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Details

Stereochemistry ACHIRAL
Molecular Formula C22H28N4O6
Molecular Weight 444.4809
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MITOXANTRONE

SMILES

OCCNCCNC1=CC=C(NCCNCCO)C2=C1C(=O)C3=C(C2=O)C(O)=CC=C3O

InChI

InChIKey=KKZJGLLVHKMTCM-UHFFFAOYSA-N
InChI=1S/C22H28N4O6/c27-11-9-23-5-7-25-13-1-2-14(26-8-6-24-10-12-28)18-17(13)21(31)19-15(29)3-4-16(30)20(19)22(18)32/h1-4,23-30H,5-12H2

HIDE SMILES / InChI

Description

Mitoxantrone (NOVANTRONE) is a synthetic antineoplastic anthracenedione. Mitoxantrone, a DNA-reactive agent that intercalates into deoxyribonucleic acid (DNA) through hydrogen bonding, causes crosslinks and strand breaks. Mitoxantrone also interferes with ribonucleic acid (RNA) and is a potent inhibitor of topoisomerase II, an enzyme responsible for uncoiling and repairing damaged DNA. It has a cytocidal effect on both proliferating and nonproliferating cultured human cells, suggesting lack of cell cycle phase specificity. Mitoxantrone has been shown in vitro to inhibit B cell, T cell, and macrophage proliferation and impair antigen pre sentation, as well as the secretion of interferon gamma, TNFα, and IL-2. NOVANTRONE is indicated for reducing neurologic disability and/or the frequency of clinical relapses in patients with secondary (chronic) progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis (i.e., patients whose neurologic status is significantly abnormal between relapses). NOVANTRONE in combination with corticosteroids is indicated as initial chemotherapy for the treatment of patients with pain related to advanced hormone-refractory prostate cancer. NOVANTRONE in combination with other approved drug(s) is indicated in the initial therapy of acute nonlymphocytic leukemia (ANLL) in adults. This category includes myelogenous, promyelocytic, monocytic, and erythroid acute leukemias.

CNS Activity

CNS Non-penetrant
1050
Curator's Comment: Mitoxantrone does not cross the blood-brain barrier to any appreciable extent.

Originator

Approval Year

1987
113
Targets

Targets

Primary TargetPharmacologyConditionPotency
Ubiquitin carboxyl-terminal hydrolase 11
2
Target ID: P51784
Gene ID: 8237.0
Gene Symbol: USP11
Target Organism: Homo sapiens (Human)
Inhibitor
8228
Inhibitor
8228
Inhibitor
8228
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8360
NOVANTRONE

Approved Use

Mitoxantrone injection USP (concentrate) is indicated for reducing neurologic disability and/or the frequency of clinical relapses in patients with secondary (chronic) progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis (i.e., patients whose neurologic status is significantly abnormal between relapses). Mitoxantrone injection USP (concentrate) is not indicated in the treatment of patients with primary progressive multiple sclerosis. The clinical patterns of multiple sclerosis in the studies were characterized as follows: secondary progressive and progressive relapsing disease were characterized by gradual increasing disability with or without superimposed clinical relapses, and worsening relapsing-remitting disease was characterized by clinical relapses resulting in a step-wise worsening of disability. Mitoxantrone injection USP (concentrate) in combination with corticosteroids is indicated as initial chemotherapy for the treatment of patients with pain related to advanced hormone-refractory prostate cancer. Mitoxantrone injection USP (concentrate) in combination with other approved drug(s) is indicated in the initial therapy of acute nonlymphocytic leukemia (ANLL) in adults. This category includes myelogenous, promyelocytic, monocytic, and erythroid acute leukemias.

Launch Date

5.6721598E11
Primary
Approved
8360
NOVANTRONE

Approved Use

NOVANTRONE is indicated for reducing neurologic disability and/or the frequency of clinical relapses in patients with secondary (chronic) progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis (i.e., patients whose neurologic status is significantly abnormal between relapses). NOVANTRONE is not indicated in the treatment of patients with primary progressive multiple sclerosis. The clinical patterns of multiple sclerosis in the studies were characterized as follows: secondary progressive and progressive relapsing disease were characterized by gradual increasing disability with or without superimposed clinical relapses, and worsening relapsing-remitting disease was characterized by clinical relapses resulting in a step-wise worsening of disability. NOVANTRONE in combination with corticosteroids is indicated as initial chemotherapy for the treatment of patients with pain related to advanced hormone-refractory prostate cancer. NOVANTRONE in combination with other approved drug(s) is indicated in the initial therapy of acute nonlymphocytic leukemia (ANLL) in adults. This category includes myelogenous, promyelocytic, monocytic, and erythroid acute leukemias.

Launch Date

5.6721598E11
Primary
Approved
8360
NOVANTRONE

Approved Use

NOVANTRONE is indicated for reducing neurologic disability and/or the frequency of clinical relapses in patients with secondary (chronic) progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis (i.e., patients whose neurologic status is significantly abnormal between relapses). NOVANTRONE is not indicated in the treatment of patients with primary progressive multiple sclerosis. The clinical patterns of multiple sclerosis in the studies were characterized as follows: secondary progressive and progressive relapsing disease were characterized by gradual increasing disability with or without superimposed clinical relapses, and worsening relapsing-remitting disease was characterized by clinical relapses resulting in a step-wise worsening of disability. NOVANTRONE in combination with corticosteroids is indicated as initial chemotherapy for the treatment of patients with pain related to advanced hormone-refractory prostate cancer. NOVANTRONE in combination with other approved drug(s) is indicated in the initial therapy of acute nonlymphocytic leukemia (ANLL) in adults. This category includes myelogenous, promyelocytic, monocytic, and erythroid acute leukemias.

Launch Date

5.6721598E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6.429 mg/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/8402672
90 mg/m² single, intravenous
dose: 90 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
MITOXANTRONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5.195 mg × h/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/8402672
90 mg/m² single, intravenous
dose: 90 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
MITOXANTRONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1922 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/8410125
40 mg/m² single, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
MITOXANTRONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1.26 μg × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/1558794
12 mg/m² 1 times / 3 weeks multiple, intravenous
dose: 12 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
MITOXANTRONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
37.1 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/8410125
40 mg/m² single, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
MITOXANTRONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
19.83 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/1558794
12 mg/m² 1 times / 3 weeks multiple, intravenous
dose: 12 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
MITOXANTRONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
22%
DRUG LABEL
https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/fcb8ef8a-f770-4416-8fc5-fa01d98c8eee/spl-doc?hl=MITOXANTRONE
MITOXANTRONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
DLT: Granulocytopenia...
Other AEs: Thrombocytopenia, Nausea and vomiting...
Dose limiting toxicities:
Granulocytopenia (grade 4, 11 patient)
Other AEs:
Thrombocytopenia (grade 3, 11 patient)
Nausea and vomiting (grade 1-2, 9 patients)
Stomatitis (grade 1-3, 6 patients)
Alopecia (grade 1-3, 5 patients)
Diarrhea (grade 1-2, 3 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Disc. AE: Urinary tract infection, Leukopenia...
Other AEs: Nausea, Alopecia...
AEs leading to
discontinuation/dose reduction:
Urinary tract infection (32%)
Leukopenia (19%)
Depression (1 patient)
Left ventricular dysfunction (1 patient)
Bone pain (1 patient)
Emesis (1 patient)
Renal failure (1 patient)
Other AEs:
Nausea (76%)
Alopecia (61%)
Menstrual disorder (61%)
Amenorrhea (43%)
Upper respiratory tract infection (53%)
Stomatitis (19%)
Arrhythmia (18%)
Diarrhea (16%)
Urine abnormal (11%)
ECG abnormal (11%)
Constipation (10%)
Back pain (8%)
Sinusitis (6%)
Headache (6%)
Gamma-GT increased (15%)
SGOT increased (8%)
Granulocytopenia (6%)
Anemia (6%)
SGPT increased (5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Diarrhea grade 1-2, 3 patients
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
Nausea and vomiting grade 1-2, 9 patients
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
Alopecia grade 1-3, 5 patients
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
Stomatitis grade 1-3, 6 patients
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
Thrombocytopenia grade 3, 11 patient
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
Granulocytopenia grade 4, 11 patient
DLT
39 mg/m2 1 times / 4 weeks multiple, intravenous
Highest studied dose
Dose: 39 mg/m2, 1 times / 4 weeks
Route: intravenous
Route: multiple
Dose: 39 mg/m2, 1 times / 4 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
unhealthy, adult
n = 11
Health Status: unhealthy
Condition: metastatic breast cancer
Age Group: adult
Sex: F
Population Size: 11
Sources:
https://pubmed.ncbi.nlm.nih.gov/10445421/
Bone pain 1 patient
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Depression 1 patient
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Emesis 1 patient
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Left ventricular dysfunction 1 patient
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Renal failure 1 patient
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Constipation 10%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
ECG abnormal 11%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Urine abnormal 11%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Gamma-GT increased 15%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Diarrhea 16%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Arrhythmia 18%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Stomatitis 19%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Leukopenia 19%
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Urinary tract infection 32%
Disc. AE
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Amenorrhea 43%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
SGPT increased 5%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Upper respiratory tract infection 53%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Anemia 6%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Granulocytopenia 6%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Headache 6%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Sinusitis 6%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Alopecia 61%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Menstrual disorder 61%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Nausea 76%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Back pain 8%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
SGOT increased 8%
12 mg/m2 1 times / 3 months multiple, intravenous
Recommended
Dose: 12 mg/m2, 1 times / 3 months
Route: intravenous
Route: multiple
Dose: 12 mg/m2, 1 times / 3 months
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: multiple sclerosis
Age Group: adult
Sex: M+F
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019297s030s031lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1579
inhibitor
1752
inhibitor
1837

OverviewOther

Other InhibitorOther SubstrateOther Inducer
OCT1
506

CYP1A2
1509

CYP2A6
704

CYP2C19
1463

CYP2E1
876

OATP1B3
700

OATP1B1
781
OATP1B1
403

BCRP
555

MRP1
106

P-gp
1527
BCRP
75
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1673
 no
CYP2A6
736
 no
CYP2C19
1537
 no
CYP2C9
1803
 no
CYP2D6
1875
 no
CYP2E1
964
 no
CYP3A4
1909
 no
OCT1
523
 weak [Ki 85 uM]
CYP2E1
964
 weak
OATP1B1
796
 weak
OATP1B3
709
 yes [IC50 3.39 uM]
BCRP
765
 yes
MRP2
459
 yes
MRP4
237
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
555
 yes
MRP1
106
 yes
OATP1B1
403
 yes
P-gp
1527
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:50729
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:50729
ChemicalBook
CB1246423
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1246423
MolPort
MolPort-003-849-239
https://www.molport.com/shop/molecule-link/MolPort-003-849-239
ZINC
ZINC000003794794
http://zinc15.docking.org/substances/ZINC000003794794
eMolecules
742146
https://www.emolecules.com/cgi-bin/more?vid=742146
PubMed

PubMed

TitleDatePubMed
Toxicity of a particulate formulation for the intraperitoneal application of mitoxantrone.
1999 Apr 15
Sinus bradycardia due to mitoxantrone.
2000 Apr
Sinus bradycardia secondary to mitoxantrone.
2000 Jun
Treatment of patients with recurrent and primary refractory acute myelogenous leukemia using mitoxantrone and intermediate-dose cytarabine: a pharmacologically based regimen.
2000 May 1
Salvage chemotherapy with mitoxantrone, fludarabine, cytarabine, and cisplatin (MIFAP) in relapsing and refractory lymphoma.
2001
Progressing prostate carcinoma.
2001
Applications of microarray technology in breast cancer research.
2001
5'-deoxy-5-fluorouridine, medroxyprogestrone acetate and mitoxantrone hydrochloride for advanced or recurrent breast cancer.
2001
HER-2 expression is a prognostic factor in patients with metastatic breast cancer treated with a combination of high-dose cyclophosphamide, mitoxantrone, paclitaxel and autologous blood stem cell support.
2001 Apr
Acute promyelocytic leukemia with additional chromosome abnormalities in a renal transplant case.
2001 Apr
High remission rate in acute myeloblastic leukemia with only two days of chemotherapy.
2001 Apr
Immunomodulatory drugs for multiple sclerosis: a systematic review of clinical and cost effectiveness.
2001 Apr
Combination chemotherapy with mitoxantrone, methotrexate, and mitomycin (MMM regimen) in malignant pleural mesothelioma: a phase II study.
2001 Apr
The DNA helicase activity of yeast Sgs1p is essential for normal lifespan but not for resistance to topoisomerase inhibitors.
2001 Aug
TRAIL/Apo2L ligand selectively induces apoptosis and overcomes drug resistance in multiple myeloma: therapeutic applications.
2001 Aug 1
Resistance to topoisomerase poisons due to loss of DNA mismatch repair.
2001 Aug 15
Docetaxel in prostate cancer.
2001 Feb
Induction therapy of adult acute lymphocytic leukemia without the use of vincristine or prednisone.
2001 Feb
Human CYP1B1 and anticancer agent metabolism: mechanism for tumor-specific drug inactivation?
2001 Feb
Phase II randomized trial comparing vinorelbine versus vinorelbine plus cisplatin in patients with recurrent salivary gland malignancies.
2001 Feb 1
Secondary leukemia after adjuvant chemotherapy for breast cancer.
2001 Feb 15
Acute heart failure after allogeneic blood stem cell transplantation due to massive myocardial infiltration by cytotoxic T cells of donor origin.
2001 Jan
Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cells.
2001 Jan
The role of laparoscopy in second-look evaluations for ovarian cancer.
2001 Jan
DNA-interactive anticancer aza-anthrapyrazoles: biophysical and biochemical studies relevant to the mechanism of action.
2001 Jan
Chemotherapy and marrow transplantation for congenital leukaemia.
2001 Jan
Detection of human herpesvirus 6 and JC virus in progressive multifocal leukoencephalopathy complicating follicular lymphoma.
2001 Jul
Radiation therapy after a partial response to CHOP chemotherapy for aggressive lymphomas.
2001 Jul 1
Resistance to mitoxantrone in multidrug-resistant MCF7 breast cancer cells: evaluation of mitoxantrone transport and the role of multidrug resistance protein family proteins.
2001 Jul 15
The prognostic value of cytogenetics is reinforced by the kind of induction/consolidation therapy in influencing the outcome of acute myeloid leukemia--analysis of 848 patients.
2001 Jun
Magnetic resonance imaging detection of avascular necrosis of the bone in children receiving intensive prednisone therapy for acute lymphoblastic leukemia or non-Hodgkin lymphoma.
2001 Jun
Incremental net benefit in randomized clinical trials.
2001 Jun 15
A functional assay for detection of the mitoxantrone resistance protein, MXR (ABCG2).
2001 Jun 6
Cladribine in combination with mitoxantrone and cyclophosphamide(CMC) in the treatment of heavily pre-treated patients with advanced indolent lymphoid malignancies.
2001 Mar
Cemp, a mitoxantrone containing combination, in the treatment of intermediate and high grade non-hodgkin's lymphoma: an effective and non toxic therapeutic alternative for adult and elderly patients.
2001 Mar
Selection and characterization of a high-activity ribozyme directed against the antineoplastic drug resistance-associated ABC transporter BCRP/MXR/ABCG2.
2001 Mar
Treatment of elderly patients with intermediate- and high-grade non-Hodgkin's lymphoma: a retrospective population-based study.
2001 Mar
Ifosfamide and mitoxantrone in the treatment of recurrent and/or metastatic squamous cell carcinoma of the head and neck.
2001 Mar
Combination therapy of percutaneous mitoxantrone injection, percutaneous ethanol injection, and transcatheter arterial embolization for intrahepatic hepatocellular carcinoma and adrenal metastasis.
2001 Mar-Apr
Phase I study of BBR 2778, a new aza-anthracenedione, in advanced or refractory non-Hodgkin's lymphoma.
2001 May
Cardiac metabolism and function in patients with multiple sclerosis: a combined 31P-MR-spectroscopy and MRI study.
2001 May
Neoadjuvant high dose chemotherapy plus peripheral blood progenitor cells in inflammatory breast cancer: a multicenter phase II pilot study.
2001 May
In vitro induction of apoptosis of neoplastic cells in low-grade non-Hodgkin's lymphomas using combinations of established cytotoxic drugs with bendamustine.
2001 May
Phase II study of docetaxel, estramustine, and low-dose hydrocortisone in men with hormone-refractory prostate cancer: a final report of CALGB 9780. Cancer and Leukemia Group B.
2001 May 1
Cytosine methylation enhances mitoxantrone-DNA adduct formation at CpG dinucleotides.
2001 May 11
Mitoxantrone is superior to doxorubicin in a multiagent weekly regimen for patients older than 60 with high-grade lymphoma: results of a BNLI randomized trial of PAdriaCEBO versus PMitCEBO.
2001 May 15
Patents

Patents

04278689
2
JP2002541200A
14
JP2002541233A
397
JP2004523497A
81
JP2004534728A
78
JP2006516548A
17
JP2007508039A
113
JP2009526755A
442
JP2011510954A
142
JP2011525180A
178
JP4527401B2
32
JP4701159B2
70
JP4758474B2
86
JP4785252B2
2
JP4818917B2
31
JP4851943B2
41
JPH06321927A
2

Sample Use Guides

In Vivo Use Guide
The recommended dosage of NOVANTRONE (Mitoxantrone) is 12 mg/m2 given as a short (approximately 5 to 15 minutes) intravenous infusion every 3 months.
Route of Administration: Intravenous
In Vitro Use Guide
Treatment of B-CLL cells for 48 h with mitoxantrone (0.5 ug/ml) induced a decrease in cell viability as determined by MTT assay.
Name Type Language
MITOXANTRONE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
mitoxantrone [INN]
Common Name English
NSC-279836
Code English
MITOXANTRONE [IARC]
Common Name English
Mitoxantrone [WHO-DD]
Common Name English
MITOXANTRONE [VANDF]
Common Name English
MISOSTOL
Brand Name English
MITOXANTRONE [MI]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 128499
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
NCI_THESAURUS C253
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
FDA ORPHAN DRUG 125199
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
WHO-ATC L01DB07
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
NDF-RT N0000000176
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
NDF-RT N0000175609
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
LIVERTOX NBK547931
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
WHO-VATC QL01DB07
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
FDA ORPHAN DRUG 96696
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
Code System Code Type Description
MESH
D008942
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
INN
4922
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
FDA UNII
BZ114NVM5P
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
DAILYMED
BZ114NVM5P
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
ChEMBL
CHEMBL58
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
WIKIPEDIA
MITOXANTRONE
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
SMS_ID
100000092117
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
CAS
65271-80-9
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
PUBCHEM
4212
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
EPA CompTox
DTXSID4046947
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
RXCUI
7005
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY RxNorm
CHEBI
50729
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
NSC
279836
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
NCI_THESAURUS
C62050
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
DRUG BANK
DB01204
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
EVMPD
SUB09012MIG
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
IUPHAR
7242
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
LACTMED
Mitoxantrone
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
MERCK INDEX
M7572
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY Merck Index
DRUG CENTRAL
1821
Created by admin on Wed Jul 05 22:38:45 UTC 2023 , Edited by admin on Wed Jul 05 22:38:45 UTC 2023
PRIMARY
ACTIVE MOIETY
Structure of MITOXANTRONE
METABOLITE (PARENT)
Structure of MITOXANTRONE GLUCURONIDE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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