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Details

Stereochemistry ACHIRAL
Molecular Formula C21H15N3O4
Molecular Weight 373.3623
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DEFERASIROX

SMILES

c1ccc(c(c1)-c2nc(-c3ccccc3O)n(-c4ccc(cc4)C(=O)O)n2)O

InChI

InChIKey=BOFQWVMAQOTZIW-UHFFFAOYSA-N
InChI=1S/C21H15N3O4/c25-17-7-3-1-5-15(17)19-22-20(16-6-2-4-8-18(16)26)24(23-19)14-11-9-13(10-12-14)21(27)28/h1-12,25-26H,(H,27,28)

HIDE SMILES / InChI

Molecular Formula C21H15N3O4
Molecular Weight 373.3623
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3495a70c-870c-4968-940e-8baea152cf85; https://www.google.com/patents/US20080312302?cl=en; http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000670/WC500033929.pdf

Deferasirox (marketed as Exjade, Desirox, Deferasirox) is an iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved for this purpose in the USA by FDA in November 2005. It is approved in the European Union by the European Medicines Agency (EMA) for children 6 years and older for chronic iron overload from repeated blood transfusions. Deferasirox is highly selective for iron as Fe3+. In approximately 1-year clinical trials of patients with transfusional chronic iron overload associated with beta-thalassaemia, sickle cell disease, myelodysplastic syndrome or other rare chronic anaemias, deferasiroxhad a beneficial effect on liver iron concentrations (LIC) and serum ferritin levels. Deferasirox can cause acute renal failure, fatal in some patients and requiring dialysis in others. It was showed that most fatalities occurred in patients with multiple comorbidities in advanced stages of their hematological disorders.

Originator

Curator's Comment:: # Novartis Pharma AG

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
EXJADE

Approved Use

Exjade is indicated for the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.

Launch Date

1130889600000
Secondary
EXJADE

Approved Use

Exjade is indicated for the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.

Launch Date

1108080000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
220 μM
30 mg/kg 1 times / day multiple, oral
dose: 30 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DEFERASIROX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
46.5 μM
1000 mg/kg 1 times / day steady-state, oral
dose: 1000 mg/kg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DEFERASIROX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3172 μM × h
30 mg/kg 1 times / day multiple, oral
dose: 30 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DEFERASIROX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
688 μM × h
1000 mg/kg 1 times / day steady-state, oral
dose: 1000 mg/kg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DEFERASIROX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
48.556 uM*h
10 mg/kg 1 times / day steady, oral
dose: 10 mg/kg
route of administration: oral
experiment type: steady
co-administered:
DEFERASIROX plasma
Homo sapiens
6.513 uM*h
10 mg/kg 1 times / day steady, oral
dose: 10 mg/kg
route of administration: oral
experiment type: steady
co-administered:
DEFERASIROX plasma
Homo sapiens
44.652 uM*h
10 mg/kg 1 times / day steady, oral
dose: 10 mg/kg
route of administration: oral
experiment type: steady
co-administered:
DEFERASIROX plasma
Homo sapiens
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
12 h
30 mg/kg 1 times / day multiple, oral
dose: 30 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DEFERASIROX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9.4 h
1000 mg/kg 1 times / day steady-state, oral
dose: 1000 mg/kg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DEFERASIROX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Disc. AE: Abnormal liver function tests, Drug-induced hepatitis...
AEs leading to
discontinuation/dose reduction:
Abnormal liver function tests (2 patients)
Drug-induced hepatitis (2 patients)
Skin rash (1 patient)
Glycosuria (1 patient)
Proteinuria (1 patient)
Henoch-Schonlein purpura (1 patient)
Hyperactivity (1 patient)
Insomnia (1 patient)
Drug fever (1 patient)
Cataract (1 patient)
Sources:
90 mg/kg single, oral
Overdose
Dose: 90 mg/kg
Route: oral
Route: single
Dose: 90 mg/kg
Sources:
unhealthy, 20 years
Health Status: unhealthy
Age Group: 20 years
Sex: M
Sources:
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea (1 patient)
Vomiting (1 patient)
Fanconi syndrome (1 patient)
Sources:
30 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg/kg, 1 times / day
Sources:
unhealthy, 23.1 years (range: 10 -51 years)
Health Status: unhealthy
Age Group: 23.1 years (range: 10 -51 years)
Sex: M+F
Sources:
Other AEs: Gastrointestinal symptom NOS, Skin rash...
Other AEs:
Gastrointestinal symptom NOS (mild, 40%)
Skin rash (18%)
ALT increased
AST increased
Sources:
130 mg single, intravenous
Dose: 130 mg
Route: intravenous
Route: single
Dose: 130 mg
Sources:
healthy, 30.5 years (range: 18-45 years)
Health Status: healthy
Age Group: 30.5 years (range: 18-45 years)
Sex: M
Sources:
20 mg/kg 1 times / day multiple, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, > 2 years
Other AEs: Toxicity renal, Hepatotoxicity...
Other AEs:
Toxicity renal
Hepatotoxicity
Gastrointestinal hemorrhage
Sources:
40 mg/kg single, oral
Highest studied dose
Dose: 40 mg/kg
Route: oral
Route: single
Dose: 40 mg/kg
Sources:
healthy
60 mg/kg 1 times / day steady, oral
Overdose
Dose: 60 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg/kg, 1 times / day
Sources:
unknown
Disc. AE: Hepatitis...
AEs leading to
discontinuation/dose reduction:
Hepatitis (1 patient)
Sources:
80 mg/kg single, oral
Overdose
Dose: 80 mg/kg
Route: oral
Route: single
Dose: 80 mg/kg
Sources:
unhealthy
Other AEs: Diarrhea, Nausea...
Other AEs:
Diarrhea (1 patient)
Nausea (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Cataract 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Drug fever 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Glycosuria 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Henoch-Schonlein purpura 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Hyperactivity 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Insomnia 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Proteinuria 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Skin rash 1 patient
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Abnormal liver function tests 2 patients
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Drug-induced hepatitis 2 patients
Disc. AE
20 mg/kg 1 times / day steady, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, 17.1 years (range: 2 -53 years)
Health Status: unhealthy
Age Group: 17.1 years (range: 2 -53 years)
Sex: M+F
Sources:
Fanconi syndrome 1 patient
90 mg/kg single, oral
Overdose
Dose: 90 mg/kg
Route: oral
Route: single
Dose: 90 mg/kg
Sources:
unhealthy, 20 years
Health Status: unhealthy
Age Group: 20 years
Sex: M
Sources:
Nausea 1 patient
90 mg/kg single, oral
Overdose
Dose: 90 mg/kg
Route: oral
Route: single
Dose: 90 mg/kg
Sources:
unhealthy, 20 years
Health Status: unhealthy
Age Group: 20 years
Sex: M
Sources:
Vomiting 1 patient
90 mg/kg single, oral
Overdose
Dose: 90 mg/kg
Route: oral
Route: single
Dose: 90 mg/kg
Sources:
unhealthy, 20 years
Health Status: unhealthy
Age Group: 20 years
Sex: M
Sources:
ALT increased
30 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg/kg, 1 times / day
Sources:
unhealthy, 23.1 years (range: 10 -51 years)
Health Status: unhealthy
Age Group: 23.1 years (range: 10 -51 years)
Sex: M+F
Sources:
AST increased
30 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg/kg, 1 times / day
Sources:
unhealthy, 23.1 years (range: 10 -51 years)
Health Status: unhealthy
Age Group: 23.1 years (range: 10 -51 years)
Sex: M+F
Sources:
Skin rash 18%
30 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg/kg, 1 times / day
Sources:
unhealthy, 23.1 years (range: 10 -51 years)
Health Status: unhealthy
Age Group: 23.1 years (range: 10 -51 years)
Sex: M+F
Sources:
Gastrointestinal symptom NOS mild, 40%
30 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 30 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg/kg, 1 times / day
Sources:
unhealthy, 23.1 years (range: 10 -51 years)
Health Status: unhealthy
Age Group: 23.1 years (range: 10 -51 years)
Sex: M+F
Sources:
Gastrointestinal hemorrhage
20 mg/kg 1 times / day multiple, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, > 2 years
Hepatotoxicity
20 mg/kg 1 times / day multiple, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, > 2 years
Toxicity renal
20 mg/kg 1 times / day multiple, oral
Recommended
Dose: 20 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg/kg, 1 times / day
Sources:
unhealthy, > 2 years
Hepatitis 1 patient
Disc. AE
60 mg/kg 1 times / day steady, oral
Overdose
Dose: 60 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg/kg, 1 times / day
Sources:
unknown
Diarrhea 1 patient
80 mg/kg single, oral
Overdose
Dose: 80 mg/kg
Route: oral
Route: single
Dose: 80 mg/kg
Sources:
unhealthy
Nausea 1 patient
80 mg/kg single, oral
Overdose
Dose: 80 mg/kg
Route: oral
Route: single
Dose: 80 mg/kg
Sources:
unhealthy
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no (co-administration study)
Comment: no significant interaction with digoxin
Page: 32
no
no (co-administration study)
Comment: no significant interaction with digoxin or cyclosporinA
Page: 33
weak [IC50 100 uM]
yes (co-administration study)
Comment: concomitant administration of deferasirox and repaglinide resulted in increased repaglinide AUC 2.3-fold and Cmax by 62%; IC50 from p26 of clnical pharmacology review
Page: 27
weak [IC50 175 uM]
yes (co-administration study)
Comment: concomitant administration of deferasirox and theophylline resulted in a 2X increase in theophylline but not change in Cmax; IC50 from p26 of clnical pharmacology review
Page: 27
weak [IC50 200 uM]
weak [IC50 200 uM]
weak [IC50 200 uM]
yes (co-administration study)
Comment: concomitant administration of deferasirox and midazolam resulted in decreased midazolam exposure by 17%
Page: 27
weak [IC50 210 uM]
weak [IC50 330 uM]
weak [IC50 >500 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
major
yes (co-administration study)
Comment: concomitant administration of deferasirox and rifampicin resulted in decreased deferasirox AUC by 44%
Page: 7
no
no (co-administration study)
Comment: cyclosporinA or verapamil did not affect deferasirox permeability; no significant interaction with digoxin
Page: 33
no
no (co-administration study)
Comment: cyclosporinA or verapamil did not affect deferasirox permeability; no significant interaction with digoxin
Page: 33
yes
yes
yes
yes
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
A randomised comparison of deferasirox versus deferoxamine for the treatment of transfusional iron overload in sickle cell disease.
2007 Feb
Iron chelators ICL670 and 311 inhibit HIV-1 transcription.
2007 Oct 25
Hepatic but not brain iron is rapidly chelated by deferasirox in aceruloplasminemia due to a novel gene mutation.
2010 Dec
The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors.
2010 Jul-Aug
Effects of deferasirox on renal function and renal epithelial cell death.
2011 Jun 10
Comparison of various iron chelators used in clinical practice as protecting agents against catecholamine-induced oxidative injury and cardiotoxicity.
2011 Nov 18
Efficacy of Deferasirox (Exjade®) in Modulation of Iron Overload in Patients with β-Thalassemia Intermedia.
2015
Hypersensitivity reaction with deferasirox.
2015 Apr-Jun
Effects of deferasirox-deferoxamine on myocardial and liver iron in patients with severe transfusional iron overload.
2015 Jun 18
Chelation efficacy and erythroid response during deferasirox treatment in patients with myeloproliferative neoplasms in fibrotic phase.
2016 Jun
Patents

Sample Use Guides

The recommended initial dose of Exjade (deferasitox) for patients 2 years of age and older is 20 mg per kg body weight orally, once daily. After commencing therapy, monitor serum ferritin monthly and adjust the dose of Exjade, if necessary, every 3-6 months based on serum ferritin trends. Make dose adjustments in steps of 5 or 10 mg per kg and tailor adjustments to the individual patient's response and therapeutic goals. In patients not adequately controlled with doses of 30 mg per kg (e.g., serum ferritin levels persistently above 2500 mcg/L and not showing a decreasing trend over time), doses of up to 40 mg per kg may be considered. Doses above 40 mg per kg are not recommended.
Route of Administration: Oral
Cell proliferation was measured using the MTT assay after human DMS-53 small-cell lung carcinoma and SK-N-MC neuroepithelioma cells were treated with deferasirox for 72 hours at 37°C. Cellular growth assays demonstrated the antiproliferative activity of deferasirox against DMS-53 and SK-N-MC cell lines with IC50 values of12uM and 14uM respectively.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:08:55 UTC 2021
Edited
by admin
on Fri Jun 25 21:08:55 UTC 2021
Record UNII
V8G4MOF2V9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DEFERASIROX
EMA EPAR   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
4-(3,5-BIS(2-HYDROXYPHENYL)-1H-1,2,4-TRIAZOL-1-YL)BENZOIC ACID
Systematic Name English
BENZOIC ACID, 4-(3,5-BIS(2-HYDROXYPHENYL)-1H-1,2,4-TRIAZOL-1-YL)-
Common Name English
DEFERASIROX [VANDF]
Common Name English
ICL670A
Code English
OSVERAL
Brand Name English
ICL670
Code English
EXJADE
Brand Name English
DEFERASIROX [INN]
Common Name English
DEFERASIROX [USAN]
Common Name English
DEFERASIROX [USP-RS]
Common Name English
DEFERASIROX [EMA EPAR]
Common Name English
JADENU SPRINKLE
Brand Name English
DEFERASIROX [HSDB]
Common Name English
DEFERASIROX [MART.]
Common Name English
ICL-670A
Code English
JADENU
Brand Name English
DEFERASIROX [JAN]
Common Name English
DEFERASIROX [EP MONOGRAPH]
Common Name English
DEFERASIROX [ORANGE BOOK]
Common Name English
DEFERASIROX [MI]
Common Name English
DEFERASIROX [WHO-DD]
Common Name English
ICL-670
Code English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS EXJADE (AUTHORIZED: BETA-THALASSEMIA)
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
FDA ORPHAN DRUG 161002
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
NDF-RT N0000000144
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
NCI_THESAURUS C62357
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
NDF-RT N0000175522
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
WHO-VATC QV03AC03
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
LIVERTOX 272
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
WHO-ATC V03AC03
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
FDA ORPHAN DRUG 354411
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
Code System Code Type Description
NDF-RT
N0000187062
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY Cytochrome P450 2C8 Inhibitors [MoA]
INN
8193
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
PUBCHEM
214348
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
NDF-RT
N0000185506
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
EVMPD
SUB21981
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
WIKIPEDIA
Deferasirox
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
EPA CompTox
201530-41-8
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
MERCK INDEX
M4131
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY Merck Index
MESH
C415250
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
LACTMED
Deferasirox
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
EU-Orphan Drug
EU/3/02/092(EXPIRED)
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY Please note that this product was withdrawn from the Community Register of designated orphan medicinal products in September 2016 at the end of the period of market exclusivity. On 13 March 2002, orphan designation (EU/3/02/092) was granted by the European Commissin to Novartis Europharm Limited, United Kingdom, for 4-(3,5-bis-(hydroxy-phenyl)-1,2,4)triazol-1-yl)-benzoic acid for the treatment of chronic iron overload requiring chelation therapy.
NCI_THESAURUS
C48384
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
NDF-RT
N0000182138
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY Cytochrome P450 1A2 Inhibitors [MoA]
ChEMBL
CHEMBL550348
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
FDA UNII
V8G4MOF2V9
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
RXCUI
614373
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY RxNorm
CAS
201530-41-8
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
HSDB
7844
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
DRUG CENTRAL
3128
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
DRUG BANK
DB01609
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
USP_CATALOG
1165656
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY USP-RS
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> INHIBITOR
WEAK
IC50
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TARGET->LIGAND
Deferasirox is an orally active chelator that is selective for iron (as Fe3+). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio.
BINDING
METABOLIC ENZYME -> SUBSTRATE
MAJOR
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> INHIBITOR
WEAK
IC50
METABOLIC ENZYME -> SUBSTRATE
MINOR
Related Record Type Details
METABOLITE -> PARENT
PLASMA; URINE
METABOLITE -> PARENT
FECAL; URINE
METABOLITE -> PARENT
Presumably by CYP2D6
FECAL
METABOLITE -> PARENT
Presumably by CYP1A
FECAL
METABOLITE -> PARENT
URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC