dexrazoxane 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
benzodioxane derivatives 839 24584-09-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dexrazoxane
  • zinecard
  • savene
  • totect
  • dexrazoxane hydrochloride
  • dexrazoxane HCl
The (+)-enantiomorph of razoxane.
  • Molecular weight: 268.27
  • Formula: C11H16N4O4
  • CLOGP: -1.33
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 98.82
  • ALOGS: -1.41
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.50 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 11 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 42 % Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution) 0.55 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 1 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.50 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,PDK1,PDK2,PIK3CD,PRKDC,SIK2,TEK 20
kinase-selectivity-class AXL,BMX,CDK16,CDK7,CDK9,EGFR,IRAK1,MAP3K21 8
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
May 26, 1995 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 641.53 45.54 205 1816 158144 90468282
Bone marrow failure 134.11 45.54 43 1978 32178 90594248
Neutropenia 104.86 45.54 64 1957 224840 90401586
Aplastic anaemia 95.34 45.54 27 1994 13242 90613184
Off label use 90.70 45.54 116 1905 1102136 89524290
Pyomyositis 87.97 45.54 14 2007 419 90626007
Quadriparesis 57.72 45.54 13 2008 2536 90623890
Myelosuppression 52.35 45.54 25 1996 53566 90572860
Pancytopenia 50.23 45.54 32 1989 120231 90506195

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 382.32 39.41 194 2308 185509 42433324
Lymphoid tissue hypoplasia 280.67 39.41 48 2454 830 42618003
Thymus hypoplasia 274.69 39.41 47 2455 815 42618018
Disseminated aspergillosis 217.55 39.41 43 2459 1687 42617146
Clostridium difficile colitis 166.57 39.41 58 2444 21194 42597639
Fungal infection 136.14 39.41 49 2453 19673 42599160
Cytomegalovirus viraemia 132.52 39.41 41 2461 10336 42608497
Lymphopenia 124.57 39.41 47 2455 21516 42597317
Bacterial infection 116.24 39.41 48 2454 27831 42591002
Cellulitis 101.62 39.41 56 2446 61529 42557304
Off label use 95.28 39.41 148 2354 638187 41980646
Mucosal inflammation 65.54 39.41 39 2463 49335 42569498
Enterococcus test positive 65.53 39.41 16 2486 1669 42617164
Cerebral candidiasis 58.93 39.41 9 2493 72 42618761
Stomatococcal infection 56.07 39.41 10 2492 221 42618612
Aplastic anaemia 53.84 39.41 22 2480 12362 42606471
Respiratory moniliasis 47.41 39.41 9 2493 283 42618550
Product use in unapproved indication 45.61 39.41 55 2447 184401 42434432
Myelosuppression 41.13 39.41 27 2475 40434 42578399
Skin candida 40.07 39.41 9 2493 652 42618181

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 938.57 38.41 381 4108 316386 110268424
Lymphoid tissue hypoplasia 307.29 38.41 54 4435 1611 110583199
Thymus hypoplasia 299.91 38.41 53 4436 1634 110583176
Disseminated aspergillosis 254.57 38.41 49 4440 2431 110582379
Clostridium difficile colitis 200.58 38.41 73 4416 43705 110541105
Cytomegalovirus viraemia 150.29 38.41 47 4442 17717 110567093
Bone marrow failure 143.70 38.41 62 4427 57786 110527024
Lymphopenia 136.94 38.41 54 4435 40116 110544694
Aplastic anaemia 135.81 38.41 47 4442 24261 110560549
Fungal infection 131.27 38.41 56 4433 50750 110534060
Bacterial infection 129.82 38.41 54 4435 45982 110538828
Off label use 118.53 38.41 214 4275 1499971 109084839
Cellulitis 105.76 38.41 65 4424 125951 110458859
Neutropenia 96.83 38.41 96 4393 374524 110210286
Mucosal inflammation 94.71 38.41 55 4434 96086 110488724
Myelosuppression 85.12 38.41 51 4438 94289 110490521
Neutrophil count decreased 73.52 38.41 51 4438 120890 110463920
Pyomyositis 71.70 38.41 14 4475 746 110584064
Enterococcus test positive 62.72 38.41 16 4473 2888 110581922
Cerebral candidiasis 62.25 38.41 9 4480 72 110584738
Stomatococcal infection 54.56 38.41 10 4479 378 110584432
Product use in unapproved indication 52.78 38.41 77 4412 447300 110137510
Hypoalbuminaemia 49.62 38.41 24 4465 28950 110555860
Respiratory moniliasis 46.47 38.41 9 4480 459 110584351
Platelet count decreased 43.35 38.41 50 4439 230393 110354417
Hypogonadism 43.13 38.41 11 4478 1983 110582827
Tumour lysis syndrome 42.39 38.41 22 4467 30779 110554031
Quadriparesis 42.07 38.41 13 4476 4694 110580116
Platelet transfusion 39.25 38.41 11 4478 2835 110581975
Staphylococcal bacteraemia 38.49 38.41 17 4472 16671 110568139

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AF02 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Detoxifying agents for antineoplastic treatment
FDA EPC N0000180854 Cytoprotective Agent
MeSH PA D000970 Antineoplastic Agents
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D059005 Topoisomerase II Inhibitors
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:38161 chelator

Related Drugs by ATC class:

V03AF Detoxifying agents for antineoplastic treatment 10 drugs
amifostinearginineglucarpidaseleucovorinlevofolinic acidlysinemesnapaliferminrasburicasetrilaciclib

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

DiseaseRelationSNOMED_IDDOID
Extravasation Injury from Anthracycline Injection indication
Doxorubicin Induced Cardiomyopathy indication
Prevention of CMV Disease After Organ Transplant indication
Impaired renal function disorder contraindication 197663003
Non-infective meningitis contraindication 230155003
Bone marrow depression contraindication 307762000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.61 acidic
pKa2 10.22 acidic
pKa3 6.83 Basic
pKa4 2.83 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
DNA topoisomerase 2-alpha Enzyme IC50 4.40 CHEMBL
DNA topoisomerase 2-beta Enzyme IC50 4.30 CHEMBL

External reference:

IDSource
4023998 VUID
N0000189410 NUI
D03730 KEGG_DRUG
1263283-43-7 SECONDARY_CAS_RN
1294534 RXNORM
4020927 VANDF
4023998 VANDF
C0086444 UMLSCUI
CHEBI:50223 CHEBI
CHEMBL1738 ChEMBL_ID
CHEMBL1200778 ChEMBL_ID
DB00380 DRUGBANK_ID
D064730 MESH_DESCRIPTOR_UI
71384 PUBCHEM_CID
7330 IUPHAR_LIGAND_ID
6544 INN_ID
048L81261F UNII
136190 MMSL
1517 MMSL
4559 MMSL
64877 MMSL
d03841 MMSL
005011 NDDF
007168 NDDF
108825009 SNOMEDCT_US
417741009 SNOMEDCT_US
734473007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dexrazoxane HUMAN PRESCRIPTION DRUG LABEL 1 0143-9247 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 25 sections
Dexrazoxane HUMAN PRESCRIPTION DRUG LABEL 1 0143-9248 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 25 sections
Dexrazoxane Human Prescription Drug Label 1 68083-195 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 26 sections
Dexrazoxane Human Prescription Drug Label 1 68083-388 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 26 sections
Dexrazoxane Human Prescription Drug Label 1 72205-247 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 25 sections
Dexrazoxane Human Prescription Drug Label 1 72205-248 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 25 sections
Dexrazoxane HUMAN PRESCRIPTION DRUG LABEL 1 72266-101 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 26 sections
Dexrazoxane HUMAN PRESCRIPTION DRUG LABEL 1 72266-235 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 26 sections
Dexrazoxane HUMAN PRESCRIPTION DRUG LABEL 1 72611-716 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 25 sections
Dexrazoxane HUMAN PRESCRIPTION DRUG LABEL 1 72611-716 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 25 sections
Cardioxane HUMAN PRESCRIPTION DRUG LABEL 1 76310-002 INJECTION, POWDER, FOR SOLUTION 500 mg INTRAVENOUS Unapproved drug for use in drug shortage 3 sections