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mitoxantrone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antineoplastics; anthraquinone derivatives	1821	65271-80-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: mitoxantrone mitoxantrone hydrochloride dihydroxyanthraquinone mitoxanthrone mitozantrone nimitoxantron mitoxantrone dihydrochloride mitoxantrone HCl	An anthracenedione-derived antineoplastic agent. Molecular weight: 444.49 Formula: C22H28N4O6 CLOGP: 2.24 LIPINSKI: 1 HAC: 10 HDO: 8 TPSA: 163.18 ALOGS: -2.78 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

mitoxantrone
mitoxantrone hydrochloride
dihydroxyanthraquinone
mitoxanthrone
mitozantrone
nimitoxantron
mitoxantrone dihydrochloride
mitoxantrone HCl

An anthracenedione-derived antineoplastic agent.

Molecular weight: 444.49
Formula: C22H28N4O6
CLOGP: 2.24
LIPINSKI: 1
HAC: 10
HDO: 8
TPSA: 163.18
ALOGS: -2.78
ROTB: 12

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
CL (Clearance)	7.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	7 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	53 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	2.59 mg/mL	Bocci G, Oprea TI, Benet LZ
Vd (Volume of distribution)	12 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.78 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.25 %	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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Approvals:

Date	Agency	Company	Orphan
Dec. 23, 1987	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	361.51	25.39	194	6203	118255	63364370
Acute myeloid leukaemia	252.34	25.39	86	6311	17061	63465564
Myelodysplastic syndrome	174.30	25.39	65	6332	16689	63465936
Pancytopenia	145.37	25.39	101	6296	96832	63385793
Sepsis	132.21	25.39	115	6282	153008	63329617
Second primary malignancy	125.22	25.39	42	6355	7911	63474714
Acute promyelocytic leukaemia	103.78	25.39	23	6374	904	63481721
Thrombocytopenia	98.35	25.39	97	6300	151060	63331565
Neutropenia	97.00	25.39	103	6294	174902	63307723
Leukaemia recurrent	90.26	25.39	22	6375	1316	63481309

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	387.97	20.96	280	7135	136569	34812947
Myelodysplastic syndrome	171.67	20.96	83	7332	19125	34930391
Acute myeloid leukaemia	145.51	20.96	73	7342	18197	34931319
Neutropenia	119.40	20.96	156	7259	156622	34792894
Septic shock	113.46	20.96	105	7310	71729	34877787
Bronchopulmonary aspergillosis	83.88	20.96	47	7368	14612	34934904
Mucormycosis	82.67	20.96	35	7380	5907	34943609
Bone marrow failure	82.54	20.96	60	7355	29193	34920323
Second primary malignancy	73.18	20.96	35	7380	7851	34941665
Fungal infection	69.85	20.96	43	7372	15892	34933624

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	616.32	20.71	399	11562	230600	79501827
Acute myeloid leukaemia	377.15	20.71	150	11811	30735	79701692
Myelodysplastic syndrome	338.32	20.71	138	11823	30163	79702264
Second primary malignancy	193.69	20.71	75	11886	14275	79718152
Neutropenia	184.47	20.71	221	11740	287489	79444938
Bone marrow failure	154.64	20.71	96	11865	51011	79681416
Sepsis	130.12	20.71	180	11781	269248	79463179
Leukaemia recurrent	125.04	20.71	36	11925	2738	79729689
Thrombocytopenia	124.78	20.71	175	11786	265084	79467343
Septic shock	121.87	20.71	119	11842	122682	79609745

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01DB07	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS CYTOTOXIC ANTIBIOTICS AND RELATED SUBSTANCES Anthracyclines and related substances
CHEBI has role	CHEBI:23240	chromophores
CHEBI has role	CHEBI:37958	dyes
CHEBI has role	CHEBI:76924	plant metabolites
CHEBI has role	CHEBI:35610	antineoplastic agents
FDA EPC	N0000175609	Topoisomerase Inhibitor
FDA MoA	N0000000176	Topoisomerase Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D002491	Central Nervous System Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Acute myeloid leukemia, disease	indication	91861009
Relapsing remitting multiple sclerosis	indication	426373005	DOID:2378
Metastatic Prostate Carcinoma	indication
Follicular non-Hodgkin's lymphoma	off-label use	308121000
Metastatic Breast Carcinoma	off-label use
Progressive Diffuse Large B-Cell Lymphoma	off-label use
Mycosis	contraindication	3218000	DOID:1564
Viral disease	contraindication	34014006	DOID:934
Chronic heart failure	contraindication	48447003
Hepatic failure	contraindication	59927004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.37	acidic
pKa2	10.7	acidic
pKa3	9.13	Basic
pKa4	8.52	Basic
pKa5	4.01	Basic
pKa6	1.49	Basic

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Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
DNA topoisomerase 2-alpha	Enzyme	P11388	TOP2A_HUMAN	INHIBITOR	IC90	5.96	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.84	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.31	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.73	DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.74	DRUG MATRIX
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	7.11	DRUG MATRIX
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	7.05	DRUG MATRIX
Canalicular multispecific organic anion transporter 1	Transporter	Q92887	MRP2_HUMAN				WOMBAT-PK
Multidrug resistance-associated protein 1	Transporter	P33527	MRP1_HUMAN		IC50	6.29	WOMBAT-PK
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		Kact	5.16	WOMBAT-PK

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External reference:

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ID	Source
MIX	PDB_CHEM_ID
002676	NDDF
004828	NDDF
108791001	SNOMEDCT_US
203129	RXNORM
386913001	SNOMEDCT_US
4019527	VANDF
4019842	VUID
4019842	VANDF
412249002	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
mitoXANTRONE	HUMAN PRESCRIPTION DRUG LABEL	1	0703-4680	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	24 sections
mitoXANTRONE	HUMAN PRESCRIPTION DRUG LABEL	1	0703-4680	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	24 sections
mitoXANTRONE	HUMAN PRESCRIPTION DRUG LABEL	1	0703-4685	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	24 sections
mitoXANTRONE	HUMAN PRESCRIPTION DRUG LABEL	1	0703-4685	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	24 sections
mitoXANTRONE	HUMAN PRESCRIPTION DRUG LABEL	1	0703-4686	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	24 sections
mitoXANTRONE	HUMAN PRESCRIPTION DRUG LABEL	1	0703-4686	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	24 sections
Mitoxantrone	HUMAN PRESCRIPTION DRUG LABEL	1	61703-343	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	28 sections
Mitoxantrone	HUMAN PRESCRIPTION DRUG LABEL	1	61703-343	INJECTION, SOLUTION, CONCENTRATE	2 mg	INTRAVENOUS	ANDA	28 sections
Mitoxantrone	HUMAN PRESCRIPTION DRUG LABEL	1	63323-132	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	15 sections

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