pixantrone: an immunosuppressant; structure given in first source
ID Source | ID |
---|---|
PubMed CID | 134019 |
CHEMBL ID | 167731 |
CHEBI ID | 135945 |
SCHEMBL ID | 7825 |
MeSH ID | M0229455 |
Synonym |
---|
6,9-bis((2-aminoethyl)amino)benzo(g)isoquinoline-5,10-dione |
6,9-bis((2-aminoethyl)amino)benz(g)isoquinoline-5,10-dione |
unii-f5sxn2knmr |
6,9-aea-biqdo |
benz(g)isoquinoline-5,10-dione, 6,9-bis((2-aminoethyl)amino)- |
f5sxn2knmr , |
pixantrone [usan:inn:ban] |
5,8-bis((2-aminoethyl)amino)-2-aza-anthracene-9,10-dione |
pixantrone |
144510-96-3 |
pixantrone (usan/inn) |
D05522 |
bbr-2778 |
CHEBI:135945 |
AKOS005145782 |
CHEMBL167731 |
6,9-bis(2-aminoethylamino)benzo[g]isoquinoline-5,10-dione |
A808224 |
6,9-bis(2-azanylethylamino)benzo[g]isoquinoline-5,10-dione |
FT-0673961 |
FT-0689753 |
bbr2778 |
AM84406 |
HY-13727 |
SCHEMBL7825 |
gtpl7544 |
6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione |
pixantrone [usan] |
pixantrone [who-dd] |
pixantrone [mart.] |
pixantrone [inn] |
pixantrone [mi] |
PEZPMAYDXJQYRV-UHFFFAOYSA-N |
NCGC00274280-01 |
6,9-bis((2-aminoethyl)amino)benzo[g]isoquinoline-5,10-dione |
AC-26441 |
pixantrone (bbr 2778) |
DTXSID10162744 |
DB06193 |
(6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione) |
BCP05981 |
Q7199690 |
SB16817 |
benz[g]isoquinoline-5,10-dione, 6,9-bis[(2-aminoethyl)amino]- |
6,9-bis[(2-aminoethyl)amino]-5h,10h-benzo[g]isoquinoline-5,10-dione |
EN300-18707593 |
Pixantrone is a first-in-class aza-anthracenedione approved as monotherapy for treatment of relapsed or refractory aggressive diffuse B-cell non-Hodgkin's lymphoma. Pixantrone has a significantly reduced cardiotoxicity while maintaining good anti-tumor activity.
Pixantrone has a conditional European marketing approval for monotherapy in adults with multiple relapsed or refractory aggressive B-cell non-Hodgkin lymphoma.
Excerpt | Reference | Relevance |
---|---|---|
"Pixantrone has a conditional European marketing approval for monotherapy in adults with multiple relapsed or refractory aggressive B-cell non-Hodgkin lymphoma." | ( Pixantrone-rituximab versus gemcitabine-rituximab in relapsed/refractory aggressive non-Hodgkin lymphoma. Andorsky, D; Beck, JT; Belada, D; Dakhil, S; Daly, R; Dean, JP; Failloux, N; Georgiev, P; Hübel, K; Inhorn, LF; Pavlyuk, M; Pettengell, R; Quick, D, 2016) | 2.6 |
"Pixantrone (PIX) has been approved for treating aggressive B-cell non-Hodgkin's lymphoma." | ( Pixantrone Sensitizes Gram-Negative Pathogens to Rifampin. Li, L; Li, Y; Li, Z; Liu, S; She, P; Wu, Y; Yang, Y; Zhou, L, 2022) | 2.89 |
"Pixantrone has a conditional European marketing approval for monotherapy in adults with multiple relapsed or refractory aggressive B-cell non-Hodgkin lymphoma." | ( Pixantrone-rituximab versus gemcitabine-rituximab in relapsed/refractory aggressive non-Hodgkin lymphoma. Andorsky, D; Beck, JT; Belada, D; Dakhil, S; Daly, R; Dean, JP; Failloux, N; Georgiev, P; Hübel, K; Inhorn, LF; Pavlyuk, M; Pettengell, R; Quick, D, 2016) | 2.6 |
"Pixantrone has also been used for the treatment of indolent non-Hodgkin's lymphomas and the combination of pixantrone and rituximab has been shown to be superior to rituximab alone in relapsed or refractory disease in the phase III PIX302 study." | ( Pixantrone maleate for non-Hodgkin's lymphoma. Mukherji, D; Pettengell, R, 2009) | 2.52 |
"Pixantrone has been shown to be superior to other single-agent therapies for the salvage treatment of relapsed/refractory aggressive non-Hodgkin lymphoma. " | ( Pixantrone for the treatment of aggressive non-Hodgkin lymphoma. Mukherji, D; Pettengell, R, 2010) | 3.25 |
Redox inactivity in the face of high cardiac uptake suggests that pixantrone might also be safe in doxorubicin-naïve patients. Pixantrone is an analogue of MX devoid of toxic effects on cardiac tissue.
Excerpt | Reference | Relevance |
---|---|---|
" This Phase I dose escalation trial of BBR 2778 was conducted to determine the maximum tolerated dose, the dose-limiting toxicity, and the pharmacokinetic profile of BBR 2778 in patients with advanced solid tumors." | ( A phase I and pharmacokinetic study of the novel aza-anthracenedione compound BBR 2778 in patients with advanced solid malignancies. Armand, JP; Bernareggi, A; Boige, V; Buthaut, X; Camboni, G; Faivre, S; Gatineau, M; Raymond, E; Rixe, O, 2001) | 0.31 |
Class | Description |
---|---|
isoquinolines | A class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives. |
[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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.8999 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
G | Vesicular stomatitis virus | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 2.6837 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
Interferon beta | Homo sapiens (human) | Potency | 18.9991 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 6.0385 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID315337 | Effect on apoptosis in human HT29 PI+/AnnV- cells after 12 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315338 | Effect on apoptosis in human HT29 PI-/AnnV+ cells after 12 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315331 | Cytotoxicity against human HT29 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315342 | Effect on apoptosis in human HT29 PI-/AnnV+ cells after 24 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315335 | Effect on apoptosis in human HT29 PI+/AnnV+ cells after 6 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315336 | Effect on apoptosis in human HT29 PI-/AnnV- cells after 12 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID232016 | Resistance index is the ratio of IC50 of resistant cell line/IC50 of sensitive cell line | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | 6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations. |
AID315332 | Effect on apoptosis in human HT29 PI-/AnnV- cells after 6 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315334 | Effect on apoptosis in human HT29 PI-/AnnV+ cells after 6 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID102188 | Tested in vitro for cytotoxic activity against Human colon Adenocarcinoma sensitive cell line (LoVo) | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | 6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations. |
AID315341 | Effect on apoptosis in human HT29 PI+/AnnV- cells after 24 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315340 | Effect on apoptosis in human HT29 PI-/AnnV- cells after 24 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315339 | Effect on apoptosis in human HT29 PI+/AnnV+ cells after 12 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID102331 | Tested in vitro for cytotoxic activity against Doxorubicin resistant Human colon Adenocarcinoma sensitive cell line | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | 6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations. |
AID315343 | Effect on apoptosis in human HT29 PI+/AnnV+ cells after 24 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
AID315333 | Effect on apoptosis in human HT29 PI+/AnnV- cells after 6 hrs by biparametric flow cytometric analysis | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 4 (4.40) | 18.2507 |
2000's | 24 (26.37) | 29.6817 |
2010's | 50 (54.95) | 24.3611 |
2020's | 13 (14.29) | 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 (33.30) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 16 (17.39%) | 5.53% |
Reviews | 16 (17.39%) | 6.00% |
Case Studies | 3 (3.26%) | 4.05% |
Observational | 1 (1.09%) | 0.25% |
Other | 56 (60.87%) | 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 | ||
---|---|---|---|---|---|---|---|
Pixantrone (BBR 2778) Versus Other Chemotherapeutic Agents for Third-line Single Agent Treatment of Patients With Relapsed Aggressive Non-Hodgkin's Lymphoma: A Randomized, Controlled, Phase III Comparative Trial [NCT00088530] | Phase 3 | 140 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
A Phase I/II Study of Pixantrone (BBR 2778) in Patients With Refractory Acute Myelogenous Leukemia (AML) [NCT00106600] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
A Phase 1, Dose-Escalation Study of Pixantrone Monotherapy in Pediatric Patients With Relapsed or Refractory Cancer [NCT02800889] | Phase 1 | 0 participants (Actual) | Interventional | 2016-10-24 | Withdrawn(stopped due to Study withdrawn; no participants enrolled) | ||
A Multicentre, Phase II, Open Label, Single Arm Study of Pixantrone in Patients With CD20-positive Relapsed or Refractory Aggressive Non-Hodgkin Lymphoma Treated With Rituximab, Ifosfamide and Etoposide. [NCT03458260] | Phase 2 | 74 participants (Actual) | Interventional | 2018-03-26 | Active, not recruiting | ||
A Non-randomized Cohort Study With Matched Controls Investigating Pharmacokinetic Parameters and Safety of a Single Dose of Pixantrone With Metastatic Cancer and Moderate, Severe, or No Hepatic Impairment. [NCT01632436] | Phase 1 | 0 participants (Actual) | Interventional | 2012-05-31 | Withdrawn(stopped due to No eligible patients enrolled) | ||
Fludarabine, BBR 2778 (Pixantrone) and Rituximab (FP-R) vs Fludarabine and Rituximab (F-R) for Relapsed or Refractory Indolent Non-Hodgkin's Lymphoma [NCT00577161] | Phase 3 | 0 participants (Actual) | Interventional | 2007-09-30 | Withdrawn(stopped due to closed to enrollment) | ||
A Randomized Phase III Trial Comparing the Combination of Fludarabine, BBR 2778 (Pixantrone) and Rituximab (FP-R) With the Combination of Fludarabine and Rituximab (F-R) in the Treatment of Patients With Relapsed or Refractory Indolent Non-Hodgkin's Lymph [NCT00551239] | Phase 3 | 0 participants (Actual) | Interventional | 2007-08-31 | Withdrawn | ||
A Phase I Trial of BBR 2778 in Combination With Fludarabine, Dexamethasone and Rituximab in the Treatment of Patients With Relapsed or Refractory Indolent Non-Hodgkin's Lymphoma [NCT00060684] | Phase 1 | 30 participants | Interventional | 2001-12-31 | Completed | ||
A Phase II Trial of BBR 2778 in Combination With Cytarabine, Methylprednisolone and Cisplatin (BSHAP) as Salvage in Patients With Relapsed Aggressive Non-Hodgkin's Lymphoma [NCT00069966] | Phase 2 | 0 participants | Interventional | 2003-04-30 | Active, not recruiting | ||
A Phase I Trial of BBR 2778 in Combination With Cytarabine, Methylprednisolone and Cisplatin in the Treatment of Patients With Relapsed or Refractory Aggressive Non-Hodgkin's Lymphoma [NCT00053105] | Phase 1 | 0 participants | Interventional | 2002-02-28 | Active, not recruiting | ||
An Open-Label, Randomized, Phase III Comparative Trial of BBR 2778 + Rituximab Versus Rituximab in the Treatment of Patients With Relapsed or Refractory Indolent Non-Hodgkin's Lymphoma (NHL) [NCT00060671] | Phase 3 | 800 participants | Interventional | 2005-01-31 | Terminated | ||
Randomized Phase II Study of Two Doses of Pixantrone in Patients With Metastatic Breast Cancer [NCT01086605] | Phase 2 | 46 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
Phase I/II Study of the Combination of Bendamustine, Rituximab and Pixantrone in Patients With Relapsed/Refractory B Cell Non-Hodgkin's Lymphoma [NCT01491841] | Phase 1 | 33 participants (Actual) | Interventional | 2011-11-01 | Completed | ||
A Randomized Multicenter Study Comparing Pixantrone + Rituximab With Gemcitabine + Rituximab in Patients With Aggressive B-cell Non-Hodgkin Lymphoma Who Have Relapsed After Therapy With CHOP-R or an Equivalent Regimen and Are Ineligible for Stem Cell Tran [NCT01321541] | Phase 3 | 312 participants (Actual) | Interventional | 2011-04-20 | Completed | ||
The GOAL Trial: Rescue Treatment With the Monoclonal Anti CD20-antibody Obinutuzumab (GA101) in Combination With Pixantrone for the Treatment of Patients With Relapsed Aggressive B-cell Lymphoma [NCT02499003] | Phase 2 | 70 participants (Actual) | Interventional | 2015-08-14 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |