Page last updated: 2024-12-08

irofulven

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

Description

irofulven: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID148189
CHEMBL ID118218
CHEBI ID135002
SCHEMBL ID8800
MeSH IDM0268775

Synonyms (42)

Synonym
(r)-6'-hydroxy-3'-(hydroxymethyl)-2',4',6'-trimethylspiro(cyclopropane-1,5'-(5h)inden)-7'(6'h)-one
irofulven
spiro(cyclopropane-1,5'(5h)-inden)-7'(6'h)-one, 6'-hydroxy-3'-(hydroxymethyl)-2',4',6'-trimethyl-, (r)-
6-(hydroxymethyl)acylfulvene
mgi 114
acylfulvene, 6-(hydroxymethyl)-
nsc 683863
nsc-683863
nsc683863
NCI60_030149
158440-71-2
irofulven (usan/inn)
D04614
6-hydroxymethylacylfulvene
hmaf
CHEBI:135002
mgi-114
lp-100
CHEMBL118218
(hydroxymethyl)acylfulvene
(5'r)-5'-hydroxy-1'-(hydroxymethyl)-2',5',7'-trimethylspiro[cyclopropane-1,6'-indene]-4'-one
mgi.114
6b799ih05a ,
unii-6b799ih05a
irofulven [usan:inn]
bdbm50410835
(-)-irofulven
DB05786
SCHEMBL8800
irofulven [who-dd]
mgi114
irofulven [mi]
irofulven [inn]
irofulven [usan]
DTXSID50166423
AKOS027256650
Q6072197
NICJCIQSJJKZAH-AWEZNQCLSA-N
MS-23493
HY-14429
CS-0003353
spiro[cyclopropane-1,5'-[5h]inden]-7'(6'h)-one, 6'-hydroxy-3'-(hydroxymethyl)-2',4',6'-trimethyl-, (6'r)-

Research Excerpts

Overview

Irofulven is a semi-synthetic derivative of Illudin S, a toxic sesquiterpene isolated from the mushroom Omphalotus illudens. It is a potent anticancer agent with activity against a broad range of human tumors.

ExcerptReferenceRelevance
"Irofulven is a semi-synthetic derivative of Illudin S, a toxic sesquiterpene isolated from the mushroom Omphalotus illudens. "( Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
Estes, LA; Kashinatham, A; Kelner, MJ; McMorris, TC; Staake, MD, 2016
)
2.17
"Irofulven is a novel, small molecular weight semisynthetic compound, derived from a family of mushroom toxins known as illudins. "( Relation between Irofulven (MGI-114) systemic exposure and tumor response in human solid tumor xenografts.
Billups, C; Cheshire, PJ; Fouladi, M; Friedman, HS; Houghton, PJ; Leggas, M; Peterson, JK; Stewart, CF; Woo, MH, 2002
)
2.1
"Irofulven is a potent anticancer agent with activity against a broad range of human tumors in vitro and in vivo."( Irofulven, a novel inhibitor of DNA synthesis, in metastatic renal cell cancer.
Amato, RJ; Pagliaro, L; Perez, C, 2002
)
2.48
"Irofulven is a novel alkylating agent with promising clinical activity, particularly toward ovarian and hormone-refractory prostate cancers. "( Irofulven cytotoxicity depends on transcription-coupled nucleotide excision repair and is correlated with XPG expression in solid tumor cells.
Koeppel, F; Larsen, AK; Lazar, V; Poindessous, V; Raymond, E; Sarasin, A, 2004
)
3.21
"Irofulven (MGI 114) is a novel, clinically active sesquiterpene whose mechanism of action is not fully understood. "( Irofulven (6-hydroxymethylacylfulvene, MGI 114) induces caspase 8 and 9-mediated apoptosis in human pancreatic adenocarcinoma cells.
MacDonald, JR; Miller, AR; Strodel, WE; Von Hoff, DD; Wang, W; Waters, SJ,
)
3.02

Effects

Irofulven has an unusual activity spectrum with strong activity toward tumor cells of epithelial origin. It has shown promising activity in clinical trials and has been shown to induce DNA damage and apoptosis in vitro.

ExcerptReferenceRelevance
"Irofulven has an unusual activity spectrum with strong activity toward tumor cells of epithelial origin. "( Marked activity of irofulven toward human carcinoma cells: comparison with cisplatin and ecteinascidin.
Comisso, M; Koeppel, F; Larsen, AK; Poindessous, V; Raymond, E; Waters, SJ, 2003
)
2.09
"Irofulven has displayed significant antitumor activity in various clinical trials but displayed a limited therapeutic index."( Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
Estes, LA; Kashinatham, A; Kelner, MJ; McMorris, TC; Staake, MD, 2016
)
1.45
"Irofulven has an unusual activity spectrum with strong activity toward tumor cells of epithelial origin. "( Marked activity of irofulven toward human carcinoma cells: comparison with cisplatin and ecteinascidin.
Comisso, M; Koeppel, F; Larsen, AK; Poindessous, V; Raymond, E; Waters, SJ, 2003
)
2.09
"Irofulven has demonstrated potent activity against a broad range of solid tumors in both cellular and xenograft models and has shown promising activity in clinical trials."( Enhanced antitumor activity of irofulven in combination with 5-fluorouracil and cisplatin in human colon and ovarian carcinoma cells.
Cvitkovic, E; Koeppel, F; Larsen, AK; Poindessous, V; Raymond, E; Waters, SJ, 2003
)
1.33
"Irofulven has been shown to induce DNA damage and apoptosis in vitro and has shown activity in a number of human tumor xenograft models."( Phase I clinical and pharmacokinetic trial of irofulven.
Alberti, D; Arzoomanian, R; Bailey, H; Binger, K; Feierabend, C; MacDonald, J; Marnocha, R; Smith, C; Smith, S; Steele, T; Thomas, JP; Tutsch, KD; Wilding, G, 2001
)
1.29
"Irofulven has demonstrated activity against a broad range of solid tumors in both xenograft models and human trials."( Enhanced antitumor activity of irofulven in combination with thiotepa or mitomycin C.
Estes, L; Kelner, MJ; McMorris, TC; Rojas, RJ; Trani, NA, 2002
)
1.32

Actions

ExcerptReferenceRelevance
"Irofulven displays synergistic antiproliferative and pro-apoptotic effects when combined with oxaliplatin over a broad range of concentrations in human colon and breast cancer cells. "( Characterizations of irofulven cytotoxicity in combination with cisplatin and oxaliplatin in human colon, breast, and ovarian cancer cells.
Calvo, F; Cvitkovic, E; Koeppel, F; Laar, ES; Larsen, AK; Lokiec, F; Poindessous, V; Raymond, E; Serova, M; Waters, SJ, 2006
)
2.1

Treatment

Irofulven treatment resulted in rapid (12hr) dissipation of the mitochondrial membrane potential, phosphatidylserine externalization, and apoptotic DNA fragmentation. Irofulven-treated cells also demonstrated PARP3 cleavage and DAPI staining.

ExcerptReferenceRelevance
"Irofulven treatment resulted in rapid (12hr) dissipation of the mitochondrial membrane potential, phosphatidylserine externalization, and apoptotic DNA fragmentation, with progressive changes after 24hr."( Apoptosis induction by the dual-action DNA- and protein-reactive antitumor drug irofulven is largely Bcl-2-independent.
Herzig, MC; Liang, H; MacDonald, JR; Salinas, R; Trevino, AV; Waters, SJ; Woynarowska, BA; Woynarowski, JM, 2003
)
1.27
"Irofulven-treated cells also demonstrated PARP3 cleavage and DAPI staining."( Irofulven (6-hydroxymethylacylfulvene, MGI 114) induces caspase 8 and 9-mediated apoptosis in human pancreatic adenocarcinoma cells.
MacDonald, JR; Miller, AR; Strodel, WE; Von Hoff, DD; Wang, W; Waters, SJ,
)
2.3
"Irofulven treatment resulted in marginal caspase-3 processing in MDA-MB-231 and HMEC cells."( Irofulven induces apoptosis in breast cancer cells regardless of caspase-3 status.
Herzig, MC; Johnson, AE; Liang, H; Woynarowska, B; Woynarowski, JM, 2002
)
2.48

Toxicity

ExcerptReferenceRelevance
" Markedly fewer intracellular molecules of MGI 114 were required to kill human tumor cells in vitro as compared to the parent acylfulvene, indicating that MGI 114 was markedly more toxic on a cellular level."( Characterization of MGI 114 (HMAF) histiospecific toxicity in human tumor cell lines.
Bagnell, RD; Estes, L; Kelner, MJ; McMorris, TC; Montoya, MA; Rutherford, M; Samson, KM; Taetle, R; Uglik, SF, 1999
)
0.3
" The aim of this analysis was to better characterize the visual adverse events of irofulven and provide treatment guidelines."( Characterization and multiparameter analysis of visual adverse events in irofulven single-agent phase I and II trials.
Alexandre, J; Cullen, M; Cvitkovic, E; Elman, M; Kahatt, C; Lee, MS; Lokiec, F; MacDonald, JR; Misset, JL; Raymond, E; Rigolet, MH; Sutherland, W; Tombal, B, 2004
)
0.78

Pharmacokinetics

irofulven has a rapid elimination half-life of 2 to 10 minutes. The agent exhibited dose-proportional increases in both maximum plasma concentrations and area under the concentration-time curve.

ExcerptReferenceRelevance
" Pharmacokinetic studies were performed on days 1 and 5 to characterize the plasma disposition of irofulven."( Phase I and pharmacokinetic study of irofulven, a novel mushroom-derived cytotoxin, administered for five consecutive days every four weeks in patients with advanced solid malignancies.
Baker, SD; Britten, CD; Clark, GM; Drengler, R; Eckhardt, SG; Felton, S; Hammond, LA; Hidalgo, M; Kuhn, JG; MacDonald, JR; Moczygemba, J; Rowinsky, EK; Siu, L; Smith, C; Smith, SL; Villalona-Calero, MA; Von Hoff, DD; Weitman, S, 2000
)
0.8
" Pharmacokinetic studies of irofulven revealed dose-proportional increases in both maximum plasma concentrations and area under the concentration-time curve, while the agent exhibited a rapid elimination half-life of 2 to 10 minutes."( Phase I and pharmacokinetic study of irofulven, a novel mushroom-derived cytotoxin, administered for five consecutive days every four weeks in patients with advanced solid malignancies.
Baker, SD; Britten, CD; Clark, GM; Drengler, R; Eckhardt, SG; Felton, S; Hammond, LA; Hidalgo, M; Kuhn, JG; MacDonald, JR; Moczygemba, J; Rowinsky, EK; Siu, L; Smith, C; Smith, SL; Villalona-Calero, MA; Von Hoff, DD; Weitman, S, 2000
)
0.87
"Our aim was to develop a population pharmacokinetic model for irofulven and to assess covariates that might affect irofulven pharmacokinetics."( Phase I population pharmacokinetics of irofulven.
Alexandre, J; Brain, E; Cvitkovic, E; Lokiec, F; Raymond, E; Shah, A; Smith, S; Urien, S, 2003
)
0.83
"We performed a Phase I and pharmacokinetic study to determine the maximum tolerated dose of irofulven (6-hydroxymethylacylfulvene; MGI-114, MGI PHARMA, Inc."( Phase I and pharmacokinetic study of irofulven administered weekly or biweekly in advanced solid tumor patients.
Alexandre, J; Brain, EC; Cvitkovic, E; Faivre, S; Goldwasser, F; Kaci, MO; Kahatt, C; Lokiec, F; MacDonald, JR; Misset, JL; Raymond, E; Smith, SL; Yovine, A, 2004
)
0.82
"Forty patients and 75 pharmacokinetic time-courses were available for analysis."( Pharmacokinetic modelling of 5-FU production from capecitabine--a population study in 40 adult patients with metastatic cancer.
Lokiec, F; RezaĆ­, K; Urien, S, 2005
)
0.33
" The C(max), AUC(0-infinity), and terminal half-life values for total radioactivity were 1130 ng-Eq/ml, 24,400 ng-Eq ."( Pharmacokinetics, metabolism, and routes of excretion of intravenous irofulven in patients with advanced solid tumors.
Cvitkovic, E; De Valeriola, D; Deroussent, A; Kahatt, C; Lokiec, F; Paci, A; Re, M; Rezai, K; Shah, A; Vassal, G; Waters, S; Weems, G; Weill, S, 2006
)
0.57
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

irofulven displays strong activity as monotherapy and in combination with mitoxantrone or docetaxel against androgen-independent prostate cancer. These results indicate that the therapeutic activity of irofulVEN is enhanced when combined with mitomycin C or thiotepa.

ExcerptReferenceRelevance
" In this study, the potential application of MGI-114 in the treatment of colon cancer was further explored by evaluating the activity of MGI-114 in combination with irinotecan (CPT-11) and 5-fluorouracil (5FU)."( Enhanced antitumor activity of 6-hydroxymethylacylfulvene in combination with irinotecan and 5-fluorouracil in the HT29 human colon tumor xenograft model.
Britten, CD; Eckhardt, SG; Hilsenbeck, SG; MacDonald, JR; Mangold, G; Marty, J; Rowinsky, EK; Von Hoff, DD; Weitman, S, 1999
)
0.3
" The studies were conducted to evaluate the antitumor activity of MGI 114 as a single agent and in combination with topotecan against pediatric solid tumor cell lines and xenograft models."( MGI 114: augmentation of antitumor activity when combined with topotecan.
Barrera, H; Gonzalez, C; Hilsenbeck, S; MacDonald, JR; Marty, J; Moore, R; Von Hoff, D; Waters, SJ; Weitman, S,
)
0.13
" This study explored the pro-apoptosis and anti-proliferative potential of HMAF in combination with gamma radiation in human prostate tumor cell lines."( Targeting apoptosis by hydroxymethylacylfulvene in combination with gamma radiation in prostate tumor cells.
Herman, TS; MacDonald, JR; Roberts, K; Woynarowska, BA; Woynarowski, JM, 2000
)
0.31
" In this study, the potential application of MGI 114 in the treatment of lung cancer was explored by evaluating the activity of MGI 114 in combination with either topotecan (TPT) or paclitaxel."( Enhanced antitumour activity of 6-hydroxymethylacylfulvene in combination with topotecan or paclitaxel in the MV522 lung carcinoma xenograft model.
Eckhardt, SG; Hammond, LA; Hilsenbeck, SG; MacDonald, JR; Mangold, G; Marty, J; Rowinsky, EK; Von Hoff, DD; Weitman, S, 2000
)
0.31
" The potential application of administering irofulven in combination with aziridine-containing chemotherapeutic agents was evaluated in this study."( Enhanced antitumor activity of irofulven in combination with thiotepa or mitomycin C.
Estes, L; Kelner, MJ; McMorris, TC; Rojas, RJ; Trani, NA, 2002
)
0.86
"Human lung carcinoma MV522 cells and BALB/c athymic mice bearing the human lung carcinoma MV522 xenograft were used to evaluate the activity of irofulven in combination with aziridine-containing drugs."( Enhanced antitumor activity of irofulven in combination with thiotepa or mitomycin C.
Estes, L; Kelner, MJ; McMorris, TC; Rojas, RJ; Trani, NA, 2002
)
0.8
"Irofulven in combination with either thiotepa or mitomycin C demonstrated a strong synergistic (supraadditive) activity both in vitro and in vivo, that exceeded results obtained with monotherapy at the same or higher doses of these agents."( Enhanced antitumor activity of irofulven in combination with thiotepa or mitomycin C.
Estes, L; Kelner, MJ; McMorris, TC; Rojas, RJ; Trani, NA, 2002
)
2.04
"These results indicate that the therapeutic activity of irofulven is enhanced when combined with mitomycin C or thiotepa, and further evaluation of these combinations is therefore warranted."( Enhanced antitumor activity of irofulven in combination with thiotepa or mitomycin C.
Estes, L; Kelner, MJ; McMorris, TC; Rojas, RJ; Trani, NA, 2002
)
0.85
"The aim of this study was to determine the antitumor activity of irofulven when administered in combination with a variety of antimitotic agents."( Enhanced antitumor activity of irofulven in combination with antimitotic agents.
Estes, LA; Kelner, MJ; McMorris, TC; Rojas, RJ; Suthipinijtham, P; Trani, NA; Velasco, TR, 2002
)
0.84
" The enhanced cytotoxicity of irofulven in combination with cisplatin and 5-FU support the clinical application of these regimens."( Enhanced antitumor activity of irofulven in combination with 5-fluorouracil and cisplatin in human colon and ovarian carcinoma cells.
Cvitkovic, E; Koeppel, F; Larsen, AK; Poindessous, V; Raymond, E; Waters, SJ, 2003
)
0.89
" This report examines the efficacy of irofulven alone or in combination with mitoxantrone or docetaxel against androgen-independent prostate cancer cell lines."( Antitumor activity of irofulven monotherapy and in combination with mitoxantrone or docetaxel against human prostate cancer models.
MacDonald, JR; Van Laar, ES; Waters, SJ; Weitman, S, 2004
)
0.91
"These studies demonstrate that irofulven displays strong activity as monotherapy and in combination with mitoxantrone or docetaxel against androgen-independent prostate cancer in vitro and in vivo; thus, supporting the clinical investigation of irofulven against hormone-refractory prostate cancer."( Antitumor activity of irofulven monotherapy and in combination with mitoxantrone or docetaxel against human prostate cancer models.
MacDonald, JR; Van Laar, ES; Waters, SJ; Weitman, S, 2004
)
0.92
" The cytotoxic activity of irofulven is augmented when combined with agents that interact with DNA topoisomerase I; however, none of the reported studies have used the protracted dosing schedule found to be active clinically in treatment of childhood cancers."( Enhanced antitumor activity of irofulven in combination with irinotecan in pediatric solid tumor xenograft models.
Billups, C; Bjornsti, MA; Houghton, PJ; Liang, H; Peterson, JK; Woo, MH, 2005
)
0.91
" At the same doses, irofulven in combination with irinotecan demonstrated superior antitumor activity, inducing complete responses in seven of the eight xenograft lines."( Enhanced antitumor activity of irofulven in combination with irinotecan in pediatric solid tumor xenograft models.
Billups, C; Bjornsti, MA; Houghton, PJ; Liang, H; Peterson, JK; Woo, MH, 2005
)
0.94
"These studies show that the cytotoxic activity of irofulven is greater when combined with protracted administration of irinotecan."( Enhanced antitumor activity of irofulven in combination with irinotecan in pediatric solid tumor xenograft models.
Billups, C; Bjornsti, MA; Houghton, PJ; Liang, H; Peterson, JK; Woo, MH, 2005
)
0.87
"This study assessed the cytotoxic effects of irofulven in combination with oxaliplatin and cisplatin in a panel of human cancer cell lines."( Characterizations of irofulven cytotoxicity in combination with cisplatin and oxaliplatin in human colon, breast, and ovarian cancer cells.
Calvo, F; Cvitkovic, E; Koeppel, F; Laar, ES; Larsen, AK; Lokiec, F; Poindessous, V; Raymond, E; Serova, M; Waters, SJ, 2006
)
0.91
"Irofulven displays synergistic antiproliferative and pro-apoptotic effects when combined with oxaliplatin over a broad range of concentrations in human colon and breast cancer cells."( Characterizations of irofulven cytotoxicity in combination with cisplatin and oxaliplatin in human colon, breast, and ovarian cancer cells.
Calvo, F; Cvitkovic, E; Koeppel, F; Laar, ES; Larsen, AK; Lokiec, F; Poindessous, V; Raymond, E; Serova, M; Waters, SJ, 2006
)
2.1
" The human lung carcinoma MV522 cell line and its corresponding xenograft model were used to evaluate the activity of irofulven in combination with these different agents."( Synergy of Irofulven in combination with various anti-metabolites, enzyme inhibitors, and miscellaneous agents in MV522 lung carcinoma cells: marked interaction with gemcitabine and 5-fluorouracil.
Estes, LA; Kelner, MJ; McMorris, TC; Rojas, RJ; Suthipinijtham, P, 2008
)
0.94
" The aim of this study was to determine the antitumor activity of irofulven when administered in combination with 44 different DNA damaging agents, whose damage is in general detected and repaired by the genome repair pathway."( Synergy of irofulven in combination with other DNA damaging agents: synergistic interaction with altretamine, alkylating, and platinum-derived agents in the MV522 lung tumor model.
Estes, LA; Kelner, MJ; McMorris, TC; Rojas, RJ; Suthipinijtham, P, 2008
)
0.97
"The human lung carcinoma MV522 cell line and its corresponding xenograft model were used to evaluate the activity of irofulven in combination with different DNA damaging agents."( Synergy of irofulven in combination with other DNA damaging agents: synergistic interaction with altretamine, alkylating, and platinum-derived agents in the MV522 lung tumor model.
Estes, LA; Kelner, MJ; McMorris, TC; Rojas, RJ; Suthipinijtham, P, 2008
)
0.95
"These results indicate that the antitumor activity of irofulven is enhanced when combined with platinum-derived agents, altretamine, and select alkylating agents such as melphalan or chlorambucil."( Synergy of irofulven in combination with other DNA damaging agents: synergistic interaction with altretamine, alkylating, and platinum-derived agents in the MV522 lung tumor model.
Estes, LA; Kelner, MJ; McMorris, TC; Rojas, RJ; Suthipinijtham, P, 2008
)
0.98

Dosage Studied

irofulven combined with gemcitabine may have activity in patients with pancreatic tumors. The cytotoxic activity is augmented when combined with agents that interact with DNA topoisomerase I.

ExcerptRelevanceReference
"15-mg/m(2) dose level was not tolerable with repetitive dosing because of persistent thrombocytopenia."( Phase I and pharmacokinetic study of irofulven, a novel mushroom-derived cytotoxin, administered for five consecutive days every four weeks in patients with advanced solid malignancies.
Baker, SD; Britten, CD; Clark, GM; Drengler, R; Eckhardt, SG; Felton, S; Hammond, LA; Hidalgo, M; Kuhn, JG; MacDonald, JR; Moczygemba, J; Rowinsky, EK; Siu, L; Smith, C; Smith, SL; Villalona-Calero, MA; Von Hoff, DD; Weitman, S, 2000
)
0.58
" The preliminary antitumor activity documented in a patient with advanced pancreatic cancer and the striking preclinical antitumor effects of irofulven observed on intermittent dosing schedules support further disease-directed evaluations of this agent on the schedule evaluated in this study."( Phase I and pharmacokinetic study of irofulven, a novel mushroom-derived cytotoxin, administered for five consecutive days every four weeks in patients with advanced solid malignancies.
Baker, SD; Britten, CD; Clark, GM; Drengler, R; Eckhardt, SG; Felton, S; Hammond, LA; Hidalgo, M; Kuhn, JG; MacDonald, JR; Moczygemba, J; Rowinsky, EK; Siu, L; Smith, C; Smith, SL; Villalona-Calero, MA; Von Hoff, DD; Weitman, S, 2000
)
0.78
" However, the dose-response relationship was acute."( Relation between Irofulven (MGI-114) systemic exposure and tumor response in human solid tumor xenografts.
Billups, C; Cheshire, PJ; Fouladi, M; Friedman, HS; Houghton, PJ; Leggas, M; Peterson, JK; Stewart, CF; Woo, MH, 2002
)
0.65
"This study utilized MiaPaCa pancreatic xenografts to demonstrate irofulven antitumor activity using either a daily or intermittent dosing schedule."( Activity of irofulven against human pancreatic carcinoma cell lines in vitro and in vivo.
MacDonald, JR; Roth, S; Van Laar, ES; Waters, SJ; Weitman, S,
)
0.75
"Both dosing regimens of irofulven demonstrated curative activity against the MiaPaCa xenografts."( Activity of irofulven against human pancreatic carcinoma cell lines in vitro and in vivo.
MacDonald, JR; Roth, S; Van Laar, ES; Waters, SJ; Weitman, S,
)
0.82
"These results support further clinical characterization of intermittent irofulven dosing schedules and suggest that irofulven combined with gemcitabine may have activity in patients with pancreatic tumors."( Activity of irofulven against human pancreatic carcinoma cell lines in vitro and in vivo.
MacDonald, JR; Roth, S; Van Laar, ES; Waters, SJ; Weitman, S,
)
0.74
" The cytotoxic activity of irofulven is augmented when combined with agents that interact with DNA topoisomerase I; however, none of the reported studies have used the protracted dosing schedule found to be active clinically in treatment of childhood cancers."( Enhanced antitumor activity of irofulven in combination with irinotecan in pediatric solid tumor xenograft models.
Billups, C; Bjornsti, MA; Houghton, PJ; Liang, H; Peterson, JK; Woo, MH, 2005
)
0.91
" Only BILT significantly influenced the pharmacokinetics but this effect was not considered as relevant for dosing adjustment."( Pharmacokinetic modelling of 5-FU production from capecitabine--a population study in 40 adult patients with metastatic cancer.
Lokiec, F; RezaĆ­, K; Urien, S, 2005
)
0.33
" Dose-limiting toxicity (DLT) included dosing omission and delay > 1 week."( A phase I and pharmacokinetic study of irofulven and cisplatin administered in a 30-min infusion every two weeks to patients with advanced solid tumors.
Alexandre, J; Chieze, S; Cvitkovic, E; Faivre, S; Goldwasser, F; Hilgers, W; Kahatt, C; Lokiec, F; MacDonald, JR; Misset, JL; Raymond, E; Taamma, A; Weems, G, 2006
)
0.6
" Human cell lines, including colon cancer lines, were transfected with a vector containing rat PTGR1 or human PTGR1, and cell viability was examined after dosing with HMAF."( Up-regulation of human prostaglandin reductase 1 improves the efficacy of hydroxymethylacylfulvene, an antitumor chemotherapeutic agent.
Cervoni-Curet, FN; Erzinger, MM; Niederhuber, J; Pietsch, KE; Sturla, SJ; Whang, J; Yu, X, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
cyclohexenonesAny six-membered alicyclic ketone having one double bond in the ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin reductase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.05500.05500.07500.0950AID262580
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (75)

Assay IDTitleYearJournalArticle
AID1287558Cytotoxicity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287576Cytotoxicity against human TK10 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287557Cytotoxicity against human M14 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287540Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287556Cytotoxicity against human MALME-3M cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287537Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID355134Antitumor activity against human MV522 cells xenografted BALB/c nu/nu mouse assessed as increase in life span at 10 mg/kg, iv administered three times per week for 3 weeks1996Journal of natural products, Sep, Volume: 59, Issue:9
(Hydroxymethyl)acylfulvene: an illudin derivative with superior antitumor properties.
AID1287541Cytotoxicity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287583Cytotoxicity against human BT549 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1287564Cytotoxicity against human OVCAR3 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287569Cytotoxicity against human SKOV3 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287546Cytotoxicity against human HT-29 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287570Cytotoxicity against human 786-0 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287584Cytotoxicity against human T47D cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287534Cytotoxicity against human EKVX cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287573Cytotoxicity against human Caki1 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287572Cytotoxicity against human ACHN cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287538Cytotoxicity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID7788Concentration required for 50% toxicity in metastatic lung carcinoma (MV522) cells.2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
Preparation and biological activity of amino acid and peptide conjugates of antitumor hydroxymethylacylfulvene.
AID1287568Cytotoxicity against human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID387061Antiproliferative activity against human MCF7 cells at 1 to 10 uM after 24 to 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Conjugates of the fungal cytotoxin illudin M with improved tumour specificity.
AID1287579Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287565Cytotoxicity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287544Cytotoxicity against human HCT116 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287535Cytotoxicity against human HOP62 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287575Cytotoxicity against human SN12C cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287545Cytotoxicity against human HCT15 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID355133Antitumor activity against human MV522 cells xenografted BALB/c nu/nu mouse assessed as induction of tumor regression at 10 mg/kg, iv administered three times per week for 3 weeks1996Journal of natural products, Sep, Volume: 59, Issue:9
(Hydroxymethyl)acylfulvene: an illudin derivative with superior antitumor properties.
AID444001Cytotoxicity against human MV522 cells after 48 hrs by trypan blue exclusion assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Structure-activity studies of urea, carbamate, and sulfonamide derivatives of acylfulvene.
AID444003Selectivity index, ratio of IC50 for human 8392B cells to IC50 for human MV522 cells2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Structure-activity studies of urea, carbamate, and sulfonamide derivatives of acylfulvene.
AID262580Cytotoxicity against HEK293 cells transfected with recombinant AOR by MTT assay2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Investigating the role of stereochemistry in the activity of anticancer acylfulvenes: synthesis, reductase-mediated bioactivation, and cellular toxicity.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1287577Cytotoxicity against human UO31 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287563Cytotoxicity against human IGROV1 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287548Cytotoxicity against human SW620 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID262581Affinity towards rat NADP-dependent AOR, leukotriene B4 12-hydroxydehydrogenase2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Investigating the role of stereochemistry in the activity of anticancer acylfulvenes: synthesis, reductase-mediated bioactivation, and cellular toxicity.
AID398543Cytotoxicity against human HL60 cells after 48 hrs by trypan blue exclusion assay2003Journal of natural products, Feb, Volume: 66, Issue:2
Reaction of irofulven with zinc and acid.
AID1287571Cytotoxicity against human A498 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID387062Antiproliferative activity against human MDA-MB-231 cells at 1 to 10 uM after 24 to 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Conjugates of the fungal cytotoxin illudin M with improved tumour specificity.
AID1287550Cytotoxicity against human SF295 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID355132Cytotoxicity against human HL60 cells after 48 hrs by trypan blue exclusion method1996Journal of natural products, Sep, Volume: 59, Issue:9
(Hydroxymethyl)acylfulvene: an illudin derivative with superior antitumor properties.
AID1287567Cytotoxicity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287578Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287543Cytotoxicity against human HCC2998 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287554Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID444002Cytotoxicity against human 8392B cells after 48 hrs by trypan blue exclusion assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Structure-activity studies of urea, carbamate, and sulfonamide derivatives of acylfulvene.
AID1287555Cytotoxicity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287581Cytotoxicity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287547Cytotoxicity against human KM12 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID303821Antitumor activity in MV522 cells assessed as inhibition of DNA synthesis after 2 hrs2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antitumor activity of amine analogs of irofulven.
AID1287539Cytotoxicity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287560Cytotoxicity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287536Cytotoxicity against human HOP92 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287588Antitumor activity against human MV522 cells xenografted in Balb/c nu/nu mouse assessed as inhibition of tumor growth at 10 mg/kg, ip administered thrice a week for 3 weeks2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287580Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287582Cytotoxicity against human Hs 578T cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287586Cytotoxicity against human CHRF-288-11 cells after 48 hrs by trypan blue exclusion assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287551Cytotoxicity against human SF539 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287587Selectivity index, ratio of IC50 for human CHRF-288-11 cells to IC50 for human MV522 cells2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287533Cytotoxicity against human A549 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287553Cytotoxicity against human SNB75 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287585Cytotoxicity against human MV522 cells after 48 hrs by trypan blue exclusion assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID262579Cytotoxicity against HEK293 cells by MTT assay2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Investigating the role of stereochemistry in the activity of anticancer acylfulvenes: synthesis, reductase-mediated bioactivation, and cellular toxicity.
AID1287574Cytotoxicity against human RXF393 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287559Cytotoxicity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287552Cytotoxicity against human SNB19 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID303822Antitumor activity in MV522 cells assessed as cell survival after 48 hrs2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antitumor activity of amine analogs of irofulven.
AID1287562Cytotoxicity against human UACC257 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287566Cytotoxicity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287542Cytotoxicity against human COLO205 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID1287561Cytotoxicity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1287549Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Hydroxyurea derivatives of irofulven with improved antitumor efficacy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (93)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's13 (13.98)18.2507
2000's71 (76.34)29.6817
2010's6 (6.45)24.3611
2020's3 (3.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.81

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

MetricThis Compound (vs All)
Research Demand Index25.81 (24.57)
Research Supply Index4.80 (2.92)
Research Growth Index4.82 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (22.22%)5.53%
Reviews5 (5.05%)6.00%
Case Studies2 (2.02%)4.05%
Observational0 (0.00%)0.25%
Other70 (70.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (20)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase II Study of Irofulven in AR-targeted and Docetaxel-Pretreated Metastatic Castration-Resistant Prostate Cancer Patients, Who Have a Drug Response Predictor (DRPĀ®) Indicating a High Likelihood of Response to Irofulven. [NCT03643107]Phase 227 participants (Anticipated)Interventional2018-10-17Active, not recruiting
Phase I-II Clinical and Pharmacokinetic Study of Irofulven in Combination With Oxaliplatin in Patients With Advanced Solid Tumors [NCT00374660]Phase 1/Phase 263 participants (Actual)Interventional2003-06-30Completed
A Phase II Evaluation Of Irofulven (IND #55804, NSC #683863) In The Treatment Of Recurrent Or Persistent Platinium-Sensitive Ovarian Or Primary Peritoneal Cancer [NCT00053365]Phase 261 participants (Actual)Interventional2003-06-30Completed
A Multicenter Phase II Trial of MGI-114 in Patients With Stage IV Malignant Melanoma [NCT00005968]Phase 20 participants Interventional1999-11-30Completed
A Phase II Trial of MGI-114 (NSC# 683863) Administered as a 5-Minute Infusion Daily for Five Days Every 4 Weeks in Patients With Previously Untreated Advanced Colorectal Cancer [NCT00003786]Phase 20 participants (Actual)Interventional1999-04-30Withdrawn(stopped due to NO participants)
A Phase II Trial of MGI 114 in Patients With Advanced Pancreatic Adenocarcinoma [NCT00003760]Phase 23 participants (Actual)Interventional1998-11-30Completed
A Phase II Trial of 6-Hydroxymethylacylfulvene (MGI-114) in Patients With Advanced Renal Cell Carcinoma [NCT00003390]Phase 20 participants Interventional1998-06-30Completed
Phase II Trial of 6-Hydroxymethylacylfulvene (HMAF; MGI-114) in Patients With Relapsed or Refractory Non-Small Cell Lung Cancer [NCT00003666]Phase 236 participants (Actual)Interventional1998-11-30Completed
A Phase II Trial of 6-Hydroxymethylacylfulvene (HMAF; MGI-114) in Patients With Advanced Cervical Carcinoma [NCT00005070]Phase 20 participants Interventional2000-01-31Completed
Three-Arm Randomized Phase II Clinical Study of Irofulven/Prednisone, Irofulven/Capecitabine/Prednisone or Mitoxantrone/Prednisone in Docetaxel-Pretreated Hormone-Refractory Prostate Cancer Patients [NCT00124566]Phase 2135 participants (Actual)Interventional2004-06-30Completed
A Phase II Evaluation of MGI-114 in the Treatment of Recurrent or Persistent Endometrial Carcinoma [NCT00005031]Phase 20 participants Interventional2000-08-31Completed
Phase 2 Clinical Trial of Bi-weekly Dosing of Irofulven Plus Capecitabine in Patients With Anaplastic or Locally Advanced/Metastatic Differentiated Thyroid Cancer [NCT00124527]Phase 235 participants Interventional2005-03-31Completed
A Phase II Study of MGI-114 in Patients With Recurrent or Persistent Epithelial Ovarian Cancer [NCT00019552]Phase 20 participants Interventional1998-09-30Completed
A Phase II Study of Irofulven as First Line Therapy in Recurrent or Metastatic Gastric Cancer [NCT00062257]Phase 20 participants Interventional2003-06-30Completed
A Phase I/II Trial Of MGI114 For Treatment Of Patients With Recurrent Malignant Gliomas [NCT00012038]Phase 1/Phase 20 participants Interventional2001-07-31Completed
Phase III Trial Of Irofulven Vs. 5-Fluorouracil In Patients With Gemcitabine-Refractory Advanced Pancreatic Adenocarcinoma [NCT00033735]Phase 3158 participants (Actual)Interventional2000-01-31Completed
A Trial of MGI 114 in Children With Solid Tumors: A Pediatric Oncology Group Phase I Cooperative Agreement Study [NCT00003370]Phase 112 participants (Actual)Interventional1998-08-31Completed
Phase II Study of MGI-114 in Patients With Metastatic Breast Cancer [NCT00003796]Phase 232 participants (Actual)Interventional1999-05-31Completed
Phase I Study of MGI-114 (NSC#683863) in Patients With Refractory Myelodysplastic Syndromes, Acute Leukemia and Chronic Myelogenous Leukemia in Blastic Phase (CML-BP) [NCT00003997]Phase 125 participants (Actual)Interventional1999-07-31Completed
Phase II Study of MGI-114 (NSC# 683863) Administered Intravenously for Five Days Every 28 Days to Patients With Metastatic Colorectal Cancer [NCT00003441]Phase 226 participants (Actual)Interventional1998-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00053365 (3) [back to overview]Frequency and Severity of Observed Adverse Events, Grade 3 or Higher According to the National Cancer Institute Common Toxicity Criteria (NCI CTC) v2.0
NCT00053365 (3) [back to overview]Progression-free Survival
NCT00053365 (3) [back to overview]Tumor Response

Frequency and Severity of Observed Adverse Events, Grade 3 or Higher According to the National Cancer Institute Common Toxicity Criteria (NCI CTC) v2.0

(NCT00053365)
Timeframe: Assessed every cycle while on treatment, 30 days after the last cycle of treatment

,
Interventionparticipants (Number)
LeukopeniaThrombocytopeniaNeutropeniaOther hematologicConstitutionalGastrointestinalInfectionMusculoskeletalMetabolicNeuropathy (sensory)Other neurologicOcularPain
Grade 3 (CTCAE v 2.0)1111166484221241
Grade 4 (CTCAE v 2.0)0260010010000

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Progression-free Survival

Per Gynecologic Oncology Group(GOG) Response Evaluation Criteria in Solid Tumors(RECIST) Criteria, progression is defined as at least a 20% increase in the sum of longest dimesions(LD) of target lesions taking as reference the smallest sum LD or the appearance of new lesions within 8 weeks of study entry. (NCT00053365)
Timeframe: From entry into study to death or date of last contact, assessed up to 5 years

Interventionmonths (Median)
Median Overall SurvivalMedian Progression-free Survival
Treatment (Irofulven)24.16.7

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Tumor Response

"Per Gynecologic Oncology Group(GOG) Response Evaluation Criteria in Solid Tumors(RECIST) Criteria: Complete Response is disappearance of all target and non-target lesions; Partial Response is at least a 30% decrease in the sum of longest dimensions (LD) of all target measurable dimensions; Increasing Disease is at least a 20% increase in the sum of LD of target lesions taking as reference the smallest sum LD or the appearance of new lesions within 8 weeks of study entry.~Response is to be evaluated every 42 days for the first 6 months and every 6 months thereafter while the patient is receiving study treatment, then every 3 months for 2 years and every 6 months for the next 3 years until documented progression or death." (NCT00053365)
Timeframe: From entry into study until documented progression or death, assessed up to 5 years.

Interventionparticipants (Number)
Partial ResponseStable DiseaseIncrease DiseaseIndeterminate
Treatment (Irofulven)730126

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