Compounds > 10-deazaaminopterin
Page last updated: 2024-11-07

10-deazaaminopterin

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

10-Deazaaminopterin is a synthetic analog of the folate antagonist aminopterin. It exhibits potent antiproliferative activity against various cancer cell lines, particularly those expressing high levels of the reduced folate carrier (RFC). 10-Deazaaminopterin acts as a competitive inhibitor of dihydrofolate reductase (DHFR), an enzyme essential for folate metabolism and DNA synthesis. Its mechanism of action involves binding to the active site of DHFR, thereby preventing the reduction of dihydrofolate to tetrahydrofolate. This disruption of folate metabolism leads to the inhibition of DNA synthesis and cell proliferation. 10-Deazaaminopterin has been extensively studied in preclinical models and clinical trials for its potential therapeutic applications in various malignancies, including leukemia, lymphoma, and solid tumors. Its importance lies in its selective targeting of cancer cells, minimizing toxicity to normal tissues. The compound's ability to circumvent resistance mechanisms associated with conventional antifolate drugs makes it a promising candidate for the treatment of folate-resistant cancers. Ongoing research aims to further investigate its efficacy, optimize its delivery strategies, and explore its potential in combination therapies.'

Cross-References

ID SourceID
PubMed CID100516
CHEMBL ID293263
SCHEMBL ID7081697
MeSH IDM0067734

Synonyms (21)

Synonym
nsc-311469
52454-37-2
10-dam
10-deazaaminopterin
l-glutamic acid, n-(4-(2-(2,4-diamino-6-pteridinyl)ethyl)benzoyl)-
nsc 311469
10-deazaminopterin
10-deaza-aminopterin
gnf-pf-173 ,
CHEMBL293263 ,
(2s)-2-[[4-[2-(2,4-diaminopteridin-6-yl)ethyl]benzoyl]amino]pentanedioic acid
2-[[4-[2-(2,4-diaminopteridin-6-yl)ethyl]benzoyl]amino]pentanedioic acid
(s)-2-{4-[2-(2,4-diamino-pteridin-6-yl)-ethyl]-benzoylamino}-pentanedioic acid
bdbm50016461
pxj16ppe04 ,
unii-pxj16ppe04
SCHEMBL7081697
(s)-2-(4-(2-(2,4-diaminopteridin-6-yl)ethyl)benzamido)pentanedioic acid
Q27286805
(4-(2-(2,4-diaminopteridin-6-yl)ethyl)benzoyl)-l-glutamic acid
AKOS040746467

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"10-DAM appears to be as beneficial and as safe as MTX for the treatment of RA."( Efficacy and safety of 10-deazaaminopterin in the treatment of rheumatoid arthritis. A one-year continuation, double-blind study.
Alarcón, GS; Castañeda, O; Ferrándiz, M; Koopman, WJ; Krumdieck, CL, 1992)		0.59

Bioavailability

ExcerptReferenceRelevance
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011)		0.37

Dosage Studied

ExcerptRelevanceReference
" At a dosage of 6 mg/kg q1d X 5 against solid tumors, the relative tumor volumes (treated/control X 100%) were 12%/41% for Sarcoma 180, 16%/31% for Taper liver tumor, and 20%/30% for Ehrlich ascites carcinoma."( Antitumor properties of a new folate analog, 10-deaza-aminopterin, in mice.
DeGraw, JI; Dorick, DM; Moccio, DM; Sirotnak, FM, 1978)		0.26
" Against L1210 in mice, the percent increase in life span at the LD10 dosage was +151% (methotrexate), +178% (10-deazaminopterin), +235% (10-methyl analogue), and +211% (10-ethyl analogue)."( Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
Brown, VH; DeGraw, JI; Gaumont, Y; Kisliuk, RL; Sirotnak, FM; Tagawa, H, 1982)		0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Dihydrofolate reductaseHomo sapiens (human)IC50 (µMol)0.00410.00060.87267.3000AID57068
Dihydrofolate reductaseMus musculus (house mouse)Ki0.30000.00000.21713.9000AID57443; AID57451; AID57455; AID57460
Dihydrofolate reductaseLacticaseibacillus caseiIC50 (µMol)0.02040.00130.26964.9000AID57747; AID57932; AID57933; AID57934; AID57935; AID57936
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
tetrahydrobiopterin biosynthetic processDihydrofolate reductaseHomo sapiens (human)
one-carbon metabolic processDihydrofolate reductaseHomo sapiens (human)
negative regulation of translationDihydrofolate reductaseHomo sapiens (human)
axon regenerationDihydrofolate reductaseHomo sapiens (human)
response to methotrexateDihydrofolate reductaseHomo sapiens (human)
dihydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate biosynthetic processDihydrofolate reductaseHomo sapiens (human)
folic acid metabolic processDihydrofolate reductaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityDihydrofolate reductaseHomo sapiens (human)
regulation of removal of superoxide radicalsDihydrofolate reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
mRNA regulatory element binding translation repressor activityDihydrofolate reductaseHomo sapiens (human)
mRNA bindingDihydrofolate reductaseHomo sapiens (human)
dihydrofolate reductase activityDihydrofolate reductaseHomo sapiens (human)
folic acid bindingDihydrofolate reductaseHomo sapiens (human)
NADPH bindingDihydrofolate reductaseHomo sapiens (human)
sequence-specific mRNA bindingDihydrofolate reductaseHomo sapiens (human)
NADP bindingDihydrofolate reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
mitochondrionDihydrofolate reductaseHomo sapiens (human)
cytosolDihydrofolate reductaseHomo sapiens (human)
mitochondrionDihydrofolate reductaseHomo sapiens (human)
cytosolDihydrofolate reductaseMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (80)

Assay IDTitleYearJournalArticle
AID116458Percent increase in life span at given dose of 12.0 mg/kg/day against L-1210 leukemia in mice1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
AID129846Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 30 at intraperitoneal of dose 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID99542Inhibitory activity against thymidylate synthase in Lactobacillus casei was determined (glutamate residue 2)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99534Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was determined (glutamate residue 1)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID134999Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 23 at intraperitoneal dose of 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID98547Concentration required to inhibit the growth of L1210 cells1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID135171Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 44 at intraperitoneal dose of 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID99546Inhibitory activity against thymidylate synthase in Lactobacillus casei was determined (glutamate residue 6)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99536Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was determined (glutamate residue 3)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99539Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was determined (glutamate residue 6)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID228545Michaelis constant of compound was determined from affinity towards carrier component of transport mechanism1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID98160Concentration inhibiting L1210 cell growth in culture1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.
AID135154Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 30 at intraperitoneal dose of 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID134218Transport influx which is determined by competitive binding for the transport protein; expressed as Ki (uM)1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin.
AID99400Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was determined (glutamate residue 1)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID209429Concentration required to inhibit growth of Streptococcus faecium by 50%1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
AID52545Concentration required to inhibit the growth of chang liver cells1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID135169Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 37 at intraperitoneal dose of 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID116594Percent increase in life span at given dose of 9.0 mg/kg/day against L-1210 leukemia in mice1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
AID130005Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 44 at intraperitoneal of dose 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID57068Compound was tested for its inhibitory activity on Recombinant Human Dihydrofolate Reductase.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase.
AID44197Relative activity when compared to the activity of aminopterin in CCRF-CEM Human leukemia cell at a concentration of 50 uM1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase.
AID99390Concentration required to inhibit growth of Lactobacillus casei by 50%1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
AID99401Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was determined (glutamate residue 2)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99545Inhibitory activity against thymidylate synthase in Lactobacillus casei was determined (glutamate residue 5)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID135175Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 44 at intraperitoneal dose of 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID96954% increase in lifespan was measured at 15 mg/kg dosage after ip administration1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID57936Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was determined (glutamate residue 6)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99383Concentration required for the 50% growth inhibition of Streptococcus faecium ATCC 8043 organism at 1 ng/mL folate concentration1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID57747Concentration required to inhibit Lactobacillus casei derived Dihydrofolate reductase activity by 50%1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
AID132684Inhibition of growth in L1210 murine leukemia cells in culture expressed as IC50 (nM)1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin.
AID99535Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was determined (glutamate residue 2)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID130003Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 44 at intraperitoneal of dose 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID116593Percent increase in life span at given dose of 6.0 mg/kg/day against L-1210 leukemia in mice1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
AID99404Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was determined (glutamate residue 5)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID57934Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was determined (glutamate residue 4)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID129834Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 23 at intraperitoneal dose of 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID57451Concentration inhibiting dihydrofolate reductase derived from L1210 cells1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.
AID135321Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 44 at intraperitoneal dose of 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID209420Concentration required for the 50% growth inhibition of Streptococcus faecium MTX resist organism at 1 ng/mL folate concentration1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID211642Concentration required for the 50% inhibition of Lactobacillus casei thymidylate synthase1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID135160Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 37 at intraperitoneal dose of 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID130011Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 44 at intraperitoneal of dose 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID134996Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 23 at intraperitoneal dose of 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID99537Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was determined (glutamate residue 4)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID16875The efflux rate constant of the compound1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID98419Minimum inhibitory concentration of compound was tested for growth inhibition of L1210 cells1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID99382Concentration required for the 50% growth inhibition of Lactobacillus casei ATCC 7469 organism at 1 ng/mL folate concentration1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID135011Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 30 at intraperitoneal dose of 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID99543Inhibitory activity against thymidylate synthase in Lactobacillus casei was determined (glutamate residue 3)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID129848Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 30 at intraperitoneal of dose 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID129836Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 23 at intraperitoneal dose of 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID129842Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 23 at intraperitoneal dose of 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID209419Concentration required for the 50% growth inhibition of Streptococcus faecium ATCC 8043 organism at 1 ng/mL folate concentration1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID99405Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was determined (glutamate residue 6)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99538Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was determined (glutamate residue 5)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID135008Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 23 at intraperitoneal dose of 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID129991Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 37 at intraperitoneal of dose 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID99541Inhibitory activity against thymidylate synthase in Lactobacillus casei was determined (glutamate residue 1)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID135157Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 37 at intraperitoneal dose of 12 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID22603Influx velocity of the compound1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID231772Ratio of compound activity to that of MTX activity.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase.
AID98446Antitumor activity expressed as mean survival time against L1210 leukemia cells in mice after ip administration at dose 3 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID129993Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 37 at intraperitoneal of dose 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID130000Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 37 at intraperitoneal of dose 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID57929Concentration required for the 50% growth inhibition of Lactobacillus casei dihydrofolate reductase enzyme1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID98445Antitumor activity expressed as mean survival time against L1210 leukemia cells in mice after ip administration at dose 15 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID57443Binding affinity towards Dihydrofolate reductase derived from L1210 cells using [3H]- MTX as the radioligand1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.
AID99402Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was determined (glutamate residue 3)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID135014Tested for antiinflammatory activity on mouse type II collagen arthritis as Paw swelling* of all animals in each group on day 30 at intraperitoneal dose of 15 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID57933Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was determined (glutamate residue 3)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID129988Incidence of disease(mouse type II collagen arthritis) was scored as the percentage of animals within each experimental group that exhibited joint or limb inflammation on day 30 at intraperitoneal of dose 9 mg/kg1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
AID99544Inhibitory activity against thymidylate synthase in Lactobacillus casei was determined (glutamate residue 4)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID57460Tested for inhibition of dihydrofolate reductase enzyme1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID57932Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was determined (glutamate residue 2)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID99403Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was determined (glutamate residue 4)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID57455Inhibition of Dihydrofolate reductase (DHFR) enzyme derived from L1210 cells expressed as Ki (pM)1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin.
AID57935Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was determined (glutamate residue 5)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
AID96955% increase in lifespan was measured at 3 mg/kg dosage after ip administration1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-199020 (58.82)18.7374
1990's12 (35.29)18.2507
2000's1 (2.94)29.6817
2010's1 (2.94)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (5.56%)5.53%
Reviews1 (2.78%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other33 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (12)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 1, Open-label, Dose-finding Study of Pralatrexate Plus Systemic Bexarotene in Patients With Relapsed or Refractory Cutaneous T Cell Lymphoma [NCT01134341]Phase 134 participants (Actual)Interventional2010-03-31Completed
A Multi-Center, Phase 2, Open-Label Study of (RS)-10-Propargyl-10-Deazaaminopterin (Pralatrexate) With Vitamin B12 and Folic Acid Supplementation in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma [NCT00364923]Phase 2115 participants (Actual)Interventional2006-08-31Completed
A Randomized, Phase 2b, Multi-center Study of Pralatrexate Versus Erlotinib in Patients With Stage IIIB/IV Non-small Cell Lung Cancer After Failure of at Least 1 Prior Platinum-based Treatment [NCT00606502]Phase 2201 participants (Actual)Interventional2008-01-31Completed
A Phase 1/2a Open-label Study of Pralatrexate and Gemcitabine With Vitamin B12 and Folic Acid Supplementation in Patients With Relapsed or Refractory Lymphoproliferative Malignancies [NCT00481871]Phase 1/Phase 2119 participants (Actual)Interventional2007-05-31Completed
A Phase 2, Single-arm, Open-label, Multi-center Study of Pralatrexate in Patients With Relapsed or Refractory B-cell Non-Hodgkin's Lymphoma [NCT00998946]Phase 229 participants (Actual)Interventional2009-09-30Completed
A Phase 1/2 Study of Pembrolizumab Plus Pralatrexate for Treatment of Relapsed or Refractory Peripheral T-Cell Lymphomas [NCT03598998]Phase 1/Phase 213 participants (Actual)Interventional2019-02-04Active, not recruiting
A Phase 1, Open-label Study of Pralatrexate With Vitamin B12 and Folic Acid Supplementation in Patients With Relapsed or Refractory Cutaneous T-cell Lymphoma [NCT00554827]Phase 155 participants (Actual)Interventional2007-08-31Completed
A Multi-center, Randomized, Phase 3 Study of Sequential Pralatrexate Versus Observation in Patients Previously Undiagnosed Peripheral T-cell Lymphoma Who Achieved an Objective Response After Initial Treatment With CHOP-based Chemotherapy [NCT01420679]Phase 321 participants (Actual)Interventional2011-08-31Terminated
A Phase II Study of 10-Propargyl-10-Deazaaminopterin (PDX) in Relapsed or Refractory Aggressive Non-Hodgkin's Lymphomas and Hodgkin's Disease [NCT00052442]Phase 1/Phase 272 participants (Actual)Interventional2002-08-31Completed
Pralatrexate in Combination With Oxaliplatin in Advanced Esophago-gastric Cancer: A Phase II Trial With Predictive Molecular Correlates [NCT01178944]Phase 235 participants (Actual)Interventional2010-09-30Completed
Phase 2 Study of Pralatrexate in Female Patients With Previously-treated Advanced or Metastatic Breast Cancer [NCT01118624]Phase 222 participants (Actual)Interventional2010-03-31Completed
A Phase 2, Single-Arm Study of Pralatrexate in Patients With Advanced or Metastatic Relapsed Transitional Cell Carcinoma of the Urinary Bladder [NCT00722553]Phase 230 participants (Actual)Interventional2008-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00052442 (2) [back to overview]Response Rate
NCT00052442 (2) [back to overview]Toxicities of Pralatrexate
NCT00364923 (4) [back to overview]Overall Survival Per Independent Central Review
NCT00364923 (4) [back to overview]Progression-free Survival Per Independent Central Review
NCT00364923 (4) [back to overview]Response Rate Per Independent Central Review
NCT00364923 (4) [back to overview]Duration of Response Per Independent Central Review
NCT00481871 (3) [back to overview]Duration of Response
NCT00481871 (3) [back to overview]Objective Responses Assessed by International Workshop Criteria (IWC)
NCT00481871 (3) [back to overview]Progression-free Survival (PFS) Time
NCT00606502 (4) [back to overview]Overall Survival (OS) of Patients Receiving Pralatrexate vs. Erlotinib
NCT00606502 (4) [back to overview]Progression-free Survival (PFS) of Patients Receiving Pralatrexate vs. Erlotinib
NCT00606502 (4) [back to overview]Adverse Events of Patients Receiving Pralatrexate vs. Erlotinib
NCT00606502 (4) [back to overview]Response Rate (RR) to Treatment of Patients Receiving Pralatrexate vs. Erlotinib
NCT00722553 (5) [back to overview]Clinical Benefit Rate (CBR)
NCT00722553 (5) [back to overview]Duration of Response (DOR)
NCT00722553 (5) [back to overview]Objective Response Rate (ORR)
NCT00722553 (5) [back to overview]Overall Survival (OS)
NCT00722553 (5) [back to overview]Progression Free Survival (PFS)
NCT00998946 (4) [back to overview]Duration of Response (DOR)
NCT00998946 (4) [back to overview]Objective Response Rate (ORR)
NCT00998946 (4) [back to overview]Overall Survival (OS)
NCT00998946 (4) [back to overview]Progression Free Survival (PFS)
NCT01118624 (4) [back to overview]Duration of Response (DOR)
NCT01118624 (4) [back to overview]Incidence of Adverse Events (AEs) and Laboratory Abnormalities
NCT01118624 (4) [back to overview]Objective Response Rate (ORR)
NCT01118624 (4) [back to overview]Overall Survival (OS)
NCT01178944 (6) [back to overview]Number of Participants With an Adverse Event
NCT01178944 (6) [back to overview]Overall Response Rate
NCT01178944 (6) [back to overview]Overall Survival (OS)
NCT01178944 (6) [back to overview]Time to Progression (TTP)
NCT01178944 (6) [back to overview]MicroRNA Expression - miR-215-5p
NCT01178944 (6) [back to overview]Overall Survival (OS) for SNP ATIC/AICART - s10932606 Genotypes
NCT01420679 (2) [back to overview]Overall Survival (OS)
NCT01420679 (2) [back to overview]Number of Participants With Worst Grade Adverse Events (AEs), Deaths, Serious Adverse Events (SAEs), and SAEs Leading to Discontinuation of Study Treatment, and Worst Grade Laboratory Abnormalities

Response Rate

Per Response Evaluation Criteria in T-cell and B-cell Lymphoma for target lesions and assessed using computerized tomography (CT) and or Positron emission tomography CT (PET CT) by local investigators: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=50% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. (NCT00052442)
Timeframe: 3 weeks

InterventionParticipants (Count of Participants)
135 mg/m^2 Pralatrexate 1/2 Weeks15
30 mg/m^2 Pralatrexate 3/4 Weeks3
30 mg/m^2 Pralatrexate 6/7 Weeks27
45 mg/m^2 Pralatrexate 6/7 Weeks11
270 mg/m^2 Pralatrexate 2/4 Weeks15

[back to top]

Toxicities of Pralatrexate

Adverse events; number of patients with at least one adverse events reported. (NCT00052442)
Timeframe: 3 weeks

InterventionParticipants (Count of Participants)
135 mg/m^2 Pralatrexate 1/2 Weeks16
30 mg/m^2 Pralatrexate 3/4 Weeks3
30 mg/m^2 Pralatrexate 6/7 Weeks27
45 mg/m^2 Pralatrexate 6/7 Weeks11
270 mg/m^2 Pralatrexate 2/4 Weeks15

[back to top]

Overall Survival Per Independent Central Review

Calculated as date of death - date of enrollment +1, estimated using the product-limit estimator. Pts who had not died (no record of death) or were lost to follow-up were censored at the date of last contact. Pts who withdrew consent to participate in the study including consent to be followed, were censored on the date of withdrawal. Pts who withdrew from treatment without withdrawing consent were followed for survival status whenever possible. (NCT00364923)
Timeframe: Assessed every 14 weeks while on treatment, and after disease progression no less frequently than every 6 months for up to 2 years after first dose.

InterventionMonths (Median)
Evaluable Population14.5

[back to top]

Progression-free Survival Per Independent Central Review

Patients (pts) with subsequent therapy prior to PD were censored at date of last response assessment prior to subsequent therapy. Pts who were alive without PD were censored at the date of last assessment of first dose. Pts who withdrew consent to participate in the study prior to PD were censored at the date of their last disease assessment or treatment day 1. Pts who withdrew consent from treatment prior to PD without withdrawing consent for follow-up were followed for disease status & survival. Pts who did not have response assessments after baseline were censored at treatment day 1. (NCT00364923)
Timeframe: Calculated as the number of days from treatment day 1 to the date of disease progression or death, regardless of cause for up to 2 years after initial dose

InterventionDays (Median)
Evaluable Population106

[back to top]

Response Rate Per Independent Central Review

Patient response to treatment was determined by independent central review using International Workshop Criteria (IWC). Results present the best overall response. The initial response assessment was scheduled at week 7 (prior to Cycle 2) and then prior to every even-numbered cycle (every 14 weeks) for up to two years after first dose. (NCT00364923)
Timeframe: Response was assessed at 7 weeks (prior to Cycle 2) and then prior to every other even-numbered cycle (every 14 weeks) until disease progression or death for up to 2 years after initial dose

Interventionof Patients who Responded (Number)
Evaluable Population32

[back to top]

Duration of Response Per Independent Central Review

Calculated only for those pts with an objective response. Pts receiving subsequent therapy (including transplant) before progressive disease (PD) was documented were censored at date of last response assessment obtained prior to subsequent therapy, with a note indicating censoring occurrence & reason. Pts who withdrew consent to participate in the study prior to PD were censored at the date of their last evaluable assessment of response. Pts who withdrew from treatment prior to PD or initiation of subsequent therapy without withdrawing consent were followed for disease status when possible. (NCT00364923)
Timeframe: Measured from the first day of documented response, assessed at prior to every other even-numbered cycle (every 14 weeks) until disease progression or death for up to 2 years after initial dose

InterventionDays (Median)
Evaluable Population306

[back to top]

Duration of Response

Duration of response was defined as the number of days between the date of first tumor response assessment of objective response to the time of the first tumor response assessment of progressive disease (PD) or death due to any cause (date of first PD assessment or death - date of first objective response assessment + 1) (NCT00481871)
Timeframe: Response assessments were performed no less than every 3 cycles in the Phase 1 part of the study and every 8 weeks (± 1 week) in the Phase 2a part of the study

Interventiondays (Median)
Phase 1174
Phase 2 - Group B210
Phase 2 - Group C170

[back to top]

Objective Responses Assessed by International Workshop Criteria (IWC)

Number of participants who achieved an objective response. Objective response was defined as a tumor response assessment of either complete response (CR) or partial response (PR) and was determined only for patients with measurable disease at baseline. A tumor response assessment reported by IWC without PET was used for any analyses in cases where an IWC+PET evaluation was not done. (NCT00481871)
Timeframe: Assessed every 8 weeks (+/- 1 week) for Phase II and no less than every 3 cycles for Phase I

Interventionparticipants (Number)
Phase 18
Phase 2 - Group B5
Phase 2 - Group C7

[back to top]

Progression-free Survival (PFS) Time

PFS time was calculated as the number of days from study day 1 to the date of PD or death, regardless of cause (date of PD or death - study day 1 + 1). (NCT00481871)
Timeframe: Response assessments were performed no less than every 3 cycles in the Phase 1 part of the study and every 8 weeks (± 1 week) in the Phase 2a part of the study

Interventiondays (Median)
Phase 153.0
Phase 2 - Group B59.0
Phase 2 - Group C54.0

[back to top]

Overall Survival (OS) of Patients Receiving Pralatrexate vs. Erlotinib

OS was defined as the length of time from randomization until death due to any cause. Patients who were alive at the time of the data cut-off date were censored at the last contact date. (NCT00606502)
Timeframe: Assessed from date of randomization no less frequently than every 16 weeks for up to 2 years after randomization.

InterventionMonths Survival (Median)
Pralatrexate6.7
Erlotinib7.0

[back to top]

Progression-free Survival (PFS) of Patients Receiving Pralatrexate vs. Erlotinib

PFS was calculated as the number of days from randomization to the date of radiological evidence of PD or death due to any cause. (NCT00606502)
Timeframe: Assessed every 8 weeks for the first 24 weeks, then every 16 weeks for up to 2 years or until PD or start of subsequent treatment.

Interventionmonths (Median)
Pralatrexate3.4
Erlotinib2.8

[back to top]

Adverse Events of Patients Receiving Pralatrexate vs. Erlotinib

(NCT00606502)
Timeframe: Assessed every 2 weeks while on treatment through safety follow-up visit (35 +/-5 days post-last dose) or early termination visit (at time of withdrawal).

,
InterventionTreated Participants (Number)
At least one AEGrade 3 AEsGrade 4 AEsAt least one SAE
Erlotinib771802
Pralatrexate7525514

[back to top]

Response Rate (RR) to Treatment of Patients Receiving Pralatrexate vs. Erlotinib

Number of patients whose tumors responded to Pralatrexate or Erlotinib, using the Response Criteria in Solid Tumors (RECIST). (NCT00606502)
Timeframe: Assessed every 8 weeks for the first 24 weeks, then every 16 weeks for up to 2 years or until PD or start of subsequent treatment.

,
InterventionParticipants (Number)
Complete + Partial ResponseComplete Response (CR)Partial Response (PR)Stable Disease (SD)Progressive Disease (PD)Disease Control (CR+PR+SD)Unable to EvaluateMissing (off or no treatment, not confirmed)
Erlotinib716353642020
Pralatrexate202332935231

[back to top]

Clinical Benefit Rate (CBR)

The number of patients with a best confirmed or unconfirmed response of CR, PR, or stable disease (SD) for at least 24 weeks (approximately 5.5 months) (NCT00722553)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks) or per standard of care, but no more than every 12 weeks (+/- 1 week) if treatment has ended, for up to 2 years after enrollment.

Interventionparticipants (Number)
Evaluable Population3

[back to top]

Duration of Response (DOR)

Duration of time from when tumor measurement criteria were met for CR or PR (whichever status was recorded first) until the first date that recurrent disease or progressive disease (PD) or death was objectively documented. Progression is defined, using RECIST, as an increase in the smallest dimension of any target or non-target lesion, or the appearance of new lesions, since baseline. Calculated for those patients with a best overall confirmed or unconfirmed response of CR or PR. (NCT00722553)
Timeframe: Measured from the first day of documented response for up to 2 years after enrollment.

InterventionDays (Median)
Evaluable Patients82

[back to top]

Objective Response Rate (ORR)

The number of patients with a best overall confirmed response of either complete response (CR) or partial response (PR) (NCT00722553)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks), or per standard of care but no more than every 12 weeks (+/- 1 week) if treatment has ended for up to 2 years after enrollment.

Interventionparticipants (Number)
Evaluable Population1

[back to top]

Overall Survival (OS)

The number of days from study day 1 to death. Patients who had not died (no record of death) or were lost to follow-up were censored at the date of last contact. (NCT00722553)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks), or per standard of care if treatment has ended (at least every 12 weeks) for up to 2 years after enrollment. After PD or start of subsequent treatment, OS will be assessed every 4 months.

InterventionMonths (Median)
Evaluable Population9.3

[back to top]

Progression Free Survival (PFS)

Length of time from study day 1 to the date of radiological evidence of PD (date of computed tomography [CT] or magnetic resonance imaging [MRI] scan, whichever indicates PD) or death, regardless of cause. (NCT00722553)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks), or per standard of care but no more than every 12 weeks (+/- 1 week) if treatment has ended, for up to 2 years after enrollment.

InterventionMonths (Median)
Evaluable Population4.0

[back to top]

Duration of Response (DOR)

The Duration of Response was defined as the time (in months) from the date the measurement criteria were first met for CR or PR (whichever status was recorded first) until the first subsequent date that relapse or progression was documented. It was assessed according to IWC with or without PET, subject to its availability. Per IWC, progression was defined as a ≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions. (NCT00998946)
Timeframe: Up to 24 months

Interventionmonths (Median)
PralatrexateNA

[back to top]

Objective Response Rate (ORR)

Objective response rate was defined as the percentage of participants with a complete response (CR) or a partial response (PR). Tumor response was evaluated on the basis of clinical and radiological criteria, assessed according to International Workshop Criteria (IWC) with or without positron emission tomography (PET) scans. Per IWC criteria CR is defined as complete disappearance of all detectable clinical and radiographic evidence of disease and disappearance of all disease-related symptoms if present before therapy, and normalization of those biochemical abnormalities definitely assignable to non-Hodgkin's lymphoma (NHL) and PR is defined as >= 50% decrease in sum of the product of the perpendicular diameters (SPD) of the six largest dominant nodes or nodal masses and no increase in size of other nodes, liver or spleen. (NCT00998946)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
Pralatrexate4

[back to top]

Overall Survival (OS)

Overall Survival was the time (in months) from first administration of study treatment until the date of death. (NCT00998946)
Timeframe: Up to 24 months

Interventionmonths (Median)
PralatrexateNA

[back to top]

Progression Free Survival (PFS)

Progression-free survival (PFS) was the duration of time (in months) from first administration of study treatment to date of first documented progression or death from any cause. It was based on tumor assessments made according to the IWC with or without PET scans, subject to their availability. Per IWC, progression was defined as a ≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions. (NCT00998946)
Timeframe: Up to 24 months

Interventionmonths (Median)
Pralatrexate3.6

[back to top]

Duration of Response (DOR)

One patient has a PR as response and duration of response was provided for that patient. (NCT01118624)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks), or per standard of care but no less than 4 weeks and nor more than every 12 weeks (+/- 1 week) if treatment has ended.

Interventiondays (Number)
Pralatrexate112

[back to top]

Incidence of Adverse Events (AEs) and Laboratory Abnormalities

(NCT01118624)
Timeframe: Recorded at all study visits: every 2 weeks while on treatment and at safety follow-up (35 +/- 5 days post-last dose) or early termination visit (at time of withdrawal).

Interventionparticipants (Number)
Pralatrexate21

[back to top]

Objective Response Rate (ORR)

Tumor response evaluation was performed using RECIST 1.0 using CT/MRI. Proportion of patients achieving a CR or PR is considered in the overall response. (NCT01118624)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks), or per standard of care but no less than 4 weeks and nor more than every 12 weeks (+/- 1 week) if treatment has ended.

Interventionparticipants (Number)
Pralatrexate1

[back to top]

Overall Survival (OS)

Number of days from first dose of pralatrexate to death. (NCT01118624)
Timeframe: Assessed at the end of each even-numbered cycle (every 8 weeks), or per standard of care but at least every 4 weeks and no more than every 12 weeks (+/- 1 week) if treatment has ended. OS will be collected for up to 2 years from start of pralatrexate.

Interventionmonths (Median)
Pralatrexate11.3

[back to top]

Number of Participants With an Adverse Event

Number of participants with an adverse event. Please refer to the adverse event reporting for more detail. Incidence of toxicity as assessed by National Cancer Institute Common Terminology Criteria for Adverse Events version 4.0 (NCT01178944)
Timeframe: Up to 30 days after the last dose of study drug(s)

Interventionparticipants (Number)
Treatment (Pralatrexate, Oxaliplatin)35

[back to top]

Overall Response Rate

Overall response rate to combination pralatrexate and oxaliplatin as assessed by Response Evaluation Criteria in Solid Tumors version 1.1. Objective responses will be confirmed 4 weeks after first documentation of response. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. (NCT01178944)
Timeframe: Up to 5 years

Interventionpercentage of participants (Number)
Treatment (Pralatrexate, Oxaliplatin)26

[back to top]

Overall Survival (OS)

Estimated using the Kaplan-Meier method and proportional hazards models. (NCT01178944)
Timeframe: From the date of study enrollment to the time of death from any cause, assessed up to 5 years

Interventionmonths (Median)
Treatment (Pralatrexate, Oxaliplatin)7.2

[back to top]

Time to Progression (TTP)

Estimated using the Kaplan-Meier method and proportional hazards models. (NCT01178944)
Timeframe: From the date of study enrollment to the first observation of progressive disease, assessed up to 5 years

Interventionmonths (Median)
Treatment (Pralatrexate, Oxaliplatin)5.1

[back to top]

MicroRNA Expression - miR-215-5p

Mean microRNAs expression of mi-215-5p in tumor tissues of responders and non-responders using a microfabricated device called a gene chip. (NCT01178944)
Timeframe: Baseline

InterventionArbitrary fluorescent intensity (Mean)
Responders: CR+PRNon responders: stable disease/progression
Treatment (Pralatrexate, Oxaliplatin)6.65.6

[back to top]

Overall Survival (OS) for SNP ATIC/AICART - s10932606 Genotypes

Kaplan-Meier estimates of median survival time for each genotype (NCT01178944)
Timeframe: From the date of study enrollment up to 5 years

Interventionmonths (Median)
CTTC
Treatment (Pralatrexate, Oxaliplatin)10.2218.714.63

[back to top]

Overall Survival (OS)

Overall survival was defined as the time in days from randomization to the date of death, regardless of cause (date of death - date of randomization + 1). (NCT01420679)
Timeframe: From randomization until death (up to 76 months)

Interventionmonths (Median)
Pralatrexate ArmNA
Observation ArmNA

[back to top]

Number of Participants With Worst Grade Adverse Events (AEs), Deaths, Serious Adverse Events (SAEs), and SAEs Leading to Discontinuation of Study Treatment, and Worst Grade Laboratory Abnormalities

"An AE was any untoward medical occurrence in a participant who received study treatment without regard to possibility of causal relationship. An SAE was an AE resulting in any of following outcomes or deemed significant for any other reason: death, initial or prolonged inpatient hospitalization, life-threatening experience (immediate risk of dying), persistent or significant disability or incapacity, congenital anomaly. AE included both serious and non- SAEs. An AE of Hematology and Chemistry was collected and graded as per National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) Version 4.03, where Grade 3 refers to severe or medically significant but not immediately life threatening and Grade 4 refers to life-threatening consequences." (NCT01420679)
Timeframe: From first dose of study drug to 35 (±5) days after last dose of study drug for the Pralatrexate Arm, and until 35 (± 5) days after the study treatment discontinuation for the Observation Arm (Up to 2 years)

,
InterventionParticipants (Count of Participants)
Participants with Any Treatment Emergent AEsParticipants with Any Grade 3 - 4 AEsParticipants with Treatment Emergent AEs Resulting in DeathsParticipants with Treatment Emergent SAEsParticipants with Any SAEs Leading to Drug DiscontinuationHematology:Higher Than Grade 3/4 Lab AbnormalitiesChemistry:Higher Than Grade 3/4 Lab Abnormalities
Observation Arm6200010
Pralatrexate Arm14814231

[back to top]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
quinacrine
Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.		2.0610acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound		antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
pteridines
[no description available]		1.9510azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
pteridines
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid: An IBOTENIC ACID homolog and glutamate agonist. The compound is the defining agonist for the AMPA subtype of glutamate receptors (RECEPTORS, AMPA). It has been used as a radionuclide imaging agent but is more commonly used as an experimental tool in cell biological studies.		2.0610non-proteinogenic alpha-amino acid
1,3-dipropyl-8-cyclopentylxanthine
DPCPX : An oxopurine that is 7H-xanthine substituted at positions 1 and 3 by propyl groups and at position 8 by a cyclohexyl group.		2.0610oxopurineadenosine A1 receptor antagonist;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
nsc-267703
[no description available]		2.0610anthracycline
dactinomycin
[no description available]		2.0610cyclodepsipeptide
1-aminoindan-1,5-dicarboxylic acid
1-aminoindan-1,5-dicarboxylic acid: structure given in first source		2.0610
amodiaquine
Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.		2.0610aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		2.0610benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
berberine
[no description available]		2.0610alkaloid antibiotic;
berberine alkaloid;
botanical anti-fungal agent;
organic heteropentacyclic compound		antilipemic drug;
antineoplastic agent;
antioxidant;
EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor;
EC 1.21.3.3 (reticuline oxidase) inhibitor;
EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.1.4 (phospholipase A2) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
hypoglycemic agent;
metabolite;
potassium channel blocker
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.0610aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
aricine
[no description available]		2.0610cinchona alkaloid
clofilium
clofilium: RN given refers to parent cpd; structure		2.0610benzenes;
organic amino compound
clotrimazole
[no description available]		2.0610conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
dequalinium
Dequalinium: A topical bacteriostat that is available as various salts. It is used in wound dressings and mouth infections and may also have antifungal action, but may cause skin ulceration.. dequalinium : A quinolinium ion comprising decane in which one methyl hydrogen at each end of the molecule has been replaced by a 4-amino-2-methylquinolin-1-yl group.		2.0610quinolinium ionantifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor
nsc-526417
[no description available]		2.0610
gentian violet
crystal violet cation : An iminium ion that is malachite green cation in which the hydrogen at the para- psition of the monosubstituted phenyl group is replaced by a dimethylamino group.		2.0610iminium ionantibacterial agent;
antifungal agent
hexahydrosiladifenidol
[no description available]		2.0610
mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.		2.0610organofluorine compound;
piperidines;
quinolines;
secondary alcohol
moclobemide
Moclobemide: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.. moclobemide : A member of the class of benzamides that is benzamide substituted by a chloro group at position 4 and a 2-(morpholin-4-yl)ethyl group at the nitrogen atom. It acts as a reversible monoamine oxidase inhibitor and is used in the treatment of depression.		2.0610benzamides;
monochlorobenzenes;
morpholines		antidepressant;
environmental contaminant;
xenobiotic
n-acetyl-4-nitrophenylserinol
N-acetyl-4-nitrophenylserinol: RN given refers to cpd without isomeric designation; structure		2.0610
oxiracetam
oxiracetam: structure in first source		2.0610organonitrogen compound;
organooxygen compound
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		2.0610aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
potassium chloride
Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.		1.9610inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		710benzoic acids;
sulfonamide		uricosuric drug
pronethalol
pronethalol: was heading 1964-94 (Prov 1964-66); NAPHTHYLISOPROTERENOL was see PRONETHALOL 1977-94; use ETHANOLAMINES to search PRONETHALOL 1966-94		2.0610naphthalenes
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		2.0610aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
pyrimethamine
Maloprim: contains above 2 cpds		2.0610aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
scriptaid
scriptide: provokes translocation of GLUT4 to increase glucose uptake; structure in first source		2.0610isoquinolines
6,18,30-trimethyl-3,9,12,15,21,24,27,33,36-nona(propan-2-yl)-1,7,13,19,25,31-hexaoxa-4,10,16,22,28,34-hexazacyclohexatriacontane-2,5,8,11,14,17,20,23,26,29,32,35-dodecone
[no description available]		2.0610cyclodepsipeptide
cycloheximide
Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.		2.0610antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol		anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
phanquinone
phanquinone: structure. phanquone : An orthoquinone that is the 5,6-diketo derivative of 4,7-phenanthroline.		2.0610orthoquinones
diphenan
[no description available]		2.0610diarylmethane
2-phenylacetamide
2-phenylacetamide: structure. 2-phenylacetamide : A monocarboxylic acid amide that is acetamide substituted by a phenyl group at position 2.		2.0610monocarboxylic acid amidemouse 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.		1.9810mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
tetraphenylborate
Tetraphenylborate: An anionic compound that is used as a reagent for determination of potassium, ammonium, rubidium, and cesium ions. It also uncouples oxidative phosphorylation and forms complexes with biological materials, and is used in biological assays.		2.0610
cycloguanil hydrochloride
cycloguanil hydrochloride : The hydrochloride salt of cycloguanil.		2.0610hydrochloride;
organic molecular entity
cycloguanil
cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source. cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil.		2.0610triazinesantifolate;
antiinfective agent;
antimalarial;
antiparasitic agent;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
triphenyltetrazolium
triphenyltetrazolium: RN given refers to parent cpd. 2,3,5-triphenyltetrazolium : An organic cation that is tetrazole carrying three phenyl substituents at positions 2, 3 and 5.		2.0610organic cation
berbamine
[no description available]		2.0610phenylpropanoid
emetine
Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties.		2.0610isoquinoline alkaloid;
pyridoisoquinoline		antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
dequalinium chloride
dequalinium chloride : An organic chloride salt that is the dichloride salt of dequalinium.		2.0610organic chloride saltantifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor
Berberine chloride (TN)
[no description available]		2.0610organic molecular entity
9,10-dimethylanthracene
9,10-dimethylanthracene: RN given refers to parent ion		2.0610
c 137
C 137: RN given refers to parent cpd		2.0610
palmatine
burasaine: structure in first source		2.0610berberine alkaloid;
organic heterotetracyclic compound		plant metabolite
4,6-diamino-2,2-dimethyl-1,2-dihydro-1-phenyl-s-triazine
4,6-diamino-2,2-dimethyl-1,2-dihydro-1-phenyl-s-triazine: structure in first source		2.0610
buquinolate
[no description available]		2.0610
propranolol glycol
propranolol glycol: propranolol metabolite; potent anticonvulsant against strychnine induced convulsions		2.0610
naphthoxybutanolcyclohexylamine
naphthoxybutanolcyclohexylamine: structure		2.0610
staurosporine
[no description available]		2.0610indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
propamidine
propamidine: structure given in first source. propamidine : A polyether that is the bis(4-guanidinophenyl) ether of propane-1,3-diol. Used (as its isethionate salt) for the treatment of minor eye or eyelid infections, such as conjunctivitis and blepharitis.		2.0610aromatic ether;
guanidines;
polyether		antimicrobial agent;
antiseptic drug
neocuproine
neocuproine: Spectrophotometric determination of copper and ultramicro blood sugar determinations; structure; RN given refers to parent cpd. neocuproine : A member of the class of phenanthrolines that is 1,10-phenanthroline bearing two methyl substituents at positions 2 and 9.		2.0610phenanthrolineschelator;
copper chelator
toxoflavin
toxoflavin: azapteridine antibiotic; structure. toxoflavin : A pyrimidotriazine that is 1,6-dimethyl-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine with oxo groups at positions 5 and 7.		2.0610carbonyl compound;
pyrimidotriazine		antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
toxin;
virulence factor;
Wnt signalling inhibitor
plasmenylserine
plasmenylserine: RN given refers to (L)-isomer. O-phospho-L-serine : The L-enantiomer of O-phosphoserine.. O-phosphoserine : A serine derivative that is serine substituted at the oxygen atom by a phosphono group.		2.0610O-phosphoserineEC 1.4.7.1 [glutamate synthase (ferredoxin)] inhibitor;
EC 2.5.1.49 (O-acetylhomoserine aminocarboxypropyltransferase) inhibitor;
EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
quinocide
quinocide: Russian drug; RN given refers to parent cpd; structure		2.0610
2,2',2''-terpyridine
2,2',2''-terpyridine: RN given refers to parent cpd. 2,2':6',2''-terpyridine : A tridentate heterocyclic ligand that binds metals at three meridional sites giving two adjacent 5-membered MN2C2 chelate rings.		2.0610terpyridineschelator
clobetasone butyrate
[no description available]		2.0610organic molecular entity
cletoquine
[no description available]		2.0610
jatrorrhizine
jatrorrhizine: isolated from bark of Enantia chlorantha (Annonaceae); structure given in first source		2.0610alkaloid
lycorine
lycorine: from bulbs of LYCORIS & other plants; RN given refers to (1 alpha,2 beta)-isomer; structure in Merck Index, 9th ed, #5444. lycorine : An indolizidine alkaloid that is 3,12-didehydrogalanthan substituted by hydroxy groups at positions and 2 and a methylenedioxy group across positions 9 and 10. Isolated from Crinum asiaticum, it has been shown to exhibit antimalarial activity.		2.0610indolizidine alkaloidanticoronaviral agent;
antimalarial;
plant metabolite;
protein synthesis inhibitor
bathophenanthroline
4,7-diphenyl-1,10-phenanthroline : A member of the class of phenanthrolines that is 1,10-phenanthroline bearing two phenyl substituents at positions 4 and 7.		2.0610benzenes;
phenanthrolines		chelator
LSM-4272
[no description available]		2.0610beta-carbolines
tryptanthrine
tryptanthrine: minor constituent of traditional Chinese medicine qing dai		2.0610alkaloid antibiotic;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound
ethylhydrocupreine
ethylhydrocupreine: structure; RN given refers to parent cpd. optochin : A cinchona alkaloid consisting of 10,11-dihydrocinchonan bearing hydroxy and ethoxy substituents at positions 9 and 6' respectively.		2.0610aromatic ether;
cinchona alkaloid		EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
2,4-diamino-5,6-dihydro-6,6-dimethyl-5-(4'-methoxyphenyl)-s-triazine
2,4-diamino-5,6-dihydro-6,6-dimethyl-5-(4'-methoxyphenyl)-s-triazine: RN given refers to parent cpd; structure given in first source		2.0610
cinchonine
[no description available]		2.0610(8xi)-cinchonan-9-ol;
cinchona alkaloid		metabolite
7-chloro-4-aminoquinoline
7-chloro-4-aminoquinoline: structure given in first source		2.0610aminoquinoline
mmv665852
MMV665852: an antischistosomal agent		2.0610
1,3,4,10-Tetrahydro-9(2H)-acridinone
[no description available]		2.0610acridines
wr 158122
WR 158122: structure		2.0610
dihydroergocristine
Dihydroergocristine: A 9,10alpha-dihydro derivative of ERGOTAMINE that contains an isopropyl sidechain at the 2' position of the molecule.. dihydroergocristine : Ergocristine in which a single bond replaces the double bond between positions 9 and 10. It is used as the mesylate salt for the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease.		2.0610ergot alkaloidadrenergic antagonist;
vasodilator agent
benzamil
[no description available]		2.0610guanidines;
pyrazines
3',4'-dichlorobenzamil
3',4'-dichlorobenzamil: inhibits Na-Ca exchange in membrane vesicle & papillary muscle preparations from guinea pig heart		2.0610guanidines;
pyrazines
cleistanthin b
cleistanthin B: toxic constituent of Cleistanthus collinus. cleistanthin B : A member of the class of cleistanthins that is cleistanthin A in which the 3,4-di-O-methyl-D-xylopyranosyl group is replaced by a beta-D-glucopyranosyl group.		2.0610beta-D-glucoside;
cleistanthins;
monosaccharide derivative		alpha-adrenergic antagonist;
antihypertensive agent;
diuretic
n-acetyltyramine
N-acetyltyramine: structure given in first source. N-acetyltyramine : A member of the class of tyramines that is tyramine in which one of the hydrogens of the amino group is replaced by an acetyl group.		2.0610acetamides;
tyramines		animal metabolite;
Aspergillus metabolite;
bacterial metabolite;
marine metabolite;
quorum sensing inhibitor
1,3-di(4-imidazolinophenoxyl)propane
1,3-di(4-imidazolinophenoxyl)propane: structure given in first source		2.0610
methotrexate
[no description available]		6.4232dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
7h-pyrido(4,3-c)carbazole
7H-pyrido(4,3-c)carbazole: structure given in first source		2.0610
imiloxan
[no description available]		2.0610benzodioxine
cl 246738
3,6-bis(2-piperidinoethoxy)acridine trihydrochloride: immunomodulator; structure given in first source; RN given for tri-HCl		2.0610
celastrol methyl ester
celastrol methyl ester: isolated from Tripterygium wilfordii; potent inhibitory activity on both Kir2.1 and ERG1 potassium channels, leading to LONG QT SYNDROME		2.0610carboxylic ester
epiberberine
epiberberine: isolated in plants of Coptis from China		2.0610
2-phenyl-4-oxohydroquinoline
2-phenyl-4-oxohydroquinoline: structure given in first source		2.0610
aminopterin
Aminopterin: A folic acid derivative used as a rodenticide that has been shown to be teratogenic.		6.65302dicarboxylic acidEC 1.5.1.3 (dihydrofolate reductase) inhibitor;
mutagen
cypripedin
cypripedin: sensitizing agent for contact dermatitis from Lady Slipper (Cypripedium calceolus); structure		2.0610phenanthrol
respinomycin d
respinomycin D: structure given in first source; isolated from Streptomyces xanthocidicus		2.0610
acetoxycycloheximide
acetoxycycloheximide: structure		2.0610
(R)-Roemerine
[no description available]		2.0610isoquinoline alkaloid
2-guanidine-4-methylquinazoline
2-guanidine-4-methylquinazoline: structure given in first source		2.0610
mensacarcin
mensacarcin: structure in first source		2.0610
puromycin
[no description available]		2.0610puromycinsantiinfective agent;
antimicrobial agent;
antineoplastic agent;
EC 3.4.11.14 (cytosol alanyl aminopeptidase) inhibitor;
EC 3.4.14.2 (dipeptidyl-peptidase II) inhibitor;
nucleoside antibiotic;
protein synthesis inhibitor
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		2.0610cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
cephaelin
cephaelin: do not confuse with cephalin of brain; after emetine this is the most important alkaloid of ipecac; protein synthesis inhibitor. cephaeline : A pyridoisoquinoline comprising emetam having a hydroxy group at the 6'-position and methoxy substituents at the 7'-, 10- and 11-positions.		2.0610pyridoisoquinoline
n-formylmethionine leucyl-phenylalanine
N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.		1.9710tripeptide
epothilone b
[no description available]		2.0610epothilone;
epoxide		antineoplastic agent;
apoptosis inducer;
microtubule-stabilising agent
wr-142,490
(+)-(11R,2'S)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (+)-(11R,2'S)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		2.0610[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		2.0610actinomycinmutagen
1,3,6-trimethylpyrimido[5,4-e][1,2,4]triazine-5,7-dione
[no description available]		2.0610pyrimidotriazine
jp-1302
[no description available]		2.0610
7-hydroxy-2-methoxy-1,4-phenanthrenedione
7-hydroxy-2-methoxy-1,4-phenanthrenedione: structure in first source; from Dendrobium densiflorum		2.0610
cgp 60474
[no description available]		2.0610substituted aniline
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol
[no description available]		2.0610alkylbenzene
2-[2-hydroxy-6,7-dimethoxy-4-(4-morpholinyl)-1-naphthalenyl]-N-phenylacetamide
[no description available]		2.0610naphthols
N4-(3-chlorophenyl)-6-methyl-N2-(phenylmethyl)pyrimidine-2,4-diamine
[no description available]		2.0610aralkylamine
n-(4-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine
N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine: calcium-activated small conductance potassium channels inhibitor; structure in first source		2.0610
2,6-bis(benzimidazol-2-yl)pyridine
2,6-bis(benzimidazol-2-yl)pyridine: structure in first source		2.0610benzimidazoles
n-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine
N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine: an SK channel inhibitor		2.0610
N-[4-(1-azepanyl)phenyl]-2-chloroacetamide
[no description available]		2.0610anilide
N-(4-methylphenyl)carbamic acid (cyclopentylideneamino) ester
[no description available]		2.0610toluenes
(2'-(4-aminophenyl)-(2,5'-bi-1h-benzimidazol)-5-amine)
[no description available]		2.0610benzimidazoles
1,4,8-trimethyl-12-quinolino[2,3-b]quinolinamine
[no description available]		2.0610aminoquinoline
2-furanyl-(4,4,8-trimethyl-1-sulfanylidene-5-dithiolo[3,4-c]quinolinyl)methanone
[no description available]		2.0610aromatic amide;
heteroarene
1-(6-methoxy-2,2,4-trimethyl-1-quinolinyl)-2-[[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]thio]ethanone
[no description available]		2.0610quinolines
stk295900
[no description available]		2.0610
6-(4-methyl-1-piperazinyl)-2-(3,4,5-trimethoxyphenyl)-1H-benzimidazole
[no description available]		2.0610benzimidazoles
N9-(4-butoxyphenyl)-6,8,10-triazaspiro[4.5]deca-6,9-diene-7,9-diamine
[no description available]		2.0610aromatic ether
N-[2-[5-(1,3-benzothiazol-2-yl)-3-ethyl-1-phenyl-2-benzimidazol-3-iumyl]ethenyl]-N-methylaniline
[no description available]		2.0610benzimidazoles
4-(1-adamantyl)-2-methyl-1,3-thiazole
[no description available]		2.0610thiazoles
2-amino-6-[4-(6-chloro-2-pyridinyl)-1-piperazinyl]pyridine-3,5-dicarbonitrile
[no description available]		2.0610piperazines;
pyridines
1-(4-fluorophenyl)-3-[4-(4-fluorophenyl)-2-methyl-5-(trifluoromethyl)-3-pyrazolyl]urea
[no description available]		2.0610pyrazoles;
ring assembly
2-(4,6,7-Trimethyl-2-quinazolinyl)guanidine
[no description available]		2.0610quinazolines
polysulfide rubber
[no description available]		2.0610
lch-7749944
LCH-7749944: potent p21-activated kinase 4 inhibitor, structure in first source		2.0610
4-(4-nitrophenyl)-N-prop-2-enyl-1-piperazinecarbothioamide
[no description available]		2.0610piperazines
zd 6474
CH 331: structure in first source		2.0610aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
5-bromo-1-(1-oxopropyl)-N,N-dipropyl-2,3-dihydroindole-7-sulfonamide
[no description available]		2.0610indoles
N-cyclohexyl-5,6,7,8-tetrahydro-4H-cyclohepta[d]isoxazole-3-carboxamide
[no description available]		2.0610aromatic amide;
heteroarene
2-[(3-ethyl-7-methyl-4-oxo-6,8-dihydro-5H-pyrido[2,3]thieno[2,4-b]pyrimidin-2-yl)thio]-N-(2-phenylethyl)acetamide
[no description available]		2.0610organic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
trichomonacid
trichomonacid: RN given refers to phosphate (1:3) salt		2.0610
N-(4-bromo-3-methylphenyl)-2,5-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
[no description available]		2.0610triazolopyrimidines
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(2-methoxyethyl)-3-oxo-1H-isoindole-4-carboxamide
[no description available]		2.0610isoindoles
cgp 71683 a
[no description available]		2.0610naphthalenes;
sulfonic acid derivative
2-(dimethylaminostyryl)-1-ethylpyridinium
2-(dimethylaminostyryl)-1-ethylpyridinium: fluorescent monitor for energetic state of isolated brown- adipose-tissue mitochondria; RN given refers to parent cpd; synonym DASPEI refers to iodide		2.0610pyridinium ion
hydrocortisone acetate, (11beta)-isomer
[no description available]		2.0610
xib 4035
XIB 4035: a GFRalpha-1 agonist; structure in first source		2.0610
10-hydroxy-3-methyl-8-pentyl-2,4-dihydro-1H-[1]benzopyrano[3,4-c]pyridin-5-one
[no description available]		2.0610pyridochromene
lumefantrine
Lumefantrine: A fluorene derivative that is used in combination with ARTEMETHER for the treatment of MALARIA (see ARTEMETHER-LUMEFANTRINE DRUG COMBINATION).. lumefantrine : A member of the class of fluorenes that is 9-(p-chlorobenzylidene)-9H-fluorene which is substitutec by chlorine at positions 2 and 7, and by a 2-(dibutylamino)-1-hydroxyethyl group at position 4. An antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.		2.0610fluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine		antimalarial
edatrexate
edatrexate: structure given in first source		3.85120glutamic acid derivative
norketotifen
norketotifen: Ketotifen is an antimalarial prodrug of norketotifen with blood schizonticidal and liver-stage efficacy; structure in first source		2.0610organosulfur heterocyclic compound
aee 788
AEE 788: structure in first source		2.06106-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineangiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist;
trypanocidal drug
tomaymycin
tomaymycin: structure. tomaymycin : A pyrrolobenzodiazepine that is (11aS)-2,3,5,10,11,11a-hexahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine which is substituted at positions 2,5,7,8 and 11R by ethylidene, oxo, methoxy, hydroxy and methoxy groups, respectively. It is a natural product of Streptomyces achromogenes that binds covalently with guanine in the minor groove of DNA. It is an antitumoral compound which is active in ovarian, plasmacytoma, and leukemia cancer cell lines at nanomolar concentrations.. (Z)-tomaymycin : The (Z)-isomer of tomaymycin.		2.0610tomaymycin
gramicidin a
Gramicidin: A group of peptide antibiotics from BACILLUS brevis. Gramicidin C or S is a cyclic, ten-amino acid polypeptide and gramicidins A, B, D are linear. Gramicidin is one of the two principal components of TYROTHRICIN.		2.0610
N-methyl-3-[5-(3-phenylpropyl)-1,3,4-oxadiazol-2-yl]-N-(3-thiophenylmethyl)propanamide
[no description available]		2.0610benzenes
dihydrofolate
dihydrofolic acid : A folic acid derivative acted upon by dihydrofolate reductase to produce tetrahydrofolic acid. It interacts with bacteria during cell division and is targeted by various drugs to prevent nucleic acid synthesis.		6.9610dihydrofolic acidsEscherichia coli metabolite;
mouse metabolite
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		4.4551folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
1-[amino-[(6-methoxy-4-methyl-2-quinazolinyl)amino]methylidene]-3-phenylurea
[no description available]		2.0610quinazolines
ConditionIndicatedRelationship StrengthStudiesTrials
Leucocythaemia
[description not available]		02.3720
Leukemia L 1210
[description not available]		03.5790
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)		02.3720
Carcinoma, Ehrlich Tumor
A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.		02.6530
Experimental Mammary Neoplasms
[description not available]		02.3920
Rheumatoid Arthritis
[description not available]		04.6232
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		04.6232
Infections, Plasmodium
[description not available]		02.0610
Malaria
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.		02.0610
Experimental Neoplasms
[description not available]		02.8840
Adenocarcinoma, Basal Cell
[description not available]		02.3820
Cancer of Colon
[description not available]		01.9610
Cancer of Rectum
[description not available]		01.9610
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.3820
Colonic Neoplasms
Tumors or cancer of the COLON.		01.9610
Rectal Neoplasms
Tumors or cancer of the RECTUM.		01.9610
Sarcoma 180
An experimental sarcoma of mice.		02.6630
Carcinoma, Non-Small Cell Lung
[description not available]		01.9910
Cancer of Lung
[description not available]		01.9910
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.		01.9910
Lung Neoplasms
Tumors or cancer of the LUNG.		01.9910
Cancer of Liver
[description not available]		01.9510
Plasma Cell Tumor
[description not available]		01.9510
Liver Neoplasms
Tumors or cancer of the LIVER.		01.9510
Plasmacytoma
Any discrete, presumably solitary, mass of neoplastic PLASMA CELLS either in BONE MARROW or various extramedullary sites.		01.9510
Autoimmune Disease
[description not available]		01.9810
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		01.9810
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		01.9810
Dermatitis
Any inflammation of the skin.		01.9810
Proteinuria
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.		01.9810
Benign Neoplasms
[description not available]		02.3720
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.		02.3720
Acute Myelogenous Leukemia
[description not available]		01.9610
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.		01.9610
Bladder Cancer
[description not available]		01.9610
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		01.9610
Carcinoma, Transitional Cell
A malignant neoplasm derived from TRANSITIONAL EPITHELIAL CELLS, occurring chiefly in the URINARY BLADDER; URETERS; or RENAL PELVIS.		01.9610
Breast Cancer
[description not available]		06.9710
Innate Inflammatory Response
[description not available]		01.9710
Breast Neoplasms
Tumors or cancer of the human BREAST.		01.9710
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		01.9710