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
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
Molecular Formula | C22H28N4O6 |
Molecular Weight | 444.4809 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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
Sources: https://www.medicines.org.uk/emc/medicine/10050
Curator's Comment: Mitoxantrone does not cross the blood-brain barrier to any appreciable extent.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P51784 Gene ID: 8237.0 Gene Symbol: USP11 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/23696131 |
|||
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | NOVANTRONE Approved UseMitoxantrone 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 Date1987 |
|||
Primary | NOVANTRONE Approved UseNOVANTRONE 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 Date1987 |
|||
Primary | NOVANTRONE Approved UseNOVANTRONE 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 Date1987 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
22% |
MITOXANTRONE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
DLT: Granulocytopenia... Other AEs: Thrombocytopenia, Nausea and vomiting... Dose limiting toxicities: Granulocytopenia (grade 4, 11 patient) Other AEs:Thrombocytopenia (grade 3, 11 patient) Sources: 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) |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
Disc. AE: Urinary tract infection, Leukopenia... Other AEs: Nausea, Alopecia... AEs leading to discontinuation/dose reduction: Urinary tract infection (32%) Other AEs:Leukopenia (19%) Depression (1 patient) Left ventricular dysfunction (1 patient) Bone pain (1 patient) Emesis (1 patient) Renal failure (1 patient) Nausea (76%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
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: |
unhealthy, adult n = 11 Health Status: unhealthy Condition: metastatic breast cancer Age Group: adult Sex: F Population Size: 11 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
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: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: multiple sclerosis Age Group: adult Sex: M+F Population Size: 62 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
weak [Ki 85 uM] | ||||
weak | ||||
weak | ||||
yes [IC50 3.39 uM] | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/10070941/ |
yes | |||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes | ||||
yes | ||||
yes |
PubMed
Title | Date | PubMed |
---|---|---|
A systematic overview of chemotherapy effects in acute myeloid leukaemia. | 2001 |
|
Salvage chemotherapy with mitoxantrone, fludarabine, cytarabine, and cisplatin (MIFAP) in relapsing and refractory lymphoma. | 2001 |
|
Mitoxantrone and paclitaxel combination chemotherapy in metastatic 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 |
|
Double reinforcement with fludarabine/high-dose cytarabine enhances the impact of autologous stem cell transplantation in acute myeloid leukemia patients. | 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 |
|
High-dose therapy with autologous stem cell transplantation in patients with peripheral T cell lymphomas. | 2001 Apr |
|
Immunomodulatory drugs for multiple sclerosis: a systematic review of clinical and cost effectiveness. | 2001 Apr |
|
Treatment of aggressive non-Hodgkin's lymphoma in elderly patients with thiotepa, Novantrone (mitoxantrone), vincristine, prednisone (TNOP). | 2001 Aug |
|
CMF (cyclophosphamide, methotrexate, 5-fluorouracil) versus cnf (cyclophosphamide, mitoxantrone, 5-fluorouracil) as adjuvant chemotherapy for stage II lymph-node positive breast cancer: a phase III randomized multicenter study. | 2001 Aug |
|
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 |
|
Postremission therapy in older patients with de novo acute myeloid leukemia: a randomized trial comparing mitoxantrone and intermediate-dose cytarabine with standard-dose cytarabine. | 2001 Aug 1 |
|
Resistance to topoisomerase poisons due to loss of DNA mismatch repair. | 2001 Aug 15 |
|
Multiple sclerosis treatment 2001. | 2001 Feb |
|
Docetaxel in prostate cancer. | 2001 Feb |
|
Effectiveness of interferon-alfa and mid-cycle chemotherapy added to an anthracycline-based regimen in the treatment of aggressive non-Hodgkin's lymphoma. | 2001 Jan |
|
Mitoxantrone and fludarabine in the treatment of patients with non-Hodgkin's lymphoma failing primary therapy with a doxorubicinor mitoxantrone-containing regimen. | 2001 Jan |
|
Phase II study of combination human recombinant GM-CSF with intermediate-dose cytarabine and mitoxantrone chemotherapy in patients with high-risk myelodysplastic syndromes (RAEB, RAEBT, and CMML): an Eastern Cooperative Oncology Group Study. | 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 |
|
Functional characterization of the human multidrug transporter, ABCG2, expressed in insect cells. | 2001 Jul 6 |
|
Efficacy of fludarabine, intermittent sequential high-dose cytosine arabinoside, and mitoxantrone (FIS-HAM) salvage therapy in highly resistant acute leukemias. | 2001 Jun |
|
[Chemotherapy in gastroenterologic neuroendocrine tumors]. | 2001 Jun |
|
Secondary acute myelogenous leukemia and myelodysplasia without abnormalities of chromosome 11q23 following treatment of acute leukemia with topoisomerase II-based chemotherapy. | 2001 Jun |
|
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 |
|
Results of a phase III prospective, randomised trial, comparing mitoxantrone and vinorelbine (MV) in combination with standard FAC/FEC in front-line therapy of metastatic breast cancer. | 2001 Jun |
|
Incremental net benefit in randomized clinical trials. | 2001 Jun 15 |
|
Esters of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinones with melphalan as multifunctional anticancer agents. | 2001 Jun 4 |
|
A functional assay for detection of the mitoxantrone resistance protein, MXR (ABCG2). | 2001 Jun 6 |
|
Heterogeneity of proteinkinase C activity and PKC-zeta expression in clinical breast carcinomas. | 2001 Mar |
|
Cladribine in combination with mitoxantrone and cyclophosphamide(CMC) in the treatment of heavily pre-treated patients with advanced indolent lymphoid malignancies. | 2001 Mar |
|
Pretreatment leukaemia cell drug resistance is correlated to clinical outcome in acute myeloid leukaemia. | 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 |
|
Intensive postremission chemotherapy in Taiwanese adults with acute myelogenous leukemia. | 2001 Mar-Apr |
|
Combination therapy of percutaneous mitoxantrone injection, percutaneous ethanol injection, and transcatheter arterial embolization for intrahepatic hepatocellular carcinoma and adrenal metastasis. | 2001 Mar-Apr |
|
Longitudinal effects of high-dose chemotherapy and autologous stem cell transplantation on quality of life in the treatment of metastatic breast cancer. | 2001 May |
|
Estrogen-receptor-directed neoadjuvant therapy for breast cancer: results of a randomised trial using formestane and methotrexate, mitozantrone and mitomycin C (MMM) chemotherapy. | 2001 May |
|
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 |
|
Combined action of PSC 833 (Valspodar), a novel MDR reversing agent, with mitoxantrone, etoposide and cytarabine in poor-prognosis acute myeloid leukemia. | 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 |
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Improved treatment results in high-risk pediatric acute myeloid leukemia patients after intensification with high-dose cytarabine and mitoxantrone: results of Study Acute Myeloid Leukemia-Berlin-Frankfurt-Münster 93. | 2001 May 15 |
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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 |
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9450803
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.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:06:50 GMT 2023
by
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Fri Dec 15 15:06:50 GMT 2023
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Record UNII |
BZ114NVM5P
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Record Status |
Validated (UNII)
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FDA ORPHAN DRUG |
128499
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NCI_THESAURUS |
C253
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FDA ORPHAN DRUG |
125199
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WHO-ATC |
L01DB07
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NDF-RT |
N0000000176
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NDF-RT |
N0000175609
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LIVERTOX |
NBK547931
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WHO-VATC |
QL01DB07
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FDA ORPHAN DRUG |
96696
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Code System | Code | Type | Description | ||
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D008942
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4922
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BZ114NVM5P
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BZ114NVM5P
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CHEMBL58
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MITOXANTRONE
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100000092117
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65271-80-9
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4212
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DTXSID4046947
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7005
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50729
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279836
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C62050
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DB01204
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SUB09012MIG
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7242
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PRIMARY | |||
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Mitoxantrone
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m7572
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PRIMARY | Merck Index | ||
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1821
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