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dexrazoxane 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| benzodioxane derivatives | 839 | 24584-09-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The (+)-enantiomorph of razoxane.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 26, 1995 | FDA | PHARMACIA AND UPJOHN |
FDA Adverse Event Reporting System (Female)
| 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 | 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 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 | 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 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 | 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:
| Source | Code | Description |
|---|---|---|
| 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
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| DNA topoisomerase 2-alpha | Enzyme | IC50 | 4.40 | CHEMBL | |||||
| DNA topoisomerase 2-beta | Enzyme | IC50 | 4.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |