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Identification
NameDeferasirox
Accession NumberDB01609
TypeSmall Molecule
GroupsApproved, Investigational
Description

Deferasirox is an oral 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 in the USA for this purpose.

Structure
Thumb
Synonyms
SynonymLanguageCode
DeferasiroxumLatinINN
ExjadeNot AvailableNot Available
ICL 670Not AvailableNot Available
ICL 670aNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Exjadetablet, for suspension125 mgoralNovartis Pharmaceuticals Corporation2005-11-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exjadetablet, for suspension250 mgoralNovartis Pharmaceuticals Corporation2005-11-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exjadetablet, for suspension500 mgoralNovartis Pharmaceuticals Corporation2005-11-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Exjadetablet for suspension125.0 mgoralNovartis Pharmaceuticals Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Exjadetablet for suspension500.0 mgoralNovartis Pharmaceuticals Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number201530-41-8
WeightAverage: 373.3615
Monoisotopic: 373.106255983
Chemical FormulaC21H15N3O4
InChI KeyBOFQWVMAQOTZIW-UHFFFAOYSA-N
InChI
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)
IUPAC Name
4-[bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid
SMILES
OC(=O)C1=CC=C(C=C1)N1N=C(N=C1C1=CC=CC=C1O)C1=CC=CC=C1O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenyl-1,3,4-triazoles. These are organic compounds containing a 1,3,4-triazole substituted by a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassTriazoles
Direct ParentPhenyl-1,3,4-triazoles
Alternative Parents
Substituents
  • Phenyl-1,3,4-triazole
  • Phenyl-1,2,4-triazole
  • Aminobenzoic acid or derivatives
  • Aminobenzoic acid
  • Benzoic acid
  • Benzoic acid or derivatives
  • Benzoyl
  • Phenol
  • Benzenoid
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.
PharmacodynamicsDeferasirox 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. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain.
Mechanism of actionTwo molecules of deferasirox are capable of binding to 1 atom of iron. Deferasirox works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming a stable complex which is eliminated via the kidneys.
AbsorptionThe absolute bioavailability (AUC) of deferasirox tablets for oral suspension is 70% compared to an intravenous dose.
Volume of distribution
  • 14.37 ± 2.69 L
Protein bindingDeferasirox is highly (~99%) protein bound almost exclusively to serum albumin.
Metabolism

Hepatic. CYP450-catalyzed (oxidative) metabolism of deferasirox appears to be minor in humans (about 8%). Glucuronidation is the main metabolic pathway for deferasirox, with subsequent biliary excretion.

Route of eliminationDeferasirox and metabolites are primarily (84% of the dose) excreted in the feces. Renal excretion of deferasirox and metabolites is minimal (8% of the administered dose).
Half lifeThe mean elimination half-life ranged from 8 to 16 hours following oral administration.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.993
Blood Brain Barrier+0.8508
Caco-2 permeable+0.5089
P-glycoprotein substrateNon-substrate0.7808
P-glycoprotein inhibitor INon-inhibitor0.894
P-glycoprotein inhibitor IINon-inhibitor0.8431
Renal organic cation transporterNon-inhibitor0.8708
CYP450 2C9 substrateNon-substrate0.7212
CYP450 2D6 substrateNon-substrate0.8686
CYP450 3A4 substrateNon-substrate0.6466
CYP450 1A2 substrateNon-inhibitor0.5802
CYP450 2C9 substrateNon-inhibitor0.7105
CYP450 2D6 substrateNon-inhibitor0.8221
CYP450 2C19 substrateNon-inhibitor0.5918
CYP450 3A4 substrateNon-inhibitor0.8179
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5717
Ames testNon AMES toxic0.6607
CarcinogenicityNon-carcinogens0.8519
BiodegradationNot ready biodegradable0.9524
Rat acute toxicity2.1119 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9684
hERG inhibition (predictor II)Non-inhibitor0.9072
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tablet for suspensionoral125.0 mg
Tablet for suspensionoral500.0 mg
Tablet, for suspensionoral125 mg
Tablet, for suspensionoral250 mg
Tablet, for suspensionoral500 mg
Prices
Unit descriptionCostUnit
Exjade 500 mg tablet78.61USD tablet
Exjade 250 mg tablet39.3USD tablet
Exjade 125 mg tablet19.65USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada22559512006-10-102017-06-24
United States64655041999-04-052019-04-05
United States65967501997-06-242017-06-24
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point116-117 °CNot Available
water solubility0.038 mg/mL at 37 °CYALKOWSKY,SH & DANNENFELSER,RM (1992)
logP3.52HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.0343 mg/mLALOGPS
logP4.01ALOGPS
logP4.74ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)4.55ChemAxon
pKa (Strongest Basic)0.19ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area108.47 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity125.32 m3·mol-1ChemAxon
Polarizability38.52 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Rajendra Suryabhan Patil, Kishore Charugundla, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson, “SUBSTANTIALLY PURE DEFERASIROX AND PROCESSES FOR THE PREPARATION THEREOF.” U.S. Patent US20110171138, issued July 14, 2011.

US20110171138
General ReferenceNot Available
External Links
ATC CodesV03AC03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
AbirateroneMay decrease the serum concentration of CYP3A4 Substrates.
AcenocoumarolMay increase the serum concentration of CYP1A2 Substrates.
AgomelatineCYP1A2 Inhibitors (Moderate) may increase the serum concentration of Agomelatine.
AlclometasoneCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
AlfuzosinMay decrease the serum concentration of CYP3A4 Substrates.
AlosetronMay increase the serum concentration of CYP1A2 Substrates.
AlprazolamMay decrease the serum concentration of CYP3A4 Substrates.
Aluminum hydroxideMay diminish the therapeutic effect of Deferasirox.
AmcinonideCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
AminophyllineMay decrease the serum concentration of CYP3A4 Substrates.
AmiodaroneMay decrease the serum concentration of CYP3A4 Substrates.
AmlodipineMay decrease the serum concentration of CYP3A4 Substrates.
ApixabanMay decrease the serum concentration of CYP3A4 Substrates.
ApremilastMay decrease the serum concentration of CYP3A4 Substrates.
AprepitantMay decrease the serum concentration of CYP3A4 Substrates.
ArgatrobanAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
AripiprazoleCYP3A4 Inducers may decrease the serum concentration of ARIPiprazole.
armodafinilMay decrease the serum concentration of CYP3A4 Substrates.
ArtemetherMay decrease the serum concentration of CYP3A4 Substrates.
AsenapineMay increase the serum concentration of CYP1A2 Substrates.
AtazanavirMay decrease the serum concentration of CYP3A4 Substrates.
AtorvastatinMay decrease the serum concentration of CYP3A4 Substrates.
AvanafilMay decrease the serum concentration of CYP3A4 Substrates.
AxitinibMay decrease the serum concentration of CYP3A4 Substrates.
BeclomethasoneMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
BedaquilineMay decrease the serum concentration of CYP3A4 Substrates.
BenzphetamineMay decrease the serum concentration of CYP3A4 Substrates.
BetamethasoneMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
BetaxololMay increase the serum concentration of CYP1A2 Substrates.
BiotinMay decrease the serum concentration of CYP3A4 Substrates.
BisoprololMay decrease the serum concentration of CYP3A4 Substrates.
BivalirudinAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
BoceprevirMay decrease the serum concentration of CYP3A4 Substrates.
BortezomibMay decrease the serum concentration of CYP3A4 Substrates.
BosutinibMay decrease the serum concentration of CYP3A4 Substrates.
BromazepamMay increase the serum concentration of CYP1A2 Substrates.
BudesonideMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
BuprenorphineMay decrease the serum concentration of CYP3A4 Substrates.
BuspironeMay decrease the serum concentration of CYP3A4 Substrates.
CabazitaxelMay decrease the serum concentration of CYP3A4 Substrates.
CabozantinibMay decrease the serum concentration of CYP3A4 Substrates.
CaffeineMay increase the serum concentration of CYP1A2 Substrates.
CalcipotriolCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
CalcitriolMay decrease the serum concentration of CYP3A4 Substrates.
CarbamazepineMay decrease the serum concentration of CYP3A4 Substrates.
CelecoxibNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ChlordiazepoxideMay decrease the serum concentration of CYP3A4 Substrates.
ChloroquineMay decrease the serum concentration of CYP3A4 Substrates.
CholestyramineBile Acid Sequestrants may decrease the serum concentration of Deferasirox.
CilostazolMay decrease the serum concentration of CYP3A4 Substrates.
CitalopramMay decrease the serum concentration of CYP3A4 Substrates.
Citric AcidMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ClarithromycinMay decrease the serum concentration of CYP3A4 Substrates.
ClidiniumMay decrease the serum concentration of CYP3A4 Substrates.
Clobetasol propionateCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ClocortoloneCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ClodronateBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ClomipramineMay increase the serum concentration of CYP1A2 Substrates.
ClonazepamMay decrease the serum concentration of CYP3A4 Substrates.
ClozapineMay increase the serum concentration of CYP1A2 Substrates.
ColesevelamBile Acid Sequestrants may decrease the serum concentration of Deferasirox.
ColestipolBile Acid Sequestrants may decrease the serum concentration of Deferasirox.
ConivaptanMay decrease the serum concentration of CYP3A4 Substrates.
CorticotropinCorticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
Cortisone acetateCorticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
CrizotinibMay decrease the serum concentration of CYP3A4 Substrates.
CyclobenzaprineMay increase the serum concentration of CYP1A2 Substrates.
Cyproterone acetateMay decrease the serum concentration of CYP3A4 Substrates.
Dabigatran etexilateAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DabrafenibMay increase the serum concentration of CYP2C8 Substrates.
DacarbazineMay increase the serum concentration of CYP1A2 Substrates.
DalteparinMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DanaparoidAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DantroleneMay decrease the serum concentration of CYP3A4 Substrates.
DarifenacinMay decrease the serum concentration of CYP3A4 Substrates.
DarunavirMay decrease the serum concentration of CYP3A4 Substrates.
DasatinibMay decrease the serum concentration of CYP3A4 Substrates.
DelavirdineMay decrease the serum concentration of CYP3A4 Substrates.
DesogestrelMay decrease the serum concentration of CYP3A4 Substrates.
DesoximetasoneCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DiazepamMay decrease the serum concentration of CYP3A4 Substrates.
DicoumarolMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DiflorasoneCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DiflunisalNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DifluprednateMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
DihydrocodeineMay increase the serum concentration of CYP1A2 Substrates.
DiltiazemMay decrease the serum concentration of CYP3A4 Substrates.
DisopyramideMay decrease the serum concentration of CYP3A4 Substrates.
DocetaxelMay decrease the serum concentration of CYP3A4 Substrates.
DoxazosinMay decrease the serum concentration of CYP3A4 Substrates.
DronedaroneMay decrease the serum concentration of CYP3A4 Substrates.
DrospirenoneMay decrease the serum concentration of CYP3A4 Substrates.
DuloxetineMay increase the serum concentration of CYP1A2 Substrates.
Edetic AcidMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
EliglustatMay decrease the serum concentration of CYP3A4 Substrates.
EnoxaparinAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
EnzalutamideMay decrease the serum concentration of CYP3A4 Substrates.
EplerenoneMay decrease the serum concentration of CYP3A4 Substrates.
ErlotinibMay decrease the serum concentration of CYP3A4 Substrates.
EscitalopramMay decrease the serum concentration of CYP3A4 Substrates.
EstropipateMay decrease the serum concentration of CYP3A4 Substrates.
EszopicloneMay decrease the serum concentration of CYP3A4 Substrates.
Ethinyl EstradiolMay decrease the serum concentration of CYP3A4 Substrates.
EthosuximideMay decrease the serum concentration of CYP3A4 Substrates.
Ethyl biscoumacetateMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
EthynodiolMay decrease the serum concentration of CYP3A4 Substrates.
EtodolacNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
EtoposideMay decrease the serum concentration of CYP3A4 Substrates.
EtravirineMay decrease the serum concentration of CYP3A4 Substrates.
EverolimusMay decrease the serum concentration of CYP3A4 Substrates.
ExemestaneMay decrease the serum concentration of CYP3A4 Substrates.
FelbamateMay decrease the serum concentration of CYP3A4 Substrates.
FelodipineMay decrease the serum concentration of CYP3A4 Substrates.
FenoprofenNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FesoterodineMay decrease the serum concentration of CYP3A4 Substrates.
FloctafenineNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FludrocortisoneCorticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
Fluocinolone AcetonideCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FluocinonideCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FluorometholoneCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FlurandrenolideCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FlurazepamMay decrease the serum concentration of CYP3A4 Substrates.
FlutamideMay decrease the serum concentration of CYP3A4 Substrates.
Fluticasone furoateMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
FluvoxamineMay increase the serum concentration of CYP1A2 Substrates.
Fondaparinux sodiumAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
FosamprenavirMay decrease the serum concentration of CYP3A4 Substrates.
FosaprepitantMay decrease the serum concentration of CYP3A4 Substrates.
FosphenytoinFosphenytoin may decrease the serum concentration of Deferasirox.
GefitinibMay decrease the serum concentration of CYP3A4 Substrates.
GuanfacineMay decrease the serum concentration of CYP3A4 Substrates.
HalcinonideMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
Halobetasol PropionateCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
HaloperidolMay decrease the serum concentration of CYP3A4 Substrates.
HeparinAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
HydrocodoneMay decrease the serum concentration of CYP3A4 Substrates.
HydrocortamateMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Exceptions: Beclomethasone (Nasal); Budesonide (Nasal); Ciclesonide (Nasal); Desonide; Dexamethasone (Ophthalmic); Difluprednate; Flunisolide (Nasal); Fluocinolone (Ophthalmic); Fluticasone (Nasal); Loteprednol; Mometasone (Nasal); PrednisoLONE (Ophthalmic); Triamcinolone (Nasal); Triamcinolone (Ophthalmic).
IbandronateBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
IbuprofenNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
IndinavirMay decrease the serum concentration of CYP3A4 Substrates.
IndomethacinNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
IrinotecanMay decrease the serum concentration of CYP3A4 Substrates.
IsavuconazoniumMay decrease the serum concentration of CYP3A4 Substrates.
IsomethepteneMay increase the serum concentration of CYP1A2 Substrates.
Isosorbide DinitrateMay decrease the serum concentration of CYP3A4 Substrates.
Isosorbide MononitrateMay decrease the serum concentration of CYP3A4 Substrates.
IsradipineMay decrease the serum concentration of CYP3A4 Substrates.
ItraconazoleMay decrease the serum concentration of CYP3A4 Substrates.
IvacaftorMay decrease the serum concentration of CYP3A4 Substrates.
IxabepiloneMay decrease the serum concentration of CYP3A4 Substrates.
KetoprofenNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
KetorolacNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
LansoprazoleMay decrease the serum concentration of CYP3A4 Substrates.
LapatinibMay decrease the serum concentration of CYP3A4 Substrates.
LevonorgestrelMay decrease the serum concentration of CYP3A4 Substrates.
LinagliptinMay decrease the serum concentration of CYP3A4 Substrates.
LomitapideMay decrease the serum concentration of CYP3A4 Substrates.
LopinavirRitonavir may decrease the serum concentration of Deferasirox.
LosartanMay decrease the serum concentration of CYP3A4 Substrates.
LovastatinMay decrease the serum concentration of CYP3A4 Substrates.
LumefantrineMay decrease the serum concentration of CYP3A4 Substrates.
LurasidoneMay decrease the serum concentration of CYP3A4 Substrates.
MACITENTANMay decrease the serum concentration of CYP3A4 Substrates.
MaravirocMay decrease the serum concentration of CYP3A4 Substrates.
Medroxyprogesterone AcetateMay decrease the serum concentration of CYP3A4 Substrates.
Mefenamic acidNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
MefloquineMay decrease the serum concentration of CYP3A4 Substrates.
MeloxicamNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
MestranolMay decrease the serum concentration of CYP3A4 Substrates.
MethadoneMay decrease the serum concentration of CYP3A4 Substrates.
MethylprednisoloneCorticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
MexiletineMay increase the serum concentration of CYP1A2 Substrates.
MidazolamMay decrease the serum concentration of CYP3A4 Substrates.
MifepristoneMay decrease the serum concentration of CYP3A4 Substrates.
MirtazapineMay decrease the serum concentration of CYP3A4 Substrates.
ModafinilMay decrease the serum concentration of CYP3A4 Substrates.
NabumetoneNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
NadroparinAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
NaproxenNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
NateglinideMay decrease the serum concentration of CYP3A4 Substrates.
NefazodoneMay decrease the serum concentration of CYP3A4 Substrates.
NelfinavirMay decrease the serum concentration of CYP3A4 Substrates.
NevirapineMay decrease the serum concentration of CYP3A4 Substrates.
NifedipineMay decrease the serum concentration of CYP3A4 Substrates.
NilotinibMay decrease the serum concentration of CYP3A4 Substrates.
NimodipineMay decrease the serum concentration of CYP3A4 Substrates.
NisoldipineMay decrease the serum concentration of CYP3A4 Substrates.
NorelgestrominMay decrease the serum concentration of CYP3A4 Substrates.
NorethindroneMay decrease the serum concentration of CYP3A4 Substrates.
NorgestimateMay decrease the serum concentration of CYP3A4 Substrates.
OlanzapineMay increase the serum concentration of CYP1A2 Substrates.
OndansetronMay decrease the serum concentration of CYP3A4 Substrates.
OspemifeneMay decrease the serum concentration of CYP3A4 Substrates.
OxaprozinNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
OxycodoneMay decrease the serum concentration of CYP3A4 Substrates.
PamidronateBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
PanobinostatMay decrease the serum concentration of CYP3A4 Substrates.
PazopanibMay decrease the serum concentration of CYP3A4 Substrates.
PerampanelMay decrease the serum concentration of CYP3A4 Substrates.
PhenindioneMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
PhenobarbitalPHENobarbital may decrease the serum concentration of Deferasirox.
PhenprocoumonMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
PhenytoinPhenytoin may decrease the serum concentration of Deferasirox.
PimozideMay decrease the serum concentration of CYP3A4 Substrates.
PioglitazoneMay increase the serum concentration of CYP2C8 Substrates.
PiperazineMay decrease the serum concentration of CYP3A4 Substrates.
PipotiazineMay decrease the serum concentration of CYP3A4 Substrates.
PirfenidoneCYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pirfenidone.
PiroxicamNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
PomalidomideMay decrease the serum concentration of CYP3A4 Substrates.
PraziquantelMay decrease the serum concentration of CYP3A4 Substrates.
PrednicarbateCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
PrednisoneCorticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
PrimaquineMay decrease the serum concentration of CYP3A4 Substrates.
ProgesteroneMay decrease the serum concentration of CYP3A4 Substrates.
PropranololMay increase the serum concentration of CYP1A2 Substrates.
QuetiapineMay decrease the serum concentration of CYP3A4 Substrates.
QuinidineMay decrease the serum concentration of CYP3A4 Substrates.
QuinineMay decrease the serum concentration of CYP3A4 Substrates.
RabeprazoleMay decrease the serum concentration of CYP3A4 Substrates.
RamelteonMay increase the serum concentration of CYP1A2 Substrates.
RanolazineMay decrease the serum concentration of CYP3A4 Substrates.
RasagilineMay increase the serum concentration of CYP1A2 Substrates.
RegorafenibMay decrease the serum concentration of CYP3A4 Substrates.
RepaglinideMay increase the serum concentration of Repaglinide.
RifampicinRifampin may decrease the serum concentration of Deferasirox.
RilpivirineMay decrease the serum concentration of CYP3A4 Substrates.
RimexoloneCorticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
RiociguatMay decrease the serum concentration of CYP3A4 Substrates.
RisedronateBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
RitonavirRitonavir may decrease the serum concentration of Deferasirox.
RivaroxabanMay decrease the serum concentration of CYP3A4 Substrates.
RoflumilastMay decrease the serum concentration of CYP3A4 Substrates.
RopiniroleMay increase the serum concentration of CYP1A2 Substrates.
RopivacaineMay increase the serum concentration of CYP1A2 Substrates.
RosiglitazoneMay increase the serum concentration of CYP2C8 Substrates.
RuxolitinibMay decrease the serum concentration of CYP3A4 Substrates.
SaquinavirMay decrease the serum concentration of CYP3A4 Substrates.
SaxagliptinCYP3A4 Inducers may decrease the serum concentration of Saxagliptin.
SildenafilMay decrease the serum concentration of CYP3A4 Substrates.
SilodosinMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay decrease the serum concentration of CYP3A4 Substrates.
SimvastatinMay decrease the serum concentration of CYP3A4 Substrates.
SirolimusMay decrease the serum concentration of CYP3A4 Substrates.
SolifenacinMay decrease the serum concentration of CYP3A4 Substrates.
SpiramycinMay decrease the serum concentration of CYP3A4 Substrates.
SulfamethoxazoleMay decrease the serum concentration of CYP3A4 Substrates.
SulfisoxazoleMay decrease the serum concentration of CYP3A4 Substrates.
SulindacNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
SulodexideMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
SunitinibMay decrease the serum concentration of CYP3A4 Substrates.
SuvorexantMay decrease the serum concentration of CYP3A4 Substrates.
TamoxifenMay decrease the serum concentration of CYP3A4 Substrates.
TamsulosinMay decrease the serum concentration of CYP3A4 Substrates.
TelaprevirMay decrease the serum concentration of CYP3A4 Substrates.
TelithromycinMay decrease the serum concentration of CYP3A4 Substrates.
TemsirolimusMay decrease the serum concentration of CYP3A4 Substrates.
TeniposideMay decrease the serum concentration of CYP3A4 Substrates.
TetracyclineMay decrease the serum concentration of CYP3A4 Substrates.
TheophyllineMay increase the serum concentration of Theophylline.
ThiothixeneMay increase the serum concentration of CYP1A2 Substrates.
TiagabineMay decrease the serum concentration of CYP3A4 Substrates.
Tiaprofenic acidNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
TicagrelorMay decrease the serum concentration of CYP3A4 Substrates.
TiclopidineMay decrease the serum concentration of CYP3A4 Substrates.
TiludronateBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
TinzaparinAnticoagulants may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
TipranavirMay decrease the serum concentration of CYP3A4 Substrates.
TizanidineMay increase the serum concentration of CYP1A2 Substrates.
TofacitinibMay decrease the serum concentration of CYP3A4 Substrates.
TolmetinNonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
TolterodineMay decrease the serum concentration of CYP3A4 Substrates.
TolvaptanMay decrease the serum concentration of CYP3A4 Substrates.
ToremifeneMay decrease the serum concentration of CYP3A4 Substrates.
TrabectedinMay decrease the serum concentration of CYP3A4 Substrates.
TramadolMay decrease the serum concentration of CYP3A4 Substrates.
TreprostinilMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
TretinoinMay increase the serum concentration of CYP2C8 Substrates.
TriazolamMay decrease the serum concentration of CYP3A4 Substrates.
TrifluoperazineMay increase the serum concentration of CYP1A2 Substrates.
TrimethoprimMay decrease the serum concentration of CYP3A4 Substrates.
TrimipramineMay decrease the serum concentration of CYP3A4 Substrates.
UlipristalMay decrease the serum concentration of CYP3A4 Substrates.
VandetanibMay decrease the serum concentration of CYP3A4 Substrates.
VemurafenibMay decrease the serum concentration of CYP3A4 Substrates.
VenlafaxineMay decrease the serum concentration of CYP3A4 Substrates.
VilazodoneMay decrease the serum concentration of CYP3A4 Substrates.
VinblastineMay decrease the serum concentration of CYP3A4 Substrates.
VincristineMay decrease the serum concentration of CYP3A4 Substrates.
VinorelbineMay decrease the serum concentration of CYP3A4 Substrates.
WarfarinMay enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ZoledronateBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
ZolpidemMay decrease the serum concentration of CYP3A4 Substrates.
ZonisamideMay decrease the serum concentration of CYP3A4 Substrates.
ZopicloneMay decrease the serum concentration of CYP3A4 Substrates.
Food Interactions
  • Dispersion in carbonated drinks or milk is not recommended due to foaming and slow dispersion, respectively.
  • Food causes inconsistent increases in the bioavailability of this product.
  • Tablets should be completely dispersed in water, orange juice or apple juice and the resulting suspension should be ingested immediately (after swallowing the suspension, any residue should be resuspended in a small volume of liquid and swallowed).
  • Tablets should be taken on an empty stomach at least 30 minutes before a meal, preferably at the same time everyday.

Targets

1. Iron

Kind: small molecule

Organism: Human

Pharmacological action: yes

Actions: chelator

Components

Name UniProt ID Details

References:

  1. Wang T, Gao C, Chen BA: [Deferasirox—a new oral iron chelator—review]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2010 Oct;18(5):1359-64. Pubmed
  2. Ibrahim AS, Spellberg B, Edwards J Jr: Iron acquisition: a novel perspective on mucormycosis pathogenesis and treatment. Curr Opin Infect Dis. 2008 Dec;21(6):620-5. Pubmed
  3. Devanur LD, Evans RW, Evans PJ, Hider RC: Chelator-facilitated removal of iron from transferrin: relevance to combined chelation therapy. Biochem J. 2008 Jan 15;409(2):439-47. Pubmed
  4. Lebitasy M, Ampe E, Hecq JD, Karmani L, Nick H, Galanti L: Ability of deferasirox to bind iron during measurement of iron. Clin Chem Lab Med. 2010 Mar;48(3):427-9. Pubmed
  5. Yang LP, Keam SJ, Keating GM: Deferasirox : a review of its use in the management of transfusional chronic iron overload. Drugs. 2007;67(15):2211-30. Pubmed
  6. Choudhry VP, Naithani R: Current status of iron overload and chelation with deferasirox. Indian J Pediatr. 2007 Aug;74(8):759-64. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Skerjanec A, Wang J, Maren K, Rojkjaer L: Investigation of the pharmacokinetic interactions of deferasirox, a once-daily oral iron chelator, with midazolam, rifampin, and repaglinide in healthy volunteers. J Clin Pharmacol. 2010 Feb;50(2):205-13. Epub 2009 Nov 25. Pubmed

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Drug created on August 29, 2007 13:21 / Updated on September 16, 2013 17:15