Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H19N5O2.2C4H4O4 |
Molecular Weight | 557.5094 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 2 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.NCCNC1=CC=C(NCCN)C2=C1C(=O)C3=C(C=NC=C3)C2=O
InChI
InChIKey=SVAGFBGXEWPNJC-SPIKMXEPSA-N
InChI=1S/C17H19N5O2.2C4H4O4/c18-4-7-21-12-1-2-13(22-8-5-19)15-14(12)16(23)10-3-6-20-9-11(10)17(15)24;2*5-3(6)1-2-4(7)8/h1-3,6,9,21-22H,4-5,7-8,18-19H2;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
Molecular Formula | C4H4O4 |
Molecular Weight | 116.0722 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
Molecular Formula | C17H19N5O2 |
Molecular Weight | 325.3651 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002055/WC500127970.pdfCurator's Comment: description was created based on several sources, including:
http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002055/WC500127968.pdf | https://www.medicines.org.uk/emc/PIL.30473.latest.pdf
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002055/WC500127970.pdf
Curator's Comment: description was created based on several sources, including:
http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002055/WC500127968.pdf | https://www.medicines.org.uk/emc/PIL.30473.latest.pdf
Pixantrone is a novel anthracenedione. It is a weak inhibitor of topoisomerase II. Pixantrone directly alkylates DNA forming stable DNA adducts and cross-strand breaks. Pixuvri is approved for the treatment of adult patients with multiply relapsed or refractory aggressive Non-Hodgkin lymphomas. It is used for patients whose cancer does not respond or has returned after they have received other chemotherapy treatments. The most frequent AE were seen in the blood (mainly neutropaenia), gastrointestinal (nausea, abdominal pain, constipation) and respiratory systems (cough, dyspnea). No drug-drug interaction studies have been submitted and no drug interactions have been reported in human subjects
CNS Activity
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002055/WC500127970.pdf
Curator's Comment: Known to be CNS penetrant in rodents. Human data not available.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2311221 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Pixuvri Approved UsePixuvri is used for the treatment of adult patients with multiply relapsed or refractory aggressive Non-Hodgkin lymphomas. Launch Date2012 |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
52.4 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
5 mg/m² single, intravenous dose: 5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
213.2 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
10 mg/m² single, intravenous dose: 10 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
483.2 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
16.5 mg/m² single, intravenous dose: 16.5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
762.4 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1189.6 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
35 mg/m² single, intravenous dose: 35 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1447.5 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
56 mg/m² single, intravenous dose: 56 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2241.9 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
84 mg/m² single, intravenous dose: 84 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
318.1 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
16.5 mg/m² 1 times / week multiple, intravenous dose: 16.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
701.4 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
25 mg/m² 1 times / week multiple, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1193 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
37.5 mg/m² 1 times / week multiple, intravenous dose: 37.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
4297.6 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
75 mg/m² 1 times / week multiple, intravenous dose: 75 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
7120.8 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
112.5 mg/m² 1 times / week multiple, intravenous dose: 112.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
3852.1 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
150 mg/m² 1 times / week multiple, intravenous dose: 150 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
438.1 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
5 mg/m² single, intravenous dose: 5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
451.1 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
10 mg/m² single, intravenous dose: 10 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
781.9 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
16.5 mg/m² single, intravenous dose: 16.5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1321.2 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2530.5 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
35 mg/m² single, intravenous dose: 35 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2266.8 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
56 mg/m² single, intravenous dose: 56 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3679.9 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
84 mg/m² single, intravenous dose: 84 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
502.6 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
16.5 mg/m² 1 times / week multiple, intravenous dose: 16.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1074.8 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
25 mg/m² 1 times / week multiple, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1773.4 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
37.5 mg/m² 1 times / week multiple, intravenous dose: 37.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
5027.1 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
75 mg/m² 1 times / week multiple, intravenous dose: 75 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
7882.3 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
112.5 mg/m² 1 times / week multiple, intravenous dose: 112.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
8058.5 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
150 mg/m² 1 times / week multiple, intravenous dose: 150 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
982 ng × h/mL |
33 mg/m² 1 times / week multiple, intravenous dose: 33 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1727 ng × h/mL |
49 mg/m² 1 times / week multiple, intravenous dose: 49 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3811 ng × h/mL |
88 mg/m² 1 times / week multiple, intravenous dose: 88 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
36.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
5 mg/m² single, intravenous dose: 5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
21.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
10 mg/m² single, intravenous dose: 10 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
20.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
16.5 mg/m² single, intravenous dose: 16.5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
19.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
31.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
35 mg/m² single, intravenous dose: 35 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
22.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
56 mg/m² single, intravenous dose: 56 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
17.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11432625/ |
84 mg/m² single, intravenous dose: 84 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
11.23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
16.5 mg/m² 1 times / week multiple, intravenous dose: 16.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
16.46 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
25 mg/m² 1 times / week multiple, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
13.77 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
37.5 mg/m² 1 times / week multiple, intravenous dose: 37.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
8.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
75 mg/m² 1 times / week multiple, intravenous dose: 75 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
9.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
112.5 mg/m² 1 times / week multiple, intravenous dose: 112.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
11.91 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11205916/ |
150 mg/m² 1 times / week multiple, intravenous dose: 150 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
23.3 h |
33 mg/m² 1 times / week multiple, intravenous dose: 33 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
23.3 h |
49 mg/m² 1 times / week multiple, intravenous dose: 49 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
23.3 h |
88 mg/m² 1 times / week multiple, intravenous dose: 88 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
50% |
33 mg/m² 1 times / week multiple, intravenous dose: 33 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
50% |
49 mg/m² 1 times / week multiple, intravenous dose: 49 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
50% |
88 mg/m² 1 times / week multiple, intravenous dose: 88 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PIXANTRONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
240 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose Dose: 240 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 240 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Neutropenia... Other AEs: Thrombocytopenia... Dose limiting toxicities: Neutropenia (grade 4, 40%) Other AEs:Thrombocytopenia (grade 4, 20%) Sources: |
84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Neutropenia... Other AEs: Neutropenia, Thrombopenia... Dose limiting toxicities: Neutropenia (grade 4, 50%) Other AEs:Neutropenia (grade 3, 50%) Sources: Thrombopenia (grade 4, 16.7%) Anemia (grade 3, 16.7%) Diarrhea (grade 4, 16.7%) Vomiting (grade 4, 16.7%) |
180 mg/m2 1 times / 3 weeks multiple, intravenous RP2D Dose: 180 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 180 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Neutropenia... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Thrombocytopenia | grade 4, 20% | 240 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose Dose: 240 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 240 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 4, 40% DLT |
240 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose Dose: 240 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 240 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Anemia | grade 3, 16.7% | 84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 3, 50% | 84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Diarrhea | grade 4, 16.7% | 84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Thrombopenia | grade 4, 16.7% | 84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Vomiting | grade 4, 16.7% | 84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 4, 50% DLT |
84 mg/m2 1 times / week multiple, intravenous Highest studied dose|RP2D Dose: 84 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 84 mg/m2, 1 times / week Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 3, 33.3% | 180 mg/m2 1 times / 3 weeks multiple, intravenous RP2D Dose: 180 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 180 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 5.0 |
inconclusive [IC50 18.9991 uM] | |||
likely | ||||
likely | ||||
Sources: https://www.ema.europa.eu/en/documents/assessment-report/pixuvri-epar-public-assessment-report_en.pdf Page: 22 | 39 |
moderate | |||
no | ||||
weak | ||||
weak | ||||
weak | ||||
weak | ||||
Page: 2.0 |
yes [IC50 1.8999 uM] | |||
Page: 2.0 |
yes [IC50 2.6837 uM] | |||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Topoisomerase II DNA cleavage stimulation, DNA binding activity, cytotoxicity, and physico-chemical properties of 2-aza- and 2-aza-oxide-anthracenedione derivatives. | 1995 Jul |
|
Phase I study of BBR 2778, a new aza-anthracenedione, in advanced or refractory non-Hodgkin's lymphoma. | 2001 May |
|
Pixantrone (Novuspharma). | 2003 May |
|
A comparison of the benefits of mitoxantrone and other recent therapeutic approaches in multiple sclerosis. | 2004 Apr |
|
New immunosuppressants with potential implication in multiple sclerosis. | 2004 Aug 15 |
|
Pixantrone (BBR2778): a new immunosuppressant in multiple sclerosis with a low cardiotoxicity. | 2004 Aug 15 |
|
Pixantrone (BBR2778) reduces the severity of experimental allergic encephalomyelitis. | 2004 Jun |
|
The role of pixantrone in the treatment of non-Hodgkin's lymphoma. | 2005 Aug |
|
Effects of pixantrone on immune-cell function in the course of acute rat experimental allergic encephalomyelitis. | 2005 Nov |
|
Diagnosis and management of lymphoma. | 2006 Jul |
|
EXTEND PIX301: a phase III randomized trial of pixantrone versus other chemotherapeutic agents as third-line monotherapy in patients with relapsed, aggressive non-Hodgkin's lymphoma. | 2006 Sep |
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Pixantrone can be activated by formaldehyde to generate a potent DNA adduct forming agent. | 2007 |
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A phase I/II trial of pixantrone (BBR2778), methylprednisolone, cisplatin, and cytosine arabinoside (PSHAP) in relapsed/refractory aggressive non-Hodgkin's lymphoma. | 2007 Feb |
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Compared benefit of approved and experimental immunosuppressive therapeutic approaches in multiple sclerosis. | 2007 Jun |
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Pixantrone (BBR 2778) has reduced cardiotoxic potential in mice pretreated with doxorubicin: comparative studies against doxorubicin and mitoxantrone. | 2007 Jun |
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Pixantrone: a novel aza-anthracenedione in the treatment of non-Hodgkin's lymphomas. | 2007 Oct |
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Considerations with newer regimens for indolent non-Hodgkin lymphoma. | 2008 Aug |
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Pixantrone (BBR2778) reduces the severity of experimental autoimmune myasthenia gravis in Lewis rats. | 2008 Feb 15 |
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Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones. | 2008 Feb 28 |
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Formaldehyde-activated Pixantrone is a monofunctional DNA alkylator that binds selectively to CpG and CpA doublets. | 2008 Jul |
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CE can identify small molecules that selectively target soluble oligomers of amyloid beta protein and display antifibrillogenic activity. | 2009 Apr |
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Pixantrone: a promising drug in the treatment of non-Hodgkin lymphomas. | 2009 May |
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Pixantrone maleate for non-Hodgkin's lymphoma. | 2009 Nov |
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Pixantrone for the treatment of aggressive non-Hodgkin lymphoma. | 2010 Aug |
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DNA binding by pixantrone. | 2010 Dec 7 |
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Lymphoma researchers in search of molecular targets. | 2010 Jul 21 |
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Can anthracycline therapy for pediatric malignancies be less cardiotoxic? | 2010 Nov |
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New anthracenedione derivatives with improved biological activity by virtue of stable drug-DNA adduct formation. | 2010 Oct 14 |
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Differential targeting of immune-cells by Pixantrone in experimental myasthenia gravis. | 2013 May 15 |
Patents
Sample Use Guides
The recommended dose is 50 mg/m^2 of pixantrone on day 1, 8 and 15 of each 28-day cycle for up to 6 cycles.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26660439
In separate 72-hour growth-inhibitory assays using direct cell counting, the etoposide-resistant K/VP.5 cells were 21.6-fold cross-resistant to pixantrone, yielding IC50 values of 0.04 and 0.85 uM for K562 and K/VP.5 cells, respectively.
Substance Class |
Chemical
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EMA ASSESSMENT REPORTS |
PIXUVRI (AUTHORIZED: LYMPHOMA, NON-HODGKIN)
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