deferoxamine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 ยตM/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

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 223.34 23.50 50 2121 5515 56284381
Laryngitis fungal 87.63 23.50 13 2158 134 56289762
Sickle cell anaemia with crisis 73.01 23.50 20 2151 5008 56284888
Mucormycosis 64.29 23.50 16 2155 2758 56287138
Bacterial sepsis 50.21 23.50 14 2157 3735 56286161
Iron overload 42.15 23.50 9 2162 789 56289107
Liver iron concentration increased 41.04 23.50 5 2166 8 56289888
Haemoglobin decreased 35.38 23.50 34 2137 134103 56155793
Haemosiderosis 33.69 23.50 6 2165 203 56289693
Blood creatinine increased 30.45 23.50 25 2146 80166 56209730
Infective chondritis 30.22 23.50 4 2167 16 56289880
Transplant failure 26.60 23.50 7 2164 1502 56288394
Maculopathy 24.49 23.50 7 2164 2037 56287859
Caesarean section 24.20 23.50 12 2159 16079 56273817
Injection site abscess 23.84 23.50 6 2165 1080 56288816

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 181.67 23.28 47 1975 5745 31689577
Blood iron increased 37.36 23.28 9 2013 815 31694507
Spinal X-ray abnormal 34.64 23.28 4 2018 0 31695322
Iron overload 33.92 23.28 9 2013 1202 31694120
Liver iron concentration increased 30.98 23.28 4 2018 6 31695316
Visual acuity reduced 29.74 23.28 16 2006 15327 31679995
Myelodysplastic syndrome 28.96 23.28 17 2005 19234 31676088
Blood creatinine increased 27.44 23.28 31 1991 89047 31606275

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 289.51 21.18 70 3227 8935 70916212
Fundoscopy abnormal 140.26 21.18 18 3279 41 70925106
Laryngitis fungal 78.26 21.18 12 3285 128 70925019
Mucormycosis 72.28 21.18 23 3274 7991 70917156
Spinal X-ray abnormal 52.21 21.18 7 3290 25 70925122
Sickle cell anaemia with crisis 49.17 21.18 16 3281 5962 70919185
Iron overload 48.71 21.18 12 3285 1641 70923506
Liver iron concentration increased 48.37 21.18 6 3291 9 70925138
Visual acuity reduced 47.39 21.18 24 3273 27906 70897241
Haemoglobin decreased 40.97 21.18 49 3248 205110 70720037
Myelodysplastic syndrome 37.55 21.18 21 3276 29764 70895383
Agranulocytosis 36.62 21.18 23 3274 40275 70884872
Maculopathy 34.20 21.18 10 3287 2616 70922531
Bacterial sepsis 34.17 21.18 13 3284 7634 70917513
Haemosiderosis 33.77 21.18 7 3290 440 70924707
Blood creatinine increased 31.59 21.18 36 3261 142965 70782182
Blood iron increased 30.32 21.18 8 3289 1436 70923711
Infective chondritis 27.23 21.18 4 3293 31 70925116
Haemochromatosis 26.28 21.18 7 3290 1304 70923843
Optic neuropathy 23.96 21.18 8 3289 3225 70921922
Retinopathy 23.32 21.18 8 3289 3498 70921649
Foetal distress syndrome 22.21 21.18 5 3292 463 70924684
Thalassaemia beta 21.56 21.18 3 3294 15 70925132

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
CHEBI has role CHEBI:26672 siderochromes
CHEBI has role CHEBI:38157 iron chelating agents
CHEBI has role CHEBI:173084 ferroptosis inhibitors
MeSH PA D002614 Chelating Agents
MeSH PA D007502 Iron Chelating Agents
MeSH PA D064449 Sequestering Agents
MeSH PA D017262 Siderophores
CHEBI has role CHEBI:50247 antidotes

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Desferal HUMAN PRESCRIPTION DRUG LABEL 1 0078-0467 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR NDA 31 sections
Desferal HUMAN PRESCRIPTION DRUG LABEL 1 0078-0467 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR NDA 31 sections
Deferoxamine Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-2336 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 19 sections
Deferoxamine Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-2337 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 19 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 47781-623 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 12 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 47781-623 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 12 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 47781-624 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 12 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 47781-624 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 12 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 11 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-6237 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 11 sections
Deferoxamine mesylate HUMAN PRESCRIPTION DRUG LABEL 1 60505-6238 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 12 sections
Deferoxamine Human Prescription Drug Label 1 63323-597 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 95 mg INTRAVENOUS ANDA 17 sections
Deferoxamine Human Prescription Drug Label 1 63323-599 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 95 mg INTRAVENOUS ANDA 17 sections
Deferoxamine mesylate Human Prescription Drug Label 1 68083-172 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR ANDA 11 sections
Deferoxamine mesylate Human Prescription Drug Label 1 68083-173 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2 g INTRAMUSCULAR ANDA 11 sections