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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
Structure of VOSAROXIN

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

HIDE SMILES / InChI

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

Description
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

Curator's Comment: Radiolabeling experiments in mice indicate that vosaroxin crosses the blood–brain barrier

Originator

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

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1916 ng/mL
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
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
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
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
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
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
31245 ng × h/mL
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
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
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
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
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
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
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
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
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
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
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
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

T1/2

ValueDoseCo-administeredAnalytePopulation
25.13 h
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
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
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
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
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
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
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
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
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
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
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
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

Funbound

ValueDoseCo-administeredAnalytePopulation
28%
VOSAROXIN serum
Homo sapiens
Doses

Doses

DosePopulationAdverse 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...
Other AEs:
Neutropenia (grade 3, 16.7%)
Sources:
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%)
Constipation (grade 3, 9%)
Nausea (grade 3, 18%)
Vomiting (grade 3, 9%)
Sepsis (grade 3, 9%)
Dyspnea (grade 3, 18%)
Sources:
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%)
Pleural effusion (grade 3, 25%)
Sources:
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%)
Neutropenia (grade 3-4, 50%)
Other AEs:
Influenza (grade 3, 12.5%)
Pneumonia (grade 3, 12.5%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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:
PubMed

PubMed

TitleDatePubMed
Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 2.
2004 Apr 8
Patents

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
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 Mon Mar 31 18:12:14 GMT 2025
Edited
by admin
on Mon Mar 31 18:12:14 GMT 2025
Record UNII
K6A90IIZ19
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID, 1,4-DIHYDRO-7-((3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL)-4-OXO-1-(2-THIAZOLYL)-
Preferred Name English
VOSAROXIN
INN   MART.   USAN   WHO-DD  
INN   USAN  
Official Name English
VOSAROXIN [MART.]
Common Name English
SNS-595
Code English
Vosaroxin [WHO-DD]
Common Name English
(+)-7-((3S,4S)-3-METHOXY-4-(METHYLAMINO)PYRROLIDIN-1-YL)-4-OXO-1-(THIAZOL-2-YL)-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID
Systematic Name English
VORELOXIN
Common Name English
VOSAROXIN [USAN]
Common Name English
vosaroxin [INN]
Common Name English
AG-7352
Code English
SPC-595
Code English
Classification Tree Code System Code
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
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
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
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
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
Code System Code Type Description
EPA CompTox
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
PRIMARY
DRUG BANK
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
PRIMARY
PUBCHEM
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
PRIMARY
WIKIPEDIA
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
PRIMARY
ChEMBL
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
PRIMARY
EVMPD
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
PRIMARY
SMS_ID
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
PRIMARY
USAN
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
PRIMARY
MESH
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
PRIMARY
CAS
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
PRIMARY
INN
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
PRIMARY
FDA UNII
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
PRIMARY
NCI_THESAURUS
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
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY