Page last updated: 2024-10-15

rifabutin

Cross-References

ID SourceID
PubMed CID135398743
SCHEMBL ID36043
MeSH IDM0026934
PubMed CID135415564
CHEMBL ID444633
CHEMBL ID287414
CHEBI ID45367
MeSH IDM0026934

Synonyms (72)

Synonym
brn 3584778
hsdb 3577
rifamycin xiv, 1',4-didehydro-1-deoxy-1,4-dihydro-5'-(2-methylpropyl)-1-oxo-
rifamycin xiv, 1,4-dihydro-1-deoxy-1',4-didehydro-5'-(2-methylpropyl)-1-oxo-
(9s,12e,14s,15r,16s,17r,18r,19r,20s,21s,22e,24z)-6-16,18,20-tetrahydroxy-1'-isobutyl-14-methoxy-7,9,15,17,19,21,25-heptamethylspiro(9,4-(epoxypentadeca(1,11,13)trienimino)-2h-furo(2',3':7,8)naphth(1,2-d)imidazole-2,4'-piperidine)-5,10,26(3h,9h)-trione,16-
drg-0085
AB01274733-01
ansatipin
PRESTWICK2_001109
MLS001061256
smr001227203
lm427
assatipin
(trihydroxy-1'-isobutyl-methoxy-heptamethyl-trioxo-spiro[[?]-4,4'-piperidine]yl) acetate
rifabutine
alfacid
mycobutin
ansatipine
spiro[9,4-(epoxypentadeca[1,11,13]trienimino)-2h-furo[2',3':7,8]naphth[1,2-d]imidazole-2,4'-piperidine]-5,10,26(3h,9h)-trione, 16-(acetyloxy)-6,18,20-trihydroxy-14-methoxy-7,9,15,17,19,21,25-heptamethyl-1'-(2-methylpropyl)-, (9s,12e,14s,15r,16s,17r,18r,19
C07235
1,4-dihydro-1-deoxy-1',4-didehydro-5'-(2-methylpropyl)-1-oxorifamycin xiv
4-n-isobutylspiropiperidylrifamycin s
4-deoxo-3,4-(2-spiro(n-isobutyl-4-piperidyl)-2,5-dihydro-1h-imidazo)-rifamycin s
ansamicin
DB00615
(9s,12e,14s,15r,16s,17r,18r,19r,20s,21s,22e,24z)-6,18,20-trihydroxy-1'-isobutyl-14-methoxy-7,9,15,17,19,21,25-heptamethyl-5,10,26-trioxo-3,5,9,10-tetrahydrospiro[9,4-(epoxypentadeca[1,11,13]trienoimino)furo[2',3':7,8]naphtho[1,2-d]imidazole-2,4'-piperidin
HMS1571M20
NCGC00090762-02
HMS3259D12
rifabutin [usan:usp:inn:ban:jan]
unii-1w306tda6s
rifabutina
rifabutinum
CCG-221109
AB01209745-01
SCHEMBL36043
AB01274733_02
mfcd00866816
HMS3715M20
Q1135705
PD002887
AC-19109
CHEBI:45367 ,
D00424
rifabutin (jan/usp/inn)
CHEMBL444633
1',4-didehydro-1-deoxy-1,4-dihydro-5'-(2-methylpropyl)-1-oxorifamycin xiv
dtxsid0033960 ,
AKOS015963033
rifabutin [hsdb]
rifabutin [mart.]
rifabutin [who-dd]
rifabutin [usp-rs]
rifabutin [mi]
rifabutin [ep monograph]
4-deoxo-3,4-(2-spiro-(n-isobutyl-4-piperidyl))-(1h)-imidazo-(2,5-dihydro)rifamycin s
rifabutin [usan]
rifabutin [usp monograph]
rifabutin [vandf]
rifabutin [inn]
rifabutin component of talicia
rifabutin [orange book]
talicia component rifabutin
rifabutin [jan]
1,4-dihydro-1-deoxy-1?,4-didehydro-5?-(2-methylpropyl)-1-oxo-rifamycinxi;1,4-dihydro-1-deoxy-1?,4-didehydro-5?-(2-methylpropyl)-1-oxorifamycinxiv;
NC00720
bdbm50237607
[(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,32-tetrahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-1'-(2-methylpropyl)-6,23-dioxospiro[8,33-dioxa-24,27,29-triazapentacyclo[23.6.1.14,7.05,31.026,30]tritriaconta-1(32),2,4,9,19,21,24,26,30-no
(9s,12e,14s,15r,16s,17r,18r,19r,20s,21s,22e,24z)-6,18,20-trihydroxy-14-methoxy-7,9,15,17,19,21,25-heptamethyl-1'-(2-methylpropyl)-5,10,26-trioxo-3,5,9,10-tetrahydrospiro[9,4-(epoxypentadeca[1,11,13]trienoimino)furo[2',3':7,8]naphtho[1,2-d]imidazole-2,4'-p
CHEMBL287414
gtpl12015
R0211

Toxicity

ExcerptReference
"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
)
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
" Since the therapeutic and toxic effects of this class of drugs are strongly influenced by their lipid affinity, we concerned specifically on the ability of this antibiotic to affect the membrane biophysical properties."( Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
Arêde, M; Caio, JM; Lúcio, M; Moiteiro, C; Nunes, C; Pinheiro, M; Reis, S, 2013
)

Pharmacokinetics

ExcerptReference
" A randomized, open-label, two-period, two-sequence, balanced, crossover drug interaction study was conducted with 22 healthy adult subjects to compare steady-state plasma RFB pharmacokinetic parameters during concomitant administration of FPV-RTV (700/100 mg twice a day [BID]) with a 75%-reduced RFB dose (150 mg every other day [QOD]) to the standard RFB regimen (300 mg once per day [QD]) by geometric least-squares mean ratios."( Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
Borland, J; Chen, YC; Ford, SL; Lou, Y; Min, SS; Shelton, MJ; Yuen, GJ, 2008
)
" 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
)

Bioavailability

ExcerptReference
"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
)
"Macrocycles are ideal in efforts to tackle "difficult" targets, but our understanding of what makes them cell permeable and orally bioavailable is limited."( Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?
Giordanetto, F; Kihlberg, J, 2014
)
" Its bioavailability at an oral dose of 2 mg/kg was 15%."( Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
Beuerman, RW; Cao, D; Corkran, HM; Dick, T; Koh, JJ; Lakshminarayanan, R; Lim, F; Lin, S; Liu, S; Mukherjee, D; Stocker, BL; Tan, DTH; Tan, DZ; Tan, JK; Timmer, MSM; Zou, H, 2016
)

Dosage Studied

ExcerptReference
" aureus septicemia model following administration by either oral or parenteral dosing routes."( Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
Chapo, K; Combrink, KD; Ding, CZ; Kim, IH; Ma, Z; Morris, TW; Pulse, M; Renick, P; Simecka, JW; Yan, D, 2007
)
" Increased systemic exposure to RFB and its equipotent active metabolite, 25-O-desacetyl-RFB (dAc-RFB), has been reported during concomitant administration of CYP3A4 inhibitors, including ritonavir (RTV), lopinavir, and amprenavir (APV); therefore, a reduction in the RFB dosage is recommended when it is coadministered with these protease inhibitors."( Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
Borland, J; Chen, YC; Ford, SL; Lou, Y; Min, SS; Shelton, MJ; Yuen, GJ, 2008
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (45)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency56.23410.004023.8416100.0000AID485290
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
LuciferasePhotinus pyralis (common eastern firefly)Potency25.57480.007215.758889.3584AID624030
interleukin 8Homo sapiens (human)Potency66.82420.047349.480674.9780AID651758
15-lipoxygenase, partialHomo sapiens (human)Potency39.81070.012610.691788.5700AID887
USP1 protein, partialHomo sapiens (human)Potency43.92850.031637.5844354.8130AID504865; AID743255
GLS proteinHomo sapiens (human)Potency28.18380.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency19.47630.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency44.66840.000221.22318,912.5098AID588516
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency10.00000.001318.074339.8107AID926; AID938
farnesoid X nuclear receptorHomo sapiens (human)Potency39.81070.375827.485161.6524AID588527
pregnane X nuclear receptorHomo sapiens (human)Potency0.79430.005428.02631,258.9301AID720659
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency27.71700.001024.504861.6448AID588534; AID588535
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency28.62880.001019.414170.9645AID588536; AID588537
IDH1Homo sapiens (human)Potency7.30780.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.81070.354828.065989.1251AID504847
flap endonuclease 1Homo sapiens (human)Potency39.81070.133725.412989.1251AID588795
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency32.19680.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency25.11890.020010.786931.6228AID912
lamin isoform A-delta10Homo sapiens (human)Potency31.62280.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
[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)15.90000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)26.70000.11007.190310.0000AID1443980; AID1443989; AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)49.80002.41006.343310.0000AID1473739
[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)
twin arginine protein translocation system - TatA proteinEscherichia coli str. K-12 substr. MG1655AC5015.88600.707010.915145.8560AID504941
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
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 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (307)

Assay IDTitleYearJournalArticle
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID298731Antibacterial activity against intermediate rifamycin-resistant Staphylococcus aureus CB372 with rpoB Asp471Tyr mutation2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
AID424418Toxicity in human assessed as insomnia at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1473853AUC in human at 300 to 900 mg, po QD 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.
AID1653528Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in armadillo assessed as bacterial counts in footpad at 6 mg/kg administered with food daily for 8 weeks (Rvb = 162%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1879505Antibacterial activity against metronidazole-resistant Helicobacter pylori CB1573 harboring rdxAR16S mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID285161Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID571672Cmax in 10'6 mouse alveolar macrophages at 4 to 5 mg/kg administered as inhalable dose measured 6 hrs postinhalation by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID424382Toxicity in human assessed as gastrointestinal disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID571682Clearance in BALB/c mouse at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
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.
AID298730Antibacterial activity against rifamycin-sensitive Staphylococcus aureus CB1902007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
AID571675Plasma concentration in BALB/c mouse at 4 to 5 mg/kg administered as inhalable bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID424362Cmax in human at 150 mg, po QOD co-treated with 700 mg, po fosamprenavir BID and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653515Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.1 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID424375Toxicity in human assessed as headache at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID634275Antimycobacterial activity against Mycobacterium tuberculosis isolate 307 expressing rpoB Ser531Leu mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
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).
AID424388Toxicity in human assessed as decrease in neutrophile count at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID348174Antimycobacterial activity against Mycobacterium avium 1581 at 0.2 mg/mL after 15 days relative to control2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID424404Toxicity in human assessed as myalgia at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID634271Antimycobacterial activity against Mycobacterium tuberculosis isolate MA03 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID424380Toxicity in human assessed as pollakiurea at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1443989Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to 2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID424394Toxicity in human assessed as general disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424409Toxicity in human assessed as rash generalized at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID298734Antibacterial activity against Staphylococcus aureus ATCC 6538 induced-septicemia in sc dosed mouse2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
AID1065394Oral bioavailability in human2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?
AID424355AUC (0 to 48 hrs) in human at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID436367Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days by serial dilution technique2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines.
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.
AID424405Toxicity in human assessed as myalgia at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424389Toxicity in human assessed as decrease in neutrophile count at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1473854Drug concentration at steady state in human at 300 to 900 mg, po QD 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.
AID634284Antimycobacterial activity against Mycobacterium tuberculosis isolate 364 expressing rpoB Ser522Leu mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID722443Drug localization in DPH-PA probe-labeled DMPC liposomes at 37 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
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.
AID1879508Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1902 harboring rpoBV149F mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1653542Plasma concentration in rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse at 6 mg/kg administered with food daily for 16 weeks by high-pressure liquid chromatography analysis2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID722436Binding affinity to DPH probe-labeled DMPC liposomes assessed as binding constant by fluorescence quenching assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
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).
AID1653538Plasma concentration in rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse at 6 mg/kg administered with food daily for 2 weeks by high-pressure liquid chromatography analysis2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID722439Drug localization in DPH probe-labeled DMPC liposomes at 42 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
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.
AID534422Antibacterial activity against Mycobacterium bovis BCG-japan2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID722434Binding affinity to DPH-PA probe-labeled DMPC liposomes assessed as binding constant by fluorescence quenching assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID1653525Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in armadillo assessed as bacterial counts in footpad at 6 mg/kg administered with food daily for 1 week (Rvb = 110%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
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).
AID30135Volume of distribution of the compound2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Property-based design: optimization of drug absorption and pharmacokinetics.
AID348173Antimycobacterial activity against Mycobacterium avium 1581 at 0.1 mg/mL after 15 days relative to control2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID424359Cmax in human at 150 mg, po QD po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID424386Toxicity in human assessed as nausea at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653530Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in armadillo assessed as bacterial counts in footpad at 6 mg/kg administered with food daily for 16 weeks (Rvb = 226%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID722444Partition co-efficient, Log D of the compound in DMPC liposomes at pH 7.4 by spectrophotometry2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID424407Toxicity in human assessed as skin and subcutaneous tissue disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
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).
AID424370Average plasma concentration in human assessed as dAc-RFB level at 150 mg, po QD po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID1884635Cmax in CD-1 mouse at 5 mg/kg, iv measured at 5 to 24 hrs by LC-MS/MS analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID1653516Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653534Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse assessed as ATP level per 10'6 Mycobacterium leprae in footpad at 6 mg/kg administered with food daily for 8 weeks by Shepard's kinetic method (Rvb = 26.1 +/2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID722441Drug localization in DPH-PA probe-labeled DMPG liposomes at 37 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID276753Antimycobacterial activity against streptomycin resistant Mycobacterium tuberculosis ATCC 358202006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID634280Antimycobacterial activity against Mycobacterium tuberculosis isolate 344 expressing rpoB Ser522Leu mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1879496Antibacterial activity against Clostridioides difficile ATCC 96892022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID348176Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by resazurin method2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
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).
AID1653523Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.3 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID424356Cmax in human at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653509Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.1 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1653390Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID571670Elimination rate constant in human THP1 cells at 3 ug/ml after 10 mins by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID424372Toxicity in human assessed as nervous system disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID634273Antimycobacterial activity against Mycobacterium tuberculosis isolate 359 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
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]
AID634349Antimycobacterial activity against Mycobacterium tuberculosis isolate 80,014 expressing rpoB Arg529Lys and Leu530Met mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
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
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
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).
AID424385Toxicity in human assessed as diarrhea disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653535Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse assessed as ATP level per 10'6 Mycobacterium leprae in footpad at 6 mg/kg administered with food daily for 12 weeks by Shepard's kinetic method (Rvb = 26.9 +2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID424403Toxicity in human assessed as musculoskeletal and connective tissue disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID571683Clearance in BALB/c mouse at 4 to 5 mg/kg administered as inhalable bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
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).
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID424368AUC (0 to 48 hrs) in human assessed as dAc-RFB level at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID634282Antimycobacterial activity against Mycobacterium tuberculosis isolate 352 expressing rpoB Asp516Leu and Phe514Phe double mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID285162Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID424383Toxicity in human assessed as gastrointestinal disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653539Plasma concentration in rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse at 6 mg/kg administered with food daily for 4 weeks by high-pressure liquid chromatography analysis2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID722427Partition co-efficient, Log D of the compound in DMPG liposomes at pH 7.4 by spectrophotometry2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID348177Antimycobacterial activity against isoniazid, rifampicin and streptomycin-resistant Mycobacterium tuberculosis after 7 days by resazurin method2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID722435Drug localization in DPH-PA probe-labeled DMPG liposomes at 42 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID571668Cmax in 10'6 human THP1 cells at 3 ug/ml after 10 mins by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID1879519Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1771 harboring rpoBL525I/D530N/rdxAE75stop mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID424361AUC (0 to tau) in human at 150 mg, po QOD co-treated with 700 mg, po fosamprenavir BID and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID436369Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 30 days by serial dilution technique2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines.
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.
AID1884624Antibacterial activity against Staphylococcus aureus assessed as reduction in bacterial growth in CAMHB preincubated 6 hrs followed by human serum addition and measured after 20 hrs by microdilution assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID1653537Plasma concentration in rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse at 6 mg/kg administered with food daily for 1 week by high-pressure liquid chromatography analysis2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1879521Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1771 harboring rpoBL525I/D530N/rdxAE75stop mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution meth2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
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.
AID276754Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis ATCC 358372006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
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.
AID571673Cmax in 10'6 mouse alveolar macrophages at 4 to 5 mg/kg, iv measured after 4 hrs by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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).
AID1884628Antibacterial activity against Staphylococcus aureus assessed assessed as reduction in bacterial growth in CAMHB in absence of human serum measured after 20 hrs by microdilution assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID276757Antimycobacterial activity against rifampicin and rifabutin resistant Mycobacterium tuberculosis2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID722433Binding affinity to DPH probe-labeled DMPG liposomes assessed as binding constant by fluorescence quenching assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID27900Plasma clearance of the compound2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Property-based design: optimization of drug absorption and pharmacokinetics.
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.
AID348182Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for non-replicating Mycobacterium tuberculosis2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID424397Toxicity in human assessed as fatigue at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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).
AID424412Toxicity in human assessed as neutropenia at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID276756Antimycobacterial activity against Mycobacterium tuberculosis H37 Rv ATCC 272942006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID424406Toxicity in human assessed as skin and subcutaneous tissue disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653522Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID276758Antimycobacterial activity against rifampicin and rifabutin sensitive Mycobacterium tuberculosis2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
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]
AID571680Volume of distribution in BALB/c mouse at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID534424Antibacterial activity against Mycobacterium bovis BCG-Pasteur2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
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).
AID634277Antimycobacterial activity against Mycobacterium tuberculosis isolate 349 expressing rpoB mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID424360Average plasma concentration in human at 150 mg, po QD po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1879525Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1893 harboring rpoBL525I/D530N/rdxAR16S mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1879517Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1614 harboring rpoBL525I/D530N at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID1653419Inhibition of PGL1 synthesis in Mycobacterium leprae infected Swiss Webster mouse macrophages assessed as decrease in [U-14C]PA incorporation at 0.2 uM preincubated for 4 days post infection followed by [U-14C]PA addition and measured after 7 days by liqu2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy 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.
AID1879510Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1902 harboring rpoBV149F mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1653540Plasma concentration in rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse at 6 mg/kg administered with food daily for 8 weeks by high-pressure liquid chromatography analysis2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID722440Drug localization in DPH probe-labeled DMPG liposomes at 37 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID424408Toxicity in human assessed as rash generalized at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID634279Antimycobacterial activity against Mycobacterium tuberculosis isolate 309 expressing rpoB His526Arg mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1879523Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1893 harboring rpoBL525I/D530N/rdxAR16S mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID722438Drug localization in DPH probe-labeled DMPG liposomes at 42 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID424400Toxicity in human assessed as pain at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424373Toxicity in human assessed as nervous system disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424402Toxicity in human assessed as musculoskeletal and connective tissue disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1473855Ratio of drug concentration at steady state in human at 300 to 900 mg, po QD 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.
AID276760Antimycobacterial activity against Mycobacterium kansasii measured as susceptibility at 1 ug/mL2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
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]
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.
AID424366Average plasma concentration in human assessed as dAc-RFB level at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID722430Binding affinity to DPH-PA probe-labeled DMPC liposomes assessed as main phase transition temperature at 30 uM by steady-state fluorescence anisotrope (Rvb = 24.6 +/- 0.3 degC)2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID1653533Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse assessed as ATP level in footpad at 6 mg/kg administered with food daily for 4 weeks by Shepard's kinetic method (Rvb = 98%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
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.
AID424416Toxicity in human assessed as psychiatric disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID722442Drug localization in DPH probe-labeled DMPC liposomes at 37 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID424364AUC (0 to 48 hrs) in human assessed as dAc-RFB level at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID571674Plasma concentration in BALB/c mouse at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID436368Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by serial dilution technique2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines.
AID534419Antibacterial activity against Mycobacterium bovis BCG-Connaught2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID298733Antibacterial activity against Staphylococcus aureus ATCC 6538 induced-septicemia in po dosed mouse2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
AID1879515Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1614 harboring rpoBL525I/D530N mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID424401Toxicity in human assessed as pain at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID348179Antimycobacterial activity against non-replicating Mycobacterium tuberculosis assessed as luciferase activity incubated for 8 days measured after 24 hrs of incubation by low oxygen recover assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID1653536Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse assessed as ATP level per 10'6 Mycobacterium leprae in footpad at 6 mg/kg administered with food daily for 16 weeks by Shepard's kinetic method (Rvb = 27.9 +2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID276755Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis ATCC 358222006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1879503Antibacterial activity against metronidazole-resistant Helicobacter pylori CB1573 harboring rdxAR16S mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID424393Toxicity in human assessed as increase in neutrophile count at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424379Toxicity in human assessed as chromaturia at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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).
AID424369Cmax in human assessed as dAc-RFB level at 150 mg, po QD po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID534421Antibacterial activity against Mycobacterium bovis BCG-Denmark2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID571681Volume of distribution in BALB/c mouse at 4 to 5 mg/kg administered as inhalable bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1884627Antibacterial activity against Acinetobacter baumannii HUMC1 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
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).
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.
AID424374Toxicity in human assessed as headache at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653529Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in armadillo assessed as bacterial counts in footpad at 6 mg/kg administered with food daily for 12 weeks (Rvb = 190%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1333267Oral bioavailability in Sprague-Dawley rat2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID424381Toxicity in human assessed as pollakiurea at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424392Toxicity in human assessed as increase in neutrophile count at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424399Toxicity in human assessed as chills at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653526Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in armadillo assessed as bacterial counts in footpad at 6 mg/kg administered with food daily for 2 weeks (Rvb = 125%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653527Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in armadillo assessed as bacterial counts in footpad at 6 mg/kg administered with food daily for 4 weeks (Rvb = 141%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID424414Toxicity in human assessed as thrombocytopenia at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653392Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.3 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
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.
AID1653511Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.3 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID424395Toxicity in human assessed as general disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1653396Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.1 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653510Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1162166Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID276759Antimycobacterial activity against Mycobacterium avium-intracellulare complex measured as susceptibility at 1 ug/mL2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID634274Antimycobacterial activity against Mycobacterium tuberculosis isolate 361 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID722432Binding affinity to DPH-PA probe-labeled DMPG liposomes assessed as binding constant by fluorescence quenching assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID424411Toxicity in human assessed as blood and lymphatic system disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1879507Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1903 harboring rpoBD530V mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID424387Toxicity in human assessed as nausea at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424367AUC (0 to 48 hrs) in human assessed as total antimycobacterial agents at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424391Toxicity in human assessed as increase in ALT level at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID634283Antimycobacterial activity against Mycobacterium tuberculosis isolate 343 expressing rpoB Asp516Val mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1653417Inhibition of PGL1 synthesis in Mycobacterium leprae infected Swiss Webster mouse macrophages assessed as decrease in [U-14C]PA incorporation at 2 uM preincubated for 4 days post infection followed by [U-14C]PA addition and measured after 7 days by liquid2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID634270Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID722429Binding affinity to DPH probe-labeled DMPG liposomes assessed as main phase transition temperature at 30 uM by steady-state fluorescence anisotrope (Rvb = 24.1 +/- 0.5 degC)2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID1162167Antimycobacterial activity against Mycobacterium avium assessed as growth inhibition2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
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.
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.
AID424415Toxicity in human assessed as thrombocytopenia at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID571676AUC (OBS) in BALB/c mouse serum at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID285160Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID571677AUC (OBS) in BALB/c mouse serum at 4 to 5 mg/kg administered as inhalable bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID298732Antibacterial activity against rifamycin-resistant Staphylococcus aureus CB370 with rpoB His481Tyr mutation2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1884638Elimination half life in CD-1 mouse at 5 mg/kg, iv measured at 5 to 24 hrs by LC-MS/MS analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID1884632Water solubility of compound in PBS buffer at pH 7.4 by UPLC-MS analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID424419Toxicity in human assessed as insomnia at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID634278Antimycobacterial activity against Mycobacterium tuberculosis isolate 308 expressing rpoB His526Asp mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID634272Antimycobacterial activity against Mycobacterium tuberculosis isolate 353 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1879513Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1903 harboring rpoBD530V mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID722437Drug localization in DPH-PA probe-labeled DMPC liposomes at 42 +/- 0.1 degC by fluorescence quenching2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
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]
AID1653541Plasma concentration in rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse at 6 mg/kg administered with food daily for 12 weeks by high-pressure liquid chromatography analysis2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
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.
AID1653521Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.1 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
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).
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.
AID348181Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID1653508Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.3 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID285159Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
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]
AID424384Toxicity in human assessed as diarrhea at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID571669Cmax in 10'6 human THP1 cells at 3 ug/ml administered as microparticles after 10 mins by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
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.
AID424365Cmax in human assessed as dAc-RFB level at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424363Ctau in human at 150 mg, po QOD co-treated with 700 mg, po fosamprenavir BID and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID276752Antimycobacterial activity against rifampicin and rifabutin resistant Mycobacterium tuberculosis ATCC 358382006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID424396Toxicity in human assessed as fatigue at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID634281Antimycobacterial activity against Mycobacterium tuberculosis isolate 363 expressing rpoB Asp516Val mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1884633Water solubility of compound in HCL by UPLC-MS analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID1653531Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse assessed as ATP level in footpad at 6 mg/kg administered with food daily for 1 week by Shepard's kinetic method (Rvb = 102%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID634276Antimycobacterial activity against Mycobacterium tuberculosis isolate 311 expressing rpoB mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID571679Half life in BALB/c mouse serum at 4 to 5 mg/kg administered as inhalable bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID424358AUC (0 to 48 hrs) in human at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1884634Antibacterial activity against Acinetobacter baumannii assessed as reduction in bacterial growth in CAMHB preincubated 6 hrs followed by human serum addition and measured after 20 hrs by microdilution assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID1473856Ratio of drug concentration at steady state in human at 300 to 900 mg, po QD after 24 hrs to IC50 for human MRP2 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.
AID348178Antimycobacterial activity against isoniazid, rifampicin and ethambutol-resistant Mycobacterium tuberculosis after 7 days by resazurin method2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID1473857Ratio of drug concentration at steady state in human at 300 to 900 mg, po QD after 24 hrs to IC50 for human MRP4 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.
AID424377Toxicity in human assessed as renal and urinary disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID534425Antibacterial activity against Mycobacterium bovis BCG-Glaxo2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID424413Toxicity in human assessed as neutropenia at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424357Average plasma concentration in human at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1884643AUC (0 to infinity) in CD-1 mouse at 5 mg/kg, iv measured at 5 to 24 hrs by LC-MS/MS analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration.
AID424410Toxicity in human assessed as blood and lymphatic system disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424376Toxicity in human assessed as renal and urinary disorder at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID1879497Antibacterial activity against Helicobacter pylori ATCC 7003922022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID571671Elimination rate constant in human THP1 cells at 3 ug/ml administered as microparticles after 10 mins by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID424417Toxicity in human assessed as psychiatric disorder at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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).
AID29851Half life was measured as time taken to decrease half of its initial concentration2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Property-based design: optimization of drug absorption and pharmacokinetics.
AID1879501Antibacterial activity against Helicobacter pylori ATCC 700392 at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1879495Antibacterial activity against Staphylococcus aureus ATCC 292132022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID424390Toxicity in human assessed as increase in ALT level at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
AID722428Binding affinity to DPH-PA probe-labeled DMPG liposomes assessed as main phase transition temperature at 30 uM by steady-state fluorescence anisotrope (Rvb = 23.9 +/- 0.3 degC)2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID424378Toxicity in human assessed as chromaturia at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID722431Binding affinity to DPH probe-labeled DMPC liposomes assessed as main phase transition temperature at 30 uM by steady-state fluorescence anisotrope (Rvb = 24.4 +/- 0.2 degC)2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Differential interactions of rifabutin with human and bacterial membranes: implication for its therapeutic and toxic effects.
AID348186Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction of bacterial load in lungs at 5 mg/kg/day, intragastrically after 1 month relative to control2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID1653532Anti-leprotic activity against rifampin-susceptible Mycobacterium leprae infected in BALB/c mouse assessed as ATP level in footpad at 6 mg/kg administered with food daily for 2 weeks by Shepard's kinetic method (Rvb = 109%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID571678Half life in BALB/c mouse serum at 4 to 5 mg/kg, iv administered as single bolus dose by HPLC2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
AID348180Antimycobacterial activity against non-replicating Mycobacterium tuberculosis assessed as colony forming unit after 8 days2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID424371AUC (0 to 48 hrs) in human assessed as total antimycobacterial agents at 150 mg, po QD coadministered with 700 mg fosamprenavir and 100 mg ritonavir po BID2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
AID424398Toxicity in human assessed as chills at 300 mg, po QD2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Pharmacokinetic interaction between fosamprenavir-ritonavir and rifabutin in healthy subjects.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (36.84)29.6817
2010's21 (55.26)24.3611
2020's3 (7.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials1 (3.13%)5.53%
Reviews0 (0.00%)6.00%
Reviews5 (15.63%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
Other26 (81.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (70)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I Open-Label Trial To Investigate the Pharmacokinetic Interaction Between Rifabutin Or Rifampin And A Single Dose Of TMC207 In Healthy Subjects[NCT01341184]Phase 133 participants (Actual)Interventional2011-10-21Completed
Phase I, Single-center, Open Label, Fixed-sequence Cross-over Study to Evaluate the Effect of Rifabutin on the Pharmacokinetics of Oral Cabotegravir in Healthy Subjects[NCT03149848]Phase 115 participants (Actual)Interventional2017-06-06Completed
A Phase 2/3, Multicenter, Randomized, Open-label, Active-controlled Study to Evaluate the Efficacy and Safety of Bedaquiline Administered as Part of a Treatment Regimen With Clarithromycin and Ethambutol in Adult Patients With Treatment-refractory Mycobac[NCT04630145]Phase 2/Phase 3124 participants (Anticipated)Interventional2021-01-08Recruiting
Phase 1, Open Label, Two Arm, Fixed Sequence Study to Evaluate the Effect of Rifampin and Rifabutin on GSK1349572 Pharmacokinetics in Healthy Male and Female Volunteers[NCT01231542]Phase 127 participants (Actual)Interventional2011-05-31Completed
A Phase 1, Open-label, Fixed-sequence Study to Investigate the Effect of the Moderate CYP3A Inducer Rifabutin on the Pharmacokinetics of Zanubrutinib in Healthy Male Subjects[NCT04470908]Phase 113 participants (Actual)Interventional2020-07-29Completed
Phase IIa Prospective Study to Evaluate the Safety and Measure Efficacy of Anti-chlamydophila Antibiotic Combination (ACAC) Therapy Comprising 100mg Doxycycline, 500mg Azithromycin and 300mg Rifabutin in the Treatment of Patients With Coronary Heart Disea[NCT03618108]Phase 220 participants (Actual)Interventional2018-04-04Terminated(stopped due to COVID-19)
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics[NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
Pharmacokinetic Interaction Study to Evaluate the Pharmacokinetic Effect of Rifabutin on BMS-626529, the Active Moiety of BMS-663068, With and Without Ritonavir in Healthy Subjects[NCT02138084]Phase 1102 participants (Actual)Interventional2014-05-14Completed
Open-Label Pharmacokinetics Study to Evaluate Drug-Drug Interactions and Safety of ELPIDA® in Co-Administration With Other Drugs in Healthy Volunteers[NCT03709355]Phase 156 participants (Actual)Interventional2018-11-14Completed
An Open-label Study in HIV+ Patients to Determine the Effects of Nevirapine (VIRAMUNE®) on the Steady State Pharmacokinetics of Rifabutin (MYCOBUTIN®)[NCT02184078]Phase 419 participants (Actual)Interventional1998-10-31Completed
Rifabutin-containing Triple Therapy for Helicobacter Pylori Rescue Treatment: a Randomized Controlled Trial[NCT05874544]Phase 4357 participants (Anticipated)Interventional2023-05-16Recruiting
Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT)[NCT04310930]Phase 2/Phase 3300 participants (Anticipated)Interventional2020-03-02Recruiting
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 Single Center, Open-label Study to Investigate the Penetration of Rifabutin Into the Lung After Multiple Intravenous Administrations of BV100 (Rifabutin for Infusion) in Healthy Participants[NCT05684705]Phase 140 participants (Anticipated)Interventional2023-09-01Recruiting
Dosing, Safety and Pharmacokinetic Profile of Rifabutin in Children Receiving Concomitant Treatment With Kaletra[NCT01259219]Phase 140 participants (Anticipated)Interventional2010-11-30Recruiting
A Randomized Double Blind Active Comparator Controlled Phase III Study to Assess the Safety and Efficacy of RHB-105 in the Treatment of Confirmed Helicobacter Pylori (H. Pylori) Infection[NCT03198507]Phase 3455 participants (Actual)Interventional2017-06-18Completed
Pharmacokinetics of Rifabutin Combined With Antiretroviral Therapy in the Treatment of Tuberculosis Patient With HIV Infection in South Africa: A Phase II Trial[NCT00640887]Phase 248 participants (Anticipated)Interventional2009-02-28Completed
Interaction of Buprenorphine With HIV Medications and Tuberculosis Medications[NCT00877591]Phase 163 participants (Actual)Interventional2008-04-30Completed
Study of RHB-204 for the Treatment of Pulmonary Mycobacterium Avium Complex (MAC) Disease in Adults With Nodular Bronchiectasis (CleaR-MAC Trial)[NCT04616924]Phase 3125 participants (Anticipated)Interventional2020-12-01Active, not recruiting
A Single-centre Open-label Study in Healthy Adult Volunteers to Determine the Effects of Steady-state TPV/RTV (500 mg/200 mg) on the Single-dose Pharmacokinetics of Rifabutin (MYCOBUTIN®) 150 mg, and the Effects of Single-dose Rifabutin (150 mg) on the St[NCT02251171]Phase 124 participants (Actual)Interventional2003-08-31Completed
IMPACT-TB (Imatinib Mesylate Per Oral as a Clinical Therapeutic for TB): A Phase II Clinical Trial of the Safety, Pharmacokinetics and Hematologic Effects of Imatinib on Myelopoiesis in Adults When Given With and Without Isoniazid and Rifabutin[NCT03891901]Phase 224 participants (Actual)Interventional2020-10-27Completed
Pharmacokinetics of Rifabutin Combined With Antiretroviral Therapy in the Treatment of Tuberculosis Patient With HIV Infection in Vietnam : A Phase II Trial[NCT00651066]Phase 247 participants (Actual)Interventional2010-06-30Completed
A Comparison of the Bioavailability of Rifabutin With and Without Lopinavir/Ritonavir in Healthy Adult Subjects[NCT00743470]Phase 115 participants (Actual)Interventional2008-08-31Terminated
Special Investigation For Non-hiv Patients Of Mycobutin (Regulatory Post Marketing Commitment Plan).[NCT00810407]628 participants (Actual)Observational2008-11-30Completed
Comparison Between Tailored Therapy Guided by a Non-invasive Antibiotic Susceptibility Test and Empiric Treatment for First-line Helicobacter Pylori Eradication in Patients With Dyspepsia: a Randomized Controlled Trial.[NCT04107194]Phase 3362 participants (Anticipated)Interventional2020-01-14Recruiting
Randomized, Double-Blinded Evaluation of Rifabutin Based Therapy for Eradication of Staphylococcus Aureus Carriage in HIV Infected Individuals With Prior Skin and Skin Structure Infections[NCT00869518]Phase 212 participants (Actual)Interventional2009-07-31Terminated(stopped due to Poor enrollment)
A Prospective, Randomized, Comparative Study of the Safety and Efficacy of Clarithromycin Versus Rifabutin Versus the Combination of Clarithromycin Plus Rifabutin for the Prevention of Mycobacterium Avium Complex (MAC) Bacteremia or Disseminated MAC Disea[NCT00001030]Phase 31,100 participants InterventionalCompleted
An Open-Label, Randomized Trial of Four Treatment Regimens for Patients With Disseminated Mycobacterium Avium Complex Disease and Acquired Immunodeficiency Syndrome (AIDS)[NCT00001047]Phase 3400 participants InterventionalCompleted
DRUG USE INVESTIGATION FOR HIV INFECTION PATIENTS OF MYCOBUTIN (REGULATORY POST MARKETING COMMITMENT PLAN).[NCT00810446]72 participants (Actual)Observational2009-06-30Completed
Effect of Fluconazole, Clarithromycin, and Rifabutin on the Pharmacokinetics of Sulfamethoxazole and Dapsone and Their Hydroxylamine Metabolites[NCT00000826]Phase 148 participants InterventionalCompleted
Steady-State Pharmacokinetic Interaction Study of Indinavir and Rifabutin[NCT00000877]Phase 131 participants InterventionalCompleted
Open, Noncomparative Trial of Multidrug Regimens Containing Azithromycin and Rifabutin Administered Three Times Per Week for the Treatment of M. Avium Complex (MAC) Lung Disease[NCT00598962]Phase 458 participants (Actual)Interventional1994-12-31Completed
Study to Evaluate the Exposure of Rifabutin Administered in an Alternate Regimen in Combination With Atazanavir and Ritonavir Healthy Subjects[NCT00646776]Phase 185 participants (Actual)Interventional2008-04-30Completed
Rifabutin Versus Rifampicin for Treatment of Staphylococcal Prosthetic Joint Infection Treated With Debridement, Antibiotics and Implant Retention (DAIR Strategy): a Multicenter Randomized, Open-label, Non-inferiority Trial[NCT04672525]Phase 3436 participants (Anticipated)Interventional2021-11-08Recruiting
Genotypic Resistance-guided Triple Therapy Versus Empirical Concomitant Therapy for First-line H. Pylori Eradication.[NCT04090021]Phase 4304 participants (Anticipated)Interventional2019-09-01Recruiting
An Open Label Study to Assess the Efficacy and Safety of Fixed-Dose Combination RHB-104 in Subjects With Active Crohn's Disease Despite 26 Weeks of Participation in the MAP US RHB-104-01 Study[NCT03009396]Phase 354 participants (Actual)Interventional2017-03-18Completed
Treatment of Crohn's Disease With an Antibiotic Regimen Directed Against Mycobacterium Avium Paratuberculosis[NCT00513552]Phase 40 participants (Actual)Interventional2007-07-31Withdrawn(stopped due to No patient)
Toxicity and Pharmacokinetics of Different Rifabutin Doses in HIV-infected Adults and Adolescents Taking Lopinavir / Ritonavir as Second-line Anti-retroviral Therapy (ART) (EARNEST Rifabutin PK Substudy)[NCT01663168]Phase 2140 participants (Anticipated)Interventional2011-12-31Recruiting
Rifabutin-containing Triple Therapy for Rescue Treatment of Helicobacter Pylori: A Randomized Clinical Trial[NCT04879992]413 participants (Actual)Interventional2021-05-07Completed
Phase 2C Clinical Trial of Novel, Short-course Regimens for the Treatment of Pulmonary Tuberculosis: CRUSH-TB (Combination Regimens for Shortening TB Treatment)[NCT05766267]Phase 2/Phase 3288 participants (Anticipated)Interventional2023-03-01Not yet recruiting
Effectiveness of Rifabutin Triple Therapy for First-line and Rescue Treatment of Helicobacter Pylori Infection[NCT04652284]Phase 3300 participants (Anticipated)Interventional2021-05-01Not yet recruiting
Open, Noncomparative Trial of Multidrug Regimens Containing Clarithromycin and Rifabutin Administered Three Times Per Week for the Treatment of M. Avium Complex (MAC) Lung Disease[NCT00598897]Phase 489 participants (Actual)Interventional1995-08-31Completed
TBTC Study 23C: Intensive Pharmacokinetic Study of Intermittent Rifabutin and Isoniazid With Daily Efavirenz in Combination With Two Nucleoside Analogs for Treatment of HIV and Tuberculosis Co-infections[NCT00023413]Phase 220 participants Interventional1999-11-30Completed
A Ph2 Randomized Trial to Evaluate the Safety Preliminary Efficacy and Biomarker Response of Host Directed Therapies Added to Rifabutin-modified Standard Therapy in Adults With Drug-Sensitive Smear-Positive Pulmonary TB[NCT02968927]Phase 2200 participants (Actual)Interventional2016-11-30Active, not recruiting
Intensive Pharmacokinetics of the Nelfinavir-Rifabutin Interaction in Patients With HIV-Related Tuberculosis Treated With a Rifabutin-Based Regimen[NCT00018083]0 participants InterventionalRecruiting
TBTC Study 23: Treatment of HIV-Related Tuberculosis Using a Rifabutin-Based Regimen[NCT00023361]215 participants Interventional1999-02-28Completed
TBTC Study 23B:Intensive Pharmacokinetics of the Nelfinavir Rifabutin Interaction in Patients With HIV-Related Tuberculosis Treated With a Rifabutin-Based Regimen[NCT00023400]Phase 420 participants Interventional2000-02-29Completed
TBTC Study 23A: Pharmacokinetics of Intermittent Isoniazid and Rifabutin in USPHS Study 23: Treatment of HIV-Related Tuberculosis Using a Rifabutin-Based Regimen[NCT00023348]Phase 2/Phase 3150 participants Interventional1999-07-31Completed
Evaluation of the Safety, Tolerance and Pharmacokinetics of Rifabutin/Clarithromycin Combination and Rifabutin/Azithromycin Combination in HIV-Infected Patients[NCT00001023]91 participants InterventionalCompleted
A Randomized, Phase 2b Study of a Double-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifampin-Based Tuberculosis Treatment Versus a Standard-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifabutin-Based Tuberculosis Treatment W[NCT01601626]Phase 271 participants (Actual)Interventional2013-07-13Terminated(stopped due to The study was stopped early due to feasibility concerns.)
A Double-Blind Randomized Clinical Trial of a Rifabutin Regimen in the Treatment of Mycobacterium-Avium Complex (MAC) Bacteremia in Patients With AIDS[NCT00001995]200 participants InterventionalCompleted
An Open-Label Randomized Pharmacokinetic/Pharmacodynamic Study of Mycobutin (Rifabutin) or Rifabutin in Combination With Myambutol (Ethambutol) for Prophylaxis of Mycobacterium Avium Complex (MAC) Bacteremia in AIDS Patients With CD4 Counts <= 100 Cells/m[NCT00002343]Phase 4200 participants InterventionalCompleted
Rifabutin Therapy for the Prevention of Mycobacterium Avium Complex (MAC) Bacteremia in AIDS Patients With CD4 Counts = or < 200: A Double-Blind, Placebo-Controlled Trial[NCT00002032]750 participants InterventionalCompleted
Rifabutin Therapy for the Prevention of Mycobacterium Avium Complex (MAC) Bacteremia in HIV Positive Patients With CD4 Counts = or < 200: Treatment IND Study[NCT00002080]0 participants InterventionalCompleted
A Randomized Study of Daily and Intermittent Prophylactic Regimens for the Prevention of Disseminated Mycobacterium Avium Complex (MAC) and Fungal Infections in HIV-Infected Patients[NCT00002122]Phase 3720 participants InterventionalCompleted
A Phase I, Open-Label Study in Healthy Subjects, to Explore the Pharmacokinetics of Different Dosing Regimens of Rilpivirine in Combination With Rifabutin, at Steady-State[NCT01615614]Phase 120 participants (Actual)Interventional2012-04-30Completed
A Phase II/III Prospective, Multicenter, Randomized, Controlled Trial Comparing the Safety and Efficacy of Three Clarithromycin-Containing Combination Drug Regimens for the Treatment of Disseminated Mycobacterium Avium Complex (MAC) Disease in Persons Wit[NCT00001058]Phase 2246 participants InterventionalCompleted
A Three-Arm Comparative Trial for the Treatment of MAC Bacteremia in AIDS: A Clarithromycin/Ethambutol Regimen Containing Rifabutin (450 Mg) or Rifabutin (300 Mg) or Placebo[NCT00002101]Phase 3450 participants InterventionalCompleted
Viral and Immune Dynamics in HIV-Infected Patients With Tuberculosis[NCT00004736]Phase 144 participants InterventionalCompleted
Rifabutin Therapy for the Prevention of Mycobacterium Avium Complex (MAC) Bacteremia in AIDS Patients With CD4 Counts = or < 200: A Double-Blind, Placebo-Controlled Trial[NCT00002267]750 participants InterventionalCompleted
Clinical Efficacy of Rifabutin in the Treatment of Serious and Life Threatening Infections Due to Mycobacterium Avium Complex, or Drug Resistant Mycobacterium Tuberculosis, or Other Drug Resistant Mycobacterium[NCT03164291]Phase 3170 participants (Actual)Interventional1984-06-30Completed
A Pilot Study of the Pharmacokinetics and Safety of Rifabutin 150 mg Once Daily Versus Rifabutin 300 mg Thrice Weekly With Lopinavir/Ritonavir Based HAART in HIV/TB Co-infected Patients[NCT02415985]Phase 240 participants (Actual)Interventional2015-06-30Completed
New Super-short Course Regimen for Retreatment Pulmonary Tuberculosis[NCT02331823]Phase 4864 participants (Anticipated)Interventional2013-06-30Recruiting
A Phase 1, Open-label, Multicohort Study to Evaluate the Impact of Inhibitors and Inducers of Cytochrome P450 Enzyme (CYP)3A, P-glycoprotein (P-gp), and Breast Cancer Resistant Protein (BCRP) on the Pharmacokinetics (PK) of Vesatolimod (VES) in Virologica[NCT05458102]Phase 118 participants (Actual)Interventional2022-08-19Terminated(stopped due to Sponsor's decision to change the clinical development plan of this molecule. This decision is not based on efficacy or safety concerns.)
An Open-label, Non-randomized, Monocenter, Single-dose, Phase I Study to Evaluate Pharmacokinetics and Safety of BV100 Administered as Single Intravenous In-fusion to Subjects With Renal Impairment[NCT05086107]Phase 148 participants (Actual)Interventional2021-10-08Completed
Impact of Rifabutin on the Pharmacokinetics of Elexacaftor/Tezacaftor/Ivacaftor[NCT04840862]Phase 424 participants (Anticipated)Interventional2022-05-09Recruiting
A Drug Interaction Study Investigating the Effect of Rifabutin on the Pharmacokinetics of Maraviroc[NCT01894776]Phase 115 participants (Actual)Interventional2013-06-30Completed
A Phase 2 Randomized, Open-Label Trial of PA-824-Containing Regimens Versus Standard Treatment for Drug-Sensitive Sputum Smear-Positive Pulmonary Tuberculosis[NCT02256696]Phase 2157 participants (Actual)Interventional2015-04-29Completed
Open-Label, Randomized, 3-Way Crossover Study To Estimate The Interaction Between Multiple Dose Rifabutin And Lersivirine (UK-453,061) In Healthy Subjects[NCT00925535]Phase 118 participants (Actual)Interventional2010-05-31Completed
The Efficacy and Safety Evaluation of Standardized Treatment Included Rifampicin or Rifabutin in HIV/AIDs Patients Combined With Pulmonary Tuberculosis. A Prospective Study.[NCT03478033]230 participants (Anticipated)Interventional2018-04-15Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00646776 (26) [back to overview]Cmax of ATV
NCT00646776 (26) [back to overview]Cmax of 25-O-Desacetylrifabutin (25-O-Desacetyl-RIB)
NCT00646776 (26) [back to overview]Average Area Under the Plasma Concentration-time Curve for 24 Hours (AUC24avg) for Rifabutin (RIB)
NCT00646776 (26) [back to overview]AUC24avg for 25-O-Desacetyl-RIB
NCT00646776 (26) [back to overview]AUC(TAU) for RTV
NCT00646776 (26) [back to overview]AUC(TAU) for ATV
NCT00646776 (26) [back to overview]Number of Participants With MAs in Serum Chemistry: Alkaline Phosphatase (ALP),Aspartate Aminotransferase (AST),Alanine Aminotransferase (ALT),Bilirubin (Total),Bilirubin (Direct),Blood Urea Nitrogen (BUN),Creatinine,Sodium (Serum),Potassium (Serum)
NCT00646776 (26) [back to overview]Number of Participants With MAs in Hematology: Neutrophils + Bands (Absolute), Lymphocytes (Absolute), Monocytes (Absolute), Basophils (Absolute) and Eosinophils (Absolute)
NCT00646776 (26) [back to overview]Terminal Elimination Half-life (T-half) of ATV
NCT00646776 (26) [back to overview]Number of Participants With Marked Abnormalities (MAs) in Hematology: Hemoglobin, Hematocrit, Platelet Count and Leukocytes
NCT00646776 (26) [back to overview]Number of Participants Who Died, Experienced Other Serious Adverse Events (SAEs), Experienced Adverse Events (AEs) and Experienced Events Leading to Discontinuation.
NCT00646776 (26) [back to overview]Total Area Under the Plasma Concentration-time Curve (AUCtot)
NCT00646776 (26) [back to overview]Tmax of RTV
NCT00646776 (26) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of ATV
NCT00646776 (26) [back to overview]T-half of RTV
NCT00646776 (26) [back to overview]Number of Participants With Identified Electrocardiogram (ECG) Abnormalities
NCT00646776 (26) [back to overview]Number of Participants With Clinically Significant Vital Signs or Physical Examination Findings
NCT00646776 (26) [back to overview]Maximum Plasma Concentration (Cmax) of RIB
NCT00646776 (26) [back to overview]Number of Participants With MAs in Serum Chemistry: Glucose (Fasting Serum), Albumin, Creatine Kinase, Uric Acid, Lactate Dehydrogenase (LDH)
NCT00646776 (26) [back to overview]Cmin of RTV
NCT00646776 (26) [back to overview]Cmin of ATV
NCT00646776 (26) [back to overview]Cmin of 25-O-Desacetyl-RIB
NCT00646776 (26) [back to overview]Cmax of RTV
NCT00646776 (26) [back to overview]Minimum Plasma Concentration (Cmin) of RIB
NCT00646776 (26) [back to overview]Number of Participants With MAs in Urinalysis
NCT00646776 (26) [back to overview]Number of Participants With MAs in Serum Chemistry: Chloride (Serum), Calcium (Total), Protein (Total), Bicarbonate, Phosphorous (Inorganic)
NCT00810407 (9) [back to overview]Number of Participants With Treatment-Related Adverse Events Unexpected From Japanese Package Insert
NCT00810407 (9) [back to overview]Clinical Efficacy Rate by Age
NCT00810407 (9) [back to overview]Clinical Efficacy Rate by Diagnosis
NCT00810407 (9) [back to overview]Clinical Efficacy Rate by Gender
NCT00810407 (9) [back to overview]Number of Participants With Treatment-Related Adverse Events
NCT00810407 (9) [back to overview]Number of Participants With Treatment-Related Adverse Events by Age
NCT00810407 (9) [back to overview]Number of Participants With Treatment-Related Adverse Events by Diagnosis
NCT00810407 (9) [back to overview]Number of Participants With Treatment-Related Adverse Events by Gender
NCT00810407 (9) [back to overview]Clinical Efficacy Rate
NCT00810446 (9) [back to overview]Number of Patients With Adverse Drug Reactions in This Surveillance
NCT00810446 (9) [back to overview]Number of Participants With Adverse Drug Reactions by Gender
NCT00810446 (9) [back to overview]Clinical Response Rate (Therapeutic)
NCT00810446 (9) [back to overview]The Number of Participants Who Experienced an Adverse Drug Reaction Not Expected From the Local Product Document (Unknown Adverse Drug Reactions)
NCT00810446 (9) [back to overview]Clinical Response Rate (Therapeutic) by Age
NCT00810446 (9) [back to overview]Number of Participants With Adverse Drug Reactions by Diagnosis
NCT00810446 (9) [back to overview]Clinical Response Rate (Therapeutic) by Gender
NCT00810446 (9) [back to overview]Number of Participants With Adverse Drug Reactions by Age
NCT00810446 (9) [back to overview]Clinical Response Rate (Therapeutic) by Diagnosis
NCT00869518 (3) [back to overview]Eradication of S. Aureus Colonization
NCT00869518 (3) [back to overview]Eradication of S. Aureus Colonization
NCT00869518 (3) [back to overview]Recurrent Skin and Skin Structure Infections (SSTI)
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 24
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 48
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 72
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 8
NCT01601626 (26) [back to overview]Cumulative Probability of HIV Virologic Failure at Week 72
NCT01601626 (26) [back to overview]LPV AUC in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Sign or Symptom
NCT01601626 (26) [back to overview]Number of Participants Who Experienced MTB IRIS
NCT01601626 (26) [back to overview]Percent of Participants Who Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness or Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced HIV Virologic Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced Sputum Conversion at Week 8.
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Treatment Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48
NCT01601626 (26) [back to overview]RAL AUC in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]RBT AUC in Participants Enrolled in Arms A and C
NCT01601626 (26) [back to overview]LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]RAL Cmax and Cmin in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]RBT Cmax and Cmin in Participants Enrolled in Arms A and C
NCT01894776 (3) [back to overview]Safety/Tolerability of the Treatments
NCT01894776 (3) [back to overview]Maraviroc and Rifabutin C12/C24/Cmax PK Concentrations in Plasma.
NCT01894776 (3) [back to overview]Pharmacokinetics of Maraviroc and Rifabutin AUC 0-12/24
NCT02256696 (8) [back to overview]Steady State Pharmacokinetics (PK) (AUC) of PA-824 When Given With Rifampin or Rifabutin
NCT02256696 (8) [back to overview]Relationship Between PA-824 Exposure (AUC) and Rate of Change in Time to Positivity (TTP) Over 12 Weeks
NCT02256696 (8) [back to overview]PK (Cmax) of PA-824 at 200 mg Once Daily With Rifampin or Rifabutin-containing Treatment
NCT02256696 (8) [back to overview]Number of Participants With Permanent Discontinuation of Assigned Study Regimen
NCT02256696 (8) [back to overview]Number of Participants With Grade 3 or Higher Adverse Events
NCT02256696 (8) [back to overview]Time to Sputum Culture Conversion on Liquid Medium
NCT02256696 (8) [back to overview]Percentage of Participants With Sputum Culture Conversion by 8 Weeks of Treatment
NCT02256696 (8) [back to overview]Time to Culture Conversion on Solid Medium
NCT03009396 (8) [back to overview]Number of Weeks the Patients Are in Response.
NCT03009396 (8) [back to overview]Number of Weeks to Achieve Response
NCT03009396 (8) [back to overview]Response at Week 16
NCT03009396 (8) [back to overview]The Number of Weeks for Patients to Achieve Remission
NCT03009396 (8) [back to overview]Durable Remission Week 16 Through Week 52
NCT03009396 (8) [back to overview]Increase in Milliseconds (ms) QT Wave
NCT03009396 (8) [back to overview]Number of Patients in Remission at Week 16
NCT03009396 (8) [back to overview]Number of Weeks the Patients Are in Remission
NCT03149848 (22) [back to overview]Assessment of Plasma CAB PK Parameter: Maximum Observed Concentration (Cmax)
NCT03149848 (22) [back to overview]Assessment of Plasma CAB PK Parameter: The Apparent Oral Clearance (CL/F)
NCT03149848 (22) [back to overview]Assessment of Plasma CAB PK Parameter: Time of Occurrence of Cmax (Tmax)
NCT03149848 (22) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings
NCT03149848 (22) [back to overview]Number of Participants With Abnormal Urinalysis Result
NCT03149848 (22) [back to overview]Assessment of Clinical Chemistry Parameters: Albumin and Protein
NCT03149848 (22) [back to overview]Assessment of Clinical Chemistry Parameters: Alkaline Phosphatase (ALP), Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), Creatine Kinase (CK) and Gamma Glutamyl Transferase (GGT)
NCT03149848 (22) [back to overview]Assessment of Clinical Chemistry Parameters: Direct Bilirubin (DB), Bilirubin and Creatinine
NCT03149848 (22) [back to overview]Assessment of Hematology Parameter: Eryrocyte Mean Corpuscular Hemoglobin
NCT03149848 (22) [back to overview]Assessment of Hematology Parameter: Erythrocye Mean Corpuscular Volume
NCT03149848 (22) [back to overview]Assessment of Hematology Parameter: Hemoglobin
NCT03149848 (22) [back to overview]Assessment of Hematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes
NCT03149848 (22) [back to overview]Assessment of Hematology Parameters: Erythrocytes and Reticulocytes
NCT03149848 (22) [back to overview]Assessment of Hematology Parameters: Erythrocytes Distribution Width (EDW)
NCT03149848 (22) [back to overview]Assessment of Hematology Parameters: Hematocrit and Reticulocytes/Erythrocytes (R/E)
NCT03149848 (22) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT03149848 (22) [back to overview]Concurrent Medication Assessment in Treatment Period 1 and 2
NCT03149848 (22) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT03149848 (22) [back to overview]Assessment of Clinical Chemistry Parameters: Calcium, Chloride, Carbon Dioxide, Glucose, Potassium, Sodium and Urea
NCT03149848 (22) [back to overview]Assessment of Plasma CAB Pharmacokinetic (PK) Parameter: Area Under the Concentration-time Curve Over One Dosing Interval (AUC [0 to Tau])
NCT03149848 (22) [back to overview]Assessment of Plasma CAB PK Parameter: Concentration at the End of the Dosing Interval (Ctau)
NCT03149848 (22) [back to overview]Change From Baseline in Pulse Rate
NCT03198507 (4) [back to overview]Number of Participants With H. Pylori Cultures That Presented Antibiotic Resistance and Susceptibility
NCT03198507 (4) [back to overview]Number of Participants With Adverse Events That Are Related to Treatment
NCT03198507 (4) [back to overview]Number of Participants With Eradication of H. Pylori in the Pharmacokinetic Population (PKP)
NCT03198507 (4) [back to overview]Number of Participants With Eradication of H. Pylori
NCT03891901 (20) [back to overview]Elimination Rate Constant (Ke) of Imatinib
NCT03891901 (20) [back to overview]Area Under the Curve (AUC) for Imatinib
NCT03891901 (20) [back to overview]Maximum Concentration (Cmax) of Rifabutin
NCT03891901 (20) [back to overview]Maximum Concentration (Cmax) of Isoniazid
NCT03891901 (20) [back to overview]Half-life (T1/2) of Rifabutin
NCT03891901 (20) [back to overview]Half-life (T1/2) of Isoniazid
NCT03891901 (20) [back to overview]Frequency of Serious Adverse Events (SAEs)
NCT03891901 (20) [back to overview]Frequency of Grade 3 or 4 Adverse Events (AEs)
NCT03891901 (20) [back to overview]Elimination Rate Constant (Ke) of Rifabutin
NCT03891901 (20) [back to overview]Elimination Rate Constant (Ke) of Isoniazid
NCT03891901 (20) [back to overview]White Blood Cell Count
NCT03891901 (20) [back to overview]Area Under the Curve (AUC) for Rifabutin
NCT03891901 (20) [back to overview]Area Under the Curve (AUC) for Isoniazid
NCT03891901 (20) [back to overview]Half-life (T1/2) of Imatinib
NCT03891901 (20) [back to overview]Half-life (T1/2) of Imatinib
NCT03891901 (20) [back to overview]Elimination Rate Constant (Ke) of Imatinib
NCT03891901 (20) [back to overview]Area Under the Curve (AUC) for Imatinib
NCT03891901 (20) [back to overview]Number of Myelomonocytic Cells in the Blood
NCT03891901 (20) [back to overview]Maximum Concentration (Cmax) of Imatinib
NCT03891901 (20) [back to overview]Maximum Concentration (Cmax) of Imatinib
NCT04470908 (9) [back to overview]Time to the Maximum Observed Plasma Concentration (Tmax) of Zanubrutinib
NCT04470908 (9) [back to overview]AUC From Time Zero to Infinity (AUC0-∞) of Zanubrutinib
NCT04470908 (9) [back to overview]Area Under the Curve (AUC) From Time Zero to the Time of the Last Quantifiable Concentration (AUC0-t) of Zanubrutinib
NCT04470908 (9) [back to overview]Apparent Volume of Distribution (Vz/F) of Zanubrutinib
NCT04470908 (9) [back to overview]Apparent Terminal Elimination Half-life (t1/2) of Zanubrutinib
NCT04470908 (9) [back to overview]Apparent Oral Clearance (CL/F) of Zanubrutinib
NCT04470908 (9) [back to overview]Number of Participants Experiencing Adverse Events (AEs)
NCT04470908 (9) [back to overview]Time of the Last Quantifiable Concentration (Tlast) of Zanubrutinib
NCT04470908 (9) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Zanubrutinib

Cmax of ATV

Cmax was derived from the plasma concentration versus time for ATV and was recorded directly from experimental observations for each treatment period. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly5633

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Cmax of 25-O-Desacetylrifabutin (25-O-Desacetyl-RIB)

Cmax was derived from the plasma concentration versus time for 25-O-Desacetyl-RIB (a metabolite of RIB) and was recorded directly from experimental observations for each treatment period. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
RIB 150 mg Once Daily (QD)13.44
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly104.36

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Average Area Under the Plasma Concentration-time Curve for 24 Hours (AUC24avg) for Rifabutin (RIB)

AUC24avg is AUC(0-24 hour) following dosing on Day 10 for RIB 150mg once daily (QD); AUC24avg is the area under the plasma concentration-time curve in 1 dosing interval (AUC[TAU]) divided by the number of days over the sampling duration for ATV/RTV 300/100 mg QD+RIB 150 mg twice weekly, i.e. AUC(TAU)/7. (NCT00646776)
Timeframe: Pre-dose (0 hours [h]) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionnanograms*hour /milliliters (ng*h/mL) (Geometric Mean)
RIB 150 mg Once Daily (QD)1565
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly2311

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AUC24avg for 25-O-Desacetyl-RIB

AUC24avg is AUC(0-24 hour) following dosing on Day 10 for RIB 150 mg QD; AUC24avg is the area under the plasma concentration-time curve in 1 dosing interval (AUC[TAU]) divided by the number of days over the sampling duration for ATV/RTV 300/100 mg QD+RIB 150 mg twice weekly, i.e. AUC(TAU)/7 (NCT00646776)
Timeframe: Pre-dose (0h) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng*h/mL (Geometric Mean)
RIB 150 mg Once Daily (QD)117.7
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly1283

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AUC(TAU) for RTV

AUC(TAU) was derived from the plasma concentration versus time for RTV, and was calculated by linear and log-linear trapezoidal summations using a mixed log-linear algorithm. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng*h/mL (Geometric Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly8699

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AUC(TAU) for ATV

AUC(TAU) was derived from the plasma concentration versus time for ATV, and was calculated by linear and log-linear trapezoidal summations using a mixed log-linear algorithm. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng*h/mL (Geometric Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly51795

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Number of Participants With MAs in Serum Chemistry: Alkaline Phosphatase (ALP),Aspartate Aminotransferase (AST),Alanine Aminotransferase (ALT),Bilirubin (Total),Bilirubin (Direct),Blood Urea Nitrogen (BUN),Creatinine,Sodium (Serum),Potassium (Serum)

MAs=laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following serum chemistry MA definitions specify MA criteria. ALP, AST, ALT:>1.25xULN (if pre-Rx >ULN, then >1.25xpre-Rx). Bilirubin (total), bilirubin (direct), BUN:>1.1xULN (if pre-Rx >ULN, then >1.25xpre-Rx). Creatinine:>1.33xpre-Rx. Sodium (serum):<0.95xLLN or >1.05xULN (if pre-Rx ULN. If pre-Rx >ULN, then >1.05xpre-Rx or 1.1xULN (if pre-Rx ULN. If pre-Rx >ULN, then >1.1xpre-Rx or NCT00646776)
Timeframe: Pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14, 20 and 26 for RIB 150 mg QD; and pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14 and 18 for ATV/RTV 300/100 mg QD + RIB 150 mg twice weekly.

,
InterventionParticipants (Number)
ALPASTALTBilirubin (total)Bilirubin (direct)BUNCreatinineSodium (serum)Potassium (serum)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly00017160100
RIB 150 mg Once Daily (QD)000000000

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Number of Participants With MAs in Hematology: Neutrophils + Bands (Absolute), Lymphocytes (Absolute), Monocytes (Absolute), Basophils (Absolute) and Eosinophils (Absolute)

MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following hematology MA definitions specify the criteria for the data presented. Neutrophils+bands (absolute): <=1.50 x 10^3 cells/microliter (uL). Lymphocytes (absolute): <0.75 x 10^3 cells/uL or >7.50 x 10^3 cells/uL. Monocytes (absolute): >2.00 x 10^3 cells/uL. Basophils (absolute): >0.40 x 10^3 cells/uL. Eosinophils (absolute): >0.75 x 10^3 cells/uL. (NCT00646776)
Timeframe: Pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14, 20 and 26 for RIB 150 mg QD; and pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14 and 18 for ATV/RTV 300/100 mg QD + RIB 150 mg twice weekly.

,
InterventionParticipants (Number)
Neutrophils+bands (absolute)Lymphocytes (absolute)Monocytes (absolute)Basophils (absolute)Eosinophils (absolute)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly105000
RIB 150 mg Once Daily (QD)11000

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Terminal Elimination Half-life (T-half) of ATV

T-half was obtained directly from the concentration-time data. T-half following doses administered for treatment ATV/RTV 300/100 mg QD+RIB 150 mg twice weekly. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

InterventionHour (Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly11.89

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Number of Participants With Marked Abnormalities (MAs) in Hematology: Hemoglobin, Hematocrit, Platelet Count and Leukocytes

MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following hematology MA definitions specify the criteria for the data presented. Hemoglobin/hematocrit: <0.85 x pre-treatment (pre-Rx) value. Platelet count: <0.85 x lower limit of normal (LLN) (or, if pre-Rx value 1.5 x upper limit of normal (ULN). Leukocytes: <0.9 x LLN or >1.2 x ULN (or, if pre-Rx value ULN. If pre-Rx value >ULN, then >1.15 x pre-Rx or NCT00646776)
Timeframe: Pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14, 20 and 26 for RIB 150 mg QD; and pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14 and 18 for ATV/RTV 300/100 mg QD + RIB 150 mg twice weekly.

,
InterventionParticipants (Number)
HemoglobinHematocritPlatelet countLeukocytes
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly1107
RIB 150 mg Once Daily (QD)0001

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Number of Participants Who Died, Experienced Other Serious Adverse Events (SAEs), Experienced Adverse Events (AEs) and Experienced Events Leading to Discontinuation.

AEs were defined as new, untoward medical occurrences/worsening of pre-existing medical condition, whether drug-related or not. SAEs were defined as any AE that: resulted in death; was life threatening; resulted in a persistent or significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; was a cancer; or was an overdose. Discontinuation from the study was due either to an AE or was conducted at the investigator's discretion. (NCT00646776)
Timeframe: From Day 1 to 30 days after the last dose of study drug.

,
InterventionParticipants (Number)
DeathsOther SAEsAEsAE leading to discontinuationDiscontinuation due to investigator discretion
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly021394
RIB 150 mg Once Daily (QD)00510

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Total Area Under the Plasma Concentration-time Curve (AUCtot)

AUCtot represents the total free RIB plus 25-O-Desacetyl-RIB output. It is calculated as: AUCtot (micromolar[µM]*h) = AUC24avg(RIB)(ng*h/mL)/847.016 (g/mole) + AUC24avg(25-O-Desacetyl-RIB)(ng*h/mL)/804.979(g/mole). The 300 mg RIB arm represents an extrapolation from the 150 mg RIB group. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

InterventionµM*h (Geometric Mean)
RIB 150 mg Once Daily (QD)2.00
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly4.38

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Tmax of RTV

Tmax was derived from the plasma concentration versus time for RTV and was recorded directly from experimental observations for each treatment period. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

InterventionHour (Median)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly4.00

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Time to Reach Maximum Observed Plasma Concentration (Tmax) of ATV

Tmax was derived from the plasma concentration versus time for ATV and was recorded directly from experimental observations for each treatment period. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

InterventionHour (Median)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly2.00

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T-half of RTV

T-half was obtained directly from the concentration-time data. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

InterventionHour (Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly4.45

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Number of Participants With Identified Electrocardiogram (ECG) Abnormalities

ECG abnormalities were defined as findings that are clinically meaningful as judged by the investigator. A 12-lead ECG was recorded at least 5 minutes after the participant had been lying down and all ECG recordings were evaluated by the investigator. Abnormalities, if present at any study time point, were listed. (NCT00646776)
Timeframe: Pre-dose on Day -1 and study discharge.

InterventionParticipants (Number)
RIB 150 mg Once Daily (QD)0
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly3

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Number of Participants With Clinically Significant Vital Signs or Physical Examination Findings

Vital signs assessments and physical examination were conducted throughout the study. Vital signs assessments included body temperature, respiratory rate, blood pressure (systolic and diastolic), and heart rate. Physical examination included a neurological examination (if ocular signs or symptoms occurred, a reflex to slit lamp exam was performed by an ophthalmologist). The investigator used his/her clinical judgment to decide whether or not abnormalities in vital signs or physical examination were clinically meaningful. (NCT00646776)
Timeframe: Vital signs:screening, prior to dosing on Day 1, Day 7, study discharge. Physical examination:screening, Day -1, Day 7, study discharge

InterventionParticipants (Number)
RIB 150 mg Once Daily (QD)0
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly0

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Maximum Plasma Concentration (Cmax) of RIB

Cmax was derived from plasma concentration versus time for RIB and was recorded directly from experimental observations for each treatment period. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
RIB 150 mg Once Daily (QD)159.0
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly395.6

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Number of Participants With MAs in Serum Chemistry: Glucose (Fasting Serum), Albumin, Creatine Kinase, Uric Acid, Lactate Dehydrogenase (LDH)

MAs=laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following serum chemistry MA definitions specify MA criteria. Glucose (fasting serum): <0.8 x LLN or >1.5 ULN (if pre-Rx ULN. If pre-Rx >ULN, then >2.0 x pre-Rx or 1.5 x ULN (if pre-Rx >ULN, then >1.5 x pre-Rx). Uric acid: >1.2 x ULN (if pre-Rx >ULN, then >1.25 x pre-Rx). LDH: >1.25 x ULN (if pre-Rx >ULN, then >1.5 x pre-Rx). (NCT00646776)
Timeframe: Pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14, 20 and 26 for RIB 150 mg QD; and pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14 and 18 for ATV/RTV 300/100 mg QD + RIB 150 mg twice weekly.

,
InterventionParticipants (Number)
Glucose (Fasting Serum)AlbuminCreatine KinaseUric AcidLDH
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly00000
RIB 150 mg Once Daily (QD)00000

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Cmin of RTV

Cmin was derived from the plasma concentration versus time for RTV. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly40.54

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Cmin of ATV

Cmin was derived from the plasma concentration versus time for ATV. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly920.69

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Cmin of 25-O-Desacetyl-RIB

Cmin was derived from plasma concentration versus time for 25-O-Desacetyl-RIB. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
RIB 150 mg Once Daily (QD)2.79
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly31.97

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Cmax of RTV

Cmax was derived from the plasma concentration versus time for RTV and was recorded directly from experimental observations for each treatment period. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 4, 8, 11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly1466

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Minimum Plasma Concentration (Cmin) of RIB

Cmin was derived from plasma concentration versus time for RIB. (NCT00646776)
Timeframe: Pre-dose (0h) on Days 6, 8, 10, and 11, and post-dose (1h,2h,3h,4h,6h,8h,12h) on Day 10 for RIB 150 mg QD; and pre-dose (0h) on Days 4, 8,11 to 18 and post-dose (1h,2h,3h,4h,6h,8h,12h) on Days 11 and 15 for ATV/RTV + RIB.

Interventionng/mL (Geometric Mean)
RIB 150 mg Once Daily (QD)28.89
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly40.49

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Number of Participants With MAs in Urinalysis

MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following definitions specify the criteria for MAs. Protein, glucose and blood: >=2+ (or, if pre-treatment value >=1+, then >= 2 x pre-treatment value). (NCT00646776)
Timeframe: Pre-dose on Day -1, Day 7 and discharge.

,
InterventionParticipants (Number)
ProteinGlucoseBlood
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly101
RIB 150 mg Once Daily (QD)000

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Number of Participants With MAs in Serum Chemistry: Chloride (Serum), Calcium (Total), Protein (Total), Bicarbonate, Phosphorous (Inorganic)

MAs=laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following serum chemistry MA definitions specify MA criteria. Chloride (serum), calcium (total), protein (total):<0.9xLLN or >1.1xULN (if pre-Rx ULN. If pre-Rx >ULN, then >1.1xpre-Rx or 1.2xULN (if pre-Rx value ULN. If pre-Rx >ULN, then >1.2xpre-Rx value or 1.25xULN (if pre-Rx ULN, then >1.25x re-Rx or NCT00646776)
Timeframe: Pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14, 20 and 26 for RIB 150 mg QD; and pre-dose on Day -1 and post-dose on Days 3, 7, 11, 14 and 18 for ATV/RTV 300/100 mg QD + RIB 150 mg twice weekly.

,
InterventionParticipants (Number)
Chloride (serum)Calcium (total)Protein (total)BicarbonatePhosphorous (inorganic)
ATV/RTV 300/100 mg QD+RIB 150 mg Twice Weekly00000
RIB 150 mg Once Daily (QD)00000

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Clinical Efficacy Rate by Age

"Clinical effectiveness rate, which was defined as the percentage of participants who achieved clinical effectiveness over the total number of assessable effectiveness analysis population, was presented. Clinical effectiveness of Mycobutin was assessed as effective, ineffective, or unassessable by the physician/investigator. Overall effectiveness of Mycobutin was determined by the physician/investigator based on clinical symptoms, laboratory values, and other examinations such as bacterial values. Participants achieved clinical effectiveness by age were counted to assess whether they contribute to the clinical effectiveness." (NCT00810407)
Timeframe: 1 year

InterventionPercentage of Participants (Number)
˂15 years≥15 and <65 years≥65 yearsUnknown
Mycobutin (Rifabutin)0.071.857.150

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Clinical Efficacy Rate by Diagnosis

"Clinical effectiveness rate, which was defined as the percentage of participants who achieved clinical effectiveness over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Clinical effectiveness of Mycobutin was assessed as effective, ineffective, or unassessable by the physician/investigator. Overall effectiveness of Mycobutin was determined by the physician/investigator based on clinical symptoms, laboratory values, and other examinations such as bacterial values. Participants achieved clinical effectiveness by diagnosis were counted to assess whether they contribute to the clinical effectiveness." (NCT00810407)
Timeframe: 1 year

InterventionPercentage of Participants (Number)
TuberculosisMycobacterium Avium Complex (MAC)Non-tuberculous Mycobacteria Other Than MACCoinfectionOthers
Mycobutin (Rifabutin)82.353.958.3100.00.0

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Clinical Efficacy Rate by Gender

"Clinical effectiveness rate, which was defined as the percentage of participants who achieved clinical effectiveness over the total number of assessable effectiveness analysis population, was presented. Clinical effectiveness of Mycobutin was assessed as effective, ineffective, or unassessable by the physician/investigator. Overall effectiveness of Mycobutin was determined by the physician/investigator based on clinical symptoms, laboratory values, and other examinations such as bacterial values. Participants achieved clinical effectiveness by gender were counted to assess whether they contribute to the clinical effectiveness." (NCT00810407)
Timeframe: 1 year

InterventionPercentage of Participants (Number)
MaleFemale
Mycobutin (Rifabutin)71.155.7

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Clinical Efficacy Rate

"Clinical effectiveness rate, which was defined as the percentage of participants who achieved clinical effectiveness over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Clinical effectiveness of Mycobutin was assessed as effective, ineffective, or unassessable by the physician/investigator. Overall effectiveness of Mycobutin was determined by the physician/investigator based on clinical symptoms, laboratory values, and other examinations such as bacterial values." (NCT00810407)
Timeframe: 1 year

InterventionPercentage of Participants (Number)
Mycobutin (Rifabutin)62.7

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Number of Patients With Adverse Drug Reactions in This Surveillance

An adverse drug reaction (ADR) was any untoward medical occurrence attributed to MYCOBUTIN Capsules in a participant who received MYCOBUTIN Capsules. A serious ADR was an ADR resulting in any of the following outcomes or deemed significant for any other reason: death; life-threatening experience (immediate risk of dying); initial or prolonged inpatient hospitalization; persistent or significant disability/incapacity; congenital anomaly. Relatedness to MYCOBUTIN Capsules was assessed by the physician. (NCT00810446)
Timeframe: 6.5 years at maximum (therapeutic) and 8.5 years at maximum (preventive)

InterventionParticipants (Number)
ADRSerious ADR
MYCOBUTIN Capsules (Rifabutin)167

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Number of Participants With Adverse Drug Reactions by Gender

An adverse drug reaction (ADR) was any untoward medical occurrence attributed to MYCOBUTIN Capsules in a participant who received MYCOBUTIN Capsules. Relatedness to MYCOBUTIN Capsules was assessed by the physician. Participants with ADRs were counted by gender to access whether it was a risk factor for the ADR. (NCT00810446)
Timeframe: 6.5 years at maximum (therapeutic) and 8.5 years at maximum (preventive)

InterventionParticipants (Number)
MaleFemale
MYCOBUTIN Capsules (Rifabutin)160

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Clinical Response Rate (Therapeutic)

Clinical response rate was defined as the percentage of participants who achieved clinical response over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Clinical efficacy of MYCOBUTIN Capsules were determined by the investigator at the final observation point based on clinical symptoms and examinations, according to the following categories: (1) markedly improved, (2) improved, (3) slightly improved (4) unchanged, (5) aggravated, or (6) indeterminable. The participants assessed as (1) markedly improved and (2) improved were considered to have achieved clinical response. (NCT00810446)
Timeframe: 6.5 years (at maximum)

InterventionPercentage of Participants (Number)
MYCOBUTIN Capsules (Rifabutin)80.6

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The Number of Participants Who Experienced an Adverse Drug Reaction Not Expected From the Local Product Document (Unknown Adverse Drug Reactions)

An adverse drug reaction (ADR) was any untoward medical occurrence attributed to MYCOBUTIN Capsules in a participant who received MYCOBUTIN Capsules. Relatedness to MYCOBUTIN Capsules was assessed by the physician. Expectedness of the adverse drug reaction was determined according to the Japanese package insert. (NCT00810446)
Timeframe: 6.5 years at maximum (therapeutic) and 8.5 years at maximum (preventive)

InterventionParticipants (Number)
MYCOBUTIN Capsules (Rifabutin)7

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Clinical Response Rate (Therapeutic) by Age

Clinical response rate was defined as the percentage of participants who achieved clinical response over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Clinical efficacy of MYCOBUTIN Capsules were determined by the investigator at the final observation point based on clinical symptoms and examinations, according to the following categories: (1) markedly improved, (2) improved, (3) slightly improved (4) unchanged, (5) aggravated, or (6) indeterminable. The participants assessed as (1) markedly improved and (2) improved were considered to have achieved clinical response. Participants who achieved clinical response by age were counted to assess whether it contributed to clinical response. (NCT00810446)
Timeframe: 6.5 years (at maximum)

InterventionPercentage of Participants (Number)
≥15 and <65 years≥65 years
MYCOBUTIN Capsules (Rifabutin)80.0100.0

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Number of Participants With Adverse Drug Reactions by Diagnosis

An adverse drug reaction (ADR) was any untoward medical occurrence attributed to MYCOBUTIN Capsules in a participant who received MYCOBUTIN Capsules. Relatedness to MYCOBUTIN Capsules was assessed by the physician. Participants with ADRs were counted by diagnosis to assess whether it was a risk factor for the ADR. (NCT00810446)
Timeframe: 6.5 years at maximum (therapeutic) and 8.5 years at maximum (preventive)

InterventionParticipants (Number)
MAC (Therapeutic)TuberculosisNTM Infections Other Than MACMAC (Therapeutic) and NTM Infection Other Than MACOthers
MYCOBUTIN Capsules (Rifabutin)78010

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Clinical Response Rate (Therapeutic) by Gender

Clinical response rate was defined as the percentage of participants who achieved clinical response over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Clinical efficacy of MYCOBUTIN Capsules were determined by the investigator at the final observation point based on clinical symptoms and examinations, according to the following categories: (1) markedly improved, (2) improved, (3) slightly improved (4) unchanged, (5) aggravated, or (6) indeterminable. The participants assessed as (1) markedly improved and (2) improved were considered to have achieved clinical response. Participants who achieved clinical response by gender were counted to assess whether it contributed to clinical response. (NCT00810446)
Timeframe: 6.5 years (at maximum)

InterventionPercentage of Participants (Number)
MaleFemale
MYCOBUTIN Capsules (Rifabutin)80.0100.0

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Number of Participants With Adverse Drug Reactions by Age

An adverse drug reaction (ADR) was any untoward medical occurrence attributed to MYCOBUTIN Capsules in a participant who received MYCOBUTIN Capsules. Relatedness to MYCOBUTIN Capsules was assessed by the physician. Participants with ADRs were counted by age to assess whether it was a risk factor for the ADR. (NCT00810446)
Timeframe: 6.5 years at maximum (therapeutic) and 8.5 years at maximum (preventive)

InterventionParticipants (Number)
≥15 and <65 years≥65 years
MYCOBUTIN Capsules (Rifabutin)160

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Clinical Response Rate (Therapeutic) by Diagnosis

Clinical response rate was defined as the percentage of participants who achieved clinical response over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Clinical efficacy of MYCOBUTIN Capsules were determined by the investigator at the final observation point based on clinical symptoms and examinations, according to the following categories: (1) markedly improved, (2) improved, (3) slightly improved (4) unchanged, (5) aggravated, or (6) indeterminable. The participants assessed as (1) markedly improved and (2) improved were considered to have achieved clinical response. Participants who achieved clinical response by diagnosis were counted to assess whether it contributed to clinical response. (NCT00810446)
Timeframe: 6.5 years (at maximum)

InterventionPercentage of Participants (Number)
MAC (Therapeutic)TuberculosisNTM Infections Other Than MACMAC (Therapeutic) and NTM Infection Other Than MACOthers
MYCOBUTIN Capsules (Rifabutin)78.389.757.150.0100.0

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Eradication of S. Aureus Colonization

Eradication was measured by performing cultures for S aureus at the nose, throat, and groin (NCT00869518)
Timeframe: 30 days following completion of treatment

Interventionparticipants (Number)
Rifabutin0
Placebo0

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Eradication of S. Aureus Colonization

Eradication was measured by performing cultures for S aureus at the nose, throat, and groin (NCT00869518)
Timeframe: 7 days following completion of treatment

Interventionparticipants (Number)
Rifabutin3
Placebo1

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Recurrent Skin and Skin Structure Infections (SSTI)

recurrent SSTI was by self-report and exam, followed until positive colonization (NCT00869518)
Timeframe: up to 30 days following completion of treatment

Interventionparticipants (Number)
Rifabutin0
Placebo0

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Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one TB drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through to the discontinuation of the last TB drug

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT13.0

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CD4 Count Change From Baseline to Week 24

The difference in CD4 count from baseline to week 24 was calculated as the CD4 count at week 24 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 24 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT20
B: Double-dose LPV/r w/RIF56
C: Standard-Dose LPV/r + RAL w/RBT13

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CD4 Count Change From Baseline to Week 48

The difference in CD4 count from baseline to week 48 was calculated as the CD4 count at week 48 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 48 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT99
B: Double-dose LPV/r w/RIF119
C: Standard-Dose LPV/r + RAL w/RBT74

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CD4 Count Change From Baseline to Week 72

The difference in CD4 count from baseline to week 72 was calculated as the CD4 count at week 72 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 72 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT126
B: Double-dose LPV/r w/RIF212
C: Standard-Dose LPV/r + RAL w/RBT54

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CD4 Count Change From Baseline to Week 8

The difference in CD4 count from baseline to week 8 was calculated as the CD4 count at week 8 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 8 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF26
C: Standard-Dose LPV/r + RAL w/RBT37

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Cumulative Probability of HIV Virologic Failure at Week 72

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. The percent of participants with HIV virologic failure at week 72 was calculated using a Kaplan-Meier estimator with an associated standard error. The confidence interval was calculated using a log-log transformation. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventioncumulative events per 100 participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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LPV AUC in Participants Enrolled in Arms A, B, and C

Describe LPV plasma PK characteristics (area under the curve [AUC] between 0 and 12 hours) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT159796
B: Double-dose LPV/r w/RIF161772
C: Standard-Dose LPV/r + RAL w/RBT149247

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Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) laboratory abnormality were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT6
B: Double-dose LPV/r w/RIF3
C: Standard-Dose LPV/r + RAL w/RBT5

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Number of Participants Reporting a Grade 3 or 4 Sign or Symptom

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) sign or symptom were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF5
C: Standard-Dose LPV/r + RAL w/RBT5

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Number of Participants Who Experienced MTB IRIS

The number of participants who experienced MTB immune reconstitution inflammatory syndrome (IRIS) was summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT1
B: Double-dose LPV/r w/RIF2
C: Standard-Dose LPV/r + RAL w/RBT3

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Percent of Participants Who Died

The percent of participants who died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF4.7
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced a New AIDS-defining Illness

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Percent of Participants Who Experienced a New AIDS-defining Illness or Died

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness or died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced HIV Virologic Failure

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. Participants who were missing data due to being lost-to-follow-up or dead were coded as virologic failures. The percent of participants who experienced HIV virologic failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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Percent of Participants Who Experienced Sputum Conversion at Week 8.

Sputum conversion was defined as culture MTB-negative at week 8 or AFB smear negative at week 8 (and culture contaminated or missing at week 8); there were no Xpert MTB/RIF results at week 8. The percent of participants experienced sputum conversion at week 8 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 8 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT87.5
B: Double-dose LPV/r w/RIF81.8
C: Standard-Dose LPV/r + RAL w/RBT70.0

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Percent of Participants Who Experienced TB Relapse/Recurrence

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The percent of participants who experienced TB relapse/recurrence was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The drug resistance was determined based on phenotypic methods. The percent of participants who experienced TB relapse/recurrence and who had TB drug resistance was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionparticipants (Number)
B: Double-dose LPV/r w/RIF0
C: Standard-Dose LPV/r + RAL w/RBT0

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Percent of Participants Who Experienced TB Treatment Failure

TB treatment failure was defined as having a MTB-positive culture after 16 weeks of TB treatment for a participant who was documented to be taking TB medications. The percent of participants who experienced TB treatment failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After 16 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF0.0
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one HIV drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF16.7
C: Standard-Dose LPV/r + RAL w/RBT21.7

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Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.

The percent of participants whose HIV viral load was less than 400 copies/mL at week 48 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. Participants who were lost-to-follow-up or dead by week 48 or had missing results at week 48 were coded as having HIV viral load greater than 400 copies/mL. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT58.3
B: Double-dose LPV/r w/RIF66.7
C: Standard-Dose LPV/r + RAL w/RBT60.9

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Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48

The percent of participants whose HIV viral load was less than 50 copies/mL at week 48 was calculated with an associated standard error. Participants who were lost-to-follow-up or dead by week 48 or had missing RNA at week 48 were coded as having HIV viral load greater than 50 copies/mL. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT45.8
B: Double-dose LPV/r w/RIF54.2
C: Standard-Dose LPV/r + RAL w/RBT56.5

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RAL AUC in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
C: Standard-Dose LPV/r + RAL w/RBT11338

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RBT AUC in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT7374
C: Standard-Dose LPV/r + RAL w/RBT5516

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LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C

Describe LPV plasma pharmacokinetic (PK) characteristics (maximum concentration [Cmax] and minimum concentration [Cmin]) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

,,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT185319920
B: Double-dose LPV/r w/RIF181388033
C: Standard-Dose LPV/r + RAL w/RBT168028548

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RAL Cmax and Cmin in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
C: Standard-Dose LPV/r + RAL w/RBT2830166

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RBT Cmax and Cmin in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT461161
C: Standard-Dose LPV/r + RAL w/RBT349115

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Safety/Tolerability of the Treatments

description and frequency of adverse events for all participants during the study. (NCT01894776)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Maraviroc72220849Maraviroc + Rifabutin72220849
Number of Participants with Adverse EventsNumber of Participants without Adverse Events
Maraviroc6
Maraviroc8
Maraviroc7

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Maraviroc and Rifabutin C12/C24/Cmax PK Concentrations in Plasma.

Maraviroc + Rifabutin pharmacokinetics: Maraviroc only Cmax (μg/L), Maraviroc only C12 (μg/L), Maraviroc + Rifabutin Cmax (μg/L), Maraviroc + Rifabutin C12 (μg/L), Rifabutin Cmax (μg/L), Rifabutin C24 (μg/L), 25-O-desacetyl rifabutin Cmax (μg/L), 25-O-desacetyl rifabutin C24 (μg/L). (NCT01894776)
Timeframe: Maraviroc: 0, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10 and 12 hour. Rifabutin: 0, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 24 hour..

Interventionμg/L (Geometric Mean)
Maraviroc only Cmax (μg/L)Maraviroc only C12 (μg/L)Maraviroc + Rifabutin Cmax (μg/L)Maraviroc + Rifabutin C12 (μg/L)Rifabutin Cmax (μg/L)Rifabutin C24 (μg/L)25-O-desacetyl rifabutin Cmax (μg/L)25-O-desacetyl rifabutin C24 (μg/L)
Maraviroc304.623.3239.816.3542.271.242.35.5

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Pharmacokinetics of Maraviroc and Rifabutin AUC 0-12/24

Maraviroc pharmacokinetics: Maraviroc only AUC (h*μg/L), Maraviroc + Rifabutin AUC (h*μg/L), Rifabutin AUC (h*μg/L), 25-O-desacetyl rifabutin AUC (h*μg/L). (NCT01894776)
Timeframe: Maraviroc: 0, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10 and 12 hour. Rifabutin: 0, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 24 hour..

Interventionh*μg/L (Geometric Mean)
Maraviroc only AUC (h*μg/L)Maraviroc + Rifabutin AUC (h*μg/L)Rifabutin AUC (h*μg/L)25-O-desacetyl rifabutin AUC (h*μg/L)
Maraviroc1026.2847.04221.9331.9

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Steady State Pharmacokinetics (PK) (AUC) of PA-824 When Given With Rifampin or Rifabutin

AUC of PA-824 when given with either rifampicin or rifabutin to determine steady state Pharmacokinetics (PK) of PA-824. (NCT02256696)
Timeframe: pre-dose and 1, 2, 5, 8, and 24 hours post-dose on Day 14

Interventionmg*h/L (Mean)
Arm 131.91
Arm 259.05

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Relationship Between PA-824 Exposure (AUC) and Rate of Change in Time to Positivity (TTP) Over 12 Weeks

Relationship between PA-824 exposure (AUC) and rate of change in TTP over 12 weeks, using non-linear mixed effects modeling. The data is reported as percentage increase in TTP per 10 unit increase in PA-824 AUC (% increase/10 unit increase PA-824 AUC). (NCT02256696)
Timeframe: 12 weeks

Intervention% increase/10 unit increase PA-824 AUC (Number)
Arms 1 and 2 (Pretomanid-containing Arms)9.4

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PK (Cmax) of PA-824 at 200 mg Once Daily With Rifampin or Rifabutin-containing Treatment

The Pharmacokinetic results (Cmax) of the study drug when given with a rifampin or a rifabutin. (NCT02256696)
Timeframe: pre-dose and 1, 2, 5, 8, and 24 hours post-dose on Day 14

Interventionmg/L (Mean)
Arm 12.03
Arm 22.69

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Number of Participants With Permanent Discontinuation of Assigned Study Regimen

If it is in the best interest of a participant to stop the study regimen for any reason (NCT02256696)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm 12
Arm 27
Arm 30

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Number of Participants With Grade 3 or Higher Adverse Events

Any Grade 3 event according to the Division of AIDS (DAIDS) toxicity table (NCT02256696)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm 13
Arm 26
Arm 32

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Time to Sputum Culture Conversion on Liquid Medium

The time (days) it takes for the sputum to convert from positive to negative. (NCT02256696)
Timeframe: 12 weeks

,,
Interventiondays (Median)
Time to culture conversion (mITT)Time to culture conversion (per protocol)
Arm 14242
Arm 22828
Arm 35656

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Percentage of Participants With Sputum Culture Conversion by 8 Weeks of Treatment

Percentage of participants whose sputum converts from positive to negative at Week 8 time point, on solid and liquid media. (NCT02256696)
Timeframe: 8 weeks

,,
Interventionpercentage of participants (Number)
Liquid mediaSolid media
Arm 17998
Arm 289100
Arm 36996

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Time to Culture Conversion on Solid Medium

The time (days) it takes for the sputum to convert form positive to negative on solid medium (NCT02256696)
Timeframe: 12 weeks

,,
Interventiondays (Median)
Time to conversion on solid culture (mITT)Time to conversion on solid culture (per protocol)
Arm 12828
Arm 22121
Arm 34242

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Number of Weeks the Patients Are in Response.

Duration of response is defined as the number of weeks the subject is in a state of response (a reduction from baseline of ≥ 100 in CDAI score). It is calculated as the first date following response at which the reduction from baseline in CDAI is <100 minus the date of first response, plus 1 day, divided by 7. Subjects who experienced response and continued to be in response at the time of their last CDAI assessment are censored at the date of their last CDAI assessment. (NCT03009396)
Timeframe: Baseline through week 52

InterventionWeeks (Median)
RHB-104 From ACTIVE Arm of RHB-104-0129.4
RHB-104 From PLACEBO Arm of RHB-104-0145.0

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Number of Weeks to Achieve Response

[Date of first observed response (a reduction from baseline of ≥ 100 in CDAI score) - Date of first dose or date of randomization if not dosed + 1] / 7 Days. Subjects who never experienced response during the study are censored at the date of their last CDAI assessment. (NCT03009396)
Timeframe: Baseline through week 52

InterventionWeeks (Median)
RHB-104 From ACTIVE Arm of RHB-104-01NA
RHB-104 From PLACEBO Arm of RHB-104-0126.1

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Response at Week 16

Reduction of the total Crohn's Disease Activity Index (CDAI) score by a minimum of 100 points Lower CDAI scores indicate a better outcome. (NCT03009396)
Timeframe: Week 16

InterventionParticipants (Count of Participants)
RHB-104 From ACTIVE Arm of RHB-104-014
RHB-104 From PLACEBO Arm of RHB-104-0114

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The Number of Weeks for Patients to Achieve Remission

[Date of first observed remission (CDAI less than 150) - date of first dose, or date of randomization if not dosed, plus 1] / 7 days. Subject who never experience remission during the study are censored at the time of their last CDAI assessment. (NCT03009396)
Timeframe: Baseline through week 52

Interventionweeks (Median)
RHB-104 From ACTIVE Arm of RHB-104-01NA
RHB-104 From PLACEBO Arm of RHB-104-0125.1

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Durable Remission Week 16 Through Week 52

When a subject is in remission with a maximum CDAI score of 149 at every visit from week 16 through and including week 52. (NCT03009396)
Timeframe: Week 16 through week 52

InterventionParticipants (Count of Participants)
RHB-104 From ACTIVE Arm of RHB-104-011
RHB-104 From PLACEBO Arm of RHB-104-017

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Increase in Milliseconds (ms) QT Wave

The increase in the number of milliseconds change-from-baseline to week 52 in QTcF (Fridericia's Correction Formula of QT wave interval) (based on cardiac safety report). (NCT03009396)
Timeframe: week 52

Interventionms (Least Squares Mean)
RHB-104 From ACTIVE Arm of RHB-104-0123.9
RHB-104 From PLACEBO Arm of RHB-104-0127.6

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Number of Patients in Remission at Week 16

"The number of patients who achieved a reduction of the total Crohn's Disease Activity Index (CDAI) score to less than 150 points.~Lower CDAI scores indicate a better outcome." (NCT03009396)
Timeframe: Week 16

InterventionParticipants (Count of Participants)
RHB-104 From ACTIVE Arm of RHB-104-013
RHB-104 From PLACEBO Arm of RHB-104-0114

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Number of Weeks the Patients Are in Remission

Duration of remission is defined as the number of weeks the subject is in remission (CDAI score < 150). It is calculated as the first date following remission at which CDAI is ≥150 minus the date of first remission, plus 1 day, divided by 7. Subjects who experienced remission and continued to be in remission at the time of their last CDAI assessment are censored at the date of their last CDAI assessment. (NCT03009396)
Timeframe: Baseline through week 52

Interventionweeks (Median)
RHB-104 From ACTIVE Arm of RHB-104-0111.7
RHB-104 From PLACEBO Arm of RHB-104-0145.0

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Assessment of Plasma CAB PK Parameter: Maximum Observed Concentration (Cmax)

Blood samples for PK analysis of CAB were collected at pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28. Cmax was determined directly from the concentration-time data. Comparisons were made for the repeated dose PK parameters of CAB when given alone in Period 1 and when co-administered with steady-state RBT in Period 2. (NCT03149848)
Timeframe: Pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28

InterventionMicrograms per milliliter (Geometric Mean)
CAB 30 mg6.356
RBT 300 mg + CAB 30 mg5.246

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Assessment of Plasma CAB PK Parameter: The Apparent Oral Clearance (CL/F)

Blood samples for PK analysis of CAB were collected at pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28. CL/F was calculated as CL/F =Dose/AUC(0 to tau). (NCT03149848)
Timeframe: Pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28

InterventionLiters per hour (Geometric Mean)
CAB 30 mg0.289
RBT 300 mg + CAB 30 mg0.367

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Assessment of Plasma CAB PK Parameter: Time of Occurrence of Cmax (Tmax)

Blood samples for PK analysis of CAB were collected at pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28. Tmax was determined directly from the concentration-time data. (NCT03149848)
Timeframe: Pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28

InterventionHours (Median)
CAB 30 mg3.000
RBT 300 mg + CAB 30 mg2.500

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Number of Participants With Abnormal Electrocardiogram (ECG) Findings

ECG measurements was performed with the participant in a semi-supine position having rested in this position for at least 10 minutes beforehand. Data has been presented for Period 1, Day 14 pre-dose which showed abnormal- not clinically significant ECG finding. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day 1, 14, 21, 28 and follow-up (10 to 14 days after last dose)

InterventionParticipants (Count of Participants)
CAB 30 mg1
RBT 300 mg + CAB 30 mg0

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Number of Participants With Abnormal Urinalysis Result

Samples for urinalysis assessment was collected at Day -1, Day 13, Day 21, Day 27 and during follow-up period (10 to 14 daya after last dose). Data for participants with abnormal urinalysis results has been presented. (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionParticipants (Count of Participants)
CAB 30 mg0
RBT 300 mg + CAB 30 mg0

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Assessment of Clinical Chemistry Parameters: Albumin and Protein

Samples for clinical chemistry assessment were collected for Albumin and Protein. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionGrams per Liter (Mean)
Albumin, Day -1, n=15Albumin, On-treatment, Period 1 Day 13, n=14Albumin, On-treatment, Period 2 Day 21, n=13Albumin, On-treatment, Period 2 Day 27, n=12Albumin, Follow-up, Period 1 Day 13, n=1Albumin, Follow-up, Period 2 Day 21, n=1Albumin, Follow-up, Period 2 Day 27, n=1Albumin, Follow-up, n=15Protein, Day -1, n=15Protein, On-treatment, Period 1 Day 13, n=14Protein, On-treatment, Period 2 Day 21, n=13Protein, On-treatment, Period 2 Day 27, n=12Protein, Follow-up, Period 1 Day 13, n=1Protein, Follow-up, Period 2 Day 21, n=1Protein, Follow-up, Period 2 Day 27, n=1Protein, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg45.244.243.443.738.044.042.042.767.967.365.165.860.063.070.063.7

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Assessment of Clinical Chemistry Parameters: Alkaline Phosphatase (ALP), Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), Creatine Kinase (CK) and Gamma Glutamyl Transferase (GGT)

Samples for clinical chemistry assessment were collected for ALP, AST, ALT, CK and GGT. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionInternational units per Liter (Mean)
ALP, Day -1, n=15ALP, On-treatment, Period 1 Day 13, n=14ALP, On-treatment, Period 2 Day 21, n=13ALP, On-treatment, Period 2 Day 27, n=12ALP, Follow-up, Period 1 Day 13, n=1ALP, Follow-up, Period 2 Day 21, n=1ALP, Follow-up, Period 2 Day 27, n=1ALP, Follow-up, n=15ALT, Day -1, n=15ALT, On-treatment, Period 1 Day 13, n=14ALT, On-treatment, Period 2 Day 21, n=13ALT, On-treatment, Period 2 Day 27, n=12ALT, Follow-up, Period 1 Day 13, n=1ALT, Follow-up, Period 2 Day 21, n=1ALT, Follow-up, Period 2 Day 27, n=1ALT, Follow-up, n=15AST, Day -1, n=15AST, On-treatment, Period 1 Day 13, n=14AST, On-treatment, Period 2 Day 21, n=13AST, On-treatment, Period 2 Day 27, n=12AST, Follow-up, Period 1 Day 13, n=1AST, Follow-up, Period 2 Day 21, n=1AST, Follow-up, Period 2 Day 27, n=1AST, Follow-up, n=15CK, Day -1, n=15CK, On-treatment, Period 1 Day 13, n=14CK, On-treatment, Period 2 Day 21, n=13CK, On-treatment, Period 2 Day 27, n=12CK, Follow-up, Period 1 Day 13, n=1CK, Follow-up, Period 2 Day 21, n=1CK, Follow-up, Period 2 Day 27, n=1CK, Follow-up, n=15GGT, Day -1, n=15GGT, On-treatment, Period 1 Day 13, n=14GGT, On-treatment, Period 2 Day 21, n=13GGT, On-treatment, Period 2 Day 27, n=12GGT, Follow-up, Period 1 Day 13, n=1GGT, Follow-up, Period 2 Day 21, n=1GGT, Follow-up, Period 2 Day 27, n=1GGT, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg62.760.160.759.951.061.056.060.723.525.530.230.8155.039.034.037.318.520.720.923.383.026.037.024.9133.6227.1104.288.71278.0177.0164.0144.325.522.626.828.117.036.082.036.1

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Assessment of Clinical Chemistry Parameters: Direct Bilirubin (DB), Bilirubin and Creatinine

Samples for clinical chemistry assessment were collected for DB, bilirubin and creatinine. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionMicromoles per Liter (Mean)
DB, Day -1, n=15DB, On-treatment, Period 1 Day 13, n=14DB, On-treatment, Period 2 Day 21, n=13DB, On-treatment, Period 2 Day 27, n=12DB, Follow-up, Period 1 Day 13, n=1DB, Follow-up, Period 2 Day 21, n=1DB, Follow-up, Period 2 Day 27, n=1DB, Follow-up, n=15Bilirubin, Day -1, n=15Bilirubin, On-treatment, Period 1 Day 13, n=14Bilirubin, On-treatment, Period 2 Day 21, n=13Bilirubin, On-treatment, Period 2 Day 27, n=12Bilirubin, Follow-up, Period 1 Day 13, n=1Bilirubin, Follow-up, Period 2 Day 21, n=1Bilirubin, Follow-up, Period 2 Day 27, n=1Bilirubin, Follow-up, n=15Creatinine, Day -1, n=15Creatinine, On-treatment, Period 1 Day 13, n=14Creatinine, On-treatment, Period 2 Day 21, n=13Creatinine, On-treatment, Period 2 Day 27, n=12Creatinine, Follow-up, Period 1 Day 13, n=1Creatinine, Follow-up, Period 2 Day 21, n=1Creatinine, Follow-up, Period 2 Day 27, n=1Creatinine, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg3.53.52.42.24.01.02.02.99.810.16.65.310.03.05.07.983.185.988.483.864.071.091.080.7

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Assessment of Hematology Parameter: Eryrocyte Mean Corpuscular Hemoglobin

Blood samples for hematology assessment was collected for Eryrocyte Mean Corpuscular Hemoglobin. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionPicograms (Mean)
Day -1, n=15On-treatment, Period 1 Day 13, n=14On-treatment, Period 2 Day 21, n=13On-treatment, Period 2 Day 27, n=12Follow-up, Period 1 Day 13, n=1Follow-up, Period 2 Day 21, n=1Follow-up, Period 2 Day 27, n=1Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg29.7729.5430.1329.7429.3027.8030.9029.49

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Assessment of Hematology Parameter: Erythrocye Mean Corpuscular Volume

Blood samples for hematology assessment was collected for Erythrocyte Mean Corpuscular Volume. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionFemtoliters (Mean)
Day -1, n=15On-treatment, Period 1 Day 13, n=14On-treatment, Period 2 Day 21, n=13On-treatment, Period 2 Day 27, n=12Follow-up, Period 1 Day 13, n=1Follow-up, Period 2 Day 21, n=1Follow-up, Period 2 Day 27, n=1Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg84.6087.9485.3987.7388.2079.2087.1086.59

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Assessment of Hematology Parameter: Hemoglobin

Blood samples for hematology assessment was collected for Hemoglobin. NA indicate data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionGrams per Liter (Mean)
Day -1, n=15Period 1 Day 13, n=14Period 2 Day 21, n=13Period 2 Day 27, n=12Follow-up, Period 1 Day 13, n=1Follow-up, Period 2 Day 21, n=1Follow-up, Period 2 Day 27, n=1Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg144.7143.5146.4144.2137.0147.0146.0140.1

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Assessment of Hematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes

Blood samples for hematology assessment were collected for basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelets and leukocytes. NA indicate data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

Intervention10^9 cells/Liter (Mean)
Basophils, Day -1, n=15Basophils, On-treatment, Period 1 Day 13, n=14Basophils, On-treatment, Period 2 Day 21, n=13Basophils, On-treatment, Period 2 Day 27, n=12Basophils, Follow-up, Period 1 Day 13, n=1Basophils, Follow-up, Period 2 Day 21, n=1Basophils, Follow-up, Period 2 Day 27, n=1Basophils, Follow-up, n=15Eosinophils, On-treatment, Day -1, n=15Eosinophils, On-treatment, Period 1 Day 13, n=14Eosinophils, On-treatment, Period 2 Day 21, n=13Eosinophils, On-treatment, Period 2 Day 27, n=12Eosinophils, Follow-up, Period 1 Day 13, n=1Eosinophils, Follow-up, Period 2 Day 21, n=1Eosinophils, Follow-up, Period 2 Day 27, n=1Eosinophils, Follow-up, n=15Lymphocytes, Day -1, n=15Lymphocytes, On-treatment, Period 1 Day 13, n=14Lymphocytes, On-treatment, Period 2 Day 21, n=13Lymphocytes, On-treatment, Period 2 Day 27, n=12Lymphocytes, Follow-up, Period 1 Day 13, n=1Lymphocytes, Follow-up, Period 2 Day 21, n=1Lymphocytes, Follow-up, Period 2 Day 27, n=1Lymphocytes, Follow-up, n=15Monocytes, Day -1, n=15Monocytes, On-treatment, Period 1 Day 13, n=14Monocytes, On-treatment, Period 2 Day 21, n=13Monocytes, On-treatment, Period 2 Day 27, n=12Monocytes, Follow-up, Period 1 Day 13, n=1Monocytes, Follow-up, Period 2 Day 21, n=1Monocytes, Follow-up, Period 2 Day 27, n=1Monocytes, Follow-up, n=15Neutrophils, Day -1, n=15Neutrophils, On-treatment, Period 1 Day 13, n=14Neutrophils, On-treatment, Period 2 Day 21, n=13Neutrophils, On-treatment, Period 2 Day 21, n=12Neutrophils, Follow-up, Period 1 Day 13, n=1Neutrophils, Follow-up, Period 2 Day 21, n=1Neutrophils, Follow-up, Period 2 Day 27, n=1Neutrophils, Follow-up, n=15Platelets, Day -1, n=15Platelets, On-treatment, Period 1 Day 13, n=14Platelets, On-treatment, Period 2 Day 21, n=13Platelets, On-treatment, Period 2 Day 27, n=12Platelets, Follow-up, Period 1 Day 13, n=1Platelets, Follow-up, Period 2 Day 21, n=1Platelets, Follow-up, Period 2 Day 27, n=1Platelets, Follow-up, n=15Leukocytes, Day -1, n=15Leukocytes, On-treatment, Period 1 Day 13, n=14Leukocytes, On-treatment, Period 2 Day 21, n=13Leukocytes, On-treatment, Period 2 Day 27, n=12Leukocytes, Follow-up, Period 1 Day 13, n=1Leukocytes, Follow-up, Period 2 Day 21, n=1Leukocytes, Follow-up, Period 2 Day 27, n=1Leukocytes, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg0.0250.0310.0280.0180.0300.0100.0100.0230.2590.2850.3150.2190.3700.0100.1200.2732.5092.2242.0711.5511.2000.3100.4802.1400.5610.5480.6280.4880.3600.4800.7900.5454.2793.3062.8181.9792.3403.8303.9702.840234.7210.7214.5193.9206.0206.0169.0229.87.6336.3945.8594.2564.3004.6405.3705.822

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Assessment of Hematology Parameters: Erythrocytes and Reticulocytes

Blood samples for hematology assessment were collected for Erythrocytes and reticulocytes. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

Intervention10^12 cells/Liter (Mean)
Erythrocytes, Day -1, n=15Erythrocytes, On-treatment, Period 1 Day 13, n=14Erythrocytes, On-treatment, Period 2 Day 21, n=13Erythrocytes, On-treatment, Period 2 Day 27, n=12Erythrocytes, Follow-up, Period 1 Day 13, n=1Erythrocytes, Follow-up, Period 2 Day 21, n=1Erythrocytes, Follow-up, Period 2 Day 27, n=1Erythrocytes, Follow-up, n=15Reticulocytes, Day -1, n=15Reticulocytes, On-treatment, Period 1 Day 13, n=14Reticulocytes, On-treatment, Period 2 Day 21, n=13Reticulocytes, On-treatment, Period 2 Day 27, n=12Reticulocytes, Follow-up, Period 1 Day 13, n=1Reticulocytes, Follow-up, Period 2 Day 21, n=1Reticulocytes, Follow-up, Period 2 Day 27, n=1Reticulocytes, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg4.8704.8694.8684.8554.6805.2904.7304.7610.0430.0400.0400.0280.0640.0510.0140.049

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Assessment of Hematology Parameters: Erythrocytes Distribution Width (EDW)

Blood samples for hematology assessment was collected for EDW. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionPercentage of EDW (Mean)
Day -1, n=15On-treatment, Period 1 Day 13, n=14On-treatment, Period 2 Day 21, n=13On-treatment, Period 2 Day 27, n=12Follow-up, Period 1 Day 13, n=1Follow-up, Period 2 Day 21, n=1Follow-up, Period 2 Day 27, n=1Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg12.9113.1312.8912.9013.4013.6012.4012.90

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Assessment of Hematology Parameters: Hematocrit and Reticulocytes/Erythrocytes (R/E)

Blood samples for hematology assessment were collected for Hematocrit and R/E. NA indicate data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionProportion of red blood cells in blood (Mean)
Hematocrit, Day -1, n=15Hematocrit, On-treatment, Period 1 Day 13, n=14Hematocrit, On-treatment, Period 2 Day 21, n=13Hematocrit, On-treatment, Period 2 Day 27, n=12Hematocrit, Follow-up, Period 1 Day 13, n=1Hematocrit, Follow-up, Period 2 Day 21, n=1Hematocrit, Follow-up, Period 2 Day 27, n=1Hematocrit, Follow-up, n=15R/E, Day -1, n=15R/E, On-treatment, Period 1 Day 13, n=14R/E, On-treatment, Period 2 Day 21, n=13R/E, On-treatment, Period 2 Day 27, n=12R/E, Follow-up, Period 1 Day 13, n=1R/E, Follow-up, Period 2 Day 21, n=1R/E, Follow-up, Period 2 Day 27, n=1R/E, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg0.4110.4270.4150.4250.4130.4190.4120.4110.0080.0080.0080.0060.0130.0090.0030.010

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Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

Vital signs measurement was done in semi-supine position after 10 minutes rest and included SBP and DBP. Two blood pressure measurement were taken at pre-dose on Day 1, at least 1 minute apart. The mean value recorded at pre-dose was classified as Baseline. Single blood pressure was obtained at all other time points during the study. Change from Baseline was calculated by subtracting the post-dose value from the Baseline value. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Baseline to follow-up (10 to 14 days after last dose)

InterventionMillimeters of Mercury (Mean)
SBP, On-treatment, Period 1 Day 14, n=14SBP, On-treatment, Period 2 Day 21, n=13SBP, On-treatment, Period 2 Day 28, n=12SBP, Follow-up, Period 2 Day 21, n=1SBP, Follow-up, n=15DBP, On-treatment, Period 1 Day 14, n=14DBP, On-treatment, Period 2 Day 21, n=13DBP, On-treatment, Period 2 Day 28, n=12DBP, Follow-up, Period 2 Day 21, n=1DBP, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg-2.51.50.517.03.70.82.0-1.69.53.3

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Concurrent Medication Assessment in Treatment Period 1 and 2

Concurrent medications included paracetamol and ibuprofen. Number of participants who took concurrent medications during the study are presented. (NCT03149848)
Timeframe: Up to 10 weeks

,
InterventionParticipants (Count of Participants)
ParacetamolIbuprofen
CAB 30 mg00
RBT 300 mg + CAB 30 mg31

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE is any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. A SAE is defined as any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect and associated with liver injury and impaired liver function. Safety Population comprised of all participants who enrolled in the study and received at least one dose of study drug. (NCT03149848)
Timeframe: Up to 10 weeks

,
InterventionParticipants (Count of Participants)
Any AEsAny SAEs
CAB 30 mg10
RBT 300 mg + CAB 30 mg71

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Assessment of Clinical Chemistry Parameters: Calcium, Chloride, Carbon Dioxide, Glucose, Potassium, Sodium and Urea

Samples for clinical chemistry assessment were collected for Calcium, Chloride, Carbon Dioxide, Glucose, Potassium, Sodium and Urea. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Day -1, Day 13, Day 21, Day 27 and follow-up (10 to 14 days after last dose)

InterventionMillimoles per Liter (Mean)
Calcium, Day -1, n=15Calcium, On-treatment, Period 1 Day 13, n=14Calcium, On-treatment, Period 2 Day 21, n=13Calcium, On-treatment, Period 2 Day 27, n=12Calcium, Follow-up, Period 1 Day 13, n=1Calcium, Follow-up, Period 2 Day 21, n=1Calcium, Follow-up, Period 2 Day 27, n=1Calcium, Follow-up, n=15Chloride, Day -1, n=15Chloride, On-treatment, Period 1 Day 13, n=14Chloride, On-treatment, Period 2 Day 21, n=13Chloride, On-treatment, Period 2 Day 27, n=12Chloride, Follow-up, Period 1 Day 13, n=1Chloride, Follow-up, Period 2 Day 21, n=1Chloride, Follow-up, Period 2 Day 27, n=1Chloride, Follow-up, n=15Carbon Dioxide, Day -1, n=15Carbon Dioxide, On-treatment, Period 1 Day13, n=14Carbon Dioxide, On-treatment, Period 2 Day21, n=13Carbon Dioxide, On-treatment, Period 2 Day27, n=12Carbon Dioxide, Follow-up, Period 1 Day 13, n=1Carbon Dioxide, Follow-up, Period 2 Day 21, n=1Carbon Dioxide, Follow-up, Period 2 Day 27, n=1Carbon Dioxide, Follow-up, n=15Glucose, Day -1, n=15Glucose, On-treatment, Period 1 Day 13, n=14Glucose, On-treatment, Period 2 Day 21, n=13Glucose, On-treatment, Period 2 Day 27, n=12Glucose, Follow-up, Period 1 Day 13, n=1Glucose, Follow-up, Period 2 Day 21, n=1Glucose, Follow-up, Period 2 Day 27, n=1Glucose, Follow-up, n=15Potassium, Day -1, n=15Potassium, On-treatment, Period 1 Day 13, n=14Potassium, On-treatment, Period 2 Day 21, n=13Potassium, On-treatment, Period 2 Day 27, n=12Potassium, Follow-up, Period 1 Day 13, n=1Potassium, Follow-up, Period 2 Day 21, n=1Potassium, Follow-up, Period 2 Day 27, n=1Potassium, Follow-up, n=15Sodium, Day -1, n=15Sodium, On-treatment, Period 1 Day 13, n=14Sodium, On-treatment, Period 2 Day 21, n=13Sodium, On-treatment, Period 2 Day 27, n=12Sodium, Follow-up, Period 1 Day 13, n=1Sodium, Follow-up, Period 2 Day 21, n=1Sodium, Follow-up, Period 2 Day 27, n=1Sodium, Follow-up, n=15Urea, Day -1, n=15Urea, On-treatment, Period 1 Day 13, n=14Urea, On-treatment, Period 2 Day 21, n=13Urea, On-treatment, Period 2 Day 27, n=12Urea, Follow-up, Period 1 Day 13, n=1Urea, Follow-up, Period 2 Day 21, n=1Urea, Follow-up, Period 2 Day 27, n=1Urea, Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg2.312.342.292.282.272.382.062.28101.0100.5101.1101.8101.0100.099.0102.525.625.327.424.725.027.020.025.75.275.515.455.955.005.406.005.354.224.294.364.293.904.004.104.31141.1139.6140.3139.8139.0140.0137.0141.15.735.195.695.184.692.794.095.34

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Assessment of Plasma CAB Pharmacokinetic (PK) Parameter: Area Under the Concentration-time Curve Over One Dosing Interval (AUC [0 to Tau])

Blood samples for PK analysis of CAB were collected at pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28. AUC (0 to tau) was calculated using the linear trapezoidal rule for each incremental trapezoid and the log trapezoidal rule for each decremental trapezoid. PK Summary Population included participants who had CAB PK parameter estimates from both serial PK sampling time periods 1 and 2. Comparisons were made for the repeated dose PK parameters of CAB when given alone in Period 1 and when co-administered with steady-state RBT in Period 2. (NCT03149848)
Timeframe: Pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28

InterventionMicrogram * hour per milliliter (Geometric Mean)
CAB 30 mg103.978
RBT 300 mg + CAB 30 mg81.715

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Assessment of Plasma CAB PK Parameter: Concentration at the End of the Dosing Interval (Ctau)

Blood samples for PK analysis of CAB were collected at pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28. Comparisons were made for the repeated dose PK parameters of CAB when given alone in Period 1 and when co-administered with steady-state RBT in Period 2. (NCT03149848)
Timeframe: Pre-dose (within 15 minutes prior to dose) on Days 13 and 14; and 1, 2, 3, 4, 8, 12, and 24 hours post-dose on Day 14, pre-dose (within 15 minutes prior to dose) on Days 26, 27 and 28; and 1, 2, 3, 4, 8, 12 and 24 hours post-dose on Day 28

InterventionMicrograms per milliliter (Geometric Mean)
CAB 30 mg3.359
RBT 300 mg + CAB 30 mg2.479

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Change From Baseline in Pulse Rate

Vital signs measurement was done in semi-supine position after 10 minutes rest and included pulse rate. Two pulse rate measurement were taken at pre-dose on Day 1, at least 1 minute apart. The mean value recorded at pre-dose was classified as Baseline. Single pulse rate was obtained at all other time points during the study. Change from Baseline was calculated by subtracting the post-dose value from the Baseline value. NA indicated data not available since only one participant was analyzed, therefore standard deviation was not derived. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles). (NCT03149848)
Timeframe: Baseline to follow-up (10 to 14 days after last dose)

InterventionBeats/minute (Mean)
On-treatment, Period 1 Day 14, n=14On-treatment, Period 2 Day 21, n=13On-treatment, Period 2 Day 28, n=12Follow-up, Period 2 Day 21, n=1Follow-up, n=15
CAB 30 mg Followed by RBT 300 mg + CAB 30 mg-4.5-6.23.439.0-1.3

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Number of Participants With H. Pylori Cultures That Presented Antibiotic Resistance and Susceptibility

"The primary endpoint was summarized within subgroups formed by the presence of H. pylori susceptibility and resistance to amoxicillin, clarithromycin, metronidazole, and rifabutin from H. pylori cultures from samples obtained prior to initiating study treatment (i.e. baseline).~A participant is considered a responder when H. pylori is eradicated after treatment as confirmed via 13C Urea Breath Test (UBT). A participant is considered a non-responder when H. pylori is not eradicated after treatment." (NCT03198507)
Timeframe: 43-71 days after initiation of treatment

InterventionParticipants (Count of Participants)
Rifabutin resistant72525830Rifabutin resistant72525831Rifabutin Susceptible72525830Rifabutin Susceptible72525831Amoxicillin Resistant72525830Amoxicillin Resistant72525831Amoxicillin Susceptible72525830Amoxicillin Susceptible72525831Clarithromycin Resistant72525831Clarithromycin Resistant72525830Clarithromycin Susceptible72525831Clarithromycin Susceptible72525830Metronidazole Resistant72525830Metronidazole Resistant72525831Metronidazole Susceptible72525830Metronidazole Susceptible72525831
ResponderNon-responder
RHB-1050
Active Comparator0
RHB-105147
Active Comparator99
RHB-10527
Active Comparator72
RHB-1059
Active Comparator4
Active Comparator5
RHB-105138
Active Comparator95
Active Comparator67
RHB-10521
Active Comparator22
RHB-1054
Active Comparator13
RHB-105126
Active Comparator77
RHB-10523
Active Comparator59
RHB-10557
Active Comparator45
RHB-10514
Active Comparator34
RHB-10590
Active Comparator53
RHB-10513
Active Comparator38

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Number of Participants With Eradication of H. Pylori in the Pharmacokinetic Population (PKP)

"A pre-specified responder analysis of eradication of H. pylori confirmed via 13C Urea Breath Test (UBT) was performed in the PK population.~The PK population was generated based on the measurement of plasma concentrations of amoxicillin, omeprazole, rifabutin, and the rifabutin metabolite 25-O-desacetyl-rifabutin (on Day 13). It included those subjects in the FAS who had demonstrable presence of any component of investigational drug at Visit 3 or had no levels detected >250 hours after the last dose. For all subjects, the reason for exclusion from the PKP was the absence of any pharmacokinetic component of study drug at Visit 3 within 250 hours of the last reported dose. Two hundred fifty hours was selected to account for approximately 10 times the terminal half-life of rifabutin." (NCT03198507)
Timeframe: 43-71 days after initiation of treatment

InterventionParticipants (Count of Participants)
RHB-105187
Active Comparator119

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Number of Participants With Eradication of H. Pylori

Eradication of H. pylori confirmed via 13C Urea Breath Test (UBT) testing. Subjects with negative test results (eradication of H. pylori) were considered treatment successes. Subjects who tested positive for H. pylori infection (no eradication) were considered treatment failures. (NCT03198507)
Timeframe: 43-71 days after initiation of treatment

InterventionParticipants (Count of Participants)
RHB-105191
Active Comparator131

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Elimination Rate Constant (Ke) of Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The elimination rate constant is the rate that imatinib is removed from the body. (NCT03891901)
Timeframe: Day 14, Day 28

Intervention1/hour (Median)
After 14 days of imatinib
Imatinib (100 mg)0.06

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Area Under the Curve (AUC) for Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter AUC is the overall exposure to imatinib. (NCT03891901)
Timeframe: Day 14, Day 28

,
Interventionhour*mcg/mL (Median)
After 14 days of imatinibAfter 14 days of imatinib plus rifabutin and isoniazid
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid4.767.52
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid9.467.49

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Maximum Concentration (Cmax) of Rifabutin

Blood samples for pharmacokinetic (PK) analyses of rifabutin were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter Cmax is the highest concentration of the drug in blood following dosing. (NCT03891901)
Timeframe: Day 28

Interventionmcg/mL (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid0.37
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid0.53

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Maximum Concentration (Cmax) of Isoniazid

Blood samples for pharmacokinetic (PK) analyses of isoniazid were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter Cmax is the highest concentration of the drug in blood following dosing. (NCT03891901)
Timeframe: Day 28

Interventionmcg/mL (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid3.14
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid3.66

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Half-life (T1/2) of Rifabutin

Blood samples for pharmacokinetic (PK) analyses of rifabutin were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter T1/2 is the time when the drug in blood is half of the maximum concentration. (NCT03891901)
Timeframe: Day 28

Interventionhours (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid9.65
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid8.14

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Half-life (T1/2) of Isoniazid

Blood samples for pharmacokinetic (PK) analyses of isoniazid were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter T1/2 is the time when the drug in blood is half of the maximum concentration. (NCT03891901)
Timeframe: Day 28

Interventionhours (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid1.59
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid2.44

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Frequency of Serious Adverse Events (SAEs)

"The number of serious adverse events occurring among study participants is presented here. Adverse events are graded using the FDA Guidance Document, Toxicity Grading Scale for Healthy Adult and Adolescent Volunteers Enrolled in Preventive Vaccine Clinical Trials Guidance for Industry, September 2007, or other guidance, as applicable." (NCT03891901)
Timeframe: Measured through Day 50

Interventionserious adverse events (Number)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid0
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid0
Imatinib (100 mg)0

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Frequency of Grade 3 or 4 Adverse Events (AEs)

"The number of grade 3 or 4 adverse events occurring among study participants is presented here. Adverse events are graded using the FDA Guidance Document, Toxicity Grading Scale for Healthy Adult and Adolescent Volunteers Enrolled in Preventive Vaccine Clinical Trials Guidance for Industry, September 2007, or other guidance, as applicable." (NCT03891901)
Timeframe: Measured through Day 50

InterventionGrade 3 or 4 adverse events (Number)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid4
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid6
Imatinib (100 mg)0

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Elimination Rate Constant (Ke) of Rifabutin

Blood samples for pharmacokinetic (PK) analyses of rifabutin were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The elimination rate constant is the rate that the drug is removed from the body. (NCT03891901)
Timeframe: Day 28

Intervention1/hour (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid0.07
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid0.09

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Elimination Rate Constant (Ke) of Isoniazid

Blood samples for pharmacokinetic (PK) analyses of isoniazid were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The elimination rate constant is the rate that the drug is removed from the body. (NCT03891901)
Timeframe: Day 28

Intervention1/hour (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid0.44
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid0.28

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White Blood Cell Count

The normal range for white blood cell counts is between 4,000 and 11,000 cells per microliter. White blood cell counts increase during infections, autoimmune diseases and some types of cancer. Low white blood cell counts occur with immune system diseases and certain types of cancer. (NCT03891901)
Timeframe: Days 1, 7, 14, 21, 28, 42

,,
Interventioncells/µL (Mean)
Day 1Day 7Day 14Day 21Day 28Day 42
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid555853915841487541415841
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid630059005150365016005800
Imatinib (100 mg)590055005400475048005300

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Area Under the Curve (AUC) for Rifabutin

Blood samples for pharmacokinetic (PK) analyses of rifabutin were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter AUC is the overall exposure to the drug. (NCT03891901)
Timeframe: Day 28

Interventionhour*mcg/mL (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid3.68
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid5.11

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Area Under the Curve (AUC) for Isoniazid

Blood samples for pharmacokinetic (PK) analyses of isoniazid were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter AUC is the overall exposure to the drug. (NCT03891901)
Timeframe: Day 28

Interventionhour*mcg/mL (Median)
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid9.79
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid16.11

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Half-life (T1/2) of Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter T1/2 is the time when imatinib in blood is half of the maximum concentration. (NCT03891901)
Timeframe: Day 14, Day 28

,
Interventionhours (Median)
After 14 days of imatinibAfter 14 days of imatinib plus rifabutin and isoniazid
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid11.329.91
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid15.017.83

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Half-life (T1/2) of Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter T1/2 is the time when imatinib in blood is half of the maximum concentration. (NCT03891901)
Timeframe: Day 14, Day 28

Interventionhours (Median)
After 14 days of imatinib
Imatinib (100 mg)11.00

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Elimination Rate Constant (Ke) of Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The elimination rate constant is the rate that imatinib is removed from the body. (NCT03891901)
Timeframe: Day 14, Day 28

,
Intervention1/hour (Median)
After 14 days of imatinibAfter 14 days of imatinib plus rifabutin and isoniazid
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid0.060.07
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid0.050.09

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Area Under the Curve (AUC) for Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter AUC is the overall exposure to imatinib. (NCT03891901)
Timeframe: Day 14, Day 28

Interventionhour*mcg/mL (Median)
After 14 days of imatinib
Imatinib (100 mg)5.80

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Number of Myelomonocytic Cells in the Blood

Immunologic effects of the study treatment are assessed by counting myelomonocytic cells in blood samples. An increase in myelomonocytic cells is used to determine the appropriate therapeutic dose of imatinib. (NCT03891901)
Timeframe: Days 1, 7, 14, 21, 28, 42

,,
Interventioncells per microliter (µL) (Mean)
Day 1Day 7Day 14Day 21Day 28Day 42
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid319732413418302123563629
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid434036803195256011404425
Imatinib (100 mg)339030753195278524803255

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Maximum Concentration (Cmax) of Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter Cmax is the highest concentration of imatinib in blood following dosing. (NCT03891901)
Timeframe: Day 14, Day 28

,
Interventionmicrograms per milliliter (mcg/mL) (Median)
After 14 days of imatinibAfter 14 days of imatinib plus rifabutin and isoniazid
Cohort 1a: Imatinib (50 mg) + Rifabutin + Isoniazid0.410.71
Cohort 1b: Imatinib (100 mg) + Rifabutin + Isoniazid0.690.69

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Maximum Concentration (Cmax) of Imatinib

Blood samples for pharmacokinetic (PK) analyses of imatinib were collected at 6 time points over approximately 24 hours. Samples collection occurred at hour 0 (pre-dose), and 0.5 hours, 2 hours, 4.0 hours, 8.0 hours, and 24 hours post-dose. PK samples were taken after 14 days of imatinib alone (all study arms) and after 14 days of imatinib with rifabutin and isoniazid (Cohorts 1a and 1b). The PK parameter Cmax is the highest concentration of imatinib in blood following dosing. (NCT03891901)
Timeframe: Day 14, Day 28

Interventionmicrograms per milliliter (mcg/mL) (Median)
After 14 days of imatinib
Imatinib (100 mg)0.51

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Time to the Maximum Observed Plasma Concentration (Tmax) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

InterventionHours (Median)
Zanubrutinib1.50
Zanubrutinib + Rifabutin2.00

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AUC From Time Zero to Infinity (AUC0-∞) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

Interventionh*ng/mL (Geometric Mean)
Zanubrutinib2780
Zanubrutinib + Rifabutin1590

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Area Under the Curve (AUC) From Time Zero to the Time of the Last Quantifiable Concentration (AUC0-t) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

Interventionh*ng/mL (Geometric Mean)
Zanubrutinib2700
Zanubrutinib + Rifabutin1530

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Apparent Volume of Distribution (Vz/F) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

InterventionLiters (Geometric Mean)
Zanubrutinib1080
Zanubrutinib + Rifabutin1750

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Apparent Terminal Elimination Half-life (t1/2) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

InterventionHours (Mean)
Zanubrutinib7.24
Zanubrutinib + Rifabutin7.00

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Apparent Oral Clearance (CL/F) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

InterventionLiters/hour (Geometric Mean)
Zanubrutinib115
Zanubrutinib + Rifabutin201

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Number of Participants Experiencing Adverse Events (AEs)

Adverse events (AEs) and serious adverse events included for summary, AEs that start during or after the first dose, or start prior to the first dose and increases in severity after the first dose, including vital signs, physical examination, electrocardiogram, and laboratory parameters (NCT04470908)
Timeframe: From the date of first study drug administration to 30 days after last dose (up to 3.5 months)

,,
InterventionParticipants (Count of Participants)
At least 1 treatment-emergent adverse event (TEAE)Serious adverse eventsVital sign TEAEsPhysical examination TEAEsElectrocardiogram TEAEsLaboratory-related TEAEs
Rifabutin on Days 3 to 10600000
Zanubrutinib + Rifabutin on Day 11000000
Zanubrutinib on Day 1100000

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Time of the Last Quantifiable Concentration (Tlast) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

InterventionHours (Median)
Zanubrutinib36.0
Zanubrutinib + Rifabutin36.0

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Maximum Observed Plasma Concentration (Cmax) of Zanubrutinib

(NCT04470908)
Timeframe: Predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 36 hours postdose on Days 1 and 11

Interventionng/mL (Geometric Mean)
Zanubrutinib489
Zanubrutinib + Rifabutin253

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