Mitoxantrone

Topoisomerase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Mitoxantrone is an ofp drug in the Topoisomerase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1987. Its mechanism of action is classified as Topoisomerase Inhibitors. DrugCentral lists 28 molecular targets, including PIM1, CHRM2 and CHRM4. Recorded indications include Acute myeloid leukemia, disease, Metastatic Prostate Carcinoma and Relapsing remitting multiple sclerosis.

• Approval status: ofp (first approved 1987 by the FDA).
• Drug class: Topoisomerase Inhibitor.
• Mechanism of action: Topoisomerase Inhibitors.
• Molecular targets: PIM1, CHRM2, CHRM4 and CHRM1 (28 listed in DrugCentral).
• Indications: Acute myeloid leukemia, disease, Metastatic Prostate Carcinoma and Relapsing remitting multiple sclerosis.
• ATC code: L01DB07 (Anthracyclines and related substances).
• Molecular formula: C22H28N4O6; molecular weight 444.49 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Acute myeloid leukemia, disease
• Metastatic Prostate Carcinoma
• Relapsing remitting multiple sclerosis

Off-label uses (3)

• Follicular non-Hodgkin's lymphoma
• Metastatic Breast Carcinoma
• Progressive Diffuse Large B-Cell Lymphoma

Contraindications (18)

• Acute disease of cardiovascular system
• Acute infectious disease
• Anemia
• Bacterial infectious disease
• Bone marrow depression
• Breastfeeding (mother)
• Chronic heart failure
• Disease of liver
• Hepatic failure
• Left heart failure
• Leukopenia
• Mycosis
• Neutropenic disorder
• Pregnancy, function
• Radiation oncology AND/OR radiotherapy
• Seizure disorder
• Thrombocytopenic disorder
• Viral disease

Mechanism & targets

• Mechanism of action (MoA): Topoisomerase Inhibitors
• Established pharmacologic class: Topoisomerase Inhibitor

Molecular targets (28)

Target	Gene	Action	Activity
Serine/threonine-protein kinase pim-1	PIM1	unknown	IC50 7.29
Muscarinic acetylcholine receptor M2	CHRM2	unknown	Ki 7.11
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 7.05
Muscarinic acetylcholine receptor M1	CHRM1	unknown	Ki 6.74
Multidrug and toxin extrusion protein 1	SLC47A1	unknown	IC50 6.72
Multidrug resistance-associated protein 1	ABCC1	unknown	IC50 6.29
Multidrug and toxin extrusion protein 2	SLC47A2	unknown	IC50 6.28
Tyrosine-protein kinase BTK	BTK	unknown	IC50 6.00
DNA topoisomerase 2-alpha	TOP2A	inhibitor	IC90 5.96
Tyrosine-protein kinase Fyn	FYN	unknown	IC50 5.90
Multidrug resistance protein 1	ABCB1	unknown	IC50 5.84
Arachidonate 15-lipoxygenase	ALOX15	unknown	IC50 5.75
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 5.73
DNA-(apurinic or apyrimidinic site) lyase	APEX1	unknown	IC50 5.70
Receptor tyrosine-protein kinase erbB-2	ERBB2	unknown	IC50 5.69
DNA-3-methyladenine glycosylase	MPG	unknown	IC50 5.60
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	Ki 5.53
Proto-oncogene tyrosine-protein kinase ROS	ROS1	unknown	IC50 5.52
Integrase	pol	unknown	IC50 5.42
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.31

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1987-12-23	FDA	—	—	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01DB07	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › CYTOTOXIC ANTIBIOTICS AND RELATED SUBSTANCES › Anthracyclines and related substances

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Febrile neutropenia	1451.8
Acute myeloid leukaemia	542.3
Myelodysplastic syndrome	496.1
Neutropenia	400.7
Thrombocytopenia	287.0
Sepsis	262.5
Second primary malignancy	249.9
Bone marrow failure	241.5
Pancytopenia	218.9
Leukaemia recurrent	201.7
Septic shock	200.2
Bronchopulmonary aspergillosis	180.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Mitoxantrone is on its molecule page.

• Molecular formula: C₂₂H₂₈N₄O₆
• Molecular weight: 444.49 g/mol
• CAS number: —
• InChIKey: KKZJGLLVHKMTCM-UHFFFAOYSA-N
• PubChem CID: 4212

OCCNCCNC1=CC=C(NCCNCCO)C2=C1C(=O)C1=C(O)C=CC(O)=C1C2=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Mitoxantrone used for?

DrugCentral lists the following indications for Mitoxantrone: Acute myeloid leukemia, disease, Metastatic Prostate Carcinoma and Relapsing remitting multiple sclerosis.

How does Mitoxantrone work?

Mitoxantrone is classified as Topoisomerase Inhibitors; its molecular targets in DrugCentral include PIM1, CHRM2, CHRM4 and CHRM1.

When was Mitoxantrone first approved?

Mitoxantrone was first approved by the FDA in 1987.

What drug class does Mitoxantrone belong to?

Mitoxantrone is in the Topoisomerase Inhibitor class.

What is the chemical formula of Mitoxantrone?

Mitoxantrone has the molecular formula C22H28N4O6 and a molecular weight of 444.49 g/mol.

Sources

• DrugCentral drug card 1821 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1417019 — compound record and bioactivity
• PubChem CID 4212 — chemical identifiers
• DrugBank DB01204 — drug record
• FDA UNII BZ114NVM5P — substance identity
• DailyMed: FDA labels for Mitoxantrone — current prescribing information (label search)
• UniProt P11309 (PIM1) — target protein
• UniProt P08172 (CHRM2) — target protein
• UniProt P08173 (CHRM4) — target protein
• UniProt P11229 (CHRM1) — target protein
• UniProt Q96FL8 (SLC47A1) — target protein
• UniProt P33527 (ABCC1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.