Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H19N5O4S |
Molecular Weight | 401.44 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN[C@H]1CN(C[C@@H]1OC)C2=NC3=C(C=C2)C(=O)C(=CN3C4=NC=CS4)C(O)=O
InChI
InChIKey=XZAFZXJXZHRNAQ-STQMWFEESA-N
InChI=1S/C18H19N5O4S/c1-19-12-8-22(9-13(12)27-2)14-4-3-10-15(24)11(17(25)26)7-23(16(10)21-14)18-20-5-6-28-18/h3-7,12-13,19H,8-9H2,1-2H3,(H,25,26)/t12-,13-/m0/s1
Molecular Formula | C18H19N5O4S |
Molecular Weight | 401.44 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.sunesis.com/qinprezo.phpCurator's Comment: Description was created using several sources including:
https://www.ncbi.nlm.nih.gov/pubmed/15056007
Sources: https://www.sunesis.com/qinprezo.php
Curator's Comment: Description was created using several sources including:
https://www.ncbi.nlm.nih.gov/pubmed/15056007
Vosaroxin is a small molecule and a naphthyridine analogue with antineoplastic activity. This quinolone-based topoisomerase II inhibitor is a new therapeutic for acute myeloid leukemia (AML). Being a DNA intercalating topoisomerase II inhibitor that causes the induction of apoptosis via double-strand DNA breaks vosoroxin is chemically distinct from other topoisomerase inhibitors with its stable quinolone-based core. Due to the stability of this core, vosaroxin is not associated with significant formation of toxic metabolites, free radicals, or reactive oxygen species, which are associated with off-target organ damage and cardiotoxicity. Furthermore, vosaroxin evades two common mechanisms of drug resistance, as it is not a substrate for the P-glycoprotein efflux pump and its activity is maintained in cells with p53 deletion. Vosaroxin has beeт tested in several investigator-sponsored studies, both as a single-agent and in combination with other therapies, for the treatment of AML and myelodysplastic syndromes. Both the U.S. Food and Drug Administration (FDA) and European Commission have granted orphan drug designation to vosaroxin for the treatment of AML. Additionally, vosaroxin has been granted fast track designation by the FDA for the potential treatment of relapsed or refractory AML in combination with cytarabine. Vosaroxin is an investigational drug that has not been approved for use in any jurisdiction. The trademark name QINPREZO is conditionally accepted by the FDA and the EMA as the proprietary name for the vosaroxin drug product candidate.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=27484675
Curator's Comment: Radiolabeling experiments in mice indicate that vosaroxin crosses the blood–brain barrier
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15056007
Curator's Comment: In 2003 Sunesis licensed worldwide development and commercialization rights to vosaroxin from Sumitomo Dainippon Pharma Co., Ltd. (http://www.sunesis.com/ongoing-partnerships.php)
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094255 Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=27484675 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1916 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3028 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2450 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2865 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / 3 days multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3328 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
90 mg/m² 1 times / 3 days multiple, intravenous dose: 90 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5792 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / 3 days multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4148 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
90 mg/m² 1 times / 3 days multiple, intravenous dose: 90 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
31245 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
18 mg/m² 1 times / week multiple, intravenous dose: 18 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
39450 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
14212 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
17067 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
15637 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
15983 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
903 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
228 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
848 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / 3 days multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
838 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
90 mg/m² 1 times / 3 days multiple, intravenous dose: 90 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
539 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / 3 days multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
462 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
90 mg/m² 1 times / 3 days multiple, intravenous dose: 90 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
25.13 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
18 mg/m² 1 times / week multiple, intravenous dose: 18 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
26.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
26.58 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
28.21 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
22.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
23.74 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21760592/ |
9 mg/m² 2 times / week multiple, intravenous dose: 9 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
22.51 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
27.29 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / week multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
28.27 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / 3 days multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
23.57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
90 mg/m² 1 times / 3 days multiple, intravenous dose: 90 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
23.52 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
72 mg/m² 1 times / 3 days multiple, intravenous dose: 72 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
20.41 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25403830/ |
90 mg/m² 1 times / 3 days multiple, intravenous dose: 90 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
VOSAROXIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
28% |
VOSAROXIN serum | Homo sapiens |
Doses
Dose | Population | Adverse events |
---|---|---|
90 mg/m2 3 times / 4 weeks multiple, intravenous Highest studied dose Dose: 90 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 90 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Stomatitis... Dose limiting toxicities: Stomatitis (grade 3, 80%) Sources: |
15 mg/m2 3 times / 4 weeks multiple, intravenous MTD Dose: 15 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 15 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Neutropenia... |
40 mg/m2 4 times / 4 weeks multiple, intravenous MTD Dose: 40 mg/m2, 4 times / 4 weeks Route: intravenous Route: multiple Dose: 40 mg/m2, 4 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Stomatitis... Dose limiting toxicities: Stomatitis (grade 3, 30%) Sources: |
48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 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, Constipation... Dose limiting toxicities: Neutropenia (grade 4, 63%) Other AEs:Thrombocytopenia (grade 4, 9%) Sources: Constipation (grade 3, 9%) Nausea (grade 3, 18%) Vomiting (grade 3, 9%) Sepsis (grade 3, 9%) Dyspnea (grade 3, 18%) |
72 mg/m2 3 times / 4 weeks multiple, intravenous MTD Dose: 72 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 72 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Stomatitis... Other AEs: Bowel obstruction... Dose limiting toxicities: Stomatitis (grade 3, 8.3%) Other AEs:Bowel obstruction (8.3%) Sources: |
18 mg/m2 3 times / 4 weeks multiple, intravenous Studied dose Dose: 18 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 18 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Neutropenia, Pleural effusion... Dose limiting toxicities: Neutropenia (grade 3, 50%) Sources: Pleural effusion (grade 3, 25%) |
60 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 60 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 60 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
DLT: Febrile neutropenia, Neutropenia... Other AEs: Influenza, Pneumonia... Dose limiting toxicities: Febrile neutropenia (grade 3, 12.5%) Other AEs:Neutropenia (grade 3-4, 50%) Influenza (grade 3, 12.5%) Sources: Pneumonia (grade 3, 12.5%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Stomatitis | grade 3, 80% DLT |
90 mg/m2 3 times / 4 weeks multiple, intravenous Highest studied dose Dose: 90 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 90 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 3, 16.7% | 15 mg/m2 3 times / 4 weeks multiple, intravenous MTD Dose: 15 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 15 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Stomatitis | grade 3, 30% DLT |
40 mg/m2 4 times / 4 weeks multiple, intravenous MTD Dose: 40 mg/m2, 4 times / 4 weeks Route: intravenous Route: multiple Dose: 40 mg/m2, 4 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Dyspnea | grade 3, 18% | 48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Nausea | grade 3, 18% | 48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Constipation | grade 3, 9% | 48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Sepsis | grade 3, 9% | 48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Vomiting | grade 3, 9% | 48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 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, 63% DLT |
48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Thrombocytopenia | grade 4, 9% | 48 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 48 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 48 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Bowel obstruction | 8.3% | 72 mg/m2 3 times / 4 weeks multiple, intravenous MTD Dose: 72 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 72 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Stomatitis | grade 3, 8.3% DLT |
72 mg/m2 3 times / 4 weeks multiple, intravenous MTD Dose: 72 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 72 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pleural effusion | grade 3, 25% DLT, Disc. AE |
18 mg/m2 3 times / 4 weeks multiple, intravenous Studied dose Dose: 18 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 18 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 3, 50% DLT |
18 mg/m2 3 times / 4 weeks multiple, intravenous Studied dose Dose: 18 mg/m2, 3 times / 4 weeks Route: intravenous Route: multiple Dose: 18 mg/m2, 3 times / 4 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Influenza | grade 3, 12.5% | 60 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 60 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 60 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pneumonia | grade 3, 12.5% | 60 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 60 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 60 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Febrile neutropenia | grade 3, 12.5% DLT |
60 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 60 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 60 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutropenia | grade 3-4, 50% DLT |
60 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 60 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 60 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Sample Use Guides
50 mg/m2 on Days 1 and 4 of 28 day cycle (Dose level 1), 72 mg/m2 on Days 1 and 4 of 28 day cycle (Dose level 2), 50 mg/m2 on Days 1, 4, 8 and 11 of 28 day cycle (Dose level 3), 72 mg/m2 on Days 1, 4, 8 and 11 of 28 day cycle (Dose level 4)
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20058009
Inhibition of proliferation by vosaroxin was studied in three cancer cell lines: HL-60 (acute promyelocytic leukemia), MV4-11 (AML), and CCRF-CEM (Acute lymphoblastic leukemia) using initial concentrations of voreloxin: CCRF-CEM, 1.5 uM; MV4-11, 1.0 uM; HL-60, 9 uM. Cells were seeded in opaque, clear bottom 96-well plates at 1 × 10^5/well in growth media. Voreloxin was serially diluted in growth media and added to the appropriate wells. CellTiter-Glo Luminescent Cell Viability Assay (Promega, Madison, WI) was performed as per manufacturer’s protocol, and the median of three replicate wells was used for IC50 curve generation. The average IC50 for voreloxin in the AML cell lines MV4-11 and HL-60 was 95 ± 8 nM and 884 ± 114 nM, respectively. CCRF-CEM cell line was also sensitive to voreloxin with an average IC50 of 166 ± 0.4 nM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:12:14 GMT 2025
by
admin
on
Mon Mar 31 18:12:14 GMT 2025
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Record UNII |
K6A90IIZ19
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Record Status |
Validated (UNII)
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Record Version |
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-
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FDA ORPHAN DRUG |
294509
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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EU-Orphan Drug |
EU/3/12/990
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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NCI_THESAURUS |
C259
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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WHO-ATC |
L01XX53
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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NCI_THESAURUS |
C795
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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Code System | Code | Type | Description | ||
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DTXSID50938662
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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DB11999
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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9952884
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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Vosaroxin
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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CHEMBL68117
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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SUB76117
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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100000137627
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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SS-107
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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C485113
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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175414-77-4
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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9066
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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K6A90IIZ19
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY | |||
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C95148
Created by
admin on Mon Mar 31 18:12:14 GMT 2025 , Edited by admin on Mon Mar 31 18:12:14 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |