General
Preferred name
PIXANTRONE
Synonyms
BBR-2778 ()
BBR 2778 dimaleate ()
Pixantrone Maleate ()
PIXANTRONE DIMALEATE ()
Pixantrone (maleate) ()
BBR 2778 ()
BBR 2778 DIMALEATE ()
BBR-2778 DIMALEATE ()
NSC-752341 ()
Pixuvri ()
Pixantrone maleate ()
Pixantrone dimaleate salt ()
Pixantrone-d8 (maleate) ()
P&D ID
PD016142
CAS
144675-97-8
144510-96-3
Tags
nuisance
drug candidate
drug
available
Approved by
EMA
First approval
2012
Drug Status
investigational
approved
Drug indication
Follicular lymphoma
Diffuse large B-cell lymphoma
Pediatric cancer
Multiple sclerosis
Max Phase
Phase 4
Phase 3
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Pixantrone is an experimental antineoplastic drug and also shows immunosuppressant activity .
PHARMACODYNAMICS
Pixantrone has a wide range of antitumor activity, especially in terms of treating leukemias and lymphomas [3]. ; ; Pixantrone lacks cardio-toxic effects. It has postulated that his is because of its redox inactivity and lack and inhibition of doxorubicinol formation in human myocardium. [3]
DESCRIPTION
Pixantrone is an antineoplastic drug that also shows immunosuppressant activity . It is administered clinically as pixantrone dimaleate (PubChem CID: 9937618).
(GtoPdb)
INDICATION
Currently in Phase III investigation for treatment of relapsed or refractory aggressive non-Hodgkin's lymphoma in patients who have failed two prior lines of therapy. Presently, no standard therapy exists for patients with relapsed or refractory NHL. [2] After first line therapy has been initiated, most patients have received their lifetime limit of doxorubicin and further use of anthracyclines may potentially lead to anthracycline-induced congestive heart failure (CHF). Pixantrone is an attractive alternative as a second line agent, due to its lack of cardiac toxicity. [2] ; ; The phase III trial, PIX-R, is ongoing and will compare pixantrone multidrug therapy with an equivalent regimen in patients with diffuse large B-cell lymphoma (the most common type of NHL).; ; Previous study results have also suggested the possibility that pixantrone may be safe and effective in doxorubicin naive patients. In myocardial strips which are doxorubicin naive, pixantrone is taken up to a higher degree than in myocardial strips which are doxorubicin exposed, and once absorbed exhibits redox inactivity. [3] ; ; Pixantrone dimaleate has also been investigated as a treatment for acute myelogenous leukemia, diffuse large B-cell lymphoma, follicular lymphoma, metastatic breast cancer, low grade small lymphocytic lymphomas and general metastatic cancers.
DESCRIPTION
Pixantrone is a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity. Pixantrone is a potentially more effective, less cardiotoxic alternative to doxorubicin for patients with aggressive non-Hodgkin lymphoma (aNHL).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
19
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMatrix
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Nuisance compounds in cellular assays
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
41
Molecular Weight
325.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
4
Rotatable Bonds
6
Ring Count
3
Aromatic Ring Count
2
cLogP
0.6
TPSA
123.13
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
6.0
QED
0.52
Structural alerts
3
quinone_A(370)
[!#6&!#1]=[#6]-1-[#6]=,:[#6]-[#6](=[!#6&!#1])-[#6]=,:[#6]-1
PAINS Family A
anthranil_one_A(38)
c:1:c:c:c:c(:c:1-[#7&!H0;!H1,!$([#7]-[#6]=[#8])])-[#6](-[#6]:[#6])=[#8]
PAINS Family B
Intercalation
Nuisance compounds in cellular assays
Related compounds
Custom attributes
(extracted from source data)
Target
Topoisomerase
TOP2A
Pathway
Cell Cycle/DNA Damage
DNA Damage
Indication
non-Hodgkin lymphoma (NHL)
MOA
Topoisomerase inhibitor
Source data
