deferoxamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 792 | 70-51-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 1, 1968 | FDA | NOVARTIS |
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 |
|---|---|---|---|---|---|---|
| Serum ferritin increased | 228.42 | 22.88 | 51 | 2170 | 6131 | 63480670 |
| Laryngitis fungal | 88.90 | 22.88 | 13 | 2208 | 134 | 63486667 |
| Sickle cell anaemia with crisis | 71.43 | 22.88 | 20 | 2201 | 5983 | 63480818 |
| Mucormycosis | 70.40 | 22.88 | 17 | 2204 | 2854 | 63483947 |
| Bacterial sepsis | 50.81 | 22.88 | 14 | 2207 | 3944 | 63482857 |
| Liver iron concentration increased | 41.53 | 22.88 | 5 | 2216 | 8 | 63486793 |
| Haemoglobin decreased | 37.78 | 22.88 | 35 | 2186 | 145450 | 63341351 |
| Iron overload | 36.43 | 22.88 | 8 | 2213 | 883 | 63485918 |
| Haemosiderosis | 34.19 | 22.88 | 6 | 2215 | 206 | 63486595 |
| Infective chondritis | 30.61 | 22.88 | 4 | 2217 | 16 | 63486785 |
| Blood creatinine increased | 30.59 | 22.88 | 25 | 2196 | 87819 | 63398982 |
| Transplant failure | 26.93 | 22.88 | 7 | 2214 | 1578 | 63485223 |
| Caesarean section | 24.66 | 22.88 | 12 | 2209 | 17020 | 63469781 |
| Maculopathy | 24.47 | 22.88 | 7 | 2214 | 2255 | 63484546 |
| Injection site abscess | 23.83 | 22.88 | 6 | 2215 | 1192 | 63485609 |
| Thalassaemia beta | 23.63 | 22.88 | 3 | 2218 | 9 | 63486792 |
| Haemochromatosis | 23.14 | 22.88 | 5 | 2216 | 511 | 63486290 |
| Agranulocytosis | 22.93 | 22.88 | 13 | 2208 | 25121 | 63461680 |
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 |
|---|---|---|---|---|---|---|
| Serum ferritin increased | 173.12 | 22.21 | 45 | 2003 | 6101 | 34948782 |
| Blood iron increased | 37.47 | 22.21 | 9 | 2039 | 877 | 34954006 |
| Spinal X-ray abnormal | 34.98 | 22.21 | 4 | 2044 | 0 | 34954883 |
| Liver iron concentration increased | 31.32 | 22.21 | 4 | 2044 | 6 | 34954877 |
| Visual acuity reduced | 30.25 | 22.21 | 16 | 2032 | 16133 | 34938750 |
| Iron overload | 29.13 | 22.21 | 8 | 2040 | 1325 | 34953558 |
| Blood creatinine increased | 27.97 | 22.21 | 31 | 2017 | 94945 | 34859938 |
| Mucormycosis | 23.95 | 22.21 | 10 | 2038 | 5932 | 34948951 |
| Haemoglobin decreased | 23.52 | 22.21 | 32 | 2016 | 120740 | 34834143 |
| Myelodysplastic syndrome | 22.46 | 22.21 | 14 | 2034 | 19194 | 34935689 |
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 |
|---|---|---|---|---|---|---|
| Serum ferritin increased | 295.06 | 22.16 | 71 | 3299 | 9776 | 79731242 |
| Fundoscopy abnormal | 140.23 | 22.16 | 18 | 3352 | 47 | 79740971 |
| Mucormycosis | 81.61 | 22.16 | 25 | 3345 | 8444 | 79732574 |
| Laryngitis fungal | 78.90 | 22.16 | 12 | 3358 | 134 | 79740884 |
| Spinal X-ray abnormal | 52.87 | 22.16 | 7 | 3363 | 25 | 79740993 |
| Visual acuity reduced | 51.32 | 22.16 | 25 | 3345 | 29444 | 79711574 |
| Liver iron concentration increased | 48.94 | 22.16 | 6 | 3364 | 9 | 79741009 |
| Sickle cell anaemia with crisis | 46.24 | 22.16 | 16 | 3354 | 7906 | 79733112 |
| Haemoglobin decreased | 44.96 | 22.16 | 51 | 3319 | 222068 | 79518950 |
| Iron overload | 43.43 | 22.16 | 11 | 3359 | 1853 | 79739165 |
| Agranulocytosis | 36.29 | 22.16 | 23 | 3347 | 45007 | 79696011 |
| Bacterial sepsis | 34.50 | 22.16 | 13 | 3357 | 8185 | 79732833 |
| Maculopathy | 34.41 | 22.16 | 10 | 3360 | 2815 | 79738203 |
| Blood creatinine increased | 32.01 | 22.16 | 36 | 3334 | 155021 | 79585997 |
| Haemochromatosis | 31.61 | 22.16 | 8 | 3362 | 1342 | 79739676 |
| Myelodysplastic syndrome | 30.90 | 22.16 | 18 | 3352 | 30283 | 79710735 |
| Blood iron increased | 30.12 | 22.16 | 8 | 3362 | 1622 | 79739396 |
| Infective chondritis | 27.61 | 22.16 | 4 | 3366 | 31 | 79740987 |
| Haemosiderosis | 27.61 | 22.16 | 6 | 3364 | 521 | 79740497 |
| Optic neuropathy | 24.12 | 22.16 | 8 | 3362 | 3476 | 79737542 |
| Retinopathy | 23.25 | 22.16 | 8 | 3362 | 3883 | 79737135 |
| Foetal distress syndrome | 22.44 | 22.16 | 5 | 3365 | 487 | 79740531 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Hypoxia-inducible factor 1-alpha | Transcription factor | EC50 | 4.75 | CHEMBL | |||||
| Deoxyhypusine hydroxylase | Enzyme | IC50 | 5.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |
| 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 | 30 sections |
| Deferoxamine Mesylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-2336 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 500 mg | INTRAMUSCULAR | ANDA | 30 sections |
| Deferoxamine Mesylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-2337 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 30 sections |
| Deferoxamine Mesylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-2337 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 30 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 | 60505-6236 | 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 | 60505-6237 | 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 | 24 sections |
| Deferoxamine mesylate | Human Prescription Drug Label | 1 | 68083-172 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 500 mg | INTRAMUSCULAR | ANDA | 24 sections |
| Deferoxamine mesylate | Human Prescription Drug Label | 1 | 68083-173 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 24 sections |
| Deferoxamine mesylate | Human Prescription Drug Label | 1 | 68083-173 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 2 g | INTRAMUSCULAR | ANDA | 24 sections |