Page last updated: 2024-11-12

gx 15-070

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

Description

obatoclax: a pan-Bcl-2 inhibitor potentially useful in treating mantle cell lymphoma [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID45356963
MeSH IDM0541159

Synonyms (13)

Synonym
gx15-070
obatoclax
obatoclax [inn]
1h-indole, 2-(2-((3,5-dimethyl-1h-pyrrol-2-yl)methylene)-3-methoxy-2h-pyrrol-5-yl)-
qn4128b52a ,
2-(2-((3,5-dimethyl-1h-pyrrol-2-yl)methylene)-3-methoxy-2h-pyrrol-5-yl)-1h-indole
gx-15-070
unii-qn4128b52a
gx 05-070
gx 015-070
803712-67-6
2-[5(3,5-dimethyl-1h-pyrrol-2-ylmethylene)-4-methoxy-5h-pyrrol-2-yl]-1h-indole
DTXSID701029688

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Collectively, our data demonstrate that Obatoclax mediated inhibition of MCL-1 rapidly enhances Lapatinib toxicity in tumor cells via a toxic form of autophagy and via AIF release from the mitochondrion."( Inhibition of MCL-1 enhances lapatinib toxicity and overcomes lapatinib resistance via BAK-dependent autophagy.
Dent, P; Grant, S; Martin, AP; Mitchell, C; Nephew, KP; Rahmani, M, 2009
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" In combination with VSV, obatoclax synergistically induced cell death in primary CLL samples and reduced tumor growth in severe combined immunodeficient (SCID) mice-bearing A20 lymphoma tumors."( VSV oncolysis in combination with the BCL-2 inhibitor obatoclax overcomes apoptosis resistance in chronic lymphocytic leukemia.
Bell, J; Hiscott, J; Nguyên, TL; Oliere, S; Samuel, S; Shamy, A; Tumilasci, VF, 2010
)
0.36
" A phase I trial was conducted to evaluate the safety of obatoclax, a Bcl-2 family inhibitor, given in combination with standard chemotherapy."( A phase I trial of pan-Bcl-2 antagonist obatoclax administered as a 3-h or a 24-h infusion in combination with carboplatin and etoposide in patients with extensive-stage small cell lung cancer.
Berger, MS; Blakely, J; Chiappori, AA; Chu, QS; Moezi, MM; Ross, HJ; Salgia, R; Schnyder, J; Schreeder, MT; Stephenson, JJ; Subramaniam, DS, 2012
)
0.38
" Patients were treated with escalating doses of obatoclax, either as a 3- or 24-h infusion, on days 1-3 of a 21-day cycle, in combination with carboplatin (area under the curve 5, day 1 only) and etoposide (100 mg m(-2), days 1-3)."( A phase I trial of pan-Bcl-2 antagonist obatoclax administered as a 3-h or a 24-h infusion in combination with carboplatin and etoposide in patients with extensive-stage small cell lung cancer.
Berger, MS; Blakely, J; Chiappori, AA; Chu, QS; Moezi, MM; Ross, HJ; Salgia, R; Schnyder, J; Schreeder, MT; Stephenson, JJ; Subramaniam, DS, 2012
)
0.38
"Although associated with a higher incidence of transient CNS AEs than the 24-h infusion, 3-h obatoclax infusion combined with carboplatin-etoposide was generally well tolerated at doses of 30 mg per day."( A phase I trial of pan-Bcl-2 antagonist obatoclax administered as a 3-h or a 24-h infusion in combination with carboplatin and etoposide in patients with extensive-stage small cell lung cancer.
Berger, MS; Blakely, J; Chiappori, AA; Chu, QS; Moezi, MM; Ross, HJ; Salgia, R; Schnyder, J; Schreeder, MT; Stephenson, JJ; Subramaniam, DS, 2012
)
0.38
"Obatoclax was administered with docetaxel in patients with relapsed or refractory NSCLC- docetaxel as a 1-hour infusion on day 1 and obatoclax as a 24-hour infusion on days 1 and 2-every 3 weeks for up to eight cycles."( Obatoclax mesylate, a pan-bcl-2 inhibitor, in combination with docetaxel in a phase 1/2 trial in relapsed non-small-cell lung cancer.
Adams, JW; Berger, MS; Chiappori, A; Edelman, MJ; Haura, EB; Malik, S; Northfelt, DW; Rosen, P; Van Echo, DA; Williams, C, 2014
)
0.4
" It is concluded that obatoclax can be safely administered to relapsed CLL patients in combination with FR and shows promising clinical activity."( Obatoclax in combination with fludarabine and rituximab is well-tolerated and shows promising clinical activity in relapsed chronic lymphocytic leukemia.
Brown, JR; Fisher, DC; Freedman, AS; Mikler, E; Neuberg, D; Reynolds, HM; Takebe, N; Tesar, B; Thompson, C; Werner, L; Yu, L, 2015
)
0.42
"Obatoclax is a pan-Bcl-2 inhibitor with promising efficacy, especially when combined with other antineoplastic agents."( Obatoclax as a perpetrator in drug-drug interactions and its efficacy in multidrug resistance cell lines.
Allendorf, D; Jassowicz, A; Köhler, BC; Theile, D; Weiss, J, 2015
)
0.42
"The present study aimed to investigate the effects of obatoclax (OBX) combined with gemcitabine (GEM) treatment on the proliferation, migration, invasion and epithelial‑mesenchymal transition (EMT) related proteins of pancreatic cancer cell line BxPC‑3 under hypoxic conditions."( Effects of obatoclax combined with gemcitabine on the biological activity of pancreatic cancer cells under hypoxic conditions.
Hou, XF; Li, K; Li, S; Wang, JF; Wu, C; Xu, SN, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (174)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's24 (13.79)29.6817
2010's138 (79.31)24.3611
2020's12 (6.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (8.57%)5.53%
Reviews20 (11.43%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other140 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]