Compounds > th 302
Page last updated: 2024-11-12

th 302

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

Description

TH 302: an hypoxia-activated prodrug of bromo-isophosphoramide mustard; an antineoplastic agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11984561
CHEMBL ID260046
SCHEMBL ID15691894
SCHEMBL ID2357174
MeSH IDM0550416

Synonyms (50)

Synonym
HY-10535
evofosfamide
hap-302
th-302 ,
CHEMBL260046
evofosfamide [usan:inn]
unii-8a9rz3hn8w
phosphorodiamidic acid, n,n'-bis(2-bromoethyl)-, (1-methyl-2-nitro-1h-imidazol-5-yl)methyl ester
918633-87-1
8a9rz3hn8w ,
th302
th 302
CS-0616
evofosfamide [who-dd]
evofosfamide [usan]
1-methyl-2-nitro-l h-imidazole-5-yl) n,n-bis(2-bromoethyl)diamidophosphate
(1-methyl-2-nitro-1h-imidazol-5-yl)methyl n,n'-bis(2-bromoethyl)diamidophosphate
(1-methyl-2-nitro-1h-imidazole-5-yl)methyl n,n'-bis(2-bromoethyl) diamidophosphate
evofosfamide [inn]
evofosfamide [jan]
S2757
n,n'-bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1h-imidazol-5-yl)methyl ester
SCHEMBL15691894
c9h16br2n5o4p
SCHEMBL2357174
evofosfamide (jan/usan/inn)
D10704
2-bromo-n-[(2-bromoethylamino)-[(3-methyl-2-nitroimidazol-4-yl)methoxy]phosphoryl]ethanamine
gtpl8695
compound 3b
AC-29025
FT-0696771
AKOS026673946
J-523214
DTXSID60238721
(2-bromoethyl)({[(2-bromoethyl)amino][(1-methyl-2-nitro-1h-imidazol-5-yl)methoxy]phosphoryl})amine
AS-74462
EX-A1740
th-302; evofosfamide;hap-302
evofosfamide(th-302)
BCP06074
phosphorodiamidic acid, n,n'-bis(2-bromoethyl)-, (1-methyl-2-nitro-1h-imidazol-5-yl)methyl ester.
DB06091
Q7670203
AMY16615
SB17116
CCG-269225
A901406
th302n,n'-bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1h-imidazol-5-yl)methyl ester
bdbm50543112

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most common adverse events were nausea, skin rash, fatigue, and vomiting."( Phase 1 study of the safety, tolerability, and pharmacokinetics of TH-302, a hypoxia-activated prodrug, in patients with advanced solid malignancies.
Bendell, JC; Borad, MJ; Burris, HA; Chiorean, EG; Infante, JR; Jones, SF; Kroll, S; Lacouture, ME; Langmuir, VK; Lee, H; Lewandowski, K; Molina, JR; Ramanathan, RK; Tibes, R; Weiss, GJ, 2011)		0.37
" Common adverse events included fatigue, nausea and skin rash."( A phase I study of the safety and pharmacokinetics of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.
Adkins, D; Butrynski, JE; Chawla, SP; Cranmer, LD; Ganjoo, KN; Kroll, S; Langmuir, VK; Lorente, G; Okuno, SH; Rushing, D, 2011)		0.37
" The most common adverse events during induction were fatigue, nausea, and skin and/or mucosal toxicities as well as anemia, thrombocytopenia, and neutropenia."( Phase II study of the safety and antitumor activity of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.
Adkins, DR; Butrynski, JE; Chawla, SP; Cranmer, LD; Ganjoo, KN; Hendifar, AE; Kroll, S; Okuno, SH; Reed, DR; Van Tine, BA, 2014)		0.4

Pharmacokinetics

ExcerptReferenceRelevance
" There was no evidence of pharmacokinetic interaction between TH-302 and doxorubicin."( A phase I study of the safety and pharmacokinetics of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.
Adkins, D; Butrynski, JE; Chawla, SP; Cranmer, LD; Ganjoo, KN; Kroll, S; Langmuir, VK; Lorente, G; Okuno, SH; Rushing, D, 2011)		0.37
"3 l/m(2), respectively, resulting in a terminal elimination half-life of about 36 min."( Pharmacokinetics of TH-302: a hypoxically activated prodrug of bromo-isophosphoramide mustard in mice, rats, dogs and monkeys.
Cai, X; Duan, JX; Jiao, H; Jung, D; Lin, L; Matteucci, M, 2012)		0.38
"TH-302 exhibited good safety, efficacy and pharmacokinetic properties in nonclinical species, translating into favorable properties in humans."( Pharmacokinetics of TH-302: a hypoxically activated prodrug of bromo-isophosphoramide mustard in mice, rats, dogs and monkeys.
Cai, X; Duan, JX; Jiao, H; Jung, D; Lin, L; Matteucci, M, 2012)		0.38
" The pharmacokinetics of TH-302 was characterized by a short half-life of 12."( Metabolism, pharmacokinetics and excretion of a novel hypoxia activated cytotoxic prodrug, TH-302, in rats.
Duan, JX; Jiao, H; Jung, D; Matteucci, M; Wang, R, 2012)		0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
"The purpose of this study was to determine the dose-limiting toxicities (DLT), maximum tolerated dose (MTD), safety, pharmacokinetics and preliminary activity of TH-302, a hypoxia-activated prodrug, in combination with doxorubicin in patients with advanced soft tissue sarcoma."( A phase I study of the safety and pharmacokinetics of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.
Adkins, D; Butrynski, JE; Chawla, SP; Cranmer, LD; Ganjoo, KN; Kroll, S; Langmuir, VK; Lorente, G; Okuno, SH; Rushing, D, 2011)		0.37
"The hematologic toxicity of doxorubicin is increased when combined with TH-302."( A phase I study of the safety and pharmacokinetics of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.
Adkins, D; Butrynski, JE; Chawla, SP; Cranmer, LD; Ganjoo, KN; Kroll, S; Langmuir, VK; Lorente, G; Okuno, SH; Rushing, D, 2011)		0.37
" This phase II study investigated TH-302 in combination with doxorubicin, followed by single-agent TH-302 maintenance therapy in patients with first-line advanced soft tissue sarcoma (STS) to assess progression-free survival (PFS), response rate, overall survival, safety, and tolerability."( Phase II study of the safety and antitumor activity of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma.
Adkins, DR; Butrynski, JE; Chawla, SP; Cranmer, LD; Ganjoo, KN; Hendifar, AE; Kroll, S; Okuno, SH; Reed, DR; Van Tine, BA, 2014)		0.4
" Here we investigated the hypoxia-activated prodrug evofosfamide in combination with different treatment regimens of IR against lung A549- and head&neck UT-SCC-14-derived tumor xenografts."( The hypoxia-activated prodrug evofosfamide in combination with multiple regimens of radiotherapy.
Bender, S; Grgic, I; Guckenberger, M; Nytko, KJ; Ott, J; Pruschy, M; Riesterer, O, 2017)		0.46
" This study assessed the anticancer efficacy of evofosfamide in combination with the Proapoptotic Receptor Agonists (PARAs) dulanermin and drozitumab against human osteosarcoma in vitro and in an intratibial murine model of osteosarcoma."( Anticancer efficacy of the hypoxia-activated prodrug evofosfamide is enhanced in combination with proapoptotic receptor agonists against osteosarcoma.
Atkins, GJ; DeNichilo, M; Difelice, C; Evdokiou, A; Findlay, DM; Hay, S; Ingman, W; Liapis, V; Panagopoulos, V; Ponomarev, V; Shoubridge, A; Zannettino, ACW; Zinonos, I; Zysk, A, 2017)		0.46
" The cytotoxicity of evofosfamide impacted the generation of in vitro drug-drug interaction (DDI) data, especially in vitro induction results."( A Novel PBPK Modeling Approach to Assess Cytochrome P450 Mediated Drug-Drug Interaction Potential of the Cytotoxic Prodrug Evofosfamide.
Dolgos, H; Dyroff, M; El Bawab, S; Gallemann, D; Hecht, S; Johne, A; Jung, D; Lüpfert, C; von Richter, O, 2018)		0.48

Dosage Studied

ExcerptRelevanceReference
"TH-302 was administered intravenously over 30 to 60 minutes in two regimens: three times weekly dosing followed by 1 week off (arm A) and every 3-week dosing (arm B)."( Phase 1 study of the safety, tolerability, and pharmacokinetics of TH-302, a hypoxia-activated prodrug, in patients with advanced solid malignancies.
Bendell, JC; Borad, MJ; Burris, HA; Chiorean, EG; Infante, JR; Jones, SF; Kroll, S; Lacouture, ME; Langmuir, VK; Lee, H; Lewandowski, K; Molina, JR; Ramanathan, RK; Tibes, R; Weiss, GJ, 2011)		0.37
" In acute and chronic safety studies, there was no accumulation of TH-302 following once weekly dosing for 3 weeks in the rat and dog."( Pharmacokinetics of TH-302: a hypoxically activated prodrug of bromo-isophosphoramide mustard in mice, rats, dogs and monkeys.
Cai, X; Duan, JX; Jiao, H; Jung, D; Lin, L; Matteucci, M, 2012)		0.38
" TH-302 treatment resulted in a reduction in the volume of the HF 48 hours after dosing and a corresponding increase in the necrotic fraction."( Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer.
Ahluwalia, D; Ammons, WS; Curd, JG; Duan, JX; Ferraro, D; Hart, CP; Liu, Q; Matteucci, MD; Sun, JD; Wang, J; Wang, Y, 2012)		0.38
" The antitumor activity, different dosing sequences, and dosing regimens of TH-302 in combination with commonly used conventional chemotherapeutics were investigated in human tumor xenograft models."( TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules.
Ahluwalia, D; Ammons, WS; Baker, AF; Cranmer, LD; Curd, JG; Duan, JX; Ferraro, D; Hart, CP; Liu, Q; Matteucci, MD; Sun, JD; Wang, J; Wang, Y, 2012)		0.38
" Simultaneous administration of TH-302 and chemotherapeutics increased toxicity versus schedules with dosing separations."( TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules.
Ahluwalia, D; Ammons, WS; Baker, AF; Cranmer, LD; Curd, JG; Duan, JX; Ferraro, D; Hart, CP; Liu, Q; Matteucci, MD; Sun, JD; Wang, J; Wang, Y, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-enolaseHomo sapiens (human)IC50 (µMol)2.14750.05101.25094.8380AID1661325; AID1661326; AID1661328; AID1661329
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIAlpha-enolaseHomo sapiens (human)
gluconeogenesisAlpha-enolaseHomo sapiens (human)
response to virusAlpha-enolaseHomo sapiens (human)
positive regulation of plasminogen activationAlpha-enolaseHomo sapiens (human)
negative regulation of cell growthAlpha-enolaseHomo sapiens (human)
negative regulation of DNA-templated transcriptionAlpha-enolaseHomo sapiens (human)
positive regulation of muscle contractionAlpha-enolaseHomo sapiens (human)
canonical glycolysisAlpha-enolaseHomo sapiens (human)
negative regulation of hypoxia-induced intrinsic apoptotic signaling pathwayAlpha-enolaseHomo sapiens (human)
positive regulation of ATP biosynthetic processAlpha-enolaseHomo sapiens (human)
glycolytic processAlpha-enolaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
magnesium ion bindingAlpha-enolaseHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingAlpha-enolaseHomo sapiens (human)
transcription corepressor bindingAlpha-enolaseHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificAlpha-enolaseHomo sapiens (human)
transcription corepressor activityAlpha-enolaseHomo sapiens (human)
RNA bindingAlpha-enolaseHomo sapiens (human)
phosphopyruvate hydratase activityAlpha-enolaseHomo sapiens (human)
protein bindingAlpha-enolaseHomo sapiens (human)
protein homodimerization activityAlpha-enolaseHomo sapiens (human)
cadherin bindingAlpha-enolaseHomo sapiens (human)
GTPase bindingAlpha-enolaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
extracellular spaceAlpha-enolaseHomo sapiens (human)
nucleusAlpha-enolaseHomo sapiens (human)
nuclear outer membraneAlpha-enolaseHomo sapiens (human)
cytoplasmAlpha-enolaseHomo sapiens (human)
cytosolAlpha-enolaseHomo sapiens (human)
plasma membraneAlpha-enolaseHomo sapiens (human)
cell cortexAlpha-enolaseHomo sapiens (human)
cell surfaceAlpha-enolaseHomo sapiens (human)
membraneAlpha-enolaseHomo sapiens (human)
M bandAlpha-enolaseHomo sapiens (human)
extracellular exosomeAlpha-enolaseHomo sapiens (human)
phosphopyruvate hydratase complexAlpha-enolaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (53)

Assay IDTitleYearJournalArticle
AID1366811Selectivity index, ratio of prodrug IC50 under normoxic condition to prodrug IC50 under hypoxic condition2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1366810Cytotoxicity against human NCI-H460 cells after 24 hrs under normoxic condition by luminescence-based Cell-Titer Glo assay2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1594193Selectivity ratio of IC50 for human SW620 cells under aerobic condition to IC50 for human SW620 cells under hypoxic condition2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
AID1661327Cytotoxicity against human D423 cells with ENO1 deficient assessed as reduction in cell viability incubated for 5 days in presence of 1 % oxygen by crystal violet staining based spectrophotometry2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
AID1594184Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
AID1594185Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
AID1408786Antiproliferative activity against human HEMC-SS cells treated for 24 hrs under hypoxic condition followed by compound wash-out and incubated under normoxic condition for 48 hrs by alamar blue assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Structure-activity relationship study of hypoxia-activated prodrugs for proteoglycan-targeted chemotherapy in chondrosarcoma.
AID1661329Inhibition of ENO1 in wild-type human LN319 cells incubated for 5 days in presence of 1 % oxygen by crystal violet staining based spectrophotometry2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
AID1366803Prodrug activation assessed as recombinant human cytochrome P450-reductase-mediated drug metabolism by measuring bromo-isophosphoramide mustard level under hypoxic condition after 2 hrs by LC-MS analysis2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1470603Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID1366798Prodrug activation assessed as recombinant human cytochrome P450-reductase-mediated drug metabolism by measuring parent compound remaining under hypoxic condition after 2 hrs by LC-MS analysis2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1408787Selectivity index, ratio of IC50 for human HEMC-SS cells under normoxic condition to IC50 for human HEMC-SS cells under hypoxic condition2018European journal of medicinal chemistry, Oct-05, Volume: 158Structure-activity relationship study of hypoxia-activated prodrugs for proteoglycan-targeted chemotherapy in chondrosarcoma.
AID329313Toxicity against human MIAPaCa2-RFP cells xenografted mouse2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1470600Cytotoxicity against human HT-29 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID329299Ratio of IC50 for human H460 cells under normoxic condition to hypoxic condition by Alamar blue staining assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID329304Cytotoxicity against human HT29 cells under normoxic condition after 2 hrs by clonogenic assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID329306Ratio of IC50 for human HT29 cells under normoxic condition to hypoxic condition by clonogenic assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID329301Cytotoxicity against human H460 cells under normoxic condition after 2 hrs by clonogenic assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1366809Cytotoxicity against human NCI-H460 cells after 24 hrs under hypoxic condition by luminescence-based Cell-Titer Glo assay2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID329311Toxicity against human MIAPaCa2 cells xenografted mouse assessed as survival time at 30 mg/kg, ip administered daily once for 5 days a week for 15 days2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1504939Cytotoxicity against human DU145 cells incubated for 2 hrs under hypoxic condition measured after 72 hrs by Alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Synthesis and Evaluation of Radiolabeled Phosphoramide Mustard with Selectivity for Hypoxic Cancer Cells.
AID329300Metabolic stability in mouse liver microsomes at 5 uM after 30 mins2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1408785Antiproliferative activity against human HEMC-SS cells treated for 24 hrs under normoxic condition followed by compound wash-out and incubated under normoxic condition for 48 hrs by alamar blue assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Structure-activity relationship study of hypoxia-activated prodrugs for proteoglycan-targeted chemotherapy in chondrosarcoma.
AID1470605Selectivity ratio of IC50 for human NCI-H460 cells under normoxic condition to IC50 for human NCI-H460 cells under hypoxic condition2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID329297Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by Alamar blue staining assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1366795Prodrug activation assessed as recombinant human cytochrome P450-reductase-mediated drug metabolism by measuring prodrug remaining under normoxic condition after 2 hrs by LC-MS analysis2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1470604Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID1504940Cytotoxicity against human PC3 cells incubated for 2 hrs under normoxic condition measured after 72 hrs by Alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Synthesis and Evaluation of Radiolabeled Phosphoramide Mustard with Selectivity for Hypoxic Cancer Cells.
AID1661326Inhibition of ENO1 in wild-type human LN319 cells incubated for 5 days in presence of 21 % oxygen by crystal violet staining based spectrophotometry2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
AID1504941Cytotoxicity against human DU145 cells incubated for 2 hrs under normoxic condition measured after 72 hrs by Alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Synthesis and Evaluation of Radiolabeled Phosphoramide Mustard with Selectivity for Hypoxic Cancer Cells.
AID329305Cytotoxicity against human HT29 cells under hypoxic condition after 2 hrs by clonogenic assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1366802Prodrug activation assessed as recombinant human cytochrome P450-reductase-mediated drug metabolism by measuring bromo-isophosphoramide mustard level under normoxic condition after 2 hrs by LC-MS analysis2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1504942Selectivity index, ratio of IC50 for human PC3 cells under normoxic condition to IC50 for human PC3 cells under hypoxic condition2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Synthesis and Evaluation of Radiolabeled Phosphoramide Mustard with Selectivity for Hypoxic Cancer Cells.
AID1504938Cytotoxicity against human PC3 cells incubated for 2 hrs under hypoxic condition measured after 72 hrs by Alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Synthesis and Evaluation of Radiolabeled Phosphoramide Mustard with Selectivity for Hypoxic Cancer Cells.
AID1470602Selectivity ratio of IC50 for human HT-29 cells under normoxic condition to IC50 for human HT-29 cells under hypoxic condition2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID329302Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by clonogenic assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1470601Cytotoxicity against human HT-29 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID1661328Inhibition of ENO1 in overexpressed human D423 cells incubated for 5 days in presence of 1 % oxygen by crystal violet staining based spectrophotometry2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
AID329298Cytotoxicity against human H460 cells under normoxic condition after 2 hrs by Alamar blue staining assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID329303Ratio of IC50 for human H460 cells under normoxic condition to hypoxic condition by clonogenic assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1520230Antiproliferative activity against human NCI-H460 cells in presence of O22019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Nitro-Group-Containing Drugs.
AID1504943Selectivity index, ratio of IC50 for human DU145 cells under normoxic condition to IC50 for human DU145 cells under hypoxic condition2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Synthesis and Evaluation of Radiolabeled Phosphoramide Mustard with Selectivity for Hypoxic Cancer Cells.
AID1661324Cytotoxicity against human D423 cells with ENO1 deficient assessed as reduction in cell viability incubated for 5 days in presence of 21 % oxygen by crystal violet staining based spectrophotometry2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
AID1520229Antiproliferative activity against human NCI-H460 cells2019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Nitro-Group-Containing Drugs.
AID1594189Cytotoxicity against human SW620 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
AID1366808Induction of DNA (unknown origin) alkylation assessed as amount remaining of unalkylated test oligonucleotides after 18 hrs by LC/MS/UV analysis2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.
AID1520231Antiproliferative activity against human NCI-H460 cells in presence of N22019Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
Nitro-Group-Containing Drugs.
AID329307Aqueous solubility at 100 mg at pH 7.42008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1661325Inhibition of ENO1 in overexpressed human D423 cells incubated for 5 days in presence of 21 % oxygen by crystal violet staining based spectrophotometry2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.
AID1594190Cytotoxicity against human SW620 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
AID1594188Selectivity ratio of IC50 for human MDA-MB-468 cells under aerobic condition to IC50 for human MDA-MB-468 cells under hypoxic condition2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.
AID329309Antitumor activity against human MIAPaCa2 cells xenografted mouse assessed as tumor growth inhibition at 30 mg/kg, ip administered once daily for 5 days a week for 15 days2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (83)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (1.20)29.6817
2010's65 (78.31)24.3611
2020's17 (20.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.27

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

MetricThis Compound (vs All)
Research Demand Index27.27 (24.57)
Research Supply Index4.58 (2.92)
Research Growth Index6.38 (4.65)
Search Engine Demand Index30.30 (26.88)
Search Engine Supply Index2.20 (0.95)

This Compound (27.27)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials14 (16.87%)5.53%
Reviews2 (2.41%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other67 (80.72%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
hydroxylamine
amino alcohol : An alcohol containing an amino functional group in addition to the alcohol-defining hydroxy group.		2.2110hydroxylaminesalgal metabolite;
bacterial xenobiotic metabolite;
EC 1.1.3.13 (alcohol oxidase) inhibitor;
EC 4.2.1.22 (cystathionine beta-synthase) inhibitor;
EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor;
nitric oxide donor;
nucleophilic reagent
pyruvic acid
Pyruvic Acid: An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed). pyruvic acid : A 2-oxo monocarboxylic acid that is the 2-keto derivative of propionic acid. It is a metabolite obtained during glycolysis.		2.1102-oxo monocarboxylic acidcofactor;
fundamental metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		2.1110isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
hydralazine
Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent.		2.110azaarene;
hydrazines;
ortho-fused heteroarene;
phthalazines		antihypertensive agent;
vasodilator agent
ifosfamide
[no description available]		3.5111ifosfamidesalkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic
floxuridine
Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.. floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.		2.2110nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
radiosensitizing agent
ethylamine
ethylamine : A two-carbon primary aliphatic amine.		2.0710primary aliphatic aminehuman metabolite
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.1110mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		2.0810diazine;
pyrazines		Daphnia magna metabolite
azomycin
azomycin: RN given refers to parent cpd with specified locant; structure		13.467115C-nitro compound;
imidazoles		antitubercular agent
deoxycytidine
[no description available]		7.2353pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.0710delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
misonidazole
Misonidazole: A nitroimidazole that sensitizes normally radio-resistant hypoxic cells to radiation. It may also be directly cytotoxic to hypoxic cells and has been proposed as an antineoplastic.		2.7620
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		4.8321taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
pimonidazole
pimonidazole: structure given in first source		2.1110
topotecan
Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.		2.1310pyranoindolizinoquinolineantineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		7.3763organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
irinotecan
[no description available]		2.0710carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.11101,2,3-triazole
adriamycinol
doxorubicinol : A member of the class of tetracenequinones that is the major metabolite of the anthracycline doxorubicin, a chemotherapeutic agent effective against a broad range of malignant neoplasms. It is thought to exhibit cardiotoxic properties.		3.4511aminoglycoside;
anthracycline antibiotic;
aromatic ether;
deoxy hexoside;
p-quinones;
phenols;
polyol;
tetracenequinones		cardiotoxic agent;
drug metabolite
fluoromisonidazole
[no description available]		3.1130
isophosphamide mustard
isophosphamide mustard: antitumor metabolite of ifosfamide; palifosfamide-tris is a salt with tris; structure in first source		2.5120phosphorodiamide
sn 38
SN-38 : A member of the class of pyranoindolizinoquinolines that is (4S)-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione bearing two additional ethyl substituents at positions 4 and 11 as well as two additional hydroxy substituents at positions 4 and 9. It is the active metabolite of irinotecan and is ~1000 times more active than irinotecan itself.		2.1510delta-lactone;
phenols;
pyranoindolizinoquinoline;
tertiary alcohol		antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		2.7830secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
bortezomib
[no description available]		2.0810amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		2.2110L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
su 11248
[no description available]		4.6211monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
apaziquone
apaziquone: structure given in first source; RN given refers to (E)-isomer		3.1910indoles
aq4n
AQ4N: structure given in first source		3.1910
pr-104
PR-104: 3,5-dinitrobenzamide nitrogen mustard, an alkyating antineoplastic; structure in first source		3.1910
chitosan
[no description available]		2.3110
azd2014
vistusertib: potent and selective dual mTORC1 and mTORC2 inhibitor; structure in first source		2.1710
guanine
[no description available]		2.07102-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
pemetrexed
pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).		2.0710N-acyl-L-glutamic acid;
pyrrolopyrimidine		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
tirapazamine
Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4.		4.1140aromatic amine;
benzotriazines;
N-oxide		antibacterial agent;
antineoplastic agent;
apoptosis inducer
ConditionIndicatedRelationship StrengthStudiesTrials
Anoxemia
[description not available]		06.47202
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		06.47202
Bone Cancer
[description not available]		03.2450
Bone Neoplasms
Tumors or cancer located in bone tissue or specific BONES.		03.2450
Chondrosarcoma
A slowly growing malignant neoplasm derived from cartilage cells, occurring most frequently in pelvic bones or near the ends of long bones, in middle-aged and old people. Most chondrosarcomas arise de novo, but some may develop in a preexisting benign cartilaginous lesion or in patients with ENCHONDROMATOSIS. (Stedman, 25th ed)		02.5720
Benign Neoplasms
[description not available]		05.6761
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		17.6761
Carcinoma, Squamous Cell of Head and Neck
[description not available]		04.5441
Carcinoma, Epidermoid
[description not available]		02.6120
Cancer of Head
[description not available]		04.6751
Squamous Cell Carcinoma of Head and Neck
The most common type of head and neck carcinoma that originates from cells on the surface of the NASAL CAVITY; MOUTH; PARANASAL SINUSES, SALIVARY GLANDS, and LARYNX. Mutations in TNFRSF10B, PTEN, and ING1 genes are associated with this cancer.		04.5441
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		02.6120
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		04.6751
Cancer of Pancreas
[description not available]		010.14165
Carcinoma, Ductal, Pancreatic
[description not available]		05.2331
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		112.14165
Carcinoma, Pancreatic Ductal
Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.		05.2331
Cancer of Stomach
[description not available]		02.610
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.610
Adenocarcinoma, Basal Cell
[description not available]		05.5851
Cancer of Colon
[description not available]		02.6120
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.5670
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		05.5851
Colonic Neoplasms
Tumors or cancer of the COLON.		02.6120
Cancer of Esophagus
[description not available]		04.8721
Esophageal Neoplasms
Tumors or cancer of the ESOPHAGUS.		16.8721
Experimental Neoplasms
[description not available]		03.0540
Biliary Tract Cancer
[description not available]		02.3110
Biliary Tract Neoplasms
Tumors or cancer in the BILIARY TRACT including the BILE DUCTS and the GALLBLADDER.		14.3110
Hepatocellular Carcinoma
[description not available]		02.2510
Cancer of Liver
[description not available]		02.5920
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		02.2510
Liver Neoplasms
Tumors or cancer of the LIVER.		02.5920
Kahler Disease
[description not available]		02.830
Osteolysis
Dissolution of bone that particularly involves the removal or loss of calcium.		02.3110
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		14.830
Astrocytoma, Grade IV
[description not available]		04.5822
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		16.5822
Sarcoma, Epithelioid
[description not available]		06.5963
Sarcoma
A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.		18.5963
Soft Tissue Neoplasms
Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc.		02.6120
ER-Negative PR-Negative HER2-Negative Breast Cancer
[description not available]		02.5920
Triple Negative Breast Neoplasms
Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.		02.5920
Cancer, Second Primary
[description not available]		04.6211
Germinoblastoma
[description not available]		02.1510
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		02.1510
Osteogenic Sarcoma
[description not available]		02.5320
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		02.5320
Benign Neoplasms, Brain
[description not available]		03.5611
Local Neoplasm Recurrence
[description not available]		03.5611
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		03.5611
Colorectal Cancer
[description not available]		02.1710
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.1710
Nasopharyngeal Carcinoma
A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes.		02.1710
Cancer of Nasopharynx
[description not available]		02.1710
Nasopharyngeal Neoplasms
Tumors or cancer of the NASOPHARYNX.		02.1710
Response Evaluation Criteria in Solid Tumors
An internationally recognized set of published rules used for evaluation of cancer treatment that define when tumors found in cancer patients improve, worsen, or remain stable during treatment. These criteria are based specifically on the response of the tumor(s) to treatment, and not on the overall health status of the patient resulting from treatment.		03.5611
Cancer of Prostate
[description not available]		02.8430
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.8430
Disease Exacerbation
[description not available]		08.0865
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		02.2110
Neuroendocrine Tumors
Tumors whose cells possess secretory granules and originate from the neuroectoderm, i.e., the cells of the ectoblast or epiblast that program the neuroendocrine system. Common properties across most neuroendocrine tumors include ectopic hormone production (often via APUD CELLS), the presence of tumor-associated antigens, and isozyme composition.		02.2110
Acute Myelogenous Leukemia
[description not available]		03.8921
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		03.8921
Breast Cancer
[description not available]		02.5220
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.5220
Metastase
[description not available]		02.1110
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.1110
Carcinoma, Non-Small Cell Lung
[description not available]		03.9121
Cancer of Lung
[description not available]		03.9121
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		03.9121
Lung Neoplasms
Tumors or cancer of the LUNG.		03.9121
HPV Infection
[description not available]		02.1110
Papillomavirus Infections
Neoplasms of the skin and mucous membranes caused by papillomaviruses. They are usually benign but some have a high risk for malignant progression.		02.1110
Leucocythaemia
[description not available]		03.9221
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		03.9221
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.1310
Rhabdomyosarcoma
A malignant solid tumor arising from mesenchymal tissues which normally differentiate to form striated muscle. It can occur in a wide variety of sites. It is divided into four distinct types: pleomorphic, predominantly in male adults; alveolar (RHABDOMYOSARCOMA, ALVEOLAR), mainly in adolescents and young adults; embryonal (RHABDOMYOSARCOMA, EMBRYONAL), predominantly in infants and children; and botryoidal, also in young children. It is one of the most frequently occurring soft tissue sarcomas and the most common in children under 15. (From Dorland, 27th ed; Holland et al., Cancer Medicine, 3d ed, p2186; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, pp1647-9)		02.1310
Acute Lymphoid Leukemia
[description not available]		03.5111
Bilirubinemia
[description not available]		03.5111
Mucositis, Oral
[description not available]		04.4422
Esophagitis
INFLAMMATION, acute or chronic, of the ESOPHAGUS caused by BACTERIA, chemicals, or TRAUMA.		03.5111
Stomatitis
INFLAMMATION of the soft tissues of the MOUTH, such as MUCOSA; PALATE; GINGIVA; and LIP.		04.4422
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		03.5111
Experimental Hepatoma
[description not available]		02.0510
Angiogenesis, Pathologic
[description not available]		02.4720
Phlegmon
[description not available]		03.4511
Dermatitis Medicamentosa
[description not available]		03.4511
Lymphocytopenia
[description not available]		03.4511
Abscess
Accumulation of purulent material in tissues, organs, or circumscribed spaces, usually associated with signs of infection.		03.4511
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		03.4511
Cellulitis
An acute, diffuse, and suppurative inflammation of loose connective tissue, particularly the deep subcutaneous tissues, and sometimes muscle, which is most commonly seen as a result of infection of a wound, ulcer, or other skin lesions.		03.4511
Lymphopenia
Reduction in the number of lymphocytes.		03.4511
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		03.4511
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0710