Strong CYP3A4 Inhibitor (Itraconazole) on the Pharmacokinetics of Bardoxolone Methyl in Healthy Volunteers [NCT03264079]Phase 116 participants (Actual)Interventional2017-10-16Completed
Pharmacokinetics of Itraconazole in Pediatric Cancer Patients [NCT01409018]Phase 16 participants (Actual)Interventional2009-06-30Completed
Pilot Biomarker Trial to Evaluate the Efficacy of Itraconazole in Patients With Basal Cell Carcinomas [NCT01108094]Phase 229 participants (Actual)Interventional2010-04-30Completed
A Phase 1, Open-label Study in Healthy Adult Subjects to Evaluate Effects of Cytochrome P450 Inhibition and Induction on the Pharmacokinetics of CC-99677 and the Effects of CC-99677 on the Pharmacokinetics of Digoxin, Metformin, Methotrexate, Midazolam, R [NCT04268394]Phase 148 participants (Actual)Interventional2020-03-13Completed
A Single-arm, Multiple-Dose, Steady-State, Bioavailability Study With Twice Daily Dosing of Lozanoc™ (65 mg Itraconazole Capsules, Mayne) Taken Regardless of Food [NCT02755857]Phase 220 participants (Actual)Interventional2016-07-31Completed
A Pilot Trial of Itraconazole Pharmacokinetics in Patients With Metastatic Breast Cancer [NCT00798135]13 participants (Actual)Interventional2008-11-30Completed
A Phase 1 Open-label, Two-cohort, One-sequence Crossover Study to Investigator the Effect of P-glycoprotien Inhibitor (Itraconazole) and Inducer (Rifampin) on the Pharmacokinetics, Safety, and Tolerability of Sitravatinib in Health Subjects [NCT05255276]Phase 136 participants (Actual)Interventional2022-01-29Completed
Evaluation of the Effect of Food, Omeprazole, Itraconazole, and Carbamazepine on the Pharmacokinetics of LY3484356 in Healthy Females of Non-Child-Bearing Potential [NCT04840888]Phase 182 participants (Actual)Interventional2021-04-26Completed
A Non-Randomized, Open-Label, Three-Part, Drug-Drug Interaction Study to Evaluate the Effects of Itraconazole, Carbamazepine, and Quinidine on the Pharmacokinetics and Safety of EDP-514 in Healthy Subjects [NCT04783753]Phase 172 participants (Actual)Interventional2020-11-05Completed
A Single-Center, Three-Part, Open Label Study to Evaluate the Relative Bioavailability of Two Formulations, Food Effect, and Interaction With Itraconazole Following Single Dose of GSK2140944 in Healthy Subjects and Effect of Food on Safety, Tolerability, [NCT02045849]Phase 146 participants (Actual)Interventional2014-01-28Completed
Pilot Study To Determine the Feasibility of Itraconazole for Primary Treatment and Suppression of Relapse of Disseminated Histoplasmosis in Patients With the Acquired Immunodeficiency Syndrome [NCT00000975]Phase 230 participants InterventionalCompleted
Evaluation Of The Treatment With Oral Itraconazole In Patients With Basocellular Carcinoma Of Skin, Locally Limited Disease. [NCT03972748]28 participants (Anticipated)Interventional2018-01-05Recruiting
A Non-randomised, Open-label, Sequential, Three-part, Phase I Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of Olaparib Following Oral Dosing of a Tablet Formulation, and to Provide Data on the Effect of Olaparib [NCT01900028]Phase 185 participants (Actual)Interventional2013-10-31Completed
A Phase I Randomized, Open-label, 3-arm Parallel-design Study to Determine the Effect of Multiple-dose Gemfibrozil or Itraconazole on the Pharmacokinetics, Safety and Tolerability of Single-dose MDV3100 (ASP9785) in Healthy Male Subjects [NCT01913379]Phase 141 participants (Actual)Interventional2011-08-31Completed
A Phase Ib Study of Extending Relugolix Dosing Intervals Through Addition of the CYP3A4 and Pg-P Inhibitor Itraconazole or Ritonavir in Prostate Cancer Patients [NCT05679388]Phase 1100 participants (Anticipated)Interventional2023-02-13Recruiting
Observational Prospective Multicenter Study to Evaluate the Infective Risk in Myelodysplastic Syndrome Patients: Antimicrobial Prophylaxis and Granulocyte Growth Factors. [NCT01951430]229 participants (Actual)Observational2014-03-31Completed
A Single-Center, Open-Label, One-Sequence, 2-Period, Within-Subject Study in 2 Cohorts to Investigate the Effect of Multiple Doses of Itraconazole (Cohort 1) and Fluoxetine (Cohort 2) on the Pharmacokinetics of a Single Dose of RO5285119 in Healthy Subjec [NCT01967979]Phase 128 participants (Actual)Interventional2013-10-31Completed
Phase 1, Open-label, Parallel, 2-arm, Fixed-sequence Study to Investigate the Effect of Coadministration of CYP3A4 Inhibitor and CYP3A4 Inducer on the Pharmacokinetics, Safety, and Tolerability of KBP-5074 in Healthy Subjects [NCT04606537]Phase 124 participants (Actual)Interventional2020-10-24Completed
Assessment of Mechanisms of Improved Wound Healing of Anabolic Agents and Diet in Severely Burned Patients [NCT00673309]Phase 2/Phase 3644 participants (Actual)Interventional2000-07-31Completed
A Phase I, Single-center, Open-label, 3-group, Fixed-sequence Study to Assess the Effect of Itraconazole, a Potent CYP3A4 Inhibitor, or Diltiazem, a Moderate CYP3A4 Inhibitor, on the Pharmacokinetics of AZD3293 and the Effects of AZD3293 on the Pharmacoki [NCT02010970]Phase 156 participants (Actual)Interventional2013-12-31Completed
A Randomized Double Blind Protocol Comparing Amphotericin B With Flucytosine to Amphotericin B Alone Followed by a Comparison of Fluconazole and Itraconazole in the Treatment of Acute Cryptococcal Meningitis [NCT00000639]400 participants InterventionalCompleted
A Phase I, Open-label, Fixed-Sequence Study to Evaluate the Effect of Multiple-dose Itraconazole or Rifampicin Capsules on the Single-dose PK (Pharmacokinetics) Profiles of IMP4297 Capsules in Healthy Subjects [NCT04584515]Phase 132 participants (Actual)Interventional2020-11-02Completed
An Open-Label Study of the Effect of Tesetaxel on the QTc Interval and the Effect of Food, Itraconazole, and Rifampin on Tesetaxel Pharmacokinetics in Patients With Advanced Solid Tumors [NCT04312282]Phase 193 participants (Actual)Interventional2020-03-06Terminated(stopped due to The Sponsor has discontinued the development of tesetaxel)
The Relationship of Defeverscence and Itraconazole Plasma Level Using Sporanox IV as an Empiric Therapy in Immunocompromised Patients Who Have Been Treated With Sporanox Oral Solution as Prophylaxis [NCT01021683]203 participants (Actual)Observational2009-07-31Completed
A Multicenter Cohort Study of the Short and Long-term Safety of Micafungin and Other Parenteral Antifungal Agents [NCT01686607]40,110 participants (Actual)Observational2012-10-01Completed
A Phase 1, Single-Center, Parallel-Group, Open-Label, Randomized, Drug-Drug Interaction Study to Assess the Effect of Itraconazole, Phenytoin, and Gemfibrozil on the Pharmacokinetics of a Single Oral Dose of BMS-986166 in Healthy Participants [NCT04956627]Phase 115 participants (Actual)Interventional2021-07-28Completed
Assessment of the Treatment of the Severely Burned With Anabolic Agents on Clinical Outcomes, Recovery and Rehabilitation [NCT00675714]Phase 2/Phase 31,126 participants (Actual)Interventional2004-01-31Terminated(stopped due to At the request of the study site, this study has been closed and access to study-related data is unavailable. We are unable to submit the results-data.)
Change in SCIO (Scoring Clinical Index For Onychomycosis) in Toenail Onychomycosis Treating With Itraconazole Capsules [NCT00871728]Phase 4132 participants (Actual)Interventional2007-01-31Completed
Oral Arsenic Trioxide and Itraconazole for the Treatment of Patients With Advanced Basal Cell Carcinoma [NCT02699723]Early Phase 10 participants (Actual)Interventional2020-12-31Withdrawn(stopped due to Logistics)
An Open-Label Fixed-Sequence Study to Assess the Effects of Itraconazole and Rifampicin on the Single-Dose Pharmacokinetics of JNJ-53718678 in Healthy Adult Subjects [NCT02729467]Phase 133 participants (Actual)Interventional2016-03-31Completed
A Single Center, Two Part, Randomized, Open Label Cross-over Study to Evaluate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of GSK525762 in Healthy Female Subjects of Non Child Bearing Potential [NCT02706535]Phase 129 participants (Actual)Interventional2016-05-05Completed
An Open-label, Fixed-sequence, Phase 1 Study of the Effect of CYP3A4 Inhibition by Itraconazole on the Pharmacokinetics of BIIB074 in Healthy Subjects [NCT02698267]Phase 116 participants (Actual)Interventional2016-02-29Completed
Assessment of the Steady State Pharmacokinetics of Itraconazole and Hydroxy-Itraconazole in Healthy Subjects After Administration of a New Itraconazole 200 mg Film Coated Tablet Once Daily for Fourteen Days in Fed Condition [NCT00695071]Phase 116 participants (Actual)Interventional2008-06-30Completed
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 440 participants (Actual)Interventional2015-11-30Completed
A Proof-of-concept Clinical Trial Assessing the Safety of the Coordinated Undermining of Survival Paths by 9 Repurposed Drugs Combined With Metronomic Temozolomide (CUSP9v3 Treatment Protocol) for Recurrent Glioblastoma [NCT02770378]Phase 1/Phase 210 participants (Actual)Interventional2016-11-30Completed
A Phase 1, Randomized, Participant-and Investigator-Blind, Placebo-Controlled, Single-and Multiple-Ascending Dose, Drug-Drug Interaction and Food Effect Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of LY3509754 in Healthy Non-Japanese [NCT04586920]Phase 1104 participants (Actual)Interventional2020-10-20Terminated(stopped due to Terminated due to safety findings)
A Drug-Drug Interaction Study to Evaluate the Effects of Strong CYP3A Induction and Inhibition on the Pharmacokinetics of Segesterone Acetate and Ethinyl Estradiol From the Annovera™ Contraceptive Vaginal System [NCT04290390]Phase 167 participants (Actual)Interventional2020-02-12Completed
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)Interventional2022-06-15Recruiting
Monthly Itraconazole Versus Classic Homeopathy for the Treatment of Recurrent Vulvovaginal Candidiasis: a Randomised Trial [NCT00895453]144 participants (Actual)Interventional2000-05-31Completed
A 2-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effects of Multiple Doses of Itraconazole and Rifampin on the Single-Dose Pharmacokinetics of LOXO-292 in Healthy Adult Subjects [NCT05338489]Phase 124 participants (Actual)Interventional2018-05-11Completed
Discontinuation of Primary and Secondary Prophylaxis for Opportunistic Infections in HIV-infected Patients Who Had CD4+ Cell Count <200 Cells/mm3 But Undetectable Plasma HIV-1 RNA [NCT01392430]74 participants (Actual)Interventional2009-06-30Completed
A Multicenter, Randomized Trial Comparing The Efficacy of Intravenous Followed by Oral Itraconazole With Intravenous Caspofungin For Empiric Antifungal Therapy in Neutropenic Subjects With Hematological Malignancy [NCT02895529]Phase 461 participants (Actual)Interventional2016-11-30Terminated(stopped due to Study is a commitment for license renew, we target on Apr19 submission, considering timeline, a cut off should be scheduled in Apr18.)
An Open-label, 3-Arm, Parallel Design Pharmacokinetic Interaction Study Between MYK-224 and Cytochrome P450 3A4 Inhibitors Itraconazole and Verapamil in Healthy Participants [NCT05304533]Phase 145 participants (Actual)Interventional2022-04-21Completed
Concentration of Itraconazole Solution in Nasal Secretions [NCT00588016]Phase 16 participants (Actual)Interventional2007-04-30Completed
Effect of Itraconazole on the Pharmacokinetics of a Single Oral Dose of BI 1815368 in Healthy Male Subjects (an Open-label, Two-period Fixed-sequence Design Study) [NCT05965583]Phase 114 participants (Actual)Interventional2023-08-02Completed
A First-in-Human Multi-Part Phase 1 Study in Healthy Volunteers to Evaluate the Safety, Tolerability, Pharmacokinetics, and Drug-Drug Interaction Potential of Single and Multiple Doses of ALG-097558 [NCT05840952]Phase 1144 participants (Anticipated)Interventional2023-07-04Recruiting
Phase 1, First-in-human, Double-blind, Placebo-controlled Study to Evaluate the Safety, Tolerability, and PK of Single and Multiple Ascending Oral Doses of XEN1101 and Preliminary Open-label Pharmacodynamic Assessment in Healthy Subjects Addendum: Phase 1 [NCT03340220]Phase 1130 participants (Actual)Interventional2017-11-13Completed
An Open-label Fixed Sequence Trial to Investigate the Potential Drug-drug Interaction of Intravenous Volasertib Co-administered With a P-gp and CYP3A4 Inhibitor (Itraconazole p.o.) in Patients With Various Solid Tumours [NCT01772563]Phase 128 participants (Actual)Interventional2013-02-04Completed
A Phase 1, Open-Label, Fixed-Sequence Study to Evaluate CYP3A4-Mediated, Oral Contraceptive, and pH Modifier Drug Interactions for ABI-H2158 in Healthy Adult Subjects [NCT04142762]Phase 180 participants (Actual)Interventional2019-10-18Completed
A Phase 1, Open-Label, 4-Part, Fixed-Sequence Study to Assess the Effect of Itraconazole, a Strong CYP3A Inhibitor, the Effect of Fluconazole, a Moderate CYP3A/2C9 Inhibitor, the Effect of Rifampin, a Strong CYP3A Inducer, and the Effect of Rabeprazole, a [NCT05602597]Phase 159 participants (Actual)Interventional2022-06-01Completed
A Phase 1, Two Period Fixed-sequence Crossover Study to Assess the Effects of Itraconazole, a Strong CYP3A Inhibitor, on the Pharmacokinetics of Surufatinib in Healthy Subjects [NCT04372407]Phase 113 participants (Actual)Interventional2020-07-09Completed
A Single-Sequence, Open-Label, 2-Period Crossover Trial to Evaluate the Effect of the Potent Cytochrome P-450 3A4 Inhibitor Itraconazole on the Pharmacokinetics of TAK-954 in Healthy Adult Subjects [NCT03173170]Phase 110 participants (Actual)Interventional2017-05-31Completed
A Crossover, Phase 1, Open-label, One-arm Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of S-309309 in Healthy Male and Female Participants [NCT06106334]Phase 114 participants (Anticipated)Interventional2023-11-15Recruiting
Comparative Study Between Pulse Therapy With Oral Itraconazole Versus Continuous Oral Terbinafine Therapy for Treatment of Onychomycosis [NCT05578950]Phase 1100 participants (Actual)Interventional2022-03-01Completed
An Open Labe Study to Evaluate the Drug-Drug Interaction of Itraconazole With GST-HG171/Ritonavir in Healthy Adult Chinese Participants [NCT06087055]Phase 112 participants (Actual)Interventional2023-05-12Completed
A Phase 1 Study of Oral TAK-788 to Evaluate the Drug-Drug Interaction With Itraconazole and Rifampin in Healthy Adult Subjects [NCT03928327]Phase 124 participants (Actual)Interventional2019-05-02Completed
A Three-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effect of Multiple Doses of Itraconazole, Phenytoin, and Paroxetine on the Single-Dose Pharmacokinetics of Poziotinib in Healthy Adult Subjects [NCT04981704]Phase 174 participants (Actual)Interventional2021-04-08Completed
Pharmacokinetics Study of Intravenous Itraconazole Followed by Oral Dosing at 200 Mg Twice Daily in Patients With Advanced HIV Infection [NCT00002370]36 participants InterventionalCompleted
A Phase 1, Fixed-Sequence, Open-Label Drug-Drug Interaction Study to Assess the Effect of Fluvoxamine (CYP1A2 Inhibitor), Cigarette Smoking (CYP1A2 Inducer) and Itraconazole (CYP3A4 Inhibitor) on the Pharmacokinetics of TD-9855 in Healthy Subjects [NCT03432793]Phase 141 participants (Actual)Interventional2018-02-28Completed
A Phase 1 Study to Evaluate the Effects of Multiple Doses of Itraconazole or Carbamazepine on the Single-Dose Pharmacokinetics of LY3537982 in Healthy Adult Subjects [NCT05860933]Phase 130 participants (Anticipated)Interventional2023-05-08Recruiting
Effect of Cold Atmospheric Plasma on Malassezia Folliculitis: a Randomized Controlled Trial [NCT04886323]50 participants (Actual)Interventional2022-08-03Completed
A Phase 1, Open-Label Study to Evaluate the Effect of Rifampin or Itraconazole on the Pharmacokinetics of GDC-0032 in Healthy Subjects [NCT01814709]Phase 132 participants (Actual)Interventional2013-04-30Completed
A Single-center, Open, Single Does, Drug-drug Interaction Study to Investigate the Effects of Itraconazole on the Pharmacokinetics of Healthy Chinese Adult Subjects After Oral Administration of SHR2554 Tablets [NCT04627129]Phase 118 participants (Actual)Interventional2020-06-01Completed
Effect of Itraconazole on the Pharmacokinetics of Apatinib in Chinese Healthy Volunteers [NCT02836171]Phase 120 participants (Actual)Interventional2016-07-31Completed
A Study to Assess the Effect of Itraconazole Capsules on the Pharmacokinetics of ZX-7101A Tablets in Healthy Adult Subjects in China [NCT05949385]Phase 116 participants (Anticipated)Interventional2023-07-12Not yet recruiting
A Phase 1, Single-center, Open-label, Sequential Dose-Escalation Study of ACP-196 in Healthy Subjects to Evaluate Safety, Pharmacokinetics, Pharmacodynamics, Food Effects, and Drug-Drug Interactions [NCT04901923]Phase 159 participants (Actual)Interventional2014-03-15Completed
SUBA-Itraconazole Therapy for Coccidioidomycosis Refractory or Intolerant to Fluconazole [NCT04809649]Phase 20 participants (Actual)Interventional2021-05-15Withdrawn(stopped due to Sponsor is not proceeding with study due to budget cuts as a result of COVID-19.)
Randomized Study Comparing Itraconazole to Placebo in the Prevention of Histoplasmosis in Patients With Human Immunodeficiency Virus Infection [NCT00002438]0 participants InterventionalCompleted
A Phase 1, Open-label, 2-Part, 2-Period Fixed-Sequence Crossover Study to Assess the Effect of Itraconazole, and the Effect of Rifampin on the Pharmacokinetics of HMPL-523 in Healthy Volunteers [NCT05720767]Phase 128 participants (Actual)Interventional2022-11-04Completed
An Open-label, Fixed Sequence Study in Healthy Subjects to Assess the Pharmacokinetics of Capivasertib When Administered Alone and In Combination With Itraconazole [NCT04712396]Phase 111 participants (Actual)Interventional2021-02-01Completed
Itraconazole for the Prevention of Fungal Infections in Chronic Granulomatous Disease [NCT00001280]Phase 2100 participants Interventional1991-01-31Completed
Relative Bioavailability of a Single Oral Dose of BI 691751 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, Randomised, Two-period, Two-sequence Crossover Study) [NCT02044393]Phase 120 participants (Actual)Interventional2014-01-31Completed
Randomized Trial Of Safety And Tolerability Of Intravenous/Oral Voriconazole Versus Intravenous/Oral Itraconazole For Long-Term Antifungal Prophylaxis In Allogeneic Hematopoietic Stem Cell Transplant Recipients [NCT00079222]0 participants Interventional2003-11-30Completed
An Open-label Study to Evaluate the Drug-drug Interaction Effect of Itraconazole, a CYP3A4 Inhibitor, on the Pharmacokinetics of AMG 510 in Healthy Subjects [NCT05568082]Phase 114 participants (Actual)Interventional2019-12-03Completed
A Randomized, Double-Blind, Placebo-Controlled, Dose-Ranging, Phase II Study of the Safety and Antifungal Activity of Subcutaneous Recombinant Interferon-Gamma 1b (rIFN-Gamma 1b) in Conjunction With Standard Therapy in Patients With Acute Cryptococcal Men [NCT00012467]Phase 260 participants Interventional2000-01-31Completed
Randomized, Double-blind, Placebo-controlled, Escalating Single Dose Study of the Safety, Tolerability, and Pharmacokinetics of Orally Administered BAY1161116 in Healthy Postmenopausal Women Including Food-effect and Drug-drug-interaction With Itraconazol [NCT03119077]Phase 132 participants (Actual)Interventional2017-04-27Terminated(stopped due to Study early terminated due to lower drug exposure)
Comparative Study Between Pulsed and Continuous Itraconazole for the Treatment of Onychomychosis [NCT05567484]Phase 160 participants (Actual)Interventional2021-05-01Completed
An Open-label, Fixed Sequence Study in Healthy Subjects to Assess the Pharmacokinetics of AZD4831 When Administered Alone and in Combination With Itraconazole [NCT05236543]Phase 121 participants (Actual)Interventional2022-02-18Completed
Prediction of Itraconazole Oral Absorption From In Vitro Dissolution [NCT04035187]Phase 417 participants (Actual)Interventional2020-02-10Completed
Relative Bioavailability of a Single Oral Dose of BI 894416 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, One-way Crossover Study) [NCT03722173]Phase 114 participants (Actual)Interventional2018-11-13Completed
Randomized Double-Blinded Controlled Trial of Oral Antifungal for the Treatment of Fungal Sensitive Chronic Rhinosinusitis With Nasal Polyps [NCT02285283]Phase 2/Phase 358 participants (Actual)Interventional2014-11-30Terminated(stopped due to Recruitment failure.)
A Phase I/IIa Study Assessing Single and Multiple Doses of IDX21437 in Healthy and HCV-Infected Subjects [NCT01974687]Phase 1/Phase 2178 participants (Actual)Interventional2013-10-31Completed
Effect of Multiple Doses of Itraconazole on the Pharmacokinetics of a Single Oral Dose of BI 1026706 in Healthy Male Subjects (an Open-label, Randomised, Two-period, Two-sequence Crossover Study) [NCT02513446]Phase 116 participants (Actual)Interventional2015-09-29Completed
An Open-label Fixed Sequence Trial to Investigate the Potential Drug-drug Interaction When BI 907828 is Co-administered With an OATP1B1 and/or OATP1B3 Transporter Inhibitor or With a CYP3A4 Inhibitor in Patients With Various Solid Tumours [NCT05372367]Phase 132 participants (Anticipated)Interventional2022-06-30Recruiting
An Open-label, Non-randomized, Fixed Sequence Study Assessing the Pharmacokinetics of AZD7986 When Administered Alone and With Multiple Doses of Verapamil and Itraconazole or Diltiazem in Healthy Subjects [NCT02653872]Phase 115 participants (Actual)Interventional2016-01-22Completed
Signal TrAnsduction Pathway Activity Analysis in OVarian cancER [NCT03458221]Phase 2/Phase 3148 participants (Anticipated)Interventional2023-01-31Recruiting
A Phase 1 Open-label 2-Part 2-Period Fixed-sequence Crossover Study To Assess The Effect Of Itraconazole, A Strong CYP3A Inhibitor, And The Effect Of Rifampin, A Strong CYP3A Inducer, On Pharmacokinetics Of Fruquintinib In Healthy Subjects [NCT04557397]Phase 128 participants (Actual)Interventional2020-09-02Completed
A Two-Part Phase 1 Study to Evaluate the Potential Drug Interaction Between ACH-0145228 and Midazolam, Digoxin, and Itraconazole in Healthy Adult Subjects [NCT04709081]Phase 138 participants (Actual)Interventional2019-12-22Completed
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 2175 participants (Actual)Interventional2008-11-30Completed
Effect of Itraconazole on the Pharmacokinetics of a Single Oral Dose of BI 474121 in Healthy Male Subjects (an Open-label, Two-period Fixed Sequence Design Study) [NCT04716894]Phase 114 participants (Actual)Interventional2021-02-01Completed
Relative Bioavailability of a Single Oral Dose of BI 1291583 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, Two-period, Fixed Sequence Study) [NCT03890887]Phase 114 participants (Actual)Interventional2019-04-12Completed
A Single-center, Non-randomized, Open-lable, Self-controlled Clinical Trial to Evaluate JAB-21822 Drug-drug Interactions in Healthy Subjects [NCT06162169]Phase 166 participants (Anticipated)Interventional2023-11-25Recruiting
Open-label, Randomised, Two-way Crossover Study to Assess the Effect of Once Daily Itraconazole on the Pharmacokinetics of BI 409306 After a Single Oral Dose in Healthy Male Volunteers Genotyped as Poor and Extensive Metabolizers of CYP2C19 [NCT02248259]Phase 125 participants (Actual)Interventional2014-10-31Completed
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 132 participants (Anticipated)Interventional2021-11-24Active, not recruiting
Evaluation and Validation of Metabolic Markers for the Prediction of Drug-drug Interaction of Various CYP3A4 Substrates and Inhibitors in Healthy Male Subjects [NCT02975037]Phase 132 participants (Actual)Interventional2017-02-06Completed
A Phase 1, Open-label, Fixed-sequence Study to Estimate the Effects of Multiple-dose Administration of Itraconazole on the Pharmacokinetics of SHR8554 in Healthy Adult Subjects [NCT05928988]Phase 117 participants (Actual)Interventional2022-01-04Completed
A Phase 1, Open-label Study to Evaluate the Effect of Fluconazole, Bupropion, or Itraconazole on the Pharmacokinetics and Safety of BMS-986235 [NCT04464577]Phase 10 participants (Actual)Interventional2021-04-01Withdrawn(stopped due to Business objectives have changed.)
Retrospective Observation of Empirical Antifungal Therapy With Itraconazole [NCT01706562]138 participants (Actual)Observational2011-05-31Completed
A Phase 1, Open-Label Study to Examine the Effect of Ciprofloxacin, Itraconazole, and Rifampin on the Pharmacokinetics of Lumacaftor in Combination With Ivacaftor in Healthy Adult Subjects [NCT01768663]Phase 180 participants (Actual)Interventional2013-01-31Completed
A Clinical Drug-Drug Interaction Study to Evaluate the Effect of a Proton Pump Inhibitor, a Combined P-gp/CYP3A4 Inhibitor, and a CYP2C9 Inhibitor on the Pharmacokinetics of Vismodegib [NCT01772290]Phase 192 participants (Actual)Interventional2013-02-28Completed
A Phase 1 Study to Evaluate the Effect of Itraconazole, a Strong CYP3A Inhibitor, on the Pharmacokinetics of Alisertib (MLN8237) in Adult Patients With Advanced Solid Tumors or Relapsed/Refractory Lymphoma [NCT02259010]Phase 124 participants (Actual)Interventional2014-10-22Completed
A Phase I, Single-center, Open-label, Fixed-sequence Clinical Study to Evaluate the Effects of Multiple Administrations of Rifampin or Itraconazole on the Pharmacokinetic Characteristics of a Single Administration of Orelabrutinib Tablets in Healthy Subje [NCT05316857]Phase 136 participants (Actual)Interventional2021-12-16Completed
A Phase 1, Open-label, Fixed-sequence Study To Estimate The Effects Of Multiple-dose Administration Of Itraconazole On The Pharmacokinetics Of Pf 04958242 In Healthy Adult Subjects [NCT02341482]Phase 113 participants (Actual)Interventional2015-02-05Completed
A Single Centre, Open Label, One Sequence, Cross-over Study to Evaluate the Effect of Itraconazole on the Pharmacokinetics of Single Inhaled Doses of Nemiralisib in Healthy Subjects [NCT03398421]Phase 120 participants (Actual)Interventional2018-01-17Completed
Relative Bioavailability of a Single Oral Dose of BI 425809 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Trial) [NCT02342717]Phase 116 participants (Actual)Interventional2015-01-31Completed
Effect of P-gp Inhibition, OATP-inhibition and Food on the Kinetics of a Single Oral Dose BI 685509 in Healthy Male Subjects [NCT03116893]Phase 115 participants (Actual)Interventional2017-04-19Completed
An Open Study of the Effect of Itraconazole Oral Solution for the Treatment of Fluconazole Refractory Oropharyngeal Candidiasis in HIV-Positive Subjects. [NCT00002133]0 participants InterventionalCompleted
A Prospective, Two-center, Clinical Study to Optimize the Treatment for Allergic Bronchopulmonary Aspergillosis (ABPA) [NCT05129033]100 participants (Anticipated)Interventional2021-11-15Not yet recruiting
An Open-lable, Two- Period, Single-sequence, Self-controlled Study to Evaluate the Effect of Oral Rifampicin or Itraconazole on the Pharmacokinetics of ASK120067 Tablets [NCT05631678]Phase 148 participants (Actual)Interventional2022-06-06Completed
A Randomized Trial of Itraconazole in Acute Stages of Allergic Bronchopulmonary Aspergillosis [NCT02440009]Phase 2/Phase 3191 participants (Actual)Interventional2014-05-31Completed
A Phase 1, Randomized, Open-label, 3-sequence, 4-treatment, Incomplete Block Design To Estimate The Effect Of Steady State Cyp3a4 Inhibitors (Itraconazole, Diltiazem Or Verapamil) On The Pharmacokinetics Of Singe Dose Pf-00489791 In Healthy Volunteers [NCT02319148]Phase 122 participants (Actual)Interventional2014-07-31Completed
An Open-label, Randomized, 2-Period Crossover Study to Evaluate the Effect of Co-administration of Itraconazole or Diltiazem on the Single-dose Pharmacokinetics of Danicamtiv in Healthy Participants [NCT05162222]Phase 130 participants (Actual)Interventional2021-12-15Completed
A Multicenter, Prospective, Randomized, Double-Blind Clinical Trial Comparing Itraconazole Oral Solution in Cyclodextrin to Placebo in the Treatment of Aspergilloma [NCT00005668]Phase 296 participants InterventionalCompleted
A Phase 1, Open-Label, Drug-Drug Interaction Study in Healthy Subjects to Determine the Effects of a Strong Inhibitor (Itraconazole) of Cytochrome P450 3A on Exposure to Mifepristone and Its Metabolites [NCT03259542]Phase 133 participants (Actual)Interventional2017-08-09Completed
Drug-drug Interaction Study With TS-142 in Healthy Adult Subjects (Concomitant Administration of Itraconazole) [NCT04557163]Phase 110 participants (Actual)Interventional2020-10-13Completed
Study on Food Influence and Drug-drug Interaction of HLX208 Tablets in Chinese Healthy Subjects [NCT05902728]Phase 152 participants (Anticipated)Interventional2023-07-04Not yet recruiting
Efficacy of Itraconazole and of Voriconazole in Patients With Cystic Fibrosis and Presenting With Persistent Positive Sputums for Aspergillus. [NCT01576315]Phase 211 participants (Actual)Interventional2014-06-30Completed
A Randomized Phase II Clinical Trial of Two Dose-levels of Itraconazole in Patients With Metastatic Castration-resistant Prostate Cancer [NCT00887458]Phase 246 participants (Actual)Interventional2009-07-31Completed
Phase II Study of Concurrent Chemoradiotherapy With Itraconazole in Treating Patients With Locally Advanced Esophageal Squamous Cancer [NCT04481100]Phase 238 participants (Anticipated)Interventional2020-10-01Recruiting
Efficacy and Safety of Ambulatory Low-dose Venetoclax and Azacitidne as First Line Therapy in Newly Diagnosed AML: a Pilot Study [NCT05048615]Phase 215 participants (Actual)Interventional2021-07-26Completed
A Phase 1, Drug-Drug Interaction Study to Evaluate the Effect of Itraconazole on the Pharmacokinetics of TAK-272 and the Effect of TAK-272 on the Pharmacokinetics of Digoxin or Midazolam In the Healthy Adult Participants [NCT02370615]Phase 134 participants (Actual)Interventional2015-02-28Completed
Relative Bioavailability of a Single Oral Dose of BI 1015550 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects [NCT03403439]Phase 116 participants (Actual)Interventional2018-05-03Completed
A Phase 1, Open-Label, 2-period Drug-Drug Interaction Study to Investigate the Effect of Multiple Doses of Itraconazole on the Single-Dose Pharmacokinetic Profile of AB928 in Healthy Adult Participants [NCT05154136]Phase 120 participants (Actual)Interventional2021-10-20Completed
A Randomized, Double Blind Phase II Proof-of-Concept Superiority Trial of Fosravuconazole 200 mg or 300 mg Weekly Dose Versus Itraconazole 400 mg Daily, All Three Arms in Combination With Surgery, in Patients With Eumycetoma in Sudan [NCT03086226]Phase 2138 participants (Anticipated)Interventional2017-04-30Recruiting
A Phase I/II Trial Investigating the Tolerability, Toxicity and Efficacy of Hydroxychloroquine and Itraconazole in Patients With Advanced Platinum-resistant Epithelial Ovarian Cancer (EOC) (HYDRA-1 Study) [NCT03081702]Phase 1/Phase 213 participants (Actual)Interventional2017-07-25Completed
Phase 0 Pharmacodynamic Study of the Effects of Itraconazole on Tumor Angiogenesis and the Hedgehog Pathway in Early-stage Non-small Cell Lung Cancer [NCT02357836]Early Phase 113 participants (Actual)Interventional2015-06-30Completed
An Open-label, 3-period Fixed-sequence Study in Healthy Subjects to Assess the Pharmacokinetics (PK) of Savolitinib When Administered Alone and in Combination With Itraconazole [NCT04121910]Phase 116 participants (Actual)Interventional2019-11-07Completed
A Phase 1, Multicenter, Open-label, Single Sequence Crossover Study to Evaluate Drug-drug Interaction Potential of OATP1B/CYP3A Inhibitor on the Pharmacokinetics of DS-8201a in Subjects With HER2-expressing Advanced Solid Malignant Tumors [NCT03383692]Phase 140 participants (Actual)Interventional2018-01-12Completed
A Study to Determine the Effect of CYP3A Inhibition on the Pharmacokinetics of LY2623091 and the Effect of LY2623091 on the Pharmacokinetics of CYP3A Substrates in Healthy Subjects [NCT02300259]Phase 148 participants (Actual)Interventional2014-11-30Completed
Pilot Study to Determine the Feasibility of Itraconazole for Suppression of Relapse of Disseminated Histoplasmosis in Patients With the Acquired Immunodeficiency Syndrome [NCT00000992]Phase 130 participants InterventionalCompleted
Randomized, Controlled, Double-Blind Study of Itraconazole Oral Solution Versus Fluconazole Tablets for the Treatment of Esophageal Candidiasis. [NCT00002132]0 participants InterventionalCompleted
An Open-Label Extension Study of Maintenance Therapy in HIV-Positive Subjects With Fluconazole-Refractory Oropharyngeal Candidiasis Who Have Responded to Itraconazole Oral Solution [NCT00002341]0 participants InterventionalCompleted
An Open-label, Fixed Sequence Study to Evaluate the Effects of Multi-dose of Itraconazole or Rifampin on the Pharmacokinetic Profiles of Single Dose of SPH3127 in Healthy Volunteers [NCT05359055]Phase 1/Phase 240 participants (Actual)Interventional2021-12-13Completed
A Randomized, Comparative Study of Itraconazole Versus Fluconazole for Prevention of Aspergillus Infections in Peripheral Blood Stem Cell and Marrow Transplant Recipients [NCT00003883]Phase 3578 participants (Anticipated)Interventional1998-10-31Completed
A Phase 1 Study to Evaluate the Effects of Fluconazole and Itraconazole CYP3A-Mediated Inhibition on the Pharmacokinetics, Safety, and Tolerability of MLN4924 in Patients With Advanced Solid Tumors [NCT02122770]Phase 151 participants (Actual)Interventional2014-04-01Completed
A Phase 1, Open-Label Study to Evaluate the Effect of Itraconazole on the Pharmacokinetics of Cobimetinib in Healthy Subjects [NCT01929876]Phase 116 participants (Actual)Interventional2013-07-31Completed
A Randomized, Open, Comparative Multicenter Study of Initial Treatment With Intravenous Itraconazole Versus Amphotericin B Followed by Consolidation Treatment With Itraconazole Capsules in Patients With Blastomycosis or Histoplasmosis [NCT00002159]Phase 360 participants InterventionalCompleted
A Phase I, Open-label, Non-randomised Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of a Single Oral Dose of AZD9291 in Patients With EGFRm Positive NSCLC Whose Disease Has Progressed on an EGFR TKI [NCT02157883]Phase 139 participants (Actual)Interventional2014-11-06Completed
Effect of Itraconazole on the Pharmacokinetics of a Single Oral Dose of BI 706321 in Healthy Male Subjects (an Open-label, Two-period Fixed Sequence Design Study) [NCT04714073]Phase 114 participants (Actual)Interventional2021-02-11Completed
Open-label, Non-randomized, One Sequence Cross-over Study to Investigate the Effect of Inhibition of CYP3A4/5 by Itraconazole on the Pharmacokinetics of CHF6001 in Healthy Subjects [NCT04739774]Phase 124 participants (Actual)Interventional2021-02-22Completed
Randomized, Double-Blinded, Placebo-Controlled Single and Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of BMS-986141 in Healthy Subjects [NCT02341638]Phase 1148 participants (Actual)Interventional2014-09-30Completed
A Phase 1, Open-label, Parallel-group, Fixed-sequence Study to Investigate the Effect of the CYP3A Inducer Rifampin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of BGB-3111 in Healthy Subjects [NCT03301181]Phase 140 participants (Actual)Interventional2017-09-18Completed
An Open-label Study to Evaluate the Effect of Repeated Oral Administration of 200 mg Itraconazole(ITZ) Given Once Daily Over 14 Days on the Single Oral Dose Pharmacokinetics of Vilaprisan (BAY1002670) as Well as Assessment of Absolute Bioavailability Usin [NCT02456129]Phase 114 participants (Actual)Interventional2015-07-31Completed
A Phase I, Open Label, Drug-drug Interaction Study to Evaluate the Effects of Itraconazole and Rifampin on the Pharmacokinetics of ASC40 in Healthy Subjects [NCT04843449]Phase 124 participants (Actual)Interventional2021-04-04Completed
Single Center, Open-Label, Single-Sequence, Within-Subject Study In Two Cohorts Of Healthy Male Subjects Comparing Single-Dose Pharmacokinetics Of Fedovapagon Alone And In Combination With A CYP3A4 Inhibitor, Itraconazole, Or A CYP3A4 Inducer, Rifampicin [NCT02440841]Phase 129 participants (Actual)Interventional2015-05-31Completed
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 163 participants (Actual)Interventional2017-04-18Completed
An Open-Label Phase I Trial to Evaluate the Safety and Tolerability of ATRA, Celecoxib, and Itraconazole Administered As Maintenance Treatment Post-Autologous Transplantation in Relapsed Multiple Myeloma [NCT02401295]Phase 11 participants (Actual)Interventional2015-05-31Completed
Single-Ascending Dose, Safety, Tolerability, Pharmacokinetic, and Cytochrome P450 Interaction Study of LY3154207 in Healthy Subjects [NCT02365571]Phase 164 participants (Actual)Interventional2015-02-28Completed
Phase IIb Open-label Trial of SUBA™-Itraconazole in Subjects With Basal Cell Carcinoma Nevus Syndrome (BCCNS) [NCT02354261]Phase 238 participants (Actual)Interventional2015-08-07Completed
Evaluation and Validation of Metabolic Markers for the Assessment of CYP3A Activity and Prediction of Drug-drug Interaction in Korean Healthy Subjects [NCT02328443]Phase 124 participants (Actual)Interventional2014-01-31Completed
A Single-centre, Open, Single-dose, Self-control Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of SHR6390 in Healthy Chinese Adult Subjects. [NCT04423601]Phase 118 participants (Actual)Interventional2020-06-10Completed
UVX as an Adjuvant in the Treatment of Fungal Keratitis [NCT03138785]20 participants (Actual)Interventional2015-01-01Active, not recruiting
A Phase 1, Open Label, Two-part, Fixed-sequence Drug Interaction Study to Investigate the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and CYP3A4 Inducer (Rifampin) on the Pharmacokinetics of LOXO 305 in Healthy Adult Subjects [NCT05134337]Phase 124 participants (Actual)Interventional2020-02-12Completed
AN INTERVENTIONAL, PHASE 1, OPEN-LABEL, FIXED SEQUENCE, 2-PERIOD STUDY TO ESTIMATE THE EFFECT OF MULTIPLE DOSES OF ITRACONAZOLE ON THE PHARMACOKINETICS OF SINGLE DOSE ARV-471 IN THE FED CONDITION IN HEALTHY ADULT MALES, AND FEMALES OF NONCHILDBEARING POTE [NCT05538312]Phase 112 participants (Actual)Interventional2023-02-23Completed
Evaluating the Healing of Diabetic Foot Ulcers With Compounded Anti-Infective Irrigation [NCT05076955]Early Phase 1100 participants (Anticipated)Interventional2021-03-31Recruiting
PHASE 1 SAFETY, PHARMACOKINETIC AND PHARMACODYNAMIC STUDY OF PF-02341066, A MET/HGFR SELECTIVE TYROSINE KINASE INHIBITOR, ADMINISTERED ORALLY TO PATIENTS WITH ADVANCED CANCER [NCT00585195]Phase 1596 participants (Actual)Interventional2006-04-19Completed
Human Immunodeficiency Virus Negative Host Talaromyces Between Voriconazole and Amphotericin B Sequential Itraconazole Therapy [NCT03827278]200 participants (Anticipated)Interventional2018-12-30Recruiting
A Drug-drug Interaction Study Evaluating the Pharmacokinetic Effects of Itraconazole or Rifampin or Esomeprazole on XZP-3621 Tablets in Healthy Subjects [NCT05586568]Phase 172 participants (Anticipated)Interventional2022-11-15Not yet recruiting
A Pilot Study to Assess The Therapeutic Effectiveness Of Isotretinoin In Preventing Recurrences In Chronic Recurrent Dermatophytosis [NCT03471455]Phase 2100 participants (Anticipated)Interventional2018-04-30Not yet recruiting
A Phase 1, Parallel-group, 3-part, 2-period, Fixed-sequence, Crossover, Open-label, Nonrandomized, Drug-drug Interaction Study to Assess the Pharmacokinetics of CC-92480 (BMS-986348) After Coadministration With Rifampin and Itraconazole, and Pharmacokinet [NCT05389722]Phase 124 participants (Actual)Interventional2022-06-09Completed
Treatment of Aspergillus Fumigatus in Patients With Cystic Fibrosis: A Randomized, Double-blind, Placebo-Controlled Trial [NCT00528190]Phase 435 participants (Actual)Interventional2007-10-31Completed
A Phase 2 Study of Itraconazole in Castrate-resistant Prostate Cancer Post-chemotherapy [NCT01450683]Phase 24 participants (Actual)Interventional2010-09-30Terminated(stopped due to Low accrual)
A Randomized Phase II Study of Itraconazole and Pemetrexed in Patients With Previously Treated Non-Squamous Non-Small Cell Lung Cancer [NCT00769600]Phase 223 participants (Actual)Interventional2008-11-30Terminated(stopped due to Low accrual.)
Interventional, Open-label, Randomized, Two-sequence Study Evaluating the Effect of CYP3A4 Inhibition on the Pharmacokinetics, Safety and Tolerability of Lu AG06466 in Healthy Men and Women [NCT04405323]Phase 116 participants (Actual)Interventional2020-05-20Completed
Clinical Efficacy and Safety of Itraconazole Injection/Oral Solution Sequential Therapy for Treatment of Invasive Pulmonary Fungal Infections [NCT01823289]Phase 471 participants (Actual)Interventional2007-06-30Completed
Feasibility of Itraconazole as a Targeted Therapy for Inhibition of Hedgehog Pathway Signaling in Patients With Esophageal Cancer [NCT02749513]Early Phase 118 participants (Actual)Interventional2016-01-31Active, not recruiting
Relative Bioavailability of a Single Oral Dose of BI 1358894 When Administered Alone or in Combination With Multiple Oral Doses of Itraconazole in Healthy Male Subjects (an Open-label, Fixed Sequence Study) [NCT03843151]Phase 116 participants (Actual)Interventional2019-03-19Completed
A Phase 1, Open-label, Dose Finding Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of CC-90011 in Subjects With Relapsed and/or Refractory Solid Tumors and Non-Hodgkin's Lymphomas [NCT02875223]Phase 191 participants (Anticipated)Interventional2016-08-31Active, not recruiting
[NCT00004811]Phase 1/Phase 27 participants Interventional1985-03-31Completed
The Effect of Multiple Doses of Itraconazole on the Pharmacokinetics of a Single Oral Dose of BI 1810631 in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Trial) [NCT05833139]Phase 116 participants (Actual)Interventional2023-04-14Completed
Hedgehog Inhibition as a Non-Castrating Approach to Hormone Sensitive Prostate Cancer: A Phase II Study of Itraconazole in Biochemical Relapse [NCT01787331]Phase 221 participants (Actual)Interventional2013-10-29Completed
Itraconazole Repurposing to Reduce Residual Cancer Risk in Patients With High-risk Barrett's Esophagus After Ablation [NCT05609253]Phase 110 participants (Anticipated)Interventional2022-09-14Recruiting
Investigation of Interactions Between Faldaprevir, Itraconazole, Atorvastatin and Rosuvastatin in Healthy Male and Female Subjects (Open-label, Fixed-sequence) [NCT01795937]Phase 151 participants (Actual)Interventional2013-02-28Completed
A Phase 1, Open-Label, 4-Part Study to Evaluate the Effect of Food, Cytochrome P 450 Inhibition and Induction on the Pharmacokinetics of CC 122 in Healthy Adult Subjects [NCT03340662]Phase 181 participants (Actual)Interventional2017-11-09Completed
A Phase 1, Open-label, Three-Part, Fixed-Sequence Trial in Healthy Adult Participants to Evaluate the Effects of Itraconazole and Carbamazepine on the Single-Dose Pharmacokinetics of Emraclidine, and the Effect of Emraclidine on the Single-Dose Pharmacoki [NCT05965219]Phase 160 participants (Anticipated)Interventional2023-08-15Recruiting
A Phase I Single-Center, Randomized, Open-label, Single Dose, Crossover Study in Korean Healthy Male Volunteers to Evaluate Pharmacokinetics of Lozanoc and Sporanox [NCT02493738]Phase 124 participants (Actual)Interventional2015-07-31Completed
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 23 participants (Actual)Interventional2013-03-31Terminated(stopped due to Low Accrual)
A Randomized Trial Comparing the Role of Prednisolone, Itraconazole, or Their Combination in Patients With Acute Stage of Allergic Bronchopulmonary Aspergillosis [NCT06174922]Phase 3300 participants (Anticipated)Interventional2023-12-31Recruiting
A Phase I, Open-label, Non-randomised Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor), Rifampicin (a CYP3A4 Inducer), and Omeprazole (a Proton Pump Inhibitor) on the Pharmacokinetics of a Single Oral Dose of Adavosertib in Patients With Ad [NCT04959266]Phase 15 participants (Actual)Interventional2021-06-28Terminated(stopped due to The study terminated because the clinical development programme for Adavosertib has been discontinued)
COVID-19: A PHASE 1, OPEN-LABEL, FIXED SEQUENCE, 2-PERIOD CROSSOVER STUDY TO ESTIMATE THE EFFECT OF ITRACONAZOLE ON THE PHARMACOKINETICS OF PF-07321332/RITONAVIR IN HEALTHY PARTICIPANTS [NCT04962022]Phase 112 participants (Actual)Interventional2021-07-20Completed
A 2-Part, Non-randomized, Open-label Study to Evaluate the Effect of Itraconazole, Rifampicin, Rabeprazole, and Omeprazole on the Pharmacokinetics of Belumosudil (KD025) [NCT03530995]Phase 173 participants (Actual)Interventional2018-04-09Completed
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 158 participants (Actual)Interventional2018-02-09Completed
A Randomized, Open-Label, Four-Cohort, Parallel Design Study to Evaluate the Effect of Itraconazole or Rifampin on the Single-Dose Pharmacokinetics of BMS-986205 in Normal Healthy Participants [NCT03346837]Phase 153 participants (Actual)Interventional2017-11-22Completed
A Phase II Trial Evaluating the Effectiveness of Itraconazole in Improving Pathologic Complete Response Rates in Patients With Esophageal Cancer Through Inhibition of the Hedgehog and AKT Signaling Pathways [NCT04018872]Phase 278 participants (Anticipated)Interventional2019-06-24Recruiting
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO EVALUATE THE EFFECT OF ITRACONAZOLE AND CYCLOSPORINE ON THE SINGLE-DOSE PHARMACOKINETICS OF PF-07081532 IN OVERWEIGHT OR OBESE ADULT PARTICIPANTS [NCT05745701]Phase 116 participants (Actual)Interventional2023-02-22Completed
A Randomized Controlled Trial to Compare the Clinical Outcomes of Six Months Versus 12 Months of Oral Itraconazole Therapy for Management of Treatment naïve Subjects With Chronic Pulmonary Aspergillosis [NCT03920527]Phase 3164 participants (Actual)Interventional2019-07-01Completed
A Phase 1, Open-Label, Fixed-Sequence, Drug-Drug Interaction Study of APX001 to Evaluate the Effects of CYP3A4 Inhibition and Pan-CYP Induction in Two Parallel Groups of Healthy Male and Female Subjects [NCT04166669]Phase 136 participants (Actual)Interventional2019-11-12Completed
Pilot Study on the Evaluation of the Efficacy, Tolerability and Safety of Topical and Oral Antifungals in the Treatment of Onychomycosis and Creation of a Library of Dermatological Clinical Isolates [NCT05482763]200 participants (Anticipated)Observational [Patient Registry]2022-07-20Recruiting
Single- and Multiple-Ascending Dose, Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Study of LY3202626 [NCT02323334]Phase 194 participants (Actual)Interventional2014-12-31Completed
A Phase 1 Open-Label, Fixed-Sequence Drug-Drug Interaction Study to Evaluate the Effects of Steady-state Itraconazole and Rifampin on the Single-dose Pharmacokinetics of Lazertinib Tablets in Healthy Adult Participants [NCT04410094]Phase 132 participants (Actual)Interventional2020-09-14Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00045942 (36) [back to overview]Summary of CGP62221 Plasma Concentration for 100 mg Bid Arm (E1)
NCT00045942 (36) [back to overview]Summary of CGP52421 Plasma Concentration for 50 mg Bid Arm (E1)
NCT00045942 (36) [back to overview]Summary of CGP62221 Concentration (E2)
NCT00045942 (36) [back to overview]Summary of CGP62221 Plasma Concentration (Core)
NCT00045942 (36) [back to overview]Summary of CGP62221 Plasma Concentration for 50 mg Bid Arm (E1)
NCT00045942 (36) [back to overview]Summary of Midostaurin Concentration in the PKC412 Dose Escalation Arms(E2)
NCT00045942 (36) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) for CGP52421 in the PKC412 + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Summary of Midostaurin Plasma Concentration (Core)
NCT00045942 (36) [back to overview]Summary of PKC412 Plasma Concentration for 50 mg Twice Daily (Bid) Arm (E1)
NCT00045942 (36) [back to overview]Terminal Elimination Half-life (T1/2) for PKC412 in the PKC + Itrconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Time to Reach the Maximum Concentration After Drug Administration (Tmax) for CGP52421 in the PKC412 + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Time to Reach the Maximum Concentration After Drug Administration (Tmax) for CGP62221 in the PKC412 + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Time to Reach the Maximum Concentration After Drug Administration (Tmax) for PKC412 in the PKC412 + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Duration of Best Clinical Response (E1)
NCT00045942 (36) [back to overview]Event-free Survival (E1)
NCT00045942 (36) [back to overview]Number of Participants With Best Clinical Response (Core)
NCT00045942 (36) [back to overview]Overall Survival (E2)
NCT00045942 (36) [back to overview]Overall Survival (OS) (E1)
NCT00045942 (36) [back to overview]Terminal Elimination Half-life (T1/2) for CGP62221 in the PKC + Itrconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Time to Disease Progression (E1)
NCT00045942 (36) [back to overview]Time to Disease Progression (E2)
NCT00045942 (36) [back to overview]Time to Disease Progression (TTP) (Core)
NCT00045942 (36) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval Tau (AUCtau) for CGP52421 Plasma in the PKC + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval Tau (AUCtau) for CGP62221 Plasma in the PKC + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval Tau (AUCtau) for PKC412 Plasma in the PKC + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Summary of PKC412 Plasma Concentration for 100 mg Bid Arm (E1)
NCT00045942 (36) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) for CGP622221 in the PKC412 + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) for PKC412 in the PKC412 + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Best Clinical Response (E2)
NCT00045942 (36) [back to overview]Number of Participants With Overall Clinical Response (E1)
NCT00045942 (36) [back to overview]Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax) for CGP52421 in the PKC + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax) for CGP62221 in the PKC + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax) for PKC412 in the PKC + Itraconazole Combination Arm (E2)
NCT00045942 (36) [back to overview]Summary of CGP52421 Concentration (E2)
NCT00045942 (36) [back to overview]Summary of CGP52421 Plasma Concentration (Core)
NCT00045942 (36) [back to overview]Summary of CGP52421 Plasma Concentration for 100 mg Bid Arm (E1)
NCT00289991 (9) [back to overview]Duration of Treatment
NCT00289991 (9) [back to overview]Percent of Subjects With Use of Other Systemic Antifungal Agents as Empirical or Therapeutic Treatment
NCT00289991 (9) [back to overview]Survival: Percent of Subjects Who Died Within 1 Year
NCT00289991 (9) [back to overview]Time to Breakthrough Invasive Fungal Infection (IFI)
NCT00289991 (9) [back to overview]Time to Discontinuation of Study Treatment
NCT00289991 (9) [back to overview]Percent of Subjects With Occurrence of Breakthrough IFI
NCT00289991 (9) [back to overview]Success at Day 100: Percent of Responders (Randomization Strata)
NCT00289991 (9) [back to overview]Success at Day 180: Percent of Responders (Randomization Strata)
NCT00289991 (9) [back to overview]Survival: Percent of Subjects Who Died at or Before Day 180
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
NCT00356915 (4) [back to overview]Clinical and Mycological Cure of Target Toenail
NCT00528190 (1) [back to overview]The Primary Outcome Measure Will be the Number of Patients Who Experience a Respiratory Exacerbation Requiring Intravenous Antibiotics in the Two Treatment Groups Over the 24 Week Trial Treatment Period.
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Overall Survival (OS)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Duration of Response (DOR)
NCT00585195 (53) [back to overview]Probability of Participant Survival at Month 6
NCT00585195 (53) [back to overview]Itraconazole Cohort: Trough Plasma Concentration (Ctrough) of Crizotinib When Taken Alone and When Taken With Itraconazole
NCT00585195 (53) [back to overview]Itraconazole Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken Alone and When Taken With Itraconazole
NCT00585195 (53) [back to overview]Itraconazole Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib When Taken Alone and When Taken With Itraconazole
NCT00585195 (53) [back to overview]Dose-Escalation Cohort: Recommended Phase 2 Dose (RP2D) of Crizotinib
NCT00585195 (53) [back to overview]Dose-Escalation Cohort: Number of Participants With Dose-limiting Toxicities (DLT)
NCT00585195 (53) [back to overview]Dose-Escalation Cohort: Maximum Tolerated Dose (MTD) of Crizotinib
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Trough Concentration (Ctrough) of Crizotinib on Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Trough Concentration (Ctrough) of Crizotinib Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib on Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib on Cycle 1 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib Cycle 2 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 24 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Plasma Decay Half-Life (t1/2) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Cycle 1 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Cycle 1 Day 1
NCT00585195 (53) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Midazolam When Taken Alone or Taken With Crizotinib
NCT00585195 (53) [back to overview]Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib Alone and When Taken With Rifampin
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at End of Treatment
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 9 Day 1
NCT00585195 (53) [back to overview]Midazolam Interaction Cohort: Maximum Observed Plasma Concentration (Cmax) of Midazolam When Taken Alone or Taken With Crizotinib
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 6 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 4 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 30 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 27 Day 1
NCT00585195 (53) [back to overview]Probability of Participant Survival at Month 12
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 21 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 2 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 18 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 15 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 12 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Number of Participants With Treatment Emergent Adverse Events (TEAES) and Serious Adverse Events (SAEs)
NCT00585195 (53) [back to overview]RP2D Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken With Food
NCT00585195 (53) [back to overview]RP2D Cohort: Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Crizotinib When Taken With Food
NCT00585195 (53) [back to overview]Rifampin Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib Alone and When Taken With Rifampin
NCT00585195 (53) [back to overview]Rifampin Cohort: Ctrough of Crizotinib Alone and When Taken With Rifampin
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Time to Response (TTR)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Progression Free Survival (PFS)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Probability of Being Event Free at Month 6
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Percentage of Participants With Objective Response (OR)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Percentage of Participants With Disease Control at Week 8
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Percentage of Participants With Disease Control at Week 16
NCT00769600 (3) [back to overview]Progression Free Survival as Measured by Number of Days Without Disease Progression
NCT00769600 (3) [back to overview]RECIST Response
NCT00769600 (3) [back to overview]Overall Survival
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
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]"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)"
NCT00798135 (3) [back to overview]Pharmacokinetics (PK) of Oral Itraconazole
NCT00798135 (3) [back to overview]Time to Progression.
NCT00798135 (3) [back to overview]Number of Patients With Adverse Events Grade 3 or 4 That Are Related to Study Treatment
NCT00871728 (7) [back to overview]Percentage of Participants Showing Mycological Cure
NCT00871728 (7) [back to overview]Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 9
NCT00871728 (7) [back to overview]Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 5
NCT00871728 (7) [back to overview]Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 49
NCT00871728 (7) [back to overview]Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 25
NCT00871728 (7) [back to overview]Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 13
NCT00871728 (7) [back to overview]Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 37
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.
NCT00895453 (1) [back to overview]Candida Culture Free After Maintenance Therapy
NCT01021683 (9) [back to overview]Plasma Concentration of Itraconazole by Overall Success Rate (OSR) in Participants Who Received the Study Treatment
NCT01021683 (9) [back to overview]Percentage of Participants Achieving Plasma Level of Itraconazole at 1000 Nanogram Per Milliliter (ng/mL) or Higher After Administration of Study Treatment
NCT01021683 (9) [back to overview]Duration of Neutropenia
NCT01021683 (9) [back to overview]Percentage of Participants With Baseline Fungal Infection
NCT01021683 (9) [back to overview]Absolute Neutrophil Count (ANC)
NCT01021683 (9) [back to overview]Percentage of Participants With Deferevescence After Administration of Study Treatment
NCT01021683 (9) [back to overview]Percentage of Participants With Defervescence by Plasma Level of Itraconazole
NCT01021683 (9) [back to overview]Plasma Concentration of Itraconazole by Breakthrough Fungal Infection
NCT01021683 (9) [back to overview]Mean Time to Defervescence in Participants Who Received the Study Treatment
NCT01108094 (3) [back to overview]Change of GLI1 Tumor Biomarker
NCT01108094 (3) [back to overview]Ki67 Tumor Proliferation Biomarker
NCT01108094 (3) [back to overview]Tumor Size
NCT01450683 (1) [back to overview]Reduction in Serum PSA
NCT01772563 (3) [back to overview]Maximum Measured Concentration of Volasertib and Its Metabolite CD 10899 in Plasma (Cmax)
NCT01772563 (3) [back to overview]Area Under the Plasma Concentration-time Curve Over the Time Interval From 0 to Infinity (AUC0-∞) of Volasertib and Its Metabolite CD 10899
NCT01772563 (3) [back to overview]Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to the Last Quantifiable Drug Plasma Concentration After Dose Administration (AUC0-tz) of Volasertib and Its Metabolite CD 10899
NCT01787331 (6) [back to overview]Mean Percent Change in PSA Doubling Time
NCT01787331 (6) [back to overview]Median Time to Clinical Progression
NCT01787331 (6) [back to overview]Median Time to PSA Progression
NCT01787331 (6) [back to overview]Percentage of Participants With Treatment-related, Adverse Changes in Vital Signs
NCT01787331 (6) [back to overview]Number of Patients Who Achieve a Greater Than or Equal to 50% Decline in Serum Prostate Specific Antigen (PSA)
NCT01787331 (6) [back to overview]Percentage of Participants With Treatment-related, Clinical Laboratory Adverse Events
NCT01795937 (10) [back to overview]AUC0-∞ of Atorvastatin (Statins Part)
NCT01795937 (10) [back to overview]AUC0-∞ of Rosuvastatin (Statins Part)
NCT01795937 (10) [back to overview]AUC0-tz of Atorvastatin
NCT01795937 (10) [back to overview]AUC0-tz of Rosuvastatin
NCT01795937 (10) [back to overview]AUCτ,ss (Itraconazole Part)
NCT01795937 (10) [back to overview]AUCτ,ss of Faldaprevir (Statins Part)
NCT01795937 (10) [back to overview]Cmax of Atorvastatin (Statins Part)
NCT01795937 (10) [back to overview]Cmax of Rosuvastatin
NCT01795937 (10) [back to overview]Cmax,ss (Itraconazole Part)
NCT01795937 (10) [back to overview]Cmax,ss of Faldaprevir (Statins Part)
NCT01823289 (3) [back to overview]Number of Participants With Clinical Efficacy
NCT01823289 (3) [back to overview]Number of Participants With Comprehensive Efficacy
NCT01823289 (3) [back to overview]Number of Participants With Mycological Efficacy
NCT01929876 (10) [back to overview]Tmax of Itraconazole and Hydroxy-Itraconazole
NCT01929876 (10) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of Cobimetinib With and Without Itraconazole
NCT01929876 (10) [back to overview]Plasma Half-Life (t1/2) of Cobimetinib With and Without Itraconazole
NCT01929876 (10) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Cobimetinib With and Without Itraconazole
NCT01929876 (10) [back to overview]Cmax of Itraconazole and Hydroxy-Itraconazole
NCT01929876 (10) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-t)] of Cobimetinib With and Without Itraconazole
NCT01929876 (10) [back to overview]Area Under the Curve From Time Zero to 24 Hours [AUC (0-24)] of Itraconazole and Hydroxy-Itraconazole
NCT01929876 (10) [back to overview]Apparent Volume of Distribution (Vz/F) of Cobimetinib With and Without Itraconazole
NCT01929876 (10) [back to overview]Apparent Clearance (CL/F) of Cobimetinib With and Without Itraconazole
NCT01929876 (10) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - Inf)] of Cobimetinib With and Without Itraconazole
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)
NCT01974687 (81) [back to overview]Cmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants (Group C)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)
NCT01974687 (81) [back to overview]Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1,HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]Reduction in HCV RNA From Baseline on Day 8 Following Uprifosbuvir 50-450 mg for 7 Days in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]Percentage of Participants Who Experienced at Least One Treatment-emergent Grade 1, 2, 3, 4 or 5 Laboratory Abnormality
NCT01974687 (81) [back to overview]Maximum Reduction in log10 HCV RNA From Baseline - Normal Participants (From Groups B and C) vs. Mild Hepatic Impairment Participants (Group E)
NCT01974687 (81) [back to overview]Maximum Reduction in log10 HCV RNA From Baseline - Normal Participants (From Groups B and C) vs. Mild Hepatic Impairment Participants (Group E)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)
NCT01974687 (81) [back to overview]Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]Area Under the Plasma Drug Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]AUC0-t of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)
NCT01974687 (81) [back to overview]Cmax of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]Cmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]Cmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]Cmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)
NCT01974687 (81) [back to overview]Cumulative Urine Excretion of Unchanged M6 in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Cumulative Urine Excretion of Unchanged Uprifosbuvir in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Maximum (Peak) Observed Plasma Drug Concentration (Cmax) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Observed Terminal Half-Life (t1/2) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to a Treatment-emergent AE
NCT01974687 (81) [back to overview]Percentage of Participants Who Experienced a Treatment-emergent Dose-limiting Toxicity (DLT)
NCT01974687 (81) [back to overview]Percentage of Participants Who Experienced at Least One Treatment-emergent Adverse Event (AE)
NCT01974687 (81) [back to overview]Percentage of Participants Who Experienced at Least One Treatment-emergent Serious AE (SAE)
NCT01974687 (81) [back to overview]t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)
NCT01974687 (81) [back to overview]t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]t1/2 of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]t1/2 of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]t1/2 of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)
NCT01974687 (81) [back to overview]t1/2 of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants (Group C)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants, With Itraconazole (Group F)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]t1/2 of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-infected Participants (Group B)
NCT01974687 (81) [back to overview]Time to Maximum Plasma Concentration (Tmax) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Tmax of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]Tmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]Tmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)
NCT01974687 (81) [back to overview]Tmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Singe Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)
NCT01974687 (81) [back to overview]Tmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-infected Participants (Group B)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)
NCT01974687 (81) [back to overview]AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)
NCT02044393 (3) [back to overview]AUC0-infinity (Area Under the Concentration-time Curve of BI 691751 in Plasma and Whole Blood Over the Time Interval From 0 Extrapolated to Infinity)
NCT02044393 (3) [back to overview]AUC0-tz (Area Under the Concentration-time Curve of BI 691751 in Plasma and Whole Blood Over the Time Interval From 0 up to the Last Quantifiable Concentration)
NCT02044393 (3) [back to overview]Cmax (Maximum Measured Concentration of BI 691751 in Plasma and Whole Blood)
NCT02122770 (17) [back to overview]Part A: Terminal Phase Elimination Half-life (T1/2) for MLN4924
NCT02122770 (17) [back to overview]Number of Participants With TEAEs Related to Clinically Significant Laboratory Evaluation Findings
NCT02122770 (17) [back to overview]Number of Participants With Clinically Significant Change From Baseline in Body Weight Measurements
NCT02122770 (17) [back to overview]Number of Participants With TEAEs Related to Clinically Significant Vital Sign Findings
NCT02122770 (17) [back to overview]Part A AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for MLN4924 and MLN4924 + Fluconazole
NCT02122770 (17) [back to overview]Number of Participants Who Experience at Least 1 Treatment-emergent Adverse Event (TEAE) and Serious Adverse Event (SAE)
NCT02122770 (17) [back to overview]Part B: Percentage of Participants With Objective Response
NCT02122770 (17) [back to overview]Part B: Duration of Response
NCT02122770 (17) [back to overview]Part A AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for MLN4924 and MLN4924 + Itraconazole
NCT02122770 (17) [back to overview]Part A Cmax: Maximum Observed Plasma Concentration for MLN4924 and MLN4924 + Itraconazole
NCT02122770 (17) [back to overview]Part A Cmax: Maximum Observed Plasma Concentration for MLN4924 and MLN4924 + Fluconazole
NCT02122770 (17) [back to overview]Part A AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for MLN4924 and MLN4924 + Itraconazole
NCT02122770 (17) [back to overview]Part A: Volume of Distribution (Vz) for MLN4924
NCT02122770 (17) [back to overview]Part A AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for MLN4924 and MLN4924 + Fluconazole
NCT02122770 (17) [back to overview]Part A Tmax: Time to Reach the Cmax for MLN4924
NCT02122770 (17) [back to overview]Part A: Blood to Plasma (B/P) Concentration Ratio for MLN4924
NCT02122770 (17) [back to overview]Part A: Plasma Clearance (CLp) for MLN4924
NCT02157883 (12) [back to overview]AUC(0-t) of AZD9291
NCT02157883 (12) [back to overview]CL/F of AZD9291
NCT02157883 (12) [back to overview]AUC of AZ5104
NCT02157883 (12) [back to overview]AUC of AZ7550
NCT02157883 (12) [back to overview]AUC of AZD9291
NCT02157883 (12) [back to overview]AUC(0-120) of AZD9291
NCT02157883 (12) [back to overview]Cmax of AZ5104
NCT02157883 (12) [back to overview]Cmax of AZ7550
NCT02157883 (12) [back to overview]Cmax of AZD9291
NCT02157883 (12) [back to overview]t1/2 of AZD9291
NCT02157883 (12) [back to overview]Tmax of AZD9291
NCT02157883 (12) [back to overview]Vz/F of AZD9291
NCT02259010 (13) [back to overview]Number of Participants With Clinically Significant Change in Vital Sign Reported as AEs
NCT02259010 (13) [back to overview]Number of Participants With Abnormal Laboratory Values Reported as AEs
NCT02259010 (13) [back to overview]Cmax: Maximum Observed Plasma Concentration for Alisertib Metabolites M1 and M2 in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Alisertib Metabolites M1 and M2 in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]Tmax: Time to Reach Maximum Plasma Concentration of Alisertib in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]Number of Participants With Clinically Significant Change in Weight Reported as AEs
NCT02259010 (13) [back to overview]Cmax: Maximum Observed Concentration of Alisertib in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]CL/F: Oral Clearance of Alisertib in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]AUC∞: Area Under the Plasma Concentration Curve From Time 0 to Infinity of Alisertib in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]AUC(Last): Area Under the Plasma Concentration Curve From Time 0 to the Time of the Last Quantifiable Concentration of Alisertib in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]Terminal Phase Elimination Half-Life of Alisertib in Presence and Absence of Itraconazole in Part A
NCT02259010 (13) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT02259010 (13) [back to overview]Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Alisertib Metabolites M1 and M2 in Presence and Absence of Itraconazole in Part A
NCT02285283 (2) [back to overview]Number of Participants With Adverse Events During Time Frame of Taking Medication/Placebo
NCT02285283 (2) [back to overview]Number of Participants With Recurrence of Nasal Polyps Requiring Intervention
NCT02300259 (6) [back to overview]Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2623091
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of LY2623091
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of LY2623091
NCT02300259 (6) [back to overview]Pharmacokinetics: Maximum Drug Concentration (Cmax) of Simvastatin and Simvastatin Acid
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of Simvastatin and Simvastatin Acid
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Simvastatin and Simvastatin Acid
NCT02319148 (12) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
NCT02319148 (12) [back to overview]Number of Participants With Potentially Clinically Significant Vital Signs Findings
NCT02319148 (12) [back to overview]Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Findings
NCT02319148 (12) [back to overview]Number of Participants Who Used at Least 1 Concomitant Medication
NCT02319148 (12) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-00489791
NCT02319148 (12) [back to overview]Number of Participants With Laboratory Abnormalities Meeting the Criteria for Potential Clinical Concern
NCT02319148 (12) [back to overview]Maximum Observed Plasma Concentration (Cmax) of PF-00489791
NCT02319148 (12) [back to overview]Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of PF-00489791
NCT02319148 (12) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-00489791
NCT02319148 (12) [back to overview]Apparent Volume of Distribution (Vz/F) of PF-00489791
NCT02319148 (12) [back to overview]Apparent Oral Clearance (CL/F) of PF-00489791
NCT02319148 (12) [back to overview]Terminal Elimination Half-Life (t1/2) of PF-00489791
NCT02323334 (7) [back to overview]PD Biomarker: Cerebral Spinal Fluid (CSF) Minimum Amyloid-beta Peptide (A-beta) 1-40 Concentration
NCT02323334 (7) [back to overview]PD Biomarker: Change From Baseline in Cerebrospinal Fluid (CSF) Amyloid-beta Peptide (A-beta) 1-40 Concentration
NCT02323334 (7) [back to overview]Pharmacodynamic(PD) Biomarker: Plasma Minimum Amyloid-Beta Peptide (A-beta) 1-40 Concentration
NCT02323334 (7) [back to overview]Pharmacokinetics (PK): Maximum Drug Concentration (Cmax) of LY3202626
NCT02323334 (7) [back to overview]PK: Area Under the Concentration Time Curve (AUC) of LY3202626
NCT02323334 (7) [back to overview]PK: CSF Concentration of LY3202626
NCT02323334 (7) [back to overview]Number of Participants With One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration
NCT02341482 (13) [back to overview]Number of Participants With Significant Change in Physical Examination From Previous Examination
NCT02341482 (13) [back to overview]Area Under the Concentration-Time Profile From Time 0 to Time Tau, the Dosing Interval, Where Tau = 12 Hours (AUCtau) of PF-04958242
NCT02341482 (13) [back to overview]Apparent Oral Clearance (CL/F) of PF-04958242
NCT02341482 (13) [back to overview]Maximum Observed Plasma Concentration (Cmax) of PF-04958242
NCT02341482 (13) [back to overview]Number of Participants With Significant Change in Neurological Examination From Previous Examination
NCT02341482 (13) [back to overview]Predose Concentration (Ctrough) of PF-04958242
NCT02341482 (13) [back to overview]Number of Participants With Positive Response to Columbia-Suicide Severity Rating Scale (C-SSRS)
NCT02341482 (13) [back to overview]Number of Participants With Electrocardiogram Data Meeting Criteria of Potential Clinical Concern
NCT02341482 (13) [back to overview]Number of Participants With Abnormal Clinical Laboratory Measurements
NCT02341482 (13) [back to overview]Lowest Concentration Observed During the Dosing Interval (Cmin) of PF-04958242
NCT02341482 (13) [back to overview]Time for Cmax (Tmax) of PF-04958242
NCT02341482 (13) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT02341482 (13) [back to overview]Number of Participants With Vital Signs Data Meeting Criteria of Potential Clinical Concern
NCT02357836 (8) [back to overview]Mean Percent Change in Angiogenic Cytokines From Baseline
NCT02357836 (8) [back to overview]Mean Percent Change in Other Plasma Cytokine From Baseline to Post-Treatment
NCT02357836 (8) [back to overview]Change in Skin Biopsy PTCH1 Levels From Baseline
NCT02357836 (8) [back to overview]Itraconazole Levels in Post-treatment Serum
NCT02357836 (8) [back to overview]Changes in Tumor Tissue Microvessel Density [MVD] From Baseline
NCT02357836 (8) [back to overview]Changes in Perfusion (Ktrans)
NCT02357836 (8) [back to overview]Itraconazole Levels in Tumor Tissue
NCT02357836 (8) [back to overview]Change in Skin Biopsy GLI1 Levels From Baseline
NCT02370615 (17) [back to overview]Cumulative Urinary Excretion Ratio of TAK 272F and TAK 272-M-I From 0 to 72 Hours Postdose in Cohort 1
NCT02370615 (17) [back to overview]Cmax: Maximum Observed Plasma Concentration for TAK 272F and TAK 272-Metabolite (M-I) in Cohort 1
NCT02370615 (17) [back to overview]Cmax: Maximum Observed Plasma Concentration for Midazolam and 1'Hydroxymidazolam in Cohort 2
NCT02370615 (17) [back to overview]AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK 272F and TAK 272-M-I in Cohort 1
NCT02370615 (17) [back to overview]Number of Participants With Clinically Significant Change From Baseline in Continuous Pulse Oximetry (SpO2) in Cohort 2
NCT02370615 (17) [back to overview]AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Midazolam and 1'Hydroxymidazolam in Cohort 2
NCT02370615 (17) [back to overview]Urinary Excretion Ratio of Digoxin From 0 to 48 Hours Postdose in Cohort 2
NCT02370615 (17) [back to overview]Number of Participants With TEAEs Related to Vital Signs
NCT02370615 (17) [back to overview]AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK 272F and TAK 272-M-I in Cohort 1
NCT02370615 (17) [back to overview]AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Midazolam and 1'Hydroxymidazolam in Cohort 2
NCT02370615 (17) [back to overview]Number of Participants With TEAEs Related to Body Weight
NCT02370615 (17) [back to overview]Number of Participants Who Had Clinically Significant Changes From Baseline in 12-lead Electrocardiograms
NCT02370615 (17) [back to overview]Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
NCT02370615 (17) [back to overview]Cmax: Maximum Observed Plasma Concentration for Digoxin in Cohort 2
NCT02370615 (17) [back to overview]AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Digoxin in Cohort 2
NCT02370615 (17) [back to overview]AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Digoxin in Cohort 2
NCT02370615 (17) [back to overview]Number of Participants With TEAEs Categorized Into Investigations System Organ Class (SOC) Related to Chemistry, Hematology or Urinalysis
NCT02513446 (3) [back to overview]Maximum Concentration of BI 1026706 (Cmax)
NCT02513446 (3) [back to overview]Area Under the Curve of BI 1026706 From 0 to the Last Quantifiable Data Point (AUC0-tz)
NCT02513446 (3) [back to overview]Area Under the Curve of BI 1026706 From 0 Extrapolated to Infinity (AUC0-inf)
NCT02653872 (9) [back to overview]Assessment of the Tmax of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.
NCT02653872 (9) [back to overview]Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC).
NCT02653872 (9) [back to overview]Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Observed Maximum Plasma Concentration (Cmax).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration-time Curve (t½λz).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Total Body Clearance After Extravascular Administration Estimated as Dose Divided by AUC (CL/F).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Volume of Distribution During the Terminal Phase After Extravascular Administration (Vz/F).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC [0-t]).
NCT02653872 (9) [back to overview]Pharmacokinetics (PK) of AZD7986 by Assessment of the Time to Reach Maximum Plasma Concentration (Tmax)
NCT02653872 (9) [back to overview]Assessment of the Area Under the Plasma Concentration-curve Over the Dosing Interval (AUC [0 - τ]) of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.
NCT02989389 (7) [back to overview]Part B Pharmacodynamics (PD): Change From Baseline in Cerebrospinal Fluid (CSF) Amyloid Beta (Aβ)₁-₄₀ and Aβ₁-₄₂
NCT02989389 (7) [back to overview]Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of LY3323795 in Plasma
NCT02989389 (7) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Tlast (AUC[0-tlast]) of LY3323795 in Plasma
NCT02989389 (7) [back to overview]Number of Participants With One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration
NCT02989389 (7) [back to overview]Part B Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Tlast (AUC[0-tlast]) of LY3323795 in Cerebrospinal Fluid (CSF)
NCT02989389 (7) [back to overview]Pharmacodynamics (PD): Change From Baseline in Plasma Amyloid Beta (Aβ)₁-₄₀ and Aβ₁-₄₂
NCT02989389 (7) [back to overview]Part B Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of LY3323795 in Cerebrospinal Fluid (CSF)
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC0-inf) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Number of Participants With Clinically Significant Abnormalities in Electrocardiogram (ECG)
NCT03077607 (19) [back to overview]Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Number of Participants With Clinically Significant Abnormalities in Vital Signs
NCT03077607 (19) [back to overview]Number of Participants With Clinically Significant Physical Examination Findings
NCT03077607 (19) [back to overview]Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT03077607 (19) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Profile From Time Zero to Extrapolated Infinity (AUC0-inf) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Number of Participants With Clinical Significance Abnormalities in Laboratory Parameters
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Rifampin
NCT03161405 (3) [back to overview]AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-906
NCT03161405 (3) [back to overview]AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-906
NCT03161405 (3) [back to overview]Cmax: Maximum Observed Plasma Concentration for TAK-906
NCT03173170 (2) [back to overview]AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-954
NCT03173170 (2) [back to overview]Cmax: Maximum Observed Plasma Concentration for TAK-954
NCT03383692 (11) [back to overview]Best Objective Response as Confirmed By The Investigator's Assessment in Participants With HER2-Expressing Advanced Solid Malignant Tumors
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve Following Treatment With DS-8201a and Ritonavir - Cohort 1
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve Following Treatment With DS-8201a and Itraconazole - Cohort 2
NCT03383692 (11) [back to overview]Objective Response Rate as Confirmed By The Investigator's Assessment in Participants With HER2-Expressing Advanced Solid Malignant Tumors
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) Following Treatment With DS-8201a and Ritonavir - Cohort 1
NCT03383692 (11) [back to overview]Objective Response Ratio (ORR) as Confirmed By The Investigator's Assessment in Participants With HER2-Expressing Advanced Solid Malignant Tumors
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) of MAAA-1181a Following Treatment With DS-8201a and Itraconazole - Cohort 2
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) For MAAA-1181a Following Treatment With DS-8201a and Ritonavir - Cohort 1
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) Following Treatment With DS-8201a and Itraconazole - Cohort 2
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve of MAAA-1181a Following Treatment With DS-8201a and Ritonavir - Cohort 1
NCT03383692 (11) [back to overview]Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve of MAAA-1181a Following Treatment With DS-8201a and Itraconazole - Cohort 2
NCT03398421 (52) [back to overview]Change From Baseline of Clinical Chemistry Parameters When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered: Alkaline Phosphate, Alanine Aminotransferase (ALT) and Aspartate Aminotransferase (AST)
NCT03398421 (52) [back to overview]Change From Baseline in Temperature When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Respiratory Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose
NCT03398421 (52) [back to overview]Change From Baseline in SBP and DBP When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose
NCT03398421 (52) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Temperature When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose
NCT03398421 (52) [back to overview]Change From Baseline of Clinical Chemistry Parameters When Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose: Bilirubin, Direct Bilirubin and Creatinine
NCT03398421 (52) [back to overview]Change From Baseline of Clinical Chemistry Parameters When Nemiralisib 100 mcg When Co-administered With Itraconazole 200 mg Repeated Dose: Alkaline Phosphate, ALT and AST
NCT03398421 (52) [back to overview]Change From Baseline of Clinical Chemistry Parameters When Nemiralisib 100 mcg When Co-administered With Itraconazole 200 mg Repeated Dose: Calcium, Glucose, Potassium and Sodium
NCT03398421 (52) [back to overview]Number of Participants With Abnormal Urinalysis Parameter
NCT03398421 (52) [back to overview]Change From Baseline of Clinical Chemistry Parameters When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered: Calcium, Glucose, Potassium and Sodium
NCT03398421 (52) [back to overview]Change From Baseline of Clinical Chemistry Parameters When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered:Bilirubin, Direct Bilirubin and Creatinine
NCT03398421 (52) [back to overview]Change From Baseline of Total Protein When Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose
NCT03398421 (52) [back to overview]Cmax of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2
NCT03398421 (52) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Number of Participants With Abnormal Microscopic Examinations: Casts, Epithelial Cells, Erythrocytes and Leukocytes
NCT03398421 (52) [back to overview]Number of Participants With Abnormal Urinalysis Parameter
NCT03398421 (52) [back to overview]Area Under the Concentration-time Curve From Time Zero (Pre-dose) Extrapolated to Infinite Time (AUC[0-inf]) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT03398421 (52) [back to overview]Number of Participants With Urine Potential of Hydrogen (pH) at Indicated Time Points
NCT03398421 (52) [back to overview]Number of Participants With Urine Potential of Hydrogen (pH) at Indicated Time Points
NCT03398421 (52) [back to overview]Specific Gravity at Indicated Time Points
NCT03398421 (52) [back to overview]Specific Gravity at Indicated Time Points
NCT03398421 (52) [back to overview]T1/2 of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2
NCT03398421 (52) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Tmax of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2
NCT03398421 (52) [back to overview]Area Under the Concentration-time Curve From Time Zero (Pre-dose) Extrapolated to Infinite Time (AUC[0-inf]) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Apparent Terminal Half-life (t1/2) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Apparent Terminal Half-life (t1/2) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings
NCT03398421 (52) [back to overview]Change From Baseline of Total Protein When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Reticulocyte Percentage When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg
NCT03398421 (52) [back to overview]Area Under the Concentration-time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Area Under the Concentration-time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Nemiralisib in Plasma
NCT03398421 (52) [back to overview]Change From Baseline in Reticulocyte Percentage When Single Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]AUC(0-inf) of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2
NCT03398421 (52) [back to overview]AUC(0-t) of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2
NCT03398421 (52) [back to overview]Change From Baseline in Hematology Parameters When Single Oral Dose of Nemiralisib 100 mcg Administered: Lymphocytes, Neutrophils, Platelets, Basophils, Eosinophils, Monocytes, Erythrocytes and White Blood Cells (WBC)
NCT03398421 (52) [back to overview]Change From Baseline in Hematology Parameters When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose: Lymphocytes, Neutrophils, Platelets, Basophils, Eosinophils, Monocytes, Erythrocytes and WBC
NCT03398421 (52) [back to overview]Change From Baseline in Pulse Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose
NCT03398421 (52) [back to overview]Change From Baseline in Respiratory Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Pulse Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in MCV When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg
NCT03398421 (52) [back to overview]Change From Baseline in MCH When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg
NCT03398421 (52) [back to overview]Change From Baseline in Hemoglobin When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg
NCT03398421 (52) [back to overview]Change From Baseline in Hemoglobin When Single Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Hematocrit When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg
NCT03398421 (52) [back to overview]Change From Baseline in Hematocrit When Single Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Erythrocyte Mean Corpuscular Volume (MCV) When Single Oral Dose of Nemiralisib 100 mcg Administered
NCT03398421 (52) [back to overview]Change From Baseline in Erythrocyte Mean Corpuscular Hemoglobin (MCH) When Single Oral Dose of Nemiralisib 100 mcg Administered
NCT03530995 (5) [back to overview]Pharmacokinetics: AUC(0-24) of KD025m1 for Part 1 and for Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025m1 in Part 1
NCT03530995 (5) [back to overview]Pharmacokinetics: AUC(0-inf) and AUC(0-24) of KD025 and KD025 m2 for Subject in Part 1 and Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025 and KD025m2 in Part 1
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025, KD025m1, and KD025m2 in Part 2
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
NCT03579719 (14) [back to overview]Maximum Plasma Concentration (Cmax) for M3 Metabolite
NCT03579719 (14) [back to overview]Maximum Plasma Concentration (Cmax) for M2 Metabolite (as Applicable)
NCT03579719 (14) [back to overview]Trough Plasma Concentration (Ctrough) for M3 Metabolite
NCT03579719 (14) [back to overview]Trough Plasma Concentration (Ctrough) for M2 Metabolite (as Applicable)
NCT03579719 (14) [back to overview]Trough Plasma Concentration (Ctrough) for Balovaptan
NCT03579719 (14) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) for M3 Metabolite
NCT03579719 (14) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) for M2 Metabolite (as Applicable)
NCT03579719 (14) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) for Balovaptan
NCT03579719 (14) [back to overview]Maximum Plasma Concentration (Cmax) for Balovaptan
NCT03579719 (14) [back to overview]Area Under the Concentration Vs Time Curve Over the Dosing Interval (AUC0-tau) for M3 Metabolite
NCT03579719 (14) [back to overview]Area Under the Concentration Vs Time Curve Over the Dosing Interval (AUC0-tau) for M2 Metabolite (as Applicable)
NCT03579719 (14) [back to overview]Area Under the Concentration Vs Time Curve Over the Dosing Interval (AUC0-tau) for Balovaptan
NCT03579719 (14) [back to overview]Percentage of Participants With Adverse Events
NCT03579719 (14) [back to overview]Time to Steady State for Balovaptan
NCT03722173 (3) [back to overview]Maximum Measured Concentration of BI 894416 in Plasma (Cmax)
NCT03722173 (3) [back to overview]Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)
NCT03722173 (3) [back to overview]Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
NCT03774576 (4) [back to overview]Change in Suicide Risk as Assessed Using the Columbia Suicide Severity Rating Scale (C-SSRS)
NCT03774576 (4) [back to overview]Cmax of Itraconazole in Plasma
NCT03774576 (4) [back to overview]Maximum Concentration (Cmax) of RO7017773 in Plasma
NCT03774576 (4) [back to overview]Percentage of Participants With Adverse Events (AEs)
NCT03782987 (3) [back to overview]Area Under the Concentration-time Curve of the BI 730357 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
NCT03782987 (3) [back to overview]Maximum Measured Concentration of the BI 730357 in Plasma (Cmax)
NCT03782987 (3) [back to overview]Area Under the Concentration-time Curve of the BI 730357 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)
NCT03928327 (7) [back to overview]Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32914
NCT03928327 (7) [back to overview]Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32960
NCT03928327 (7) [back to overview]Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of TAK-788
NCT03928327 (7) [back to overview]Treatment B Vs Treatment A (Part 1), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914
NCT03928327 (7) [back to overview]Treatment B vs Treatment A (Part 1), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914
NCT03928327 (7) [back to overview]Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914
NCT03928327 (7) [back to overview]Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914
NCT03994211 (20) [back to overview]Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part B
NCT03994211 (20) [back to overview]Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part A
NCT03994211 (20) [back to overview]Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part B
NCT03994211 (20) [back to overview]Number of Participants With Clinically Significant Abnormalities in Laboratory Assessments, Vital Signs, ECG Parameters and Physical Examinations
NCT03994211 (20) [back to overview]Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT04035187 (2) [back to overview]Cmax
NCT04035187 (2) [back to overview]AUC
NCT04604795 (84) [back to overview]Part C: Time to Maximum Observed Plasma Drug Concentration (Tmax) Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: t1/2 of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ
NCT04604795 (84) [back to overview]Part C: t1/2 of GSK3915393 Following IV Dose of GSK3915393+ITZ
NCT04604795 (84) [back to overview]Part C: Number of Participants With Treatment-related AEs Following Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With Abnormal Physical Examination Findings Following Administration of GSK3915393
NCT04604795 (84) [back to overview]Part C: Maximum Observed Plasma Drug Concentration (Cmax) Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: Fraction of Drug Escaping Hepatic Metabolism (FH) Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: Fraction of Drug Escaping Gut Metabolism (FG) Following Oral Administration of GSK3915393+Water
NCT04604795 (84) [back to overview]Part C: Fraction of Drug Absorbed (FA) Following Oral Administration of GSK3915393+Water
NCT04604795 (84) [back to overview]Part C: FH Following IV Administration of GSK3915393+ITZ
NCT04604795 (84) [back to overview]Part C: Cmax of GSK3915393 Following IV Dose of GSK3915393+ITZ
NCT04604795 (84) [back to overview]Part C: Cmax Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ
NCT04604795 (84) [back to overview]Part C: AUCLST(0-24) of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ
NCT04604795 (84) [back to overview]Part C: AUCLST(0-24) of GSK3915393 Following IV Dose of GSK3915393+ITZ
NCT04604795 (84) [back to overview]Part C: AUC(0-inf) of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ
NCT04604795 (84) [back to overview]Part C: AUC(0-inf) of GSK3915393 Following IV Dose of GSK3915393+ITZ
NCT04604795 (84) [back to overview]Part C: AUC From Time Zero to Infinity (AUC[0-inf]) Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: Area Under Curve up to the Last Measurable Concentration (AUCLST[0-10]) Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: Apparent Terminal Half-life (t1/2) of GSK3915393 Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Trough Concentration (Ctau) Following Dose of 20 mg BID and 80 mg BID of GSK3915393 on Day 14
NCT04604795 (84) [back to overview]Part B: Trough Concentration (Ctau) Following Dose of 160 mg of GSK3915393 on Day 14
NCT04604795 (84) [back to overview]Part B: Number of Participants With Treatment-related AEs
NCT04604795 (84) [back to overview]Part B: Number of Participants With Abnormal Physical Examination Findings Following Administration of Repeat Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Volume of Distribution (Vd) Following Single IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Tmax Following Single Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Tmax Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: t1/2 Following Single IV Dose of GSK3915393 100 mcg IV
NCT04604795 (84) [back to overview]Part A: Product of Fraction of Drug Absorbed and Fraction of Drug Escaping Gut Metabolism (FA*FG) Following Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Treatment-related AEs Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Abnormal Physical Examination Findings Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Abnormal Physical Examination Findings Following Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Fraction of Drug Escaping Hepatic Metabolism (FH) Following Single Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Cmax Following Single Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Cmax Following Single IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Clearance (CL) Following Single IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: AUCLST(0-24) Following Single Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: AUC(0-inf) Following Single Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: AUC(0-inf) Following Single IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Absolute Bioavailability (F) Following Single Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Tmax(0-10) Following Dosing of GSK3915393 on Days 1 and 14
NCT04604795 (84) [back to overview]Part A: AUCLST(0-6) Following Single IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Tmax(0-10) Following First Dosing of GSK3915393 on Days 3, 5 and 7 (for Food-effect Assessment)
NCT04604795 (84) [back to overview]Part B: Tmax(10-24) Following Dose 160 mg (QD) of GSK3915393
NCT04604795 (84) [back to overview]Part B: Tmax(10-24) Following Repeat Dose 20 mg BID and 80 mg BID of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With All Non-serious AEs and SAEs
NCT04604795 (84) [back to overview]Part C: Number of Participants With Worst Case Chemistry Results: Creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With Worst Case Chemistry Results: Urea by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With Worst Case Post-Baseline Abnormal ECG Findings Following Administration of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393
NCT04604795 (84) [back to overview]Part B: AUCLST(0-10) Following Dosing of GSK3915393
NCT04604795 (84) [back to overview]Part B: AUC(10-24) Following Repeat Dose of GSK3915393 160 mg (QD)
NCT04604795 (84) [back to overview]Part B: AUC(10-24) Following Repeat Dose 20 mg BID and 80 mg BID of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Post-Baseline Abnormal Electrocardiogram (ECG) Findings Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Post-Baseline Abnormal ECG Findings Following Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part C: Number of Participants With Worst Case Chemistry Results by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Chemistry Results-urea by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Chemistry Results-urea by PCI Criteria Post-Baseline Relative to Baseline Following Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Chemistry Results-creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Chemistry Results-creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Administration Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Chemistry Results by Potential Clinical Importance (PCI) Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part B: Cmax(10-24) Following Dose 160 mg (QD) of GSK3915393
NCT04604795 (84) [back to overview]Part B: Cmax(10-24) Following Repeat Dose 20 mg and 80 mg of GSK3915393
NCT04604795 (84) [back to overview]Part B: Number of Participants With All Non-serious AEs and SAEs
NCT04604795 (84) [back to overview]Part B: Number of Participants With Worst Case Chemistry Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Repeat Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Number of Participants With Worst Case Chemistry Results-creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Repeat Oral Dose
NCT04604795 (84) [back to overview]Part A: Number of Participants With Worst Case Chemistry Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part A: Number of Participants With All Non-serious AEs and SAEs Following Administration Administration of IV Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: AUCLST(0-10) Following First Dosing of GSK3915393 on Days 3, 5 and 7 (for Food-effect Assessment)
NCT04604795 (84) [back to overview]Part B: Number of Participants With Worst Case Chemistry Results-urea by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Repeat Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Repeat Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Number of Participants With Worst Case Post-Baseline Abnormal ECG Findings Following Repeat Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following Repeat Oral Dose of GSK3915393
NCT04604795 (84) [back to overview]Part B: Cmax(0-10) Following First Dosing of GSK3915393 on Days 3, 5 and 7 (for Food-effect Assessment)
NCT04604795 (84) [back to overview]Part B: Cmax(0-10) Following Dosing of GSK3915393 on Days 1 and 14
NCT04604795 (84) [back to overview]Part B: AUCLST(0-24) Following Repeat Dose 20 mg BID and 80 mg BID of GSK3915393
NCT04604795 (84) [back to overview]Part B: AUCLST(0-24) Following Dose of GSK3915393 160 mg (QD)
NCT04604795 (84) [back to overview]Part A: Number of Participants With All Non-serious Adverse Events (AEs) and Serious AEs (SAEs) Following Administration of Oral Dose
NCT04604795 (84) [back to overview]Part C: Tmax of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ
NCT04604795 (84) [back to overview]Part C: Tmax of GSK3915393 Following IV Dose of GSK3915393+ITZ
NCT04962022 (16) [back to overview]Apparent Clearance(CL/F) of PF-07321332
NCT04962022 (16) [back to overview]Apparent Volume of Distribution (Vz/F) of PF-07321332
NCT04962022 (16) [back to overview]Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration(AUClast) of PF-07321332
NCT04962022 (16) [back to overview]Area Under the Plasma Concentration-time Profile From Time Zero to Time Tau (τ), Where Tau=12-hour Dosing Interval(AUCtau) for PF-07321332
NCT04962022 (16) [back to overview]Maximum Observed Concentration (Cmax) of PF-07321332
NCT04962022 (16) [back to overview]Terminal Half-life(t1/2) of PF-07321332
NCT04962022 (16) [back to overview]Time for Cmax (Tmax) for PF-07321332
NCT04962022 (16) [back to overview]Change From Baseline in Vital Signs Data - Supine Diastolic Blood Pressure
NCT04962022 (16) [back to overview]Change From Baseline in Vital Signs Data - Supine Diastolic Blood Pressure
NCT04962022 (16) [back to overview]Change From Baseline in Vital Signs Data - Supine Pulse Rate
NCT04962022 (16) [back to overview]Change From Baseline in Vital Signs Data - Supine Systolic Blood Pressure
NCT04962022 (16) [back to overview]Change From Baseline in Vital Signs Data - Supine Systolic Blood Pressure
NCT04962022 (16) [back to overview]Number of Participants With Clinically Significant 12-lead Electrocardiogram (ECG) Findings
NCT04962022 (16) [back to overview]Number of Participants With Laboratory Abnormalities (Without Regard to Baseline Abnormality)
NCT04962022 (16) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT04962022 (16) [back to overview]Change From Baseline in Vital Signs Data - Supine Pulse Rate
NCT05064449 (13) [back to overview]Part 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Soticlestat When Administered Alone and With Itraconazole
NCT05064449 (13) [back to overview]Parts 1 and 2: Number of Participants With Clinically Significant Abnormal Values for Electrocardiogram (ECG)
NCT05064449 (13) [back to overview]Parts 1 and 2: Number of Participants With Clinically Significant Abnormal Values for Laboratory Evaluations
NCT05064449 (13) [back to overview]Parts 1 and 2: Number of Participants With Clinically Significant Abnormal Values for Vital Signs
NCT05064449 (13) [back to overview]Parts 1 and 2: Number of Participants With Suicidal Ideation or Suicidal Behavior as Measured Using Columbia-Suicide Severity Rating Scale (C-SSRS)
NCT05064449 (13) [back to overview]Part 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Soticlestat When Administered Alone and With Itraconazole
NCT05064449 (13) [back to overview]Part 1, Cmax: Maximum Observed Plasma Concentration for Soticlestat When Administered Alone and With Itraconazole
NCT05064449 (13) [back to overview]Part 1, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Soticlestat When Administered Alone and With Itraconazole
NCT05064449 (13) [back to overview]Part 2, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Soticlestat When Administered Alone and With Mefenamic Acid
NCT05064449 (13) [back to overview]Part 2, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Soticlestat When Administered Alone and With Mefenamic Acid
NCT05064449 (13) [back to overview]Part 2, Cmax: Maximum Observed Plasma Concentration for Soticlestat When Administered Alone and With Mefenamic Acid
NCT05064449 (13) [back to overview]Part 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Soticlestat When Administered Alone and With Mefenamic Acid
NCT05064449 (13) [back to overview]Parts 1 and 2: Number of Participants Reported One or More Treatment-emergent Adverse Event (TEAE)

Summary of CGP62221 Plasma Concentration for 100 mg Bid Arm (E1)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (0h, 4h, 24 h), 3 (0h), 8 (0h); cycle 2: days 1 (0h); cycle 3: day 1 (0h); cycle 4: day 1 (0h); cycle 5: day 1 (0h) and cycle 6: day 1 (0h)

Interventionng/ml (Mean)
Cycle 1, day 1 (0h) (n=39)Cycle 1, day 1 (4h) (n=34)Cycle 1, day 1 (24h) (n=36)Cycle 1, day 3 (0h) (n=29)Cycle 1, day 8 (0h) (n=24)Cycle 2, day 1 (0h) (n=15)Cycle 3, day 2 (0h) (n=6)Cycle 4, day 1 (0h) (n=6)Cycle 5, day 1 (0h) (n4)Cycle 6, day 1 (0h) (n=4)
FLT3 Mutated and Wild Type PKC412 200 mg/Day0.000471.6351134.7641944.0692898.7081828.6671258.3331602.9501111.2501662.500

[back to top]

Summary of CGP52421 Plasma Concentration for 50 mg Bid Arm (E1)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (0h, 4h, 24 h), 3 (0h), 8 (0h); cycle 2: days 1 (0h); cycle 3: day 1 (0h); cycle 4: day 1 (0h)

Interventionng/ml (Mean)
Cycle 1, day 1 (0h) (n=41)Cycle 1, day 1 (4h) (n=38)Cycle 1, day 1 (24h) (n=39)Day 1, day 3 (0h) (n=34)Cycle 1, day 8 (0h) (n=30)Cycle 2, day 1 (0h) (n=22)Cycle 3, day 1 (0h) (n=12)Cycle 4, day 1 (0h) (n=4)
FLT3 Mutated and Wild Type PKC412 100 mg/Day Arms Combined0.000203.013436.2821188.3592840.8336467.5918175.0006205.000

[back to top]

Summary of CGP62221 Concentration (E2)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1, 2 (24 hr post day 1), 3, 8, 15, 16 (24 hr post day 15), 17, 22; Cycle 2: days 1, 2 (24 hr post day 1), 3, 8, 15

Interventionng/ml (Median)
Cycle 1, day 1 (n=7)Cycle 1, day 2 (24 hr post day 1) (n=12)Cycle 1, day 3 (n=12)Cycle 1, day 8 (n=8)Cycle 1, day 15 (n=6)Cycle 1, day 16 (24 hr post day 15) (n=6)Cycle 1, day 17 (n=5)Cycle 1, day 22 (n=5)Cycle 2, day 1 (n=4)Cycle 2, day 2 (24 hr post day 1) (n=4)Cycle 2, day 3 (n=4)Cycle 2, day 8 (n=4)Cycle 2, day 15 (n=3)
FLT3 Mutated and Wild Type PKC412 Dose Escalation Combined01320.02750.02380.01505.01425.01480.01520.01545.01945.02070.02030.01740.0

[back to top]

Summary of CGP62221 Plasma Concentration (Core)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (24 hour), 3, 8; Cycle 2: day 1,

Interventionng/ml (Mean)
Cycle 1, day 1 (24 hour) (n=10)Cycle 1, day 3 (n=7)Cycle 1, day 8 (n=9)Cycle 2, day 1 (n=6)
PKC412 in FLT3 Mutated Participants (Core)1636.003143.714873.332816.67

[back to top]

Summary of CGP62221 Plasma Concentration for 50 mg Bid Arm (E1)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (0h, 4h, 24 h), 3 (0h), 8 (0h); cycle 2: days 1 (0h); cycle 3: day 1 (0h); cycle 4: day 1 (0h)

Interventionng/ml (Mean)
Cycle 1, day 1 (0h) (n=44)Cycle 1, day 1 (4h) (n=38)Cycle 1, day 1 (24h) (n=39)Cycle 1, day 3 (0h) (n=34)Cycle 1, day 8 (0h) (n=30)Cycle 2, day 1 (0h) (n=22)Cycle 3, day 1 (0h) (n=12)Cycle 4, day 1 (0h) (n=4)
FLT3 Mutated and Wild Type PKC412 100 mg/Day Arms Combined0.000367.079808.1821400.4762868.9331930.0001971.5001207.500

[back to top]

Summary of Midostaurin Concentration in the PKC412 Dose Escalation Arms(E2)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1, 2 (24 hr post day 1), 3, 8, 15, 16 (24 hr post day 15), 17, 22; Cycle 2: days 1, 2 (24 hr post day 1), 3, 8, 15

Interventionng/ml (Median)
Cycle 1, day 1 (=7)Cycle 1, day 2 (24 hours post day 1) (n=12)Cycle 1, day 3 (n=12)Cycle 1, day 8 (n=8)Cycle 1, day 15 (n=6)Cycle 1, day 16 (24 hr post day 15) (n=6)Cycle 1, day 17 (n=5)Cycle 1, day 22 (n=5)Cycle 2, day 1 (n=4)Cycle 2, day 2 (24 hr post day 1) (n=4)Cycle 2, day3 (n=4)Cycle 2, day 8 (n=4)Cycle 2, day 15 (n=3)
FLT3 Mutated and Wild Type PKC412 Dose Escalation Combined02565.03100.01640.0744.5836.0800.01410.0772.01141.01295.01210.0834.0

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) for CGP52421 in the PKC412 + Itraconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionh*ng/ml (Mean)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined38899.8441035.5044447.05

[back to top]

Summary of Midostaurin Plasma Concentration (Core)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (24 hour), 3, 8; Cycle 2: day 1,

Interventionng/ml (Mean)
Cycle 1, day 1(24 hour) (n=10)Cycle 1, day 3 (n=7)Cycle 1, day 8 (n=9)Cycle 2, day 1 (n=6)
PKC412 in FLT3 Mutated Participants (Core)3801.07152.865154.441873.17

[back to top]

Summary of PKC412 Plasma Concentration for 50 mg Twice Daily (Bid) Arm (E1)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (0h, 4h, 24 h), 3 (0h), 8 (0h); cycle 2: days 1 (0h); cycle 3: day 1 (0h); cycle 4: day 1 (0h)

Interventionng/ml (Mean)
Cycle 1, day 1 (0h) (n=43)Cycle 1, day 1 (4h) (n=38)Cycle 1, day 1 (24h) (n=39)Cycle 1, day 3 (0h) (n=34)Cycle 1, day 8 (0h) (n=30)Cycle 2, day 1 (0h) (n=22)Cycle 3, day 1 (0h) (n=12)Cycle 4, day 1 (0h) (n=4)
FLT3 Mutated and Wild Type PKC412 100 mg/Day Arms Combined0.0001198.0001735.9742585.4713576.4671756.5002038.417820.750

[back to top]

Terminal Elimination Half-life (T1/2) for PKC412 in the PKC + Itrconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21 and 22

Interventionhour (Mean)
Cycle 1, day 21 (n=6)Cycle 1, day 22 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined18.1313.23

[back to top]

Time to Reach the Maximum Concentration After Drug Administration (Tmax) for CGP52421 in the PKC412 + Itraconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionhour (Median)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined3.52.12.2

[back to top]

Time to Reach the Maximum Concentration After Drug Administration (Tmax) for CGP62221 in the PKC412 + Itraconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionhour (Median)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined3.72.33.3

[back to top]

Time to Reach the Maximum Concentration After Drug Administration (Tmax) for PKC412 in the PKC412 + Itraconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionhour (Median)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined1.61.92.2

[back to top]

Duration of Best Clinical Response (E1)

Duration of best clinical response was measured from the time that the measurement criteria were met for CR, PR, MR (with or without blast reduction) or BR until the first date that recurrent disease was documented (event) or until the date of last follow up. (NCT00045942)
Timeframe: from date of FPFV, 27-Mar-2003, to date of LPLV, 06-Sep-2004

Interventiondays (Median)
FLT3 Mutated PKC412 100 mg/Day (E1)57.0
FLT3 Mutated PKC412 200 mg/Day (E1)29.0
FLT3 Wild Type PKC412 100 mg/Day (E1)56.0
FLT3 Wild Type PKC412 200 mg/Day (E1)58.0

[back to top]

Event-free Survival (E1)

Event-free survival was defined as the time from date of start of treatment to the date of death from any cause, treatment failure or relapse (NCT00045942)
Timeframe: from date of FPFV, 27-Mar-2003, to date of LPLV, 06-Sep-2004

Interventiondays (Median)
FLT3 Mutated PKC412 100 mg/Day (E1)60.0
FLT3 Mutated PKC412 200 mg/Day (E1)50.0
FLT3 Wild Type PKC412 100 mg/Day (E1)58.0
FLT3 Wild Type PKC412 200 mg/Day (E1)1.0

[back to top]

Number of Participants With Best Clinical Response (Core)

Best clinical response was defined as complete response (CR) or partial response (PR), according to NCI definitions for AML and the guidelines for defining responses in MDS. (NCT00045942)
Timeframe: from date of first patient first visit (FPFV), 29-Jan-2002, to date of last participant last visit (LPLV), 04-Sep-2003

InterventionParticipants (Number)
PKC412 in FLT3 Mutated Participants (Core)0

[back to top]

Overall Survival (E2)

OS was measured from the date of the first dose of treatment to the date of death from any cause or the last date the patient was known to be alive (censored observation) (NCT00045942)
Timeframe: date of FPFV, 21-Aug-2003, to date of LPLV, 27-Mar-2008

Interventiondays (Median)
FLT3 Mutated PKC412 Dose Escalation (E2)116.0
FLT3 Mutated PKC+Itraconazole (E2)75.0
FLT3 Wild Type PKC412 Dose Escalation (E2)372.0
FLT3 Wild Type PKC+Itraconazole (E2)220.0

[back to top]

Overall Survival (OS) (E1)

OS was measured from the date of the first dose of treatment to the date of death from any cause or to the last date that the patient was known to be alive (a censored observation). (NCT00045942)
Timeframe: from date of FPFV, 27-Mar-2003, to date of LPLV, 06-Sep-2004

Interventiondays (Median)
FLT3 Mutated PKC412 100 mg/Day (E1)99.0
FLT3 Mutated PKC412 200 mg/Day (E1)93.0
FLT3 Wild Type PKC412 100 mg/Day (E1)145.0
FLT3 Wild Type PKC412 200 mg/Day (E1)159.0

[back to top]

Terminal Elimination Half-life (T1/2) for CGP62221 in the PKC + Itrconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: day 22,

Interventionhour (Mean)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined14.37

[back to top]

Time to Disease Progression (E1)

TTP was defined as the time from the first dose date to the date of disease progression (defined as the study completion date for unsatisfactory treatment effect, date of response assessment of progressive disease, or date of death from any cause). One participant from the wild type 200 mg group did not have any assessment on treatment and therefore was not taken into account for TTP. (NCT00045942)
Timeframe: from date of FPFV, 27-Mar-2003, to date of LPLV, 06-Sep-2004

Interventiondays (Median)
FLT3 Mutated PKC412 100 mg/Day (E1)77.0
FLT3 Mutated PKC412 200 mg/Day (E1)50.0
FLT3 Wild Type PKC412 100 mg/Day (E1)62.0
FLT3 Wild Type PKC412 200 mg/Day (E1)54.0

[back to top]

Time to Disease Progression (E2)

TTP was defined as the time from the first dose date to the date of disease progression, which was defined as the study completion date for unsatisfactory treatment effect, the date of response assessment of progressive disease, or the date of death from any cause (NCT00045942)
Timeframe: date of FPFV, 21-Aug-2003, to date of LPLV, 27-Mar-2008

Interventiondays (Median)
FLT3 Mutated PKC412 Dose Escalation (E2)49.0
FLT3 Mutated PKC+Itraconazole (E2)26.0
FLT3 Wild Type PKC412 Dose Escalation (E2)169.0
FLT3 Wild Type PKC+Itraconazole (E2)78.0

[back to top]

Time to Disease Progression (TTP) (Core)

TTP was defined as the time from first dose date to date of disease progression which is identified as study completion date for unsatisfactory treatment effect or date of death from any cause within the 28 day cutoff post treatment. (NCT00045942)
Timeframe: from date of FPFV, 29-Jan-2002, to date of LPLV, 04-Sep-2003

Interventiondays (Median)
PKC412 in FLT3 Mutated Participants (Core)63.0

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval Tau (AUCtau) for CGP52421 Plasma in the PKC + Itraconazole Combination Arm (E2)

Blood samples were collected for pharmacokinetic (PK) analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionh*ng/ml (Mean)
Cycle 1, day 21 (n=9)Cycle 1, day 22 (n=7)Cycle 1, day 28 (n=7)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined40258.6542950.7649758.77

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval Tau (AUCtau) for CGP62221 Plasma in the PKC + Itraconazole Combination Arm (E2)

Blood samples were collected for pharmacokinetic (PK) analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionh*ng/ml (Mean)
Cycle 1, day 21 (n=8)Cycle 1, day 22 (n=7)Cycle 1, day 28 (n=7)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined30217.8223824.6931545.54

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval Tau (AUCtau) for PKC412 Plasma in the PKC + Itraconazole Combination Arm (E2)

Blood samples were collected for pharmacokinetic (PK) analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionh*ng/ml (Mean)
Cycle 1, day 21 (n=9)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=7)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined22261.5337578.8535630.45

[back to top]

Summary of PKC412 Plasma Concentration for 100 mg Bid Arm (E1)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (0h, 4h, 24 h), 3 (0h), 8 (0h); cycle 2: days 1 (0h); cycle 3: day 1 (0h); cycle 4: day 1 (0h); cycle 5: day 1 (0h) and cycle 6: day 1 (0h)

Interventionng/ml (Mean)
Cycle 1, day 1 (0h) (n=38)Cycle 1, day 1 (4h) (n=34)Cycle 1, day 1 (24h) (n=36)Cycle 1, day 3 (0h) (n=29)Cycle 1, day 8 (0h) (n=24)Cycle 2, day 1 (0h) (n=15)Cycle 3, day 2 (0h) (n=6)Cycle 4, day 1 (0h) (n=6)Cycle 5, day 1 (0h) (n=4)Cycle 6, day 1 (0h) (n=4)
FLT3 Mutated and Wild Type PKC412 200 mg/Day0.0002087.0882849.7313756.4834447.5831226.333754.5001187.167572.2501433.250

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) for CGP622221 in the PKC412 + Itraconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionh*ng/ml (Mean)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined31699.9331182.9026688.60

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) for PKC412 in the PKC412 + Itraconazole Combination Arm (E2)

Blood samples were collected for PK analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionh*ng/ml (Mean)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28, (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined32120.5834684.633020.17

[back to top]

Best Clinical Response (E2)

Best clinical response was defined as CR, PR, MR, MR+BR, or BR . CR and PR was defined according to NCI definitions, and MR and BR was defined according to the guidelines for defining hematologic improvement in MDS. (NCT00045942)
Timeframe: date of FPFV, 21-Aug-2003, to date of LPLV, 27-Mar-2008

,,,
InterventionParticipants (Number)
Complete responsePartial responseMinor responseMinor response and blast responseBlast responseBest clinical response
FLT3 Mutated PKC+Itraconazole (E2)000000
FLT3 Mutated PKC412 Dose Escalation (E2)000145
FLT3 Wild Type PKC+Itraconazole (E2)101114
FLT3 Wild Type PKC412 Dose Escalation (E2)000202

[back to top]

Number of Participants With Overall Clinical Response (E1)

Overall clinical response was defined as CR, PR, minor response (MR) or blast response (BR). CR and PR was defined according to NCI definitions, and MR and BR was defined according to the guidelines for defining hematologic improvement in MDS. (NCT00045942)
Timeframe: from date of FPFV, 27-Mar-2003, to date of LPLV, 06-Sep-2004

,,,
InterventionParticipants (Number)
Complete responsePartial responseMinor responseBlast responseOverall response
FLT3 Mutated PKC412 100 mg/Day (E1)0011112
FLT3 Mutated PKC412 200 mg/Day (E1)0101213
FLT3 Wild Type PKC412 100 mg/Day (E1)0061521
FLT3 Wild Type PKC412 200 mg/Day (E1)003811

[back to top]

Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax) for CGP52421 in the PKC + Itraconazole Combination Arm (E2)

Blood samples were collected for pharmacokinetic (PK) analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionng/ml (Mean)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined4173.004293.004875.00

[back to top]

Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax) for CGP62221 in the PKC + Itraconazole Combination Arm (E2)

Blood samples were collected for pharmacokinetic (PK) analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionng/ml (Mean)
Cycle 1, day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined3259.303221.403032.25

[back to top]

Observed Maximum Plasma Concentration Following Drug Administration at Steady State (Cmax) for PKC412 in the PKC + Itraconazole Combination Arm (E2)

Blood samples were collected for pharmacokinetic (PK) analysis. (NCT00045942)
Timeframe: Cycle 1: days 21, 22, 28

Interventionng/ml (Mean)
Cycle 1 , day 21 (n=10)Cycle 1, day 22 (n=10)Cycle 1, day 28 (n=8)
FLT3 Mutated and FLT3 Wild Type PKC + Itraconazole Combined3945.003968.703931.25

[back to top]

Summary of CGP52421 Concentration (E2)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1, 2 (24 hr post day 1), 3, 8, 15, 16 (24 hr post day 15), 17, 22; Cycle 2: days 1, 2 (24 hr post day 1), 3, 8, 15

Interventionng/ml (Median)
Cycle 1, day 1 (n=7)Cycle 1, day 2 (24 hr post day 1) (n=12)Cycle 1, day 3 (n=12)Cycle 1, day 8 (n=8)Cycle 1, day 15 (n=6)Cycle 1, day 16 (24 hr post day 15) (n=6)Cycle 1, day 17 (n=5)Cycle 1, day 22 (n=5)Cycle 2, day 1 (n=4)Cycle 2, day 2 (24 hr post day 1) (n=4)Cycle 2, day 3 (n=4)Cycle 2, day 8 (n=4)Cycle 2, day 15 (n=3)
FLT3 Mutated and Wild Type PKC412 Dose Escalation Combined0684.01185.02835.03845.03830.03620.04470.04915.04455.04470.04860.04030.0

[back to top]

Summary of CGP52421 Plasma Concentration (Core)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (24 hour), 3, 8; Cycle 2: day 1,

Interventionng/ml (Mean)
Cycle 1, day 1 (24 hour) (n=10)Cycle 1, day 3 (n=7)Cycle 1, day 8 (n=9)Cycle 2, day 1 (n=6)
PKC412 in FLT3 Mutated Participants (Core)951.701846.576342.2212978.33

[back to top]

Summary of CGP52421 Plasma Concentration for 100 mg Bid Arm (E1)

Blood samples were collected for analysis. (NCT00045942)
Timeframe: Cycle 1: days 1 (0h, 4h, 24 h), 3 (0h), 8 (0h); cycle 2: days 1 (0h); cycle 3: day 1 (0h); cycle 4: day 1 (0h); cycle 5: day 1 (0h) and cycle 6: day 1 (0h)

Interventionng/ml (Mean)
Cycle 1, day 1 (0h) (n=38)Cycle 1, day 1 (4h) (n=34)Cycle 1, day 1 (24h) (n=36)Cycle 1, day 3 (0h) (n=29)Cycle 1, day 8 (0h) (n=24)Cycle 2, day 1 (0h) (n=15)Cycle 3, day 2 (0h) (n=6)Cycle 4, day 1 (0h) (n=6)Cycle 5, day 1 (0h) (n4)Cycle 6, day 1 (0h) (n=4)
FLT3 Mutated and Wild Type PKC412 200 mg/Day0.000257.391666.1941394.0624447.5009196.6678811.6676266.6677845.0008710.000

[back to top]

Duration of Treatment

Median duration in days of treatment. Treatment is defined as the total number of days on which subjects took medication. (NCT00289991)
Timeframe: Day 1 up to Day 180

Interventiondays (Median)
Voriconazole96.0
Itraconazole68.0

[back to top]

Percent of Subjects With Use of Other Systemic Antifungal Agents as Empirical or Therapeutic Treatment

Percent of subjects who used other systemic antifungal agents as empirical or therapeutic treatment, defined as either empirical: subject took a systemic antifungal agent at any time after the day of first dose of medication and did not develop a breakthrough proven or probable IFI during the study or therapeutic: subject developed a breakthrough proven or probable IFI. (NCT00289991)
Timeframe: Day 1 up to Day 180

Interventionpercent of participants (Number)
Voriconazole40.6
Itraconazole49.4

[back to top]

Survival: Percent of Subjects Who Died Within 1 Year

Percent of subjects who died within 1 year after transplant, derived from the crude death rate. All subjects in the MITT population included in this proportion. Only deaths up until and including 365 days after first dose of study medication included in the analysis. (NCT00289991)
Timeframe: Day 1 up to 1 year (Day 365)

Interventionpercent of participants (Number)
Voriconazole25.9
Itraconazole30.7

[back to top]

Time to Breakthrough Invasive Fungal Infection (IFI)

Summary of time (in days) from start of prophylaxis to first recorded occurrence of breakthrough proven or probable IFI. (NCT00289991)
Timeframe: Day 1 up to Day 180 (Visit 9)

Interventiondays (Mean)
Voriconazole119.0
Itraconazole77.0

[back to top]

Time to Discontinuation of Study Treatment

Time in days to discontinuation of study treatment defined as the number of days from first dose to last dose inclusive as recorded in the dosing log. (NCT00289991)
Timeframe: Day 1 up to Day 180 (Visit 9)

Interventiondays (Mean)
Voriconazole88.7
Itraconazole71.5

[back to top]

Percent of Subjects With Occurrence of Breakthrough IFI

Percent of subjects with occurrence of breakthrough IFI (proven or probable). Included all subjects in the MITT population. (NCT00289991)
Timeframe: Day 1 up to Day 100 (Visit 7) and Day 180 (Visit 9)

,
Interventionpercent of participants (Number)
Day 100Day 180
Itraconazole1.21.7
Voriconazole0.91.3

[back to top]

Success at Day 100: Percent of Responders (Randomization Strata)

Percent of responders (by randomization strata) with success of antifungal prophylaxis at 100 days after allogeneic HSCT. Success defined as: alive at Day 100 (Visit 7), had not developed a breakthrough proven or probable IFI by Visit 7, and received full course of study drug prophylaxis without an interruption of >14 days in total during the prophylaxis period; defined as failure if these criteria were not met. Additionally, if subject withdrew from study completely before Visit 7, imputed as failure at Visit 7 (programmatically). (NCT00289991)
Timeframe: Day 100 (Visit 7)

,
Interventionpercent of participants (Number)
Myeloablative/matched related (n=66, 85)Myeloablative/mismatched unrelated (n=59, 58)Non-myeloablative/matched related (n=58, 57)Non-myeloablative/mismatched unrelated (n=41, 41)
Itraconazole50.627.638.636.6
Voriconazole65.255.943.148.8

[back to top]

Success at Day 180: Percent of Responders (Randomization Strata)

Percent of responders (by randomization strata) with success of antifungal prophylaxis at 180 days after allogeneic hematopoietic stem cell transplant (HSCT). Success: alive at Day 180 (Visit 9), had not developed a breakthrough proven or probable invasive fungal infection (IFI) by Visit 9, and received full course of study drug prophylaxis without interruption of greater than 14 days in total during the prophylaxis period; defined as failure if these criteria were not met. Additionally, if subject withdrew from study completely before Visit 9, imputed as failure at Visit 9 (programmatically). (NCT00289991)
Timeframe: Day 180 (Visit 9)

,
Interventionpercent of participants (Number)
Myeloablative/matched related (n=66, 85)Myeloablative/mismatched unrelated (n=59, 58)Non-myeloablative/matched related (n=58, 57)Non-myeloablative/mismatched unrelated (n=41, 41)
Itraconazole44.725.928.126.8
Voriconazole59.152.534.546.3

[back to top]

Survival: Percent of Subjects Who Died at or Before Day 180

Percent of subjects who died at or before Day 180, derived from the crude death rate. All subjects in the MITT population included in this proportion. (NCT00289991)
Timeframe: Day 1 up to Day 180 (Visit 9)

Interventionpercent of participants (Number)
Voriconazole15.6
Itraconazole15.4

[back to top]

Clinical Improvement Compared to Placebo

"Clinical Improvement consisted of a mycological cure and an Investigator's Global Assessment (IGA) score less than or equal to 1 at week 52.~The Investigator's Global Assessment(IGA)assesses the overall severity of onychomycosis on the target toenail and takes into consideration, onycholysis, hyperkeratosis and percent nail involvement.~0 = Clinical Cure: No evidence of onychomycosis.~1 = Clinical Improvement: Minimal evidence of onychomycosis. 2 = Mild: ≤25% dystrophy and/or onycholysis. 3 = Moderate: ≤50% dystrophy with onycholysis. 4 = Severe: >50% dystrophy with onycholysis." (NCT00356915)
Timeframe: 12 months

Interventionpercentage of participants (Number)
Itraconazole Tablets33.7
Placebo Tablets2

[back to top]

Clinical Improvement of the Target Toenail

"Clinical Improvement consisted of a mycological cure and an Investigator's Global Assessment (IGA) score less than or equal to 1 at week 52.~The Investigator's Global Assessment (IGA) assesses the overall severity of onychomycosis on the target toenail and takes into consideration, onycholysis, hyperkeratosis and percent nail involvement.~0 = Clinical Cure: No evidence of onychomycosis.~1 = Clinical Improvement: Minimal evidence of onychomycosis. 2 = Mild: ≤25% dystrophy and/or onycholysis. 3 = Moderate: ≤50% dystrophy with onycholysis. 4 = Severe: >50% dystrophy with onycholysis." (NCT00356915)
Timeframe: 12 months

Interventionpercentage of participants (Number)
Itraconazole Tablets33.7
Itraconazole Capsules29.3

[back to top]

Complete Cure - Itraconazole Tablets Compared to Itraconazole Capsules

The primary efficacy endpoint was Compete Cure (consisting of a Clinical Cure and a Mycological Cure) at week 52. In this study, Clinical Cure was defined as an Investigator's Global Assessment (IGA) score of 0 for the target toenail; Mycological Cure was defined as a negative potassium hydroxide (KOH) examination and a negative culture outcome for dermatophytes of the target toenail. The efficacy analyses were conducted to demonstrate the non-inferiority of 1 itraconazole 200-mg tablet to 2 itraconazole 100-mg capsule. (NCT00356915)
Timeframe: 12 months

InterventionPercentage of participants (Number)
Itraconazole Tablets22.3
Itraconazole Capsules21.7
Placebo Tablets1.0

[back to top]

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

InterventionPercentage of participants (Number)
Itraconazole Tablets22.3
Placebo Tablets1

[back to top]

The Primary Outcome Measure Will be the Number of Patients Who Experience a Respiratory Exacerbation Requiring Intravenous Antibiotics in the Two Treatment Groups Over the 24 Week Trial Treatment Period.

The Primary outcome measure will be the number of patients who experience a respiratory exacerbation requiring intravenous antibiotics in the two treatment groups over the 24 week trial treatment period. (NCT00528190)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
Itraconazole4
Placebo5

[back to top] [back to top] [back to top]

Probability of Participant Survival at Month 6

Probability of survival was defined as the probability of being alive at Month 6. (NCT00585195)
Timeframe: Month 6

InterventionProbability of participants survival (Number)
RP2D Cohort: ROS1-Positive NSCLC: Crizotinib 250 mg90.5
RP2D Cohort: MET Exon 14 Alterations NSCLC: Crizotinib 250 mg86.7
RP2D Cohort: MET Amplification NSCLC: Crizotinib 250 mg67.8
RP2D Cohort: ALK-Positive Cohort, NSCLC: Crizotinib 250 mg90.0

[back to top]

Itraconazole Cohort: Trough Plasma Concentration (Ctrough) of Crizotinib When Taken Alone and When Taken With Itraconazole

Ctrough refers to plasma concentration of Crizotinib observed just before treatment administration. (NCT00585195)
Timeframe: pre-dose on Cycle 1 Day 15 (crizotinib with itraconazole) and Cycle 2 Day 1 (itraconazole alone)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg Alone136.0
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg With Itraconazole214.0

[back to top]

Itraconazole Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken Alone and When Taken With Itraconazole

(NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9 and 24 hours post dose on Cycle 1 Day 15 (Crizotinib with itraconazole) and Cycle 2 Day 1 (itraconazole alone)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg Alone259.9
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg With Itraconazole353.2

[back to top]

Itraconazole Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib When Taken Alone and When Taken With Itraconazole

Area under the plasma concentration versus time curve from time 0 to end of dosing interval (AUCtau), where dosing interval is 24 hours. (NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9 and 24 hours post dose on Cycle 1 Day 15 (Crizotinib with itraconazole) and Cycle 2 Day 1 (itraconazole alone)

Interventionnanogram*hour per milliliter (Geometric Mean)
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg Alone4102
Itraconazole Interaction Cohort: Crizotinib 250 mg + Itraconazole6665

[back to top] [back to top]

Dose-Escalation Cohort: Number of Participants With Dose-limiting Toxicities (DLT)

Dose-limiting toxicity (DLT) was defined as any of the following: Hematologic- prolonged grade 4 neutropenia for >7 days. Febrile neutropenia, defined as grade 4 neutropenia with fever greater than (>)38.5 degree Celsius, both sustained over a 24 hour period, neutropenic infection: greater than or equal to (>=)Grade 3 neutropenia with Grade >=3 infection. Grade >=3 thrombocytopenia with bleeding or grade 4 lasting >=7 days Lymphopenia was not considered a DLT unless accompanied by infection. Other non-hematologic toxicity: Grade 3 or 4 toxicities (except for alopecia, Grade 3/4 hypophosphatemia, grade 3 hypertension with controlled blood pressure [less than (<) 140/90], and Grade 3/4 hyperuricemia without signs and symptoms of gout). Nausea, vomiting or diarrhea must persist at grade 3 or 4 despite maximal medical therapy. (NCT00585195)
Timeframe: Cycle 1 (28 days)

InterventionParticipants (Count of Participants)
Low Dose Escalation Cohort: Crizotinib 50 mg QD0
Low Dose Escalation Cohort: Crizotinib 100 mg QD0
Low Dose Escalation Cohort: Crizotinib 200 mg QD1
Low Dose Escalation Cohort: Crizotinib 200 mg BID0
Low Dose Escalation Cohort: Crizotinib 250 mg BID0
Low Dose Escalation Cohort: Crizotinib 300 mg BID2
High Dose Escalation Cohort: Crizotinib 300 mg QD0
High Dose Escalation Cohort: Crizotinib 400 mg QD0
High Dose Escalation Cohort: Crizotinib 500 mg QD0
High Dose Escalation Cohort: Crizotinib 650 mg QD0
High Dose Escalation Cohort: Crizotinib 800 mg QD0

[back to top]

Dose-Escalation Cohort: Maximum Tolerated Dose (MTD) of Crizotinib

MTD: Dose level at which at most 1 of 6 participants experienced DLT within and including 28 days of treatment (during Cycle 1 [1 cycle=28 days]) with next higher dose having at least 2/3 or 2/6 participants experiencing a DLT. DLT was defined as any of following: Hematologic toxicities- 1) prolonged grade 4 neutropenia for >7 days. 2) Febrile neutropenia: grade 4 neutropenia with fever greater than (>) 38.5 degree Celsius, both sustained over a 24 hour period (3) neutropenic infection: greater than or equal to (>=) Grade 3 neutropenia with Grade >=3 infection. (4) Grade >=3 thrombocytopenia with bleeding/grade 4 lasting >=7 days. Other non-hematologic toxicity included: Grade 3/4 toxicities (except for alopecia, Grade 3/4 hypophosphatemia, grade 3 hypertension with controlled blood pressure [less than (<) 140/90 millimeter of mercury, and Grade 3/4 hyperuricemia without signs and symptoms of gout). Nausea, vomiting/diarrhea must persist at grade 3/4 despite maximal medical therapy. (NCT00585195)
Timeframe: Cycle 1 (28 days)

Interventionmilligram (Number)
Low Dose Escalation Cohort: Crizotinib 50 mg QD250
Low Dose Escalation Cohort: Crizotinib 100 mg QD250
Low Dose Escalation Cohort: Crizotinib 200 mg QD250
Low Dose Escalation Cohort: Crizotinib 200 mg BID250
Low Dose Escalation Cohort: Crizotinib 250 mg BID250
Low Dose Escalation Cohort: Crizotinib 300 mg BID250
High Dose Escalation Cohort: Crizotinib 300 mg QD250
High Dose Escalation Cohort: Crizotinib 400 mg QD250
High Dose Escalation Cohort: Crizotinib 500 mg QD250
High Dose Escalation Cohort: Crizotinib 650 mg QD250
High Dose Escalation Cohort: Crizotinib 800 mg QD250

[back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 24 Day 1

Geometric mean of ratio (Cycle 24 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 24 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.390.701.130.690.532.350.200.90

[back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top]

Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Midazolam When Taken Alone or Taken With Crizotinib

AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). (NCT00585195)
Timeframe: pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Day -7 (midazolam alone arm), pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Cycle 2 Day 1 (midazolam with crizotinib arm)

Interventionnanogram*hour per milliliter (Geometric Mean)
Low Dose Escalation Cohort: Crizotinib 100 mg QD (Midazolam Alone)41.77
Low Dose Escalation Cohort: Crizotinib 100 mg QD + Midazolam90.78
Low Dose Escalation Cohort: Crizotinib 300 mg BID (Midazolam Alone)37.71
Low Dose Escalation Cohort: Crizotinib 300 mg BID + Midazolam151.45
RP2D Cohort: Crizotinib 250 mg (Midazolam Alone)32.10
RP2D Cohort: Crizotinib 250 mg +Midazolam112.78

[back to top]

Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib Alone and When Taken With Rifampin

Area under the plasma concentration versus time curve from time 0 to end of dosing interval (AUCtau). (NCT00585195)
Timeframe: pre-dose, 2, 4, 6, 8 and 10 hours on Cycle 1 Day 15 (Crizotinib alone arm) and Cycle 2 Day 1 (Crizotinib with Rifampin arm)

Interventionnanogram*hour per milliliter (Geometric Mean)
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg Alone3110
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg With Rifampin509.6

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at End of Treatment

Geometric mean of ratio (End of treatment/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, End of Treatment (28 days post last dose)

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.400.661.480.520.850.620.640.41

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 9 Day 1

Geometric mean of ratio (Cycle 9 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 9 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.380.561.190.720.831.230.190.72

[back to top]

Midazolam Interaction Cohort: Maximum Observed Plasma Concentration (Cmax) of Midazolam When Taken Alone or Taken With Crizotinib

Cmax is defined as the observed maximum plasma concentration post drug administration. (NCT00585195)
Timeframe: pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Day -7 (midazolam alone arm), pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Cycle 2 Day 1 (midazolam with crizotinib arm)

Interventionnanogram per milliliter (Geometric Mean)
Low Dose Escalation Cohort: Crizotinib 100 mg QD (Midazolam Alone)14.98
Low Dose Escalation Cohort: Crizotinib 100 mg QD + Midazolam19.26
Low Dose Escalation Cohort: Crizotinib 300 mg BID (Midazolam Alone)13.65
Low Dose Escalation Cohort: Crizotinib 300 mg BID + Midazolam32.62
RP2D Cohort: Crizotinib 250 mg (Midazolam Alone)12.78
RP2D Cohort: Crizotinib 250 mg + Midazolam25.37

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 6 Day 1

Geometric mean of ratio (Cycle 6 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 6 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.490.750.690.781.071.710.250.87

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 4 Day 1

Geometric mean of ratio (Cycle 4 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 4 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.480.660.840.750.881.630.220.81

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 30 Day 1

Geometric mean of ratio (Cycle 30 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 30 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.160.381.140.850.801.250.090.71

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 27 Day 1

Geometric mean of ratio (Cycle 27 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 27 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.460.971.480.700.661.860.240.95

[back to top]

Probability of Participant Survival at Month 12

Probability of survival was defined as the probability of being alive at Month 12. (NCT00585195)
Timeframe: Month 12

Interventionprobability of participants survival (Number)
RP2D Cohort: ROS1-Positive NSCLC: Crizotinib 250 mg78.8
RP2D Cohort: MET Exon 14 Alterations NSCLC: Crizotinib 250 mg66.0
RP2D Cohort: MET Amplification NSCLC: Crizotinib 250 mg37.1
RP2D Cohort: ALK-Positive Cohort, NSCLC: Crizotinib 250 mg80.5

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 21 Day 1

Geometric mean of ratio (Cycle 21 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 21 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.230.481.460.530.771.230.150.72

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 2 Day 1

Geometric mean of ratio (Cycle 2 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 2 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.470.720.890.420.691.310.240.85

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 18 Day 1

Geometric mean of ratio (Cycle 18 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 18 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.320.551.640.690.891.100.180.69

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 15 Day 1

Geometric mean of ratio (Cycle 15 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 15 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.491.031.320.900.811.710.240.76

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 12 Day 1

Geometric mean of ratio (Cycle 12 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 12 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.380.661.060.881.021.390.230.75

[back to top]

Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 1 Day 15

Geometric mean of ratio (Cycle1Day15/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 1 Day 15

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLuteinizing Hormone (LH) SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.460.531.190.580.770.960.360.97

[back to top] [back to top]

RP2D Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken With Food

Cmax is defined as the observed maximum plasma concentration post drug administration. (NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9, and 24 hours post-dose on Day -7

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Crizotinib 250 mg With Food106.24

[back to top]

RP2D Cohort: Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Crizotinib When Taken With Food

AUC0-24 of Crizotinib was defined as the area under the free plasma concentration time curve from time 0 to 24 hours post-dose. (NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9, and 24 hours post-dose on Day -7

Interventionnanogram*hour per milliliter (Geometric Mean)
RP2D Cohort: Crizotinib 250 mg With Food1212.86

[back to top]

Rifampin Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib Alone and When Taken With Rifampin

(NCT00585195)
Timeframe: pre-dose, 2, 4, 6, 8 and 10 hours on Cycle 1 Day 15 (Crizotinib alone) and Cycle 2 Day 1 (Crizotinib with Rifampin)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg Alone326.4
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg With Rifampin71.53

[back to top]

Rifampin Cohort: Ctrough of Crizotinib Alone and When Taken With Rifampin

Ctrough refers to plasma concentration of Crizotinib observed just before treatment administration. (NCT00585195)
Timeframe: pre-dose on Cycle 1 Day 15 (Crizotinib alone arm) and Cycle 2 Day 1 (Crizotinib with Rifampin arm)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg Alone251.7
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg With Rifampin26.67

[back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top]

Progression Free Survival as Measured by Number of Days Without Disease Progression

(NCT00769600)
Timeframe: 1 year

Interventiondays (Median)
Itraconazole Open Label Added to Standard of Care Pemetrexed168
Single Agent Pemetrexed84

[back to top]

RECIST Response

Number of participants with partial response (PR), stable disease (SD) and progressive disease (PD) as defined by Response Evaluation Criteria in Solid Tumors (RECIST) (NCT00769600)
Timeframe: Up to 3 years

,
InterventionParticipants (Count of Participants)
PRSDPDInevaluable
Itraconazole Open Label Added to Standard of Care Pemetrexed3822
Single Agent Pemetrexed0521

[back to top]

Overall Survival

Median number of days alive (NCT00769600)
Timeframe: up to 3 years

Interventiondays (Median)
Arm A971
Arm B242

[back to top]

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

If the lower bound 95% confidence interval of the difference between the proportion of patients in the test group compared to the reference group considered a cure at the visit being analyzed was greater than -20 then non-inferiority was considered to have been demonstrated (NCT00791219)
Timeframe: Week 12

InterventionParticipants (Count of Participants)
Placebo0
Test0
Reference0

[back to top]

Superiority of Test Treatment Over Placebo for Mycological Cure

All primary and secondary endpoints were tested for superiority against Placebo. The intent to treat (ITT) was used for all superiority testing. For the three primary endpoints and all four dichotomous secondary endpoints, if the difference between the proportion of patients considered a cure in the Test or Reference group was statistically greater (p < 0.05) than the proportion of patients considered a cure in the Placebo group, then superiority of that treatment over placebo was considered to have been demonstrated. A one-sided continuity corrected Z-test was used for superiority testing. (NCT00791219)
Timeframe: week 6

InterventionParticipants (Count of Participants)
Placebo0
Test11
Reference5

[back to top]

"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)"

If the lower bound 95% confidence interval of the difference between the proportion of patients in the Test group compared to the Reference group considered a Clinical Cure at Visit 7 was greater than 20 then non-inferiority was considered to have been demonstrated (NCT00791219)
Timeframe: Week 24

InterventionParticipants (Count of Participants)
Placebo0
Test12
Reference4

[back to top]

"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)"

If the lower bound 95% confidence interval of the difference between the proportion of patients in the test group compared to the reference group considered a cure at the visit being analyzed was greater than -20 then non-inferiority was considered to have been demonstrated (NCT00791219)
Timeframe: week 12

InterventionParticipants (Count of Participants)
Placebo3
Test16
Reference16

[back to top]

"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)"

If the lower bound 95% confidence interval of the difference between the proportion of patients in the Test group compared to the Reference group considered a Mycological Cure at Visit 7 was greater than 20 then non-inferiority was considered to have been demonstrated (NCT00791219)
Timeframe: Week 24

InterventionParticipants (Count of Participants)
Placebo1
Test25
Reference22

[back to top]

"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)"

If the lower bound 95% confidence interval of the difference between the proportion of patients in the Test group compared to the Reference group considered a Therapeutic Cure at Visit 7 was greater than 20 then non-inferiority was considered to have been demonstrated (NCT00791219)
Timeframe: Week 24

InterventionParticipants (Count of Participants)
Placebo0
Test8
Reference3

[back to top]

"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)"

If the lower bound 95% confidence interval of the difference between the proportion of patients in the test group compared to the reference group considered a cure at the visit being analyzed was greater than -20 then non-inferiority was considered to have been demonstrated (NCT00791219)
Timeframe: week 12

InterventionParticipants (Count of Participants)
Placebo0
Test1
Reference0

[back to top]

Pharmacokinetics (PK) of Oral Itraconazole

To determine the pharmacokinetics (PK) of oral itraconazole in patients with MBC by measuring mean trough plasma levels at steady state at weeks 2 and 4. (NCT00798135)
Timeframe: pre-dose at Weeks 2 and 4

Interventionng/mL (Mean)
Week 2 Intraconazole ConcentrationWeek 4 Intraconazole ConcentrationWeek 2 6-OH Itraconazole ConcentrationWeek 4 6-OH Itraconazole Concentration
Itraconazole230.7305.8454.8501.6

[back to top]

Time to Progression.

This is calculated as time till progression from treatment start until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 100 months. If a patient did not progress, they were censored at the last evaluation visit. The median time till progression is calculated with its 95% confidence interval. (NCT00798135)
Timeframe: up to 100 months

InterventionMonths (Median)
Itraconazole1.54

[back to top] [back to top]

Percentage of Participants Showing Mycological Cure

Mycological cure was defined as a case in which the results of both potassium hydroxide (KOH) smear test and bacterial identification test (BIT) were found to be negative at each pre-defined time point. (NCT00871728)
Timeframe: Week 13, 25, 37 and 49

Interventionpercentage of participants (Number)
Negative KOH Smear Test : Week 13 (n=109)Negative KOH Smear Test : Week 25 (n=103)Negative KOH Smear Test : Week 37 (n=102)Negative KOH Smear Test : Week 49 (n=99)Negative BIT : Week 13 (n=108)Negative BIT : Week 25 (n=103)Negative BIT : Week 37 (n=102)Negative BIT : Week 49 (n=97)
Itraconazole70.683.590.283.864.879.681.482.5

[back to top]

Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 9

The SCIO is based on clinical state and its items include major factors that can have an effect on the outcome of onychomycosis treatment. The factors include the clinical form, depth of an infected area and subungal hyperkeratosis. The SCIO score range from 1 to 30 and higher score indicates more severity. The score is classified into 7 steps and as there is treatment for each step, treatment based on the clinical state can be applied consistently. Percentage of participants who show an improvement in SCIO score by 10 percent or more at Week 9 compared to Baseline were reported. (NCT00871728)
Timeframe: Baseline and Week 9

Interventionpercentage of participants (Number)
Itraconazole50.4

[back to top]

Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 5

The SCIO is based on clinical state and its items include major factors that can have an effect on the outcome of onychomycosis treatment. The factors include the clinical form, depth of an infected area and subungal hyperkeratosis. The SCIO score range from 1 to 30 and higher score indicates more severity. The score is classified into 7 steps and as there is treatment for each step, treatment based on the clinical state can be applied consistently. Percentage of participants who show an improvement in SCIO score by 10 percent or more at Week 5 compared to Baseline were reported. (NCT00871728)
Timeframe: Baseline and Week 5

Interventionpercentage of participants (Number)
Itraconazole25.6

[back to top]

Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 49

The SCIO is based on clinical state and its items include major factors that can have an effect on the outcome of onychomycosis treatment. The factors include the clinical form, depth of an infected area and subungal hyperkeratosis. The SCIO score range from 1 to 30 and higher score indicates more severity. The score is classified into 7 steps and as there is treatment for each step, treatment based on the clinical state can be applied consistently. Percentage of participants who show an improvement in SCIO score by 10 percent or more at Week 49 compared to Baseline were reported. (NCT00871728)
Timeframe: Baseline and Week 49

Interventionpercentage of participants (Number)
Itraconazole80.3

[back to top]

Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 25

The SCIO is based on clinical state and its items include major factors that can have an effect on the outcome of onychomycosis treatment. The factors include the clinical form, depth of an infected area and subungal hyperkeratosis. The SCIO score range from 1 to 30 and higher score indicates more severity. The score is classified into 7 steps and as there is treatment for each step, treatment based on the clinical state can be applied consistently. Percentage of participants who show an improvement in SCIO score by 10 percent or more at Week 25 compared to Baseline were reported. (NCT00871728)
Timeframe: Baseline and Week 25

Interventionpercentage of participants (Number)
Itraconazole84.6

[back to top]

Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 13

The SCIO is based on clinical state and its items include major factors that can have an effect on the outcome of onychomycosis treatment. The factors include the clinical form, depth of an infected area and subungal hyperkeratosis. The SCIO score range from 1 to 30 and higher score indicates more severity. The score is classified into 7 steps and as there is treatment for each step, treatment based on the clinical state can be applied consistently. Percentage of participants who show an improvement in SCIO score by 10 percent or more at Week 13 compared to Baseline were reported. (NCT00871728)
Timeframe: Baseline and Week 13

Interventionpercentage of participants (Number)
Itraconazole80.3

[back to top]

Percentage of Participants Showing 10 Percent or Higher Response in Scoring Clinical Index for Onychomycosis (SCIO) Score at Week 37

The SCIO is based on clinical state and its items include major factors that can have an effect on the outcome of onychomycosis treatment. The factors include the clinical form, depth of an infected area and subungal hyperkeratosis. The SCIO score range from 1 to 30 and higher score indicates more severity. The score is classified into 7 steps and as there is treatment for each step, treatment based on the clinical state can be applied consistently. Percentage of participants who show an improvement in SCIO score by 10 percent or more at Week 37 compared to Baseline were reported. (NCT00871728)
Timeframe: Baseline and Week 37

Interventionpercentage of participants (Number)
Itraconazole86.3

[back to top]

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

Will be reported as the percentage of men with ≥ 50% PSA reduction from baseline. (NCT00887458)
Timeframe: Baseline and approximately 2 years from open enrollment

Interventionpercentage (Number)
Low Dose0
High Dose14.3

[back to top]

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.

"To Determine the Proportion of Patients With Metastatic CRPC Who do Not Have Prostate Specific Antigen (PSA) Progression After 24 Weeks of Therapy. PSA progression is defined as a 25% increase in PSA over baseline [or nadir (lowest)] and an increase in absolute PSA level by at least 2 ng/mL, both confirmed by a second value at least 4 weeks later." (NCT00887458)
Timeframe: Up to 24 weeks

Interventionpercent of patients (Number)
Low Dose Itraconazole11.8
High Dose Itraconazole48

[back to top]

Candida Culture Free After Maintenance Therapy

candida culture free (monthly vaginal cultures were obtained) (NCT00895453)
Timeframe: 12 months

Interventionparticipants (Number)
Itraconazole18
Itraconazole + Lactobacillus Gasseri19
Classic Homeopathy9

[back to top]

Plasma Concentration of Itraconazole by Overall Success Rate (OSR) in Participants Who Received the Study Treatment

Plasma level of itraconazole was defined as the sum of IC and HIC. The OSR was defined based on satisfaction of the following criteria: (1) participants if treated for baseline fungal infection, there was either eradication (removal of fungus in culture), or presumed eradication; no evidence in culture but appeared to be treated clinically, (2) absence of breakthrough fungal infection during the treatment and for 7 days after completing the treatment, (3) survival for 7 days after completing the treatment, (4) absence of early withdrawal due to adverse events or lack of efficacy, and (5) defervescence. The presence and absence of OS was reported. (NCT01021683)
Timeframe: Day 5

Interventionng/mL (Mean)
Presence of OS (n=95)Absence of OS (n=39)
Itraconazole2328.101690.90

[back to top]

Percentage of Participants Achieving Plasma Level of Itraconazole at 1000 Nanogram Per Milliliter (ng/mL) or Higher After Administration of Study Treatment

Percentage of participants who achieved more than or equal to 1000 ng/ml level after administration of study treatment were reported. Plasma level of itraconazole was defined as the sum of itraconazole concentration (IC) and hydroxyitraconazole concentration (HIC). (NCT01021683)
Timeframe: Day 5

InterventionPercentage of Participants (Number)
Itraconazole68.0

[back to top]

Duration of Neutropenia

The duration of neutropenia was reported. Neutropenia was defined as neutrophil count less than or equal to (<=) 500 cells per cubic millimeter (cells/mm^3), or neutrophil count <=1000 cells/mm^3 and anticipated to decrease to <=500 cells/mm^3 within several days. (NCT01021683)
Timeframe: Day 0 up to Day 14

InterventionDays (Mean)
Itraconazole2.64

[back to top]

Percentage of Participants With Baseline Fungal Infection

Blood cultures (a laboratory test on a sample of blood) were assessed to identify fungus. Percentage of participants with presence or absence of fungus before starting the study drug were calculated. (NCT01021683)
Timeframe: Baseline (Day 0)

InterventionPercentage of Participants (Number)
Itraconazole5.3

[back to top]

Absolute Neutrophil Count (ANC)

The mean values for ANC based on blood tests performed on Day 0 (before starting the study treatment) constitute a Baseline measure for ANC. (NCT01021683)
Timeframe: Baseline (Day 0)

InterventionCells/mm^3 (Mean)
Itraconazole56.26

[back to top]

Percentage of Participants With Deferevescence After Administration of Study Treatment

Defervescence was defined as fall of the body temperature below 38.0 degree Celsius (C) at least once after starting to receive the study treatment. (NCT01021683)
Timeframe: Day 0 up to Day 14

InterventionPercentage of Participants (Number)
Itraconazole87.3

[back to top]

Percentage of Participants With Defervescence by Plasma Level of Itraconazole

Defervescence was defined as fall of the body temperature below 38.0 degree C at least once after starting to receive the study treatment. Plasma level of itraconazole was defined as the sum of IC and HIC. (NCT01021683)
Timeframe: Day 5

InterventionPercentage of Participants (Number)
IC+HIC < 1000ng/mL (n=48)IC+HIC >= 1000ng/mL (n=102)
Itraconazole70.895.1

[back to top]

Plasma Concentration of Itraconazole by Breakthrough Fungal Infection

Plasma level of itraconazole was defined as the sum of IC and HIC. A breakthrough fungal infection was defined as any fungal infection that was diagnosed more than (>) 3 days on or during therapy or within 7 days after completion of therapy. Blood cultures were assessed to identify fungus. (NCT01021683)
Timeframe: Day 5

Interventionng/mL (Mean)
Presence of Breakthrough Fungal infection (n=128)Absence of Breakthrough Fungal infection (n=6)
Itraconazole2155.701864.20

[back to top]

Mean Time to Defervescence in Participants Who Received the Study Treatment

The mean time to defervescence was reported in participants who received the study treatment. Defervescence was defined as fall of the body temperature below 38.0 degree C at least once after starting to receive the study treatment. (NCT01021683)
Timeframe: Day 0 up to Day 14

InterventionDays (Mean)
Itraconazole3.14

[back to top]

Change of GLI1 Tumor Biomarker

Tumor biomarker GLI1 (glioma-associated oncogene 1), part of the Hedgehog (HH) pathway, was assessed in vismodegib-naïve participants at baseline and after 1 month of treatment by quantitative polymerase chain reaction (qPCR). The relative expression of the biomarker was measured as the fold increase of GLI1 expression compared to that of housekeeping gene hypoxanthine-guanine phosphoribosyltransferase (HPRT), and the outcome was assessed as the percent change from the mean of the pre-treatment measurements to the mean of the post-treatment measurements. A negative mean indicates an overall reduction in GLI1 expression. (NCT01108094)
Timeframe: 1 month

InterventionPercent change (Mean)
Cohort A1 - Itraconazole 400 mg (Vismodegib-naïve)-40.3
Cohort A2 - Itraconazole 400 mg (Prior Vismodegib)-16.2

[back to top]

Ki67 Tumor Proliferation Biomarker

"Percent change in Ki67 tumor proliferation biomarker was assessed at baseline and after 1 month of treatment, for Cohort A1 (vismodegib-naïve participants receiving 400 mg as 200 mg twice daily) vs control patients. The outcome is expressed as the % change from baseline of cells with a positive signal after staining for Ki67.~Paired analysis of tumors shows percent change between baseline (prior to treatment) and post itraconazole treatment in individual patients, & is reported as the mean of the changes observed for those lesions for which both baseline and treated valued are available.~Unpaired analysis shows percent change between individual tumors from control patients and itraconazole treated patients, and is reported as the change in mean of the group of baseline basal cell carcinoma (BCC) lesion measurements and the group of treated BCC lesion measurements." (NCT01108094)
Timeframe: 1 month

,
InterventionMean percent change (Mean)
Unpaired AnalysisPaired Analysis
Cohort A1 - Itraconazole 400 mg (Vismodegib-naïve)18-19
Untreated Control013

[back to top]

Tumor Size

Tumor size was assessed by caliper measurement of the longest perpendicular diameters before and after itraconazole treatment, and determination of tumor area by multiplication of the measurements for each tumor. The outcome is expressed as the mean percent change in tumor area from baseline, with standard deviation. A negative value indicates a reduction in size. (NCT01108094)
Timeframe: Up to 3 months

InterventionMean percent change (Mean)
Cohort A1 - Itraconazole 400 mg (Vismodegib-naïve)-25.4
Cohort B - Itraconazole 200 mg (Vismodegib-naïve)-20

[back to top]

Reduction in Serum PSA

Number of subjects with > 50% drop in serum PSA as compared to baseline, at 12 weeks and confirmed at 15 weeks (NCT01450683)
Timeframe: 12 weeks treatment, with primary outcome assessed at 15 weeks

Interventionparticipants (Number)
Itraconazole0

[back to top]

Maximum Measured Concentration of Volasertib and Its Metabolite CD 10899 in Plasma (Cmax)

Maximum measured concentration of the analyte (volasertib and its metabolite CD 10899) in plasma (Cmax) is reported. (NCT01772563)
Timeframe: 30 minutes before volasertib administration and 1 hour (h), 1.75h, 4h, 6h, 8h, 12h, 24, 36h, 48h, 72h, 168h, 336h, 504 h after volasertib administration on Day 1 of Cycle 1 (Volasertib+ Itraconazole) and of Cycle 2 (Volasertib).

,
Interventionnanogram/milliliter (ng/mL) (Geometric Mean)
volasertibCD 10899
Volasertib (Cycle 2)4147.10
Volasertib+ Itraconazole (Cycle 1)3284.51

[back to top]

Area Under the Plasma Concentration-time Curve Over the Time Interval From 0 to Infinity (AUC0-∞) of Volasertib and Its Metabolite CD 10899

Area under the plasma concentration-time curve over the time interval from 0 to infinity (AUC0-∞) of volasertib and its metabolite CD 10899 is reported. (NCT01772563)
Timeframe: 30 minutes before volasertib administration and 1 hour (h), 1.75h, 4h, 6h, 8h, 12h, 24h, 36h, 48h, 72h, 168h, 336h, 504 h after volasertib administration on Day 1 of Cycle 1 (Volasertib+ Itraconazole) and of Cycle 2 (Volasertib).

,
Interventionnanogram*hour/milliliter (ng*h/mL) (Geometric Mean)
volasertibCD 10899
Volasertib (Cycle 2)76101310
Volasertib+ Itraconazole (Cycle 1)73601020

[back to top]

Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to the Last Quantifiable Drug Plasma Concentration After Dose Administration (AUC0-tz) of Volasertib and Its Metabolite CD 10899

Area under the plasma concentration-time curve over the time interval from zero to the last quantifiable drug plasma concentration after dose administration (AUC0-tz) of volasertib and its metabolite CD 10899 is reported. (NCT01772563)
Timeframe: 30 minutes before volasertib administration and 1 hour (h), 1.75h, 4h, 6h, 8h, 12h, 24h, 36h, 48h, 72h, 168h, 336h, 504 h after volasertib administration on Day 1 of Cycle 1 (Volasertib+ Itraconazole) and of Cycle 2 (Volasertib).

,
Interventionnanogram*hour/milliliter (ng*h/mL) (Geometric Mean)
volasertibCD 10899
Volasertib (Cycle 2)71401130
Volasertib+ Itraconazole (Cycle 1)6690855

[back to top]

Mean Percent Change in PSA Doubling Time

The mean percent change in PSA doubling time from pre-treatment to after 12 weeks of protocol therapy (NCT01787331)
Timeframe: Up to 12 weeks

InterventionPercent change in PSA doubling time (Mean)
Treatment (Itraconazole)-0.64

[back to top]

Median Time to Clinical Progression

"Clinical progression will be defined as the first occurrence of either the development of metastases or initiation of non-protocol therapy, and will exclude PSA-only progression.~The probability distribution of the time to clinical progression will be estimated using the Kaplan-Meier product limit method measured from the time of start of protocol therapy. The results will be summarized by the estimated median with 95% confidence intervals." (NCT01787331)
Timeframe: Up to 2 years

Interventionmonths (Median)
Treatment (Itraconazole)21.7

[back to top]

Median Time to PSA Progression

PSA progression defined as: 1. If no PSA decline is observed on therapy, PSA progression will be defined as an increase in serum PSA > 50% above the baseline PSA, and an absolute increase of > 2 ng/mL above baseline, confirmed by repeat measurement at least 2 weeks later. 2. If PSA declines on therapy, PSA progression will be defined as an increase in serum PSA > 50% above the nadir PSA on therapy, and an absolute increase > 2 ng/mL above the nadir, confirmed by repeat measurement at least 2 weeks later. The probability distribution of the time to PSA progression will be estimated using the Kaplan-Meier product limit method measured from the start of protocol therapy. The results will be summarized by the estimated median with 95% confidence intervals. (NCT01787331)
Timeframe: Up to 2 years

Interventionmonths (Median)
Treatment (Itraconazole)4.68

[back to top]

Percentage of Participants With Treatment-related, Adverse Changes in Vital Signs

All patients who receive at least one dose of study drug will be analyzed for safety endpoints. All adverse events will be graded and classified according to the NCI Common Terminology Criteria for Adverse Events (CTCAE) v. 4. Percentage of patients with grade 1 or higher, treatment-related adverse events based on the following vital sign assessments will be reported: blood pressure, pulse, respiration rate and temperature. (NCT01787331)
Timeframe: Up to 2 years

Interventionpercentage of participants (Number)
Blood PressureWeightPulseRespiration RateTemperature
Treatment (Itraconazole)14.30000

[back to top]

Number of Patients Who Achieve a Greater Than or Equal to 50% Decline in Serum Prostate Specific Antigen (PSA)

The number of patients with biochemically relapsed disease after prior definitive local therapy who achieve a ≥ 50% decline from baseline in serum PSA after 12 weeks of therapy with itraconazole, confirmed by repeat measurement at least 2 weeks later. (NCT01787331)
Timeframe: At 12 weeks after start of treatment

InterventionParticipants (Count of Participants)
Treatment (Itraconazole)1

[back to top]

Percentage of Participants With Treatment-related, Clinical Laboratory Adverse Events

All patients who receive at least one dose of study drug will be analyzed for safety endpoints. All adverse events will be graded and classified according to the NCI Common Terminology Criteria for Adverse Events (CTCAE) v. 4.. Percentage of patients with grade 1 or higher, treatment-related adverse events based on the following labs will be reported: potassium, sodium, alkaline phosphatase, total bilirubin, alanine aminotransferase (ALT), aspartate aminotransferase (AST), Hematocrit, Hemoglobin, platelets, white blood cells, atypical lymphs, basophils, eosinophils, monocytes, neutrophils, blood urea nitrogen, and creatinine. (NCT01787331)
Timeframe: Up to 2 years

Interventionpercentage of participants (Number)
PotassiumAlanine aminotransferaseSodiumAlkaline phosphataseTotal bilirubinAspartate aminotransferaseHematocritHemoglobinPlateletsWhite blood cellsAtypical lymphsBasophilsEosinophilsMonocytesNeutrophilsBlood urea nitrogenCreatinine
Treatment (Itraconazole)9.524.76000000000000000

[back to top]

AUC0-∞ of Atorvastatin (Statins Part)

"Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞) of atorvastatin after single dose administration. Outcome measure for the statins part of this trial, treatment sequence C_D.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of atorvastatin on Day 1 of both periods.

Interventionng*h/mL (Geometric Mean)
Atorvastatin13.7
Atorvastatin+Faldaprevir129.0

[back to top]

AUC0-∞ of Rosuvastatin (Statins Part)

"Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞) of rosuvastatin after single dose administration of rosuvastatin. Outcome measure for the statins part of this trial, treatment sequence E_F.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of rosuvastatin on Day 1 of both periods

Interventionng*h/mL (Geometric Mean)
Rosuvastatin24.9
Rosuvastatin+Faldaprevir365.0

[back to top]

AUC0-tz of Atorvastatin

"Area under the plasma concentration-time curve of the analyte over the time interval from 0 to the time tz of the last measurable concentration (AUC0-tz) of atorvastatin. Outcome measure for the statins part of this trial, treatment sequence C_D.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of atorvastatin on Day 1 of both periods

Interventionng*h/mL (Geometric Mean)
Atorvastatin9.5
Atorvastatin+Faldaprevir129.6

[back to top]

AUC0-tz of Rosuvastatin

"Area under the plasma concentration-time curve of the analyte over the time interval from 0 to the time tz of the last measurable concentration (AUC0-tz) of rosuvastatin. Outcome measure for the statins part of this trial, treatment sequence E_F.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of rosuvastatin on Day 1 of both periods

Interventionng*h/mL (Geometric Mean)
Rosuvastatin21.5
Rosuvastatin+Faldaprevir361.0

[back to top]

AUCτ,ss (Itraconazole Part)

Area under the concentration-time curve of the analyte in plasma at steady state over the dosing interval τ (AUCτ,ss) of faldaprevir. Outcome measure for the itraconazole part (treatment sequence A_B) of this trial. The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities. (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00 h (hours) after administration of faldaprevir on Day 1 of both periods

Interventionng*h/mL (Geometric Mean)
Faldaprevir29900
Faldaprevir+Itraconazole59500

[back to top]

AUCτ,ss of Faldaprevir (Statins Part)

Area under the concentration-time curve of the analyte in plasma at steady state over the dosing interval τ (AUCτ,ss) of faldaprevir. Outcome measure for the statins part of this trial, treatment sequences C_D and E_F. (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of rosuvastatin/atorvastatin on Day 1 of the second periods of each treatment sequence.

Interventionng*h/mL (Geometric Mean)
Atorvastatin+Faldaprevir145000
Rosuvastatin+Faldaprevir136000

[back to top]

Cmax of Atorvastatin (Statins Part)

"Maximum measured concentration of the analyte in plasma of atorvastatin (Cmax). Outcome measure for the statins part of this trial, treatment sequence C_D.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of atorvastatin on Day 1 of both periods

Interventionng/mL (Geometric Mean)
Atorvastatin0.94
Atorvastatin+Faldaprevir31.10

[back to top]

Cmax of Rosuvastatin

"Maximum measured concentration of the analyte in plasma of rosuvastatin (Cmax). Outcome measure for the statins part of this trial, treatment sequence E_F.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of rosuvastatin on Day 1 of both periods

Interventionng/mL (Geometric Mean)
Rosuvastatin2.73
Rosuvastatin+Faldaprevir89.6

[back to top]

Cmax,ss (Itraconazole Part)

"Maximum measured concentration of the analyte in plasma at steady state over the dosing interval (Cmax,ss) of faldaprevir. Outcome measure for the itraconazole part (Treatment sequence A_B) of this trial.~The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00 h after administration of faldaprevir on Day 1 of both periods.

Interventionng/mL (Geometric Mean)
Faldaprevir2780
Faldaprevir+Itraconazole5030

[back to top]

Cmax,ss of Faldaprevir (Statins Part)

Maximum measured concentration of the analyte in plasma at steady state over the dosing interval (Cmax,ss) of faldaprevir. Outcome measure for the statins part of this trial, treatment sequences C_D and E_F. (NCT01795937)
Timeframe: -1:30, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 48:00, 60:00 h after administration of rosuvastatin/atorvastatin on Day 1 of the second periods of each treatment sequence.

Interventionng/mL (Geometric Mean)
Atorvastatin+Faldaprevir12900
Rosuvastatin+Faldaprevir12200

[back to top]

Number of Participants With Clinical Efficacy

Clinical efficacy was assessed as cured: the signs and symptoms of invasive fungal infections (IFI) completely disappeared or full or nearby resolution of radiographic manifestations; markedly improved: the signs and symptoms of IFI were improved or disappeared and at least 50 percent improvement of radiographic findings; improved: the signs and symptoms of IFI were moderately improved and less than 50 percent improvement of radiographic findings; failed: the clinical symptoms and signs of IFI were not changed or worsened. (NCT01823289)
Timeframe: Week 6

Interventionparticipants (Number)
CuredMarkedly ImprovedImprovedFailed
Itraconazole Sequential Therapy829185

[back to top]

Number of Participants With Comprehensive Efficacy

Comprehensive efficacy was assessed as cured: the symptoms, signs, laboratory examination and pathogenic examination were return to normal; markedly improved: the disease condition was markedly improved but symptoms, signs, laboratory examination and pathogenic examination were not return to normal; improved: the disease condition was improved to some extent after drug administration, but the improvement was not significant enough; failed: the disease condition was not improved significantly or worsened after drug administration. (NCT01823289)
Timeframe: Week 6

Interventionparticipants (Number)
CuredMarkedly ImprovedImprovedFailed
Itraconazole Sequential Therapy832164

[back to top]

Number of Participants With Mycological Efficacy

Mycological efficacy was assessed as fungi cleared: negative for fungal microscopic examination and culture (test for infection or organisms that could cause infection); fungi not cleared: positive for fungal microscopic examinations and/or culture. (NCT01823289)
Timeframe: Week 6

Interventionparticipants (Number)
Fungi clearedFungi not cleared
Itraconazole Sequential Therapy2010

[back to top]

Tmax of Itraconazole and Hydroxy-Itraconazole

Time to reach maximum observed plasma concentration of itraconazole and its metabolite hydroxy-itraconazole was assessed using a model independent approach. (NCT01929876)
Timeframe: Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionhours (Median)
ItraconazoleHydroxy-Itraconazole
Cobimetinib + Itraconazole2.004.00

[back to top]

Time to Reach Maximum Observed Plasma Concentration (Tmax) of Cobimetinib With and Without Itraconazole

Time to reach maximum observed plasma concentration of cobimetinib with and without itraconazole was assessed using a model independent approach. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionhours (Median)
Period1: Cobimetinib AlonePeriod 2: Cobimetinib With Itraconazole
Cobimetinib + Itraconazole2.004.00

[back to top]

Plasma Half-Life (t1/2) of Cobimetinib With and Without Itraconazole

Plasma half-life is the time measured for the plasma concentration to decrease by one half. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionhours (Median)
Period1: Cobimetinib Alone (n=14)Period 2: Cobimetinib With Itraconazole (n=12)
Cobimetinib + Itraconazole58.6118

[back to top]

Maximum Observed Plasma Concentration (Cmax) of Cobimetinib With and Without Itraconazole

Maximum observed plasma concentration of cobimetinib with and without itraconazole was assessed using a model independent approach. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Period 1: Cobimetinib AlonePeriod 2: Cobimetinib With Itraconazole
Cobimetinib + Itraconazole5.2116.5

[back to top]

Cmax of Itraconazole and Hydroxy-Itraconazole

Maximum observed plasma concentration of itraconazole and its metabolite hydroxy-itraconazole was assessed using a model independent approach. (NCT01929876)
Timeframe: Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionng/mL (Geometric Mean)
ItraconazoleHydroxy-Itraconazole
Cobimetinib + Itraconazole14801243

[back to top]

Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-t)] of Cobimetinib With and Without Itraconazole

AUC (0-t) = Area under the plasma concentration versus time curve from time zero (predose) to time of last quantifiable concentration (0-t) of cobimetinib with and without itraconazole was assessed. It was calculated using the linear trapezoidal rule for increasing concentrations and the logarithmic rule for decreasing concentrations using a model independent approach. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
Period 1: Cobimetinib AlonePeriod 2: Cobimetinib With Itraconazole
Cobimetinib + Itraconazole2091220

[back to top]

Area Under the Curve From Time Zero to 24 Hours [AUC (0-24)] of Itraconazole and Hydroxy-Itraconazole

AUC (0-24) = Area under the plasma concentration versus time curve from time zero (predose) to 24 hours postdose (0-24) of itraconazole and its metabolite hydroxy-itraconazole was assessed using a model independent approach. (NCT01929876)
Timeframe: Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24 hours post cobimetinib dose on Day 4

Interventionng*hr/mL (Geometric Mean)
ItraconazoleHydroxy-Itraconazole
Cobimetinib + Itraconazole1560723176

[back to top]

Apparent Volume of Distribution (Vz/F) of Cobimetinib With and Without Itraconazole

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction of drug absorbed. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionliter (L) (Geometric Mean)
Period1: Cobimetinib Alone (n=14)Period 2: Cobimetinib With Itraconazole (n=12)
Cobimetinib + Itraconazole32331065

[back to top]

Apparent Clearance (CL/F) of Cobimetinib With and Without Itraconazole

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated using a model independent approach. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionliter per hour (L/hr) (Geometric Mean)
Period1: Cobimetinib Alone (n=14)Period 2: Cobimetinib With Itraconazole (n=12)
Cobimetinib + Itraconazole41.46.27

[back to top]

Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - Inf)] of Cobimetinib With and Without Itraconazole

AUC (0 - inf) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - inf). It is obtained from AUC (0 - t) plus AUC (t - inf) of cobimetinib with and without itraconazole, assessed using a model independent approach. (NCT01929876)
Timeframe: Period 1: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192 hours postdose on Day 1; Period 2: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 144, 192, 240 hours post cobimetinib dose on Day 4

Interventionng*hr/mL (Geometric Mean)
Period 1: Cobimetinib Alone (n=14)Period 2: Cobimetinib With Itraconazole (n=12)
Cobimetinib + Itraconazole2411596

[back to top]

AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group F: Uprifosbuvir 300 mg (Tablet)10.69.39

[back to top]

AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,,,
Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Groups C & D: Uprifosbuvir 150 mg (Capsule)1.010.935
Groups C & D: Uprifosbuvir 300 mg (Capsule)2.802.42
Groups C & D: Uprifosbuvir 400 mg (Capsule)5.544.59
Groups C & D: Uprifosbuvir 50 mg (Capsule)0.3940.347

[back to top]

AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group A: Uprifosbuvir 300 mg (Cohort 6a)3.623.77

[back to top]

AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group C: Uprifosbuvir 300 mg (Tablet)2.001.82
Group C: Uprifosbuvir 450 mg (Tablet)3.112.88

[back to top]

Cmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

Maximum observed plasma drug concentration was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)63.2
Group A: Uprifosbuvir 25 mg (Cohort 2a)146
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)758
Group A: Uprifosbuvir 300 mg (Cohort 5a)1190
Group A: Uprifosbuvir 50 mg (Cohort 3a)283

[back to top]

Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants, With Itraconazole (Group F)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Day 1Day 7
Group F: Uprifosbuvir 300 mg (Tablet)2.001.00

[back to top]

Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants (Group C)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionhours (Median)
Day 1Day 7
Group C: Uprifosbuvir 300 mg (Tablet)1.000.50
Group C: Uprifosbuvir 450 mg (Tablet)2.000.50

[back to top]

Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Day 1Day 7
Group A: Uprifosbuvir 300 mg (Cohort 6a)0.750.50

[back to top]

Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-infected Participants (Groups C and D)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,,,
Interventionhours (Median)
Day 1Day 7
Groups C & D: Uprifosbuvir 150 mg (Capsule)0.500.50
Groups C & D: Uprifosbuvir 300 mg (Capsule)1.000.50
Groups C & D: Uprifosbuvir 400 mg (Capsule)0.500.50
Groups C & D: Uprifosbuvir 50 mg (Capsule)0.850.97

[back to top]

Tmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionhours (Median)
Day 1Day 7
Group E: Uprifosbuvir 300 mg (Cohort 2e)1.001.00
Group E: Uprifosbuvir 450 mg (Cohort 3e)1.001.00

[back to top]

Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Day 1Day 7
Group F: Uprifosbuvir 300 mg (Tablet)10.004.00

[back to top]

Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionhours (Median)
Day 1Day 7
Group C: Uprifosbuvir 300 mg (Tablet)4.004.00
Group C: Uprifosbuvir 450 mg (Tablet)4.004.00

[back to top]

Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Day 1Day 7
Group A: Uprifosbuvir 300 mg (Cohort 6a)3.002.50

[back to top]

Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,,,
Interventionhours (Median)
Day 1Day 7
Groups C & D: Uprifosbuvir 150 mg (Capsule)3.002.00
Groups C & D: Uprifosbuvir 300 mg (Capsule)3.003.00
Groups C & D: Uprifosbuvir 400 mg (Capsule)4.004.00
Groups C & D: Uprifosbuvir 50 mg (Capsule)4.002.00

[back to top]

Tmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1,HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionhours (Median)
Day 1Day 7
Group E: Uprifosbuvir 300 mg (Cohort 2e)3.002.00
Group E: Uprifosbuvir 450 mg (Cohort 3e)4.004.00

[back to top]

AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group F: Uprifosbuvir 300 mg (Tablet)13.223.8

[back to top]

AUC0-t of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group E: Uprifosbuvir 300 mg (Cohort 2e)3.192.31
Group E: Uprifosbuvir 450 mg (Cohort 3e)4.213.51

[back to top]

Reduction in HCV RNA From Baseline on Day 8 Following Uprifosbuvir 50-450 mg for 7 Days in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

Reduction in HCV RNA from baseline on Day 8 following uprifosbuvir 50-450 mg for 7 Days in Genotype 1, 2 and 3, HCV-infected participants was obtained. (NCT01974687)
Timeframe: Baseline and Day 8

,,,,,,
Interventionlog10 IU/mL (Mean)
BaselineDay 8
Groups C & D: Placebo (Pooled)6.270.42
Groups C & D: Uprifosbuvir 150 mg (Capsule)6.002.49
Groups C & D: Uprifosbuvir 300 mg (Capsule)6.164.22
Groups C & D: Uprifosbuvir 300 mg (Tablet)5.923.34
Groups C & D: Uprifosbuvir 400 mg (Capsule)6.114.39
Groups C & D: Uprifosbuvir 450 mg (Tablet)5.974.50
Groups C & D: Uprifosbuvir 50 mg (Capsule)5.820.78

[back to top]

Percentage of Participants Who Experienced at Least One Treatment-emergent Grade 1, 2, 3, 4 or 5 Laboratory Abnormality

Laboratory abnormalities were graded using the Division of AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events. Treatment-emergent AEs (TEAEs)were graded as: Grade 1: Mild TEAE as Worst Severity; Grade 2: Moderate TEAE as Worst Severity; Grade 3: Severe TEAE as Worst Severity; Grade 4: Potentially Life-Threatening TEAE as Worst Severity; Grade 5: TEAE Leading to Death. The percentage of participants who experienced at least one Grade 1, 2, 3, 4 or 5 laboratory abnormality is presented. (NCT01974687)
Timeframe: Up to 42 days

,,,,,,,,,,,,,,,,,,,,,,,,
InterventionPercentage of Participants (Number)
Grade 1Grade 2Grade 3Grade 4Grade 5
Group A: Placebo (Cohort 1a-Cohort 5a - Pooled)50.000.00.00.00.0
Group A: Placebo (Cohort 6a)50.00.00.00.00.0
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.00.00.00.00.0
Group A: Uprifosbuvir 150 mg (Cohort 4a) (Fasted and Fed)50.016.70.00.00.0
Group A: Uprifosbuvir 25 mg (Cohort 2a)16.716.70.00.00.0
Group A: Uprifosbuvir 300 mg (Cohort 5a)33.316.70.00.00.0
Group A: Uprifosbuvir 300 mg (Cohort 6a)33.30.00.00.00.0
Group A: Uprifosbuvir 50 mg (Cohort 3a)16.716.70.00.00.0
Group B: Uprifosbuvir 10 mg (Cohort 1b)0.00.033.30.00.0
Group B: Uprifosbuvir 150 mg (Cohort 4b)66.70.00.00.00.0
Group B: Uprifosbuvir 25 mg (Cohort 2b)66.70.00.00.00.0
Group B: Uprifosbuvir 300 mg (Cohort 5b)66.733.30.00.00.0
Group B: Uprifosbuvir 50 mg (Cohort 3b)33.30.00.00.00.0
Group E: Uprifosbuvir 150 mg (Cohort 1e)0.00.00.00.00.0
Group E: Uprifosbuvir 300 mg (Cohort 2e)100.00.00.00.00.0
Group E: Uprifosbuvir 450 mg (Cohort 3e)12.537.512.50.00.0
Group F: Uprifosbuvir 300 mg (Tablet)0.037.50.00.00.0
Groups C & D: Placebo (Pooled)33.333.30.00.00.0
Groups C & D: Uprifosbuvir 150 mg (Capsule)60.00.010.00.00.0
Groups C & D: Uprifosbuvir 250 mg (Capsule)37.550.00.00.00.0
Groups C & D: Uprifosbuvir 300 mg (Capsule)33.35.65.60.00.0
Groups C & D: Uprifosbuvir 300 mg (Tablet)37.537.50.00.00.0
Groups C & D: Uprifosbuvir 400 mg (Capsule)0.062.50.00.00.0
Groups C & D: Uprifosbuvir 450 mg (Tablet)25.025.00.012.50.0
Groups C & D: Uprifosbuvir 50 mg (Capsule)45.518.29.10.00.0

[back to top]

Maximum Reduction in log10 HCV RNA From Baseline - Normal Participants (From Groups B and C) vs. Mild Hepatic Impairment Participants (Group E)

Reduction in HCV RNA from baseline on Day 8 following uprifosbuvir 50-450 mg for 7 Days in Genotype (Gt) 1, HCV-infected participants was obtained. (NCT01974687)
Timeframe: Baseline and 28 days after last dose of study drug (Up to 42 days)

,
Interventionlog10 IU/mL (Mean)
BaselineNormal hepatic fcn: Gt1aMild hepatic impairment: Gt1aNormal hepatic fcn: Gt1bMild hepatic impairment: Gt1bNormal hepatic fcn: Gt1 (pooled 1a+1b)Mild hepatic impairment;Gt1 (pooled 1a+1b)
Group C: Uprifosbuvir 300 mg (Capsule)6.164.822.923.823.594.193.15
Group E: Uprifosbuvir 450 mg6.145.063.604.283.084.503.16

[back to top]

Maximum Reduction in log10 HCV RNA From Baseline - Normal Participants (From Groups B and C) vs. Mild Hepatic Impairment Participants (Group E)

Reduction in HCV RNA from baseline on Day 8 following uprifosbuvir 50-450 mg for 7 Days in Genotype (Gt) 1, HCV-infected participants was obtained. (NCT01974687)
Timeframe: Baseline and 28 days after last dose of study drug (Up to 42 days)

Interventionlog10 IU/mL (Mean)
BaselineNormal hepatic fcn: Gt1aNormal hepatic fcn: Gt1bMild hepatic impairment: Gt1bNormal hepatic fcn: Gt1 (pooled 1a+1b)Mild hepatic impairment;Gt1 (pooled 1a+1b)
Group B: Uprifosbuvir 150 mg (Cohort 4b)5.910.961.351.361.151.36

[back to top]

Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group C: Uprifosbuvir 300 mg (Tablet)618537
Group C: Uprifosbuvir 450 mg (Tablet)778717

[back to top]

Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group A: Uprifosbuvir 300 mg (Cohort 6a)23002320

[back to top]

Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

Maximum observed plasma drug concentration was obtained. All participants were fasted. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,,,
Interventionnmol/L (Geometric Mean)
Day 1Day 7
Groups C & D: Uprifosbuvir 150 mg (Capsule)524587
Groups C & D: Uprifosbuvir 300 mg (Capsule)13601200
Groups C & D: Uprifosbuvir 400 mg (Capsule)23202490
Groups C & D: Uprifosbuvir 50 mg (Capsule)286199

[back to top]

Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group F: Uprifosbuvir 300 mg (Tablet)21401910

[back to top]

Cmax of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group E: Uprifosbuvir 300 mg (Cohort 2e)14401550
Group E: Uprifosbuvir 450 mg (Cohort 3e)1090929

[back to top]

Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group F: Uprifosbuvir 300 mg (Tablet)7381180

[back to top]

Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group C: Uprifosbuvir 300 mg (Tablet)10101420
Group C: Uprifosbuvir 450 mg (Tablet)12101680

[back to top]

Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group A: Uprifosbuvir 300 mg (Cohort 6a)13101630

[back to top]

Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,,,
Interventionnmol/L (Geometric Mean)
Day 1Day 7
Groups C & D: Uprifosbuvir 150 mg (Capsule)641931
Groups C & D: Uprifosbuvir 300 mg (Capsule)11301420
Groups C & D: Uprifosbuvir 400 mg (Capsule)15601760
Groups C & D: Uprifosbuvir 50 mg (Capsule)298471

[back to top]

Cmax of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionnmol/L (Geometric Mean)
Day 1Day 7
Group E: Uprifosbuvir 300 mg (Cohort 2e)11001550
Group E: Uprifosbuvir 450 mg (Cohort 3e)11801740

[back to top]

Area Under the Plasma Drug Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.0410
Group A: Uprifosbuvir 25 mg (Cohort 2a)0.0837
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)1.67
Group A: Uprifosbuvir 300 mg (Cohort 5a)2.78
Group A: Uprifosbuvir 50 mg (Cohort 3a)0.246

[back to top]

AUC0-inf of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group E: Uprifosbuvir 150 mg (Cohort 1e)1.05

[back to top]

AUC0-inf of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)17.9

[back to top]

AUC0-inf of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group B: Uprifosbuvir 10 mg (Cohort 1b)2.26
Group B: Uprifosbuvir 25 mg (Cohort 2b)5.78
Group B: Uprifosbuvir 50 mg (Cohort 3b)7.31
Group B: Uprifosbuvir 150 mg (Cohort 4b)17.5
Group B: Uprifosbuvir 300 mg (Cohort 5b)33.4

[back to top]

AUC0-inf of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

Area under the drug concentration-time curve from time zero to infinity for M6, a metabolite of uprifosbuvir, estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)1.68
Group A: Uprifosbuvir 25 mg (Cohort 2a)5.01
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)19.8
Group A: Uprifosbuvir 300 mg (Cohort 5a)29.7
Group A: Uprifosbuvir 50 mg (Cohort 3a)8.77

[back to top]

AUC0-t of Uprifosbuvir After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group E: Uprifosbuvir 150 mg (Cohort 1e)1.05

[back to top]

AUC0-t of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)1.05

[back to top]

AUC0-t of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)

AUC0-t was calculated using linear log trapezoidal summation from time zero to last measurable concentration. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Group B: Uprifosbuvir 10 mg (Cohort 1b)0.0640
Group B: Uprifosbuvir 25 mg (Cohort 2b)0.228
Group B: Uprifosbuvir 50 mg (Cohort 3b)0.341
Group B: Uprifosbuvir 150 mg (Cohort 4b)1.17
Group B: Uprifosbuvir 300 mg (Cohort 5b)1.39

[back to top]

Cmax of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group E: Uprifosbuvir 150 mg (Cohort 1e)597

[back to top]

Cmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)509

[back to top]

Cmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group B: Uprifosbuvir 10 mg (Cohort 1b)55.0
Group B: Uprifosbuvir 25 mg (Cohort 2b)170
Group B: Uprifosbuvir 50 mg (Cohort 3b)279
Group B: Uprifosbuvir 150 mg (Cohort 4b)710
Group B: Uprifosbuvir 300 mg (Cohort 5b)1210

[back to top]

Cmax of Uprifosbuvir After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group E: Uprifosbuvir 150 mg (Cohort 1e)613

[back to top]

Cmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)293

[back to top]

Cmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)

Maximum observed plasma drug concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group B: Uprifosbuvir 10 mg (Cohort 1b)43.6
Group B: Uprifosbuvir 25 mg (Cohort 2b)122
Group B: Uprifosbuvir 50 mg (Cohort 3b)168
Group B: Uprifosbuvir 150 mg (Cohort 4b)510
Group B: Uprifosbuvir 300 mg (Cohort 5b)667

[back to top]

Cumulative Urine Excretion of Unchanged M6 in Healthy Participants (Group A)

Cumulative urine excretion of unchanged M6 in healthy participants was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionumol (Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)5.93
Group A: Uprifosbuvir 25 mg (Cohort 2a)15.2
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)101
Group A: Uprifosbuvir 300 mg (Cohort 5a)200
Group A: Uprifosbuvir 50 mg (Cohort 3a)31.8

[back to top]

Cumulative Urine Excretion of Unchanged Uprifosbuvir in Healthy Participants (Group A)

Cumulative urine excretion of unchanged MK-3682 in healthy participants was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionumol (Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.280
Group A: Uprifosbuvir 25 mg (Cohort 2a)0.586
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)7.73
Group A: Uprifosbuvir 300 mg (Cohort 5a)13.1
Group A: Uprifosbuvir 50 mg (Cohort 3a)1.56

[back to top]

Maximum (Peak) Observed Plasma Drug Concentration (Cmax) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

Maximum observed plasma drug concentration was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionnmol/L (Geometric Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)29.6
Group A: Uprifosbuvir 25 mg (Cohort 2a)47.7
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)1120
Group A: Uprifosbuvir 300 mg (Cohort 5a)1530
Group A: Uprifosbuvir 50 mg (Cohort 3a)119

[back to top]

Observed Terminal Half-Life (t1/2) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.839
Group A: Uprifosbuvir 25 mg (Cohort 2a)0.872
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)1.05
Group A: Uprifosbuvir 300 mg (Cohort 5a)1.13
Group A: Uprifosbuvir 50 mg (Cohort 3a)0.979

[back to top]

Percentage of Participants Who Discontinued Study Drug Due to a Treatment-emergent AE

The percentage of participants who discontinued study drug due to an AE is presented. (NCT01974687)
Timeframe: Up to 14 days

InterventionPercentage of Participants (Number)
Group A: Placebo (Cohort 1a-Cohort 5a - Pooled)0.0
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.0
Group A: Uprifosbuvir 25 mg (Cohort 2a)0.0
Group A: Uprifosbuvir 50 mg (Cohort 3a)0.0
Group A: Uprifosbuvir 150 mg (Cohort 4a) (Fasted and Fed)0.0
Group A: Uprifosbuvir 300 mg (Cohort 5a)0.0
Group A: Uprifosbuvir 300 mg (Cohort 6a)0.0
Group A: Placebo (Cohort 6a)0.0
Group B: Uprifosbuvir 10 mg (Cohort 1b)0.0
Group B: Uprifosbuvir 25 mg (Cohort 2b)0.0
Group B: Uprifosbuvir 50 mg (Cohort 3b)0.0
Group B: Uprifosbuvir 150 mg (Cohort 4b)0.0
Group B: Uprifosbuvir 300 mg (Cohort 5b)0.0
Groups C & D: Uprifosbuvir 50 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 150 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 250 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 300 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 400 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 300 mg (Tablet)0.0
Groups C & D: Uprifosbuvir 450 mg (Tablet)0.0
Groups C & D: Placebo (Pooled)0.0
Group E: Uprifosbuvir 150 mg (Cohort 1e)0.0
Group E: Uprifosbuvir 300 mg (Cohort 2e)0.0
Group E: Uprifosbuvir 450 mg (Cohort 3e)0.0
Group F: Uprifosbuvir 300 mg (Tablet)0.0

[back to top]

Percentage of Participants Who Experienced a Treatment-emergent Dose-limiting Toxicity (DLT)

A DLT was defined as any of the following events: Any SAE considered by the investigator to be at least reasonably or possibly related to study drug; Any Grade 3 clinical AE considered by the investigator to be at least reasonably or possibly related to study drug; Any Grade 3 confirmed laboratory abnormalities considered by the investigator to be at least reasonably or possibly related to study drug, except for asymptomatic Grade ¾ cholesterol and triglyceride; Any clinical or laboratory AE of any intensity that is considered by the investigator to be at least reasonably or possibly related to study drug that necessitates permanent discontinuation of study drug; Confirmed increase in QT interval corrected for heart rate using Fridericia's (QTcF) formula ≥60 msec over Baseline or an absolute QTcF ≥500 msec. (NCT01974687)
Timeframe: Up to 13 days

InterventionPercentage of Participants (Number)
Group A: Placebo (Cohort 1a-Cohort 5a - Pooled)0.0
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.0
Group A: Uprifosbuvir 25 mg (Cohort 2a)0.0
Group A: Uprifosbuvir 50 mg (Cohort 3a)0.0
Group A: Uprifosbuvir 150 mg (Cohort 4a) (Fasted and Fed)0.0
Group A: Uprifosbuvir 300 mg (Cohort 5a)0.0
Group A: Uprifosbuvir 300 mg (Cohort 6a)0.0
Group A: Placebo (Cohort 6a)0.0
Group B: Uprifosbuvir 10 mg (Cohort 1b)0.0
Group B: Uprifosbuvir 25 mg (Cohort 2b)0.0
Group B: Uprifosbuvir 50 mg (Cohort 3b)0.0
Group B: Uprifosbuvir 150 mg (Cohort 4b)0.0
Group B: Uprifosbuvir 300 mg (Cohort 5b)0.0
Groups C & D: Uprifosbuvir 50 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 150 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 250 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 300 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 400 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 300 mg (Tablet)0.0
Groups C & D: Uprifosbuvir 450 mg (Tablet)0.0
Groups C & D: Placebo (Pooled)0.0
Group E: Uprifosbuvir 150 mg (Cohort 1e)0.0
Group E: Uprifosbuvir 300 mg (Cohort 2e)0.0
Group E: Uprifosbuvir 450 mg (Cohort 3e)0.0
Group F: Uprifosbuvir 300 mg (Tablet)0.0

[back to top]

Percentage of Participants Who Experienced at Least One Treatment-emergent Adverse Event (AE)

An AE was defined as any untoward medical occurrence in a participant administered study drug, and that does not necessarily have a causal relationship with the study drug(s). An AE can be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug(s), whether or not related to study drug(s). The percentage of participants who experienced at least one AE is presented. (NCT01974687)
Timeframe: Up to 42 days

InterventionPercentage of Participants (Number)
Group A: Placebo (Cohort 1a-Cohort 5a - Pooled)50.0
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.0
Group A: Uprifosbuvir 25 mg (Cohort 2a)33.3
Group A: Uprifosbuvir 50 mg (Cohort 3a)33.3
Group A: Uprifosbuvir 150 mg (Cohort 4a) (Fasted and Fed)66.7
Group A: Uprifosbuvir 300 mg (Cohort 5a)50.0
Group A: Uprifosbuvir 300 mg (Cohort 6a)33.3
Group A: Placebo (Cohort 6a)50.0
Group B: Uprifosbuvir 10 mg (Cohort 1b)33.3
Group B: Uprifosbuvir 25 mg (Cohort 2b)66.7
Group B: Uprifosbuvir 50 mg (Cohort 3b)33.3
Group B: Uprifosbuvir 150 mg (Cohort 4b)66.7
Group B: Uprifosbuvir 300 mg (Cohort 5b)66.7
Groups C & D: Uprifosbuvir 50 mg (Capsule)72.7
Groups C & D: Uprifosbuvir 150 mg (Capsule)70.0
Groups C & D: Uprifosbuvir 250 mg (Capsule)87.5
Groups C & D: Uprifosbuvir 300 mg (Capsule)44.4
Groups C & D: Uprifosbuvir 400 mg (Capsule)62.5
Groups C & D: Uprifosbuvir 300 mg (Tablet)75.0
Groups C & D: Uprifosbuvir 450 mg (Tablet)62.5
Groups C & D: Placebo (Pooled)66.7
Group E: Uprifosbuvir 150 mg (Cohort 1e)0.0
Group E: Uprifosbuvir 300 mg (Cohort 2e)100.0
Group E: Uprifosbuvir 450 mg (Cohort 3e)62.5
Group F: Uprifosbuvir 300 mg (Tablet)37.5

[back to top]

Percentage of Participants Who Experienced at Least One Treatment-emergent Serious AE (SAE)

An SAE was defined as any untoward medical occurrence that at any dose that: resulted in death, was life threatening, required inpatient hospitalization or prolongation of existing hospitalization, resulted in persistent or significant disability/incapacity, was a congenital anomaly/birth defect, or was an important medical event. The percentage of participants who experienced at least one SAE is presented. (NCT01974687)
Timeframe: Up to 42 days

InterventionPercentage of Participants (Number)
Group A: Placebo (Cohort 1a-Cohort 5a - Pooled)0.0
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.0
Group A: Uprifosbuvir 25 mg (Cohort 2a)0.0
Group A: Uprifosbuvir 50 mg (Cohort 3a)0.0
Group A: Uprifosbuvir 150 mg (Cohort 4a) (Fasted and Fed)0.0
Group A: Uprifosbuvir 300 mg (Cohort 5a)0.0
Group A: Uprifosbuvir 300 mg (Cohort 6a)0.0
Group A: Placebo (Cohort 6a)0.0
Group B: Uprifosbuvir 10 mg (Cohort 1b)0.0
Group B: Uprifosbuvir 25 mg (Cohort 2b)0.0
Group B: Uprifosbuvir 50 mg (Cohort 3b)0.0
Group B: Uprifosbuvir 150 mg (Cohort 4b)0.0
Group B: Uprifosbuvir 300 mg (Cohort 5b)0.0
Groups C & D: Uprifosbuvir 50 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 150 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 250 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 300 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 400 mg (Capsule)0.0
Groups C & D: Uprifosbuvir 300 mg (Tablet)0.0
Groups C & D: Uprifosbuvir 450 mg (Tablet)0.0
Groups C & D: Placebo (Pooled)0.0
Group E: Uprifosbuvir 150 mg (Cohort 1e)0.0
Group E: Uprifosbuvir 300 mg (Cohort 2e)0.0
Group E: Uprifosbuvir 450 mg (Cohort 3e)0.0
Group F: Uprifosbuvir 300 mg (Tablet)0.0

[back to top]

t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group E: Uprifosbuvir 300 mg (Cohort 2e)27.5
Group E: Uprifosbuvir 450 mg (Cohort 3e)26.2

[back to top]

t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Groups C & D: Uprifosbuvir 50 mg (Capsule)25.5
Groups C & D: Uprifosbuvir 150 mg (Capsule)28.9
Groups C & D: Uprifosbuvir 300 mg (Capsule)32.6
Groups C & D: Uprifosbuvir 400 mg (Capsule)35.8

[back to top]

t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group A: Uprifosbuvir 300 mg (Cohort 6a)32.2

[back to top]

t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group C: Uprifosbuvir 300 mg (Tablet)32.4
Group C: Uprifosbuvir 450 mg (Tablet)30.8

[back to top]

t1/2 of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants, With Itraconazole (Group F)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group F: Uprifosbuvir 300 mg (Tablet)38.9

[back to top]

t1/2 of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group E: Uprifosbuvir 150 mg (Cohort 1e)24.0

[back to top]

t1/2 of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)27.1

[back to top]

t1/2 of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group B: Uprifosbuvir 10 mg (Cohort 1b)20.1
Group B: Uprifosbuvir 25 mg (Cohort 2b)21.2
Group B: Uprifosbuvir 50 mg (Cohort 3b)21.7
Group B: Uprifosbuvir 150 mg (Cohort 4b)26.9
Group B: Uprifosbuvir 300 mg (Cohort 5b)28.0

[back to top]

t1/2 of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group A: Uprifosbuvir 10 mg (Cohort 1a)22.5
Group A: Uprifosbuvir 25 mg (Cohort 2a)24.6
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)29.1
Group A: Uprifosbuvir 300 mg (Cohort 5a)28.8
Group A: Uprifosbuvir 50 mg (Cohort 3a)22.9

[back to top]

t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group E: Uprifosbuvir 300 mg (Cohort 2e)1.18
Group E: Uprifosbuvir 450 mg (Cohort 3e)2.38

[back to top]

t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-infected Participants (Groups C and D)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Groups C & D: Uprifosbuvir 50 mg (Capsule)1.04
Groups C & D: Uprifosbuvir 150 mg (Capsule)1.11
Groups C & D: Uprifosbuvir 300 mg (Capsule)154.
Groups C & D: Uprifosbuvir 400 mg (Capsule)2.58

[back to top]

t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants (Group C)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group C: Uprifosbuvir 300 mg (Tablet)2.50
Group C: Uprifosbuvir 450 mg (Tablet)3.64

[back to top]

t1/2 of Uprifosbuvir After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-infected Participants, With Itraconazole (Group F)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group F: Uprifosbuvir 300 mg (Tablet)4.30

[back to top]

t1/2 of Uprifosbuvir After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group E: Uprifosbuvir 150 mg (Cohort 1e)1.16

[back to top]

t1/2 of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)1.63

[back to top]

t1/2 of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-infected Participants (Group B)

The time measured for the plasma concentration to decrease by one half (t1/2) was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Geometric Mean)
Group B: Uprifosbuvir 10 mg (Cohort 1b)1.36
Group B: Uprifosbuvir 25 mg (Cohort 2b)0.926
Group B: Uprifosbuvir 50 mg (Cohort 3b)1.09
Group B: Uprifosbuvir 150 mg (Cohort 4b)1.11
Group B: Uprifosbuvir 300 mg (Cohort 5b)1.59

[back to top]

Time to Maximum Plasma Concentration (Tmax) of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

Time to maximum plasma concentration was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group A: Uprifosbuvir 10 mg (Cohort 1a)0.80
Group A: Uprifosbuvir 25 mg (Cohort 2a)1.00
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)0.76
Group A: Uprifosbuvir 300 mg (Cohort 5a)0.50
Group A: Uprifosbuvir 50 mg (Cohort 3a)1.00

[back to top]

Tmax of M6 After Single Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group E: Uprifosbuvir 150 mg (Cohort 1e)4.00

[back to top]

Tmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)6.00

[back to top]

Tmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-Infected Participants (Group B)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group B: Uprifosbuvir 10 mg (Cohort 1b)4.00
Group B: Uprifosbuvir 25 mg (Cohort 2b)4.00
Group B: Uprifosbuvir 50 mg (Cohort 3b)2.05
Group B: Uprifosbuvir 150 mg (Cohort 4b)3.52
Group B: Uprifosbuvir 300 mg (Cohort 5b)4.00

[back to top]

Tmax of M6 After Single Dose of Uprifosbuvir as the Capsule Formulation in Healthy Participants (Group A)

Time to maximum plasma concentration was obtained. All participants were fasted. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group A: Uprifosbuvir 10 mg (Cohort 1a)3.01
Group A: Uprifosbuvir 25 mg (Cohort 2a)3.50
Group A: Uprifosbuvir 150 mg (Cohort 4a Fasted)2.53
Group A: Uprifosbuvir 300 mg (Cohort 5a)3.50
Group A: Uprifosbuvir 50 mg (Cohort 3a)4.00

[back to top]

Tmax of Uprifosbuvir After Singe Dose of Uprifosbuvir as Capsule Formulation in Genotype 1, HCV-infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 1e)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group E: Uprifosbuvir 150 mg (Cohort 1e)0.75

[back to top]

Tmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Fed State in Healthy Participants (Group A - Cohort 4a)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group A: Uprifosbuvir 150 mg (Cohort 4a Fed)3.04

[back to top]

Tmax of Uprifosbuvir After Single Dose of Uprifosbuvir as the Capsule Formulation in Genotype 1, HCV-infected Participants (Group B)

Time to maximum plasma concentration was obtained. (NCT01974687)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionhours (Median)
Group B: Uprifosbuvir 10 mg (Cohort 1b)0.50
Group B: Uprifosbuvir 25 mg (Cohort 2b)1.00
Group B: Uprifosbuvir 50 mg (Cohort 3b)1.00
Group B: Uprifosbuvir 150 mg (Cohort 4b)0.76
Group B: Uprifosbuvir 300 mg (Cohort 5b)1.00

[back to top]

AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as Capsule or Tablet Formulation in Genotype 1, HCV-Infected Participants With Mildly Impaired Hepatic Function (Child Pugh Class A) (Group E - Cohort 2e and Cohort 3e)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group E: Uprifosbuvir 300 mg (Cohort 2e)13.417.5
Group E: Uprifosbuvir 450 mg (Cohort 3e)18.426.1

[back to top]

AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Genotype 1, 2 and 3, HCV-Infected Participants (Groups C and D)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,,,
Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Groups C & D: Uprifosbuvir 150 mg (Capsule)8.9412.2
Groups C & D: Uprifosbuvir 300 mg (Capsule)14.419.0
Groups C & D: Uprifosbuvir 400 mg (Capsule)19.424.4
Groups C & D: Uprifosbuvir 50 mg (Capsule)4.747.12

[back to top]

AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Capsule Formulation in Healthy Participants (Group A - Cohort 6a)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group A: Uprifosbuvir 300 mg (Cohort 6a)15.120.6

[back to top]

AUC0-inf of M6 After Multiple Doses of Uprifosbuvir Once-Daily x 7 Days as the Tablet Formulation in Genotype 1, HCV-Infected Participants (Group C)

Area under the drug concentration-time curve from time zero to infinity estimated as AUC0-t + Cest/λz, where λz is the terminal elimination rate constant, calculated for the first dose only. (NCT01974687)
Timeframe: Days 1 & 7: predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 20, 24, 36, 48, 72, 96, and 120 hours postdose

,
Interventionh*umol/L (Geometric Mean)
Day 1Day 7
Group C: Uprifosbuvir 300 mg (Tablet)14.721.4
Group C: Uprifosbuvir 450 mg (Tablet)16.124.7

[back to top]

AUC0-infinity (Area Under the Concentration-time Curve of BI 691751 in Plasma and Whole Blood Over the Time Interval From 0 Extrapolated to Infinity)

AUC0-infinity (area under the concentration-time curve of BI 691751 in plasma and whole blood over the time interval from 0 extrapolated to infinity). (NCT02044393)
Timeframe: from day 1 to 31 days postdose relative to BI 691751 administration time: -2:00, 0:10, 0:20, 0:40, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00, 34:00, 47:00, 71:00, 95:00, 119:00, 143:00, 215:00, 287:00, 383:00, 551:00, 719:00h.

,
Interventionnmol*h/L (Geometric Mean)
in plasmain whole blood
BI 691751316027700
IT + BI 691751236024600

[back to top]

AUC0-tz (Area Under the Concentration-time Curve of BI 691751 in Plasma and Whole Blood Over the Time Interval From 0 up to the Last Quantifiable Concentration)

AUC0-tz: area under the concentration-time curve of BI 691751 in plasma and whole blood over the time interval from 0 up to the last quantifiable concentration. (NCT02044393)
Timeframe: from day 1 to 31 days postdose relative to BI 691751 administration (h:min): -2:00, 0:10, 0:20, 0:40, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00, 34:00, 47:00, 71:00, 95:00, 119:00, 143:00, 215:00, 287:00, 383:00, 551:00, 719:00h.

,
Interventionnmol*h/L (Geometric Mean)
in plasmain whole blood
BI 691751283025000
IT + BI 691751209021600

[back to top]

Cmax (Maximum Measured Concentration of BI 691751 in Plasma and Whole Blood)

Cmax (maximum measured concentration of BI 691751 in plasma and whole blood). (NCT02044393)
Timeframe: From day 1 to 31 days postdose relative to BI 691751 administration (h:min): -2:00, 0:10, 0:20, 0:40, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00, 34:00, 47:00, 71:00, 95:00, 119:00, 143:00, 215:00, 287:00, 383:00, 551:00, 719:00h.

,
Interventionnmol/L (Geometric Mean)
in plasmain whole blood
BI 691751157217
IT + BI 691751150203

[back to top]

Part A: Terminal Phase Elimination Half-life (T1/2) for MLN4924

(NCT02122770)
Timeframe: Days 1 and 8: predose and at multiple time-points (up to 72 hours) postdose for Part A

,,,
Interventionhour (Geometric Mean)
Day 1Day 8
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg9.7411.0
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg9.8810.7
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg11.011.6
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg10.613.3

[back to top] [back to top]

Number of Participants With Clinically Significant Change From Baseline in Body Weight Measurements

(NCT02122770)
Timeframe: Part A: Baseline up to Day 40; Part B: Baseline up to approximately Cycle 29

,,,,,
Interventionparticipants (Number)
Grade 1 AE: 5 < 10% decrease from baselineGrade 2 AE: 10 - <20% decrease from baselineGrade 3 AE: >=20% decrease from baseline
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg000
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg110
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg000
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg000
Part B: MLN4924 + Carboplatin or Paclitaxel100
Part B: MLN4924 + Docetaxel100

[back to top] [back to top]

Part A AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for MLN4924 and MLN4924 + Fluconazole

(NCT02122770)
Timeframe: Day 1 (MLN4924) and Day 8 (MLN4924 + Fluconazole): pre-dose and at multiple time points (up to 72 hours) post-dose

Interventionhour*nanogram per milliliter (h*ng/mL) (Geometric Mean)
Part A: MLN4924 8 mg/m^2445
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg491

[back to top]

Number of Participants Who Experience at Least 1 Treatment-emergent Adverse Event (TEAE) and Serious Adverse Event (SAE)

(NCT02122770)
Timeframe: Baseline up to 30 days after the last dose of study drug (Day 40 for Part A; approximately Cycle 29 for Part B)

,,,,,
InterventionParticipants (Count of Participants)
TEAESAE
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg62
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg185
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg133
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg133
Part B: MLN4924 + Carboplatin or Paclitaxel136
Part B: MLN4924 + Docetaxel2314

[back to top]

Part B: Percentage of Participants With Objective Response

Percentage of participants with objective response based on assessment of complete response (CR) or partial response (PR) according to Response Evaluation Criteria in Solid Tumors (RECIST) v1.1. CR was defined as complete disappearance of all target lesions. All pathological lymph nodes, both target and non-target, must decrease to normal (short axis less than [<]10 millimeter [mm]). PR was defined as at least 30% decrease under baseline of the sum of diameters of all target lesions. (NCT02122770)
Timeframe: Baseline up to symptomatic deterioration, progressive disease (PD), treatment discontinuation, or until the study is stopped (approximately Cycle 29)

Interventionpercentage of participants (Number)
Part B: MLN4924 + Docetaxel10.5
Part B: MLN4924 + Carboplatin or Paclitaxel22.2

[back to top]

Part B: Duration of Response

The duration of response was defined in participants with disease response (CR or PR) as the time between the first documentation of response and progressive disease (PD). Responders without PD will be censored at the last clinical assessment of response. CR was defined as complete disappearance of all target lesions. All pathological lymph nodes, both target and non-target, must decrease to normal (short axis <10 mm). PR was defined as at least 30% decrease under baseline of the sum of diameters of all target lesions. PD was defined as at least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). (NCT02122770)
Timeframe: Time from the date of first documentation of a response and PD (approximately up Cycle 29)

Interventionmonths (Mean)
Part B: MLN4924 + Docetaxel4.07
Part B: MLN4924 + Carboplatin or Paclitaxel8.46

[back to top]

Part A AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for MLN4924 and MLN4924 + Itraconazole

(NCT02122770)
Timeframe: Day 1 (MLN4924) and Day 8 (MLN4924 + Itraconazole): pre-dose and at multiple time points (up to 72 hours) post-dose

Interventionh*ng/mL (Geometric Mean)
Part A: MLN4924 8 mg/m^2465
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg585
Part A: MLN4924 15 mg/m^2798
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg1060
Part A: MLN4924 20 mg/m^21120
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg1130

[back to top]

Part A Cmax: Maximum Observed Plasma Concentration for MLN4924 and MLN4924 + Itraconazole

(NCT02122770)
Timeframe: Day 1 (MLN4924) and Day 8 (MLN4924 + Itraconazole): pre-dose and at multiple time points (up to 72 hours) post-dose

Interventionng/mL (Geometric Mean)
Part A: MLN4924 8 mg/m^259.1
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg66.8
Part A: MLN4924 15 mg/m^2121
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg193
Part A: MLN4924 20 mg/m^2178
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg137

[back to top]

Part A Cmax: Maximum Observed Plasma Concentration for MLN4924 and MLN4924 + Fluconazole

(NCT02122770)
Timeframe: Day 1 (MLN4924) and Day 8 (MLN4924 + Fluconazole): pre-dose and at multiple time points (up to 72 hours) post-dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Part A: MLN4924 8 mg/m^251.6
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg51.0

[back to top]

Part A AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for MLN4924 and MLN4924 + Itraconazole

(NCT02122770)
Timeframe: Day 1 (MLN4924) and Day 8 (MLN4924 + Itraconazole): pre-dose and at multiple time points (up to 72 hours) post-dose

Interventionh*ng/mL (Geometric Mean)
Part A: MLN4924 8 mg/m^2459
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg571
Part A: MLN4924 15 mg/m^2793
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg1030
Part A: MLN4924 20 mg/m^21110
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg1140

[back to top]

Part A: Volume of Distribution (Vz) for MLN4924

(NCT02122770)
Timeframe: Days 1 and 8: predose and at multiple time-points (up to 72 hours) postdose for Part A

,,,
InterventionLiter (L) (Geometric Mean)
Day 1Day 8
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg494421
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg511550
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg503477
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg445445

[back to top]

Part A AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for MLN4924 and MLN4924 + Fluconazole

(NCT02122770)
Timeframe: Day 1 (MLN4924) and Day 8 (MLN4924 + Fluconazole): pre-dose and at multiple time points (up to 72 hours) post-dose

Interventionh*ng/mL (Geometric Mean)
Part A: MLN4924 8 mg/m^2450
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg498

[back to top]

Part A Tmax: Time to Reach the Cmax for MLN4924

(NCT02122770)
Timeframe: Days 1 and 8: predose and at multiple time-points (up to 72 hours) postdose for Part A

,,,
Interventionhour (Median)
Day 1Day 8
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg1.241.03
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg1.051.13
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg1.041.21
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg1.021.50

[back to top]

Part A: Blood to Plasma (B/P) Concentration Ratio for MLN4924

(NCT02122770)
Timeframe: Day 1 up to 24 hours post infusion

,,,
InterventionRatio (Geometric Mean)
End of infusion2 hours post infusion8 hours post infusion24 hours post infusion
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg55.266.570.766.3
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg35.148.856.758.0
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg51.169.271.171.9
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg43.754.773.767.6

[back to top]

Part A: Plasma Clearance (CLp) for MLN4924

(NCT02122770)
Timeframe: Days 1 and 8: predose and at multiple time-points (up to 72 hours) postdose for Part A

,,,
Interventionliter per hour (L/h) (Geometric Mean)
Day 1Day 8
Part A: MLN4924 15 mg/m^2 + Itraconazole 200 mg35.226.5
Part A: MLN4924 20 mg/m^2 + Itraconazole 200 mg35.835.5
Part A: MLN4924 8 mg/m^2 + Fluconazole 400 mg31.728.6
Part A: MLN4924 8 mg/m^2 + Itraconazole 200 mg29.223.2

[back to top]

AUC(0-t) of AZD9291

Pharmacokinetics of AZD9291 by assessment of area under the plasma concentration curve from time zero to last quantifiable dose (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone12260
AZD9291+Itraconazole14520

[back to top]

CL/F of AZD9291

Rate and extent of absorption of AZD9291 by assessment of apparent clearance following oral administration (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionL/h (Geometric Mean)
AZD9291 Alone11.84
AZD9291+Itraconazole9.368

[back to top]

AUC of AZ5104

Pharmacokinetics of AZ5104 (metabolite to AZD9291) by assessment of area under the plasma concentration time curve from zero to infinity (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone1155
AZD9291+Itraconazole941.4

[back to top]

AUC of AZ7550

Pharmacokinetics of AZ7550 (metabolite to AZD9291) by assessment of area under the plasma concentration time curve from zero to infinity (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone624.1
AZD9291+Itraconazole292.1

[back to top]

AUC of AZD9291

Pharmacokinetics of AZD9291 by assessment of area under the plasma concentration time curve from zero to infinity (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone13520
AZD9291+Itraconazole17090

[back to top]

AUC(0-120) of AZD9291

Pharmacokinetics of AZD9291 by assessment of area under the plasma concentration time curve from zero to 120 hours (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone10280
AZD9291+Itraconazole11370

[back to top]

Cmax of AZ5104

Pharmacokinetics of AZ5104 (metabolite to AZD9291) by assessment of maximum plasma AZ5104 concentration (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM (Geometric Mean)
AZD9291 Alone8.568
AZD9291+Itraconazole5.746

[back to top]

Cmax of AZ7550

Pharmacokinetics of AZ7550 (metabolite to AZD9291) by assessment of maximum plasma AZ7550 concentration (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM (Geometric Mean)
AZD9291 Alone4.321
AZD9291+Itraconazole1.897

[back to top]

Cmax of AZD9291

Pharmacokinetics of AZD9291 by assessment of maximum plasma AZD9291 concentration (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionnM (Geometric Mean)
AZD9291 Alone242.5
AZD9291+Itraconazole201.7

[back to top]

t1/2 of AZD9291

Pharmacokinetics of AZD9291 by assessment of the terminal half-life (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

Interventionhours (Geometric Mean)
AZD9291 Alone61.05
AZD9291+Itraconazole78.36

[back to top]

Tmax of AZD9291

Pharmacokinetics of AZD9291 by assessment of time to Cmax (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

Interventionhours (Median)
AZD9291 Alone4.00
AZD9291+Itraconazole6.04

[back to top]

Vz/F of AZD9291

Rate and extent of absorption of AZD9291 by assessment of the apprarent volume of distribution (NCT02157883)
Timeframe: Blood samples collected on Day 1 and Day 10 at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 168, and 216 hours post AZD9291 dose in Part A.

InterventionL (Geometric Mean)
AZD9291 Alone1019
AZD9291+Itraconazole1059

[back to top]

Number of Participants With Clinically Significant Change in Vital Sign Reported as AEs

Vital signs will include body temperature (oral), sitting blood pressure (after the participant has rested for at least 5 minutes), and pulse (bpm). (NCT02259010)
Timeframe: First dose of study drug to 30 days after the last dose of study drug (up to 12 months)

InterventionParticipants (Count of Participants)
PyrexiaPalpitationsTachycardia
Alisertib Without Itraconazole321

[back to top]

Number of Participants With Abnormal Laboratory Values Reported as AEs

Standard safety laboratory tests included Chemistry and Hematology. Abnormal laboratory values that led to discontinuation or delay in treatment, dose modification, therapeutic intervention, or were considered by the investigator to be a clinically significant change from baseline were reported as AEs. (NCT02259010)
Timeframe: First dose of study drug to 30 days after the last dose of study drug (up to 12 months)

InterventionParticipants (Count of Participants)
HypokalemiaElevated blood creatinineIncreased international normalized ratioHypercalcemiaHypomagnesemiaHypoalbuminemiaDecreased blood potassiumDecreased blood sodiumElevated blood alkaline phosphataseAnemiaNeutropeniaLeukopeniaThrombocytopeniaDecreased lymphocyte countDecreased white blood cell countDecreased platelet count
Part A: Alisertib 30 mg+Itraconazole; Part B: Alisertib 50 mg3321111115422211

[back to top]

Cmax: Maximum Observed Plasma Concentration for Alisertib Metabolites M1 and M2 in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

,
Interventionnmol/L (Mean)
Metabolite 1 (M1)Metabolite 2 (M2)
Alisertib With Itraconazole450.0103.5
Alisertib Without Itraconazole409.4114.0

[back to top]

AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Alisertib Metabolites M1 and M2 in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

,
Interventionhr*nmol/L (Mean)
Metabolite 1 (M1)Metabolite 2 (M2)
Alisertib With Itraconazole15776.15081.6
Alisertib Without Itraconazole10550.85880.6

[back to top]

Tmax: Time to Reach Maximum Plasma Concentration of Alisertib in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

Interventionhr (Median)
Alisertib Without Itraconazole2.920
Alisertib With Itraconazole2.920

[back to top]

Number of Participants With Clinically Significant Change in Weight Reported as AEs

Change relative to baseline in participant's weight measured throughout study. (NCT02259010)
Timeframe: First dose of study drug to 30 days after the last dose of study drug (up to 12 months)

InterventionParticipants (Count of Participants)
Part A: Alisertib 30 mg+Itraconazole; Part B: Alisertib 50 mg2

[back to top]

Cmax: Maximum Observed Concentration of Alisertib in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

Interventionnmol/L (Mean)
Alisertib Without Itraconazole1060.3
Alisertib With Itraconazole1002.8

[back to top]

CL/F: Oral Clearance of Alisertib in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

InterventionL/hr (Mean)
Alisertib Without Itraconazole4.416
Alisertib With Itraconazole3.177

[back to top]

AUC∞: Area Under the Plasma Concentration Curve From Time 0 to Infinity of Alisertib in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

Interventionhr*nmol/L (Mean)
Alisertib Without Itraconazole16804.6
Alisertib With Itraconazole23488.7

[back to top]

AUC(Last): Area Under the Plasma Concentration Curve From Time 0 to the Time of the Last Quantifiable Concentration of Alisertib in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

Interventionhr*nmol/L (Mean)
Alisertib Without Itraconazole15541.6
Alisertib With Itraconazole20219.5

[back to top]

Terminal Phase Elimination Half-Life of Alisertib in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

Interventionhr (Mean)
Alisertib Without Itraconazole22.55
Alisertib With Itraconazole25.37

[back to top]

Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An AE is considered any unfavorable and unintended sign, symptom, or disease associated with the use of the study drug, whether or not considered related to the study drug. Preexisting conditions that worsened during the study were reported as adverse events. A SAE is any experience that suggests a significant hazard, contraindication, side effect or precaution that: results in death, is life-threatening, required in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or is medically significant. A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug. (NCT02259010)
Timeframe: First dose of study drug to 30 days after the last dose of study drug (up to 12 months)

InterventionParticipants (Count of Participants)
AEsSAEs
Part A: Alisertib 30 mg+Itraconazole; Part B: Alisertib 50 mg2412

[back to top]

Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Alisertib Metabolites M1 and M2 in Presence and Absence of Itraconazole in Part A

(NCT02259010)
Timeframe: Day 1 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib without itraconazole arm; Day 10 pre-dose and at multiple time points (up to 96 hours) post-dose in Cycle 1 for alisertib with itraconazole arm

,
Interventionhr (Median)
Metabolite 1 (M1)Metabolite 2 (M2)
Alisertib With Itraconazole3.80023.600
Alisertib Without Itraconazole3.0909.360

[back to top]

Number of Participants With Adverse Events During Time Frame of Taking Medication/Placebo

Adverse events during time frame of taking medication/placebo (NCT02285283)
Timeframe: 24 weeks

InterventionParticipants (Count of Participants)
Placebo0
Itraconazole0

[back to top]

Number of Participants With Recurrence of Nasal Polyps Requiring Intervention

Recurrence of nasal polyps requiring intervention (NCT02285283)
Timeframe: 48 weeks

InterventionParticipants (Count of Participants)
Placebo3
Itraconazole4

[back to top]

Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2623091

(NCT02300259)
Timeframe: Group 1 (Days 1 and 6) Group 4 (Days 1 and 4): Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours (hr) postdose; additionally for Group 1 (Day 6): 264, 288, 312, 336, 360 hr postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
LY2623091 (Group 1)61.9
Itraconazole + LY2623091 (Group 1)66.9
LY2623091 (Group 4)61.8
Diltiazem + LY2623091 (Group 4)64.2

[back to top]

Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of LY2623091

(NCT02300259)
Timeframe: Group 1 (Days 1 and 6) Group 4 (Days 1 and 4): Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours (hr) postdose; additionally for Group 1 (Day 6): 264, 288, 312, 336, 360 hr postdose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
LY2623091 (Group 1)2540
Itraconazole + LY2623091 (Group 1)5660
LY2623091 (Group 4)2390
Diltiazem + LY2623091 (Group 4)3360

[back to top]

Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of LY2623091

(NCT02300259)
Timeframe: Group 1 (Days 1 and 6) Group 4 (Days 1 and 4): Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours (hr) postdose; additionally for Group 1 (Day 6): 264, 288, 312, 336, 360 hr postdose

Interventionng*hr/mL (Geometric Mean)
LY2623091 (Group 1)2480
Itraconazole + LY2623091 (Group 1)5240
LY2623091 (Group 4)2340
Diltiazem + LY2623091 (Group 4)3130

[back to top]

Pharmacokinetics: Maximum Drug Concentration (Cmax) of Simvastatin and Simvastatin Acid

(NCT02300259)
Timeframe: Days 1 and 12: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 hours postdose

,
Interventionng/mL (Geometric Mean)
SimvastatinSimvastatin Acid
LY2623091 + Simvastatin (Group 2)9.890.877
Simvastatin (Group 2)7.780.720

[back to top]

Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of Simvastatin and Simvastatin Acid

(NCT02300259)
Timeframe: Days 1 and 12: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 hours postdose

,
Interventionng*h/mL (Geometric Mean)
SimvastatinSimvastatin Acid
LY2623091 + Simvastatin24.18.88
Simvastatin (Group 2)17.47.15

[back to top]

Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Simvastatin and Simvastatin Acid

(NCT02300259)
Timeframe: Days 1 and 12: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 hours postdose

,
Interventionng*hr/mL (Geometric Mean)
SimvastatinSimvastatin Acid
LY2623091 + Simvastatin23.06.87
Simvastatin (Group 2)16.55.42

[back to top]

Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 28 days after last dose that were absent before treatment or that worsened relative to pre-treatment state. AEs included both SAEs and non-SAEs. (NCT02319148)
Timeframe: Baseline up to 28 days after last study drug administration

,,,,,,
Interventionparticipants (Number)
AEsSAEs
Diltiazem 240 mg40
Itraconazole 200 mg60
PF-00489791 20 mg180
PF-00489791 20 mg + Diltiazem 240 mg40
PF-00489791 20 mg + Itraconazole 200 mg60
PF-00489791 20 mg + Verapamil 240 mg50
Verapamil 240 mg30

[back to top]

Number of Participants With Potentially Clinically Significant Vital Signs Findings

Vital signs assessment included pulse rate and blood pressure. Criteria for vital sign values meeting potential clinical concern included: supine/sitting pulse rate <40 or >120 beats per minute (bpm), standing pulse rate <40 or >140 bpm; systolic blood pressure (SBP) of >=30 millimeters of mercury (mm Hg) change from baseline in same posture or SBP <90 mm Hg, diastolic blood pressure (DBP) >=20 mmHg change from baseline in same posture or DBP <50 mm Hg. (NCT02319148)
Timeframe: Baseline up to Day 9

,,,
Interventionparticipants (Number)
Supine SBP <90 mm Hg (n=22,7,7,8)Standing SBP <90 mm Hg (n=22,7,6,8)Supine DBP <50 mm Hg (n=22,7,7,8)Standing DBP <50 mm Hg (n=22,7,6,8)Supine Pulse Rate <40 or >120 bpm (n=22,7,7,8)Standing Pulse Rate <40 or >120 bpm (n=22,7,6,8)Supine SBP >=30 mm Hg IFB (n=22,6,6,7)Standing SBP >=30 mm Hg IFB (n=22,6,6,7)Supine DBP >=20 mm Hg IFB (n=22,6,6,7)Standing DBP >=20 mm Hg IFB (n=22,6,6,7)Supine SBP >=30 mm Hg DFB (n=22,6,6,7)Standing SBP >=30 mm Hg DFB (n=22,6,6,7)Supine DBP >=20 mm Hg DFB (n=22,6,6,7)Standing DBP >=20 mm Hg DFB (n=22,6,6,7)
PF-00489791 20 mg00000000000001
PF-00489791 20 mg + Diltiazem 240 mg00000000000101
PF-00489791 20 mg + Itraconazole 200 mg00000000000000
PF-00489791 20 mg + Verapamil 240 mg11010000000101

[back to top]

Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Findings

ECG parameters included PR interval, QRS interval, and corrected QT interval using Fridericia's formula (QTcF). Criteria for ECG changes meeting potential clinical concern included: PR interval greater than or equal to (>=)300 milliseconds (msec) or >=25% increase when baseline is greater than (>)200 msec and >=50% increase when baseline is less than or equal to (≤)200 msec; QRS interval >=140 msec or >=50% increase from baseline (IFB); and QTcF >=450 msec or >=30 msec increase. The number of participants with potentially clinically significant ECG findings at any visit were reported. (NCT02319148)
Timeframe: Pre-dose (Periods 1 and 2), 4, 72 and 96 hours post-dose in Period 2

,,,
Interventionparticipants (Number)
PR Interval >=300 msec (n=22,7,7,8)QRS Complex >=140 msec (n=22,7,7,8)QTcF Interval 450-<480 msec (n=22,7,7,8)QTcF Interval 480-<500 msec (n=22,7,7,8)QTcF Interval >=500 msec (n=22,7,7,8)PR Interval >=25/50% IFB (n=22,6,6,7)QRS Interval >=50% IFB (n=22,6,6,7)QTcF Interval 30-<60 msec IFB (n=22,6,6,7)QTcF Interval >=60 msec IFB (n=22,6,6,7)
PF-00489791 20 mg000000000
PF-00489791 20 mg + Diltiazem 240 mg000000000
PF-00489791 20 mg + Itraconazole 200 mg000000010
PF-00489791 20 mg + Verapamil 240 mg000000000

[back to top]

Number of Participants Who Used at Least 1 Concomitant Medication

Participants were to abstain from all concomitant treatments, except for the treatment of AEs. Treatments taken after the first dose of study treatment were documented as concomitant treatments. (NCT02319148)
Timeframe: Baseline up to Day 15 (final study evaluation)

,,,
Interventionparticipants (Number)
Drug TreatmentsNon-Drug Treatments
PF-00489791 20 mg100
PF-00489791 20 mg + Diltiazem 240 mg40
PF-00489791 20 mg + Itraconazole 200 mg20
PF-00489791 20 mg + Verapamil 240 mg20

[back to top]

Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-00489791

(NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionhour (Median)
PF-00489791 20 mg4.00
PF-00489791 20 mg + Itraconazole 200 mg3.50
PF-00489791 20 mg + Diltiazem 240 mg4.00
PF-00489791 20 mg + Verapamil 240 mg4.00

[back to top]

Number of Participants With Laboratory Abnormalities Meeting the Criteria for Potential Clinical Concern

The following laboratory parameters were analyzed: hematology (hemoglobin, hematocrit, red blood cell [RBC] count, RBC morphology, platelet count, white blood cell [WBC] count, total neutrophils, eosinophils, monocytes, basophils, lymphocytes); blood chemistry (blood urea nitrogen [BUN], creatinine, glucose, calcium, sodium, potassium, chloride, total bicarbonate, aspartate aminotransferase [AST], alanine aminotransferase [ALT], total bilirubin, alkaline phosphatase, uric acid, albumin, and total protein; urinalysis (pH, glucose, protein, blood, ketones, nitrites, leukocyte esterase, microscopy [if urine dipstick was positive for blood, protein, nitrites or leukocyte esterase]); others (coagulation panel, circulating immune complex, and complement activation). (NCT02319148)
Timeframe: Baseline up to 28 days after last study drug administration

Interventionparticipants (Number)
PF-00489791 20 mg3
PF-00489791 20 mg + Itraconazole 200 mg0
PF-00489791 20 mg + Diltiazem 240 mg0
PF-00489791 20 mg + Verapamil 240 mg2

[back to top]

Maximum Observed Plasma Concentration (Cmax) of PF-00489791

(NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
PF-00489791 20 mg1140
PF-00489791 20 mg + Itraconazole 200 mg1238
PF-00489791 20 mg + Diltiazem 240 mg1198
PF-00489791 20 mg + Verapamil 240 mg1186

[back to top]

Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of PF-00489791

AUC is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
PF-00489791 20 mg17880
PF-00489791 20 mg + Itraconazole 200 mg18140
PF-00489791 20 mg + Diltiazem 240 mg16840
PF-00489791 20 mg + Verapamil 240 mg19560

[back to top]

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-00489791

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast). (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionng.hr/mL (Geometric Mean)
PF-00489791 20 mg17580
PF-00489791 20 mg + Itraconazole 200 mg17980
PF-00489791 20 mg + Diltiazem 240 mg16760
PF-00489791 20 mg + Verapamil 240 mg19400

[back to top]

Apparent Volume of Distribution (Vz/F) of PF-00489791

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionliter (Geometric Mean)
PF-00489791 20 mg18.06
PF-00489791 20 mg + Itraconazole 200 mg21.65
PF-00489791 20 mg + Diltiazem 240 mg19.98
PF-00489791 20 mg + Verapamil 240 mg19.23

[back to top]

Apparent Oral Clearance (CL/F) of PF-00489791

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionmilliliter per minute (mL/min) (Geometric Mean)
PF-00489791 20 mg18.64
PF-00489791 20 mg + Itraconazole 200 mg18.37
PF-00489791 20 mg + Diltiazem 240 mg19.81
PF-00489791 20 mg + Verapamil 240 mg17.02

[back to top]

Terminal Elimination Half-Life (t1/2) of PF-00489791

t1/2 is the time measured for the plasma concentration to decrease by one half. (NCT02319148)
Timeframe: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8 and 12 hours after PF-00489791 administration

Interventionhour (Mean)
PF-00489791 20 mg11.39
PF-00489791 20 mg + Itraconazole 200 mg13.85
PF-00489791 20 mg + Diltiazem 240 mg11.75
PF-00489791 20 mg + Verapamil 240 mg13.29

[back to top]

PD Biomarker: Cerebral Spinal Fluid (CSF) Minimum Amyloid-beta Peptide (A-beta) 1-40 Concentration

CSF minimum A-beta 1-40 concentration or nadir concentration (Cnadir) is defined as the lowest concentration of CSF A-beta 1-40 following dose administration. (NCT02323334)
Timeframe: Part B: -4, -2, Predose, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 14, 16, 18, 20, 24, 28, 32, and 36 hours postdose

Interventionpg/mL (Geometric Mean)
Part B Placebo7980
Part B 1.6 mg LY32026265700
Part B 6mg LY32026265770
Part B 26mg LY32026262980

[back to top]

PD Biomarker: Change From Baseline in Cerebrospinal Fluid (CSF) Amyloid-beta Peptide (A-beta) 1-40 Concentration

CSF Aβ1-40 change from baseline at Day 15 endpoint, 24 hours postdose (+/- 4 hours) following multiple doses of LY3202626. (NCT02323334)
Timeframe: Parts C: Baseline, Day 15

Interventionpercent change in concentration (Mean)
Part C Placebo-21.3
Part C 1mg LY3202626-50.1
Part C 6mg LY3202626-75.7
Part C 26mg LY3202626-93.7

[back to top]

Pharmacodynamic(PD) Biomarker: Plasma Minimum Amyloid-Beta Peptide (A-beta) 1-40 Concentration

Plasma minimum A-beta 1-40 concentration or nadir concentration (Cnadir) is defined as the lowest concentration of plasma A-beta 1-40 following dose administration. (NCT02323334)
Timeframe: Part A Day 1: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 120 postdose; Part C Day 14: Predose 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 120, 168, and 216 postdose

InterventionPicogram per milliliter (pg/mL) (Geometric Mean)
Part A Placebo107
Part A 0.1mg LY320262658.1
Part A 0.4mg LY320262661.8
Part A 1.6 mg LY320262633.4
Part A 5mg LY320262625.2
Part A 15mg LY320262617.0
Part A 45mg LY32026267.93
Part C Placebo84.6
Part C 1mg LY3202626 QD24.0
Part C 6mg LY3202626 QD5.80
Part C 26mg LY3202626 QD4.2

[back to top]

Pharmacokinetics (PK): Maximum Drug Concentration (Cmax) of LY3202626

Summary of PK parameters of LY3202626 in plasma following oral administration of single doses for Parts A and B and multiple doses for Part C. (NCT02323334)
Timeframe: Part A and B Day 1:Predose, 0.5,1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 120 hours postdose; Part C Day 1:Predose, 0.5,1, 2, 4, 6, 8, and 12 hours postdose; Part C Day 14:Predose, 0.5,1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, and 216 hours postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Part A 0.1mg LY32026260.169
Part A 0.4mg LY32026260.486
Part A 1.6mg LY32026262.89
Part A 5mg LY32026267.91
Part A 15mg LY320262621.3
Part A 45mg LY320262692.5
Part B 1.6mg LY32026262.90
Part B 10mg LY32026263.75
Part B 26mg LY320262636.1
Part C 1mg LY3202626 QD2.57
Part C 6mg LY3202626 QD11.2
Part C 26mg LY3202626 QD72.8

[back to top]

PK: Area Under the Concentration Time Curve (AUC) of LY3202626

Pharmacokinetic parameters for Part A and B were assessed on Day 1 using AUC 0-infinity (AUC0-inf). Pharmacokinetic parameters for Part C were assessed on Day 1 using AUC zero to time to last (AUC0-tlast), Day 14 using AUC steady state. (NCT02323334)
Timeframe: Part A and B Day 1: Predose, 0.5,1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 120 hours postdose; Part C Day 1:Presdose, 0.5,1, 2, 4, 6, 8,12 hours postdose; Day 14: Predose, 0.5,1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168, and 216 hours postdose

Interventionnanogram x hour/milliliter (ng*hr/mL) (Geometric Mean)
Part A 0.1mg LY3202626NA
Part A 0.4mg LY3202626NA
Part A 1.6mg LY320262660.6
Part A 5mg LY3202626197
Part A 15mg LY3202626393
Part A 45mg LY32026261680
Part B 1.6mg LY320262649.9
Part B 10mg LY3202626102
Part B 26mg LY3202626575
Part C 1mg LY3202626 QD38.6
Part C 6mg LY3202626 QD151
Part C 26mg LY3202626 QD1020

[back to top]

PK: CSF Concentration of LY3202626

(NCT02323334)
Timeframe: Part C: Day 15 at 24 hours +/- 4 hours (hr) postdose

Interventionng/mL (Geometric Mean)
Part C 1mg LY32026260.0648
Part C 6 mg LY32026260.202
Part C 26mg LY32026261.26

[back to top] [back to top] [back to top]

Area Under the Concentration-Time Profile From Time 0 to Time Tau, the Dosing Interval, Where Tau = 12 Hours (AUCtau) of PF-04958242

AUCtau = area under the concentration-time profile from time 0 to time tau, the dosing interval, where tau = 12 hours. Collected at Day 3 for PF-04958242 0.025 mg Arm and Day 17 for PF-04958242 0.025 mg + itraconazole 200 mg Arm. (NCT02341482)
Timeframe: Day 1 (0,1.5,12,13.5 hours post-dose), Day 2 (0,1.5,12,13.5 hours post-dose), Day 3 (0,0.5,1,1.5,2,3,4,6,8,12 hours post-dose), Day 4, Day 7, Day 10, Day 13, Day 16, Day 17 (0,0.5,1,1.5,2,3,4,5,6,8,12 hours post-dose) Day 18, Day 19, Day 20, Day 21

Interventionpicogram*hours per milliliter pg*h/mL (Geometric Mean)
PF-04958242 0.025 mg4242
PF-04958242 0.025 mg + Itraconazole 200 mg4073

[back to top]

Apparent Oral Clearance (CL/F) of PF-04958242

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population PK modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. Collected at Day 3 for PF-04958242 0.025 mg Arm and Day 17 for PF-04958242 0.025 mg + itraconazole 200 mg Arm. (NCT02341482)
Timeframe: Day 1 (0,1.5,12,13.5 hours post-dose), Day 2 (0,1.5,12,13.5 hours post-dose), Day 3 (0,0.5,1,1.5,2,3,4,6,8,12 hours post-dose), Day 4, Day 7, Day 10, Day 13, Day 16, Day 17 (0,0.5,1,1.5,2,3,4,5,6,8,12 hours post-dose) Day 18, Day 19, Day 20, Day 21

Interventionmilliliters per minute (mL/min) (Geometric Mean)
PF-04958242 0.025 mg98.25
PF-04958242 0.025 mg + Itraconazole 200 mg102.3

[back to top]

Maximum Observed Plasma Concentration (Cmax) of PF-04958242

Collected at Day 3 for PF-04958242 0.025 mg Arm and Day 17 for PF-04958242 0.025 mg + itraconazole 200 mg Arm. (NCT02341482)
Timeframe: Day 1 (0,1.5,12,13.5 hours post-dose), Day 2 (0,1.5,12,13.5 hours post-dose), Day 3 (0,0.5,1,1.5,2,3,4,6,8,12 hours post-dose), Day 4, Day 7, Day 10, Day 13, Day 16, Day 17 (0,0.5,1,1.5,2,3,4,5,6,8,12 hours post-dose) Day 18, Day 19, Day 20, Day 21

Interventionpg/mL (Geometric Mean)
PF-04958242 0.025 mg553.4
PF-04958242 0.025 mg + Itraconazole 200 mg541.6

[back to top] [back to top]

Predose Concentration (Ctrough) of PF-04958242

(NCT02341482)
Timeframe: 0 hour at Day 1, Day 2, Day 3, Day 4, Day 7, Day 10, Day 13, Day 16, and Day 17 (pre-dose)

Interventionpg/mL (Geometric Mean)
PF-04958242 0.025 mg289.3
PF-04958242 0.025 mg + Itraconazole 200 mg255.0

[back to top]

Number of Participants With Positive Response to Columbia-Suicide Severity Rating Scale (C-SSRS)

"The C-SSRS (mapped to Columbia Classification Algorithm of Suicide Assessment [C-CASA]) is an interview-based rating scale to systematically assess suicidal ideation and suicidal behavior. C-SSRS assessed whether participant experienced the following: completed suicide (1), suicide attempt (2) (response of Yes on actual attempt), preparatory acts toward imminent suicidal behavior (3)(Yes on preparatory acts or behavior), suicidal ideation (4) (Yes on wish to be dead, non-specific active suicidal thoughts, active suicidal ideation with methods without intent to act or some intent to act, without specific plan or with specific plan and intent), any suicidal behavior or ideation, self-injurious behavior (7)(Yes on Has participant engaged in non-suicidal self-injurious behavior)." (NCT02341482)
Timeframe: Baseline up to Day 21

Interventionparticipants (Number)
All Subjects0

[back to top]

Number of Participants With Electrocardiogram Data Meeting Criteria of Potential Clinical Concern

Electrocardiogram (ECG) parameters included time from ECG Q wave to the end of the T wave corresponding to electrical systole (QT) interval, beginning of the P wave until the beginning of the QRS complex (PR) interval, time from ECG Q wave to the end of the S wave corresponding to ventricle depolarization (QRS) interval, QT interval corrected for heart rate (QTc) interval, and corrected QT interval using Fridericia's formula (QTcF). Criteria for ECG changes meeting potential clinical concern included: PR interval >=300 milliseconds (msec) or >=25% increase when baseline is >200 msec and >=50% increase when baseline is less than or equal to (=<)200 msec; QRS interval >=140 msec or >=50% increase from baseline; and QTcF >=450 to <480, 480 to <500 and >=500 msec or >=30 to 60 msec increase and also >=60 msec increase. The number of participants with potentially clinically significant ECG findings at any visit were reported. (NCT02341482)
Timeframe: Baseline up to Day 21

Interventionparticipants (Number)
All Subjects0

[back to top]

Number of Participants With Abnormal Clinical Laboratory Measurements

The following laboratory parameters were analyzed: hematology (hemoglobin, hematocrit, red blood cell [RBC] count, mean corpuscular volume [MCV], mean corpuscular hemoglobin [MCH], mean corpuscular hemoglobin concentration [MCHC], platelet count, white blood cell [WBC] count, total neutrophils, eosinophils, monocytes, basophils, lymphocytes); blood chemistry (blood urea nitrogen [BUN], creatinine, glucose, calcium, sodium, potassium, chloride, total bicarbonate, aspartate aminotransferase [AST], alanine aminotransferase [ALT], total bilirubin, alkaline phosphatase, uric acid, albumin, and total protein; urinalysis (pH, glucose, protein, blood, ketones, nitrites, leukocyte esterase, urobilinogen, urine bilirubin and microscopy [if urine dipstick was positive for blood, protein, nitrites or leukocyte esterase]); others (follicle stimulating hormone [FSH], urine cotinine, and urine drug screening). (NCT02341482)
Timeframe: Baseline up to Day 21

Interventionparticipants (Number)
All Subjects1

[back to top]

Lowest Concentration Observed During the Dosing Interval (Cmin) of PF-04958242

(NCT02341482)
Timeframe: Day 1 (0,1.5,12,13.5 hours post-dose), Day 2 (0,1.5,12,13.5 hours post-dose), Day 3 (0,0.5,1,1.5,2,3,4,6,8,12 hours post-dose), Day 4, Day 7, Day 10, Day 13, Day 16, Day 17 (0,0.5,1,1.5,2,3,4,5,6,8,12 hours post-dose) Day 18, Day 19, Day 20, Day 21

Interventionpg/mL (Geometric Mean)
PF-04958242 0.025 mg256.5
PF-04958242 0.025 mg + Itraconazole 200 mg238.2

[back to top]

Time for Cmax (Tmax) of PF-04958242

Collected at Day 3 for PF-04958242 0.025 mg Arm and Day 17 for PF-04958242 0.025 mg + itraconazole 200 mg Arm. (NCT02341482)
Timeframe: Day 1 (0,1.5,12,13.5 hours post-dose), Day 2 (0,1.5,12,13.5 hours post-dose), Day 3 (0,0.5,1,1.5,2,3,4,6,8,12 hours post-dose), Day 4, Day 7, Day 10, Day 13, Day 16, Day 17 (0,0.5,1,1.5,2,3,4,5,6,8,12 hours post-dose) Day 18, Day 19, Day 20, Day 21

Interventionhours (Median)
PF-04958242 0.025 mg1.50
PF-04958242 0.025 mg + Itraconazole 200 mg1.50

[back to top]

Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 28 days after last dose that were absent before treatment or that worsened relative to pre-treatment state. (NCT02341482)
Timeframe: Baseline up to 28 days after last study drug administration

,,
Interventionparticipants (Number)
AEsSAEs
PF-04958242 0.025 mg20
PF-04958242 0.025 mg + Itraconazole 200 mg70
PF-04958242 0.1 mg10

[back to top]

Number of Participants With Vital Signs Data Meeting Criteria of Potential Clinical Concern

Vital signs assessment included pulse rate and blood pressure. Criteria for vital sign values meeting potential clinical concern included: supine/sitting pulse rate more than (<)40 or less than (>)120 beats per minute (bpm); systolic blood pressure (SBP) more than or equal to (>=)30 millimeters of mercury (mm Hg) change from baseline in same posture or SBP <90 mm Hg, diastolic blood pressure (DBP) >=20 mm Hg change from baseline in same posture or DBP <50 mm Hg. IFB = increase from baseline; DFB = decrease from baseline. (NCT02341482)
Timeframe: Baseline up to Day 21

Interventionparticipants (Number)
Supine SBP <90 mmHgSupine DBP <50 mmHgSupine Pulse Rate <40 BPMSupine Pulse Rate >120 BPMSupine SBP >=30 mmHg IFBSupine DBP >=20 mmHg IFBSupine SBP >=30 mmHg DFBSupine DBP >=20 mmHg DFB
All Subjects00002100

[back to top]

Mean Percent Change in Angiogenic Cytokines From Baseline

A commercially available kit will be used to measure Angiogenic Cytokines levels. (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

InterventionPercent change (Mean)
IL-8PDGF-bbVEGFFGF-b
Itraconazole-4.53917.7116-13.5786-35.5341

[back to top]

Mean Percent Change in Other Plasma Cytokine From Baseline to Post-Treatment

The following plasma cytokines were measured using a commercially available kit. (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

InterventionPercent change (Mean)
IL-1bIL-1raIL-2IL-4IL-5IL-6IL-7IL-9IL-10IL-12IL-13IL-15IL-17IP-10MCP-1MIP-1aMIP-1bRANTESTNF-aIFN-gEotaxinG-CSFGM-CSF
Itraconazole-14.4159-16.9648-21.5999-5.0114-13.7573-62.5420-21.9919-0.92092.9705-30.0689-16.1310-27.7823-24.3512-16.7481-11.3317-14.72910.07675.1468-18.0238-39.72802.8770-4.4567-45.6701

[back to top]

Change in Skin Biopsy PTCH1 Levels From Baseline

We analyzed serial skin biopsies for PTCH1 mRNA by qPCR. (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

Interventionrelative units (Mean)
Itraconazole0.03164

[back to top]

Itraconazole Levels in Post-treatment Serum

Itraconazole levels assessed by post-treatment serum (NCT02357836)
Timeframe: Post Treatment (after 7-10 days of itraconazole bid)

Interventionng/mL (Mean)
Itraconazole1264

[back to top]

Changes in Tumor Tissue Microvessel Density [MVD] From Baseline

Images of DAPI (4',6-Diamidino-2-Phenylindole) , CD31 (cluster of differentiation 31 ), and CD34 (cluster of differentiation 34) were taken from the same field of view and then merged. (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

InterventionPercent area fraction (Mean)
Itraconazole0.005

[back to top]

Changes in Perfusion (Ktrans)

DCE (dynamic contrast enhanced ) MRI is an established technology to assess microvessel density (MVD) and tumor capillary permeability. (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

Interventionmin-1 (Mean)
Itraconazole0.008

[back to top]

Itraconazole Levels in Tumor Tissue

Itraconazole levels assessed by tumor tissue (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

Interventionng/g (Mean)
Itraconazole2585

[back to top]

Change in Skin Biopsy GLI1 Levels From Baseline

We analyzed serial skin biopsies for GLI1 mRNA by qPCR (quantitative polymerase chain reaction). (NCT02357836)
Timeframe: Baseline and Post Treatment (after 7-10 days of itraconazole bid)

Interventionrelative units (Mean)
Itraconazole0.27347

[back to top]

Cumulative Urinary Excretion Ratio of TAK 272F and TAK 272-M-I From 0 to 72 Hours Postdose in Cohort 1

(NCT02370615)
Timeframe: Day 1 and Day 10: pre-dose and at multiple time-points (upto 72 hours) postdose; Day 1 for Cohort 1: TAK-272 and Day 10 for Cohort 1: TAK-272 + Itraconazole

,
Interventionpercentage of dose (Mean)
TAK 272TAK 272-M-I
Cohort 1: TAK-27211.5230.556
Cohort 1: TAK-272 + Itraconazole37.8030.071

[back to top]

Cmax: Maximum Observed Plasma Concentration for TAK 272F and TAK 272-Metabolite (M-I) in Cohort 1

(NCT02370615)
Timeframe: Day 1 and Day 10: pre-dose and at multiple time-points (upto 72 hours) postdose; Day 1 for Cohort 1: TAK-272 and Day 10 for Cohort 1: TAK-272 + Itraconazole

,
Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
TAK 272TAK 272-M-I
Cohort 1: TAK-272387.810.02
Cohort 1: TAK-272 + Itraconazole780.30.9550

[back to top]

Cmax: Maximum Observed Plasma Concentration for Midazolam and 1'Hydroxymidazolam in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 24 hours) postdose; Day 1 for Cohort 2: Midazolam and Day 7 for Cohort 2: Midazolam + TAK-272

,
Interventionng/mL (Geometric Mean)
Midazolam1'hydroxymidazolam
Cohort 2: Midazolam10.024.813
Cohort 2: Midazolam + TAK-27212.374.270

[back to top]

AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK 272F and TAK 272-M-I in Cohort 1

(NCT02370615)
Timeframe: Day 1 and Day 10: pre-dose and at multiple time-points (upto 72 hours) postdose; Day 1 for Cohort 1: TAK-272 and Day 10 for Cohort 1: TAK-272 + Itraconazole

,
Interventionng*hr/mL (Geometric Mean)
TAK 272TAK 272-M-I
Cohort 1: TAK-272184238.34
Cohort 1: TAK-272 + Itraconazole86590.9092

[back to top]

Number of Participants With Clinically Significant Change From Baseline in Continuous Pulse Oximetry (SpO2) in Cohort 2

(NCT02370615)
Timeframe: Cohort 2: Baseline up to Day 15

Interventionparticipants (Number)
Cohort 2: Midazolam + Digoxin + TAK-2720

[back to top]

AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Midazolam and 1'Hydroxymidazolam in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 24 hours) postdose; Day 1 for Cohort 2: Midazolam and Day 7 for Cohort 2: Midazolam + TAK-272

,
Interventionng*hr/mL (Geometric Mean)
Midazolam1'hydroxymidazolam
Cohort 2: Midazolam26.7712.49
Cohort 2: Midazolam + TAK-27238.1613.25

[back to top]

Urinary Excretion Ratio of Digoxin From 0 to 48 Hours Postdose in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 48 hours) postdose; Day 1 for Cohort 2: Digoxin and Day 7 for Cohort 2: Digoxin + TAK-272

Interventionpercentage of dose (Mean)
Cohort 2: Digoxin31.391
Cohort 2: Digoxin + TAK-27235.983

[back to top] [back to top]

AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK 272F and TAK 272-M-I in Cohort 1

(NCT02370615)
Timeframe: Day 1 and Day 10: pre-dose and at multiple time-points (upto 72 hours) postdose; Day 1 for Cohort 1: TAK-272 and Day 10 for Cohort 1: TAK-272 + Itraconazole

,
Interventionnanogram hours per milliliter (ng*hr/mL) (Geometric Mean)
TAK 272TAK 272-M-I
Cohort 1: TAK-272186146.53
Cohort 1: TAK-272 + Itraconazole90989.373

[back to top]

AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Midazolam and 1'Hydroxymidazolam in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 24 hours) postdose; Day 1 for Cohort 2: Midazolam and Day 7 for Cohort 2: Midazolam + TAK-272

,
Interventionng*hr/mL (Geometric Mean)
Midazolam1'hydroxymidazolam
Cohort 2: Midazolam27.1113.00
Cohort 2: Midazolam + TAK-27238.5514.06

[back to top] [back to top]

Number of Participants Who Had Clinically Significant Changes From Baseline in 12-lead Electrocardiograms

"Number of participants who had ECG findings changed from within normal limit or abnormal, clinically significant to abnormal and clinically significant after study drug administration." (NCT02370615)
Timeframe: Cohort 1: Baseline up to Day 19; Cohort 2: Baseline up to Day 15

Interventionparticipants (Number)
Cohort 1: TAK-272 + Itraconazole0
Cohort 2: Midazolam + Digoxin + TAK-2720

[back to top]

Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)

(NCT02370615)
Timeframe: Cohort 1: Baseline up to Day 19; Cohort 2: Baseline up to Day 15

Interventionparticipants (Number)
Cohort 1: TAK-272 + Itraconazole10
Cohort 2: Midazolam + Digoxin + TAK-2727

[back to top]

Cmax: Maximum Observed Plasma Concentration for Digoxin in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 48 hours) postdose; Day 1 for Cohort 2: Digoxin and Day 7 for Cohort 2: Digoxin + TAK-272

Interventionng/mL (Geometric Mean)
Cohort 2: Digoxin1.212
Cohort 2: Digoxin + TAK-2721.635

[back to top]

AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Digoxin in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 48 hours) postdose; Day 1 for Cohort 2: Digoxin and Day 7 for Cohort 2: Digoxin + TAK-272

Interventionng*hr/mL (Geometric Mean)
Cohort 2: Digoxin9.191
Cohort 2: Digoxin + TAK-27210.61

[back to top]

AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Digoxin in Cohort 2

(NCT02370615)
Timeframe: Day 1 and Day 7: pre-dose and at multiple time-points (upto 48 hours) postdose; Day 1 for Cohort 2: Digoxin and Day 7 for Cohort 2: Digoxin + TAK-272

Interventionng*hr/mL (Geometric Mean)
Cohort 2: Digoxin15.49
Cohort 2: Digoxin + TAK-27215.79

[back to top] [back to top]

Maximum Concentration of BI 1026706 (Cmax)

Maximum measured concentration of BI 1026706 in plasma (Cmax) (NCT02513446)
Timeframe: 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 47h, 71h and 95h after drug administration

Interventionnmol/L (Geometric Mean)
Treatment R (BI 1026706 Alone)206
Treatment T (Itraconazole + BI 1026706)279

[back to top]

Area Under the Curve of BI 1026706 From 0 to the Last Quantifiable Data Point (AUC0-tz)

Area under the concentration-time curve of BI 1026706 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) (NCT02513446)
Timeframe: -3 hours (h) before drug administration and 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 47h, 71h and 95h after drug administration

Interventionnmol*h/L (Geometric Mean)
Treatment R (BI 1026706 Alone)921
Treatment T (Itraconazole + BI 1026706)1580

[back to top]

Area Under the Curve of BI 1026706 From 0 Extrapolated to Infinity (AUC0-inf)

Area under the concentration-time curve of BI 1026706 in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf) (NCT02513446)
Timeframe: -3 hours (h) before drug administration and 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 47h, 71h and 95h after drug administration

Interventionnmol*h/L (Geometric Mean)
Treatment R (BI 1026706 Alone)943
Treatment T (Itraconazole + BI 1026706)1600

[back to top]

Assessment of the Tmax of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.

To assess the time to reach maximum observed concentration of Verapamil, Itraconazole and OH-itraconazole (a metabolite of itraconazole) following co-administration of AZD7986 with Verapamil or Itraconazole. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionhours (Median)
Verapamil4.00
Itraconazole1.50
OH-itraconazole (a Metabolite of Itraconazole)5.00

[back to top]

Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC).

To assess the effect of verapamil and itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionh*nmol/L (Geometric Mean)
AZD79866697
AZD7986 + Verapamil8857
AZD7986 + Itraconazole7615

[back to top]

Effect of Verapamil and the Effect of Itraconazole on the PK of AZD7986 by Assessment of the Observed Maximum Plasma Concentration (Cmax).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionnmol/L (Geometric Mean)
AZD7986385.8
AZD7986 + Verapamil591.9
AZD7986 + Itraconazole234.1

[back to top]

Pharmacokinetics (PK) of AZD7986 by Assessment of Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration-time Curve (t½λz).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionhours (Mean)
AZD798623.35
AZD7986 + Verapamil20.36
AZD7986 + Itraconazole27.89

[back to top]

Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Total Body Clearance After Extravascular Administration Estimated as Dose Divided by AUC (CL/F).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

InterventionL/h (Mean)
AZD79869.807
AZD7986 + Verapamil7.359
AZD7986 + Itraconazole8.308

[back to top]

Pharmacokinetics (PK) of AZD7986 by Assessment of the Apparent Volume of Distribution During the Terminal Phase After Extravascular Administration (Vz/F).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

InterventionLitres (Mean)
AZD7986297.1
AZD7986 + Verapamil194.6
AZD7986 + Itraconazole317.8

[back to top]

Pharmacokinetics (PK) of AZD7986 by Assessment of the Area Under Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC [0-t]).

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionh*nmol/L (Geometric Mean)
AZD79866545
AZD7986 + Verapamil8739
AZD7986 + Itraconazole7361

[back to top]

Pharmacokinetics (PK) of AZD7986 by Assessment of the Time to Reach Maximum Plasma Concentration (Tmax)

To assess the effect of Verapamil and Itraconazole on the PK of AZD7986. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionhours (Median)
AZD79860.75
AZD7986 + Verapamil1.50
AZD7986 + Itraconazole1.50

[back to top]

Assessment of the Area Under the Plasma Concentration-curve Over the Dosing Interval (AUC [0 - τ]) of Verapamil, Itraconazole and OH-itraconazole Following Co-administration of AZD7986 With Verapamil or Itraconazole.

To assess the area under the plasma concentration-time curve from time over the dosing interval tau (24 hours) of Verapamil, itraconazole and OH-itraconazole (a metabolite of Itraconazole) following co-administration of AZD7986 with Verapamil or Itraconazole. (NCT02653872)
Timeframe: Period 1,2&3: Day1 (AZD7986),Day5 (AZD7986+Verapamil) & Day6 (AZD7986): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12,24,48,72,96,120 & 144 hours post-dose; Period 3: Day6 (Itraconazole): pre-dose,0.25,0.5,0.75,1,1.5,2,3,4,5,8,9,12 & 24 hours post-dose

Interventionh*nmol/L (Geometric Mean)
Verapamil2178
Itraconazole18090
OH-itraconazole (a Metabolite of Itraconazole)31390

[back to top]

Part B Pharmacodynamics (PD): Change From Baseline in Cerebrospinal Fluid (CSF) Amyloid Beta (Aβ)₁-₄₀ and Aβ₁-₄₂

Amyloid beta is a peptide fragment of the amyloid precursor protein, CSF concentrations of Aβ1-40, Aβ1-42 were determined using validated immunoassay methods. (NCT02989389)
Timeframe: Baseline through 36 hours

,,,
InterventionPicogram per milliliter (pg/mL) (Mean)
Aβ 1-40Aβ 1-42
Part B, 20 mg LY3323795-69-71
Part B, 6 mg LY3323795-51-37
Part B, 80 mg LY3323795-88-81
Placebo-12-17

[back to top]

Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of LY3323795 in Plasma

Pharmacokinetics (PK): Maximum observed drug concentration (Cmax) of LY3323795 in plasma. (NCT02989389)
Timeframe: 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96,120,144 hours, post dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Part A, Cohort 1, 0.3 mg LY33237950.503
Part A, Cohort 2, 1 mg LY33237951.77
Part A, Cohort 1, 3 mg LY33237954.79
Part A, Cohort 2, 10 mg LY332379515.7
Part A, Cohort 1, 30 mg LY332379534.6
Part A, Cohort 2, 100 mg LY332379589.1
Part B, 6 mg LY332379510.4
Part B, 20 mg LY332379527.2
Part B, 80 mg LY332379588.1

[back to top]

Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Tlast (AUC[0-tlast]) of LY3323795 in Plasma

Pharmacokinetics (PK): Area under the concentration time curve from time zero to tlast (AUC[0-tlast]) of LY3323795 in plasma. (NCT02989389)
Timeframe: 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96,120,144 hours, post dose

Interventionnanogram*hour per milliliter (ng*h/mL) (Geometric Mean)
Part A, Cohort 1, 0.3 mg LY33237955.67
Part A, Cohort 2, 1 mg LY332379525.2
Part A, Cohort 1, 3 mg LY332379573.4
Part A, Cohort 2, 10 mg LY3323795274
Part A, Cohort 1, 30 mg LY3323795663
Part A, Cohort 2, 100 mg LY33237952370
Part B, 6 mg LY3323795156
Part B, 20 mg LY3323795441
Part B, 80 mg LY33237951950

[back to top] [back to top]

Part B Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Tlast (AUC[0-tlast]) of LY3323795 in Cerebrospinal Fluid (CSF)

Part B Pharmacokinetics (PK): Area under the concentration time curve from time zero to tlast (AUC[0-tlast]) of LY3323795 in cerebrospinal fluid (CSF). (NCT02989389)
Timeframe: -4, -2, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 14, 16, 18, 20, 24, 28, 32, 36 hours, post dose

Interventionng*h/mL (Geometric Mean)
Part B, 6 mg LY33237955.46
Part B, 20 mg LY332379513.7
Part B, 80 mg LY332379555.1

[back to top]

Pharmacodynamics (PD): Change From Baseline in Plasma Amyloid Beta (Aβ)₁-₄₀ and Aβ₁-₄₂

Amyloid beta is a peptide fragment of the amyloid precursor protein, plasma concentrations of Aβ1-40 and Aβ1-42 were determined using validated immunoassay methods. (NCT02989389)
Timeframe: Baseline through 144 hours

,,,,,,,,,
InterventionPicogram per milliliter (pg/mL) (Mean)
Aβ1-40Aβ1-42
Part A, Cohort 1, 0.3 mg LY3323795-39-22
Part A, Cohort 1, 3 mg LY3323795-71-49
Part A, Cohort 1, 30 mg LY3323795-76-63
Part A, Cohort 2, 1 mg LY3323795-52-33
Part A, Cohort 2, 10 mg LY3323795-76-60
Part A, Cohort 2, 100 mg LY3323795-89-75
Part B, 20 mg LY3323795-81-58
Part B, 6 mg LY3323795-79-54
Part B, 80 mg LY3323795-89-64
Placebo-23-12

[back to top]

Part B Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of LY3323795 in Cerebrospinal Fluid (CSF)

Part B Pharmacokinetics (PK): Maximum observed drug concentration (Cmax) of LY3323795 in cerebrospinal fluid (CSF). (NCT02989389)
Timeframe: -4, -2, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 14, 16, 18, 20, 24, 28, 32, 36 hours, post dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Part B, 6 mg LY33237950.293
Part B, 20 mg LY33237950.788
Part B, 80 mg LY33237952.86

[back to top]

Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionHour*picogram per milliliter (hr*pg/mL) (Geometric Mean)
Talazoparib 0.5 mg Alone98532.30
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID145944.59

[back to top]

Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC0-inf) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

Interventionhr*pg/mL (Geometric Mean)
Talazoparib 1.0 mg Alone209521.62
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD194307.67

[back to top]

Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Rifampin

"Apparent volume of distribution was defined as the theoretical volume in which the total amount of talazoparib would need to be uniformly distributed to produce its desired plasma concentration. T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionLiter (Geometric Mean)
Talazoparib 1.0 mg Alone623.89
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD588.14

[back to top]

Number of Participants With Clinically Significant Abnormalities in Electrocardiogram (ECG)

ECG abnormalities: a) QT Interval: new absolute values greater than (>) 450, >480, >500 milliseconds (msec), increase from baseline >30 and >60 msec, b) QT interval using Fridericia's correction (QTcF) Interval: new absolute values >450, >480, >500 msec, increase from baseline >30 and > 60 msec, c) Heart rate: increase from baseline >25 percentage (%) and to a value >100 bpm, decrease from baseline >25% and to a value <50 bpm, d) PR Interval: increase from baseline > 25% and to a value >200 msec, e) QRS duration: increase from baseline > 25% and to a value >100 msec. Clinical significance of ECG abnormalities was judged by investigator. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone0
Itraconazole 100 mg BID Alone1
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID0
Talazoparib 1.0 mg Alone0
Rifampin 600 mg QD Alone0
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD0

[back to top]

Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Rifampin

"Clearance of talazoparib was measure of the rate at which it was metabolized or eliminated by normal biological processes. T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionLiter per hour (Geometric Mean)
Talazoparib 1.0 mg Alone4.77
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD5.15

[back to top]

Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Itraconazole

"Clearance of talazoparib was measure of the rate at which it was metabolized or eliminated by normal biological processes. T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionLiter per hour (Geometric Mean)
Talazoparib 0.5 mg Alone4.55
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID3.29

[back to top]

Number of Participants With Clinically Significant Abnormalities in Vital Signs

Vital sign abnormalities: a) systolic blood pressure (SBP): 1) minimum less than (<) 90 millimeter of mercury (mmHg), 2) change from baseline maximum decrease greater than equal to (>=) 30 mmHg, 3) change from baseline maximum increase >=30 mmHg; b) diastolic blood pressure (DBP): 1) minimum <50 mmHg, 2) change from baseline maximum decrease >=20 mmHg, 3) change from baseline maximum increase >=20 mmHg; c) supine pulse rate: 1) minimum <40 beats per minute (bpm), 2) maximum >120 bpm; d) standing pulse rate: 1) minimum <40 bpm and 2) maximum >140 bpm. Clinical significance of vital signs abnormalities was judged by investigator. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone0
Itraconazole 100 mg BID Alone0
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1
Talazoparib 1.0 mg Alone0
Rifampin 600 mg QD Alone0
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD1

[back to top]

Number of Participants With Clinically Significant Physical Examination Findings

Physical examination included examination of abdomen, cardiovascular, eyes, ears, nose, throat, general appearance, head, neck, thyroid, lymph nodes, musculoskeletal, neurological, skin / subcutaneous tissue, thorax / lungs, abdomen including spleen size, breasts (female only) and respiratory. Clinical significance of physical examination was judged by investigator. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone0
Itraconazole 100 mg BID Alone0
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1
Talazoparib 1.0 mg Alone1
Rifampin 600 mg QD Alone0
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD0

[back to top]

Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Itraconazole

"Terminal elimination half-life was defined as time measured for the plasma concentration of talazoparib to decrease by one half. T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionHours (Mean)
Talazoparib 0.5 mg Alone101.26
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID118.47

[back to top]

Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Rifampin

"Terminal elimination half-life was defined as time measured for the plasma concentration of talazoparib to decrease by one half. T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionHours (Mean)
Talazoparib 1.0 mg Alone92.05
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD80.61

[back to top]

Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionHours (Median)
Talazoparib 0.5 mg Alone1.00
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1.02

[back to top]

Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Itraconazole

"Apparent volume of distribution was defined as the theoretical volume in which the total amount of talazoparib would need to be uniformly distributed to produce its desired plasma concentration. T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionLiter (Geometric Mean)
Talazoparib 0.5 mg Alone644.81
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID552.01

[back to top]

Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionHours (Median)
Talazoparib 1.0 mg Alone1.00
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD1.00

[back to top]

Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study treatment without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death, initial or prolonged inpatient hospitalization, life-threatening experience (immediate risk of dying), persistent or significant disability or incapacity, congenital anomaly. A TEAE was defined as an event that emerged during the treatment period that was absent before treatment, or worsened during the treatment period relative to the pre-treatment state. AEs included both serious and non-serious adverse events. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

,,,,,
InterventionParticipants (Count of Participants)
AEsSAEs
Itraconazole 100 mg BID Alone30
Rifampin 600 mg QD Alone92
Talazoparib 0.5 mg Alone123
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID51
Talazoparib 1.0 mg Alone60
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD50

[back to top]

Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

Interventionpg/mL (Geometric Mean)
Talazoparib 1.0 mg Alone6007.01
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD8336.83

[back to top]

Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionPicogram per milliliter (pg/mL) (Geometric Mean)
Talazoparib 0.5 mg Alone2092.00
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID2936.82

[back to top]

Area Under the Plasma Concentration-Time Profile From Time Zero to Extrapolated Infinity (AUC0-inf) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

Interventionhr*pg/mL (Geometric Mean)
Talazoparib 0.5 mg Alone109762.10
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID151919.63

[back to top]

Number of Participants With Clinical Significance Abnormalities in Laboratory Parameters

Chemistry:(sodium135-146,potassium3.5-5.5,chloride95-109,glucose3.3-5.5,urea2.8-7.2,calcium2.2-2.65,phosphate0.8-1.45,triglyceride0.4-1.7,cholesterol2.6-5.2)millimoles/L, (bilirubin[direct0-3,total2-21],creatinine53- 110)micromole/L, (albumin35-52,protein65-83)g/L,(alkaline phosphatase30-120, aspartate amino[A]transferase[T]4-46, alanine AT4-49, lactic acid dehydrogenase200-460, gammaglutamylT7-50,creatinine kinase24-170)U/L. Hematology: hemoglobin(Hb)120-177, hematocrit0.35-0.49L/L, RBC4-5.9T/L, (platelet150- 400,WBC4-10,basophil<0.10,eosinophil<0.40, neutrophil1.50-7.00,monocyte<1.20,lymphocyte1.0 -3.70)G/L. Urine:(glucose,protein,ketone,Hb:negative/positive), specific gravity1.010-1.030g/cm^3, pH4.8-7.8, pale yellow-deep amber, microscopy[WBC0-5,leukocyte0-5,Hb0-3,cast0-1,bacteria0-500,epithelial0-6])Pcs/area. Coagulation:(activated partial thromboplastine time25-43,prothrombin time13.7-15.6) seconds,international normalized ratio0.89-1.1. Investigator judged clinical significance. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone3
Itraconazole 100 mg BID Alone0
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1
Talazoparib 1.0 mg Alone2
Rifampin 600 mg QD Alone1
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD1

[back to top]

Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

Interventionhr*pg/mL (Geometric Mean)
Talazoparib 1.0 mg Alone196631.34
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD196100.69

[back to top]

AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-906

(NCT03161405)
Timeframe: TAK-906 maleate 25mg: Day 1 pre-dose and at multiple time points (up to 48 hours) post-TAK-906 maleate-dose; Itraconazole 200 mg + TAK-906 maleate 25mg: Day 4 pre-dose and at multiple time points (up to 48 hours) post- TAK-906 maleate-dose

Interventionh*ng/mL (Geometric Mean)
TAK-906 Maleate 25 mg24.41
Itraconazole 200 mg + TAK-906 Maleate 25 mg31.45

[back to top]

AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-906

(NCT03161405)
Timeframe: TAK-906 maleate 25mg: Day 1 pre-dose and at multiple time points (up to 48 hours) post-TAK-906 maleate-dose; Itraconazole 200 mg + TAK-906 maleate 25mg: Day 4 pre-dose and at multiple time points (up to 48 hours) post- TAK-906 maleate-dose

Interventionhour*nanogram per milliliter (h*ng/mL) (Geometric Mean)
TAK-906 Maleate 25 mg24.10
Itraconazole 200 mg + TAK-906 Maleate 25 mg30.73

[back to top]

Cmax: Maximum Observed Plasma Concentration for TAK-906

(NCT03161405)
Timeframe: TAK-906 maleate 25mg: Day 1 pre-dose and at multiple time points (up to 48 hours) post-TAK-906 maleate-dose; Itraconazole 200 mg + TAK-906 maleate 25mg: Day 4 pre-dose and at multiple time points (up to 48 hours) post- TAK-906 maleate-dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
TAK-906 Maleate 25 mg9.532
Itraconazole 200 mg + TAK-906 Maleate 25 mg17.999

[back to top]

AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-954

(NCT03173170)
Timeframe: TAK-954 0.2 mg: Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose; Itraconazole 200 mg and TAK-954 0.2mg: Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose

Interventionhour*nanogram per milliliter (hr*ng/mL) (Geometric Mean)
TAK-954 0.2 mg28.59
Itraconazole 200 mg and TAK-954 0.2mg43.15

[back to top]

Cmax: Maximum Observed Plasma Concentration for TAK-954

(NCT03173170)
Timeframe: TAK-954 0.2 mg: Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose; Itraconazole 200 mg and TAK-954 0.2 mg: Day 4 pre-dose and at multiple time points (up to 120 hours) post-dose

Interventionnanogram/milliliter (ng/mL) (Geometric Mean)
TAK-954 0.2 mg2.642
Itraconazole 200 mg and TAK-954 0.2 mg2.840

[back to top]

Best Objective Response as Confirmed By The Investigator's Assessment in Participants With HER2-Expressing Advanced Solid Malignant Tumors

Best objective response (BOR) was assessed by the investigator based on Response Evaluation Criteria In Solid Tumors (RECIST) version 1.1. Completed response (CR) was defined as a disappearance of all target lesions, PR was defined as at least a 30% decrease in the sum of diameters of target lesions, and stable disease (SD) was defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for progressive disease (PD; at least a 20% increase in the sum of diameters of target lesions. (NCT03383692)
Timeframe: Baseline up to disease progression, death, lost to follow up, or study discontinuation (whichever comes first), up to approximately 9 months post-dose

,
InterventionParticipants (Count of Participants)
Complete response (CR)Partial response (PR)Stable disease (SD)Non-CR/Non-PRProgressive disease (PD)Non evaluable
Cohort 1: DS-8201a + Ritonavir098000
Cohort 2: DS-8201a + Itraconazole0108010

[back to top]

Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve Following Treatment With DS-8201a and Ritonavir - Cohort 1

Area under the serum concentration-time curve from time zero to 17 days (AUC17d) and during the dosing interval (AUCtau) for DS-8201a and total anti-HER2 antibody were assessed. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionug*d/mL (Mean)
DS-8201a, Cycle 2 (DS-8201a only): AUC17dDS-8201a, Cycle 2 (DS-8201a only): AUCtauDS-8201a, Cycle 3 (DS-8201a + ritonavir): AUC17dDS-8201a, Cycle 3 (DS-8201a + ritonavir): AUCtauTotal Anti-HER2 antibody, Cycle 2 (DS-8201a only): AUC17dTotal Anti-HER2 antibody, Cycle 2 (DS-8201a only): AUCtauTotal Anti-HER2 antibody, Cycle 3 (DS-8201a + ritonavir): AUC17dTotal Anti-HER2 antibody, Cycle 3 (DS-8201a + ritonavir): AUCtau
Cohort 1: DS-8201a + Ritonavir650701754810723791796860

[back to top]

Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve Following Treatment With DS-8201a and Itraconazole - Cohort 2

Area under the serum concentration-time curve from time zero to 17 days (AUC17d) and during the dosing interval (AUCtau) were assessed for DS-8201a and total anti-HER2 antibody. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionug*d/mL (Mean)
DS-8201a, Cycle 2 (DS-8201a only): AUC17dDS-8201a, Cycle 2 (DS-8201a only): AUCtauDS-8201a, Cycle 3 (DS-8201a + ritonavir): AUC17dDS-8201a, Cycle 3 (DS-8201a + ritonavir): AUCtauTotal Anti-HER2 antibody, Cycle 2 (DS-8201a only): AUC17dTotal Anti-HER2 antibody, Cycle 2 (DS-8201a only): AUCtauTotal Anti-HER2 antibody, Cycle 3 (DS-8201a + ritonavir): AUC17dTotal Anti-HER2 antibody, Cycle 3 (DS-8201a + ritonavir): AUCtau
Cohort 2: DS-8201a + Itraconazole644706710789707790781883

[back to top]

Objective Response Rate as Confirmed By The Investigator's Assessment in Participants With HER2-Expressing Advanced Solid Malignant Tumors

Objective response rate (defined as participants who achieved CR and PR) was assessed by the investigator based on Response Evaluation Criteria In Solid Tumors (RECIST) version 1.1. CR was defined as a disappearance of all target lesions and PR was defined as at least a 30% decrease in the sum of diameters of target lesions. ORR with confirmation is Objective Response Rate applying a confirmed response of CR/PR in RECIST version 1.1. (NCT03383692)
Timeframe: Baseline up to disease progression, death, lost to follow up, or study discontinuation (whichever comes first), up to approximately 9 months post-dose

InterventionParticipants (Count of Participants)
Cohort 1: DS-8201a + Ritonavir8
Cohort 2: DS-8201a + Itraconazole7

[back to top]

Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) Following Treatment With DS-8201a and Ritonavir - Cohort 1

Maximum concentration (Cmax) was assessed for DS-8201a and total Anti-HER2 antibody. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionug/mL (Mean)
DS-8201a, Cycle 2: DS-8201a onlyDS-8201a, Cycle 3: DS-8201a + ritonavirTotal Anti-HER2 antibody, Cycle 2: DS-8201a onlyTotal Anti-HER2 antibody, Cycle 3: DS-8201a + ritonavir
Cohort 1: DS-8201a + Ritonavir133140121126

[back to top]

Objective Response Ratio (ORR) as Confirmed By The Investigator's Assessment in Participants With HER2-Expressing Advanced Solid Malignant Tumors

Objective response ratio (ORR) was defined as the proportion of participants who achieved CR and PR as assessed by the investigator based on Response Evaluation Criteria In Solid Tumors (RECIST) version 1.1. CR was defined as a disappearance of all target lesions and PR was defined as at least a 30% decrease in the sum of diameters of target lesions. (NCT03383692)
Timeframe: Baseline up to disease progression, death, lost to follow up, or study discontinuation (whichever comes first), up to approximately 9 months post-dose

InterventionParticipants (Count of Participants)
Cohort 1: DS-8201a + Ritonavir9
Cohort 2: DS-8201a + Itraconazole10

[back to top]

Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) of MAAA-1181a Following Treatment With DS-8201a and Itraconazole - Cohort 2

Maximum concentration (Cmax) was assessed for MAAA-1181a. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionng/mL (Mean)
MAAA-1181a, Cycle 2: DS-8201a onlyMAAA-1181a, Cycle 3: DS-8201a + ritonavir
Cohort 2: DS-8201a + Itraconazole8.658.93

[back to top]

Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) For MAAA-1181a Following Treatment With DS-8201a and Ritonavir - Cohort 1

Maximum concentration (Cmax) was assessed for MAAA-1181a. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionng/mL (Mean)
MAAA-1181a, Cycle 2: DS-8201a onlyMAAA-1181a, Cycle 3: DS-8201a + ritonavir
Cohort 1: DS-8201a + Ritonavir8.988.95

[back to top]

Pharmacokinetic Parameter of Maximum (Peak) Observed Serum Concentration (Cmax) Following Treatment With DS-8201a and Itraconazole - Cohort 2

Maximum concentration (Cmax) was assessed for DS-8201a and total Anti-HER2 antibody. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionug/mL (Mean)
DS-8201a, Cycle 2: DS-8201a onlyDS-8201a, Cycle 3: DS-8201a + ritonavirTotal Anti-HER2 antibody, Cycle 2: DS-8201a onlyTotal Anti-HER2 antibody, Cycle 3: DS-8201a + ritonavir
Cohort 1: DS-8201a + Itraconazole139142119130

[back to top]

Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve of MAAA-1181a Following Treatment With DS-8201a and Ritonavir - Cohort 1

Area under the serum concentration-time curve from time zero to 17 days (AUC17d) and during the dosing interval (AUCtau) were assessed for MAAA-1181a. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionng*d/mL (Mean)
MAAA-1181a, Cycle 2 (DS-8201a only): AUC17dMAAA-1181a, Cycle 2 (DS-8201a only): AUCtauMAAA-1181a, Cycle 3 (DS-8201a + ritonavir): AUC17dMAAA-1181a, Cycle 3 (DS-8201a + ritonavir): AUCtau
Cohort 1: DS-8201a + Ritonavir32.735.037.239.2

[back to top]

Pharmacokinetic Parameter of Area Under the Serum Concentration-time Curve of MAAA-1181a Following Treatment With DS-8201a and Itraconazole - Cohort 2

Area under the serum concentration-time curve from time zero to 17 days (AUC17d) and during the dosing interval (AUCtau) were assessed for MAAA-1181a. (NCT03383692)
Timeframe: Cycle 1: Day 1, pre-dose and end of infusion (EOI); Cycles 2 and 3: Day 1, pre-dose, EOI, 2 hours, 4 hours, 7 hours; Day 2, 4, 8, 12, 17, and 22; Cycles 4, 6 and 8: Day 1, pre-dose and EOI (each cycle is 22 days)

Interventionng*d/mL (Mean)
MAAA-1181a, Cycle 2 (DS-8201a only): AUC17dMAAA-1181a, Cycle 2 (DS-8201a only): AUCtauMAAA-1181a, Cycle 3 (DS-8201a + ritonavir): AUC17dMAAA-1181a, Cycle 3 (DS-8201a + ritonavir): AUCtau
Cohort 2: DS-8201a + Itraconazole29.932.434.837.7

[back to top]

Change From Baseline of Clinical Chemistry Parameters When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered: Alkaline Phosphate, Alanine Aminotransferase (ALT) and Aspartate Aminotransferase (AST)

Blood samples were collected for the analysis of clinical chemistry parameters including alkaline phosphate, ALT and AST at indicated time points. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionInternational Units/ Liter (Mean)
Alkaline phosphateALTAST
Nemiralisib 100 mcg0.81.5-0.5

[back to top]

Change From Baseline in Temperature When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered

Temperature of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose) and Day 6

InterventionCelsius (Mean)
Nemiralisib 100 mcg0.04

[back to top]

Change From Baseline in Respiratory Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose

Respiratory rate of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose), Days 2, 4, 6, 8 and 10

InterventionBreaths per minute (Mean)
Day 2Day 4Day 6Day 8Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-1.30.3-0.50.1-0.5

[back to top]

Change From Baseline in SBP and DBP When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose

Blood pressure of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose) and Days 2, 4, 6, 8 and 10

InterventionMillimeter of mercury (Mean)
SBP, Day 2SBP, Day 4SBP, Day 6SBP, Day 8SBP, Day 10DBP, Day 2DBP, Day 4DBP, Day 6DBP, Day 8DBP, Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 50.2-1.2-2.6-1.81.4-1.0-0.7-3.5-3.4-0.5

[back to top]

Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered

Blood pressure of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose) and Day 6

InterventionMillimeter of mercury (Mean)
SBPDBP
Nemiralisib 100 mcg-1.2-0.5

[back to top]

Change From Baseline in Temperature When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose

Temperature of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose), Days 2, 4, 6, 8 and 10

InterventionCelsius (Mean)
Day 2Day 4Day 6Day 8Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-0.03-0.07-0.03-0.08-0.07

[back to top]

Change From Baseline of Clinical Chemistry Parameters When Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose: Bilirubin, Direct Bilirubin and Creatinine

Blood samples were collected for the analysis of clinical chemistry parameters including bilirubin, direct bilirubin and creatinine at indicated time points. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline, Day 2, 4, 6, 8 and 10

InterventionMicromoles per liter (Mean)
Bilirubin, Day 2Bilirubin, Day 4Bilirubin, Day 6Bilirubin, Day 8Bilirubin, Day 10Direct bilirubin, Day 2Direct bilirubin, Day 4Direct bilirubin, Day 6Direct bilirubin, Day 8Direct bilirubin, Day 10Creatinine, Day 2Creatinine, Day 4Creatinine, Day 6Creatinine, Day 8Creatinine, Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 50.4281.7962.9072.3093.5062.9072.3941.7962.0522.9070.4422.2100.8840.4420.000

[back to top]

Change From Baseline of Clinical Chemistry Parameters When Nemiralisib 100 mcg When Co-administered With Itraconazole 200 mg Repeated Dose: Alkaline Phosphate, ALT and AST

Blood samples were collected for the analysis of clinical chemistry parameters including alkaline phosphate, ALT and AST at indicated time points. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline, Day 2, 4, 6, 8 and 10

InterventionInternational Units/ Liter (Mean)
Alkaline phosphate, Day 2Alkaline phosphate, Day 4Alkaline phosphate, Day 6Alkaline phosphate, Day 8Alkaline phosphate, Day 10ALT, Day 2ALT, Day 4ALT, Day 6ALT, Day 8ALT, Day 10AST, Day 2AST, Day 4AST, Day 6AST, Day 8AST, Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-7.0-8.5-7.2-7.6-5.3-3.2-3.2-2.9-2.6-2.8-2.6-3.0-2.4-3.2-2.0

[back to top]

Change From Baseline of Clinical Chemistry Parameters When Nemiralisib 100 mcg When Co-administered With Itraconazole 200 mg Repeated Dose: Calcium, Glucose, Potassium and Sodium

Blood samples were collected for the analysis of clinical chemistry parameters including calcium, glucose, potassium and sodium. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day -1), Day 2, 4, 6, 8 and 10

InterventionMillimoles/Liter (Mean)
Glucose, Day 2Glucose, Day 4Glucose, Day 6Glucose, Day 8Glucose, Day 10Calcium, Day 2Calcium, Day 4Calcium, Day 6Calcium, Day 8Calcium, Day 10Potassium, Day 2Potassium, Day 4Potassium, Day 6Potassium, Day 8Potassium, Day 10Sodium, Day 2Sodium, Day 4Sodium, Day 6Sodium, Day 8Sodium, Day 10
Nemiralisib 100 mcg With Itraconazole 200 mg-0.08-0.121.22-0.22-0.220.020.030.050.000.030.070.290.010.210.20-1.00.0-1.6-1.0-1.6

[back to top]

Number of Participants With Abnormal Urinalysis Parameter

The dipstick test gives results in a semi-quantitative manner and results for urinalysis parameters can be read as Trace and 2+ indicating proportional concentrations in the urine sample. Only participants with abnormal findings for urinalysis at any visit has been presented. (NCT03398421)
Timeframe: Days -1, 6 and 10

InterventionParticipants (Count of Participants)
Ketones, Day -1, Trace, n=20,19Protein, Day -1, Trace, n=20,19Erythrocytes, Day-1,Trace, n=20,19Erythrocytes, Day-1,2+, n=20,19Leukocytes, Day 6, Trace, n=20,0Leukocytes, Day 6, 2+, n=20,0
Nemiralisib 100 mcg201121

[back to top]

Change From Baseline of Clinical Chemistry Parameters When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered: Calcium, Glucose, Potassium and Sodium

Blood samples were collected for the analysis of clinical chemistry parameters including calcium, glucose, potassium and sodium. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day -1) and Day 6

InterventionMillimoles/Liter (Mean)
GlucoseCalciumPotassiumSodium
Nemiralisib 100 mcg-0.120.060.20-0.9

[back to top]

Change From Baseline of Clinical Chemistry Parameters When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered:Bilirubin, Direct Bilirubin and Creatinine

Blood samples were collected for the analysis of clinical chemistry parameters including bilirubin, direct bilirubin and creatinine at indicated time points. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionMicromoles per liter (Mean)
BilirubinDirect bilirubinCreatinine
Nemiralisib 100 mcg5.5572.394-3.094

[back to top]

Change From Baseline of Total Protein When Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose

Blood samples were collected for the analysis of total protein at indicated time points. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline, Day 2, 4, 6, 8 and 10

InterventionGram per liter (Mean)
Day 2Day 4Day 6Day 8Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-3.8-3.40.2-2.4-1.8

[back to top]

Cmax of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2

Blood samples were collected at indicated time points after administration of repeated doses of Itraconazole and Hydroxy Itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose (itraconazole) on Day 1; Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose (itraconazole) on Day 5

InterventionNanogram per milliliter (Geometric Mean)
Itraconazole, Day 1Itraconazole, Day 5Hydroxy Itraconazole, Day 1Hydroxy Itraconazole, Day 5
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5156.90472.52240.3541.2

[back to top]

Maximum Observed Plasma Concentration (Cmax) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time frames after the administration of study treatment to investigate pharmacokinetic parameters of Nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionPicogram per milliliter (Geometric Mean)
Day 1; n=20, 0
Nemiralisib 100 mcg478.7

[back to top]

Maximum Observed Plasma Concentration (Cmax) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time frames after the administration of study treatment to investigate pharmacokinetic parameters of Nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionPicogram per milliliter (Geometric Mean)
Day 5; n=0, 20
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5384.0

[back to top]

Number of Participants With Abnormal Microscopic Examinations: Casts, Epithelial Cells, Erythrocytes and Leukocytes

"A microscopic examination was performed as part of a routine urinalysis. The microscopic exam was performed on urine sediment - urine was centrifuged to concentrate the substances in it at the bottom of a tube. The fluid at the top of the tube was then discarded and the drops of fluid remaining were examined under a microscope. Cells, crystals, and other substances were counted and reported either as the number observed per low power field (LPF) or per high power field (HPF)." (NCT03398421)
Timeframe: Day -1

,
InterventionParticipants (Count of Participants)
Cast0, n=2,2Cast2, n=2,2Cast3, n=2,2Cast10, n=2,2Epithelial cells 0, n=2,2Epithelial cells 1, n=2,2Erythrocytes 1, n=2,2Erythrocytes 3, n=2,2Erythrocytes 7, n=2,2Erythrocytes 9, n=2,2Leukocytes 1, n=2,2Leukocytes 2, n=2,2
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5010111010111
Nemiralisib 100 mcg101020101020

[back to top]

Number of Participants With Abnormal Urinalysis Parameter

The dipstick test gives results in a semi-quantitative manner and results for urinalysis parameters can be read as Trace and 2+ indicating proportional concentrations in the urine sample. Only participants with abnormal findings for urinalysis at any visit has been presented. (NCT03398421)
Timeframe: Days -1, 6 and 10

InterventionParticipants (Count of Participants)
Ketones, Day -1, Trace, n=20,19Protein, Day -1, Trace, n=20,19Erythrocytes, Day-1,Trace, n=20,19Erythrocytes, Day-1,2+, n=20,19
Itraconazole 200 mg and 100mcg Nemiralisib on Day 52101

[back to top]

Area Under the Concentration-time Curve From Time Zero (Pre-dose) Extrapolated to Infinite Time (AUC[0-inf]) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time points after the administration of study treatment to investigate pharmacokinetic parameters of nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. Pharmacokinetic population comprised of all participants enrolled in the study who took at least 1 dose of nemiralisib and for whom a nemiralisib pharmacokinetic sample was obtained and analyzed. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHours*picogram per milliliter (Geometric Mean)
Day 1, n=20, 0
Nemiralisib 100 mcg3199.0

[back to top]

Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. A SAE is defined as any untoward medical occurrence that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly/birth defect, associated with liver injury and impaired liver function or any other situations as per Medical or scientific judgement. Safety population comprised of all participants enrolled in the study, who took at least one dose of study treatment. (NCT03398421)
Timeframe: Up to 35 days

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Itraconazole 200 mg and 100mcg Nemiralisib on Day 540
Nemiralisib 100 mcg10

[back to top]

Number of Participants With Urine Potential of Hydrogen (pH) at Indicated Time Points

Urine samples were collected for analysis of urine pH. pH is calculated on a scale of 0 to 14, values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH of less than 7 is acidic and a pH of greater than 7 is basic. Normal urine has a slightly acidic pH (5.0-6.0). (NCT03398421)
Timeframe: Day -1, 6 and 10

InterventionParticipants (Count of Participants)
Day -1, pH=5, n=20,19Day -1, pH=6, n=20,19Day -1, pH=7, n=20,19Day -1, pH=8, n=20,19Day 10, pH=5, n=0,20Day 10, pH=6, n=0,20Day 10, pH=7, n=0,20
Itraconazole 200 mg and 100mcg Nemiralisib on Day 58830947

[back to top]

Number of Participants With Urine Potential of Hydrogen (pH) at Indicated Time Points

Urine samples were collected for analysis of urine pH. pH is calculated on a scale of 0 to 14, values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH of less than 7 is acidic and a pH of greater than 7 is basic. Normal urine has a slightly acidic pH (5.0-6.0). (NCT03398421)
Timeframe: Day -1, 6 and 10

InterventionParticipants (Count of Participants)
Day -1, pH=5, n=20,19Day -1, pH=6, n=20,19Day -1, pH=7, n=20,19Day -1, pH=8, n=20,19Day 6, pH=5, n=20,0Day 6, pH=6, n=20,0Day 6, pH=7, n=20,0
Nemiralisib 100 mcg8921983

[back to top]

Specific Gravity at Indicated Time Points

Urine samples were collected for analysis of specific gravity of urine. Urinary specific gravity is the measure of the concentration solutes in the urine. It measures the ratio of urine density compared with water density and provides information on the kidney's ability to concentrate urine. (NCT03398421)
Timeframe: Days -1, 6 and 10

InterventionGrams per cubic centimeter (Mean)
Day -1, n=20, 19Day 10, n=0, 20
Itraconazole 200 mg and 100mcg Nemiralisib on Day 51.02071.0175

[back to top]

Specific Gravity at Indicated Time Points

Urine samples were collected for analysis of specific gravity of urine. Urinary specific gravity is the measure of the concentration solutes in the urine. It measures the ratio of urine density compared with water density and provides information on the kidney's ability to concentrate urine. (NCT03398421)
Timeframe: Days -1, 6 and 10

InterventionGrams per cubic centimeter (Mean)
Day -1, n=20, 19Day 6, n=20, 0
Nemiralisib 100 mcg1.01981.0188

[back to top]

T1/2 of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2

Blood samples were collected at indicated time points after administration of repeated doses of Itraconazole and Hydroxy Itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose (itraconazole) on Day 1; Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose (itraconazole) on Day 5

InterventionHour (Geometric Mean)
Itraconazole, Day 1Itraconazole, Day 5Hydroxy Itraconazole, Day 1Hydroxy Itraconazole, Day 5
Itraconazole 200 mg and 100mcg Nemiralisib on Day 53.865NANANA

[back to top]

Time to Maximum Observed Plasma Concentration (Tmax) of Nemiralisib in Plasma

Blood samples were collected at indicated time points after administration of repeated doses of itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHour (Median)
Day 1; n=20, 0
Nemiralisib 100 mcg0.070

[back to top]

Time to Maximum Observed Plasma Concentration (Tmax) of Nemiralisib in Plasma

Blood samples were collected at indicated time points after administration of repeated doses of itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHour (Median)
Day 5; n=0, 20
Itraconazole 200 mg and 100mcg Nemiralisib on Day 50.088

[back to top]

Tmax of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2

Blood samples were collected at indicated time points after administration of repeated doses of Itraconazole and Hydroxy Itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose (itraconazole) on Day 1; Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose (itraconazole) on Day 5

InterventionHour (Median)
Itraconazole, Day 1Itraconazole, Day 5Hydroxy Itraconazole, Day 1Hydroxy Itraconazole, Day 5
Itraconazole 200 mg and 100mcg Nemiralisib on Day 54.0014.0014.0044.004

[back to top]

Area Under the Concentration-time Curve From Time Zero (Pre-dose) Extrapolated to Infinite Time (AUC[0-inf]) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time points after the administration of study treatment to investigate pharmacokinetic parameters of nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. Pharmacokinetic population comprised of all participants enrolled in the study who took at least 1 dose of nemiralisib and for whom a nemiralisib pharmacokinetic sample was obtained and analyzed. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHours*picogram per milliliter (Geometric Mean)
Day 5, n=0, 14
Itraconazole 200 mg and 100mcg Nemiralisib on Day 56272.7

[back to top]

Apparent Terminal Half-life (t1/2) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time frames after the administration of study treatment to investigate pharmacokinetic parameters of Nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHours (Geometric Mean)
Day 5, n=0, 14
Itraconazole 200 mg and 100mcg Nemiralisib on Day 564.00

[back to top]

Apparent Terminal Half-life (t1/2) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time frames after the administration of study treatment to investigate pharmacokinetic parameters of Nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHours (Geometric Mean)
Day 1, n=20, 0
Nemiralisib 100 mcg40.03

[back to top]

Number of Participants With Abnormal Electrocardiogram (ECG) Findings

Full 12-lead ECGs were recorded with the participant in a supine position. The number of participants with abnormal clinically significant ECG findings for worst case post-Baseline is presented. (NCT03398421)
Timeframe: Period 1: Up to Day 6; Period 2: Up to Day 10

InterventionParticipants (Count of Participants)
Nemiralisib 100 mcg0
Itraconazole 200 mg and 100mcg Nemiralisib on Day 50

[back to top]

Change From Baseline of Total Protein When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered

Blood samples were collected for the analysis of total protein at indicated time points. Day -1 was defined as Baseline for clinical chemistry parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionGram per liter (Mean)
Nemiralisib 100 mcg3.3

[back to top]

Change From Baseline in Reticulocyte Percentage When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg

Blood samples were collected for the analysis of reticulocyte percentage at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 10

InterventionPercentage (Mean)
Itraconazole 200 mg and 100mcg Nemiralisib on Day 50.065

[back to top]

Area Under the Concentration-time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time frames after the administration of study treatment to investigate pharmacokinetic parameters of Nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHour*picogram per milliliter (Geometric Mean)
Day 1; n=20, 0
Nemiralisib 100 mcg2677.1

[back to top]

Area Under the Concentration-time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Nemiralisib in Plasma

Blood samples were collected from participants at indicated time frames after the administration of study treatment to investigate pharmacokinetic parameters of Nemiralisib in both treatment period 1 and 2. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Period 1: Pre-dose, and 5, 30 minutes, 2, 6, 12, 24, 48, 72, 96 and 120 hours post-dose on Day 1. Period 2: Pre-dose, and 5 min, 30 min, 2, 6, 12, 24, 48, 72, 96, 120 and 144 hours post-dose on Day 5

InterventionHour*picogram per milliliter (Geometric Mean)
Day 5; n=0, 20
Itraconazole 200 mg and 100mcg Nemiralisib on Day 54802.3

[back to top]

Change From Baseline in Reticulocyte Percentage When Single Oral Dose of Nemiralisib 100 mcg Administered

Blood samples were collected for the analysis of reticulocyte percentage at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionPercentage (Mean)
Nemiralisib 100 mcg-0.038

[back to top]

AUC(0-inf) of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2

Blood samples were collected at indicated time points after administration of repeated doses of itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose (itraconazole) on Day 1; Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose (itraconazole) on Day 5

InterventionHour*nanogram per milliliter (Geometric Least Squares Mean)
Itraconazole, Day 1Itraconazole, Day 5Hydroxy Itraconazole, Day 1Hydroxy Itraconazole, Day 5
Nemiralisib 100 mcg With Itraconazole 200 mg1201.3NANANA

[back to top]

AUC(0-t) of Itraconazole and Hydroxy Itraconazole When Co-administered With Nemiralisib in Treatment Period 2

Blood samples were collected at indicated time points after administration of repeated doses of Itraconazole along with Nemiralisib. Pharmacokinetic analysis was conducted using standard non-compartmental methods. (NCT03398421)
Timeframe: Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 hours post-dose (itraconazole) on Day 1; Pre-dose, 30 minutes, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose (itraconazole) on Day 5

InterventionHour*nanogram per milliliter (Geometric Mean)
Itraconazole, Day 1Itraconazole, Day 5Hydroxy Itraconazole, Day 1Hydroxy Itraconazole, Day 5
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5891.74939.61862.610106.4

[back to top]

Change From Baseline in Hematology Parameters When Single Oral Dose of Nemiralisib 100 mcg Administered: Lymphocytes, Neutrophils, Platelets, Basophils, Eosinophils, Monocytes, Erythrocytes and White Blood Cells (WBC)

Blood samples were collected for the analysis of hematology parameters including lymphocytes, neutrophils, platelets, basophils, eosinophils, monocytes, erythrocytes and WBCs at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

Intervention10^9 cells per liter (Mean)
LymphocytesNeutrophilsPlateletsBasophilsEosinophilsMonocytesErythrocytesWBC
Nemiralisib 100 mcg-0.2640.1988.40.003-0.038-0.054242.0-0.174

[back to top]

Change From Baseline in Hematology Parameters When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose: Lymphocytes, Neutrophils, Platelets, Basophils, Eosinophils, Monocytes, Erythrocytes and WBC

Blood samples were collected for the analysis of hematology parameters including lymphocytes, neutrophils, platelets, basophils, eosinophils, monocytes, erythrocytes and WBCs at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 10

Intervention10^9 cells per liter (Mean)
LymphocytesNeutrophilsPlateletsBasophilsEosinophilsMonocytesErythrocytesWBC
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-0.202-0.127-5.7-0.0040.003-0.01476.0-0.366

[back to top]

Change From Baseline in Pulse Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg Repeated Dose

Pulse rate of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose) and Days 2, 4, 6, 8 and 10

InterventionBeats per minute (Mean)
Day 2Day 4Day 6Day 8Day 10
Itraconazole 200 mg and 100mcg Nemiralisib on Day 51.93.21.43.52.3

[back to top]

Change From Baseline in Respiratory Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered

Respiratory rate of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose) and Day 6

InterventionBreaths per minute (Mean)
Nemiralisib 100 mcg-0.4

[back to top]

Change From Baseline in Pulse Rate When Single Inhaled Oral Dose of Nemiralisib 100 mcg Administered

Pulse rate of participants were measured at indicated time points in semi-supine position after 5 minutes rest. Day 1 (Pre-dose) value was defined as Baseline for vital sign parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline (Day 1, pre-dose) and Day 6

InterventionBeats per minute (Mean)
Nemiralisib 100 mcg-1.9

[back to top]

Change From Baseline in MCV When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg

Blood samples were collected for the analysis of MCV at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 10

InterventionFemtoliter (Mean)
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-1.09

[back to top]

Change From Baseline in MCH When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg

Blood samples were collected for the analysis of MCH at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 10

InterventionPicograms per liter (Mean)
Itraconazole 200 mg and 100mcg Nemiralisib on Day 5-0.12

[back to top]

Change From Baseline in Hemoglobin When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg

Blood samples were collected for the analysis of hemoglobin at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 10

InterventionGrams per liter (Mean)
Itraconazole 200 mg and 100mcg Nemiralisib on Day 51.9

[back to top]

Change From Baseline in Hemoglobin When Single Oral Dose of Nemiralisib 100 mcg Administered

Blood samples were collected for the analysis of hemoglobin at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionGrams per liter (Mean)
Nemiralisib 100 mcg7.3

[back to top]

Change From Baseline in Hematocrit When Single Oral Dose of Nemiralisib 100 mcg Co-administered With Itraconazole 200 mg

Blood samples were collected for the analysis of hematocrit at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 10

InterventionPercentage of red blood cells in blood (Mean)
Itraconazole 200 mg and 100mcg Nemiralisib on Day 50.14

[back to top]

Change From Baseline in Hematocrit When Single Oral Dose of Nemiralisib 100 mcg Administered

Blood samples were collected for the analysis of hematocrit at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionPercentage of red blood cells in blood (Mean)
Nemiralisib 100 mcg1.94

[back to top]

Change From Baseline in Erythrocyte Mean Corpuscular Volume (MCV) When Single Oral Dose of Nemiralisib 100 mcg Administered

Blood samples were collected for the analysis of MCV at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionFemtoliter (Mean)
Nemiralisib 100 mcg-0.47

[back to top]

Change From Baseline in Erythrocyte Mean Corpuscular Hemoglobin (MCH) When Single Oral Dose of Nemiralisib 100 mcg Administered

Blood samples were collected for the analysis of MCH at indicated time points. Day -1 was defined as Baseline for hematology parameters. Change from Baseline is calculated as the value at specified time point minus the Baseline value. (NCT03398421)
Timeframe: Baseline and Day 6

InterventionPicograms per liter (Mean)
Nemiralisib 100 mcg-0.03

[back to top]

Pharmacokinetics: AUC(0-24) of KD025m1 for Part 1 and for Part 2

Area under concentration-time curve from zero hours to 24 hours post-dose (AUC[0-24]) for Metabolite 1, KD025m1, for subjects in Part 1 and for subjects in Part 2 (NCT03530995)
Timeframe: Part 1: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12, and 24 hours post-dose; Part 2: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22, and 24 hours post-dose

Intervention(ng*h)/mL (Geometric Mean)
Part 1, Period 1: Belumosudil Alone75.6
Part 1, Period 4: Belumosudil + Rifampicin148
Part 2, Period 1: Belumosudil Alone138
Part 2, Period 2: Belumosudil + Omeprazole91.5

[back to top]

Pharmacokinetics: Cmax of KD025m1 in Part 1

Maximum concentration (Cmax) of Metabolite 1 (KD025m1) for belumosudil alone and for belumosudil + rifampicin up to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose

Interventionng/mL (Geometric Mean)
Part 1, Period 1: Belumosudil Alone23.2
Part 1, Period 4: Belumosudil + Rifampicin52.5

[back to top]

Pharmacokinetics: AUC(0-inf) and AUC(0-24) of KD025 and KD025 m2 for Subject in Part 1 and Part 2

Area under concentration-time curve from zero hours to infinity (AUC[0-inf]) and from zero hours to 24 hours post-dose (AUC[0-24)) for the parent drug KD025, and Metabolite 2, KD025m2, for subjects up to 48 hours each for Part 1 and for Part 2 (NCT03530995)
Timeframe: Part 1: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose; Part 2: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22,24,36, and 48 hours post-dose

,,,,,
Intervention(ng*h)/mL (Geometric Mean)
AUC(0-inf): KD025AUC(0-inf): KD025m2AUC(0-24): KD025AUC(0-24): KD025m2
Part 1, Period 1: Belumosudil Alone9080123084301100
Part 1, Period 2: Belumosudil + Itraconazole1120084310400745
Part 1, Period 3: Belumosudil + Rabeprazole16801741510110
Part 1, Period 4: Belumosudil + Rifampicin25003962490376
Part 2, Period 1: Belumosudil Only188001900168001950
Part 2, Period 2: Belumosudil + Omeprazole988011107970767

[back to top]

Pharmacokinetics: Cmax of KD025 and KD025m2 in Part 1

Maximum concentration (Cmax) of the parent drug, KD025, Metabolite 1 (KD025m1), and Metabolite 2 (KD025m2) for belumosudil alone, belumosudil + itraconazole, belumosudil + rabeprazole, and belumosudil + rifampicin at 0 to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose

,,,
Interventionng/mL (Geometric Mean)
Parent Drug KD025KD025m2
Part 1, Period 1: Belumosudil Alone1770337
Part 1, Period 2: Belumosudil + Itraconazole2130221
Part 1, Period 3: Belumosudil + Rabeprazole22723.5
Part 1, Period 4: Belumosudil + Rifampicin712148

[back to top]

Pharmacokinetics: Cmax of KD025, KD025m1, and KD025m2 in Part 2

Maximum concentration (Cmax) of the parent drug (KD025), for Metabolite 1 (KD025m1), and for Metabolite 2 (KD025m2), for belumosudil alone and for belumosudil + omeprazole up to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22,24,36, and 48 hours post-dose

,
Interventionng/mL (Geometric Mean)
Cmax--1st dose: KD025Cmax--2nd dose: KD025Cmax--1st Dose: KD025m1Cmax--2nd Dose: KD025m1Cmax--1st Dose: KD025m2Cmax--2nd Dose: KD025m2
Part 2, Period 1: Belumosudil Alone1790176023.823.6282257
Part 2, Period 2: Belumosudil + Omeprazole57590318.018.972.3115

[back to top]

Comparison of Plasma Itraconazole Levels and Hydroxyitraconazole Levels at Day 14

Percentage of participants to achieve therapeutic itraconazole and hydroxyitraconazole levels by evaluating Inter-patient variability as calculated by co-efficient of variation on plasma specimens collected on Day 14 (NCT03572049)
Timeframe: Day 14

Interventionpercentage of participants (Number)
SUBA Itraconazole60.5
Conventional Itraconazole71.0

[back to top]

Comparison of Plasma Itraconazole Levels and Hydroxyitraconazole Levels at Day 42

Percentage of patients with therapeutic itraconazole and hydroxyitraconazole levels as measured in plasma trough levels Day 42 (NCT03572049)
Timeframe: Day 42

Interventionpercentage of participants (Number)
SUBA Itraconazole69.3
Conventional Itraconazole58.0

[back to top] [back to top]

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

We will measure specific signs and symptoms related to endemic fungal infection, comparing baseline findings to Day 42 findings using physical examination and patient history. (NCT03572049)
Timeframe: Day 42

InterventionParticipants (Count of Participants)
SUBA Itraconazole29
Conventional Itraconazole30

[back to top]

The Number of Days of Hospitalization at Day 180

The number of days of Hospitalization occurring between Day 1-180 (NCT03572049)
Timeframe: Day 180

InterventionDays (Mean)
SUBA Itraconazole5
Conventional Itraconazole7

[back to top]

Maximum Plasma Concentration (Cmax) for M3 Metabolite

Cmax is the observed peak analyte concentration obtained directly from the experimental data without interpolation, expressed in concentration units. (NCT03579719)
Timeframe: Day 10 of Period 1, Day 10 and Day 15 of Period 2

Interventionng/mL (Geometric Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole19.921.328.6

[back to top]

Maximum Plasma Concentration (Cmax) for M2 Metabolite (as Applicable)

Cmax is the observed peak analyte concentration obtained directly from the experimental data without interpolation, expressed in concentration units. (NCT03579719)
Timeframe: Day 10 of Period 1, Day 10 and Day 15 of Period 2

Interventionng/mL (Geometric Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole11.06.347.60

[back to top]

Trough Plasma Concentration (Ctrough) for M3 Metabolite

(NCT03579719)
Timeframe: Day 10 of Period 1; Day 10 and Day 15 of Period 2

Interventionng/mL (Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole15.118.923.9

[back to top]

Trough Plasma Concentration (Ctrough) for M2 Metabolite (as Applicable)

(NCT03579719)
Timeframe: Day 10 of Period 1; Day 10 and Day 15 of Period 2

Interventionng/mL (Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole9.935.826.88

[back to top]

Trough Plasma Concentration (Ctrough) for Balovaptan

(NCT03579719)
Timeframe: Day 10 of Period 1; Day 10 and Day 15 of Period 2

Interventionng/mL (Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole13.391.9102

[back to top]

Time to Maximum Observed Plasma Concentration (Tmax) for M3 Metabolite

(NCT03579719)
Timeframe: Day 10 of Period 1; Day 10 and Day 15 of Period 2

InterventionHour(s) (Median)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole4.009.003.50

[back to top]

Time to Maximum Observed Plasma Concentration (Tmax) for M2 Metabolite (as Applicable)

(NCT03579719)
Timeframe: Day 10 of Period 1; Day 10 and Day 15 of Period 2

InterventionHour(s) (Median)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole5.006.006.00

[back to top]

Time to Maximum Observed Plasma Concentration (Tmax) for Balovaptan

(NCT03579719)
Timeframe: Day 10 of Period 1; Day 10 and Day 15 of Period 2

InterventionHour(s) (Median)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole3.004.004.00

[back to top]

Maximum Plasma Concentration (Cmax) for Balovaptan

Cmax is the observed peak analyte concentration obtained directly from the experimental data without interpolation, expressed in concentration units. (NCT03579719)
Timeframe: Day 10 of Period 1, Day 10 and Day 15 of Period 2

Interventionng/mL (Geometric Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole31.5125140

[back to top]

Area Under the Concentration Vs Time Curve Over the Dosing Interval (AUC0-tau) for M3 Metabolite

(NCT03579719)
Timeframe: Day 10 of Period 1, Day 10 and Day 15 of Period 2

Interventionng.h/mL (Geometric Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole402449570

[back to top]

Area Under the Concentration Vs Time Curve Over the Dosing Interval (AUC0-tau) for M2 Metabolite (as Applicable)

(NCT03579719)
Timeframe: Day 10 of Period 1, Day 10 and Day 15 of Period 2

Interventionng.h/mL (Geometric Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole230129156

[back to top]

Area Under the Concentration Vs Time Curve Over the Dosing Interval (AUC0-tau) for Balovaptan

(NCT03579719)
Timeframe: Day 10 of Period 1, Day 10 and Day 15 of Period 2

Interventionng.h/mL (Geometric Mean)
Balovaptan Day 10 of Period 1Balovaptan + itraconazole Day 10 of Period 2Balovaptan + itraconazole Day 15 of Period 2
Balovaptan + Itraconzole46423042587

[back to top]

Percentage of Participants With Adverse Events

(NCT03579719)
Timeframe: Up to 21 days postdose

InterventionPercentage (Number)
Balovaptan + Itraconzole73

[back to top]

Time to Steady State for Balovaptan

(NCT03579719)
Timeframe: Days 1, 3, 5, 8, 9, 10 in Period 1 and Days 1, 3, 5, 8, 9, 10, 13, 14, 15 in Period 2

InterventionDay (Number)
BalovaptanBalovaptan + itraconazole
Balovaptan + Itraconzole413

[back to top]

Maximum Measured Concentration of BI 894416 in Plasma (Cmax)

Cmax, maximum measured concentration of BI 894416 in plasma is presented. Standard error (SE) is actually geometric (g) SE. Pharmacokinetic (PK) samples were collected 3 hours (h) prior dosing and 15minutes (min), 30 min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h and 34h after BI 894416 on day 1 of both periods and additionally on 48h and 72h after BI 894416 administration in period 2. (NCT03722173)
Timeframe: Up to 34 h (period 1) and up to 72 h (period 2) (please refer timeframe in detail in description)

InterventionNanomole/ Litre (nmol/ L) (Geometric Mean)
BI 894416 Alone (R)59.93
BI 894416 + Itraconazole (T)67.91

[back to top]

Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)

AUC0-tz, area under the concentration-time curve of BI 894416 in plasma over the time interval from 0 to the last quantifiable data point is presented. Standard Error (SE) is actually a geometric (g) SE. Pharmacokinetic (PK) samples were collected 3 hours (h) prior dosing and 15 minutes (min), 30 min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h and 34h after BI 894416 on day 1 of both periods and additionally on 48h and 72h after BI 894416 administration in period 2. (NCT03722173)
Timeframe: Up to 34 h (period 1) and up to 72 h (period 2) (please refer timeframe in detail in description)

InterventionNanomole*hour / Litre (nmol*h/ L) (Geometric Mean)
BI 894416 Alone (R)371.77
BI 894416 + Itraconazole (T)526.50

[back to top]

Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)

AUC0-∞, area under the concentration-time curve of BI 894416 in plasma over the time interval from 0 extrapolated to infinity is presented. Standard error (SE) is actually geometric (g) SE. Pharmacokinetic (PK) samples were collected 3 hours (h) prior dosing and 15minutes (min), 30 min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h and 34h after BI 894416 on day 1 of both periods and additionally on 48h and 72h after BI 894416 administration in period 2. (NCT03722173)
Timeframe: Up to 34 h (period 1) and up to 72 h (period 2) (please refer timeframe in detail in description)

InterventionNanomole*hour / Litre (nmol*h/ L) (Geometric Mean)
BI 894416 Alone (R)384.01
BI 894416 + Itraconazole (T)547.36

[back to top]

Change in Suicide Risk as Assessed Using the Columbia Suicide Severity Rating Scale (C-SSRS)

"The C-SSRS is an assessment tool to evaluate suicidal ideation and behavior. Categories have binary responses (yes/no) and include: Wish to be Dead; Non-specific Active Suicidal Thoughts; Active Suicidal Ideation with Any Methods (Not Plan) without Intent to Act; Active Suicidal Ideation with Some Intent to Act, without Specific Plan; Active Suicidal Ideation with Specific Plan and Intent, Preparatory Acts and Behavior; Aborted Attempt; Interrupted Attempt; Actual Attempt (non-fatal); Completed Suicide. Suicidal ideation or behavior is indicated by a yes answer to any of the listed categories. A score of 0 is assigned if no suicide risk is present." (NCT03774576)
Timeframe: From screening visit through Period 2 Day 11

,
InterventionUnits on a scale (Mean)
ScreeningPeriod 2 Day 11
RO7017773 + Itraconazole00
RO7017773 Alone00

[back to top]

Cmax of Itraconazole in Plasma

(NCT03774576)
Timeframe: Period 2

Interventionng/mL (Geometric Mean)
RO7017773 Alone724

[back to top]

Maximum Concentration (Cmax) of RO7017773 in Plasma

(NCT03774576)
Timeframe: Period 1 (RO7017773) and Period 2 (RO7017773 + Itraconazole)

Interventionng/mL (Geometric Mean)
RO7017773 Alone458
RO7017773 + Itraconazole516

[back to top]

Percentage of Participants With Adverse Events (AEs)

(NCT03774576)
Timeframe: 12 weeks

InterventionPercentage of Participants (Number)
RO7017773 Alone57.1
Itraconazole Alone14.3
RO7017773 + Itraconazole53.8

[back to top]

Area Under the Concentration-time Curve of the BI 730357 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)

AUC0-∞, area under the concentration-time curve of the BI 730357 in plasma over the time interval from 0 extrapolated to infinity is presented here. (NCT03782987)
Timeframe: Pharmacokinetic samples were taken within 3 hours (h) before administration of BI 730357 and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 34, 47, 71, 119 and 167 h in both periods and additionally at 215 and 263 h only for period 2.

Interventionnmol*h/ L (Geometric Mean)
BI 730357 + Itraconazole (T)64934.55
BI 730357 (R)6971.67

[back to top]

Maximum Measured Concentration of the BI 730357 in Plasma (Cmax)

Cmax, maximum measured concentration of the BI 730357 in plasma is presented here. (NCT03782987)
Timeframe: Pharmacokinetic samples were taken within 3 hours (h) before administration of BI 730357 and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 34, 47, 71, 119 and 167 h in both periods and additionally at 215 and 263 h only for period 2.

Interventionnmol/ L (Geometric Mean)
BI 730357 + Itraconazole (T)311.01
BI 730357 (R)186.36

[back to top]

Area Under the Concentration-time Curve of the BI 730357 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)

AUC0-tz, area under the concentration-time curve of the BI 730357 in plasma over the time interval from 0 to the last quantifiable data point is presented. (NCT03782987)
Timeframe: Pharmacokinetic samples were taken within 3 hours (h) before administration of BI 730357 and at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 34, 47, 71, 119 and 167 h in both periods and additionally at 215 and 263 h only for period 2.

InterventionNanomole* hour/ Litre (nmol*h/ L) (Geometric Mean)
BI 730357 + Itraconazole (T)43239.08
BI 730357 (R)6657.49

[back to top]

Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32914

(NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr (Median)
Part 1, Treatment A6.00
Part 1, Treatment B8.00
Part 2, Treatment C6.00
Part 2, Treatment D4.00

[back to top]

Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32960

(NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr (Median)
Part 1, Treatment A6.00
Part 1, Treatment B8.00
Part 2, Treatment C6.00
Part 2, Treatment D2.00

[back to top]

Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of TAK-788

(NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr (Median)
Part 1, Treatment A6.00
Part 1, Treatment B8.00
Part 2, Treatment C6.00
Part 2, Treatment D4.00

[back to top]

Treatment B Vs Treatment A (Part 1), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure AUC∞ for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar AUC∞ which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in hour*nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr*nM (Geometric Mean)
Part 1, Treatment A298
Part 1, Treatment B1820

[back to top]

Treatment B vs Treatment A (Part 1), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure Cmax for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar Cmax which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

InterventionnM (Geometric Mean)
Part 1, Treatment A13.7
Part 1, Treatment B39.2

[back to top]

Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure AUC∞ for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar AUC∞ which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in hour*nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Interventionhr*nM (Geometric Mean)
Part 2, Treatment C3610
Part 2, Treatment D194

[back to top]

Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure Cmax for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar Cmax which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

InterventionnM (Geometric Mean)
Part 2, Treatment C177
Part 2, Treatment D14.9

[back to top]

Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters (Median)
Part B: Pamiparib34.697
Part B:Pamiparib + Itraconazole37.589

[back to top]

Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters (Median)
Part A: Pamiparib35.491
Part A: Pamiparib + Rifampin37.712

[back to top]

AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge) 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhours*nanograms/milliLiter (h*ng/mL) (Median)
Part B: Pamiparib9163
Part B: Pamiparib + Itraconazole8894

[back to top]

Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part B: Pamiparib9.290
Part B:Pamiparib + Itraconazole11.179

[back to top]

Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part A: Pamiparib13.381
Part A: Pamiparib + Rifampin7.667

[back to top]

Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters/hour (L/h) (Median)
Part B: Pamiparib1.987
Part B:Pamiparib + Itraconazole2.147

[back to top]

Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters/hour (L/h) (Median)
Part A: Pamiparib2.132
Part A: Pamiparib + Rifampin3.232

[back to top]

AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhr*ng/mL (Median)
Part A: Pamiparib28142
Part A: Pamiparib + Rifampin18563

[back to top]

AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, and 9 hours post-dose

Interventionhr*ng/mL (Median)
Part B: Pamiparib4267.86
Part B:Pamiparib + Itraconazole3812.39

[back to top]

AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, and 9 hours post-dose

Interventionhr*ng/mL (Median)
Part A: Pamiparib11821.06
Part A: Pamiparib + Rifampin10515.14

[back to top]

AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, and 12 hours post-dose

Interventionhr*ng/mL (Median)
Part A: Pamiparib14642.90
Part A: Pamiparib + Rifampin12262.61

[back to top]

AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhours*nanograms/milliLiter (h*ng/mL) (Median)
Part A: Pamiparib28868
Part A: Pamiparib + Rifampin18351

[back to top]

AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, and 12 hours post-dose

Interventionhr*ng/mL (Median)
Part B: Pamiparib5097.06
Part B: Pamiparib + Itraconazole4647.47

[back to top]

AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge) 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhr*ng/mL (Median)
Part B: Pamiparib10072
Part B:Pamiparib + Itraconazole9353

[back to top]

Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionng/mL (Median)
Part A: Pamiparib1970
Part A: Pamiparib + Rifampin1820

[back to top]

Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge; ) 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionng/mL (Median)
Part B: Pamiparib730.5
Part B: Pamiparib + Itraconazole752.5

[back to top]

Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part A: Pamiparib2.000
Part A: Pamiparib + Rifampin2.000

[back to top]

Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part B: Pamiparib2.000
Part B:Pamiparib + Itraconazole1.000

[back to top]

Number of Participants With Clinically Significant Abnormalities in Laboratory Assessments, Vital Signs, ECG Parameters and Physical Examinations

(NCT03994211)
Timeframe: Up to approximately 26 months

,,
InterventionNumber of participants (Number)
Laboratory AssessmentsVital SignsPhysical ExaminationsECG Parameters
Core Phase: Arm A: Pamiparib + Rifampin0000
Core Phase: Arm B: Pamiparib + Itraconazole0000
Extension Phase0000

[back to top]

Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

TEAE is defined as any AE with an onset date on or after the date of first dose of study medication until the date of last study medication dose plus 30 days. Seriousness of the AE is determined by the investigator based on seriousness criteria. (NCT03994211)
Timeframe: From the date informed consent has been signed until last study medication dose plus 30 days (up to approximately 26 months)

,,
InterventionNumber of participants (Number)
All TEAEsSerious TEAEs
Core Phase: Arm A: Pamiparib + Rifampin50
Core Phase: Arm B: Pamiparib + Itraconazole61
Extension Phase182

[back to top]

Cmax

maximum concentration during the time interval (NCT04035187)
Timeframe: 0-72hr

Interventionng/mL (Mean)
Fast Tablet174.3
Medium Tablet108.5
Slow Tablet121.3
Oral Solution266.7

[back to top]

AUC

area under the curve from 0-72hr (NCT04035187)
Timeframe: 0-72hr

Interventionng*hr/mL (Mean)
Fast Tablet1624.8
Medium Tablet1365.5
Slow Tablet1282.2
Oral Solution1848.7

[back to top]

Part C: Time to Maximum Observed Plasma Drug Concentration (Tmax) Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, and 10 hours post-dose

InterventionHour (Median)
Part C: GSK3915393 100 mcg IV0.98

[back to top]

Part C: t1/2 of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. For Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, concentrations after 24 hours post-dose were expected to be non-quantifiable. t1/2 was derived based on collected assessments (up to 24 hours for Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, up to 60 hours for Part C: GSK3915393 20 mg+ ITZ). Only the quantifiable concentration time points were to be considered for assessment of pharmacokinetic parameters. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48 and 60 hours post-dose

InterventionHours (Median)
Part C: GSK3915393 20 mg+ WaterNA
Part C: GSK3915393 20 mg+ GFJNA
Part C: GSK3915393 20 mg+ ITZNA

[back to top]

Part C: t1/2 of GSK3915393 Following IV Dose of GSK3915393+ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, and 60 hours post-dose

InterventionHour (Median)
Part C: GSK3915393 100 mcg IV+ITZNA

[back to top] [back to top]

Part C: Number of Participants With Abnormal Physical Examination Findings Following Administration of GSK3915393

A full physical examination was performed which included, at a minimum, assessments of the Skin, Cardiovascular, Respiratory, Gastrointestinal and Neurological systems. (NCT04604795)
Timeframe: Up to 72 days

InterventionParticipants (Count of Participants)
Part C: GSK3915393 100 mcg IV0
Part C: GSK3915393 100 mcg+ITZ0
Part C: GSK3915393 20mg+Water0
Part C: GSK3915393 20mg+GFJ0
Part C: SK3915393 20 mg+ITZ0

[back to top]

Part C: Maximum Observed Plasma Drug Concentration (Cmax) Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, and 10 hours post-dose

InterventionNanogram per milliliter (Geometric Mean)
Part C: GSK3915393 100 mcg IV4.7220

[back to top]

Part C: Fraction of Drug Escaping Hepatic Metabolism (FH) Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. FH was expressed as ratio and was calculated as: 1 minus hepatic extraction ratio. Hepatic extraction ratio=hepatic blood clearance (milliliters per minute)/hepatic blood flow (milliliters per minute) (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hour 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, 48, and 60 hours post-dose

InterventionRatio (Median)
Part C: GSK3915393 20 mg+ Water0.6525

[back to top]

Part C: Fraction of Drug Escaping Gut Metabolism (FG) Following Oral Administration of GSK3915393+Water

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. FG was expressed as ratio and calculated as: AUC of GSK3915393+water divided by AUC of GSK3915393+GFJ. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, and 24 hours post-dose

InterventionRatio (Median)
Part C: GSK3915393 20 mg+ WaterNA

[back to top]

Part C: Fraction of Drug Absorbed (FA) Following Oral Administration of GSK3915393+Water

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. FA was expressed as ratio was calculated as absolute bioavailability (F) divided by the product of fraction of drug escaping hepatic metabolism (FH) and fraction of drug escaping gut metabolism (FG). (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, and 24 hours post-dose

InterventionRatio (Median)
Part C: GSK3915393 20 mg+ WaterNA

[back to top]

Part C: FH Following IV Administration of GSK3915393+ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. FH was expressed as ratio and was calculated as: 1 minus Hepatic extraction ratio. Hepatic extraction ratio=hepatic blood clearance (milliliters per minute)/hepatic blood flow (milliliters per minute) (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hour 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, and 60 hours post-dose

InterventionRatio (Median)
Part C: GSK3915393 100 mcg IV+ITZ0.8717

[back to top]

Part C: Cmax of GSK3915393 Following IV Dose of GSK3915393+ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, and 60 hours post-dose

InterventionNanogram per milliliter (Geometric Mean)
Part C: GSK3915393 100 mcg IV+ITZ7.8839

[back to top]

Part C: Cmax Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. For Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, concentrations after 24 hours post-dose were expected to be non-quantifiable. Cmax was derived based on collected assessments (up to 24 hours for Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, up to 60 hours for Part C: GSK3915393 20 mg+ ITZ). Only the quantifiable concentration time points were to be considered for assessment of pharmacokinetic parameters. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48 and 60 hours post-dose

InterventionNanogram per milliliter (Geometric Mean)
Part C: GSK3915393 20 mg+ Water145.5638
Part C: GSK3915393 20 mg+ GFJ145.0510
Part C: GSK3915393 20 mg+ ITZ982.5433

[back to top]

Part C: AUCLST(0-24) of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14 and 24 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part C: GSK3915393 20 mg+ Water153.8368
Part C: GSK3915393 20 mg+ GFJ223.1288
Part C: GSK3915393 20 mg+ ITZ2129.2407

[back to top]

Part C: AUCLST(0-24) of GSK3915393 Following IV Dose of GSK3915393+ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, and 24 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part C: GSK3915393 100 mcg IV+ITZ13.3393

[back to top]

Part C: AUC(0-inf) of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. For Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, concentrations after 24 hours post-dose were expected to be non-quantifiable. AUC(0-inf) was derived based on collected assessments (up to 24 hours for Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, up to 60 hours for Part C: GSK3915393 20 mg+ ITZ). Only the quantifiable concentration time points were to be considered for assessment of pharmacokinetic parameters. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48 and 60 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part C: GSK3915393 20 mg+ Water155.5203
Part C: GSK3915393 20 mg+ GFJ225.0856
Part C: GSK3915393 20 mg+ ITZ2141.8345

[back to top]

Part C: AUC(0-inf) of GSK3915393 Following IV Dose of GSK3915393+ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, and 60 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part C: GSK3915393 100 mcg IV+ITZ13.4250

[back to top]

Part C: AUC From Time Zero to Infinity (AUC[0-inf]) Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, and 10 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part C: GSK3915393 100 mcg IV5.0325

[back to top]

Part C: Area Under Curve up to the Last Measurable Concentration (AUCLST[0-10]) Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, and 10 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part C: GSK3915393 100 mcg IV5.0061

[back to top]

Part C: Apparent Terminal Half-life (t1/2) of GSK3915393 Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, and 10 hours post-dose

InterventionHours (Median)
Part C: GSK3915393 100 mcg IVNA

[back to top]

Part B: Trough Concentration (Ctau) Following Dose of 20 mg BID and 80 mg BID of GSK3915393 on Day 14

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Day 14: Pre-dose, 20, 40 minutes, 1, 1.5 ,2, 3, 4, 6, 10, 10 hour 20 minutes, 10 hours 40 minutes, 12, 12.5, 13, 14, 16 and 24 hours post-dose

InterventionNanograms per milliliter (Mean)
Part B: GSK3915393 20 mg (BID)1.8808
Part B: GSK3915393 80 mg (BID)3.3181

[back to top]

Part B: Trough Concentration (Ctau) Following Dose of 160 mg of GSK3915393 on Day 14

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Day 14: Pre-dose, 20, 40 minutes, 1, 1.5 ,2, 3, 4, 6, 10, and 24 hours post-dose

InterventionNanograms per milliliter (Mean)
Part B: GSK3915393 160 mg (QD)2.5423

[back to top] [back to top]

Part B: Number of Participants With Abnormal Physical Examination Findings Following Administration of Repeat Oral Dose of GSK3915393

A full physical examination was performed which included, at a minimum, assessments of the Skin, Cardiovascular, Respiratory, Gastrointestinal and Neurological systems. (NCT04604795)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Part B: Placebo0
Part B: GSK3915393 20 mg (BID)0
Part B: GSK3915393 80 mg (BID)0
Part B: GSK3915393 160 mg (QD)0

[back to top]

Part A: Volume of Distribution (Vd) Following Single IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionLiters (Geometric Mean)
Part A: GSK3915393 100 mcg IV30.7890

[back to top]

Part A: Tmax Following Single Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, 24 and 36 hours post-dose

InterventionHour (Median)
Part A: GSK3915393 15 mg1.50
Part A: GSK3915393 60 mg1.52
Part A: GSK3915393 160 mg1.50

[back to top]

Part A: Tmax Following IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionHour (Median)
Part A: GSK3915393 100 mcg IV0.98

[back to top]

Part A: t1/2 Following Single IV Dose of GSK3915393 100 mcg IV

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionHour (Median)
Part A: GSK3915393 100 mcg IVNA

[back to top]

Part A: Product of Fraction of Drug Absorbed and Fraction of Drug Escaping Gut Metabolism (FA*FG) Following Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. Product of FA*FG was calculated as: (absolute bioavailability [F] divided by fraction of drug escaping hepatic metabolism [FH]). (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, 24 and 36 hours post-dose

InterventionRatio (Median)
Part A: GSK3915393 15 mg0.3062
Part A: GSK3915393 60 mg0.3814
Part A: GSK3915393 160 mg0.5563

[back to top] [back to top]

Part A: Number of Participants With Abnormal Physical Examination Findings Following Administration of Oral Dose

A full physical examination was performed which included, at a minimum, assessments of the Skin, Cardiovascular, Respiratory, Gastrointestinal and Neurological systems. (NCT04604795)
Timeframe: Up to 70 days

InterventionParticipants (Count of Participants)
Part A: Placebo0
Part A: GSK3915393 15 mg0
Part A: GSK3915393 60 mg0
Part A: GSK3915393 160 mg0

[back to top]

Part A: Number of Participants With Abnormal Physical Examination Findings Following Administration of IV Dose of GSK3915393

A full physical examination was performed which included, at a minimum, assessments of the Skin, Cardiovascular, Respiratory, Gastrointestinal and Neurological systems. (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
Part A: GSK3915393 100 mcg IV0

[back to top]

Part A: Fraction of Drug Escaping Hepatic Metabolism (FH) Following Single Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. FH was expressed as ratio and was calculated as: 1 minus hepatic extraction ratio. Hepatic extraction ratio=hepatic blood clearance (milliliters per minute)/hepatic blood flow (milliliters per minute). (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, 24 and 36 hours post-dose

InterventionRatio (Median)
Part A: GSK3915393 15 mg0.5367
Part A: GSK3915393 60 mg0.4617
Part A: GSK3915393 160 mg0.5107

[back to top]

Part A: Cmax Following Single Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, 24 and 36 hours post-dose

InterventionNanogram per milliliter (Geometric Mean)
Part A: GSK3915393 15 mg58.7910
Part A: GSK3915393 60 mg235.4331
Part A: GSK3915393 160 mg1246.2994

[back to top]

Part A: Cmax Following Single IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionNanogram per milliliter (Geometric Mean)
Part A: GSK3915393 100 mcg IV4.3979

[back to top]

Part A: Clearance (CL) Following Single IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionLiters per hour (Geometric Mean)
Part A: GSK3915393 100 mcg IV22.7675

[back to top]

Part A: AUCLST(0-24) Following Single Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, and 24 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part A: GSK3915393 15 mg113.7272
Part A: GSK3915393 60 mg424.6809
Part A: GSK3915393 160 mg2221.3816

[back to top]

Part A: AUC(0-inf) Following Single Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, 24 and 36 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part A: GSK3915393 15 mg116.5279
Part A: GSK3915393 60 mg431.3298
Part A: GSK3915393 160 mg2235.3991

[back to top]

Part A: AUC(0-inf) Following Single IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part A: GSK3915393 100 mcg IV4.4790

[back to top]

Part A: Absolute Bioavailability (F) Following Single Oral Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. Absolute bioavailability is the amount of drug from a formulation that reaches the systemic circulation relative to an IV dose. It was expressed as ratio was calculated as (AUC[0-inf] for oral divided by oral dose) divided by (AUC[0-inf] for IV/dose given as IV). (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 12, 14, 24 and 36 hours post-dose

InterventionRatio (Geometric Mean)
Part A: GSK3915393 15 mg0.20
Part A: GSK3915393 60 mg0.18
Part A: GSK3915393 160 mg0.29

[back to top]

Part B: Tmax(0-10) Following Dosing of GSK3915393 on Days 1 and 14

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: Pre-dose, 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, and 10 hours post-dose

,,
InterventionHour (Median)
Day 1, n=10, 9, 9Day 14, n=9, 9, 9
Part B: GSK3915393 160 mg (QD)1.50000.6833
Part B: GSK3915393 20 mg (BID)1.25831.5000
Part B: GSK3915393 80 mg (BID)1.01670.7500

[back to top]

Part A: AUCLST(0-6) Following Single IV Dose of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5 and 6 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
Part A: GSK3915393 100 mcg IV4.4466

[back to top]

Part B: Tmax(0-10) Following First Dosing of GSK3915393 on Days 3, 5 and 7 (for Food-effect Assessment)

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 3, 5 and 7: Pre-dose, 20, 40 minutes, 1, 1.5, 2, 3, 4, 6 and 10 hours post-dose

,,
InterventionHour (Median)
Day 3, n=10, 9, 9Day 5, n= 10, 9, 9Day 7, n= 9, 9, 9
Part B: GSK3915393 160 mg (QD)1.00003.00001.5000
Part B: GSK3915393 20 mg (BID)0.66671.50001.5000
Part B: GSK3915393 80 mg (BID)1.00001.51671.5000

[back to top]

Part B: Tmax(10-24) Following Dose 160 mg (QD) of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: 10, 24 hours post-dose

InterventionHour (Median)
Day 1Day 14
Part B: GSK3915393 160 mg (QD)NANA

[back to top]

Part B: Tmax(10-24) Following Repeat Dose 20 mg BID and 80 mg BID of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: 10 hours, 10 hours 20 minutes, 10 hours 40 minutes, 12, 12.5 ,13, 14, 16, and 24 hours post-dose

,
InterventionHour (Median)
Day 1, n=10, 9Day 14, n=9, 9
Part B: GSK3915393 20 mg (BID)2.00002.0000
Part B: GSK3915393 80 mg (BID)2.00000.6667

[back to top]

Part C: Number of Participants With All Non-serious AEs and SAEs

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. SAE is defined as any serious adverse event that, at any dose which results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per investigator's medical or scientific judgment. (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
All non-serious AEsSAEs
Part C: GSK3915393 100 mcg IV50
Part C: GSK3915393 100 mcg+ITZ20
Part C: GSK3915393 20mg+GFJ20
Part C: GSK3915393 20mg+Water30
Part C: SK3915393 20 mg+ITZ20

[back to top]

Part C: Number of Participants With Worst Case Chemistry Results: Creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393

Blood samples were collected for analysis of creatinine. Participants were counted under increase of PCI if they had change from Baseline > 44.2 micromoles per Liter for any post Baseline assessment. Participants who did not meet this PCI criteria are counted as w/in range. Participants whose laboratory value became within range, were recorded in 'To within Range' category. (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
W/in RangeIncrease of PCI
Part C: GSK3915393 100 mcg IV120
Part C: GSK3915393 100 mcg+ITZ110
Part C: GSK3915393 20mg+GFJ120
Part C: GSK3915393 20mg+Water110
Part C: SK3915393 20 mg+ITZ100

[back to top]

Part C: Number of Participants With Worst Case Chemistry Results: Urea by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393

Blood samples were collected for analysis of chemistry parameters. PCI range for Urea: High >10.5 mmol/L. Participants were counted in worst case category that their value changes to ( within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
To W/in Range or No ChangeTo High
Part C: GSK3915393 100 mcg IV120
Part C: GSK3915393 100 mcg+ITZ110
Part C: GSK3915393 20mg+GFJ120
Part C: GSK3915393 20mg+Water110
Part C: SK3915393 20 mg+ITZ100

[back to top]

Part C: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393

"Blood samples were collected for analysis of hematology parameters. PCI ranges were 1*10^9 cell per liter (cells/L) (eosinophils), <0.2 or >0.54 proportion of red blood cells in blood (hematocrit), <80 or >180 grams per liter(g/L) (hemoglobin), <3 or >20 x10^9 cells/L (leukocytes), <0.8*10^9 cells/L (lymphocytes), <1.5 or >16*10^9 cells/L (neutrophils) and <100 or >550*10^9 cells/L (platelets). Participants were counted in worst case category that their value changes to (low, within range or no change or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (for example [e.g.], High to High), or whose value became within range, were recorded in To within Range or No Change category. Participants were counted twice if participant has values that changed 'To Low' & 'To High', so the percentages may not add to 100%." (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
Eosinophils: To LowEosinophils: To w/in Range or No changeEosinophils: To HighHematocrit: To LowHematocrit: To w/in Range or No changeHematocrit: To HighHemoglobin: To LowHemoglobin: To w/in Range or No changeHemoglobin: To HighLeukocytes: To LowLeukocytes: To w/in Range or No changeLeukocytes: To HighLymphocytes: To LowLymphocytes: To w/in Range or No changeLymphocytes: To HighNeutrophils: To LowNeutrophils: To w/in Range or No changeNeutrophils: To HighPlatelets: To LowPlatelets: To w/in Range or No changePlatelets: To High
Part C: GSK3915393 100 mcg IV0120012001200120012011100120
Part C: GSK3915393 100 mcg+ITZ0110011001100110011001100110
Part C: GSK3915393 20mg+GFJ0120012001200120012001200120
Part C: GSK3915393 20mg+Water0110011001100110011001100110
Part C: SK3915393 20 mg+ITZ0100010001000100010001000100

[back to top]

Part C: Number of Participants With Worst Case Post-Baseline Abnormal ECG Findings Following Administration of GSK3915393

Twelve lead ECG was obtained using an ECG machine that automatically calculated the heart rate and measured QTc, PR, QRS intervals. Abnormal findings were categorized as clinically significant and not clinically significant. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for number of participants with worst case post-Baseline abnormal ECG findings have been presented. (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
Abnormal: Not Clinically SignificantClinically Significant
Part C: GSK3915393 100 mcg IV20
Part C: GSK3915393 100 mcg+ITZ10
Part C: GSK3915393 20mg+GFJ10
Part C: GSK3915393 20mg+Water10
Part C: SK3915393 20 mg+ITZ00

[back to top]

Part C: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393

Vital signs included DBP, SBP, PR, body temperature, RR and were measured after resting for at least 5 minutes in semi-supine position. PCI ranges were, SBP (mmHg): <85 (low) or >160 (high), DBP (mmHg): <45 (low) or >100 (high), heart rate (beats per minute): <40 (low) or >110 (high), respiration rate (breaths per minute):<=8 (low) or >20 (high) and body temperature (degrees Celsius) <=35.5 (low) or >38.0 (high). Participants were counted in worst case category that their value changes to (low, within range or no change, or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To W/in Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100%. (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
SBP: To LowSBP: To w/in Range or No changeSBP: To HighDBP: To LowDBP: To w/in Range or No changeDBP: To HighPR: To LowPR: To w/in Range or No changePR: To HighTemperature: To LowTemperature: To w/in Range or No changeTemperature: To HighRR: To LowRR: To w/in Range or No changeRR: To High
Part C: GSK3915393 100 mcg IV01200120011101200111
Part C: GSK3915393 100 mcg+ITZ01100110011011000110
Part C: GSK3915393 20mg+GFJ01200120012011100120
Part C: GSK3915393 20mg+Water0110011001102900110
Part C: SK3915393 20 mg+ITZ01000100010001000100

[back to top]

Part B: AUCLST(0-10) Following Dosing of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: Pre-dose, 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, and 10 hours post-dose

,,
InterventionNanograms*hour per milliliter (Geometric Mean)
Day 1, n=10, 9, 9Day 14, n=9, 9, 9
Part B: GSK3915393 160 mg (QD)1268.95181670.9421
Part B: GSK3915393 20 mg (BID)90.7283173.2096
Part B: GSK3915393 80 mg (BID)570.8621873.9352

[back to top]

Part B: AUC(10-24) Following Repeat Dose of GSK3915393 160 mg (QD)

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: 10 and 24 hours post-dose

InterventionNanograms*hour per milliliter (Geometric Mean)
Day 1Day 14
Part B: GSK3915393 160 mg (QD)NANA

[back to top]

Part B: AUC(10-24) Following Repeat Dose 20 mg BID and 80 mg BID of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: 10 hours, 10 hours 20 minutes, 10 hours 40 minutes, 12, 12.5 ,13, 14, 16, and 24 hours post-dose

,
InterventionNanograms*hour per milliliter (Geometric Mean)
Day 1Day 14
Part B: GSK3915393 20 mg (BID)115.2199189.9773
Part B: GSK3915393 80 mg (BID)666.5290959.7659

[back to top]

Part A: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following IV Dose of GSK3915393

Vital signs included DBP, SBP, PR, body temperature, RR and were measured after resting for at least 5 minutes in semi-supine position. PCI ranges were, SBP (mmHg): <85 (low) or >160 (high), DBP (mmHg): <45 (low) or >100 (high), heart rate (beats per minute): <40 (low) or >110 (high), respiration rate (breaths per minute):<=8 (low) or >20 (high) and body temperature (degrees Celsius) <=35.5 (low) or >38.0 (high). Participants were counted in worst case category that their value changes to (low, within range or no change, or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To W/in Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100%. (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
SBP: To LowSBP: To w/in Range or No changeSBP: To HighDBP: To LowDBP: To w/in Range or No changeDBP: To HighPR: To LowPR: To w/in Range or No changePR: To HighBody temperature: To LowBody temperature: To w/in Range or No changeBody temperature: To HighRR: To LowRR: To w/in Range or No changeRR: To High
Part A: GSK3915393 100 mcg IV01200120012001200120

[back to top]

Part A: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose

Vital signs included diastolic blood pressure (DBP), systolic blood pressure (SBP), pulse rate (PR), body temperature, respiratory rate (RR) and were measured after resting for at least 5 minutes in semi-supine position. PCI ranges were, SBP (millimeters of mercury[mmHg]): <85 (low) or >160 (high), DBP (mmHg): <45 (low) or >100 (high), heart rate (beats per minute): <40 (low) or >110 (high), respiration rate (breaths per minute):<=8 (low) or >20 (high) and body temperature (degrees Celsius) <=35.5 (low) or >38.0 (high). Participants were counted in worst case category that their value changes to (low, within range or no change, or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To W/in Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100%. (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
SBP: To LowSBP: To w/in Range or No changeSBP: To HighDBP: To LowDBP: To w/in Range or No changeDBP: To HighPR: To LowPR: To w/in Range or No changePR: To HighBody temperature: To LowBody temperature: To w/in Range or No changeBody temperature: To HighRR: To LowRR: To w/in Range or No changeRR: To High
Part A: GSK3915393 15 mg090090090090090
Part A: GSK3915393 160 mg090090090090090
Part A: GSK3915393 60 mg090090090090090
Part A: Placebo090090090090090

[back to top]

Part A: Number of Participants With Worst Case Post-Baseline Abnormal Electrocardiogram (ECG) Findings Following Administration of Oral Dose

Twelve lead ECG was obtained using an ECG machine that automatically calculated the heart rate and measured QTc, PR, QRS intervals. Abnormal findings were categorized as clinically significant and not clinically significant. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for number of participants with worst case post-Baseline abnormal ECG findings have been presented. (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
Abnormal: Not Clinically SignificantClinically Significant
Part A: GSK3915393 15 mg30
Part A: GSK3915393 160 mg00
Part A: GSK3915393 60 mg10
Part A: Placebo20

[back to top]

Part A: Number of Participants With Worst Case Post-Baseline Abnormal ECG Findings Following Administration of IV Dose of GSK3915393

Twelve lead ECG was obtained using an ECG machine that automatically calculated the heart rate and measured QTc, PR, QRS intervals. Abnormal findings were categorized as clinically significant and not clinically significant. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for number of participants with worst case post-Baseline abnormal ECG findings have been presented. (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
Abnormal: Not Clinically SignificantClinically Significant
Part A: GSK3915393 100 mcg IV70

[back to top]

Part A: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose

"Blood samples were collected for analysis of hematology parameters. PCI ranges were >1*10^9 cell per liter (cells/L) (eosinophils), <0.2 or >0.54 proportion of red blood cells in blood (hematocrit), <80 or >180 grams per liter(g/L) (hemoglobin), <3 or >20 x10^9 cells/L (leukocytes), <0.8*10^9 cells/L (lymphocytes), <1.5 or >16*10^9 cells/L (neutrophils) and <100 or >550*10^9 cells/L (platelets). Participants were counted in worst case category that their value changes to (low, within range or no change or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (for example [e.g.], High to High), or whose value became within range, were recorded in To within Range or No Change category. Participants were counted twice if participant has values that changed 'To Low' & 'To High', so the percentages may not add to 100%." (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
Eosinophils: To LowEosinophils: To w/in Range or No changeEosinophils: To HighHematocrit: To LowHematocrit: To w/in Range or No changeHematocrit: To HighHemoglobin: To LowHemoglobin: To w/in Range or No changeHemoglobin: To HighLeukocytes: To LowLeukocytes: To w/in Range or No changeLeukocytes: To HighLymphocytes: To LowLymphocytes: To w/in Range or No changeLymphocytes: To HighNeutrophils: To LowNeutrophils: To w/in Range or No changeNeutrophils: To HighPlatelets: To LowPlatelets: To w/in Range or No changePlatelets: To High
Part A: GSK3915393 15 mg090090090090090090090
Part A: GSK3915393 160 mg090090090090090180090
Part A: GSK3915393 60 mg090090090090090090090
Part A: Placebo090090090090090090090

[back to top]

Part A: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of IV Dose of GSK3915393

"Blood samples were collected for analysis of hematology parameters. PCI ranges were >1*10^9 cell per liter (cells/L) (eosinophils), <0.2 or >0.54 proportion of red blood cells in blood (hematocrit), <80 or >180 grams per liter(g/L) (hemoglobin), <3 or >20 x10^9 cells/L (leukocytes), <0.8*10^9 cells/L (lymphocytes), <1.5 or >16*10^9 cells/L (neutrophils) and <100 or >550*10^9 cells/L (platelets). Participants were counted in worst case category that their value changes to (low, within range or no change or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (for example [e.g.], High to High), or whose value became within range, were recorded in To within Range or No Change category. Participants were counted twice if participant has values that changed 'To Low' & 'To High', so the percentages may not add to 100%." (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
Eosinophils: To LowEosinophils: To w/in Range or No changeEosinophils: To HighHematocrit: To LowHematocrit: To w/in Range or No changeHematocrit: To HighHemoglobin: To LowHemoglobin: To w/in Range or No changeHemoglobin: To HighLeukocytes: To LowLeukocytes: To w/in Range or No changeLeukocytes: To HighLymphocytes: To LowLymphocytes: To w/in Range or No changeLymphocytes: To HighNeutrophils: To LowNeutrophils: To w/in Range or No changeNeutrophils: To HighPlatelets: To LowPlatelets: To w/in Range or No changePlatelets: To High
Part A: GSK3915393 100 mcg IV0120012001200120012011100120

[back to top]

Part C: Number of Participants With Worst Case Chemistry Results by PCI Criteria Post-Baseline Relative to Baseline Following Dose Administration of GSK3915393

Blood samples were collected for analysis of chemistry parameters. PCI ranges were >=2*ULN (U/L)(ALT), >=2*ULN (U/L) (AST), >=2*ULN (ALP) (U/L), >=1.5*ULN (micromoles per liter) (bilirubin), <2 or >2.75 millimoles/liter (L) (mmol/L)(calcium), <3 or >11 mmol/L (glucose), <3 or >5.5 mmol/L (potassium), <130 or >150 mmol/L (sodium),<50 or >85 grams/liter (protein). Participants were counted in worst case category that their value changes to (low, within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100 percentage (%). (NCT04604795)
Timeframe: Up to 72 days

,,,,
InterventionParticipants (Count of Participants)
ALT: To LowALT: To w/in Range or No changeALT: To HighAST: To LowAST: To w/in Range or No changeAST: To HighALP: To LowALP: To w/in Range or No changeALP: To HighBilirubin: To LowBilirubin: To w/in Range or No changeBilirubin: To HighCalcium: To LowCalcium: To w/in Range or No changeCalcium: To HighGlucose: To LowGlucose: To w/in Range or No changeGlucose: To HighPotassium: To LowPotassium: To w/in Range or No changePotassium: To HighProtein: To LowProtein: To w/in Range or No changeProtein: To HighSodium: To LowSodium: To w/in Range or No changeSodium: To High
Part C: GSK3915393 100 mcg IV012001200120012001200120012001200120
Part C: GSK3915393 100 mcg+ITZ011001100110011001100110011001100110
Part C: GSK3915393 20mg+GFJ012001200120012011100120012001200120
Part C: GSK3915393 20mg+Water011001100110011001100110011001100110
Part C: SK3915393 20 mg+ITZ010001000100010001000100010001000100

[back to top]

Part A: Number of Participants With Worst Case Chemistry Results-urea by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose

Blood samples were collected for analysis of chemistry parameters. PCI range for Urea: High >10.5 mmol/L. Participants were counted in worst case category that their value changes to (within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
To w/in Range or No changeTo High
Part A: GSK3915393 15 mg90
Part A: GSK3915393 160 mg90
Part A: GSK3915393 60 mg90
Part A: Placebo90

[back to top]

Part A: Number of Participants With Worst Case Chemistry Results-urea by PCI Criteria Post-Baseline Relative to Baseline Following Administration of IV Dose of GSK3915393

Blood samples were collected for analysis of chemistry parameters. PCI range for Urea: High >10.5 mmol/L. Participants were counted in worst case category that their value changes to (within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
To w/in Range or No changeTo High
Part A: GSK3915393 100 mcg IV120

[back to top]

Part A: Number of Participants With Worst Case Chemistry Results-creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose

Blood samples were collected for analysis of creatinine. Participants were counted under increase of PCI if they had change from Baseline > 44.2 micromoles per Liter for any post Baseline assessment. Participants who did not meet this PCI criteria are counted as within (w/in) range. (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
W/in RangeIncrease of PCI
Part A: GSK3915393 15 mg90
Part A: GSK3915393 160 mg90
Part A: GSK3915393 60 mg90
Part A: Placebo90

[back to top]

Part A: Number of Participants With Worst Case Chemistry Results-creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Administration Administration of IV Dose of GSK3915393

Blood samples were collected for analysis of creatinine. Participants were counted under increase of PCI if they had change from Baseline >44.2 micromoles per Liter for any post Baseline assessment. Participants who did not meet this PCI criteria are counted as w/in range. (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
W/in RangeIncrease of PCI
Part A: GSK3915393 100 mcg IV120

[back to top]

Part A: Number of Participants With Worst Case Chemistry Results by Potential Clinical Importance (PCI) Criteria Post-Baseline Relative to Baseline Following Administration of Oral Dose

Blood samples were collected for analysis of chemistry parameters. PCI ranges were >=2*Upper limit of normal (ULN) units per liter (U/L)(Alanine Aminotransferase [ALT]), >=2*ULN (U/L) (Aspartate Aminotransferase ([AST]), >=2*ULN (Alkaline Phosphatase [ALP]) (U/L), >=1.5*ULN (micromoles per liter) (bilirubin), <2 or >2.75 millimoles/liter (L) (mmol/L)(calcium), <3 or >11 mmol/L (glucose), <3 or >5.5 mmol/L (potassium), <130 or >150 mmol/L (sodium),<50 or >85 grams/liter (protein). Participants were counted in worst case category that their value changes to (low, within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100 percentage (%). (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
ALT: To LowALT: To w/in Range or No changeALT: To HighAST: To LowAST: To w/in Range or No changeAST: To HighALP: To LowALP: To w/in Range or No changeALP: To HighBilirubin: To LowBilirubin: To w/in Range or No changeBilirubin: To HighCalcium: To LowCalcium: To w/in Range or No changeCalcium: To HighGlucose: To LowGlucose: To w/in Range or No changeGlucose: To HighPotassium: To LowPotassium: To w/in Range or No changePotassium: To HighProtein: To LowProtein: To w/in Range or No changeProtein: To HighSodium: To LowSodium: To w/in Range or No changeSodium: To High
Part A: GSK3915393 15 mg090090090090090090090090090
Part A: GSK3915393 160 mg090090090081090090090090090
Part A: GSK3915393 60 mg090090090090090090090090090
Part A: Placebo090090090090090090090090090

[back to top]

Part B: Cmax(10-24) Following Dose 160 mg (QD) of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: 10, 24 hours post-dose

InterventionNanograms per milliliter (Geometric Mean)
Day 1Day 14
Part B: GSK3915393 160 mg (QD)NANA

[back to top]

Part B: Cmax(10-24) Following Repeat Dose 20 mg and 80 mg of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: 10 hours, 10 hours 20 minutes, 10 hours 40 minutes, 12, 12.5 ,13, 14, 16, and 24 hours post-dose

,
InterventionNanograms per milliliter (Geometric Mean)
Day 1, n=10, 9Day 14, n=9, 9
Part B: GSK3915393 20 mg (BID)32.212762.0235
Part B: GSK3915393 80 mg (BID)338.2996931.2098

[back to top]

Part B: Number of Participants With All Non-serious AEs and SAEs

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. SAE is defined as any serious adverse event that, at any dose which results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per investigator's medical or scientific judgment. (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
All non-serious AEsSAEs
Part B: GSK3915393 160 mg (QD)50
Part B: GSK3915393 20 mg (BID)50
Part B: GSK3915393 80 mg (BID)10
Part B: Placebo30

[back to top]

Part B: Number of Participants With Worst Case Chemistry Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Repeat Oral Dose of GSK3915393

Blood samples were collected for analysis of chemistry parameters. PCI ranges were >=2*ULN (U/L)(ALT), >=2*ULN (U/L) (AST), >=2*ULN (ALP) (U/L), >=1.5*ULN (micromoles per liter) (bilirubin), <2 or >2.75 millimoles/liter (L) (mmol/L)(calcium), <3 or >11 mmol/L (glucose), <3 or >5.5 mmol/L (potassium), <130 or >150 mmol/L (sodium),<50 or >85 grams/liter (protein). Participants were counted in worst case category that their value changes to (low, within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100 percentage (%). (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
ALT: To LowALT: To w/in Range or No changeALT: To HighAST: To LowAST: To w/in Range or No changeAST: To HighALP: To LowALP: To w/in Range or No changeALP: To HighBilirubin: To LowBilirubin: To w/in Range or No changeBilirubin: To HighCalcium: To LowCalcium: To w/in Range or No changeCalcium: To HighGlucose: To LowGlucose: To w/in Range or No changeGlucose: To HighPotassium: To LowPotassium: To w/in Range or No changePotassium: To HighProtein: To LowProtein: To w/in Range or No changeProtein: To HighSodium: To LowSodium: To w/in Range or No changeSodium: To High
Part B: GSK3915393 160 mg (QD)090081090090090090090090090
Part B: GSK3915393 20 mg (BID)010001000100010001000100010001000100
Part B: GSK3915393 80 mg (BID)090090090090090090090090090
Part B: Placebo010001000100010001000100010001000100

[back to top]

Part B: Number of Participants With Worst Case Chemistry Results-creatinine by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Repeat Oral Dose

Blood samples were collected for analysis of creatinine. Participants were counted under increase of PCI if they had change from Baseline > 44.2 micromoles per Liter for any post Baseline assessment. Participants who did not meet this PCI criteria are counted as w/in range. Participants whose laboratory value became within range, were recorded in 'To within Range' category. (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
W/in RangeIncrease of PCI
Part B: GSK3915393 160 mg (QD)90
Part B: GSK3915393 20 mg (BID)100
Part B: GSK3915393 80 mg (BID)90
Part B: Placebo100

[back to top]

Part A: Number of Participants With Worst Case Chemistry Results by PCI Criteria Post-Baseline Relative to Baseline Following Administration Administration of IV Dose of GSK3915393

Blood samples were collected for analysis of chemistry parameters. PCI ranges were >=2*ULN (U/L)(ALT), >=2*ULN (U/L) (AST), >=2*ULN (ALP) (U/L), >=1.5*ULN (micromoles per liter) (bilirubin), <2 or >2.75 millimoles/liter (L) (mmol/L)(calcium), <3 or >11 mmol/L (glucose), <3 or >5.5 mmol/L (potassium), <130 or >150 mmol/L (sodium),<50 or >85 grams/liter (protein). Participants were counted in worst case category that their value changes to (low, within [w/in] range or no change [NC], or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100 percentage (%). (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
ALT: To LowALT: To w/in Range or No changeALT: To HighAST: To LowAST: To w/in Range or No changeAST: To HighALP: To LowALP: To w/in Range or No changeALP: To HighBilirubin: To LowBilirubin: To w/in Range or No changeBilirubin: To HighCalcium: To LowCalcium: To w/in Range or No changeCalcium: To HighGlucose: To LowGlucose: To w/in Range or No changeGlucose: To HighPotassium: To LowPotassium: To w/in Range or No changePotassium: To HighProtein: To LowProtein: To w/in Range or No changeProtein: To HighSodium: To LowSodium: To w/in Range or No changeSodium: To High
Part A: GSK3915393 100 mcg IV012001200120012001200120012001200120

[back to top]

Part A: Number of Participants With All Non-serious AEs and SAEs Following Administration Administration of IV Dose of GSK3915393

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. SAE is defined as any serious adverse event that, at any dose which results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per investigator's medical or scientific judgment. (NCT04604795)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
All non-serious AEsSAEs
Part A: GSK3915393 100 mcg IV40

[back to top]

Part B: AUCLST(0-10) Following First Dosing of GSK3915393 on Days 3, 5 and 7 (for Food-effect Assessment)

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 3, 5 and 7: Pre-dose, 20, 40 minutes, 1, 1.5 ,2, 3, 4, 6 and 10 hours post-dose

,,
InterventionNanogram*hour per milliliter (Geometric Mean)
Day 3, n=10, 9, 9Day 5, n= 10, 9, 9Day 7, n= 9, 9, 9
Part B: GSK3915393 160 mg (QD)1571.06371320.68471551.1980
Part B: GSK3915393 20 mg (BID)115.6796120.0480135.3659
Part B: GSK3915393 80 mg (BID)883.5828698.9908754.3745

[back to top]

Part B: Number of Participants With Worst Case Chemistry Results-urea by PCI Criteria Post-Baseline Relative to Baseline Following Administration of Repeat Oral Dose of GSK3915393

Blood samples were collected for analysis of chemistry parameters. PCI range for Urea: High >10.5 mmol/L. Participants were counted in worst case category that their value changes to (within [w/in] range or NC, or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To within Range No Change' category. (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
To W/in Range or No ChangeTo High
Part B: GSK3915393 160 mg (QD)90
Part B: GSK3915393 20 mg (BID)100
Part B: GSK3915393 80 mg (BID)90
Part B: Placebo100

[back to top]

Part B: Number of Participants With Worst Case Hematology Results by PCI Criteria Post-Baseline Relative to Baseline Following Repeat Oral Dose of GSK3915393

"Blood samples were collected for analysis of hematology parameters. PCI ranges were 1*10^9 cell per liter (cells/L) (eosinophils), <0.2 or >0.54 proportion of red blood cells in blood (hematocrit), <80 or >180 grams per liter(g/L) (hemoglobin), <3 or >20 x10^9 cells/L (leukocytes), <0.8*10^9 cells/L (lymphocytes), <1.5 or >16*10^9 cells/L (neutrophils) and <100 or >550*10^9 cells/L (platelets). Participants were counted in worst case category that their value changes to (low, within range or no change or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (for example [e.g.], High to High), or whose value became within range, were recorded in To within Range or No Change category. Participants were counted twice if participant has values that changed 'To Low' & 'To High', so the percentages may not add to 100%." (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
Eosinophils: To LowEosinophils: To w/in Range or No changeEosinophils: To HighHematocrit: To LowHematocrit: To w/in Range or No changeHematocrit: To HighHemoglobin: To LowHemoglobin: To w/in Range or No changeHemoglobin: To HighLeukocytes: To LowLeukocytes: To w/in Range or No changeLeukocytes: To HighLymphocytes: To LowLymphocytes: To w/in Range or No changeLymphocytes: To HighNeutrophils: To LowNeutrophils: To w/in Range or No changeNeutrophils: To HighPlatelets: To LowPlatelets: To w/in Range or No changePlatelets: To High
Part B: GSK3915393 160 mg (QD)090090090090090270090
Part B: GSK3915393 20 mg (BID)010001000100010001001900100
Part B: GSK3915393 80 mg (BID)090090090180090270090
Part B: Placebo0100010001000100010001000100

[back to top]

Part B: Number of Participants With Worst Case Post-Baseline Abnormal ECG Findings Following Repeat Oral Dose of GSK3915393

Twelve lead ECG was obtained using an ECG machine that automatically calculated the heart rate and measured QTc, PR, QRS intervals. Abnormal findings were categorized as clinically significant and not clinically significant. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for number of participants with worst case post-Baseline abnormal ECG findings have been presented. (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
Abnormal: Not Clinically SignificantClinically Significant
Part B: GSK3915393 160 mg (QD)10
Part B: GSK3915393 20 mg (BID)50
Part B: GSK3915393 80 mg (BID)01
Part B: Placebo31

[back to top]

Part B: Number of Participants With Worst Case Vital Sign Results by PCI Criteria Post-Baseline Relative to Baseline Following Repeat Oral Dose of GSK3915393

Vital signs included DBP, SBP, PR, body temperature, RR and were measured after resting for at least 5 minutes in semi-supine position. PCI ranges were, SBP (mmHg): <85 (low) or >160 (high), DBP (mmHg): <45 (low) or >100 (high), heart rate (beats per minute): <40 (low) or >110 (high), respiration rate (breaths per minute):<=8 (low) or >20 (high) and body temperature (degrees Celsius) <=35.5 (low) or >38.0 (high). Participants were counted in worst case category that their value changes to (low, within range or no change, or high), unless there is no change in their category. Participants whose laboratory value category was unchanged (e.g., High to High), or whose value became within range, are recorded in 'To W/in Range No Change' category. Participants were counted twice if participant had values that changed 'To Low' and 'To High', so percentages may not add to 100%. (NCT04604795)
Timeframe: Up to 28 days

,,,
InterventionParticipants (Count of Participants)
SBP: To LowSBP: To w/in Range or No changeSBP: To HighDBP: To LowDBP: To w/in Range or No changeDBP: To HighPR: To LowPR: To w/in Range or No changePR: To HighBody temperature: To LowBody temperature: To w/in Range or No changeBody temperature: To HighRR: To LowRR: To w/in Range or No changeRR: To High
Part B: GSK3915393 160 mg (QD)090090090090090
Part B: GSK3915393 20 mg (BID)010001001901900100
Part B: GSK3915393 80 mg (BID)090090090090090
Part B: Placebo010001000910100091

[back to top]

Part B: Cmax(0-10) Following First Dosing of GSK3915393 on Days 3, 5 and 7 (for Food-effect Assessment)

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 3, 5 and 7: Pre-dose, 20, 40 minutes, 1, 1.5, 2, 3, 4, 6 and 10 hours post-dose

,,
InterventionNanograms*hour per milliliter (Geometric Mean)
Day 3, n=10, 9, 9Day 5, n= 10, 9, 9Day 7, n= 9, 9, 9
Part B: GSK3915393 160 mg (QD)1324.4415550.0071805.5202
Part B: GSK3915393 20 mg (BID)125.529856.918777.0364
Part B: GSK3915393 80 mg (BID)819.8381235.7608355.0055

[back to top]

Part B: Cmax(0-10) Following Dosing of GSK3915393 on Days 1 and 14

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: Pre-dose, 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, and 10 hours post-dose

,,
InterventionNanograms per milliliter (Geometric Mean)
Day 1, n=10, 9, 9Day 14, n=9, 9, 9
Part B: GSK3915393 160 mg (QD)823.77041710.7385
Part B: GSK3915393 20 mg (BID)64.784395.4416
Part B: GSK3915393 80 mg (BID)408.5572820.5354

[back to top]

Part B: AUCLST(0-24) Following Repeat Dose 20 mg BID and 80 mg BID of GSK3915393

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: Pre-dose, 20 minutes, 40 minutes, 1, 1.5, 2, 3, 4, 6, 10, 10 hours 20 minutes, 10 hours 40 minutes, 12, 12.5 ,13, 14, 16, and 24 hours post-dose

,
InterventionNanograms*hour per milliliter (Geometric Mean)
Day 1, n=10, 9Day 14, n=9, 9
Part B: GSK3915393 20 mg (BID)193.1524342.1653
Part B: GSK3915393 80 mg (BID)1242.55001856.9207

[back to top]

Part B: AUCLST(0-24) Following Dose of GSK3915393 160 mg (QD)

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Days 1 and 14: Pre-dose, 20 minutes, 40 minutess, 1, 1.5, 2, 3 ,4, 6, 10 and 24 hours post-dose

InterventionNanograms*hour per milliliter (Geometric Mean)
Day 1Day 14
Part B: GSK3915393 160 mg (QD)1314.73991738.3433

[back to top]

Part A: Number of Participants With All Non-serious Adverse Events (AEs) and Serious AEs (SAEs) Following Administration of Oral Dose

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. SAE is defined as any serious adverse event that, at any dose which results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, other situations as per investigator's medical or scientific judgment. (NCT04604795)
Timeframe: Up to 70 days

,,,
InterventionParticipants (Count of Participants)
All non-serious AEsSAEs
Part A: GSK3915393 15 mg20
Part A: GSK3915393 160 mg10
Part A: GSK3915393 60 mg30
Part A: Placebo10

[back to top]

Part C: Tmax of GSK3915393 Following Oral Dose of GSK3915393 in Combination With Water, GFJ and ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. For Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, concentrations after 24 hours post-dose were expected to be non-quantifiable. Tmax was derived based on collected assessments (up to 24 hours for Part C: GSK3915393 20 mg+ Water and Part C: GSK3915393 20 mg+ GFJ, up to 60 hours for Part C: GSK3915393 20 mg+ ITZ). Only the quantifiable concentration time points were to be considered for assessment of pharmacokinetic parameters. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48 and 60 hours post-dose

InterventionHour (Median)
Part C: GSK3915393 20 mg+ Water0.67
Part C: GSK3915393 20 mg+ GFJ1.50
Part C: GSK3915393 20 mg+ ITZ1.25

[back to top]

Part C: Tmax of GSK3915393 Following IV Dose of GSK3915393+ITZ

Blood samples were collected at indicated time points for pharmacokinetic analysis of GSK3915393. (NCT04604795)
Timeframe: Pre-dose and at 20, 40 minutes, 1, 1 hour 5 minutes, 1 hour 10 minutes, 1 hours 20 minutes, 1 hour 40 minutes, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, and 60 hours post-dose

InterventionHour (Median)
Part C: GSK3915393 100 mcg IV+ITZ0.98

[back to top]

Apparent Clearance(CL/F) of PF-07321332

CL/F was apparent clearance. (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2.

InterventionL/hr (Geometric Mean)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted8.990
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted6.478

[back to top]

Apparent Volume of Distribution (Vz/F) of PF-07321332

Vz/F was apparent volume of distribution. (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2.

InterventionL (Geometric Mean)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted104.7
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted72.07

[back to top]

Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration(AUClast) of PF-07321332

AUClast of PF-07321332 was determined by Linear/Log trapezoidal method. (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2.

Interventionng*hr/mL (Geometric Mean)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted41840
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted74430

[back to top]

Area Under the Plasma Concentration-time Profile From Time Zero to Time Tau (τ), Where Tau=12-hour Dosing Interval(AUCtau) for PF-07321332

The AUCtau of PF-07321332 was determined by Linear/Log trapezoidal method. (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2.

Interventionng*hr/mL (Geometric Mean)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted33350
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted46290

[back to top]

Maximum Observed Concentration (Cmax) of PF-07321332

The Cmax of PF-07321332 in the study was observed directly from data. (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2.

Interventionng/mL (Geometric Mean)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted4678
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted5546

[back to top]

Terminal Half-life(t1/2) of PF-07321332

Terminal half-life was defined as the time measured for the plasma concentration of drug to decrease by one half. (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2

Interventionhours(hr) (Mean)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted8.255
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted7.793

[back to top]

Time for Cmax (Tmax) for PF-07321332

PF-07321332 Tmax was observed directed from data (NCT04962022)
Timeframe: Days 1, 2, 3 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours postdose on Day 3) in Period 1; Days 1, 4, 5, 6 (pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 48, and 72 hours postdose on Day 6) of Period 2

Interventionhours(hr) (Median)
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted1.020
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted1.700

[back to top]

Change From Baseline in Vital Signs Data - Supine Diastolic Blood Pressure

Vital signs(systolic and diastolic blood pressure, and pulse rate) were measured with participants after having a rest for at least 5 minutes in a supine position. Vital signs assessment were performed after collection of ECGs and prior to collection of blood draws if scheduled at the same time. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

InterventionmmHg (Mean)
Period 1/Day 3 0HPeriod 1/Day 3 1H 30min
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted-0.90.5

[back to top]

Change From Baseline in Vital Signs Data - Supine Diastolic Blood Pressure

Vital signs(systolic and diastolic blood pressure, and pulse rate) were measured with participants after having a rest for at least 5 minutes in a supine position. Vital signs assessment were performed after collection of ECGs and prior to collection of blood draws if scheduled at the same time. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

InterventionmmHg (Mean)
Period 2/Day 4 0HPeriod 2/Day 6 0HPeriod 2/Day 6 1HPeriod 2/Day 6 1H 30minPeriod 2/Day 6 72H
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted4.13.54.94.22.9

[back to top]

Change From Baseline in Vital Signs Data - Supine Pulse Rate

Vital signs(systolic and diastolic blood pressure, and pulse rate) were measured with participants after having a rest for at least 5 minutes in a supine position. Vital signs assessment were performed after collection of ECGs and prior to collection of blood draws if scheduled at the same time. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

Interventionbeats per minute(bpm) (Mean)
Period 2/Day 4 0 HPeriod 2/Day 6 0 HPeriod 2/Day 6 1 HPeriod 2/Day 6 1 H 30 minPeriod 2/Day 6 72 H
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted-2.4-2.5-0.8-2.10.3

[back to top]

Change From Baseline in Vital Signs Data - Supine Systolic Blood Pressure

Vital signs(systolic and diastolic blood pressure, and pulse rate) were measured with participants after having a rest for at least 5 minutes in a supine position. Vital signs assessment were performed after collection of ECGs and prior to collection of blood draws if scheduled at the same time. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

InterventionmmHg (Mean)
Period 1/Day 3 0 hour (H)Period 1/Day 3 1H 30min
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted1.41.5

[back to top]

Change From Baseline in Vital Signs Data - Supine Systolic Blood Pressure

Vital signs(systolic and diastolic blood pressure, and pulse rate) were measured with participants after having a rest for at least 5 minutes in a supine position. Vital signs assessment were performed after collection of ECGs and prior to collection of blood draws if scheduled at the same time. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

InterventionmmHg (Mean)
Period 2/Day 4 0HPeriod 2/Day6 0HPeriod 2/Day6 1HPeriod 2/Day6 1H 30minPeriod 2/Day6 72 H
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted2.63.65.55.36.4

[back to top]

Number of Participants With Clinically Significant 12-lead Electrocardiogram (ECG) Findings

Triplicate 12-lead ECG readings approximately 2 minutes apart were taken at each test. All ECG assessments were made after at least a 5-minute rest in a supine position and prior to any blood draws or vital sign measurements. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

,
InterventionParticipants (Count of Participants)
PR interval, Aggregate (msec) Value >= 300PR interval, Aggregate (msec) %Change >= 25/50%QRS Duration, Aggregate (msec) Value >= 140QRS Duration, Aggregate (msec) %Change >= 50%QTcF interval, Aggregate (msec) 450 < Value < = 480QTcF interval, Aggregate (msec) 480 < Value < = 500QTcF interval, Aggregate (msec) Value > 500QTcF interval, Aggregate (msec) 30 < Change < = 60QTcF interval, Aggregate (msec) Change > 60
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted000000000
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted000000000

[back to top]

Number of Participants With Laboratory Abnormalities (Without Regard to Baseline Abnormality)

Safety laboratory assessments included urinalysis, hematology, chemistry and other. All the safety laboratory samples were collected following at least a 4-hour fast. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

,
InterventionParticipants (Count of Participants)
Monocytes/Leukocytes(%)> 1.2 ✖ ULNBicarbonate(mEq/L) > 1.1 ✖ ULNFibrinogen(mg/dl) > 1.25 ✖ BaselineLeukocyte Esterase >= 1
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted2011
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted1600

[back to top]

Number of Participants With Treatment Emergent Adverse Events (TEAEs)

An Adverse event (AE) was any untoward medical occurrence in a participant. A serious AE was any untoward medical occurrence at any dose that resulted in death; was life-threatening; required hospitalization or prolongation of existing hospitalization; resulted in persistent or significant disability/incapacity; resulted in congenital anomaly/birth, was a suspected transmission via a Pfizer product of an infectious agent,pathogenic or non-pathogenic, was considered serious. The focus of AE summaries was on treatment-emergent AE (TEAE). An AE was considered TEAE if the event occurred during the on-treatment period. (NCT04962022)
Timeframe: Screening up to Day 35

,
InterventionParticipants (Count of Participants)
Participants with TEAEsParticipants with serious TEAEs
Itraconazole 200 mg QD + PF-07321332(Suspension)/Ritonavir 300/100 mg BID, Fasted100
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted70

[back to top]

Change From Baseline in Vital Signs Data - Supine Pulse Rate

Vital signs(systolic and diastolic blood pressure, and pulse rate) were measured with participants after having a rest for at least 5 minutes in a supine position. Vital signs assessment were performed after collection of ECGs and prior to collection of blood draws if scheduled at the same time. (NCT04962022)
Timeframe: Screening up to Day 9 of Period 2 or Early termination/discontinuation.

Interventionbeats per minute(bpm) (Mean)
Period 1/Day 3 0 HPeriod 1/Day 3 1 H 30 min
PF-07321332 (Suspension)/Ritonavir 300/100 mg BID, Fasted 0/1-0.5-3.1

[back to top]

Part 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Soticlestat When Administered Alone and With Itraconazole

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with itraconazole: Period 2, Day 5 pre-dose and at multiple timepoints (up to 168 hours) post-dose

Interventionnanogram*hours per milliliter(ng*hr/mL) (Geometric Mean)
Part 1: Soticlestat 300 mg Alone1483
Part 1: Soticlestat 300 mg + Itraconazole 200 mg1914

[back to top]

Parts 1 and 2: Number of Participants With Clinically Significant Abnormal Values for Electrocardiogram (ECG)

(NCT05064449)
Timeframe: Part 1: Day 1 of Period 1 up to Day 12 of Period 2; Part 2: Day 1 of Period 1 up to Day 8 of Period 2

InterventionParticipants (Count of Participants)
Part 1: Soticlestat 300 mg Alone0
Part 1: Itraconazole 200 mg Alone0
Part 1: Soticlestat 300 mg + Itraconazole 200 mg0
Part 2: Soticlestat 300 mg Alone0
Part 2: Mefenamic Acid 500 mg and 250 mg0
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg0

[back to top]

Parts 1 and 2: Number of Participants With Clinically Significant Abnormal Values for Laboratory Evaluations

(NCT05064449)
Timeframe: Part 1: Day 1 of Period 1 up to Day 12 of Period 2; Part 2: Day 1 of Period 1 up to Day 8 of Period 2

InterventionParticipants (Count of Participants)
Part 1: Soticlestat 300 mg Alone0
Part 1: Itraconazole 200 mg Alone0
Part 1: Soticlestat 300 mg + Itraconazole 200 mg0
Part 2: Soticlestat 300 mg Alone0
Part 2: Mefenamic Acid 500 mg and 250 mg0
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg0

[back to top]

Parts 1 and 2: Number of Participants With Clinically Significant Abnormal Values for Vital Signs

(NCT05064449)
Timeframe: Part 1: Day 1 of Period 1 up to Day 12 of Period 2; Part 2: Day 1 of Period 1 up to Day 8 of Period 2

InterventionParticipants (Count of Participants)
Part 1: Soticlestat 300 mg Alone0
Part 1: Itraconazole 200 mg Alone0
Part 1: Soticlestat 300 mg + Itraconazole 200 mg0
Part 2: Soticlestat 300 mg Alone0
Part 2: Mefenamic Acid 500 mg and 250 mg0
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg0

[back to top]

Parts 1 and 2: Number of Participants With Suicidal Ideation or Suicidal Behavior as Measured Using Columbia-Suicide Severity Rating Scale (C-SSRS)

"The C-SSRS is an interview-based rating scale to systematically assess any suicidality, suicidal behavior, or suicidal ideation. Any suicidality is emergence of any suicidal ideation or suicidal behavior. Any suicidal behavior was indicated when response was yes for any these questions- actual attempted to suicide, engaged in non-suicidal self-injurious behavior, interrupted attempt, aborted attempt, preparatory acts. Any suicidal ideation was indicated when response was yes for any of these questions- wish to be dead, non-specific active suicidal thoughts, active suicidal ideation with methods without intent to act or some intended to act, without specific plan or with specific plan and intended to suicide." (NCT05064449)
Timeframe: Part 1: Day 1 of Period 1 up to Day 12 of Period 2; Part 2: Day 1 of Period 1 up to Day 8 of Period 2

InterventionParticipants (Count of Participants)
Part 1: Soticlestat 300 mg Alone0
Part 1: Itraconazole 200 mg Alone0
Part 1: Soticlestat 300 mg + Itraconazole 200 mg0
Part 2: Soticlestat 300 mg Alone0
Part 2: Mefenamic Acid 500 mg and 250 mg0
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg0

[back to top]

Part 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Soticlestat When Administered Alone and With Itraconazole

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with itraconazole: Period 2, Day 5 pre-dose and at multiple timepoints (up to 168 hours) post-dose

Interventionng*hr/mL (Geometric Mean)
Part 1: Soticlestat 300 mg Alone1391
Part 1: Soticlestat 300 mg + Itraconazole 200 mg1697

[back to top]

Part 1, Cmax: Maximum Observed Plasma Concentration for Soticlestat When Administered Alone and With Itraconazole

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with itraconazole: Period 2, Day 5 pre-dose and at multiple timepoints (up to 168 hours) post-dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Part 1: Soticlestat 300 mg Alone1310
Part 1: Soticlestat 300 mg + Itraconazole 200 mg1527

[back to top]

Part 1, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Soticlestat When Administered Alone and With Itraconazole

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with itraconazole: Period 2, Day 5 pre-dose and at multiple timepoints (up to 168 hours) post-dose

Interventionhour (Median)
Part 1: Soticlestat 300 mg Alone0.500
Part 1: Soticlestat 300 mg + Itraconazole 200 mg0.503

[back to top]

Part 2, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Soticlestat When Administered Alone and With Mefenamic Acid

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with mefenamic acid: Period 2, Day 2 pre-dose and at multiple timepoints (up to 144 hours) post-dose

Interventionng*hr/mL (Geometric Mean)
Part 2: Soticlestat 300 mg Alone1533
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg1594

[back to top]

Part 2, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Soticlestat When Administered Alone and With Mefenamic Acid

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with mefenamic acid: Period 2, Day 2 pre-dose and at multiple timepoints (up to 144 hours) post-dose

Interventionng*hr/mL (Geometric Mean)
Part 2: Soticlestat 300 mg Alone1423
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg1528

[back to top]

Part 2, Cmax: Maximum Observed Plasma Concentration for Soticlestat When Administered Alone and With Mefenamic Acid

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with mefenamic acid: Period 2, Day 2 pre-dose and at multiple timepoints (up to 144 hours) post-dose

Interventionng/mL (Geometric Mean)
Part 2: Soticlestat 300 mg Alone1414
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg1517

[back to top]

Part 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Soticlestat When Administered Alone and With Mefenamic Acid

(NCT05064449)
Timeframe: Soticlestat alone: Period 1, Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose; Soticlestat with mefenamic acid: Period 2, Day 2 pre-dose and at multiple timepoints (up to 144 hours) post-dose

Interventionhour (Median)
Part 2: Soticlestat 300 mg Alone0.505
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg0.522

[back to top]

Parts 1 and 2: Number of Participants Reported One or More Treatment-emergent Adverse Event (TEAE)

(NCT05064449)
Timeframe: Part 1: from Day 1 of Period 1 up to 15 days after the last dose of soticlestat in Period 2 (up to Day 20 in Period 2); Part 2: from Day 1 of Period 1 up to 15 days after the last dose of soticlestat in Period 2 (up to Day 17 in Period 2)

InterventionParticipants (Count of Participants)
Part 1: Soticlestat 300 mg Alone1
Part 1: Itraconazole 200 mg Alone2
Part 1: Soticlestat 300 mg + Itraconazole 200 mg3
Part 2: Soticlestat 300 mg Alone1
Part 2: Mefenamic Acid 500 mg and 250 mg0
Part 2: Soticlestat 300 mg + Mefenamic Acid 500 mg and 250 mg3

[back to top]