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

Stem definitionDrug idCAS RN
792 70-51-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • deferoxamine
  • deferoxamine mesylate
  • deferoxamin
  • desferrioxamine
  • desferrioxamine mesilate
  • deferoxamine mesilate
  • desferrioxamine mesylate
Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.
  • Molecular weight: 560.69
  • Formula: C25H48N6O8
  • CLOGP: -0.18
  • LIPINSKI: 3
  • HAC: 14
  • HDO: 6
  • TPSA: 205.84
  • ALOGS: -3.75
  • ROTB: 23
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 178.35 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 5 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.35 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.33 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.05 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 50 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ZAP70 50
kinase-selectivity-class AXL,CAMK2D,CDK4,EIF2AK3,EPHB4,INSR,MAP2K6,PLK1,PRKCD,PTK2,SIK2,STK33,TEK 13
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1

Approvals:

DateAgencyCompanyOrphan
April 1, 1968 FDA NOVARTIS

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
Serum ferritin increased 232.77 22.76 51 2384 7330 90618682
Laryngitis fungal 88.39 22.76 13 2422 186 90625826
Sickle cell anaemia with crisis 82.14 22.76 22 2413 7275 90618737
Mucormycosis 70.02 22.76 17 2418 3804 90622208
Bacterial sepsis 51.35 22.76 14 2421 4941 90621071
Iron overload 49.00 22.76 10 2425 1015 90624997
Haemoglobin decreased 44.63 22.76 36 2399 161920 90464092
Liver iron concentration increased 40.22 22.76 5 2430 17 90625995
Transplant failure 37.30 22.76 9 2426 1960 90624052
Haemosiderosis 35.72 22.76 6 2429 208 90625804
Blood creatinine increased 35.49 22.76 26 2409 101360 90524652
Infective chondritis 31.66 22.76 4 2431 16 90625996
Coombs positive haemolytic anaemia 30.75 22.76 6 2429 484 90625528
Haemochromatosis 28.50 22.76 6 2429 708 90625304
Caesarean section 26.68 22.76 12 2423 18565 90607447
Coombs negative haemolytic anaemia 25.82 22.76 5 2430 388 90625624
Maculopathy 25.59 22.76 7 2428 2499 90623513
Agranulocytosis 24.78 22.76 14 2421 34988 90591024
Injection site abscess 24.25 22.76 6 2429 1448 90624564
Viral haemorrhagic cystitis 24.09 22.76 6 2429 1487 90624525
Thalassaemia beta 23.75 22.76 3 2432 12 90626000

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
Serum ferritin increased 179.65 24.79 47 2228 7172 42611888
Liver iron concentration increased 39.05 24.79 5 2270 9 42619051
Iron overload 38.15 24.79 10 2265 1525 42617535
Blood iron increased 37.08 24.79 9 2266 1007 42618053
Spinal X-ray abnormal 35.36 24.79 4 2271 0 42619060
Visual acuity reduced 30.39 24.79 16 2259 17534 42601526
Blood creatinine increased 26.59 24.79 31 2244 109972 42509088

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
Serum ferritin increased 307.42 21.71 73 3701 11774 110573751
Fundoscopy abnormal 144.07 21.71 18 3756 47 110585478
Mucormycosis 81.27 21.71 25 3749 10603 110574922
Laryngitis fungal 78.31 21.71 12 3762 178 110585347
Visual acuity reduced 57.46 21.71 26 3748 32147 110553378
Liver iron concentration increased 55.30 21.71 7 3767 21 110585504
Spinal X-ray abnormal 55.06 21.71 7 3767 22 110585503
Sickle cell anaemia with crisis 54.58 21.71 18 3756 9527 110575998
Iron overload 54.39 21.71 13 3761 2138 110583387
Haemoglobin decreased 49.18 21.71 51 3723 248676 110336849
Agranulocytosis 41.51 21.71 26 3748 61734 110523791
Haemochromatosis 37.25 21.71 9 3765 1548 110583977
Maculopathy 35.84 21.71 10 3764 3017 110582508
Blood creatinine increased 35.22 21.71 37 3737 182852 110402673
Bacterial sepsis 34.16 21.71 13 3761 10413 110575112
Myelodysplastic syndrome 33.59 21.71 19 3755 37465 110548060
Blood iron increased 29.44 21.71 8 3766 2190 110583335
Infective chondritis 28.83 21.71 4 3770 28 110585497
Haemosiderosis 28.27 21.71 6 3768 578 110584947
Pyrexia 26.76 21.71 79 3695 898186 109687339
Transplant failure 25.82 21.71 9 3765 5626 110579899
Retinopathy 23.91 21.71 8 3766 4421 110581104
Optic neuropathy 23.52 21.71 8 3766 4650 110580875
Thalassaemia beta 23.24 21.71 3 3771 11 110585514
Coombs negative haemolytic anaemia 22.56 21.71 5 3769 589 110584936
Coombs positive haemolytic anaemia 22.34 21.71 6 3768 1571 110583954
Foetal distress syndrome 22.14 21.71 5 3769 642 110584883
Treatment noncompliance 22.13 21.71 19 3755 72971 110512554
Retinal degeneration 22.02 21.71 6 3768 1660 110583865

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AC01 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Iron chelating agents
FDA MoA N0000000144 Iron Chelating Activity
FDA EPC N0000175522 Iron Chelator
MeSH PA D002614 Chelating Agents
MeSH PA D007502 Iron Chelating Agents
MeSH PA D017262 Siderophores
MeSH PA D064449 Sequestering Agents
CHEBI has role CHEBI:35526 hypoglycemic agent

Related Drugs by ATC class:

V03AC Iron chelating agents 2 drugs
deferasiroxdeferiprone

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

DiseaseRelationSNOMED_IDDOID
Poisoning by iron AND/OR its compounds indication 55381001
Chronic Iron Overload indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.38 acidic
pKa2 8.99 acidic
pKa3 9.53 acidic
pKa4 13.04 acidic
pKa5 13.65 acidic
pKa6 10.56 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
Hypoxia-inducible factor 1-alpha Transcription factor EC50 4.75 CHEMBL
Deoxyhypusine hydroxylase Enzyme IC50 5.30 CHEMBL
Lysine-specific demethylase 4A Enzyme IC50 5.49 CHEMBL
Methylcytosine dioxygenase TET2 Enzyme IC50 4.34 CHEMBL

External reference:

IDSource
4019705 VUID
N0000147797 NUI
D01186 KEGG_DRUG
138-14-7 SECONDARY_CAS_RN
3131 RXNORM
4018789 VANDF
4019705 VANDF
C0011145 UMLSCUI
CHEBI:4356 CHEBI
CHEMBL556 ChEMBL_ID
CHEMBL1234 ChEMBL_ID
D003676 MESH_DESCRIPTOR_UI
DB00746 DRUGBANK_ID
1682 INN_ID
J06Y7MXW4D UNII
2973 PUBCHEM_CID
4539 MMSL
46738 MMSL
d01402 MMSL
001089 NDDF
004540 NDDF
372825006 SNOMEDCT_US
387224002 SNOMEDCT_US
70702006 SNOMEDCT_US
KTY PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Desferal HUMAN PRESCRIPTION DRUG LABEL 1 0078-0467 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR NDA 27 sections
Deferoxamine Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-2336 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 28 sections
Deferoxamine Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-2337 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 28 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 52609-4504 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 11 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 52609-4505 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 11 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-6236 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 23 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-6237 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 23 sections
Deferoxamine HUMAN PRESCRIPTION DRUG LABEL 1 63323-597 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 95 mg INTRAVENOUS ANDA 26 sections
Deferoxamine HUMAN PRESCRIPTION DRUG LABEL 1 63323-599 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 95 mg INTRAVENOUS ANDA 26 sections
Deferoxamine mesylate Human Prescription Drug Label 1 68083-172 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 22 sections
Deferoxamine mesylate Human Prescription Drug Label 1 68083-173 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 22 sections
Desferal HUMAN PRESCRIPTION DRUG LABEL 1 87081-467 INJECTION, POWDER, FOR SOLUTION 500 mg SUBCUTANEOUS NDA 1 sections