oblimersen: targets the Bcl-2 oncogene good efficacy with low toxicity tumour regressions [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
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PubMed CID | 118984457 |
MeSH ID | M0362850 |
Synonym |
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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 |
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.
Excerpt | Reference | Relevance |
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"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 |
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.
Excerpt | Reference | Relevance |
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"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 |
Excerpt | Reference | Relevance |
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"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 |
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.
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.
Excerpt | Relevance | Reference |
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" 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 |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (1.08) | 18.2507 |
2000's | 152 (81.72) | 29.6817 |
2010's | 25 (13.44) | 24.3611 |
2020's | 7 (3.76) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (30.67) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 40 (20.51%) | 5.53% |
Reviews | 54 (27.69%) | 6.00% |
Case Studies | 1 (0.51%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 100 (51.28%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
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A Phase II Study of G3139 (Bcl-2 Antisense) And Rituximab in Patients With Recurrent B-cell Non-Hodgkinâs Lymphomas [NCT00054639] | Phase 2 | 48 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
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 2 | 15 participants (Actual) | Interventional | 2003-06-30 | Terminated(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 1 | 37 participants (Actual) | Interventional | 2008-07-23 | Terminated(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 2 | 96 participants (Actual) | Interventional | 2005-09-30 | Terminated | ||
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 3 | 0 participants | Interventional | 2006-06-30 | Withdrawn | ||
A Phase II Study of G3139 (Genasense ™) in Patients With Merkel Cell Carcinoma [NCT00079131] | Phase 2 | 37 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
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 1 | 12 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
Randomized Phase III Study of Dexamethasone With or Without Genasense (Bcl-2 Antisense Oligonucleotide) in Patients With Relapsed or Refractory Multiple Myeloma [NCT00017602] | Phase 3 | 0 participants | Interventional | 2000-12-31 | Completed | ||
"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 1 | 28 participants (Anticipated) | Interventional | 2006-11-30 | Active, not recruiting | ||
A Randomized, Open-label, Cross-over Pharmacokinetic Study of Dacarbazine in Combination With Genasense® in Subjects With Advanced Melanoma [NCT00542893] | Phase 1 | 0 participants | Interventional | 2006-04-30 | Completed | ||
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 3 | 6 participants (Actual) | Interventional | 2005-08-31 | Terminated(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 2 | 31 participants (Actual) | Interventional | 2003-05-31 | Terminated | ||
A Safety, Pharmacokinetic, and Pharmacodynamic Assessment of Genasense Administered as a 2-hour Intravenous Infusion to Subjects With Solid Tumors [NCT00636545] | Phase 1 | 25 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
Phase II Study of Genasense-Carboplatin-Paclitaxel-Combination in Uveal Melanoma [NCT01200342] | Phase 2 | 7 participants (Actual) | Interventional | 2010-12-31 | Terminated(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 2 | 116 participants (Actual) | Interventional | 2004-04-30 | Completed | ||
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 2 | 25 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
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 3 | 300 participants (Anticipated) | Interventional | 2007-07-31 | Completed | ||
A Phase I Pharmacokinetic Study of Genasense® in Subjects With Normal Renal Function and Mildly and Moderately Impaired Renal Function [NCT00543075] | Phase 1 | 23 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
A Pharmacokinetic and Safety Assessment of G3139 Administered by Subcutaneous Injection to Patients With Solid Tumors [NCT00543231] | Phase 1 | 8 participants (Anticipated) | Interventional | 2005-12-31 | Completed | ||
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 2 | 57 participants (Anticipated) | Interventional | 1997-08-31 | Completed | ||
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 | Interventional | 2003-08-31 | Active, 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 2 | 52 participants (Anticipated) | Interventional | 2006-03-31 | Terminated | ||
A Phase I/Ib Study of BP1002 (a Liposomal Bcl-2 Antisense Oligodeoxynucleotide) in Patients With Refractory/Relapsed Acute Myeloid Leukemia (AML) [NCT05190471] | Phase 1 | 48 participants (Anticipated) | Interventional | 2022-08-16 | Recruiting | ||
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 3 | 500 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
Randomized Study Of Dacarbazine Versus Dacarbazine Plus G3139 (Bcl-2 Antisense Oligonucleotide) In Patients With Advanced Malignant Melanoma [NCT00016263] | Phase 3 | 0 participants | Interventional | 2000-07-31 | Completed | ||
A Phase I Trial Of G3139 (BCL-2 Antisense, NSC# 683428, IND# 58842) Combined With Cytotoxic Chemotherapy In Relapsed Childhood Solid Tumors [NCT00039481] | Phase 1 | 15 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
Phase II Study of Genasense (Bcl-2 Antisense) Combined With Mylotarg (Gemtuzumab Ozogamicin) in Elderly Patients With Relapsed Acute Myeloid Leukemia [NCT00017589] | Phase 2 | 0 participants | Interventional | 2000-12-31 | Completed | ||
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 2 | 43 participants (Anticipated) | Interventional | 2002-11-30 | Completed | ||
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 2 | 16 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
A Phase I Study of Oblimersen (Genasense™, G3139) in Combination With Gemcitabine in Advanced Malignancies [NCT00060112] | Phase 1 | 15 participants (Actual) | Interventional | 2003-03-31 | Terminated(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 1 | 32 participants (Actual) | Interventional | 2002-04-30 | Completed | ||
A Phase II Study Of Genasense In Combination With Thalidomide And Dexamethasone In Relapsed And Refractory Multiple Myeloma [NCT00049374] | Phase 2 | 0 participants | Interventional | 2002-09-30 | Completed | ||
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 3 | 0 participants | Interventional | 2001-07-31 | Completed | ||
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 3 | 0 participants | Interventional | 2001-10-31 | Active, not recruiting | ||
Phase I/II Study of G3139 (Genasense) in Patients With Waldenstrom's Macroglobulinemia [NCT00062244] | Phase 1/Phase 2 | 58 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
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 1 | 0 participants | Interventional | 2003-07-31 | Completed | ||
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 2 | 25 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
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 2 | 160 participants (Actual) | Interventional | 2004-03-31 | Terminated | ||
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 2 | 55 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
A Phase I Study of Antisense Bcl-2 Oligonucleotide (G3139) in Combination With Carboplatin and Paclitaxel in Patients With Advanced Solid Tumors [NCT00054548] | Phase 1 | 55 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
A Phase II Study of G3139 in Combination With Doxorubicin in Advanced Hepatocellular Carcinoma [NCT00047229] | Phase 2 | 27 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
A Phase II Trial of G3139 (Genasense) Anti-Bcl-2 Antisense Oligonucleotide Plus Alpha-Interferon in Metastatic Renal Cancer [NCT00059813] | Phase 2 | 41 participants (Anticipated) | Interventional | 2003-08-31 | Completed | ||
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 2 | 0 participants | Interventional | 2000-06-30 | Completed | ||
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 2 | 12 participants (Actual) | Interventional | 2000-04-30 | Completed | ||
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 1 | 24 participants (Actual) | Interventional | 1999-10-31 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |