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mesna

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Description

Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23662354
CHEMBL ID975
CHEBI ID31824
SCHEMBL ID7993
MeSH IDM0023193

Synonyms (132)

Synonym
mesnex
sodium 2-mercaptoethanesulfonate
nsc-113891
smr000059219
MLS001074691
AC-6011
AB01274734-01
2-mercaptoethanesulphonate, sodium
mesna
2-mercaptoethanesulfonate, sodium
2-mercaptoethanesulfonic acid monosodium salt
2-mercaptoethanesulfonic acid sodium salt
ethanesulfonic acid, 2-mercapto-, monosodium salt
nsc 113891
mistabron
ccris 3712
mesnum [inn-latin]
mitexan
einecs 243-285-9
2-mercapto-ethan-sulfonsaeure, natrium-salz
natrium 2-mercaptoethansulfonat
sodium 2-mercaptoethanesulphonate
mesnum
sodium 2-mercaptoethane sulfonate
2-mercaptoethane sulfonate sodium
19767-45-4
PRESTWICK_1005
SPECTRUM5_001174
NCGC00181166-01
nsc113891
mistabronco
uromitexan
mesna (jan/usp/inn)
mesnex (tn)
D01459
uromitexan (tn)
NCGC00094939-01
NCGC00094939-02
KBIOGR_000501
KBIO3_002565
SPECTRUM2_000752
SPECTRUM3_001483
SPBIO_000764
SPECTRUM4_000041
SPECTRUM1502014
MLS001333252
MLS001333251
HMS2092N09
CHEMBL975
d-7093
d 7093
coenzyme m sodium salt
HMS502F17
M0913
HMS1921D10
HMS3259D13
EN300-49858
mesna [usan:usp:inn:ban]
unii-nr7o1405q9
nr7o1405q9 ,
dtxcid50809
dtxsid1020809 ,
NCGC00258417-01
tox21_112767
tox21_200863
cas-19767-45-4
AKOS006220661
sodium 2-sulfanylethane-1-sulfonate
2-mercaptoethanesulphonic acid sodium salt
HMS2236L05
AKOS015960755
CCG-40134
HY-13679
CS-1364
W-60283
S1735
HMS3372M11
XOGTZOOQQBDUSI-UHFFFAOYSA-M
sodium 2-sulphanylethanesulphonate
mesna [orange book]
mesna [usp impurity]
mesna [mart.]
mesna [vandf]
mesna [usan]
mesna [mi]
mesna [jan]
mesna [inn]
mesna [usp monograph]
mesna [who-dd]
mesna [ep monograph]
NC00648
SCHEMBL7993
tox21_112767_1
NCGC00178318-04
Q-201713
sodium 2-mercaptoethane-1-sulfonate
2-mercaptoethanesulfonic acid sodium
mfcd00007535
DTXSID8023264 ,
sodium;2-sulfanylethanesulfonate
HMS3655M06
mesna; sodium 2-sulfanylethanesulfonate
CHEBI:31824
HMS3715H05
SW199618-2
sodium 2-mercaptoethanesulfonate;mesnum
bdbm50247978
Q424997
3-aminooxy-n-propyl(dimethyl-t-butylsilyl)ether
mesna (uromitexan, mesnex)
mexan
AS-13260
BCP14384
ethanesulfonic acid, 2-mercapto-, sodium salt (1:1)
sodium2-mercaptoethanesulfonate
mercaptoethane sulfonate
filesna
mercaptoethanesulfonate
mesna (ep monograph)
mesna (usp impurity)
v03af01
r05cb05
ausobronc
mesnil
2-mercaptoethanesulfonate, sodium salt
mesna (mart.)
mesna (usp monograph)
mucolene
mesna injection
dtxcid103264
SY073943
Z594284202

Research Excerpts

Overview

Mesna is a thiol compound effective in the connective tissue, which is used for its chemical dissector, mucolytic, mucosal damage preventive and antioxidant effects. Mesna is an important regional antidote for protecting the urinary system of chemotherapy patients.

ExcerptReferenceRelevance
"Mesna is an important regional antidote for protecting the urinary system of chemotherapy patients, which requires monitoring its level in real time to ensure the curative effect. "( A Portable Sensing Platform Using an Upconversion-Based Nanosensor for Visual Quantitative Monitoring of Mesna.
Hu, B; Jiang, C; Shen, J; Yang, L; Zhu, J, 2022
)
2.38
"Mesna is a drug with fibrinolytic properties which has been used in surgical field to facilitate tissue dissection."( Topical Application of High-Dose Mesna Prevents Adhesion Formation: An Experimental Animal Study.
Berkesoglu, M; Dirlik, MM; Karabulut, YY; Turkmenoglu, OM; Yildirim, DD, 2020
)
1.56
"Mesna is a thiol compound effective in the connective tissue, which is used for its chemical dissector, mucolytic, mucosal damage preventive and antioxidant effects. "( Use of Mesna in the treatment of ossicular chain fixation related to tympanosclerosis; prospective, clinical study.
Calım, ÖF; Dogan, R; Eren, SB; Ozturan, O; Tugrul, S; Vural, Ö; Yenigun, A,
)
2.03
"Mesna is a chemoprotective agent with anti-inflammatory and anti-oxidant effects."( The Neuroprotective Effect of Mesna on Cisplatin-Induced Neurotoxicity: Behavioral, Electrophysiological, and Molecular Studies.
Amirshahrokhi, K; Esmaeili, H; Niapour, A; Noroozzadeh, S; Saadati, H; Shadman, J, 2021
)
1.63
"Mesna is a regional detoxificant which inactivates acrolein."( Inactivation of acrolein by sodium 2-mercaptoethanesulfonate using headspace-solid-phase microextraction gas chromatography and mass spectrometry.
Kojima, T; Sakura, N; Takamoto, S; Yashiki, M, 2003
)
1.04
"MESNA is a synthetic sulfur compound that produces mucolysis by disrupting disulfide bonds. "( Practical use of MESNA in atelectatic ears and adhesive otitis media.
Bayazit, YA; Bayramoglu, I; Goksu, N; Yilmaz, M, 2006
)
2.12
"Mesna is a thiol used for the prevention of oxazaphosphorine-induced hemorrhagic cystitis. "( Mesna protects intestinal mucosa from ischemia/reperfusion injury.
Kortsaris, A; Lambropoulou, M; Papadopoulos, N; Simopoulos, C; Tentes, I; Ypsilantis, P, 2006
)
3.22
"Mesna is a pharmacologically unremarkable, physiologically largely inert and almost totally non-toxic thio compound. "( Studies on the urotoxicity of oxazaphosphorine cytostatics and its prevention--III. Profile of action of sodium 2-mercaptoethane sulfonate (mesna).
Brock, N; Pohl, J; Scheef, W; Stekar, J, 1982
)
1.91
"Mesna (Mistabron) is a mucolytic substance that is also used for chemically assisted dissection during cholesteatoma surgery. "( Single ototopical application of mesna has no ototoxic effects on guinea pig cochlear hair cells: a morphological study.
Claes, J; Scheuermann, DW; Timmermans, JP; Van de Heyning, PH; Van Spaendonck, MP; Wuyts, FL, 1999
)
2.03
"Mesna is a sulfohydrate administered as a supportive drug in conjunction with oxazaphosphorines to prevent bladder toxicity from metabolites. "( The kinetics and mechanisms of the reaction of Mesna with cisplatin, oxiplatin and carboplatin.
Bazzazi, H; Kangarloo, B; Oprea, A; Wolff, JE,
)
1.83
"Argimesna is a sulfhydryl group containing molecule which has no effect on glutathione status or on the total thiol pool."( The effects of L-arginine mono(2-mercaptoethanesulfonate) on the ischemic and reperfused heart.
Boraso, A; Cargnoni, A; Comini, L; De Giuli, F; Ferrari, R; Scotti, C, 1992
)
0.76
"Mesna is a thiol compound designed to function as a regional detoxificant of urotoxic oxazaphosphorine cytostatics such as ifosfamide."( Ifosfamide and mesna.
Dana, WJ; Schoenike, SE, 1990
)
1.35
"Mesna is an effective uroprotective agent that prevents recurrent acute hemorrhagic cystitis, or worsening of chronic hemorrhagic cystitis, in patients receiving further oxazaphosphorine after previous ifosfamide- or cyclophosphamide-induced hematuria."( The efficacy of mesna (2-mercaptoethane sodium sulfonate) as a uroprotectant in patients with hemorrhagic cystitis receiving further oxazaphosphorine chemotherapy.
Andriole, GL; Arasi, V; Linehan, M; Magrath, IT; Miser, JS; Sandlund, JT, 1987
)
1.34
"Mesna is a sulfhydryl compound that reacts with the metabolites of cyclophosphamide that are excreted in the urine and may produce bladder wall irritation. "( Efficacy of mesna in preventing further cyclophosphamide-induced hemorrhagic cystitis.
Luce, JK; Simons, JA, 1988
)
2.1

Effects

Mesna (0.3 mmol/l) has a complete protective effect with respect to acrolein and CAA, while the protective effect versus 100 mumol/l of 4-OOH-IF is incomplete. Oral mesna has a longer mean residence time than i.v.

MESNA has been successfully used to ease abdominal myomectomies and excision of endometrial cysts. In ENT surgery, topical MESNA could be widely used, from ear and skull base to head and neck diseases.

ExcerptReferenceRelevance
"Mesna possibly has a toxic effect on bladder mucosa."( Multivariate analysis of risk factors for hemorrhagic cystitis after hematopoietic stem cell transplantation.
Hattori, K; Hotta, T; Inoue, H; Kato, S; Kawada, H; Kishi, K; Matsumoto, M; Ogawa, Y; Ohmachi, K; Shimizu, T; Tsuboi, K; Watanabe, S; Yabe, H; Yabe, M; Yasuda, Y; Yoshiba, F, 2003
)
1.04
"Mesna (0.3 mmol/l) has a complete protective effect with respect to acrolein and CAA, while the protective effect versus 100 mumol/l of 4-OOH-IF is incomplete."( Ifosfamide and mesna: effects on the Na/H exchanger activity in renal epithelial cells in culture (LLC-PK1).
Brandis, M; Küpper, N; Mohrmann, M; Schönfield, B,
)
1.21
"Oral mesna has a longer mean residence time than i.v."( Oral bioavailability of mesna tablets.
Borner, M; Cerny, T; Lauterburg, BH; Stofer-Vogel, B, 1993
)
1.05
"MESNA has been successfully used to ease abdominal myomectomies and excision of endometrial cysts; in ENT surgery, topical MESNA could be widely used, from ear and skull base to head and neck diseases, in both outpatient and operating-room settings. "( MESNA for chemically assisted tissue dissection.
Casale, M; Denaro, V; Di Martino, A; Salvinelli, F; Trombetta, M, 2010
)
3.25
"Mesna has been given in higher dosage (5 g/m2 over 24 h), but otherwise the schedule is as above."( Ifosfamide plus mesna with and without adriamycin in soft tissue sarcoma.
Fisher, C; Harmer, C; McKinna, A; Westbury, G; Wiltshaw, E, 1986
)
1.34

Actions

Mesna appears to inactivate cisplatin directly in vitro but possibly not in vivo if separate injections are used. MESNA is shown to enhance excretion of cysteine in urine.

ExcerptReferenceRelevance
"Mesna may produce gastrointestinal and allergic reactions."( Ifosfamide and mesna.
Dana, WJ; Schoenike, SE, 1990
)
1.35
"Mesna appears to inactivate cisplatin directly in vitro but possibly not in vivo if separate injections are used."( Interaction between cisplatin and mesna in mice.
Dorr, RT; Lagel, K, 1989
)
1.28
"MESNA is shown to enhance excretion of cysteine in urine."( Excretion of sodium 2-mercaptoethanesulphonate (MESNA) in the urine of volunteers after oral dosing.
Jones, MS; Murrell, RD; Shaw, IC, 1985
)
1.25

Treatment

Mesna pretreatment prevented the Pringle-induced antimitotic effect and the induction of oxidative stress. It inhibited the activation of NF-kappaB, while attenuating liver injury after PH under Pringle.

ExcerptReferenceRelevance
"Mesna pretreatment prevented the Pringle-induced antimitotic effect and the induction of oxidative stress, inhibited the activation of NF-kappaB, while attenuating liver injury after PH under Pringle."( Impaired liver regeneration following partial hepatectomy using the Pringle maneuver: Protective effect of mesna.
Anagnostopoulos, K; Kortsaris, A; Lambropoulou, M; Papadopoulos, N; Simopoulos, C; Tentes, I; Tsigalou, C; Ypsilantis, P, 2009
)
1.29
"Mesna pretreatment protects the liver against the Pringle-induced antimitotic effect after PH via the prevention of oxidative stress and the inhibition of NF-kappaB activation."( Impaired liver regeneration following partial hepatectomy using the Pringle maneuver: Protective effect of mesna.
Anagnostopoulos, K; Kortsaris, A; Lambropoulou, M; Papadopoulos, N; Simopoulos, C; Tentes, I; Tsigalou, C; Ypsilantis, P, 2009
)
1.29
"Mesna pretreatment had an antioxidant effect which varied from attenuation to prevention of oxidative stress."( Prophylaxis with mesna prevents oxidative stress induced by ischemia reperfusion in the intestine via inhibition of nuclear factor-kappaB activation.
Anagnostopoulos, K; Kortsaris, A; Lambropoulou, M; Papadopoulos, N; Simopoulos, C; Tentes, I; Ypsilantis, P, 2008
)
1.41
"Treatment with MESNA (75 and 150 mg/kg), significantly (P < 0.05-0.0001) decreased the I/R-induced increase in serum tumor necrosis factor-alpha (TNF-α) and Interleukin-1-beta (IL-1 β)."( MESNA (2-Mercaptoethanesulfonate) Attenuates Brain, Heart, and Lung Injury Induced by Carotid Ischemia-Reperfusion in Rats.
Abacioglu, N; Cetinel, S; Chukwunyere, U; Gencosman, S; Gultekin, C; Mercan, M; Sayiner, S; Sehirli, AO, 2023
)
2.69
"Pre-treatment with mesna was able to abolish the changes in pancreatic enzymes, oxidative stress markers (TBARS, SOD, GSH and GSH-Px), pancreatic inflammatory markers (TNF-α, IL-1β) as well as histological changes."( Mesna Alleviates Cerulein-Induced Acute Pancreatitis by Inhibiting the Inflammatory Response and Oxidative Stress in Experimental Rats.
Aljasser, SN; Almubrik, SA; Attia, NM; Hagar, HH, 2020
)
2.32
"Pretreatment with mesna (2-mercaptoethanesulfonic acid), which interacts with acrolein resulting in an inactive compound, inhibited all changes induced by acrolein."( A model of hemorrhagic cystitis induced with acrolein in mice.
Batista, CK; Brito, GA; Cunha, FQ; Leitão, BT; Ribeiro, RA; Souza, ML, 2006
)
0.66

Toxicity

Treatment of the patients with MESNA prevented the adverse renal effect of contrast media (median serum creatinine 293; range: 187-433 micromol/l) 48 h after coronary angiography. This selective antitoxic effect of mesna towards vepeside and taxol allows to intensify the anticancer chemotherapy.

ExcerptReferenceRelevance
"Renal dysfunction and urinary disorders are the most troublesome adverse reaction to anticancer agents such as cisplatin (CDDP) and ifosfamide (IFM)."( [New treatments for urogenital toxicity of anti-neoplastic chemotherapy].
Hirosawa, A; Niitani, H; Shibuya, M, 1990
)
0.28
" Myelosuppression occurred in all patients but was mild and reversible, with no toxic deaths."( Toxicity of high-dose ifosfamide in children.
Craft, AW; Davies, SM; Pearson, AD, 1989
)
0.28
" We observed this acute toxic effect despite the administration of sufficient mesna to prevent hemorrhagic cystitis."( Ifosfamide-induced subclinical tubular nephrotoxicity despite mesna.
Goren, MP; Horowitz, ME; Pratt, CB; Wright, RK, 1987
)
0.74
" These negative attributes may be caused by toxic and genotoxic metabolites, respectively."( In vitro/in vivo effects of Mesna on the genotoxicity and toxicity of cyclophosphamide--a study aimed at clarifying the mechanism of Mesna's anticarcinogenic activity.
Bos, RP; Niemeyer, U; Pool, BL; Schmähl, D; Theuws, JL, 1988
)
0.57
"Nephrotoxicity is a relatively common and potentially serious adverse effect of treatment with certain cytotoxic drugs (especially ifosfamide)."( Strategies to prevent nephrotoxicity of anticancer drugs.
Skinner, R, 1995
)
0.29
"With the increasing use of ifosfamide in pediatric malignancies, nephrotoxicity has emerged as a potentially serious adverse effect, which may be dose-limiting or may cause severe chronic morbidity, including glomerular impairment and/or Fanconi's syndrome."( Ifosfamide, mesna, and nephrotoxicity in children.
Craft, AW; Pearson, AD; Sharkey, IM; Skinner, R, 1993
)
0.66
" Although mesna may be capable of detoxifying the toxic metabolite(s), delivery to the renal tubule may not be sufficient to provide adequate protection of tubular glutathione from depletion by the metabolite(s), which results in a failure to prevent nephrotoxicity."( Ifosfamide, mesna, and nephrotoxicity in children.
Craft, AW; Pearson, AD; Sharkey, IM; Skinner, R, 1993
)
1.07
" Ifosfamide, although itself the effective antineoplastic drug useful in situations which have proved refractory to cyclophosphamide therapy, has the side-effect toxicities caused by its metabolities that pose clinically a very real problem."( Influence of mesna on urotoxic effects of selected bromosubstituted analogs of ifosfamide.
Konarski, L; Kowalski, P; Kuśnierczyk, H; Radzikowski, C, 1997
)
0.67
"Renal injury is a common side effect of the chemotherapeutic agent ifosfamide."( Toxicity of ifosfamide and its metabolite chloroacetaldehyde in cultured renal tubule cells.
Chan, K; Davies, S; Lu, H; Springate, J; Taub, M, 1999
)
0.3
"Adjuvant ifosfamide appears to be safe and well tolerated in patients with completely resected uterine sarcoma."( Safety and efficacy of adjuvant single-agent ifosfamide in uterine sarcoma.
Belinson, JL; Kennedy, AW; Kushner, DM; Markman, M; Rybicki, LA; Webster, KD, 2000
)
0.31
" This selective antitoxic effect of mesna towards vepeside and taxol allows to intensify the anticancer chemotherapy with these highly effective but extremely toxic cytostatics and to improve the efficiency of anticancer therapy."( Effect of mesna on lethal effect and hematological toxicity of taxol and vepeside in mice.
Bogush, EA; Bogush, TA; Khrustalev, SA; Koldaeva, EY; Konyaeva, OI; Smirnova, GB, 2001
)
0.99
"Immunosuppression incorporating intravenous cyclophosphamide before and after transplantation is safe and highly effective in sensitized cardiac transplant recipients."( Intravenous pulse administration of cyclophosphamide is an effective and safe treatment for sensitized cardiac allograft recipients.
Burke, E; Edwards, N; Itescu, S; John, R; Lietz, K; Mancini, D; Michler, R; Oz, M; Rose, E, 2002
)
0.31
"Renal injury is a common side effect of the chemotherapeutic agent ifosfamide."( Comparative toxicity of ifosfamide metabolites and protective effect of mesna and amifostine in cultured renal tubule cells.
Springate, JE; Taub, M; Zaki, EL, 2003
)
0.55
" In the clinical study, treatment of the patients with MESNA prevented the adverse renal effect of contrast media (median serum creatinine 293; range: 187-433 micromol/l) 48 h after coronary angiography/intervention."( Free reactive oxygen species and nephrotoxicity of contrast agents.
Haeussler, U; Keller, F; Riedel, M, 2004
)
0.57
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"Renal injury is a common side effect of the chemotherapeutic agent ifosfamide."( Ifosfamide toxicity in cultured proximal renal tubule cells.
Springate, J; Taub, M, 2007
)
0.34
" Abnormal clinical observations and adverse effects on clinical pathology, urinalysis, and histology indicated acute renal damage and urothelial damage and bone marrow dysfunction."( Characterization of Batracylin-induced Renal and Bladder Toxicity in Rats.
Altera, KP; Ames, MM; Buhrow, SA; Bunin, DI; Davis, M; Ji, J; Kinders, RJ; Lawrence, SM; Parman, T; Rausch, LL; Reid, JM; Samuelsson, SJ; Walden, C, 2015
)
0.42

Pharmacokinetics

The combination of BNP7787 with cisplatin did not alter the pharmacokinetic profiles of mesna. The distribution half-life of total platinum was also observed when mesna was present compared to cisplatoon without mesna (t(1/2a), 32 +/- 18 min; n = 5)

ExcerptReferenceRelevance
" mesna administration, the mean half-life of mesna was 21."( Pharmacokinetics of intravenous and oral sodium 2-mercaptoethane sulphonate (mesna) in normal subjects.
James, CA; Mant, TG; Rogers, HJ, 1987
)
1.41
" In 25 patients (27 cycles) extensive pharmacokinetic analyses were performed."( Saturable metabolism of continuous high-dose ifosfamide with mesna and GM-CSF: a pharmacokinetic study in advanced sarcoma patients. Swiss Group for Clinical Cancer Research (SAKK).
Boddy, AV; Brunner, J; Cerny, T; Honegger, P; Küpfer, A; Leyvraz, S; Schaad, R; Schmitz, SF; Sessa, C; von Briel, T, 1999
)
0.54
" Interpatient variability of pharmacokinetic parameters was high."( Saturable metabolism of continuous high-dose ifosfamide with mesna and GM-CSF: a pharmacokinetic study in advanced sarcoma patients. Swiss Group for Clinical Cancer Research (SAKK).
Boddy, AV; Brunner, J; Cerny, T; Honegger, P; Küpfer, A; Leyvraz, S; Schaad, R; Schmitz, SF; Sessa, C; von Briel, T, 1999
)
0.54
" We also evaluated potential pharmacokinetic interactions between BNP7787 and cisplatin."( Pharmacokinetics of BNP7787 and its metabolite mesna in plasma and ascites: a case report.
Boven, E; Hausheer, FH; Van der Vijgh, WJ; Verschraagen, M; Zegers, I, 2003
)
0.58
" For pharmacokinetic investigation of BNP7787 and mesna and a possible mutual pharmacokinetic interaction between BNP7787 and cisplatin, cisplatin and BNP7787 were also administered as single agents in 14 of 25 patients."( Pharmacokinetics and preliminary clinical data of the novel chemoprotectant BNP7787 and cisplatin and their metabolites.
Berkhof, J; Boven, E; Hausheer, FH; Ruijter, R; van der Born, K; van der Vijgh, WJ; Verschraagen, M, 2003
)
0.57
" The pharmacokinetic profile of mesna was unaffected by cisplatin and its metabolites."( Pharmacokinetics and preliminary clinical data of the novel chemoprotectant BNP7787 and cisplatin and their metabolites.
Berkhof, J; Boven, E; Hausheer, FH; Ruijter, R; van der Born, K; van der Vijgh, WJ; Verschraagen, M, 2003
)
0.6
" The combination of BNP7787 with cisplatin did not alter the pharmacokinetic profiles of mesna or the cisplatin metabolites."( Pharmacokinetics and preliminary clinical data of the novel chemoprotectant BNP7787 and cisplatin and their metabolites.
Berkhof, J; Boven, E; Hausheer, FH; Ruijter, R; van der Born, K; van der Vijgh, WJ; Verschraagen, M, 2003
)
0.54
" The pharmacodynamic effects of mesna on depleting plasma cysteine, a GSH precursor, were evaluated in 22 patients as part of a Phase I study."( Pharmacokinetics and pharmacodynamics of mesna-mediated plasma cysteine depletion.
Booker, BM; Creaven, P; Pendyala, L; Perez, R; Smith, PF, 2003
)
0.87
"057) in prolonged distribution half-life of total platinum was also observed when mesna was present (t(1/2a) 65 +/- 21 min; n = 3) compared to cisplatin without mesna (t(1/2a), 32 +/- 18 min; n = 5)."( Influence of mesna on the pharmacokinetics of cisplatin and carboplatin in pediatric cancer patients.
Gangopadhyay, SB; Glück, S; Kangarloo, SB; Syme, RM; Wolff, JE, 2004
)
0.92
"To investigate the prognostic value of systemic exposure to etoposide (Area Under the concentration Curve (AUC(VP16))) on overall survival (OS) in patients with small cell lung cancer (SCLC)."( Etoposide pharmacokinetics and survival in patients with small cell lung cancer: a multicentre study.
Chabaud, S; Court-Fortune, I; Falandry, C; Fournel, C; Freyer, G; Girard, P; Ribba, B; Souquet, PJ; Tod, M; Tranchand, B; Trillet-Lenoir, V; You, B, 2008
)
0.35
" Topotecan pharmacokinetic analyses were carried out, and topoisomerase I levels and activity were measured."( Phase I Study of Topotecan, Ifosfamide, and Etoposide (TIME) with autologous stem cell transplant in refractory cancer: pharmacokinetic and pharmacodynamic correlates.
Dawson, JL; Field, TL; Fields, KK; Goldstein, SC; Kim, J; Lush, RM; Maddox, BL; Neuger, AM; Partyka, JS; Perkins, JB; Simonelli, CE; Sullivan, DM, 2011
)
0.37
" Pharmacokinetic monitoring may be a valuable tool for optimizing the use of topotecan and to avoid toxicity seen with high-systemic exposures."( Phase I Study of Topotecan, Ifosfamide, and Etoposide (TIME) with autologous stem cell transplant in refractory cancer: pharmacokinetic and pharmacodynamic correlates.
Dawson, JL; Field, TL; Fields, KK; Goldstein, SC; Kim, J; Lush, RM; Maddox, BL; Neuger, AM; Partyka, JS; Perkins, JB; Simonelli, CE; Sullivan, DM, 2011
)
0.37

Compound-Compound Interactions

Metformin, a biguanide drug used in the treatment of type II diabetes, was evaluated alone and in combination with amifostine, captopril, MESNA or N-acetyl-cysteine (NAC) for its ability to protect.

ExcerptReferenceRelevance
"From July 1986 to July 1989, 40 patients (92% pretreated) with deep-seated, advanced soft tissue sarcomas (STS, 25 patients), Ewing's sarcomas (ES, eight patients), osteosarcomas (OS, three patients) and chondrosarcomas (ChS, four patients) were treated at the University of Munich in a protocol involving regional hyperthermia (RHT) combined with ifosfamide plus etoposide."( Ifosfamide plus etoposide combined with regional hyperthermia in patients with locally advanced sarcomas: a phase II study.
Berger, H; Boehm, E; Denecke, H; Issels, RD; Jauch, KW; Nagele, A; Peter, K; Prenninger, SW; Sauer, H; Wilmanns, W, 1990
)
0.28
"Thirty six patients with advanced solid tumors (24 lung: 3 oat-cell, 14 squamous, 7 adenocarcinomas, 3 soft tissue sarcomas, 6 breast carcinomas; 1 seminoma; 2 ovarian adenocarcinomas) entered a phase II study of high-dose ifosfamide (IF) administered in combination with the uroprotective agent sodium 2-mercapto-ethane-sulfonate (Mesna)."( Phase II study of ifosfamide combined with Mesna uroprotection in advanced non-small-cell lung carcinoma and other solid tumors.
Brema, F; Cinquegrana, A; Nobile, MT; Rosso, R; Santi, L, 1984
)
0.7
") infusion (CIVI) in combination with high-dose cyclophosphamide and granulocyte colony-stimulating factor (G-CSF) in the ambulatory setting to metastatic breast cancer patients."( Phase I study of paclitaxel in combination with cyclophosphamide and granulocyte colony-stimulating factor in metastatic breast cancer patients.
Barnes, CS; Cowan, KH; Denicoff, AM; Goldspiel, BR; Gossard, MR; Kohler, DR; McCabe, M; Noone, MH; O'Shaughnessy, JA; Tolcher, AW; Zujewski, J, 1996
)
0.29
"The purpose of this phase I study is to determine the maximally tolerated doses of paclitaxel and carboplatin (dosed by area under the concentration-time curve) when given at specified times in combination with 6 g/m2 ifosfamide (3 g/m2 at 8 AM on days 1 and 2) with mesna and 5 microg/kg/d filgrastim (from day 4 until the absolute neutrophil count is > 10,000/microL) every 21 days for six cycles."( Phase I trial of dose-escalated paclitaxel and carboplatin in combination with ifosfamide and filgrastim: preliminary results.
Palackdharry, CS, 1996
)
0.47
" Effective modulatory doses of etanidazole could not be given with acceptable toxicity using this schedule."( Dose escalation of the hypoxic cell sensitizer etanidazole combined with ifosfamide, carboplatin, etoposide, and autologous hematopoietic stem cell support.
Antman, KH; Ayash, LJ; Coleman, N; Elias, AD; Frei, E; Ibrahim, J; McCauley, M; Mills, L; Schnipper, L; Schwartz, G; Teicher, BA; Warren, D; Wheeler, C, 1998
)
0.3
"Evaluate response, duration of response, and toxicity of paclitaxel in combination with other drugs known to be effective in non-Hodgkin's lymphoma (NHL)."( Phase II study of paclitaxel in combination with mitoxantrone and ifosfamide/mesna for patients with relapsed or refractory non-Hodgkin's lymphoma after failure to cytarabine/cisplatin combination.
Cabanillas, F; Hagemeister, FB; McLaughlin, P; Preti, A; Rodriguez, J; Rodriguez, MA; Romaguera, JE; Sarris, AH; Younes, A, 1999
)
0.53
" The AIM regimen combined with radiation therapy may be an effective treatment option for this disease."( [Long-term remission of Langerhans cell sarcoma by AIM regimen combined with involved-field irradiation].
Fujikawa, Y; Ichikawa, N; Kirihara, T; Kobayashi, H; Nakamura, S; Sato, K; Shimizu, I; Sumi, M; Takeda, W; Uehara, T; Ueki, T; Ueno, M; Watanabe, M, 2012
)
0.38
"Metformin, a biguanide drug used in the treatment of type II diabetes, was evaluated alone and in combination with amifostine, captopril, MESNA or N-acetyl-cysteine (NAC) for its ability to protect when administered 24 h after irradiation."( Metformin exhibits radiation countermeasures efficacy when used alone or in combination with sulfhydryl containing drugs.
Grdina, DJ; Miller, RC; Murley, JS, 2014
)
0.6

Bioavailability

Recent clinical trials suggest that oral mesna has adequate bioavailability (roughly 50% by urinary thiol measurements) to prevent urotoxicity in high-dose ifosfamide regimens.

ExcerptReferenceRelevance
" Recent clinical trials suggest that oral mesna has adequate bioavailability (roughly 50% by urinary thiol measurements) to prevent urotoxicity in high-dose ifosfamide regimens."( Chemoprotectants for cancer chemotherapy.
Dorr, RT, 1991
)
0.55
" The bioavailability of ifosfamide after oral administration exceeds 95%."( Ifosfamide and mesna.
Dana, WJ; Schoenike, SE, 1990
)
0.63
" We have studied in patients with advanced cancer the feasibility and bioavailability of a subcutaneously administered isotonic and neutral (pH 7) IFO solution given continuously over 10 h for up to 5 days."( Bioavailability of subcutaneous ifosfamide and feasibility of continuous outpatient application in cancer patients.
Brunner, KW; Cerny, T; Küpfer, A; Zeugin, T, 1990
)
0.28
" The bioavailability of oral MESNA is in the range of 20-50% and its unpleasant taste severely limits patient compliance."( [Urinary bioavailability of sodium-2-mercaptoethanesulfonate (Uromitexan) following intravenous, subcutaneous and continuous subcutaneous administration].
Brunner, KW; Cerny, T; Küpfer, A; Roth, B, 1989
)
0.57
"The bioavailability of orally administered sodium 2-mercaptoethane sulfonate (mesna, Uromitexan drink ampoules) was tested in 18 healthy probands and in 5 tumor patients."( Bioavailability of orally administered mesna.
Breuel, HP; Burkert, H; Lücker, PW; Wetzelsberger, N, 1984
)
0.77
"To test the feasibility of uroprotection with sodium 2-mercaptoethane-sulfonate (mesna) in tablet form the bioavailability of mesna tablets was determined in healthy volunteers by HPLC."( Oral bioavailability of mesna tablets.
Borner, M; Cerny, T; Lauterburg, BH; Stofer-Vogel, B, 1993
)
0.82
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The authors performed a dose-escalation trial of ifosfamide with a fixed dosage of etoposide, with mesna uroprotection, in children with multiply recurrent acute leukemia. Increased hydration and dosage of mesna are administered to patients who develop IFO-induced HC.

ExcerptRelevanceReference
" It could be tested using alternate dosage schedules and in combination with other agents in treating this highly resistant neoplasm."( A phase II evaluation of ifosfamide and mesna in unresectable diffuse malignant mesothelioma. A Southwest Oncology Group study.
Balcerzak, SP; Berenberg, JL; Keppen, MD; Metch, B; Militello, L; Pierce, HI; Zidar, BL, 1992
)
0.55
", but on oral dosing of IFO."( Dosing and side-effects of ifosfamide plus mesna.
Araujo, CE; Brade, WP; Herdrich, K; Kachel-Fischer, U, 1991
)
0.54
"Maximal dosing of cytotoxic chemotherapy drugs is often limited by the development of severe nonmyelosuppressive toxicities."( Chemoprotectants for cancer chemotherapy.
Dorr, RT, 1991
)
0.28
" The dose-response profiles were monophasic for some cell lines and biphasic for others."( Inhibition of tumor cell growth in vitro by 2-mercaptoethanesulfonate (mesna) and other thiols.
Blomgren, H; Hallström, M, 1991
)
0.51
"The chemistry, pharmacology, pharmacokinetics, and adverse effects of ifosfamide and mesna are described separately, followed by a discussion of the adverse effects of concurrent ifosfamide and mesna, the clinical spectrum of ifosfamide, and the dosage and administration of the two drugs."( Ifosfamide and mesna.
Dana, WJ; Schoenike, SE, 1990
)
0.86
" It has an increased therapeutic index when given as a fractionated dosage over 3-5 days."( Bioavailability of subcutaneous ifosfamide and feasibility of continuous outpatient application in cancer patients.
Brunner, KW; Cerny, T; Küpfer, A; Zeugin, T, 1990
)
0.28
" There was no experimental evidence that the biphasic dose-response profiles were due to a more complete dimesna formation at high mesna concentrations."( Antitumor activity of 2-mercaptoethanesulfonate (mesna) in vitro.
Blomgren, H; Hallström, M; Hillgren, H, 1990
)
0.75
"One hundred and forty-six patients with advanced malignant disease were treated with 6 different dosage schedules of ifosfamide (IFX)."( Ifosfamide and mesna in the treatment of malignant disease mesna as urothelial protector.
Falkson, CI; Falkson, G; Falkson, HC, 1989
)
0.63
" Mesna has been given in higher dosage (5 g/m2 over 24 h), but otherwise the schedule is as above."( Ifosfamide plus mesna with and without adriamycin in soft tissue sarcoma.
Fisher, C; Harmer, C; McKinna, A; Westbury, G; Wiltshaw, E, 1986
)
1.53
" Following oral mesna dosing the mean peak mesna concentration was 19."( Pharmacokinetics of intravenous and oral sodium 2-mercaptoethane sulphonate (mesna) in normal subjects.
James, CA; Mant, TG; Rogers, HJ, 1987
)
0.85
" Analysis of the results according to sex, age, dosage of ifosfamide and degree of histological differentiation of the tumour cells failed to show any influence of these factors on the therapeutic results."( Treatment of advanced malignancies with ifosfamide under protection with mesna.
Brock, N; Guan, ZZ; He, YJ; Li, GC; Li, JQ, 1988
)
0.51
"The activity of HDI in these pretreated ASTS patients and the apparent circumvention of SDI resistance suggest a real dose-response relationship for ifosfamide and deserve further evaluation."( High-dose ifosfamide: circumvention of resistance to standard-dose ifosfamide in advanced soft tissue sarcomas.
Antoine, E; Brain, E; Fontaine, F; Genin, J; Janin, N; Kayitalire, L; Le Cesne, A; Le Chevalier, T; Spielmann, M; Toussaint, C, 1995
)
0.29
"3 mmol/l) displaces the dose-response curve for acrolein to the left, indicating an increased toxicity of the combination of acrolein plus Dimesna."( Ifosfamide and mesna: effects on the Na/H exchanger activity in renal epithelial cells in culture (LLC-PK1).
Brandis, M; Küpper, N; Mohrmann, M; Schönfield, B,
)
0.69
" The validated limited sampling model provides a starting point for future pharmacokinetic studies in a larger population of patients, which might lead to more insight into the relationships with the pharmacodynamic outcome of carboplatin and may help in achieving more rational dosing of patients on the basis of an AUC determination."( Validation of a limited sampling model for carboplatin in a high-dose chemotherapy combination.
Beijnen, JH; Maes, RA; Rodenhuis, S; van Tellingen, O; van Warmerdam, LJ, 1994
)
0.29
" The authors performed a dose-escalation trial of ifosfamide with a fixed dosage of etoposide, with mesna uroprotection, in children with multiply recurrent acute leukemia."( Ifosfamide with mesna uroprotection and etoposide in recurrent, refractory acute leukemia in childhood. A Pediatric Oncology Group Study.
Bell, B; Bernstein, ML; Buchanan, GR; Devine, S; Dreyer, Z; Grier, H; Krischer, J; Kung, F; Land, V; Whitehead, VM, 1993
)
0.85
" Our studies suggest a dose-response relationship for ifosfamide."( Single-agent ifosfamide studies in sarcomas of soft tissue and bone: the M.D. Anderson experience.
Benjamin, RS; Legha, SS; Nicaise, C; Patel, SR, 1993
)
0.29
" mesna, which means that uroprotection can be achieved with longer dosing intervals."( Oral bioavailability of mesna tablets.
Borner, M; Cerny, T; Lauterburg, BH; Stofer-Vogel, B, 1993
)
1.5
"Patients were assigned to dosage cohorts separately on the basis of prior exposure to the platinum alkylating agents cisplatin or carboplatin (n = 20) or the absence of such exposure (n = 9)."( A phase I study of ifosfamide with Mesna given daily for 3 consecutive days to children with malignant solid tumors.
Avery, L; Bowman, L; Douglass, EC; Marina, N; Meyer, WH; Ochs, J; Pratt, CB; Thompson, EI; Wilimas, J, 1993
)
0.56
"Myelosuppression was dose-limiting at the second dosage level (2560 mg/m2/d) for patients previously treated with platinum and at the third dosage level (3072 mg/m2/d) for those not previously treated with platinum."( A phase I study of ifosfamide with Mesna given daily for 3 consecutive days to children with malignant solid tumors.
Avery, L; Bowman, L; Douglass, EC; Marina, N; Meyer, WH; Ochs, J; Pratt, CB; Thompson, EI; Wilimas, J, 1993
)
0.56
"The patients were assigned to dosage cohorts separated on the basis of prior exposure to cisplatin (n = 10) or the absence of such exposure (n = 10)."( A phase I study of ifosfamide given on alternate days to treat children with brain tumors.
Avery, L; Douglass, EC; Heideman, R; Kellie, SJ; Kovnar, EH; Kun, L; Pratt, CB, 1993
)
0.29
" This review summarizes dosing schedules and the incidence of hematuria in 47 clinical studies, in which oral mesna was given to at least 1,986 patients who received more than 6,475 courses of ifosfamide."( Oral administration of mesna with ifosfamide.
Goren, MP, 1996
)
0.82
" For this first step a daily dosage of 300 mg/m2 of body surface resulted in only moderate leukopenia, whereas a daily dosage of 450 mg/m2 caused severe leukopenia."( Development of a canine chemotherapeutic model with ifosfamide.
Chao, EY; Donehower, RC; Frassica, FJ; Ikeda, K; Inoue, N; Tomita, K, 1996
)
0.29
" There is a definite positive dose-response curve, and bolus administration appears to be more active than continuous infusion."( High-dose ifosfamide in bone and soft tissue sarcomas: results of phase II and pilot studies--dose-response and schedule dependence.
Benjamin, RS; Burgess, MA; Hays, C; Papadopolous, N; Patel, SR; Plager, C; Vadhan-Raj, S, 1997
)
0.3
" Mesna was administered intravenously at a 20% of the ifosfamide dosage before ifosfamide and orally at 40% after 4 and 8 hours from the ifosfamide infusion."( Second line chemotherapy with ifosfamide as outpatient treatment for advanced bladder cancer.
Pensa, F; Pronzato, P; Tani, F; Vaira, F; Vanoli, M; Vigani, A, 1997
)
1.21
"Ifosfamide has important activity in pretreated soft tissue sarcomas (STS), and recent data support a clinically significant dose-response relationship for this agent."( Phase II study of continuous-infusion high-dose ifosfamide in advanced and/or metastatic pretreated soft tissue sarcomas.
Antimi, M; Gatti, C; Palmeri, S; Palumbo, R; Raffo, P; Toma, S; Villani, G, 1997
)
0.3
"The purpose of this study was to make evidence-based recommendations regarding the mode, dosage and schedule of delivery of concomitant mesna (sodium-2-mercaptoethanesulfonate) to protect against ifosfamide-induced uroepithelial toxicity."( Use of mesna to prevent ifosfamide-induced urotoxicity.
Moore, MJ; Siu, LL, 1998
)
0.96
"Adriamycin (ADM) and ifosfamide (IFO) are the two most active agents in the treatment of soft tissue sarcomas (STS) with a clear dose-response relationship."( High-dose ifosfamide plus adriamycin in the treatment of adult advanced soft tissue sarcomas: is it feasible?
Aapro, MS; De Braud, F; De Pas, T; Fazio, N; Goldhirsch, A; Munzone, E; Nolè, F; Orlando, L; Zampino, MG, 1998
)
0.3
" METHODS FOR REDUCING TOXICITY: There are several methods by which one can reduce the toxicity of cancer chemotherapy, such as the application of rationally designed dosage schedules, alternative routes of administration, biochemical modulation, and the development of drug camers and analogs."( [Anticancer chemotherapy. Prevention of complications].
Brion, N; Paule, B, 1998
)
0.3
" Following 1 cycle of MAID at the standard dose, four patients were to be treated at each of five dosage levels: +25%, +45%, +65%, +85%, +100%."( Phase I-II trial of intensification of the MAID regimen with support of lenograstim (rHuG-CSF) in patients with advanced soft-tissue sarcoma (STS).
Bui, BN; Chevallier, B; Chevreau, C; Coindre, JM; Cour-Chabernaud, V; Gil, B; Krakowski, I; Maugard, C; Mihura, J, 1999
)
0.3
"Mesna: (1) Mesna, dosed as detailed in these guidelines, is recommended to decrease the incidence of standard-dose ifosfamide-associated urothelial toxicity."( American Society of Clinical Oncology clinical practice guidelines for the use of chemotherapy and radiotherapy protectants.
Broder, G; Cohen, GI; Gradishar, WJ; Green, DM; Hensley, ML; Langdon, RJ; Lindley, C; Meropol, NJ; Mitchell, RB; Negrin, R; Pfister, DG; Schuchter, LM; Szatrowski, TP; Thigpen, JT; Von Hoff, D; Wasserman, TH; Winer, EP, 1999
)
1.75
"5 g/m(2)/day as 72-hour continuous infusion with mesna at the same dosage and schedule."( Treatment of advanced soft tissue sarcomas with ifosfamide and doxorubicin combination chemotherapy.
Altundağ, K; Baltali, E; Barişta, I; Celik, I; Firat, D; Güler, N; Güllü, I; Kars, A; Ozişik, Y; Tekuzman, G; Türker, A; Uner, A; Yalçin, S; Zengin, N, 2000
)
0.56
" Adequate dosing of either drug is necessary for protecting the cells from toxic effects of alkylating agents."( Blood thiols following amifostine and mesna infusions, a pediatric oncology group study.
Aktas, MK; Bernstein, ML; Dubowy, RL; Fahey, RC; Karjoo, S; Newton, GL; Sadowitz, PD; Sayin, OA; Souid, AK, 2001
)
0.58
"The profile of mesna excretion after intravenous and oral dosing in these children was similar to that in reported studies of ifosfamide-treated adults."( Urine mesna excretion after intravenous and oral dosing in ifosfamide-treated children.
Bush, DA; Epelman, S; Goren, MP, 2004
)
1.16
" DPIVM may allow significant financial savings in centers and hospital departments using high-cost pharmaceuticals susceptible of customized dosing --e."( [Financial assessment of device for the preparation of intravenous mixtures in hospital pharmacy].
Bonafont Pujol, X; Casado Collado, A; Clemente Bautista, S; Herdman, M; Jódar Masanés, R; Luengo Pascual, L; Napal Lecumberri, V; Serrano Padilla, G,
)
0.13
" After an initial bolus of 1 g/m(2) of mesna, mesna was applied at a dosage of 5 g/m(2) concomitantly with ifosfamide followed by additional dosages of 200 mg 3 times at 4-hour intervals after termination of the ifosfamide infusion."( Ifosfamide/mesna as salvage therapy in platinum pretreated ovarian cancer patients--long-term results of a phase II study.
Baur, M; Dittrich, C; Fazeny-Doerner, B; Hudec, M; Salzer, H; Sevelda, P, 2006
)
0.99
" Once MTD was defined, we expanded this dosing cohort to include patients with high-risk lymphoma due to activity seen during dose escalation."( Phase I Study of Topotecan, Ifosfamide, and Etoposide (TIME) with autologous stem cell transplant in refractory cancer: pharmacokinetic and pharmacodynamic correlates.
Dawson, JL; Field, TL; Fields, KK; Goldstein, SC; Kim, J; Lush, RM; Maddox, BL; Neuger, AM; Partyka, JS; Perkins, JB; Simonelli, CE; Sullivan, DM, 2011
)
0.37
" MSH provoked a dose-response reversal of the redox state of aged plasma, and the thiol action was confirmed by in vivo experiments."( The control of hyperhomocysteinemia through thiol exchange mechanisms by mesna.
Bartalini, S; Coppo, L; Di Giuseppe, D; Di Simplicio, P; Frosali, S; Margaritis, A; Priora, R; Summa, D; Ulivelli, M, 2014
)
0.63
" It is therefore necessary to investigate ketamine locally and systematically with various dosing schedules in order to reduce the bladder damage secondary to oxazaphosphorine-alkylating agents and these results may widen the spectrum of ketamine."( Protective effect of ketamine against hemorrhagic cystitis in rats receiving ifosfamide.
Onag, A; Ozguven, AA; Taneli, F; Ulman, C; Vatansever, S; Yılmaz, O,
)
0.13
" Increased hydration and dosage of mesna are administered to patients who develop IFO-induced HC; they also receive 24-h continuous infusion of mesna in subsequent treatment cycles."( A retrospective study of treatment and prophylaxis of ifosfamide-induced hemorrhagic cystitis in pediatric and adolescent and young adult (AYA) patients with solid tumors.
Kumamoto, T; Makino, Y; Ogawa, C; Saito, Y; Tamai, I; Terakado, H, 2016
)
0.71
"The incidence of IFO-induced HC may be associated with the dosage of IFO."( A retrospective study of treatment and prophylaxis of ifosfamide-induced hemorrhagic cystitis in pediatric and adolescent and young adult (AYA) patients with solid tumors.
Kumamoto, T; Makino, Y; Ogawa, C; Saito, Y; Tamai, I; Terakado, H, 2016
)
0.43
" In conclusion, hyperhydration with forced diuresis combined with aggressive mesna dosing is an effective strategy in preventing severe PTCy-associated HC, subsequently preventing any negative impact on transplant outcome."( Use of high-dose mesna and hyperhydration leads to lower incidence of hemorrhagic cystitis after posttransplant cyclophosphamide-based allogeneic transplantation.
Al Malki, MM; Aldoss, I; Ali, H; Aribi, A; Arslan, S; Artz, A; Cao, T; Chen, J; Dadwal, S; Forman, SJ; Karras, N; Koller, P; Mac, S; Marcucci, G; Nakamura, R; Ngo, D; Pullarkat, V; Salhotra, A; Sandhu, K; Stein, A; Yang, D, 2021
)
1.19
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organosulfonic acidAn organic derivative of sulfonic acid in which the sulfo group is linked directly to carbon.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency12.58930.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency43.64860.007215.758889.3584AID1224835
15-lipoxygenase, partialHomo sapiens (human)Potency6.30960.012610.691788.5700AID887
RAR-related orphan receptor gammaMus musculus (house mouse)Potency23.71010.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686978
GLI family zinc finger 3Homo sapiens (human)Potency29.84930.000714.592883.7951AID1259369
Microtubule-associated protein tauHomo sapiens (human)Potency18.25630.180013.557439.8107AID1460; AID1468
progesterone receptorHomo sapiens (human)Potency2.98490.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.70900.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.00210.001310.157742.8575AID1259256
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency12.74930.001530.607315,848.9004AID1259403
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency60.83870.001024.504861.6448AID743215
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency28.18380.060110.745337.9330AID492961
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[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 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 (114)

Assay IDTitleYearJournalArticle
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID382491Cytotoxicity against human pulp cells by MTT method2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells.
AID116961Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia sensitive cells for a dose of 100 mg/kg.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: a membrane-permeating prodrug of 5-fluoro-2'-deoxyuridylic acid (FdUMP).
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).
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).
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.
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.
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).
AID116948Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia resistant cells for a dose of 100 mg/kg.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: a membrane-permeating prodrug of 5-fluoro-2'-deoxyuridylic acid (FdUMP).
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.
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.
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.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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).
AID382489Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
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).
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.
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.
AID382492Cytotoxicity against human periodontal ligament fibroblast by MTT method2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells.
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).
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.
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.
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).
AID1808091Drug metabolism in mini gut model assessed as metabolite formation by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Searching for New Microbiome-Targeted Therapeutics through a Drug Repurposing Approach.
AID1808092Drug metabolism in human gut microbes assessed as metabolite formation by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Searching for New Microbiome-Targeted Therapeutics through a Drug Repurposing Approach.
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).
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.
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).
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).
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).
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).
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.
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.
AID115009Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia sensitive cells compared with controls for a dose of 100 mg/kg.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: a membrane-permeating prodrug of 5-fluoro-2'-deoxyuridylic acid (FdUMP).
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.
AID93938Concentration required to reduce the viability of L1210 cells by 50% after 1-h incubation at 37 degrees C1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Aldophosphamide acetal diacetate and structural analogues: synthesis and cytotoxicity studies.
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).
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).
AID382487Cytotoxicity against human HSC2 by MTT method2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells.
AID122611Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia resistant cells for a dose of 100 mg/kg.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: a membrane-permeating prodrug of 5-fluoro-2'-deoxyuridylic acid (FdUMP).
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID382490Cytotoxicity against human gingival fibroblast by MTT method2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells.
AID114997Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia resistant cells compared with controls for a dose of 100 mg/kg.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: a membrane-permeating prodrug of 5-fluoro-2'-deoxyuridylic acid (FdUMP).
AID382488Cytotoxicity against human HSC4 cells by MTT method2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells.
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.
AID122623Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia sensitive cells for a dose of 100 mg/kg.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: a membrane-permeating prodrug of 5-fluoro-2'-deoxyuridylic acid (FdUMP).
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.
AID1808093Stability of compound in mini gut model at 24 hrs by LC-MS analysis2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Searching for New Microbiome-Targeted Therapeutics through a Drug Repurposing Approach.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,174)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990305 (25.98)18.7374
1990's369 (31.43)18.2507
2000's265 (22.57)29.6817
2010's193 (16.44)24.3611
2020's42 (3.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 74.03

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index74.03 (24.57)
Research Supply Index7.30 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index132.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (74.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials251 (20.32%)5.53%
Reviews96 (7.77%)6.00%
Case Studies126 (10.20%)4.05%
Observational0 (0.00%)0.25%
Other762 (61.70%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (36)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Allogeneic Hematopoietic Stem Cell Transplant for Patients With Primary Immune Deficiencies [NCT01652092]30 participants (Anticipated)Interventional2012-09-04Recruiting
A Phase I/II Trial of Neoadjuvant ADI-PEG 20 in Combination With Ifosfamide and Radiotherapy in Soft Tissue Sarcoma (STS) [NCT05813327]Phase 1/Phase 235 participants (Anticipated)Interventional2024-01-31Not yet recruiting
Phase III Randomized Trial of Post-Radiation Chemotherapy in Patients With Newly Diagnosed Ependymoma Ages 1 to 21 Years [NCT01096368]Phase 3479 participants (Actual)Interventional2010-05-07Active, not recruiting
Evaluating Different Modalities for Pleural Adhesiolysis at Assuit University Hospital [NCT03172052]Phase 4100 participants (Anticipated)Interventional2017-08-01Not yet recruiting
Pilot Study Using Myeloablative Busulfan/Melphalan (BuMel) Consolidation Following Induction Chemotherapy for Patients With Newly Diagnosed High-Risk Neuroblastoma [NCT01798004]Phase 1150 participants (Actual)Interventional2013-04-08Active, not recruiting
Autologous Peripheral Blood Stem Cell Transplant for Germ Cell Tumors [NCT00432094]Phase 223 participants (Actual)Interventional2006-12-19Completed
A Pilot Phase II Study for Children With Infantile Fibrosarcoma [NCT00072280]Phase 27 participants (Actual)Interventional2004-11-30Terminated(stopped due to Due to poor accrual)
A Phase 2 Trial of Chemotherapy Followed by Response-Based Whole Ventricular &Amp; Spinal Canal Irradiation (WVSCI) for Patients With Localized Non-Germinomatous Central Nervous System Germ Cell Tumor [NCT04684368]Phase 2160 participants (Anticipated)Interventional2021-07-13Recruiting
Feasibility and Dose Discovery Analysis of Zoledronic Acid With Concurrent Chemotherapy in the Treatment of Newly Diagnosed Metastatic Osteosarcoma [NCT00742924]Phase 124 participants (Actual)Interventional2008-08-31Completed
Cysteine-lowering Treatment With Mesna Against Obesity: Phase I Dose-finding Study [NCT04449536]Phase 125 participants (Actual)Interventional2020-11-02Completed
Treatment of Temporomandibular Joint Internal Derangement Using MESNA Injection [NCT05882604]12 participants (Anticipated)Interventional2023-05-01Recruiting
A Phase 3 Study of Sodium Thiosulfate for Reduction of Cisplatin-Induced Ototoxicity in Children With Average-Risk Medulloblastoma and Reduced Therapy in Children With Medulloblastoma With Low-Risk Features [NCT05382338]Phase 3225 participants (Anticipated)Interventional2023-02-20Recruiting
Phase I/II Study of Metastatic Cancer That Expresses Her-2 Using Lymphodepleting Conditioning Followed by Infusion of Anti-Her-2 Gene Engineered Lymphocytes [NCT00924287]Phase 1/Phase 21 participants (Actual)Interventional2008-11-30Terminated(stopped due to This study was terminated after the first patient treated on study died as a result of the treatment.)
Sequential, Related Donor Partial Liver Transplantation Followed by Bone Marrow Transplantation for Fibrolamellar or Non-fibrolamellar Hepatocellular Carcinoma (HCC) Including Fibrolamellar HCC [NCT02702960]Phase 20 participants (Actual)Interventional2016-03-31Withdrawn(stopped due to This study was withdrawn due to lack of necessary resources from the liver transplant surgical group.)
A Multi-Center, Phase II Trial of HLA-Mismatched Unrelated Donor Bone Marrow Transplantation With Post-Transplantation Cyclophosphamide for Patients With Hematologic Malignancies [NCT02793544]Phase 280 participants (Actual)Interventional2016-12-31Completed
A Phase I/II Study of Llme Treated Non-Myeloablative Allogeneic Hematopoietic Stem Cell Transplantation for Patients With Hematological Malignancies [NCT00429416]Phase 1/Phase 214 participants (Actual)Interventional2004-03-31Completed
Dose Escalation of Total Marrow Irradiation Added to an Alkylator-Intense Conditioning Regimen for Patients With High Risk or Relapsed Solid Tumors [NCT00623077]Phase 123 participants (Actual)Interventional2005-08-31Terminated(stopped due to Replaced by another study)
Magnetic Resonance Based Non-Invasive Thermometry for Hyperthermic Treatment of Extremity Soft Tissue Sarcomas: A Multimodal Phase I/II Study [NCT00093509]Phase 1/Phase 215 participants (Actual)Interventional1999-11-30Completed
Pilot Study of Cisplatin, Etoposide, Bleomycin and Escalating Dose Cyclophosphamide Therapy for Children With High Risk Malignant Germ Cell Tumors [NCT00066482]19 participants (Actual)Interventional2004-07-31Completed
Umbilical Cord Blood Transplantation From Unrelated Donors [NCT03016806]Phase 130 participants (Anticipated)Interventional2015-06-30Recruiting
A Phase II Study of Combination Nilotinib and Hyper-CVAD in Patients Newly Diagnosed With Philadelphia-Chromosome Positive Acute Lymphoblastic Leukemia or Chronic Myeloid Leukemia Blast-Phase Lymphoid Lineage [NCT01670084]Phase 20 participants (Actual)Interventional2012-12-31Withdrawn(stopped due to No Accrual)
MESNA Zur Prophylaxe Der Kontrastmittel-Induzierten Nephropathie [NCT00223548]Phase 2106 participants Interventional2002-10-31Completed
A Phase III Randomized Trial of Steroids + Tyrosine Kinase Inhibitor (TKI) Induction With Chemotherapy or Blinatumomab for Newly Diagnosed BCR-ABL-Positive Acute Lymphoblastic Leukemia (ALL) in Adults [NCT04530565]Phase 3348 participants (Anticipated)Interventional2021-01-25Recruiting
The Effects of 12 mg/kg Intravenous Mesna on Plasma Total Homocysteine Concentration in Patients With End-stage Renal Disease Requiring Hemodialysis [NCT00524199]Phase 210 participants (Actual)Interventional2007-03-31Completed
Phase Ib/II Study of the Combination of Low-Intensity Chemotherapy and Tagraxofusp in Patients With Acute Lymphoblastic Leukemia (ALL) [NCT05032183]Phase 1/Phase 240 participants (Anticipated)Interventional2022-02-17Recruiting
A Randomized Controlled Multi-center Clinical Trial on Treatment of Stage I/II NK/T Cell Lymphoma With DDGP Regiment (Gemcitabine,Pegaspargase,Cisplatin,Dexamethasone) [NCT01501136]Phase 4200 participants (Anticipated)Interventional2011-01-31Recruiting
Haploidentical Donor Hematopoietic Stem Cell Transplantation [NCT02660281]Phase 174 participants (Actual)Interventional2015-10-31Completed
Lymphodepletion Plus Adoptive Cell Transfer With or Without Dendritic Cell Immunization in Patients With Metastatic Melanoma [NCT00338377]Phase 21,230 participants (Actual)Interventional2006-02-01Active, not recruiting
Phase I Pilot Study of Multiple Cycles of High Dose Chemotherapy With Peripheral Blood Stem Cell Infusions In Advanced Stage Neuroblastoma [NCT00002740]Phase 130 participants (Anticipated)Interventional1996-05-31Completed
Phase II Trial Investigating Tailoring First-Line Therapy For Advanced Stage Diffuse Large B-Cell Non-Hodgkin's Lymphoma Based on Mid-Treatment Positron Emission Tomography (PET) Scan Results [NCT00324467]Phase 2150 participants (Actual)Interventional2006-08-31Active, not recruiting
Phase II Study of Neoadjuvant Vincristine, Ifosfamide, Doxorubicin, and AND G-CSF in Children With Advanced Stage Non-Rhabdomyosarcoma Soft Tissue Sarcomas [NCT00002804]Phase 243 participants (Actual)Interventional1996-09-30Completed
Alkylator-Intense Conditioning Followed by Autologous Transplantation for Patients With High Risk or Relapsed Solid or CNS Tumors [NCT01505569]20 participants (Anticipated)Interventional2011-10-20Recruiting
An Open-Label Phase 1/2 Multi-Arm Study of DS-1594b as a Single-Agent and in Combination With Azacitidine and Venetoclax or Mini-HCVD for the Treatment of Patients With Acute Myeloid Leukemia (AML) and Acute Lymphoblastic Leukemia (ALL) [NCT04752163]Phase 1/Phase 217 participants (Actual)Interventional2021-03-25Completed
Effects of Rolapitant on Nausea/Vomiting in Patients With Sarcoma Receiving Multi-Day Highly Emetogenic Chemotherapy (HEC) With Doxorubicin and Ifosfamide Regimen (AI) [NCT02732015]Phase 237 participants (Actual)Interventional2016-10-12Terminated(stopped due to Terminated per PI's request)
Chemically Assisted Capsulectomy-A New Clinical Approach [NCT00758667]20 participants (Actual)Interventional2005-01-31Terminated(stopped due to preliminary analysis showed no difference)
A Randomised, Double-Blind, Double-Dummy, Placebo-Controlled, Three-Way Cross-over Study to Evaluate the Effect of AF-219 on Methacholine Hyper-Reactivity in Subjects With Asthma [NCT01993329]Phase 220 participants (Actual)Interventional2013-12-16Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00072280 (1) [back to overview]"Failure-free Survival (FFS) in Chemotherapy Plus Possible Surgery Arm"
NCT00429416 (5) [back to overview]Number of Patients Who Achieve a CD4 Count > 200/Micro-liters
NCT00429416 (5) [back to overview]Rate of Engraftment of Non-Myeloablative Transplants
NCT00429416 (5) [back to overview]Rate of Serious Infectious Complications
NCT00429416 (5) [back to overview]Safety of CD34+ Stem Cell Infusions Followed by LLME as Measured by 100-Day Mortality
NCT00429416 (5) [back to overview]Incidence of Grade II-IV Acute Graft-Versus-Host-Disease (GVHD)
NCT00432094 (5) [back to overview]Disease-free Survival (DFS)
NCT00432094 (5) [back to overview]Engraftment of Neutrophils
NCT00432094 (5) [back to overview]Engraftment of Platelets
NCT00432094 (5) [back to overview]Numbers of Patients Unable to Mobilize Peripheral Blood Stem Cells
NCT00432094 (5) [back to overview]Overall Survival (OS)
NCT00742924 (1) [back to overview]Limiting Toxicity
NCT00758667 (2) [back to overview]Compare Number of Patients With Adverse Events in the Mesna Group vs the Standard of Care
NCT00758667 (2) [back to overview]Compare Number of Patients With Capsular Contracture in Mesna Group vs Standard of Care
NCT00924287 (2) [back to overview]Number of Participants With Adverse Events
NCT00924287 (2) [back to overview]Number of Participants With In Vivo Survival of Transfused Cells
NCT01096368 (10) [back to overview]EFS in Children Who Have Completely Resected Ependymoma at Initial Surgery and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only
NCT01096368 (10) [back to overview]EFS of Children With Incompletely Resected Ependymoma Who Are Unable to Achieve a Complete Response (CR) by Post-operative Induction Chemotherapy or by Second Surgery and Who Are Non-randomly Assigned to Receive Maintenance Chemotherapy
NCT01096368 (10) [back to overview]EFS of Children With Supratentorial Classic Ependymoma Who Achieve Complete Resection at First or Second Surgery or Children Who Achieve Complete Response (CR) After Induction Chemo and Who Are Non-randomly Assigned to Observation
NCT01096368 (10) [back to overview]EFS With Incomplete Resection After Initial Surgery, Then Achieved CR After Induction Chemotherapy or GTR/NTR After Second Surgery and Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only
NCT01096368 (10) [back to overview]Event-free Survival (EFS) in Children Who Have Completely Resected Ependymoma or Achieved CR and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only
NCT01096368 (10) [back to overview]OS in Children Who Have Completely Resected Ependymoma at Initial Surgery and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only.
NCT01096368 (10) [back to overview]OS in Children With Incomplete Resection After Initial Surgery Who Then Achieved CR After Induction Chemotherapy or GTR/NTR After Second Surgery and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only
NCT01096368 (10) [back to overview]OS of Children With Incompletely Resected Ependymoma Who Are Unable to Achieve a Complete Response (CR) by Post-operative Induction Chemotherapy or by Second Surgery and Who Are Non-randomly Assigned to Receive Maintenance Chemotherapy
NCT01096368 (10) [back to overview]OS of Children With Supratentorial Classic Ependymoma Who Achieve Complete Resection at First or Second Surgery or Children Who Achieve Complete Response (CR) After Induction Chemo and Who Are Non-randomly Assigned to Observation
NCT01096368 (10) [back to overview]Overall Survival (OS) in Children Who Have Completely Resected Ependymoma or Achieved CR and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only
NCT01798004 (1) [back to overview]The Tolerability of BuMel Regimen
NCT01993329 (2) [back to overview]Provocative Concentration (PC20) After Methacholine Challenge
NCT01993329 (2) [back to overview]Highest FEV1 After Methacholine Challenge
NCT02732015 (1) [back to overview]Number of Participants With Complete Response (CR) of Rolapitant Hydrochloride Administered as a Single-dose

"Failure-free Survival (FFS) in Chemotherapy Plus Possible Surgery Arm"

Failure is defined as the occurrence of one of the following: disease progression, defined as at least a 20% increase in the disease measurement, taking as reference the smallest disease measurement recorded since the start of treatment, or the appearance of one or more new lesions; relapse (defined with same criteria as for disease progression) after response; or death as a first event. Data will be summarized as number of eligible patients in each of the following categories at the time of data cutoff for analyses of 5-year FFS: 1)Failed; 2)Failure-free through 5 years of follow-up; 3)Failure-free until data cutoff (if less than 5 years of follow-up); 4)Withdrew from study; 5)Lost to follow-up. NOTE: Reported data are through March 2008 (see Caveats section). (NCT00072280)
Timeframe: Study enrollment until failure, completion of follow-up, or completion of 5-year FFS analyses (up to 5 years)

Interventionparticipants (Number)
FailedFailure-free through 5 years of follow-upFailure-free at cutoff (if < 5 years follow-up)Withdrew from studyLost to follow-up
Chemotherapy Plus Possible Surgery10100

[back to top]

Number of Patients Who Achieve a CD4 Count > 200/Micro-liters

Determine the number of patients who achieve a CD4 count > 200/micro-liters by 60 days after transplant. (NCT00429416)
Timeframe: Through 60 Days Post Transplant

Interventionparticipants (Number)
LLME to Decrease GVHD Following HSC T13

[back to top]

Rate of Engraftment of Non-Myeloablative Transplants

Determine the engraftment rate of non-myeloablative transplants using CD34+ stem cells and LLME treated CD34- products. (NCT00429416)
Timeframe: Through 30 days post-transplant

Interventionparticipants (Number)
LLME to Decrease GVHD Following HSC T13

[back to top]

Rate of Serious Infectious Complications

"Determine the rate of serious infectious complications. A serious infection will be defined as any requiring hospitalization or parenteral therapy.~CD4 counts will be measured monthly for the first 3 months after transplant." (NCT00429416)
Timeframe: Through 3 months post-transplant

Interventionparticipants (Number)
LLME to Decrease GVHD Following HSC T2

[back to top]

Safety of CD34+ Stem Cell Infusions Followed by LLME as Measured by 100-Day Mortality

"Determine the safety of CD34+ stem cell infusions followed by the LLME treated CD34- fraction. This includes monitoring the patients for any side effects associated with the LLME treated cell infusion or any other unexpected adverse events.~This regimen will be gauged as to its safety using 100 day mortality as the measured endpoint. Deaths from all causes will be included." (NCT00429416)
Timeframe: Through 100 days post-transplant or death

Interventionparticipants (Number)
LLME to Decrease GVHD Following HSC T1

[back to top]

Incidence of Grade II-IV Acute Graft-Versus-Host-Disease (GVHD)

Determine the incidence of grade II-IV acute GVHD after administration of grafts when combined with Cyclosporine/Mycophenolate Mofetil for GVHD prophylaxis. GVHD assessments occur daily as an in patient and at each out patient visit. (NCT00429416)
Timeframe: Through 24 months post-treatment

Interventionparticipants (Number)
Developed grade II-IV GVHDDeveloped cGVHD (Chronic GVHD)
LLME to Decrease GVHD Following HSC T31

[back to top]

Disease-free Survival (DFS)

The number of patients who survive without any signs of symptions of that cancer or any other cancer. (NCT00432094)
Timeframe: 1 Year

Interventionpercentage of participants (Mean)
2 Transplants64
1 Transplant44

[back to top]

Engraftment of Neutrophils

Neutrophil engraftment is defined as the first day of three consecutive days where the neutrophil count (absolute neutrophil count) is 500 cells/mm3 (0.5 x 109/L) or greater. (NCT00432094)
Timeframe: Day 42

InterventionParticipants (Count of Participants)
2 Transplants13
1 Transplant9

[back to top]

Engraftment of Platelets

Platelet engraftment is defined as 20,000/mm^3 (20 x 10^9/L) for 3 consecutive days unsupported by a platelet transfusion. (NCT00432094)
Timeframe: Day 100

Interventionparticipants (Number)
2 Transplants13
1 Transplant8

[back to top]

Numbers of Patients Unable to Mobilize Peripheral Blood Stem Cells

Number of patients unable to achieve adequate stem cell mobilization, need to undergo one or tandem transplantation. Stem cell mobilization = A process in which certain drugs are used to cause the movement of stem cells from the bone marrow into the blood. The stem cells can be collected and stored. They may be used later to replace the bone marrow during a stem cell transplant. (NCT00432094)
Timeframe: Pre-Transplant

InterventionParticipants (Count of Participants)
2 Transplants0
1 Transplant0

[back to top]

Overall Survival (OS)

The percentage of people in a study or treatment group who are alive for a certain period of time after they were diagnosed with or treated for a disease, such as cancer. Also called survival rate. (NCT00432094)
Timeframe: 1 Year

Interventionpercentage of participants (Mean)
2 Transplants86
1 Transplant56

[back to top]

Limiting Toxicity

"The occurrence of Limiting Toxicity defined as Any CTC AE version 4 Grade 3 and 4 non-hematologic toxicity thought to be possibly, probably or definitely related to zoledronic acid with the specific exclusion of:~Grade 3 nausea and vomiting controlled with adequate antiemetic prophylaxis.~Grade 3 transaminase (AST/ALT) that occurs during the evaluation period but resolves to ≤ Grade 2, before the planned dose of therapy after definitive surgery.~Grade 3 fever or infection.~Grade 3 or 4 hypocalcemia (see Section 5.1.1)~Grade 3 mucositis.~Grade 3 fatigue that returns to ≤ Grade 2, before the planned dose of therapy after definitive surgery.~Grade 3 joint range of motion, decreased or joint effusion that is related to the primary tumor." (NCT00742924)
Timeframe: Enrollment through the first 12 weeks of therapy.

Interventionparticipants (Number)
Arm 1- Chemotherapy and 1.2 mg/m2 Zoledronic Acid1
Arm 2 - Chemotherapy and 2.3 mg/m2 Zoledronic Acid1
Arm 3 - Chemotherapy and 3.5 mg/m2 Zoledronic Acid3
Chemotherapy and 2.3 mg/m2 Zoledronic Acid After MTD2

[back to top]

Compare Number of Patients With Adverse Events in the Mesna Group vs the Standard of Care

(NCT00758667)
Timeframe: one year

Interventionparticipants (Number)
Standard0
Mesna0

[back to top]

Compare Number of Patients With Capsular Contracture in Mesna Group vs Standard of Care

(NCT00758667)
Timeframe: one year

Interventionparticipants (Number)
Standard2
Mesna4

[back to top]

Number of Participants With Adverse Events

Here are the number of participants with adverse events. For the detailed list of adverse events see the adverse event module. (NCT00924287)
Timeframe: 12 days

InterventionParticipants (Number)
Metastatic Cancer1

[back to top]

Number of Participants With In Vivo Survival of Transfused Cells

In-vivo survival of infused cells is determined by analysis of the sequence of the variable region of the T cell receptor or flow cytometry (FACS). (NCT00924287)
Timeframe: 12 days

InterventionParticipants (Number)
Metastatic Cancer1

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EFS in Children Who Have Completely Resected Ependymoma at Initial Surgery and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only

Kaplan-Meier estimates of EFS are calculated from randomization date to first occurrence of disease progression, disease recurrence, second malignant neoplasm, or death from any cause. The comparison between randomized arms (post-radiation maintenance chemotherapy versus post-radiation observation only) for this stratum is conveyed by the hazard ratio and 95% Wald confidence interval. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of EFS are presented.

Interventionpercentage of participants (Number)
Arm II: Randomized to Radiation With Maintenance Chemotherapy in Stratum 172.7
Arm III: Randomized to Radiation Only in Stratum 162.9

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EFS of Children With Incompletely Resected Ependymoma Who Are Unable to Achieve a Complete Response (CR) by Post-operative Induction Chemotherapy or by Second Surgery and Who Are Non-randomly Assigned to Receive Maintenance Chemotherapy

The Kaplan-Meier estimate of EFS is calculated from enrollment date to first occurrence of disease progression, disease recurrence, second malignant neoplasm, or death from any cause. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of EFS are presented.

Interventionpercentage of participants (Number)
Arm IV: Nonrandomly Assigned to Arm II Treatment33.6

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EFS of Children With Supratentorial Classic Ependymoma Who Achieve Complete Resection at First or Second Surgery or Children Who Achieve Complete Response (CR) After Induction Chemo and Who Are Non-randomly Assigned to Observation

The Kaplan-Meier estimate of EFS is calculated from enrollment date to first occurrence of disease progression, disease recurrence, second malignant neoplasm, or death from any cause. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of EFS are presented.

Interventionpercentage of participants (Number)
Arm I: Observation66.9

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EFS With Incomplete Resection After Initial Surgery, Then Achieved CR After Induction Chemotherapy or GTR/NTR After Second Surgery and Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only

Kaplan-Meier estimates of EFS are calculated from randomization date to first occurrence of disease progression, disease recurrence, second malignant neoplasm, or death from any cause. The comparison between randomized arms (post-radiation maintenance chemotherapy versus post-radiation observation only) for this stratum is conveyed by the hazard ratio and 95% Wald confidence interval. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of EFS are presented.

Interventionpercentage of participants (Number)
Arm II: Randomized to Radiation With Maintenance Chemotherapy in Stratum 241.7
Arm III: Randomized to Radiation Only in Stratum 267.5

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Event-free Survival (EFS) in Children Who Have Completely Resected Ependymoma or Achieved CR and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only

Kaplan-Meier estimates of EFS are calculated from randomization date to first occurrence of disease progression, disease recurrence, second malignant neoplasm, or death from any cause. The comparison between randomized arms (post-radiation maintenance chemotherapy versus post-radiation observation only) is conveyed by the hazard ratio and 90.46% stagewise adjusted Wald confidence interval. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of EFS are presented

Interventionpercentage of participants (Number)
Arm II: Randomized to Radiation With Maintenance Chemotherapy69.2
Arm III: Randomized to Radiation Only63.7

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OS in Children Who Have Completely Resected Ependymoma at Initial Surgery and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only.

Kaplan-Meier estimates of OS are calculated from randomization date to death from any cause. The comparison between randomized arms (post-radiation maintenance chemotherapy versus post-radiation observation only) for this stratum is conveyed by the hazard ratio and 95% Wald confidence interval. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of OS are presented.

Interventionpercentage of participants (Number)
Arm II: Randomized to Radiation With Maintenance Chemotherapy in Stratum 190.7
Arm III: Randomized to Radiation Only in Stratum 186.4

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OS in Children With Incomplete Resection After Initial Surgery Who Then Achieved CR After Induction Chemotherapy or GTR/NTR After Second Surgery and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only

Kaplan-Meier estimates of OS are calculated from randomization date to death from any cause. The comparison between randomized arms (post-radiation maintenance chemotherapy versus post-radiation observation only) for this stratum is conveyed by the hazard ratio and 95% Wald confidence interval. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of OS are presented.

Interventionpercentage of participants (Number)
Arm II: Randomized to Radiation With Maintenance Chemotherapy in Stratum 269.2
Arm III: Randomized to Radiation Only in Stratum 289.5

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OS of Children With Incompletely Resected Ependymoma Who Are Unable to Achieve a Complete Response (CR) by Post-operative Induction Chemotherapy or by Second Surgery and Who Are Non-randomly Assigned to Receive Maintenance Chemotherapy

The Kaplan-Meier estimate of OS is calculated from enrollment date to death from any cause. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of OS are presented.

Interventionpercentage of participants (Number)
Arm IV: Nonrandomly Assigned to Arm II Treatment74.0

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OS of Children With Supratentorial Classic Ependymoma Who Achieve Complete Resection at First or Second Surgery or Children Who Achieve Complete Response (CR) After Induction Chemo and Who Are Non-randomly Assigned to Observation

The Kaplan-Meier estimate of OS is calculated from enrollment date to death from any cause. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of OS are presented.

Interventionpercentage of participants (Number)
Arm I: Observation100

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Overall Survival (OS) in Children Who Have Completely Resected Ependymoma or Achieved CR and Are Treated With Post-radiation Maintenance Chemotherapy or Post-radiation Observation Only

Kaplan-Meier estimates of OS are calculated from randomization date to death from any cause. The comparison between randomized arms (post-radiation maintenance chemotherapy versus post-radiation observation only) is conveyed by the hazard ratio and 90.46% stagewise adjusted Wald confidence interval. (NCT01096368)
Timeframe: Up to 10 years after enrollment. 5-year estimates of OS are presented.

Interventionpercentage of participants (Number)
Arm II: Randomized to Radiation With Maintenance Chemotherapy88.3
Arm III: Randomized to Radiation Only86.9

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The Tolerability of BuMel Regimen

Number of patients who experience one or more unacceptable toxicities (severe sinusoidal obstruction syndrome [SOS] or Grade 4-5 pulmonary toxicity per Common Toxicity Criteria [CTC] v.4.0) during the Consolidation phase of therapy. (NCT01798004)
Timeframe: Up to 28 days post-consolidation therapy, up to 1 year

Interventionparticipants (Number)
All Patients9

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Provocative Concentration (PC20) After Methacholine Challenge

The provocative concentration (PC) of inhaled methacholine required to reduce forced expiratory volume in 1 second (FEV1) by 20% (PC20) was calculated from the methacholine challenge at screening and 2 hours (+15 minutes) post dose on Day 3 of each Treatment Period using a five-breath dosimeter method. The primary endpoint was the methacholine PC20 value normalized by means of a log (base 2) transformation, at 2 dose levels compared with placebo in participants with asthma following provocation with methacholine. (NCT01993329)
Timeframe: Screening (Day -21 to Day -1) and Day 3

Interventionlog [mg/mL] (Geometric Mean)
Gefapixant 500.91
Gefapixant 3000.84
Placebo0.82

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Highest FEV1 After Methacholine Challenge

Serial FEV1 was measured post inhalation of methacholine challenges for 90 minutes. The highest FEV1 at 5, 15, 30, 45, 60, and 90 minutes following methacholine challenge were evaluated for each subject. The minimum highest FEV1 was derived using the first three available measures that cover the first 30 minutes after the challenge. (NCT01993329)
Timeframe: Screening (Day -21 to Day -1) and Day 3

,,,
InterventionLiters (Mean)
+ 5 minutes+15 minutes+30 minutes+45 minutes+60 minutes+90 minutesMinimum Highest FEV1
Gefapixant 3002.432.672.832.993.063.122.43
Gefapixant 502.532.722.933.023.113.152.53
Placebo2.542.772.943.033.143.182.54
Screening2.442.692.862.932.993.102.44

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Number of Participants With Complete Response (CR) of Rolapitant Hydrochloride Administered as a Single-dose

Complete response (CR) no emetic episodes and no rescue medications. (NCT02732015)
Timeframe: Days 1-10

InterventionParticipants (Count of Participants)
Cohort 10
Cohort 25

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