Page last updated: 2024-11-13

oblimersen

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Description

oblimersen: targets the Bcl-2 oncogene good efficacy with low toxicity tumour regressions [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID118984457
MeSH IDM0362850

Synonyms (12)

Synonym
190977-41-4
genasense
g 3139
augmerosen
oblimersen sodium [usan]
dna, d(p-thio)(t-c-t-c-c-c-a-g-c-g-t-g-c-g-c-c-a-t)
oblimersen sodium
g3139
oblimersen
unii-85j5zp6ysl
85j5zp6ysl ,
d-g3139

Research Excerpts

Overview

Oblimersen (G3139) is a phosphorothioate 18-mer antisense oligonucleotide directed against the first 6 BCL2 codons. It can decrease transcription of Bcl-2 protein and increase myeloma cell susceptibility to cytotoxic agents.

ExcerptReferenceRelevance
"Oblimersen (G3139) is a phosphorothioate 18-mer antisense oligonucleotide directed against the first 6 BCL2 codons."( Phase 3 randomized trial of chemotherapy with or without oblimersen in older AML patients: CALGB 10201 (Alliance).
Bloomfield, CD; Blum, W; Byrd, JC; Carroll, AJ; Eisfeld, AK; Jacobson, S; Kohlschmidt, J; Kolitz, JE; Larson, RA; Marcucci, G; Mrózek, K; Stock, W; Stone, RM; Stuart, RK; Sutamtewagul, G; Thakuri, M; Vij, R; Walker, AR; Wang, ES; Yin, J, 2021
)
1.59
"Oblimersen sodium is a bcl-2 antisense oligonucleotide complementary to the first six codons of the open-reading frame of bcl-2 mRNA that can decrease transcription of Bcl-2 protein and increase myeloma cell susceptibility to cytotoxic agents."( Phase III randomised study of dexamethasone with or without oblimersen sodium for patients with advanced multiple myeloma.
Callander, N; Chanan-Khan, AA; Christiansen, NP; Hohl, RJ; Jagannath, S; Lister, J; Niesvizky, R; Oken, M; Schiller, GJ; Zimmerman, TM, 2009
)
1.32
"Oblimersen sodium is an antisense oligonucleotide compound designed to specifically bind to human bcl-2 mRNA, resulting in catalytic degradation of bcl-2 mRNA and subsequent decrease in bcl-2 protein translation."( Oblimersen sodium (Genasense bcl-2 antisense oligonucleotide): a rational therapeutic to enhance apoptosis in therapy of lung cancer.
Frankel, SR; Herbst, RS, 2004
)
2.49
"Oblimersen is a phosphorothioate antisense oligonucleotide complimentary to the Bcl-2 mRNA and a potent inhibitor of Bcl-2 expression which in pre-clinical testing can significantly enhance the therapeutic effect of chemotherapy, hormone and radiation therapy."( Targeting Bcl-2 with oblimersen for patients with hormone refractory prostate cancer.
Chi, KN, 2005
)
1.37
"Oblimersen sodium is an antisense oligonucleotide to the first 6 codons of the B-cell leukemia gene 2 (bcl-2) open reading frame. "( Early results of a phase I trial of oblimersen sodium for relapsed or refractory Waldenstrom's macroglobulinemia.
Badros, A; Erlichman, C; Gertz, MA; Geyer, SM; Kahl, BS, 2005
)
2.05
"Oblimersen is an 18-base oligodeoxynucleotide encoding antisense to the gene for bcl-2, an anti-apoptotic protein that is upregulated in renal and other cancers. "( Oblimersen and alpha-interferon in metastatic renal cancer: a phase II study of the California Cancer Consortium.
Baratta, T; Diamond, DJ; Dutcher, JP; Frankel, P; Gandara, DR; Lacey, SF; Lara, P; Margolin, K; Quinn, DI; Synold, TW; Xi, B, 2007
)
3.23
"Oblimersen (Genasense is a Bcl-2 antisense compound that selectively targets Bcl-2 RNA for degradation by RNase H and thereby decreases Bcl-2 protein production. "( Oblimersen in the treatment of metastatic melanoma.
Kirkwood, JM; Tarhini, AA, 2007
)
3.23
"Oblimersen is an antisense oligonucleotide developed by Genta for systemic use as an injection. "( Oblimersen: Augmerosen, BCL-2 antisense oligonucleotide - Genta, G 3139, GC 3139, oblimersen sodium.
, 2007
)
3.23
"Oblimersen is a 18-mer phosphorothioate antisense oligonucleotide designed to bind to the first six codons of the human bcl-2 mRNA."( Bcl-2-targeted antisense therapy (Oblimersen sodium): towards clinical reality.
Moreira, JN; Santos, A; Simões, S, 2006
)
1.33

Actions

Oblimersen was shown to increase in vitro and in vivo effect of RT on SCLC cell lines. It should also enhance the cytotoxic effect of chemotherapy in WM.

ExcerptReferenceRelevance
"Oblimersen was shown to increase in vitro and in vivo effect of RT on SCLC cell lines. "( Inhibition of BCL-2 in small cell lung cancer cell lines with oblimersen, an antisense BCL-2 oligodeoxynucleotide (ODN): in vitro and in vivo enhancement of radiation response.
Bourhis, J; Brown, BD; Deutsch, E; Loriot, Y; Mordant, P; Soria, JC, 2010
)
2.04
"Oblimersen should also enhance the cytotoxic effect of chemotherapy in WM."( Early results of a phase I trial of oblimersen sodium for relapsed or refractory Waldenstrom's macroglobulinemia.
Badros, A; Erlichman, C; Gertz, MA; Geyer, SM; Kahl, BS, 2005
)
1.32

Treatment

ExcerptReferenceRelevance
"Pretreatment with oblimersen followed by cyclophosphamide (Cytoxan, Neosar) markedly improved survival relative to single-agent cyclophosphamide in a murine xenograft model."( Targeting the proapoptotic factor Bcl-2 in non-Hodgkin's lymphoma.
Klasa, RJ, 2004
)
0.65

Pharmacokinetics

To assess the feasibility of administering oblimersen sodium, a phosphorothioate antisense oligonucleotide directed to the Bcl-2 mRNA, combined with irinotecan in patients with advanced colorectal carcinoma. Plasma was sampled to characterize the pharmacokinetic parameters of both Oblimersen and docetaxel. B Cl-2 protein expression was measured from paired collections of PBMCs pretreatment and post-treatment.

ExcerptReferenceRelevance
"To evaluate the pharmacokinetic (PK) properties of Bcl-2 antisense oligodeoxynucleotide G3139 when combined with the anthracycline anticancer drug doxorubicin (DOX) in a model of MDA435/LCC6 human breast cancer in severely compromised immunodeficient (SCID) mice."( Pharmacokinetics of Bcl-2 antisense oligonucleotide (G3139) combined with doxorubicin in SCID mice bearing human breast cancer solid tumor xenografts.
Lopes de Menezes, DE; Mayer, LD, 2002
)
0.31
" at 5 mg/kg revealed a biexponential plasma concentration-time curve with a Cmax of 99."( Pharmacokinetics of Bcl-2 antisense oligonucleotide (G3139) combined with doxorubicin in SCID mice bearing human breast cancer solid tumor xenografts.
Lopes de Menezes, DE; Mayer, LD, 2002
)
0.31
"To assess the feasibility of administering oblimersen sodium, a phosphorothioate antisense oligonucleotide directed to the Bcl-2 mRNA, with docetaxel to patients with hormone-refractory prostate cancer; to characterize the pertinent pharmacokinetic parameters, Bcl-2 protein inhibition in peripheral blood mononuclear cell(s) (PBMC) and tumor; and to seek preliminary evidence of antitumor activity."( A Phase I pharmacokinetic and biological correlative study of oblimersen sodium (genasense, g3139), an antisense oligonucleotide to the bcl-2 mRNA, and of docetaxel in patients with hormone-refractory prostate cancer.
Bushnell, D; Fingert, H; Hammond, LA; Izbicka, E; Kreisberg, J; Kuhn, J; Malik, S; Patnaik, A; Rowinsky, EK; Schwartz, G; Smetzer, L; Thompson, I; Tolcher, AW, 2004
)
0.83
" Plasma was sampled to characterize the pharmacokinetic parameters of both oblimersen and docetaxel, and Bcl-2 protein expression was measured from paired collections of PBMCs pretreatment and post-treatment."( A Phase I pharmacokinetic and biological correlative study of oblimersen sodium (genasense, g3139), an antisense oligonucleotide to the bcl-2 mRNA, and of docetaxel in patients with hormone-refractory prostate cancer.
Bushnell, D; Fingert, H; Hammond, LA; Izbicka, E; Kreisberg, J; Kuhn, J; Malik, S; Patnaik, A; Rowinsky, EK; Schwartz, G; Smetzer, L; Thompson, I; Tolcher, AW, 2004
)
0.79
"To determine the antitumor activity and safety of oblimersen sodium, a phosphorothioate antisense oligonucleotide directed to the bcl-2 mRNA, with docetaxel in patients with hormone-refractory prostate cancer (HRPC) and to determine if relevant pharmacokinetic and pharmacodynamic variables of oblimersen or docetaxel influence response to this therapy."( A phase II, pharmacokinetic, and biological correlative study of oblimersen sodium and docetaxel in patients with hormone-refractory prostate cancer.
Berg, K; Chi, K; D'Aloisio, S; Frankel, SR; Gleave, M; Izbicka, E; Kuhn, J; Murray, N; Patnaik, A; Rowinsky, E; Schwartz, G; Takimoto, C; Thompson, I; Tolcher, AW, 2005
)
0.82
" Plasma samples were analyzed to characterize the pharmacokinetic variables of both oblimersen and docetaxel, and paired collections of peripheral blood mononuclear cells were collected to determine Bcl-2 protein expression pretreatment and post-treatment."( A phase II, pharmacokinetic, and biological correlative study of oblimersen sodium and docetaxel in patients with hormone-refractory prostate cancer.
Berg, K; Chi, K; D'Aloisio, S; Frankel, SR; Gleave, M; Izbicka, E; Kuhn, J; Murray, N; Patnaik, A; Rowinsky, E; Schwartz, G; Takimoto, C; Thompson, I; Tolcher, AW, 2005
)
0.79
"To assess the feasibility and antitumor activity of oblimersen sodium, an antisense oligonucleotide directed to the Bcl-2 mRNA, combined with irinotecan in patients with advanced colorectal carcinoma, characterize the pharmacokinetic behavior of both oblimersen sodium and irinotecan, and examine Bcl-2 protein inhibition in peripheral blood mononuclear cells (PBMC)."( A phase I, pharmacokinetic and biologic correlative study of oblimersen sodium (Genasense, G3139) and irinotecan in patients with metastatic colorectal cancer.
Berg, K; Hammond, LA; Izbicka, E; Kuhn, J; Mita, MM; Ochoa, L; Patnaik, A; Rowinsky, EK; Schwartz, G; Tolcher, AW; Yeh, IT, 2006
)
0.83
" In striking contrast, PEGylation of 1 resulted in dramatically improved pharmacokinetic profiles in vivo, with a prolonged half-life (t1/2), increased plasma concentration, and increased area under the plasma concentration-time curve (AUC)."( Delivery of G3139 using releasable PEG-linkers: impact on pharmacokinetic profile and anti-tumor efficacy.
Benimetskaya, L; Borchard, G; Borowski, V; Lipman, J; Longley, C; Mehlig, M; Peng, P; Reddy, P; Stein, CA; Xia, J; Zhang, Y; Zhao, H, 2007
)
0.34
" The pharmacokinetic interactions between G3139 and carboplatin/paclitaxel were measured."( A phase I pharmacokinetic and pharmacodynamic correlative study of the antisense Bcl-2 oligonucleotide g3139, in combination with carboplatin and paclitaxel, in patients with advanced solid tumors.
Alberti, D; Eickhoff, J; Kolesar, J; Lee, F; Leith, C; Liu, G; Marnocha, R; McNeel, DG; Schell, K; Traynor, A; Wilding, G; Zwiebel, J, 2008
)
0.35
" The half-life of G3139 and its metabolites was observed at 31 and 68 h, respectively."( Evaluation of Pharmacokinetics and Metabolism of Phosphorothioate Antisense Oligonucleotide G3139 in Rat by Capillary Electrophoresis with Laser-Induced Fluorescence.
Ban, E; Kwon, H; Song, EJ, 2021
)
0.62

Compound-Compound Interactions

Oblimersen is an antisense oligonucleotide directed to the Bcl-2 mRNA. In combination with cisplatin and 5-flourouracil in patients with advanced gastric and esophageal carcinoma. Most severe toxicity was neutropenia.

ExcerptReferenceRelevance
" This study investigated the activity of the Bcl-2 antisense oligodeoxynucleotide (AS ODN) G3139 combined with free doxorubicin (F-DOX) or sterically stabilized liposomal doxorubicin (SL-DOX) to determine the role that drug pharmacodistribution properties may have on antitumor activity using a Bcl-2-expressing human breast solid tumor xenograft model."( Molecular and pharmacokinetic properties associated with the therapeutics of bcl-2 antisense oligonucleotide G3139 combined with free and liposomal doxorubicin.
Hudon, N; Lopes de Menezes, DE; Mayer, LD; McIntosh, N, 2000
)
0.31
"To evaluate the pharmacokinetic (PK) properties of Bcl-2 antisense oligodeoxynucleotide G3139 when combined with the anthracycline anticancer drug doxorubicin (DOX) in a model of MDA435/LCC6 human breast cancer in severely compromised immunodeficient (SCID) mice."( Pharmacokinetics of Bcl-2 antisense oligonucleotide (G3139) combined with doxorubicin in SCID mice bearing human breast cancer solid tumor xenografts.
Lopes de Menezes, DE; Mayer, LD, 2002
)
0.31
"These findings indicate that drug-drug interactions between G3139 and DOX are modest and favorable in that elevated tumor DOX levels are achieved without compromising G3139 tumor uptake or significantly altering plasma drug concentrations."( Pharmacokinetics of Bcl-2 antisense oligonucleotide (G3139) combined with doxorubicin in SCID mice bearing human breast cancer solid tumor xenografts.
Lopes de Menezes, DE; Mayer, LD, 2002
)
0.31
" The objective of this work was to investigate the antitumor efficacy of the Bcl-2 antisense oligonucleotide oblimersen (Genasense; G3139), alone and in combination with vinorelbine (VNB), in an ectopic and orthotopic xenograft model of NCI-H460 human non-small-cell lung cancer."( Antitumor efficacy of oblimersen Bcl-2 antisense oligonucleotide alone and in combination with vinorelbine in xenograft models of human non-small cell lung cancer.
Bally, MB; Bebb, G; Hu, Y; Mayer, LD; Ng, R; Sartor, JR; Tan, S; Yan, H, 2004
)
0.85
" Results showed a reduced sensitivity of melanoma cells to gimatecan following Bcl-2 transfection and inversely, increased cell sensitivity to gimatecan in combination with oblimersen."( Enhanced antitumour efficacy of gimatecan in combination with Bcl-2 antisense oligonucleotide in human melanoma xenografts.
Balsari, A; Carenini, N; De Cesare, M; Del Bufalo, D; Perego, P; Pratesi, G; Righetti, SC; Rivoltini, L; Zunino, F; Zupi, G, 2005
)
0.52
" In contrast, G3139 treatment (25 mg/kg every 3 days x 5 starting on day 7) in combination with CDDP (8 mg/kg on day 14) completely abrogated tumor engraftment in 80% of animals compared to CDDP (0%) or CDDP + control oligo (0%)."( Systemic Bcl-2 antisense oligodeoxynucleotide in combination with cisplatin cures EBV+ nasopharyngeal carcinoma xenografts in SCID mice.
Carbone, R; Cheng, YC; Grill, S; Lacy, J; Loomis, R; Srimatkandada, P, 2006
)
0.33
" We evaluated the efficacy and safety of oblimersen combined with GO in patients > or =60 years of age in first relapse with CD33+ acute myeloid leukemia."( A Phase II study of Bcl-2 antisense (oblimersen sodium) combined with gemtuzumab ozogamicin in older patients with acute myeloid leukemia in first relapse.
Giles, F; Kalaycio, M; Kolitz, J; Marcucci, G; Moore, J; Seiter, K; Stock, W; Zenk, D, 2006
)
0.87
"To determine the maximum-tolerated dose, toxicity, pharmacokinetics, and biologic effects of G3139 when administered with doxorubicin and cyclophosphamide to children with relapsed solid tumors."( Phase I Trial of G3139, a bcl-2 antisense oligonucleotide, combined with doxorubicin and cyclophosphamide in children with relapsed solid tumors: a Children's Oncology Group Study.
Adamson, PC; Blaney, SM; Chandula, R; Hogarty, MD; Krailo, MD; Rheingold, SR; Sauk-Schubert, C; Zwiebel, JA, 2007
)
0.34
"This phase I trial assessed the safety and tolerability of G3139 when given in combination with carboplatin and paclitaxel chemotherapy."( A phase I pharmacokinetic and pharmacodynamic correlative study of the antisense Bcl-2 oligonucleotide g3139, in combination with carboplatin and paclitaxel, in patients with advanced solid tumors.
Alberti, D; Eickhoff, J; Kolesar, J; Lee, F; Leith, C; Liu, G; Marnocha, R; McNeel, DG; Schell, K; Traynor, A; Wilding, G; Zwiebel, J, 2008
)
0.35
" This multicentric phase I study was carried out to evaluate maximum tolerated dose (MTD), safety and preliminary efficacy of oblimersen in combination with docetaxel, adriamycin and cyclophosphamide as neo-adjuvant systemic treatment (NST) in primary breast cancer (PBC)."( Oblimersen combined with docetaxel, adriamycin and cyclophosphamide as neo-adjuvant systemic treatment in primary breast cancer: final results of a multicentric phase I study.
Eichbaum, M; Eiermann, W; Kaufmann, M; Marmé, F; Rom, J; Scharf, A; Schlehe, B; Schneeweiss, A; Schuetz, F; Sievert, M; Sinn, HP; Sohn, C; von Minckwitz, G, 2008
)
1.99
"Previously untreated patients with PBC T2-4a-c N0-3 M0 received one cycle of docetaxel 75 mg/m(2), adriamycin 50 mg/m(2) and cyclophosphamide 500 mg/m(2) administered on day 5 combined with escalating doses of oblimersen as a 24-h continuous infusion on days 1-7 followed by five cycles of combination of docetaxel, adriamycin and cyclophosphamide (TAC) without oblimersen every 3 weeks."( Oblimersen combined with docetaxel, adriamycin and cyclophosphamide as neo-adjuvant systemic treatment in primary breast cancer: final results of a multicentric phase I study.
Eichbaum, M; Eiermann, W; Kaufmann, M; Marmé, F; Rom, J; Scharf, A; Schlehe, B; Schneeweiss, A; Schuetz, F; Sievert, M; Sinn, HP; Sohn, C; von Minckwitz, G, 2008
)
1.98
" Following oblimersen combined with TAC, the most severe toxicity was neutropenia [National Cancer Institute-Common Toxicity Criteria (NCI-CTC) grades 1-2/3/4] which developed in 0/0/56% of patients (cohort I), 11/0/56% of patients (cohort II) and 20/20/50% of patients (cohort III)."( Oblimersen combined with docetaxel, adriamycin and cyclophosphamide as neo-adjuvant systemic treatment in primary breast cancer: final results of a multicentric phase I study.
Eichbaum, M; Eiermann, W; Kaufmann, M; Marmé, F; Rom, J; Scharf, A; Schlehe, B; Schneeweiss, A; Schuetz, F; Sievert, M; Sinn, HP; Sohn, C; von Minckwitz, G, 2008
)
2.18
"Oblimersen up to a dose of 7 mg/kg/day administered as a 24-h infusion on days 1-7 can be safely administered in combination with standard TAC on day 5 as NST in patients with PBC."( Oblimersen combined with docetaxel, adriamycin and cyclophosphamide as neo-adjuvant systemic treatment in primary breast cancer: final results of a multicentric phase I study.
Eichbaum, M; Eiermann, W; Kaufmann, M; Marmé, F; Rom, J; Scharf, A; Schlehe, B; Schneeweiss, A; Schuetz, F; Sievert, M; Sinn, HP; Sohn, C; von Minckwitz, G, 2008
)
3.23
" In conclusion, oblimersen sodium can be safely combined with rituximab."( Phase II multicenter study of oblimersen sodium, a Bcl-2 antisense oligonucleotide, in combination with rituximab in patients with recurrent B-cell non-Hodgkin lymphoma.
Fayad, L; Hagemeister, F; Kwak, L; Leber, B; Lopez, A; McLaughlin, P; Pro, B; Rodriguez, A; Romaguera, J; Samaniego, F; Smith, M; Younes, A; Zwiebel, J, 2008
)
0.98
"Preclinical data showed enhancement of breast cancer cell death when G3139 was combined with anthracyclines and taxanes."( Phase I/II study of G3139 (Bcl-2 antisense oligonucleotide) in combination with doxorubicin and docetaxel in breast cancer.
Booser, DJ; Brewster, AM; Buchholz, TA; Cristofanilli, M; Esteva, FJ; Hortobagyi, GN; Hunt, KK; Lipsanen, C; Madden, TL; Moulder, SL; Symmans, WF; Valero, V; Yuan, L; Zwiebel, J, 2008
)
0.35
" for 5 days) in combination with AT."( Phase I/II study of G3139 (Bcl-2 antisense oligonucleotide) in combination with doxorubicin and docetaxel in breast cancer.
Booser, DJ; Brewster, AM; Buchholz, TA; Cristofanilli, M; Esteva, FJ; Hortobagyi, GN; Hunt, KK; Lipsanen, C; Madden, TL; Moulder, SL; Symmans, WF; Valero, V; Yuan, L; Zwiebel, J, 2008
)
0.35
"G3139 in combination with doxorubicin and docetaxel is well tolerated."( Phase I/II study of G3139 (Bcl-2 antisense oligonucleotide) in combination with doxorubicin and docetaxel in breast cancer.
Booser, DJ; Brewster, AM; Buchholz, TA; Cristofanilli, M; Esteva, FJ; Hortobagyi, GN; Hunt, KK; Lipsanen, C; Madden, TL; Moulder, SL; Symmans, WF; Valero, V; Yuan, L; Zwiebel, J, 2008
)
0.35
"To determine the maximum tolerated dose of oblimersen, an antisense oligonucleotide directed to the Bcl-2 mRNA, in combination with cisplatin and 5-flourouracil in patients with advanced gastric and esophageal carcinoma."( A phase I trial of oblimersen sodium in combination with cisplatin and 5-fluorouracil in patients with advanced esophageal, gastroesophageal junction, and gastric carcinoma.
Christos, P; Kaubisch, A; Ocean, AJ; Raab, R; Ramirez, M; Sparano, JA; Vinciguerra, V, 2010
)
0.95
"Fifteen patients received a total of 49 courses of oblimersen at doses of 3, 5, or 7 mg/kg/d given as a 7 day CIVI in combination with 4 or 5 day CIVI of 5-FU (1000 or 750 mg/m2/d) plus intravenous cisplatin (100 or 75 mg/m2 over 2 hours)."( A phase I trial of oblimersen sodium in combination with cisplatin and 5-fluorouracil in patients with advanced esophageal, gastroesophageal junction, and gastric carcinoma.
Christos, P; Kaubisch, A; Ocean, AJ; Raab, R; Ramirez, M; Sparano, JA; Vinciguerra, V, 2010
)
0.94

Dosage Studied

ExcerptRelevanceReference
" Dose-limiting reactions in phase I included hypotension and fever, and the MTD for phase II dosing was established at 3 mg/kg/d."( Phase I to II multicenter study of oblimersen sodium, a Bcl-2 antisense oligonucleotide, in patients with advanced chronic lymphocytic leukemia.
Cunningham, CC; Golenkov, AK; Novick, SC; O'Brien, SM; Rai, KR; Turkina, AG, 2005
)
0.61
"To investigate whether irradiation before antisense Bcl-2 oligodeoxynucleotide (ODN) administration enhances tissue uptake, and whether periodic dosing enhances cellular uptake of fluorescently labeled ODN relative to constant dosing."( Irradiation of human prostate cancer cells increases uptake of antisense oligodeoxynucleotide.
Anai, S; Brown, BD; Goodison, S; Hirao, Y; Nakamura, K; Rosser, CJ, 2007
)
0.34
" In addition, PC-3-Bcl-2 subcutaneous xenograft tumors were treated with or without irradiation in combination with various dosing schemas of G4243."( Irradiation of human prostate cancer cells increases uptake of antisense oligodeoxynucleotide.
Anai, S; Brown, BD; Goodison, S; Hirao, Y; Nakamura, K; Rosser, CJ, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (186)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (1.08)18.2507
2000's152 (81.72)29.6817
2010's25 (13.44)24.3611
2020's7 (3.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.67

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 Index30.67 (24.57)
Research Supply Index5.46 (2.92)
Research Growth Index6.50 (4.65)
Search Engine Demand Index35.70 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.67)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials40 (20.51%)5.53%
Reviews54 (27.69%)6.00%
Case Studies1 (0.51%)4.05%
Observational0 (0.00%)0.25%
Other100 (51.28%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (45)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase II Study of G3139 (Bcl-2 Antisense) And Rituximab in Patients With Recurrent B-cell Non-Hodgkinâs Lymphomas [NCT00054639]Phase 248 participants (Actual)Interventional2003-01-31Completed
A Phase I/II Study of Oblimersen in Combination With Cisplatin and Fluorouracil in Patients With Advanced Esophageal, Gastro-Esophageal Junction and Gastric Cancer [NCT00064259]Phase 1/Phase 215 participants (Actual)Interventional2003-06-30Terminated(stopped due to Discontinued development of G3139 (oblimersen))
Investigator Initiated Pilot Study of Microarray Directed Therapy for Diffuse Large B-cell Lymphoma Using Genasense With CHOP-R [NCT00736450]Early Phase 137 participants (Actual)Interventional2008-07-23Terminated(stopped due to Manufacturer is no longer making the drug.)
A Phase IIA Study to Determine the Safety and Efficacy of A NCI-Supplied Agent: G3139 (NSC 683428, IND 58842) and Imatinib Mesylate in Patients With Refractory or Relapsed Gastrointestinal Stromal Tumor [NCT00091078]Phase 296 participants (Actual)Interventional2005-09-30Terminated
A Randomized Phase 3 Study of Fludarabine and Rituximab With or Without Genasense® (Oblimersen Sodium) in Previously Untreated Subjects With Chronic Lymphocytic Leukemia [NCT00517218]Phase 30 participants Interventional2006-06-30Withdrawn
A Phase II Study of G3139 (Genasense ™) in Patients With Merkel Cell Carcinoma [NCT00079131]Phase 237 participants (Actual)Interventional2004-01-31Completed
A Phase I Study Of Genasense, A Bcl-2 Antisense Oligonucleotide, Combined With Carboplatin And Etoposide In Patients With Small Cell Lung Cancer [NCT00017251]Phase 112 participants (Actual)Interventional2001-04-30Completed
Randomized Phase III Study of Dexamethasone With or Without Genasense (Bcl-2 Antisense Oligonucleotide) in Patients With Relapsed or Refractory Multiple Myeloma [NCT00017602]Phase 30 participants Interventional2000-12-31Completed
"A Pilot Study of Abraxane® (Albumin-bound Paclitaxel) and Temodar® (Temozolomide) Plus Genasense® (Oblimersen Sodium) in Subjects With Advanced Melanoma (The ATG Study)." [NCT00409383]Phase 128 participants (Anticipated)Interventional2006-11-30Active, not recruiting
A Randomized, Open-label, Cross-over Pharmacokinetic Study of Dacarbazine in Combination With Genasense® in Subjects With Advanced Melanoma [NCT00542893]Phase 10 participants Interventional2006-04-30Completed
A Pharmacokinetic Study of Genasense® (Bcl-2 Antisense Oligonucleotide) in Combination With Dacarbazine (DTIC) in Subjects With Advanced Melanoma and Normal or Impaired Hepatic Function [NCT00543205]Phase 2/Phase 36 participants (Actual)Interventional2005-08-31Terminated(stopped due to Terminated due to very slow enrollment)
A Phase 1/2 Study of Bcl-2 Antisense Oligonucleotide G3139 in Combination With Doxorubicin and Docetaxel in Metastatic and Locally Advanced Breast Cancer [NCT00063934]Phase 1/Phase 231 participants (Actual)Interventional2003-05-31Terminated
A Safety, Pharmacokinetic, and Pharmacodynamic Assessment of Genasense Administered as a 2-hour Intravenous Infusion to Subjects With Solid Tumors [NCT00636545]Phase 125 participants (Actual)Interventional2007-05-31Completed
Phase II Study of Genasense-Carboplatin-Paclitaxel-Combination in Uveal Melanoma [NCT01200342]Phase 27 participants (Actual)Interventional2010-12-31Terminated(stopped due to Pharmaceutical company no longer manufacturing investigational product.)
Randomized Phase II Trial of Docetaxel (Taxotere) and Oblimersen (Antisense Oligonucleotide Directed to BCL-2) Versus Taxotere Alone in Patients With Hormone-Refractory Prostate Cancer [NCT00085228]Phase 2116 participants (Actual)Interventional2004-04-30Completed
A Phase I/II Study of G3139 (Genasense) in Combination With RICE Chemotherapy in Relapsed B-Cell Non-Hodgkin's Lymphoma [NCT00086944]Phase 1/Phase 225 participants (Actual)Interventional2004-05-31Completed
A Multicenter, Randomized, Double-blind Study of Dacarbazine With or Without Genasense in Chemotherapy-naive Subjects With Advanced Melanoma and Low LDH (The AGENDA Trial) [NCT00518895]Phase 3300 participants (Anticipated)Interventional2007-07-31Completed
A Phase I Pharmacokinetic Study of Genasense® in Subjects With Normal Renal Function and Mildly and Moderately Impaired Renal Function [NCT00543075]Phase 123 participants (Actual)Interventional2006-05-31Completed
A Pharmacokinetic and Safety Assessment of G3139 Administered by Subcutaneous Injection to Patients With Solid Tumors [NCT00543231]Phase 18 participants (Anticipated)Interventional2005-12-31Completed
A Phase I/IIA Dose-Escalating Trial of BCL-2 Antisense (G3139) Treatment for Patients With Androgen-Independent Prostate Cancer or Other Advanced Solid Tumor Malignancies [NCT00003103]Phase 1/Phase 257 participants (Anticipated)Interventional1997-08-31Completed
Continuation Protocol For G3139 (Bcl-2 Antisense Oligonucleotide) And Dacarbazine In Patients With Malignant Melanoma Who Responded To This Combination In Protocol GM301 [NCT00070343]0 participants Interventional2003-08-31Active, not recruiting
A Phase II Trial of Rituximab + Oblimersen Sodium (GenasenseTM, G3139, NSC #683428, IND #58842) in Patients With Previously Untreated Follicular Non-Hodgkin Lymphoma (NHL) [NCT00301795]Phase 252 participants (Anticipated)Interventional2006-03-31Terminated
A Phase I/Ib Study of BP1002 (a Liposomal Bcl-2 Antisense Oligodeoxynucleotide) in Patients With Refractory/Relapsed Acute Myeloid Leukemia (AML) [NCT05190471]Phase 148 participants (Anticipated)Interventional2022-08-16Recruiting
A Phase III Study of Daunorubicin and Cytarabine +/- G3139 (Genasense, Oblimersen Sodium, NSC #683428, IND #58842), a BCL2 Antisense Oligodeoxynucleotide, in Previously Untreated Patients With Acute Myeloid Leukemia (AML) > / = 60 Years [NCT00085124]Phase 3500 participants (Actual)Interventional2003-12-31Completed
Randomized Study Of Dacarbazine Versus Dacarbazine Plus G3139 (Bcl-2 Antisense Oligonucleotide) In Patients With Advanced Malignant Melanoma [NCT00016263]Phase 30 participants Interventional2000-07-31Completed
A Phase I Trial Of G3139 (BCL-2 Antisense, NSC# 683428, IND# 58842) Combined With Cytotoxic Chemotherapy In Relapsed Childhood Solid Tumors [NCT00039481]Phase 115 participants (Actual)Interventional2002-11-30Completed
Phase II Study of Genasense (Bcl-2 Antisense) Combined With Mylotarg (Gemtuzumab Ozogamicin) in Elderly Patients With Relapsed Acute Myeloid Leukemia [NCT00017589]Phase 20 participants Interventional2000-12-31Completed
A PHASE II STUDY OF G3139 (GENASENSE™, NSC # 683428 IND # 58842) + IMATINIB MESYLATE (GLEEVEC®, STI571) IN PATIENTS WITH IMATINIB-RESISTANT CHRONIC MYELOID LEUKEMIA [NCT00049192]Phase 243 participants (Anticipated)Interventional2002-11-30Completed
A Phase I/II Study of Oblimersen Sodium (G3139, Genasense) in Combination With Oxaliplatin, 5FU and Leucovorin (FOLFOX4) Regimen in Advanced Colorectal Cancer [NCT00055822]Phase 1/Phase 216 participants (Actual)Interventional2002-10-31Completed
A Phase I Study of Oblimersen (Genasense™, G3139) in Combination With Gemcitabine in Advanced Malignancies [NCT00060112]Phase 115 participants (Actual)Interventional2003-03-31Terminated(stopped due to Administratively complete.)
A Phase I Study of G3139 ( NSC # 683428) in Combination With Cytarabine and Daunorubicin in Previously Untreated Patients With Acute Myeloid Leukemia (AML)>= 60 Years of Age [NCT00039117]Phase 132 participants (Actual)Interventional2002-04-30Completed
A Phase II Study Of Genasense In Combination With Thalidomide And Dexamethasone In Relapsed And Refractory Multiple Myeloma [NCT00049374]Phase 20 participants Interventional2002-09-30Completed
Randomized Study Of Fludarabine And Cyclophosphamide With Or Without Genasense (Bcl-2 Antisense Oligonucleotide) In Subjects With Relapsed Or Refractory Chronic Lymphocytic Leukemia [NCT00024440]Phase 30 participants Interventional2001-07-31Completed
Randomized Study of Docetaxel Versus Docetaxel Plus Genasense™ (G3139; Bcl-2 Antisense Oligonucleotide) in Patients With Previously Treated Non-Small Cell Lung Cancer [NCT00030641]Phase 2/Phase 30 participants Interventional2001-10-31Active, not recruiting
Phase I/II Study of G3139 (Genasense) in Patients With Waldenstrom's Macroglobulinemia [NCT00062244]Phase 1/Phase 258 participants (Actual)Interventional2003-05-31Completed
A Phase I Study Of G3139 Antisense Oligonucleotide (Oblimersen) In Combination With CHOP And Rituximab In Untreated Advanced Stage Diffuse Large B Cell Lymphoma [NCT00070083]Phase 10 participants Interventional2003-07-31Completed
A Pilot Study of Genasense® (G3139, Oblimersen Sodium, Bcl-2 Antisense Oligonucleotide), Fludarabine and Rituximab in Previously Treated Subjects With Chronic Lymphocytic Leukemia [NCT00078234]Phase 1/Phase 225 participants (Actual)Interventional2003-11-30Completed
Standard Dose Cyclophosphamide, Doxorubicin, Vincristine, Prednisone (CHOP) and Rituximab, or Rituximab and G3139 Phosphorothioate Oligonucleotide (BCL-2 Antisense - NSC-683428) Therapy for Young Patients (< Age 60) With Advanced Stage Diffuse Large B-Cel [NCT00080847]Phase 2160 participants (Actual)Interventional2004-03-31Terminated
A Randomized Phase II Study Of Carboplatin And Etoposide With Or Without G3139 (NSC #683428, IND #58842) In Patients With Extensive Stage Small Cell Lung Cancer [NCT00042978]Phase 255 participants (Actual)Interventional2003-04-30Completed
A Phase I Study of Antisense Bcl-2 Oligonucleotide (G3139) in Combination With Carboplatin and Paclitaxel in Patients With Advanced Solid Tumors [NCT00054548]Phase 155 participants (Actual)Interventional2002-10-31Completed
A Phase II Study of G3139 in Combination With Doxorubicin in Advanced Hepatocellular Carcinoma [NCT00047229]Phase 227 participants (Actual)Interventional2002-10-31Completed
A Phase II Trial of G3139 (Genasense) Anti-Bcl-2 Antisense Oligonucleotide Plus Alpha-Interferon in Metastatic Renal Cancer [NCT00059813]Phase 241 participants (Anticipated)Interventional2003-08-31Completed
A Phase I/II, Pharmacokinetic, and Biologic Correlative Study of G3139, NSC # 683428 (Phosphorothioate Antisense Oligonucleotide Directed to Bcl-2) and Irinotecan in Patients With Metastatic Colorectal Cancer [NCT00004870]Phase 1/Phase 20 participants Interventional2000-06-30Completed
A Phase I/II Study of G3139, a BCL-2 Antisense Oligonucleotide, Combined With Paclitaxel for the Treatment of Recurrent Small Cell Lung Cancer [NCT00005032]Phase 1/Phase 212 participants (Actual)Interventional2000-04-30Completed
A Phase I Study of G3139 (NSC 683428) in Combination With Salvage Chemotherapy for Treatment of Refractory and Relapsed Acute Myeloid Leukemia (AML) and Acute Lymphoblastic Leukemia (ALL) [NCT00004862]Phase 124 participants (Actual)Interventional1999-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00054639 (1) [back to overview]Number of Patients With Objective Response
NCT00063934 (4) [back to overview]Bcl-2 Expression in Breast Cancer Tissue
NCT00063934 (4) [back to overview]Number of Participant With Toxicities
NCT00063934 (4) [back to overview]Number of Participants With Pathologic Complete Response (pCR)
NCT00063934 (4) [back to overview]Clinical Imaging Responses
NCT00064259 (1) [back to overview]Maximum Tolerated Dose (MTD) of Oblimersen in Combination With Cisplatin and 5-FU
NCT00736450 (2) [back to overview]Time to Perform Microarray Study After Receipt of Tissue
NCT00736450 (2) [back to overview]Number of Participants With Microarray Testing Results Are Completed Within 7 Days.
NCT01200342 (2) [back to overview]Overall Response Rate (Percentage Subjects With Confirmed Complete or Partial Response)
NCT01200342 (2) [back to overview]Number of Participants With Response

Number of Patients With Objective Response

Efficacy as measured by objective response complete (CR) and partial (PR) response rates at 2 months following study treatment (NCT00054639)
Timeframe: 2 months following study treatment

Interventionparticipants (Number)
Complete ResponsesPartial Responses
Oblimersen + Rituximab108

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Bcl-2 Expression in Breast Cancer Tissue

Number of participant with Bcl-2 Expression in breast cancer tissue by protein and mRNA expression before treatment and at 3-5 days after oblimersen treatment. (NCT00063934)
Timeframe: before treatment and at 3-5 days after oblimersen treatment

Interventionparticipants (Number)
Oblimersen Plus Doxorubicin + Docetaxel30

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Number of Participant With Toxicities

(NCT00063934)
Timeframe: From baseline until the date of first documented toxicity or date of death from any cause, whichever came first, assessed every three weeks up to 2 years and 5 months

InterventionParticipants (Count of Participants)
Oblimersen Plus Doxorubicin + Docetaxel30

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Number of Participants With Pathologic Complete Response (pCR)

Pathologic complete responses (pCR), defined as no evidence of residual invasive tumor, including no residual tumor in the axillary lymph nodes, measured by microscopic evaluation of tissue specimen at time of definitive surgery (after 6 courses of neoadjuvant therapy). Neoadjuvant (preoperative) therapy administered on the first five days of every 3-week cycle. Response Evaluation Criteria in Solid Tumors (RECIST) Committee [JNCI 92(3):205-216, 2000] (NCT00063934)
Timeframe: At time of definitive surgery (after 6 courses of neoadjuvant therapy in 3 week cycles), approximately 18 weeks

InterventionParticipants (Number)
Oblimersen Plus Doxorubicin + Docetaxel0

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Clinical Imaging Responses

Evaluation target lesions (clinical response) by physical exam/ultrasound measurements of primary tumor and axillary lymph nodes after 3-6 courses: Complete Response: Disappearance of all target lesions; Partial Response: >30% decrease in sum longest diameter (LD) of target lesions, reference baseline sum LD; Progressive Disease: >20% increase in sum of LD of target lesions, reference smallest sum LD recorded since treatment started or appearance of 1>new lesions; Stable Disease: Neither sufficient shrinkage for PR nor increase for PD, reference smallest sum LD since treatment started. (NCT00063934)
Timeframe: After 3 and 6 courses of 21 day treatments (up to 18 weeks)

Interventionparticipants (Number)
CRPR
Oblimersen Plus Doxorubicin + Docetaxel300

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Maximum Tolerated Dose (MTD) of Oblimersen in Combination With Cisplatin and 5-FU

Adverse events were evaluated according to the National Cancer Institute Common Toxicity Criteria (version 2.0). DLT was defined as grade 3 to 4 hematologic toxicity lasting more than 1 week after 5-FU/cisplatin, grade 3 to 4 nausea or vomiting occurring later than 11 days after cisplatin, grade 3 to 4 diarrhea occurring later than 10 days after 5-FU, and grade 3 to 4 mucositis at the beginning of the next cycle. (NCT00064259)
Timeframe: 21 days

Interventionmg/kg/d (Number)
Oblimersen + Cisplatin + 5-FU5

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Time to Perform Microarray Study After Receipt of Tissue

The time from tissue harvest to release of microarray test and IHC assay results will be noted in days. (NCT00736450)
Timeframe: Upto 14 days

Interventiondays (Mean)
Arm I4.4

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Number of Participants With Microarray Testing Results Are Completed Within 7 Days.

(NCT00736450)
Timeframe: Upto 7 days

InterventionParticipants (Count of Participants)
results within 7 days or lessresults in more than 7 days
Arm I112

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Overall Response Rate (Percentage Subjects With Confirmed Complete or Partial Response)

Tumor response by Response Evaluation Criteria in Solid Tumors for participants with measurable disease defined by presence of at least 1 measurable lesion at baseline: Complete Response (CR): disappearance all target lesions determined by 2 consecutive observations not less than 4 weeks apart. Partial Response (PR): >30% decrease in sum of LD of target lesions (LD) of target lesions taking as reference baseline sum LD determined by two consecutive observations not less than four weeks apart. Progression (PD): >20% increase in sum of LD of target lesions references smallest sum LD recorded since treatment started or appearance of one or more new lesions. Stable Disease (SD): neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD taking references smallest sum LD since treatment started. Measurable: lesions accurately measured in at least 1 dimension (longest diameter to be recorded) as 20 mm with conventional techniques or as 10 mm with spiral CT s (NCT01200342)
Timeframe: Following two 3-week cycles

InterventionPercentage of Participants (Number)
Genasense + Paclitaxel + Carboplatin0

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Number of Participants With Response

Tumor response by Response Evaluation Criteria in Solid Tumors for participants with measurable disease defined by presence of at least 1 measurable lesion at baseline: Complete Response (CR): disappearance all target lesions determined by 2 consecutive observations not less than 4 weeks apart. Partial Response (PR): >30% decrease in sum of LD of target lesions (LD) of target lesions taking as reference baseline sum LD determined by two consecutive observations not less than four weeks apart. Progression (PD): >20% increase in sum of LD of target lesions references smallest sum LD recorded since treatment started or appearance of one or more new lesions. Stable Disease (SD): neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD taking references smallest sum LD since treatment started. Measurable: lesions accurately measured in at least 1 dimension (longest diameter to be recorded) as 20 mm with conventional techniques or as 10 mm with spiral CT s (NCT01200342)
Timeframe: Following two 3-week cycles

InterventionParticipants (Number)
Complete Response (CR)Partial Response (PR)Progressive Disease (PD)Stable Disease (SD)
Genasense + Paclitaxel + Carboplatin0016

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