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Details

Stereochemistry ACHIRAL
Molecular Formula C25H48N6O8.CH4O3S
Molecular Weight 656.7918
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DEFEROXAMINE MESYLATE

SMILES

CC(=O)N(CCCCCN=C(CCC(=O)N(CCCCCN=C(CCC(=O)N(CCCCCN)O)O)O)O)O.CS(=O)(=O)O

InChI

InChIKey=IDDIJAWJANBQLJ-UHFFFAOYSA-N
InChI=1S/C25H48N6O8.CH4O3S/c1-21(32)29(37)18-9-3-6-16-27-22(33)12-14-25(36)31(39)20-10-4-7-17-28-23(34)11-13-24(35)30(38)19-8-2-5-15-26;1-5(2,3)4/h37-39H,2-20,26H2,1H3,(H,27,33)(H,28,34);1H3,(H,2,3,4)

HIDE SMILES / InChI

Molecular Formula CH4O3S
Molecular Weight 96.1068
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C25H48N6O8
Molecular Weight 560.685
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Deferoxamine (brand name Desferal) an iron chelator, is a drug for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias. Deferoxamine chelates iron by forming a stable complex that prevents the iron entering into further chemical reactions. However, drug may cause hypersensitivity reactions, systemic allergic reactions, and cardiovascular, hematologic and neurological adverse reactions. Serious adverse reactions include significant hypotension and marked body weight loss. Principally plasma enzymes metabolize deferoxamine, but the pathways have not yet been defined. The chelate is readily soluble in water and passes easily through the kidney, giving the urine a characteristic reddish color. Some is also excreted in the feces via the bile.

CNS Activity

Curator's Comment:: Known to be CNS penetrant in rats. Human data not available

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: CHEMBL2363058
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
DESFERAL

Approved Use

Deferoxamine Mesylate for Injection, USP is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias. Acute Iron Intoxication Deferoxamine mesylate is an adjunct to, and not a substitute for, standard measures used in treating acute iron intoxication, which may include the following: induction of emesis with syrup of ipecac; gastric lavage; suction and maintenance of a clear airway; control of shock with intravenous fluids, blood, oxygen, and vasopressors; and correction of acidosis. Chronic Iron Overload Deferoxamine mesylate can promote iron excretion in patients with secondary iron overload from multiple transfusions (as may occur in the treatment of some chronic anemias, including thalassemia). Long-term therapy with deferoxamine mesylate slows accumulation of hepatic iron and retards or eliminates progression of hepatic fibrosis. Iron mobilization with deferoxamine mesylate is relatively poor in patients under the age of 3 years with relatively little iron overload. The drug should ordinarily not be given to such patients unless significant iron mobilization (e.g., 1 mg or more of iron per day) can be demonstrated. Deferoxamine mesylate is not indicated for the treatment of primary hemochromatosis, since phlebotomy is the method of choice for removing excess iron in this disorder.

Launch Date

-5.5296E10
Palliative
DESFERAL

Approved Use

Deferoxamine Mesylate for Injection, USP is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias. Acute Iron Intoxication Deferoxamine mesylate is an adjunct to, and not a substitute for, standard measures used in treating acute iron intoxication, which may include the following: induction of emesis with syrup of ipecac; gastric lavage; suction and maintenance of a clear airway; control of shock with intravenous fluids, blood, oxygen, and vasopressors; and correction of acidosis. Chronic Iron Overload Deferoxamine mesylate can promote iron excretion in patients with secondary iron overload from multiple transfusions (as may occur in the treatment of some chronic anemias, including thalassemia). Long-term therapy with deferoxamine mesylate slows accumulation of hepatic iron and retards or eliminates progression of hepatic fibrosis. Iron mobilization with deferoxamine mesylate is relatively poor in patients under the age of 3 years with relatively little iron overload. The drug should ordinarily not be given to such patients unless significant iron mobilization (e.g., 1 mg or more of iron per day) can be demonstrated. Deferoxamine mesylate is not indicated for the treatment of primary hemochromatosis, since phlebotomy is the method of choice for removing excess iron in this disorder.

Launch Date

-5.5296E10
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7.4 μM
10 mg/kg 1 times / day other, intravenous
dose: 10 mg/kg
route of administration: Intravenous
experiment type: OTHER
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
12.9 μM
100 mg/kg 1 times / day other, intravenous
dose: 100 mg/kg
route of administration: Intravenous
experiment type: OTHER
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
15.7 μM
10 mg/kg single, intramuscular
dose: 10 mg/kg
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2.5 μM
10 mg/kg single, intravenous
dose: 10 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2.7 μM
100 mg/kg 1 times / day other, intravenous
dose: 100 mg/kg
route of administration: Intravenous
experiment type: OTHER
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
6.1 μM
10 mg/kg single, intravenous
dose: 10 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
7 μM
10 mg/kg single, intramuscular
dose: 10 mg/kg
route of administration: Intramuscular
experiment type: SINGLE
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
10.1 μM
40 mg/kg single, subcutaneous
dose: 40 mg/kg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
354 μM × h
10 mg/kg 1 times / day other, intravenous
dose: 10 mg/kg
route of administration: Intravenous
experiment type: OTHER
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.05 h
10 mg/kg 1 times / day other, intravenous
dose: 10 mg/kg
route of administration: Intravenous
experiment type: OTHER
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
7.59 h
40 mg/kg single, subcutaneous
dose: 40 mg/kg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
DEFEROXAMINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
700 mg/kg 1 times / day single, intravenous
Studied dose
Dose: 700 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 700 mg/kg, 1 times / day
Sources:
unhealthy, 17 years
n = 1
Health Status: unhealthy
Condition: sickle cell-beta thalassemia
Age Group: 17 years
Sex: M
Population Size: 1
Sources:
Other AEs: Renal failure...
Other AEs:
Renal failure
Sources:
135 mg/kg 1 times / day multiple, intravenous (mean)
Studied dose
Dose: 135 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 135 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
Disc. AE: Visual disturbances...
AEs leading to
discontinuation/dose reduction:
Visual disturbances
Sources:
240 mg/kg 1 times / day multiple, intravenous
Studied dose
Dose: 240 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 240 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
DLT: Lethargy, Dizziness...
Dose limiting toxicities:
Lethargy
Dizziness
Blurred vision
Leg cramps
Sources:
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
DLT: Aspiration pneumonia...
Other AEs: Hyperglycaemia, Vomiting...
Dose limiting toxicities:
Aspiration pneumonia (33.3%)
Other AEs:
Hyperglycaemia (grade 1, 16.7%)
Vomiting (grade 1, 16.7%)
Fatigue (grade 1, 16.7%)
Infection (grade 1, 16.7%)
Urinary tract infection (grade 1, 33.3%)
Blood pressure decreased (grade 1, 16.7%)
Hyponatraemia (grade 1, 16.7%)
Agitation (grade 1, 16.7%)
Convulsion (grade 1, 16.7%)
Headache (grade 1, 16.7%)
Lethargy (grade 1, 16.7%)
Delirium (grade 1, 16.7%)
Depression (grade 1, 16.7%)
Respiratory failure (grade 1, 33.3%)
Rash (grade 1, 16.7%)
Skin irritation (grade 1, 16.7%)
Deep vein thrombosis (grade 1, 16.7%)
Hypotension (grade 1, 16.7%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Renal failure
700 mg/kg 1 times / day single, intravenous
Studied dose
Dose: 700 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 700 mg/kg, 1 times / day
Sources:
unhealthy, 17 years
n = 1
Health Status: unhealthy
Condition: sickle cell-beta thalassemia
Age Group: 17 years
Sex: M
Population Size: 1
Sources:
Visual disturbances Disc. AE
135 mg/kg 1 times / day multiple, intravenous (mean)
Studied dose
Dose: 135 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 135 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
Blurred vision DLT
240 mg/kg 1 times / day multiple, intravenous
Studied dose
Dose: 240 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 240 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
Dizziness DLT
240 mg/kg 1 times / day multiple, intravenous
Studied dose
Dose: 240 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 240 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
Leg cramps DLT
240 mg/kg 1 times / day multiple, intravenous
Studied dose
Dose: 240 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 240 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
Lethargy DLT
240 mg/kg 1 times / day multiple, intravenous
Studied dose
Dose: 240 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 240 mg/kg, 1 times / day
Sources:
unhealthy, meadian age 12 years
n = 10
Health Status: unhealthy
Condition: recurrent neuroblastoma
Age Group: meadian age 12 years
Sex: M+F
Population Size: 10
Sources:
Aspiration pneumonia 33.3%
DLT
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Agitation grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Blood pressure decreased grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Convulsion grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Deep vein thrombosis grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Delirium grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Depression grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Fatigue grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Headache grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Hyperglycaemia grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Hyponatraemia grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Hypotension grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Infection grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Lethargy grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Rash grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Skin irritation grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Vomiting grade 1, 16.7%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Respiratory failure grade 1, 33.3%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Urinary tract infection grade 1, 33.3%
62 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 62 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 62 mg/kg, 1 times / day
Sources:
unhealthy, median age 70 years
n = 6
Health Status: unhealthy
Condition: intracerebral hemorrhage
Age Group: median age 70 years
Sex: M+F
Population Size: 6
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [Activation >10 uM]
no [Activation >10 uM]
no [Activation >10 uM]
no [Activation >10 uM]
no [Activation >10 uM]
yes
yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Protection from oxidative stress-induced apoptosis in cortical neuronal cultures by iron chelators is associated with enhanced DNA binding of hypoxia-inducible factor-1 and ATF-1/CREB and increased expression of glycolytic enzymes, p21(waf1/cip1), and erythropoietin.
1999 Nov 15
Inhibition of human immunodeficiency virus type 1 replication in human mononuclear blood cells by the iron chelators deferoxamine, deferiprone, and bleomycin.
2000 Feb
Interferon-gamma and lipopolysaccharide regulate the expression of Nramp2 and increase the uptake of iron from low relative molecular mass complexes by macrophages.
2000 Nov
Comparison of IY81149 with omeprazole in rat reflux oesophagitis.
2000 Oct-Dec
The role of hydroxyl radical as a messenger in Cr(VI)-induced p53 activation.
2000 Sep
Electron paramagnetic resonance detection of free radicals in UV-irradiated human and mouse skin.
2001
Hypercalcemia and human nature.
2001 Apr
mRNA localization by a 145-nucleotide region of the c-fos 3'--untranslated region. Links to translation but not stability.
2001 Apr 27
Klebsiella pneumoniae meningitis in thalassemia major patients.
2001 Apr-May
Carbon monoxide is the heme oxygenase product with a pyretic action: evidence for a cGMP signaling pathway.
2001 Feb
Radiation sensitization of mammalian cells by metal chelators.
2001 Feb
Iron status and the outcome of HIV infection: an overview.
2001 Feb
CAS agar diffusion assay for the measurement of siderophores in biological fluids.
2001 Feb 1
DNA-protein crosslinks induced by nickel compounds in isolated rat lymphocytes: role of reactive oxygen species and specific amino acids.
2001 Feb 1
Redox-active iron mediates amyloid-beta toxicity.
2001 Feb 15
Comparative effects of metal chelating agents on the neuronal cytotoxicity induced by copper (Cu+2), iron (Fe+3) and zinc in the hippocampus.
2001 Feb 16
Desferrioxamine, an iron chelator, upregulates cyclooxygenase-2 expression and prostaglandin production in a human macrophage cell line.
2001 Feb 26
Cytochrome b(5) plays a key role in human microsomal chromium(VI) reduction.
2001 Feb 28
Oxygen radicals mediate the final exacerbation of endothelin-1-induced gastric ulcer in rat.
2001 Feb 9
Temporary treatment with sirolimus and low-trough cyclosporine prevents acute islet allograft rejection, and combination with starch-conjugated deferoxamine promotes islet engraftment in the preclinical pig model.
2001 Feb-Mar
The role of oxygen-derived free radicals in augmented relaxations to levcromakalim in the aorta from hypertensive rats.
2001 Jan
Oxidative insult in sheep red blood cells induced by T-butyl hydroperoxide: the roles of glutathione and glutathione peroxidase.
2001 Jan
Inhibition of hepatitis B virus production associated with high levels of intracellular viral DNA intermediates in iron-depleted HepG2.2.15 cells.
2001 Jan
Differential inhibitory mechanism of Fe2+ and Fe3+ on contraction of ileal longitudinal smooth muscle.
2001 Jan
Lazaroid compounds prevent early but not late stages of oxidant-induced cell injury: potential explanation for the lack of efficacy of lazaroids in clinical trials.
2001 Jan
Deferoxamine pharmacokinetics.
2001 Jan
Progression of iron overload in sickle cell disease.
2001 Jan
Impairment of endothelial nitric oxide production by acute glucose overload.
2001 Jan
Interaction between iron(II) and hydroxamic acids: oxidation of iron(II) to iron(III) by desferrioxamine B under anaerobic conditions.
2001 Jan 15
Hypoxia death stimulus induces translocation of p53 protein to mitochondria. Detection by immunofluorescence on whole cells.
2001 Jan 19
Vanadium-induced nuclear factor of activated T cells activation through hydrogen peroxide.
2001 Jun 22
Possible role of hydroxyl radicals in the oxidation of dichloroacetonitrile by Fenton-like reaction.
2001 Mar
Rapid recovery with oral zinc sulphate in deferoxamine-induced presumed optic neuropathy and hearing loss.
2001 Mar
Hemoproteins affect H(2)O(2) removal from rat tissues.
2001 Mar
Inhibitory effect of reactive oxygen species on angiotensin I-converting enzyme (kininase II).
2001 Mar
Noninvasive detection of hydroxyl radical generation in lung by diesel exhaust particles.
2001 Mar 1
Atherosclerosis: defeat of the defense?
2001 Mar 16
Primary breast lymphoma detected with Tc-99m tetrofosmin scintigraphy.
2001 May
Hypoxia induces lytic replication of Kaposi sarcoma-associated herpesvirus.
2001 May 15
Patents

Sample Use Guides

Acute Iron Intoxication: Intramuscular Administration: This route is preferred and should be used for ALL PATIENTS NOT IN SHOCK: A dose of 1000 mg should be administered initially. This may be followed by 500 mg every 4 hours for two doses. Depending upon the clinical response, subsequent doses of 500 mg may be administered every 4-12 hours. The total amount administered should not exceed 6000 mg in 24 hours Intravenous Administration: THIS ROUTE SHOULD BE USED ONLY FOR PATIENTS IN A STATE OF CARDIOVASCULAR COLLAPSE AND THEN ONLY BY SLOW INFUSION. THE RATE OF INFUSION SHOULD NOT EXCEED 15 MG/KG/HR FOR THE FIRST 1000 MG ADMINISTERED. SUBSEQUENT IV DOSING, IF NEEDED, MUST BE AT A SLOWER RATE, NOT TO EXCEED 125 MG/HR: An initial dose of 1000 mg should be administered at a rate NOT TO EXCEED 15 mg/kg/hr. This may be followed by 500 mg over 4 hours for two doses. Depending upon the clinical response, subsequent doses of 500 mg may be administered over 4-12 hours. The total amount administered should not exceed 6000 mg in 24 hours. CHRONIC IRON OVERLOAD: SUBCUTANEOUS ADMINISTRATION: A daily dose of 1000-2000 mg (20-40 mg/kg/day) should be administered over 8-24 hours, utilizing a small portable pump capable of providing continuous mini-infusion. The duration of infusion must be individualized. In some patients, as much iron will be excreted after a short infusion of 8-12 hours as with the same dose given over 24 hours. Intravenous Administration: The standard recommended method of Desferal administration is via slow subcutaneous infusion over 8 – 12 hours. In patients with intravenous access, the daily dose of Desferal can be administered intravenously. The standard dose is 20 – 40 mg/kg/day for children and 40–50 mg/kg/day over 8 – 12 hours in adults for 5 – 7 days per week. In children, average doses should not exceed 40 mg/kg/day until growth has ceased. In adults, average doses should not exceed 60 mg/kg/day. The intravenous infusion rate should not exceed 15 mg/kg/hour. Intramuscular Administration: A daily dose of 500-1000 mg may be administered intramuscularly. The total daily dose should not exceed 1000 mg.
Route of Administration: Other
In Vitro Use Guide
Curator's Comment:: It was investigated the effect of deferoxamine on mesenchymal stromal cells (MSCs). Ex vivo cultured stem cells derived from tumor and bone marrow compartment were exposed to Deferoxamine (DFO). It was revealed, that DFO had growth-arresting and apoptosis-inducing effect on tumor-associated MSCs (TAMSCs) and bone marrow MSCs (BMMSCs). DFO also influenced the expression pattern of adhesion molecule VCAM-1 on both TAMSCs and BMMSCs.
Unknown
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:14:43 UTC 2021
Edited
by admin
on Fri Jun 25 21:14:43 UTC 2021
Record UNII
V9TKO7EO6K
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DEFEROXAMINE MESYLATE
ORANGE BOOK   USAN   USP   USP-RS   VANDF  
USAN  
Official Name English
DESFERRIOXAMINE MESYLATE [WHO-IP]
Common Name English
DESFERRIOXAMINE MESILATE
MART.  
Common Name English
NSC-756718
Code English
BUTANEDIAMIDE, N'(-(((((ACETYLHYDROXYAMINO)PENTYL)MINO)1,4-DIOXOBUTYL)YDROXYAMINO)ENTYL)N-(5-AMINOPENTYL)-N-HYDROXY-, MONOMETHANESULPHONATE
Common Name English
N-(5-(3-((5-AMINOPENTYL)HYDROXYCARBAMOYL)PROPIONAMIDO)PENTYL)-3-((5-(N-HYDROXYACETAMIDO)PENTYL)CARBAMOYL)PROPIONOHYDROXAMIC ACID MONOMETHANESULFONATE (SALT)
Common Name English
DEFEROXAMINE MESYLATE [USP-RS]
Common Name English
BUTANEDIAMIDE, N'(-(((((ACETYLHYDROXYAMINO)PENTYL)MINO)1,4-DIOXOBUTYL)YDROXYAMINO)ENTYL)N-(5-AMINOPENTYL)-N-HYDROXY-, MONOMETHANESULFONATE
Common Name English
DEFEROXAMINE MESYLATE [ORANGE BOOK]
Common Name English
DEFEROXAMINE MESILATE [EP MONOGRAPH]
Common Name English
DEFEROXAMINE MESYLATE [USP]
Common Name English
N-(5-(3-((5-AMINOPENTYL)HYDROXYCARBAMOYL)PROPIONAMIDO)PENTYL)-3-((5-(N-HYDROXYACETAMIDO)PENTYL)CARBAMOYL)PROPIONOHYDROXAMIC ACID MONOMETHANESULPHONATE (SALT)
Common Name English
DEFEROXAMINE METHANESULFONATE
MI  
Common Name English
DEFEROXAMINE MESILATE
EP   WHO-DD   WHO-IP  
Common Name English
DEFEROXAMINE MESILATE [JAN]
Common Name English
DEFEROXAMINI MESILAS [WHO-IP LATIN]
Common Name English
DESFERAL
Brand Name English
DEFEROXAMINE MESYLATE [VANDF]
Common Name English
DEFEROXAMINE MESYLATE [USAN]
Common Name English
DEFEROXAMINE MESILATE [WHO-IP]
Common Name English
BA-33112
Code English
DEFEROXAMINE METHANESULFONATE [MI]
Common Name English
DEFEROXAMINE MESILATE [WHO-DD]
Common Name English
DESFERRIOXAMINE MESILATE [MART.]
Common Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/04/231
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
NCI_THESAURUS C62357
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
Code System Code Type Description
EPA CompTox
138-14-7
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
NCI_THESAURUS
C417
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
EVMPD
SUB01571MIG
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
ChEMBL
CHEMBL556
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
CAS
138-14-7
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
PUBCHEM
62881
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
FDA UNII
V9TKO7EO6K
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
RXCUI
3132
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY RxNorm
ECHA (EC/EINECS)
205-314-3
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
DRUG BANK
DBSALT000964
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY
USP_CATALOG
1166003
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY USP-RS
MERCK INDEX
M4133
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY Merck Index
WHO INTERNATIONAL PHARMACOPEIA
DEFEROXAMINE MESYLATE
Created by admin on Fri Jun 25 21:14:43 UTC 2021 , Edited by admin on Fri Jun 25 21:14:43 UTC 2021
PRIMARY Description: A white to yellowish white powder; odourless or almost odourless.Solubility: Soluble in 5 parts of water; soluble in ethanol (~750 g/l) TS; slightly soluble in methanol R; practically insoluble in ether R.Category: Antidote to iron poisoning.Storage: Deferoxamine mesilate should be kept in a well-closed container, protected from light, and stored at a temperature notexceeding 4 ?C.
Related Record Type Details
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY