deferasirox 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antacids, aluminium derivatives 3128 201530-41-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ICL670A
  • ICL-670A
  • ICL 670A
  • deferasirox
  • exjade
A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.
  • Molecular weight: 373.37
  • Formula: C21H15N3O4
  • CLOGP: 3.95
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 108.47
  • ALOGS: -4.04
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 70 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.84 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.05 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.04 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK2,CDK5,CDK9,CHEK1,CLK4,CSF1R,DDR1,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,IRAK1,ITK,JAK1,JAK2,KDR,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MKNK2,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PRKAA1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,UHMK1,ULK1,ULK2,ZAP70 88
kinase-selectivity-class ACVR2A,ACVR2B,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,MAPK7,PRKDC,SIK2,STK33,TTK 14
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Sept. 26, 2019 EMA Mylan S.A.S
Nov. 2, 2005 FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sickle cell anaemia with crisis 2836.16 17.54 589 21584 6708 90599566
Serum ferritin increased 1304.57 17.54 313 21860 7068 90599206
Death 460.71 17.54 561 21612 455990 90150284
Haemoglobin decreased 340.35 17.54 296 21877 161660 90444614
Blood iron increased 314.72 17.54 77 22096 1882 90604392
Blood creatinine increased 296.85 17.54 225 21948 101161 90505113
Diarrhoea 205.88 17.54 597 21576 938593 89667681
Sickle cell anaemia 176.26 17.54 39 22134 603 90605671
Iron overload 163.17 17.54 40 22133 985 90605289
Abdominal pain 135.91 17.54 299 21874 395422 90210852
Blood bilirubin increased 132.68 17.54 99 22074 43371 90562903
Blood urea increased 127.18 17.54 84 22089 30329 90575945
Aspartate aminotransferase increased 118.82 17.54 136 22037 102801 90503473
Sickle cell disease 117.24 17.54 21 22152 98 90606176
Alanine aminotransferase increased 114.65 17.54 143 22030 118195 90488079
Drug ineffective 109.62 17.54 107 22066 1384191 89222083
Pyrexia 109.35 17.54 382 21791 660103 89946171
Platelet count decreased 102.67 17.54 146 22027 136823 90469451
Proteinuria 101.45 17.54 66 22107 23225 90583049
Renal disorder 97.57 17.54 78 22095 37781 90568493
Off label use 95.75 17.54 78 22095 1102174 89504100
Myelodysplastic syndrome transformation 94.62 17.54 22 22151 429 90605845
Hyperammonaemia 94.01 17.54 41 22132 6434 90599840
Haematocrit decreased 92.79 17.54 79 22094 41753 90564521
Haemochromatosis 89.43 17.54 23 22150 691 90605583
Acute myeloid leukaemia 88.70 17.54 58 22115 20582 90585692
Neoplasm malignant 87.72 17.54 70 22103 33810 90572464
Glycosuria 86.17 17.54 26 22147 1416 90604858
Infusion related reaction 85.23 17.54 4 22169 416776 90189498
Renal impairment 84.39 17.54 116 22057 105305 90500969
Renal failure 84.29 17.54 130 22043 130877 90475397
Myelodysplastic syndrome 80.81 17.54 55 22118 20848 90585426
Renal tubular disorder 80.12 17.54 30 22143 3177 90603097
Chromaturia 77.80 17.54 52 22121 19135 90587139
Serum ferritin decreased 74.71 17.54 27 22146 2587 90603687
Systemic lupus erythematosus 72.31 17.54 4 22169 361892 90244382
Fanconi syndrome acquired 71.97 17.54 22 22151 1252 90605022
Haemosiderosis 69.92 17.54 15 22158 199 90606075
Arthropathy 67.54 17.54 6 22167 366236 90240038
Leukaemia 67.28 17.54 30 22143 4962 90601312
Splenomegaly 67.25 17.54 41 22132 12883 90593391
Metabolic acidosis 66.64 17.54 75 22098 55601 90550673
Blood lactate dehydrogenase increased 63.78 17.54 52 22121 25880 90580394
Hepatomegaly 63.57 17.54 40 22133 13286 90592988
Blood alkaline phosphatase increased 63.14 17.54 68 22105 48011 90558263
Drug hypersensitivity 62.50 17.54 18 22155 463591 90142683
Hospitalisation 60.86 17.54 111 22062 127989 90478285
Haemolysis 60.29 17.54 33 22140 8477 90597797
Glossodynia 60.07 17.54 5 22168 321774 90284500
Therapy cessation 59.69 17.54 58 22115 36303 90569971
Sepsis 59.43 17.54 134 22039 179680 90426594
Joint swelling 58.49 17.54 25 22148 503275 90102999
Paroxysmal nocturnal haemoglobinuria 58.35 17.54 14 22159 314 90605960
Cardiac iron overload 57.80 17.54 9 22164 13 90606261
Anaemia 56.37 17.54 202 21971 352600 90253674
Abdominal pain upper 54.45 17.54 192 21981 332482 90273792
Pericarditis 53.91 17.54 3 22170 270148 90336126
Renal tubular acidosis 51.86 17.54 20 22153 2295 90603979
Hepatic failure 50.09 17.54 55 22118 39673 90566601
Vomiting 49.62 17.54 346 21827 787947 89818327
Malaise 49.21 17.54 277 21896 585709 90020565
Acute leukaemia 48.32 17.54 16 22157 1180 90605094
Jaundice 48.07 17.54 49 22124 32468 90573806
Musculoskeletal stiffness 47.01 17.54 8 22165 296524 90309750
Product dose omission issue 46.56 17.54 167 22006 291520 90314754
Pancytopenia 45.87 17.54 95 22078 120168 90486106
Product use in unapproved indication 45.39 17.54 13 22160 336223 90270051
Liver function test abnormal 45.33 17.54 59 22114 50786 90555488
Acute chest syndrome 44.96 17.54 15 22158 1133 90605141
Nausea 44.49 17.54 440 21733 1109876 89496398
Therapy interrupted 44.45 17.54 58 22115 50050 90556224
Hypophosphataemia 43.46 17.54 33 22140 14821 90591453
Red blood cell count decreased 43.23 17.54 55 22118 46296 90559978
Impaired healing 42.72 17.54 4 22169 234195 90372079
Wound 42.23 17.54 11 22162 302969 90303305
Reticulocyte count increased 41.66 17.54 14 22159 1081 90605193
Treatment failure 40.56 17.54 12 22161 303916 90302358
Intentional product use issue 38.78 17.54 4 22169 216888 90389386
Type 2 diabetes mellitus 38.35 17.54 3 22170 203241 90403033
Sinusitis 38.32 17.54 18 22155 343070 90263204
Pneumonia 38.29 17.54 277 21896 637782 89968492
Discomfort 38.15 17.54 10 22163 274325 90331949
Liver disorder 37.42 17.54 88 22085 121181 90485093
Injury 36.99 17.54 3 22170 197346 90408928
Wheezing 36.48 17.54 7 22166 238073 90368201
Stomatitis 36.37 17.54 11 22162 274687 90331587
Therapeutic product effect incomplete 36.20 17.54 3 22170 193893 90412381
White blood cell count decreased 35.97 17.54 106 22067 167003 90439271
Duodenal ulcer perforation 34.99 17.54 6 22167 221282 90384992
Ammonia increased 34.40 17.54 19 22154 4967 90601307
Product use issue 34.32 17.54 19 22154 329900 90276374
Irritable bowel syndrome 34.21 17.54 5 22168 207443 90398831
Blister 34.14 17.54 10 22163 254988 90351286
Hepatic function abnormal 34.13 17.54 49 22124 46239 90560035
Helicobacter infection 34.06 17.54 7 22166 226843 90379431
Osteoarthritis 34 17.54 4 22169 195726 90410548
Faeces discoloured 33.11 17.54 33 22140 21287 90584987
Thrombocytopenia 32.85 17.54 119 22054 208606 90397668
Hepatic siderosis 32.64 17.54 5 22168 6 90606268
Fungal endocarditis 32.56 17.54 9 22164 358 90605916
Alopecia 31.70 17.54 45 22128 495026 90111248
Lower respiratory tract infection 31.48 17.54 11 22162 250648 90355626
Serum ferritin abnormal 31.08 17.54 8 22165 241 90606033
Infective aneurysm 30.99 17.54 9 22164 429 90605845
Maculopathy 30.41 17.54 14 22159 2492 90603782
Sleep disorder 29.96 17.54 6 22167 198024 90408250
Ocular icterus 29.77 17.54 16 22157 3964 90602310
Hyperammonaemic encephalopathy 29.42 17.54 14 22159 2685 90603589
Liver iron concentration increased 29.18 17.54 5 22168 17 90606257
Arthralgia 28.22 17.54 97 22076 778425 89827849
Asthma 28.14 17.54 12 22161 242148 90364126
Blood product transfusion dependent 28.08 17.54 7 22166 185 90606089
Hypertension 27.91 17.54 43 22130 457489 90148785
Anxiety 27.90 17.54 21 22152 309751 90296523
Depression 27.57 17.54 20 22153 300581 90305693
Acute haemorrhagic ulcerative colitis 27.41 17.54 6 22167 88 90606186
Nasopharyngitis 27.06 17.54 36 22137 407068 90199206
Swelling 26.90 17.54 38 22135 419020 90187254
Colitis erosive 26.76 17.54 7 22166 225 90606049
White blood cell count increased 26.67 17.54 54 22119 67187 90539087
Yersinia infection 26.58 17.54 5 22168 32 90606242
Hepatic encephalopathy 26.50 17.54 24 22149 13748 90592526
Viral infection 26.47 17.54 41 22132 41373 90564901
Gamma-glutamyltransferase increased 26.28 17.54 39 22134 37913 90568361
Treatment noncompliance 26.05 17.54 46 22127 51681 90554593
Enterocolitis 25.72 17.54 21 22152 10469 90595805
Ill-defined disorder 25.21 17.54 7 22166 184884 90421390
Beta 2 microglobulin urine increased 24.79 17.54 5 22168 48 90606226
Eye infection bacterial 24.75 17.54 7 22166 303 90605971
Hypersensitivity 24.72 17.54 46 22127 454631 90151643
Acidosis hyperchloraemic 24.56 17.54 9 22164 897 90605377
Full blood count decreased 24.23 17.54 33 22140 29656 90576618
Peripheral swelling 24.08 17.54 40 22133 413066 90193208
Fanconi syndrome 24.04 17.54 11 22162 1932 90604342
Thalassaemia beta 23.98 17.54 4 22169 11 90606263
Hypersplenism 23.47 17.54 7 22166 366 90605908
Aplastic anaemia 23.35 17.54 22 22151 13247 90593027
Retinopathy sickle cell 23.19 17.54 5 22168 68 90606206
Coombs negative haemolytic anaemia 23.11 17.54 7 22166 386 90605888
Transformation to acute myeloid leukaemia 23.01 17.54 7 22166 392 90605882
Hepatic pain 22.90 17.54 13 22160 3582 90602692
Investigation 22.82 17.54 10 22163 1587 90604687
Cytotoxic oedema 22.76 17.54 6 22167 199 90606075
Transaminases increased 22.63 17.54 36 22137 37156 90569118
Reticulocyte count decreased 21.82 17.54 7 22166 467 90605807
Bone marrow transplant 21.32 17.54 8 22165 852 90605422
Hypoacusis 21.29 17.54 30 22143 27820 90578454
Hypouricaemia 21.25 17.54 6 22167 258 90606016
Injection site pain 21.16 17.54 8 22165 173691 90432583
Duodenal ulcer 21.09 17.54 18 22155 9534 90596740
Haematemesis 21.01 17.54 33 22140 33693 90572581
Hypoaesthesia 20.65 17.54 28 22145 314182 90292092
Toxicity to various agents 20.64 17.54 24 22149 287822 90318452
Urine output decreased 20.48 17.54 20 22153 12583 90593691
Contusion 20.20 17.54 19 22154 251197 90355077
Neutrophil count decreased 20.01 17.54 50 22123 71482 90534792
Dry mouth 20.01 17.54 10 22163 184049 90422225
Transfusion 19.97 17.54 23 22150 17465 90588809
Bursitis 19.88 17.54 4 22169 131650 90474624
Myelofibrosis 19.79 17.54 9 22164 1558 90604716
Insomnia 19.69 17.54 32 22141 333442 90272832
Extravascular haemolysis 19.63 17.54 6 22167 341 90605933
Confusional state 19.32 17.54 41 22132 386164 90220110
Basophil count increased 19.06 17.54 8 22165 1143 90605131
Adverse event 18.97 17.54 3 22170 117415 90488859
Loss of personal independence in daily activities 18.84 17.54 5 22168 136100 90470174
Apparent death 18.66 17.54 8 22165 1204 90605070
Foetal haemoglobin increased 18.65 17.54 3 22170 6 90606268
Eye colour change 18.65 17.54 6 22167 404 90605870
Blood creatinine abnormal 18.64 17.54 12 22161 4145 90602129
COVID-19 18.62 17.54 9 22164 168834 90437440
Deafness 18.33 17.54 25 22148 22489 90583785
Platelet count increased 18.27 17.54 24 22149 20835 90585439
Bone marrow failure 17.99 17.54 30 22143 32191 90574083
Wrong technique in product usage process 17.94 17.54 48 22125 71523 90534751
Cholestasis 17.91 17.54 32 22141 36267 90570007
Blood disorder 17.86 17.54 15 22158 7775 90598499
Condition aggravated 17.84 17.54 80 22093 595465 90010809
Coombs positive haemolytic anaemia 17.60 17.54 6 22167 484 90605790

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sickle cell anaemia with crisis 1136.24 15.50 301 22178 4589 42594267
Serum ferritin increased 911.70 15.50 276 22203 6943 42591913
Death 407.56 15.50 814 21665 470371 42128485
Blood creatinine increased 312.12 15.50 335 22144 109668 42489188
Haemoglobin decreased 258.42 15.50 333 22146 132138 42466718
Blood iron increased 214.30 15.50 58 22421 958 42597898
Myelodysplastic syndrome 170.92 15.50 121 22358 22624 42576232
Blood urea increased 151.83 15.50 131 22348 32662 42566194
Neoplasm malignant 139.35 15.50 107 22372 22636 42576220
Platelet count decreased 132.47 15.50 251 22228 138330 42460526
Diarrhoea 128.09 15.50 530 21949 460319 42138537
Iron overload 124.70 15.50 42 22437 1493 42597363
Off label use 116.53 15.50 100 22379 638235 41960621
Myelodysplastic syndrome transformation 115.97 15.50 31 22448 487 42598369
Serum ferritin abnormal 114.18 15.50 27 22452 249 42598607
Acute myeloid leukaemia 109.31 15.50 92 22387 22164 42576692
Acute leukaemia 101.20 15.50 34 22445 1199 42597657
Blood bilirubin increased 97.85 15.50 116 22363 42136 42556720
Pyrexia 95.30 15.50 435 22044 393607 42205249
Myelofibrosis 91.35 15.50 35 22444 1812 42597044
Renal disorder 88.55 15.50 92 22387 28888 42569968
Blast cell count increased 86.78 15.50 30 22449 1155 42597701
Aspartate aminotransferase increased 82.74 15.50 147 22332 77016 42521840
Alanine aminotransferase increased 78.08 15.50 155 22324 88251 42510605
White blood cell count decreased 77.22 15.50 176 22303 110220 42488636
Sickle cell anaemia 72.59 15.50 19 22460 274 42598582
Splenomegaly 70.67 15.50 64 22415 16983 42581873
Haematocrit decreased 68.19 15.50 88 22391 34820 42564036
Red blood cell count decreased 67.90 15.50 85 22394 32630 42566226
Drug ineffective 62.18 15.50 152 22327 630045 41968811
Haemochromatosis 61.99 15.50 23 22456 1089 42597767
Toxicity to various agents 61.59 15.50 22 22457 229114 42369742
Drug interaction 60.20 15.50 33 22446 266966 42331890
Abdominal pain 57.24 15.50 225 22254 190246 42408610
Renal failure 56.13 15.50 185 22294 143541 42455315
White blood cell count increased 55.01 15.50 91 22388 44996 42553860
Abdominal pain upper 52.59 15.50 127 22352 82482 42516374
Creatinine renal clearance decreased 51.88 15.50 29 22450 3584 42595272
Nephrolithiasis 51.33 15.50 79 22400 36751 42562105
Renal impairment 46.75 15.50 146 22333 110082 42488774
Blood lactate dehydrogenase increased 46.68 15.50 63 22416 26018 42572838
Jaundice 46.54 15.50 73 22406 34516 42564340
Acute chest syndrome 44.98 15.50 18 22461 1047 42597809
Pneumonia 44.73 15.50 377 22102 421772 42177084
Leukaemia 44.01 15.50 31 22448 5741 42593115
Neutrophil count decreased 43.07 15.50 100 22379 63315 42535541
Haemosiderosis 42.83 15.50 13 22466 328 42598528
Fanconi syndrome acquired 42.19 15.50 21 22458 2049 42596807
Liver function test abnormal 41.70 15.50 67 22412 32324 42566532
Hyperammonaemia 41.69 15.50 34 22445 7832 42591024
Product use in unapproved indication 41.24 15.50 23 22456 184433 42414423
Blood alkaline phosphatase increased 39.89 15.50 67 22412 33530 42565326
Serum ferritin decreased 39.62 15.50 16 22463 953 42597903
Urea cycle disorder 39.29 15.50 6 22473 0 42598856
Liver disorder 38.00 15.50 72 22407 39572 42559284
Completed suicide 36.75 15.50 4 22475 96461 42502395
Sickle cell disease 36.45 15.50 10 22469 174 42598682
Overdose 36.22 15.50 6 22473 105258 42493598
Gastrointestinal pain 34.33 15.50 24 22455 4391 42594465
Glycosuria 34.29 15.50 16 22463 1354 42597502
Haemolysis 33.97 15.50 33 22446 9556 42589300
Vomiting 32.89 15.50 263 22216 289460 42309396
Malaise 32.44 15.50 207 22272 211949 42386907
Chromaturia 32.30 15.50 41 22438 15948 42582908
Hepatic enzyme increased 31.96 15.50 73 22406 45711 42553145
Deafness 31.93 15.50 37 22442 13103 42585753
Anaemia 31.57 15.50 254 22225 280024 42318832
Drug hypersensitivity 31.37 15.50 7 22472 99382 42499474
Cholelithiasis 31.02 15.50 49 22430 23297 42575559
Anxiety 29.17 15.50 13 22466 118547 42480309
Extramedullary haemopoiesis 28.60 15.50 8 22471 150 42598706
Rhabdomyolysis 27.86 15.50 4 22475 78015 42520841
Fanconi syndrome 27.40 15.50 15 22464 1779 42597077
Intentional product use issue 27.31 15.50 3 22476 71830 42527026
Blood pressure increased 26.98 15.50 10 22469 101918 42496938
Hypotension 26.96 15.50 60 22419 257571 42341285
Retinal dystrophy 26.07 15.50 5 22474 14 42598842
Hepatic failure 25.76 15.50 60 22419 38040 42560816
Sepsis 25.40 15.50 186 22293 199148 42399708
Infection 24.88 15.50 121 22358 111947 42486909
Proteinuria 24.87 15.50 44 22435 22939 42575917
Hypertension 24.85 15.50 31 22448 167173 42431683
Paroxysmal nocturnal haemoglobinuria 24.60 15.50 7 22472 140 42598716
Moyamoya disease 24.51 15.50 5 22474 21 42598835
Blood product transfusion dependent 23.90 15.50 9 22470 444 42598412
Bone marrow transplant 23.86 15.50 12 22467 1197 42597659
Therapy cessation 23.23 15.50 40 22439 20410 42578446
Hypoacusis 23.13 15.50 38 22441 18664 42580192
Abdominal discomfort 22.62 15.50 89 22390 75166 42523690
Decreased immune responsiveness 22.54 15.50 14 22465 2101 42596755
Intentional product misuse 22.51 15.50 3 22476 61897 42536959
Aplasia pure red cell 22.32 15.50 23 22456 7143 42591713
Urine output decreased 22.15 15.50 28 22451 10845 42588011
Thrombocytopenia 21.69 15.50 173 22306 190106 42408750
Hospitalisation 20.81 15.50 86 22393 74244 42524612
Depression 20.70 15.50 17 22462 111346 42487510
Hyperhidrosis 20.62 15.50 11 22468 90501 42508355
Transfusion reaction 20.46 15.50 10 22469 938 42597918
Asthma 20.46 15.50 4 22475 62310 42536546
Concomitant disease progression 20.38 15.50 14 22465 2489 42596367
Tremor 20.35 15.50 13 22466 96916 42501940
Blood calcium decreased 20.12 15.50 27 22452 11081 42587775
Hepatic siderosis 19.97 15.50 6 22473 146 42598710
Alloimmunisation 19.64 15.50 3 22476 0 42598856
Neuropathy peripheral 19.62 15.50 15 22464 101838 42497018
Wheezing 19.11 15.50 3 22476 54778 42544078
Musculoskeletal stiffness 18.36 15.50 4 22475 57761 42541095
Bone marrow disorder 18.31 15.50 12 22467 1974 42596882
Neutrophilic panniculitis 18.28 15.50 4 22475 25 42598831
Disease progression 18.25 15.50 134 22345 143522 42455334
Renal colic 17.87 15.50 12 22467 2056 42596800
COVID-19 17.74 15.50 21 22458 115927 42482929
Bradycardia 17.23 15.50 12 22467 85472 42513384
Complications of bone marrow transplant 17.11 15.50 6 22473 241 42598615
Renal tubular acidosis 16.96 15.50 13 22466 2737 42596119
Pulmonary embolism 16.91 15.50 23 22456 119589 42479267
Retinopathy 16.81 15.50 12 22467 2269 42596587
Injection site pain 16.46 15.50 5 22474 57793 42541063
Myocardial infarction 16.40 15.50 25 22454 123984 42474872
Transaminases increased 16.23 15.50 46 22433 32839 42566017
Pancytopenia 16.21 15.50 112 22367 117631 42481225
Glomerular filtration rate decreased 16.03 15.50 30 22449 16321 42582535
Hepatomegaly 16.02 15.50 25 22454 11760 42587096
Splenic embolism 15.99 15.50 6 22473 293 42598563
Condition aggravated 15.95 15.50 77 22402 260677 42338179
Hyponatraemia 15.93 15.50 18 22461 101444 42497412
Electrocardiogram QT prolonged 15.90 15.50 3 22476 47942 42550914
Reticulocyte count increased 15.80 15.50 8 22471 809 42598047
Renal function test abnormal 15.75 15.50 13 22466 3044 42595812
Foetal exposure during pregnancy 15.61 15.50 3 22476 47308 42551548

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sickle cell anaemia with crisis 2515.80 16.80 568 28710 8977 110551044
Serum ferritin increased 1390.94 16.80 368 28910 11479 110548542
Death 1056.78 16.80 1098 28180 697771 109862250
Blood creatinine increased 467.78 16.80 387 28891 182502 110377519
Haemoglobin decreased 402.18 16.80 407 28871 248320 110311701
Blood iron increased 290.10 16.80 75 29203 2123 110557898
Diarrhoea 213.69 16.80 723 28555 1138782 109421239
Blood urea increased 207.84 16.80 147 29131 54810 110505211
Platelet count decreased 200.88 16.80 275 29003 230168 110329853
Myelodysplastic syndrome 184.26 16.80 118 29160 37366 110522655
Sickle cell anaemia 180.05 16.80 42 29236 765 110559256
Iron overload 165.45 16.80 48 29230 2103 110557918
Aspartate aminotransferase increased 156.40 16.80 202 29076 159734 110400287
Alanine aminotransferase increased 150.63 16.80 213 29065 183560 110376461
Pyrexia 148.94 16.80 548 28730 897717 109662304
Hyperammonaemia 146.70 16.80 72 29206 13660 110546361
Blood bilirubin increased 140.46 16.80 134 29144 75838 110484183
Abdominal pain 132.57 16.80 365 28913 512624 110047397
Acute myeloid leukaemia 121.55 16.80 92 29186 38018 110522003
Renal impairment 114.30 16.80 190 29088 188255 110371766
Fanconi syndrome acquired 105.54 16.80 37 29241 2997 110557024
White blood cell count decreased 105.48 16.80 205 29073 229185 110330836
Renal disorder 104.46 16.80 94 29184 49385 110510636
Glycosuria 102.82 16.80 35 29243 2595 110557426
Serum ferritin abnormal 102.48 16.80 24 29254 445 110559576
Neoplasm malignant 99.72 16.80 81 29197 37062 110522959
Myelofibrosis 97.74 16.80 35 29243 3016 110557005
Myelodysplastic syndrome transformation 93.98 16.80 25 29253 792 110559229
Drug ineffective 91.37 16.80 165 29113 1520375 109039646
Off label use 90.85 16.80 162 29116 1500023 109059998
Haemochromatosis 86.34 16.80 27 29251 1530 110558491
Renal failure 84.75 16.80 186 29092 226388 110333633
Metabolic acidosis 83.71 16.80 117 29161 99627 110460394
Therapy cessation 82.65 16.80 79 29199 44778 110515243
Haematocrit decreased 81.61 16.80 94 29184 66023 110493998
Infusion related reaction 81.04 16.80 5 29273 381157 110178864
Splenomegaly 80.02 16.80 60 29218 24438 110535583
Renal tubular acidosis 79.62 16.80 34 29244 4681 110555340
Hospitalisation 78.88 16.80 138 29140 142355 110417666
Red blood cell count decreased 78.48 16.80 92 29186 65831 110494190
Blast cell count increased 76.82 16.80 25 29253 1612 110558409
Anaemia 76.65 16.80 317 28961 546769 110013252
Haemosiderosis 72.58 16.80 19 29259 565 110559456
Blood lactate dehydrogenase increased 72.22 16.80 73 29205 44261 110515760
Drug hypersensitivity 72.14 16.80 16 29262 454074 110105947
Proteinuria 70.94 16.80 69 29209 39949 110520072
Renal tubular disorder 70.64 16.80 36 29242 7393 110552628
Product dose omission issue 66.75 16.80 212 29066 321570 110238451
Blood alkaline phosphatase increased 65.24 16.80 87 29191 70848 110489173
Haemolysis 64.16 16.80 44 29234 15595 110544426
Jaundice 62.87 16.80 78 29200 59158 110500863
Liver function test abnormal 62.55 16.80 84 29194 68866 110491155
Chromaturia 62.40 16.80 56 29222 29304 110530717
Leukaemia 61.68 16.80 33 29245 7485 110552536
Serum ferritin decreased 58.50 16.80 24 29254 2990 110557031
Paroxysmal nocturnal haemoglobinuria 58.47 16.80 15 29263 411 110559610
Neutrophil count decreased 56.65 16.80 109 29169 120832 110439189
Nephrolithiasis 56.03 16.80 78 29200 66134 110493887
Hepatic failure 53.78 16.80 78 29200 68661 110491360
Contraindicated product administered 53.53 16.80 3 29275 248264 110311757
Product use in unapproved indication 53.16 16.80 26 29252 447351 110112670
Thrombocytopenia 52.63 16.80 207 29071 348678 110211343
Sepsis 52.47 16.80 198 29080 327148 110232873
Abdominal pain upper 51.75 16.80 206 29072 348905 110211116
Vomiting 51.45 16.80 414 28864 910261 109649760
Joint swelling 50.73 16.80 27 29251 442818 110117203
Musculoskeletal stiffness 50.64 16.80 7 29271 279815 110280206
Urea cycle disorder 49.71 16.80 9 29269 41 110559980
Wheezing 49.62 16.80 5 29273 255225 110304796
Anxiety 49.36 16.80 15 29263 345063 110214958
Completed suicide 49.13 16.80 4 29274 242377 110317644
Fanconi syndrome 48.50 16.80 22 29256 3497 110556524
Mobility decreased 47.90 16.80 4 29274 237418 110322603
Acute leukaemia 47.38 16.80 18 29260 1831 110558190
Glossodynia 46.90 16.80 3 29275 222001 110338020
Pericarditis 46.18 16.80 3 29275 219111 110340910
Toxicity to various agents 45.92 16.80 36 29242 480519 110079502
Intentional product use issue 45.34 16.80 6 29272 247900 110312121
Acute chest syndrome 45.13 16.80 18 29260 2085 110557936
White blood cell count increased 45.00 16.80 87 29191 96755 110463266
Arthropathy 43.91 16.80 11 29267 287511 110272510
Sickle cell disease 42.47 16.80 10 29268 190 110559831
Therapeutic product effect decreased 42.17 16.80 7 29271 244309 110315712
Asthma 41.41 16.80 8 29270 250283 110309738
Sinusitis 40.47 16.80 14 29264 296674 110263347
Arthralgia 40.29 16.80 92 29186 779540 109780481
Treatment failure 39.73 16.80 12 29266 277222 110282799
Hepatic siderosis 39.11 16.80 9 29269 154 110559867
Transaminases increased 38.49 16.80 64 29214 63326 110496695
Hypoacusis 38.40 16.80 47 29231 35144 110524877
Helicobacter infection 36.86 16.80 3 29275 181874 110378147
Depression 36.84 16.80 19 29259 317316 110242705
Hypertension 36.50 16.80 49 29229 510035 110049986
Hypophosphataemia 35.70 16.80 44 29234 33138 110526883
Overdose 35.59 16.80 9 29269 233785 110326236
Reticulocyte count increased 35.35 16.80 14 29264 1592 110558429
Cardiac iron overload 34.97 16.80 7 29271 59 110559962
Hepatomegaly 34.39 16.80 35 29243 21379 110538642
Liver iron concentration increased 34.19 16.80 6 29272 22 110559999
Hyperammonaemic encephalopathy 34.09 16.80 20 29258 5414 110554607
Investigation 33.48 16.80 15 29263 2317 110557704
Hypersplenism 33.13 16.80 11 29267 755 110559266
Endocrine disorder 32.66 16.80 12 29266 1112 110558909
Transformation to acute myeloid leukaemia 32.56 16.80 13 29265 1510 110558511
Extramedullary haemopoiesis 32.36 16.80 9 29269 338 110559683
Lower respiratory tract infection 32.25 16.80 12 29266 243094 110316927
Gastrointestinal pain 32.11 16.80 26 29252 11834 110548187
Ocular icterus 32.09 16.80 20 29258 6033 110553988
Hypoaesthesia 31.99 16.80 22 29256 314201 110245820
Pneumonia 31.74 16.80 363 28915 876351 109683670
Bone marrow transplant 31.48 16.80 13 29265 1647 110558374
Disease progression 31.43 16.80 138 29140 243896 110316125
Folliculitis 30.79 16.80 4 29274 167649 110392372
Injury 30.76 16.80 5 29273 177260 110382761
Hepatic function abnormal 30.76 16.80 71 29207 89224 110470797
Cholelithiasis 30.72 16.80 58 29220 63364 110496657
Blood pressure increased 30.69 16.80 15 29263 258358 110301663
Reticulocyte count decreased 30.63 16.80 11 29267 955 110559066
Enterocolitis 30.49 16.80 31 29247 18918 110541103
Wound 30.39 16.80 12 29266 234425 110325596
Dry mouth 29.85 16.80 8 29270 199940 110360081
Sleep disorder 29.56 16.80 8 29270 198636 110361385
Liver disorder 28.79 16.80 93 29185 142150 110417871
Confusional state 28.73 16.80 50 29228 468630 110091391
Faeces discoloured 28.73 16.80 40 29238 33908 110526113
Ammonia increased 28.72 16.80 21 29257 8229 110551792
Gamma-glutamyltransferase increased 28.38 16.80 55 29223 61254 110498767
Aplasia pure red cell 28.08 16.80 22 29256 9556 110550465
Osteoarthritis 27.85 16.80 7 29271 182616 110377405
Migraine 27.32 16.80 6 29272 171646 110388375
Alopecia 27.14 16.80 34 29244 364719 110195302
Platelet count increased 26.86 16.80 34 29244 26300 110533721
Maculopathy 26.85 16.80 14 29264 3013 110557008
Psoriasis 26.54 16.80 3 29275 139990 110420031
Duodenal ulcer 26.21 16.80 29 29249 19485 110540536
Nasopharyngitis 26.10 16.80 40 29238 394321 110165700
Infective aneurysm 25.99 16.80 11 29267 1481 110558540
Pancytopenia 25.83 16.80 117 29161 209496 110350525
Acute haemorrhagic ulcerative colitis 25.43 16.80 6 29272 115 110559906
Febrile neutropenia 25.40 16.80 157 29121 316610 110243411
Blood product transfusion dependent 25.03 16.80 8 29270 487 110559534
Drug interaction 25.01 16.80 60 29218 500123 110059898
Swelling 24.81 16.80 34 29244 351007 110209014
Colitis erosive 24.76 16.80 7 29271 279 110559742
Fungal endocarditis 24.57 16.80 9 29269 827 110559194
Bone marrow failure 24.50 16.80 50 29228 57798 110502223
Insomnia 24.42 16.80 36 29242 360554 110199467
Peripheral swelling 23.95 16.80 44 29234 403990 110156031
Thalassaemia beta 23.94 16.80 4 29274 10 110560011
Hypouricaemia 23.81 16.80 8 29270 570 110559451
Beta 2 microglobulin urine increased 23.73 16.80 6 29272 155 110559866
Therapeutic product effect incomplete 23.68 16.80 15 29263 223790 110336231
Coombs negative haemolytic anaemia 23.59 16.80 8 29270 586 110559435
Discomfort 23.26 16.80 14 29264 214693 110345328
Disease complication 22.97 16.80 16 29262 5811 110554210
Arthritis 22.69 16.80 8 29270 167578 110392443
Intentional product misuse 22.51 16.80 4 29274 132900 110427121
Stomatitis 22.48 16.80 23 29255 270219 110289802
Loss of personal independence in daily activities 22.40 16.80 6 29272 150014 110410007
Product use issue 22.21 16.80 30 29248 311665 110248356
Nausea 22.20 16.80 454 28824 1235236 109324785
Retinopathy sickle cell 22.16 16.80 5 29273 78 110559943
Hyperhidrosis 22.05 16.80 11 29267 187287 110372734
Hypothalamo-pituitary disorder 21.97 16.80 12 29266 2834 110557187
Alloimmunisation 21.96 16.80 4 29274 19 110560002
Eye infection bacterial 21.95 16.80 7 29271 423 110559598
Condition aggravated 21.95 16.80 110 29168 734726 109825295
Retinopathy 21.89 16.80 14 29264 4415 110555606
Concomitant disease progression 21.89 16.80 13 29265 3597 110556424
Treatment noncompliance 21.88 16.80 55 29223 72935 110487086
Haemoglobin S increased 21.71 16.80 3 29275 0 110560021
Retinal degeneration 21.65 16.80 10 29268 1656 110558365
Malaise 21.56 16.80 272 29006 671547 109888474
Paraesthesia 21.39 16.80 25 29253 276496 110283525
Therapy interrupted 21.02 16.80 43 29235 49779 110510242
Urine output decreased 20.81 16.80 26 29252 19850 110540171
Protein urine present 20.72 16.80 20 29258 11464 110548557
Blood creatinine abnormal 20.52 16.80 15 29263 5877 110554144
Blister 20.50 16.80 18 29260 227358 110332663
Injection site pain 20.13 16.80 11 29267 177911 110382110
Gastrointestinal haemorrhage 20.10 16.80 92 29186 165426 110394595
Duodenal ulcer perforation 20.08 16.80 11 29267 177689 110382332
Transfusion 20.05 16.80 29 29249 25443 110534578
Nephropathy toxic 19.79 16.80 30 29248 27448 110532573
Retinal dystrophy 19.75 16.80 4 29274 36 110559985
Aplastic anaemia 19.61 16.80 28 29250 24280 110535741
Hypotension 18.91 16.80 73 29205 523776 110036245
Maternal exposure during pregnancy 18.70 16.80 24 29254 254859 110305162
Cholestasis 18.69 16.80 48 29230 64470 110495551
Muscular weakness 18.64 16.80 23 29255 248445 110311576
Foetal haemoglobin increased 18.42 16.80 3 29275 6 110560015
Urine calcium 18.42 16.80 3 29275 6 110560015
Flushing 18.07 16.80 3 29275 104733 110455288
Viral infection 18.02 16.80 42 29236 53097 110506924
Chest discomfort 17.91 16.80 12 29266 173836 110386185
Protein total decreased 17.85 16.80 18 29260 10872 110549149
Cytotoxic oedema 17.65 16.80 6 29272 443 110559578
Primary myelofibrosis 17.48 16.80 5 29273 208 110559813
Venoocclusive disease 17.36 16.80 14 29264 6336 110553685
Ill-defined disorder 17.31 16.80 10 29268 156843 110403178

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AC03 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Iron chelating agents
FDA MoA N0000000144 Iron Chelating Activity
FDA EPC N0000175522 Iron Chelator
MeSH PA D002614 Chelating Agents
MeSH PA D007502 Iron Chelating Agents
MeSH PA D064449 Sequestering Agents
FDA MoA N0000182138 Cytochrome P450 1A2 Inhibitors
FDA MoA N0000185506 Cytochrome P450 3A4 Inducers
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38157 iron chelator
CHEBI has role CHEBI:50646 bone density conservation agent
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

V03AC Iron chelating agents 2 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
beta Thalassemia indication 65959000 DOID:12241
Chronic Iron Overload indication
Ocular hypertension contraindication 4210003 DOID:9282
Hyperbilirubinemia contraindication 14783006 DOID:2741
Hearing loss contraindication 15188001
Agranulocytosis contraindication 17182001 DOID:12987
Cirrhosis of liver contraindication 19943007 DOID:5082
Proteinuria contraindication 29738008 DOID:576
Dehydration contraindication 34095006
Gastrointestinal ulcer contraindication 40845000
Multiple organ failure contraindication 57653000
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Gastrointestinal hemorrhage contraindication 74474003
Kidney disease contraindication 90708001 DOID:557
Bilateral cataracts contraindication 95722004
Myelodysplastic syndrome contraindication 109995007
Liver function tests abnormal contraindication 166603001
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Primary malignant neoplasm contraindication 372087000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.84 acidic
pKa2 9.3 acidic
pKa3 9.91 acidic
pKa4 1.72 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Flavin reductase (NADPH) Enzyme Kd 5.77 CHEMBL
Lysine-specific demethylase 5A Enzyme IC50 5.30 CHEMBL
Lysine-specific demethylase 6B Enzyme IC50 5.40 CHEMBL
Lysine-specific demethylase 4A Enzyme IC50 5.49 CHEMBL

External reference:

IDSource
4024936 VUID
N0000171608 NUI
D03669 KEGG_DRUG
4024936 VANDF
C1619629 UMLSCUI
CHEBI:49005 CHEBI
JBL PDB_CHEM_ID
CHEMBL550348 ChEMBL_ID
DB01609 DRUGBANK_ID
D000077588 MESH_DESCRIPTOR_UI
214348 PUBCHEM_CID
8193 INN_ID
V8G4MOF2V9 UNII
614084 RXNORM
20643 MMSL
244676 MMSL
72666 MMSL
d05659 MMSL
011097 NDDF
417910004 SNOMEDCT_US
419985007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Exjade HUMAN PRESCRIPTION DRUG LABEL 1 0078-0468 TABLET, FOR SUSPENSION 125 mg ORAL NDA 33 sections
Exjade HUMAN PRESCRIPTION DRUG LABEL 1 0078-0469 TABLET, FOR SUSPENSION 250 mg ORAL NDA 33 sections
Exjade HUMAN PRESCRIPTION DRUG LABEL 1 0078-0470 TABLET, FOR SUSPENSION 500 mg ORAL NDA 33 sections
Jadenu HUMAN PRESCRIPTION DRUG LABEL 1 0078-0654 TABLET, FILM COATED 90 mg ORAL NDA 33 sections
Jadenu HUMAN PRESCRIPTION DRUG LABEL 1 0078-0655 TABLET, FILM COATED 180 mg ORAL NDA 33 sections
Jadenu HUMAN PRESCRIPTION DRUG LABEL 1 0078-0656 TABLET, FILM COATED 360 mg ORAL NDA 33 sections
Jadenu HUMAN PRESCRIPTION DRUG LABEL 1 0078-0713 GRANULE 180 mg ORAL NDA 33 sections
Jadenu HUMAN PRESCRIPTION DRUG LABEL 1 0078-0720 GRANULE 360 mg ORAL NDA 33 sections
Jadenu HUMAN PRESCRIPTION DRUG LABEL 1 0078-0727 GRANULE 90 mg ORAL NDA 33 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 0480-7011 TABLET, FOR SUSPENSION 125 mg ORAL ANDA 27 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 0480-7012 TABLET, FOR SUSPENSION 250 mg ORAL ANDA 27 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 0480-7013 TABLET, FOR SUSPENSION 500 mg ORAL ANDA 27 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 31722-011 TABLET, FILM COATED 90 mg ORAL ANDA 27 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 31722-012 TABLET, FILM COATED 180 mg ORAL ANDA 27 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 31722-013 TABLET, FILM COATED 360 mg ORAL ANDA 27 sections
DEFERASIROX HUMAN PRESCRIPTION DRUG LABEL 1 31722-029 GRANULE 90 mg ORAL ANDA 27 sections
DEFERASIROX HUMAN PRESCRIPTION DRUG LABEL 1 31722-030 GRANULE 180 mg ORAL ANDA 27 sections
DEFERASIROX HUMAN PRESCRIPTION DRUG LABEL 1 31722-031 GRANULE 360 mg ORAL ANDA 27 sections
Deferasirox Oral Granules HUMAN PRESCRIPTION DRUG LABEL 1 42806-371 GRANULE 90 mg ORAL ANDA 28 sections
Deferasirox Oral Granules HUMAN PRESCRIPTION DRUG LABEL 1 42806-372 GRANULE 180 mg ORAL ANDA 28 sections
Deferasirox Oral Granules HUMAN PRESCRIPTION DRUG LABEL 1 42806-373 GRANULE 360 mg ORAL ANDA 28 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 43598-851 TABLET 360 mg ORAL ANDA 25 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 43598-852 TABLET 180 mg ORAL ANDA 25 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 43598-853 TABLET 90 mg ORAL ANDA 25 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 43598-854 TABLET, FOR SUSPENSION 500 mg ORAL ANDA 26 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 43598-855 TABLET, FOR SUSPENSION 125 mg ORAL ANDA 26 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 43598-856 TABLET, FOR SUSPENSION 250 mg ORAL ANDA 26 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 45963-454 TABLET, FOR SUSPENSION 125 mg ORAL ANDA 19 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 45963-454 TABLET, FOR SUSPENSION 125 mg ORAL ANDA 19 sections
Deferasirox HUMAN PRESCRIPTION DRUG LABEL 1 45963-455 TABLET, FOR SUSPENSION 250 mg ORAL ANDA 19 sections