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

Stem definitionDrug idCAS RN
nucleosides antiviral or antineoplastic agents, cytarabine or azacitidine derivatives 25 320-67-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • 5-azacytidine
  • azacitidine
  • azacytidine
  • ladakamycin
  • ledakamycin
  • vidaza
  • U-18496
A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.
  • Molecular weight: 244.21
  • Formula: C8H12N4O5
  • CLOGP: -2.20
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 4
  • TPSA: 140.97
  • ALOGS: -1.30
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 89 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 62 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 177.10 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.47 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 35 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.36 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 11 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -1.763 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 10.520 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.675 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.324 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 94.700 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 91.480 % High 1
herg hERG pIC50 3.288 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 0.899 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.334 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 86.320 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,MAP2K6,MAP3K21,MAPK7,NTRK1,NTRK2,PDK1,PDK2,PIK3CD,PRKDC 21
kinase-selectivity-class MAP2K6 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.438 High 1
mh-clint Mouse hepatocyte intrinsic clearance 1.718 High 1
mppb Mouse plasma protein binding (% unbound) 96.900 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.483 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 93.760 % High 1
rh-clint Rat hepatocyte intrinsic clearance 1.832 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 96.260 % High 1
rppb Rat plasma protein binding (% unbound) 94.300 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 905.733 uM High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 21, 2011 PMDA Nippon Shinyaku Co., Ltd.
Aug. 2, 2019 EMA Celgene Europe BV
May 19, 2004 FDA CELGENE

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
Febrile neutropenia 2191.53 22.15 986 22930 157363 90447168
Myelosuppression 1621.15 22.15 587 23329 53004 90551527
Acute myeloid leukaemia 822.27 22.15 278 23638 20362 90584169
Acute myeloid leukaemia recurrent 756.56 22.15 161 23755 1896 90602635
Neutropenia 727.77 22.15 545 23371 224359 90380172
Death 704.38 22.15 725 23191 455826 90148705
Thrombocytopenia 691.25 22.15 513 23403 208212 90396319
Pancytopenia 521.62 22.15 349 23567 119914 90484617
Sepsis 460.36 22.15 380 23536 179434 90425097
Cytopenia 388.08 22.15 153 23763 17296 90587235
Neutrophil count decreased 357.34 22.15 227 23689 71305 90533226
Platelet count decreased 351.38 22.15 290 23626 136679 90467852
Pneumonia 327.05 22.15 594 23322 637465 89967066
Septic shock 264.64 22.15 201 23715 83959 90520572
Anaemia 253.57 22.15 383 23533 352419 90252112
Blast cell count increased 244.24 22.15 50 23866 479 90604052
White blood cell count decreased 235.76 22.15 254 23662 166855 90437676
Pyrexia 207.75 22.15 504 23412 659981 89944550
Tumour lysis syndrome 197.25 22.15 83 23833 11069 90593462
Bronchopulmonary aspergillosis 192.19 22.15 82 23834 11316 90593215
Pain 164.65 22.15 32 23884 996309 89608222
Transformation to acute myeloid leukaemia 162.56 22.15 34 23882 365 90604166
Myelodysplastic syndrome transformation 147.16 22.15 32 23884 419 90604112
Bacteraemia 145.32 22.15 84 23832 22216 90582315
Differentiation syndrome 140.37 22.15 38 23878 1293 90603238
Pneumonia fungal 136.72 22.15 56 23860 6975 90597556
Disease progression 128.06 22.15 181 23735 156434 90448097
Bone marrow failure 123.95 22.15 87 23829 32134 90572397
Multiple organ dysfunction syndrome 121.90 22.15 118 23798 68218 90536313
Arthralgia 120.32 22.15 29 23887 778493 89826038
Agranulocytosis 113.01 22.15 85 23831 34917 90569614
Myelodysplastic syndrome 110.92 22.15 69 23847 20834 90583697
Respiratory failure 110.60 22.15 146 23770 118272 90486259
Allogenic stem cell transplantation 110.39 22.15 21 23895 132 90604399
Pneumonitis 107.80 22.15 91 23825 44079 90560452
Neutropenic sepsis 101.68 22.15 62 23854 18068 90586463
Granulocyte count decreased 101.37 22.15 34 23882 2418 90602113
Joint swelling 97.27 22.15 10 23906 503290 90101241
Headache 93.75 22.15 56 23860 862690 89741841
Acute febrile neutrophilic dermatosis 92.73 22.15 35 23881 3510 90601021
Cerebral haemorrhage 92.31 22.15 75 23841 34447 90570084
Protothecosis 92.01 22.15 22 23894 449 90604082
Swelling 90.34 22.15 5 23911 419053 90185478
Off label use 86.91 22.15 541 23375 1101711 89502820
Full blood count decreased 86.86 22.15 68 23848 29621 90574910
Haematotoxicity 83.75 22.15 48 23868 12487 90592044
Alopecia 83.46 22.15 15 23901 495056 90109475
Subdural haematoma 83.43 22.15 53 23863 16592 90587939
Minimal residual disease 83.38 22.15 20 23896 414 90604117
Rheumatoid arthritis 82.48 22.15 3 23913 362611 90241920
Systemic lupus erythematosus 78.99 22.15 4 23912 361892 90242639
Nasopharyngitis 78.86 22.15 8 23908 407096 90197435
Drug hypersensitivity 78.24 22.15 14 23902 463595 90140936
Leukaemia 77.87 22.15 34 23882 4958 90599573
Peripheral swelling 77.78 22.15 9 23907 413097 90191434
Leukopenia 75.84 22.15 112 23804 100598 90503933
Abdominal discomfort 75.16 22.15 17 23899 477311 90127220
Weight increased 74.14 22.15 11 23905 417916 90186615
Aspergillus infection 73.79 22.15 42 23874 10781 90593750
Soft tissue infection 70.02 22.15 27 23889 2870 90601661
Infusion related reaction 69.42 22.15 13 23903 416767 90187764
Cord blood transplant therapy 69.37 22.15 11 23905 17 90604514
Acute graft versus host disease 68.63 22.15 32 23884 5436 90599095
Hypersensitivity 68.06 22.15 18 23898 454659 90149872
Product dose omission issue 64.35 22.15 3 23913 291684 90312847
Acute myeloid leukaemia refractory 63.93 22.15 13 23903 120 90604411
Pseudomonas infection 63.91 22.15 43 23873 14822 90589709
Stenotrophomonas infection 62.66 22.15 24 23892 2505 90602026
Musculoskeletal stiffness 62.47 22.15 4 23912 296528 90308003
Systemic candida 62.18 22.15 29 23887 4930 90599601
Hypertension 61.49 22.15 22 23894 457510 90147021
Haemoglobin decreased 60.90 22.15 133 23783 161823 90442708
Maternal exposure during pregnancy 60.45 22.15 11 23905 360052 90244479
Graft versus host disease in skin 59.31 22.15 26 23890 3827 90600704
Graft versus host disease in gastrointestinal tract 59.20 22.15 27 23889 4361 90600170
Organising pneumonia 58.67 22.15 32 23884 7565 90596966
Pleural effusion 56.52 22.15 104 23812 111887 90492644
Infection 56.03 22.15 216 23700 361878 90242653
Pneumonia adenoviral 55.91 22.15 13 23903 234 90604297
Escherichia sepsis 54.86 22.15 28 23888 5788 90598743
Cardiac failure 54.40 22.15 101 23815 109395 90495136
Leukocytosis 54.27 22.15 53 23863 30937 90573594
Myelofibrosis 54.14 22.15 19 23897 1548 90602983
Mobility decreased 53.97 22.15 3 23913 250731 90353800
Disseminated intravascular coagulation 53.82 22.15 45 23871 21493 90583038
Enterococcal infection 53.05 22.15 33 23883 9958 90594573
Hypoaesthesia 51.88 22.15 10 23906 314200 90290331
Discomfort 51.55 22.15 6 23910 274329 90330202
Graft versus host disease 51.25 22.15 30 23886 8114 90596417
Anxiety 50.84 22.15 10 23906 309762 90294769
Wheezing 50.78 22.15 3 23913 238077 90366454
Dyspnoea 49.34 22.15 99 23817 880856 89723675
Asthma 48.90 22.15 4 23912 242156 90362375
Cellulitis 48.86 22.15 87 23829 91250 90513281
Blood lactate dehydrogenase increased 48.52 22.15 46 23870 25886 90578645
Adenoviral hepatitis 48.11 22.15 13 23903 439 90604092
COVID-19 pneumonia 47.55 22.15 39 23877 18138 90586393
Drug intolerance 47.16 22.15 30 23886 447561 90156970
Impaired healing 46.92 22.15 4 23912 234195 90370336
Fatigue 46.70 22.15 153 23763 1153870 89450661
Febrile bone marrow aplasia 46.31 22.15 30 23886 9708 90594823
Malaise 46.19 22.15 52 23864 585934 90018597
Hepatic enzyme increased 45.70 22.15 19 23897 360717 90243814
Periorbital cellulitis 45.34 22.15 14 23902 763 90603768
Hyperbilirubinaemia 45.32 22.15 34 23882 13902 90590629
Abdominal pain upper 44.66 22.15 16 23900 332658 90271873
Blister 44.53 22.15 7 23909 254991 90349540
Refractory anaemia with an excess of blasts 43.70 22.15 12 23904 431 90604100
Dizziness 43.55 22.15 55 23861 589229 90015302
Staphylococcal bacteraemia 43.05 22.15 26 23890 7443 90597088
Folliculitis 42.31 22.15 3 23913 204350 90400181
Insomnia 41.54 22.15 18 23898 333456 90271075
Therapeutic product effect decreased 41.47 22.15 11 23905 277560 90326971
Blast cells present 41.09 22.15 12 23904 540 90603991
Renal tubular disorder 40.97 22.15 19 23897 3188 90601343
Fusarium infection 40.78 22.15 14 23902 1068 90603463
Sleep disorder 40.74 22.15 3 23913 198027 90406504
Memory impairment 40.54 22.15 3 23913 197241 90407290
Pericardial effusion 40.02 22.15 49 23867 36784 90567747
Condition aggravated 39.58 22.15 60 23856 595485 90009046
Liver abscess 39.41 22.15 19 23897 3477 90601054
Paraesthesia 39.19 22.15 9 23907 250317 90354214
Pseudomonal bacteraemia 39.17 22.15 16 23900 1978 90602553
Pruritus 38.51 22.15 52 23864 541473 90063058
Exposure during pregnancy 38.48 22.15 8 23908 238402 90366129
Platelet count abnormal 38.38 22.15 20 23896 4315 90600216
Injury 37.86 22.15 4 23912 197345 90407186
Pain in extremity 37.68 22.15 38 23878 450491 90154040
Toxic neuropathy 36.80 22.15 11 23905 537 90603994
Sinusitis 36.12 22.15 23 23893 343065 90261466
Osteoarthritis 35.02 22.15 5 23911 195725 90408806
Chloroma 34.96 22.15 9 23907 251 90604280
Venoocclusive liver disease 34.90 22.15 21 23895 5972 90598559
Dry mouth 34.63 22.15 4 23912 184055 90420476
Graft versus host disease in liver 34.52 22.15 12 23904 951 90603580
Gait disturbance 34.16 22.15 13 23903 260483 90344048
Acute graft versus host disease in skin 33.89 22.15 19 23897 4737 90599794
Migraine 33.75 22.15 5 23911 190387 90414144
Transplant 33.51 22.15 12 23904 1037 90603494
Tonsillitis bacterial 33.15 22.15 8 23908 170 90604361
Scedosporium infection 32.35 22.15 11 23905 815 90603716
Muscle spasms 32.32 22.15 13 23903 251870 90352661
Blood disorder 32.21 22.15 22 23894 7768 90596763
Acute leukaemia 31.98 22.15 12 23904 1184 90603347
Staphylococcal sepsis 30.75 22.15 23 23893 9360 90595171
Bacillus infection 30.75 22.15 11 23905 948 90603583
Bacterial sepsis 30.51 22.15 18 23898 4937 90599594
Haemorrhage intracranial 30.49 22.15 28 23888 15134 90589397
Iron overload 30.03 22.15 11 23905 1014 90603517
COVID-19 29.64 22.15 105 23811 168738 90435793
Muscular weakness 29.37 22.15 9 23907 206657 90397874
Granulocytopenia 28.57 22.15 19 23897 6422 90598109
Rash 28.48 22.15 111 23805 795989 89808542
Overdose 28.28 22.15 4 23912 157705 90446826
Gastrooesophageal reflux disease 28.07 22.15 5 23911 166332 90438199
Gait inability 28.01 22.15 3 23913 146453 90458078
Pulmonary sepsis 27.82 22.15 13 23903 2218 90602313
Klebsiella infection 26.74 22.15 22 23894 10275 90594256
Skin maceration 26.67 22.15 7 23909 211 90604320
Chest pain 26.66 22.15 27 23889 319618 90284913
Clonal evolution 26.65 22.15 6 23910 93 90604438
Mucormycosis 26.51 22.15 15 23901 3806 90600725
Adenovirus infection 26.41 22.15 16 23900 4606 90599925
Leukaemia recurrent 26.21 22.15 11 23905 1456 90603075
Aplasia 25.90 22.15 15 23901 3976 90600555
Therapy non-responder 25.72 22.15 87 23829 136617 90467914
Chronic graft versus host disease 25.39 22.15 15 23901 4124 90600407
Neutropenic colitis 25.38 22.15 15 23901 4128 90600403
Portal vein cavernous transformation 25.30 22.15 6 23910 118 90604413
Musculoskeletal pain 25.17 22.15 7 23909 171244 90433287
Pseudomonal skin infection 24.92 22.15 4 23912 7 90604524
Bone marrow necrosis 24.71 22.15 6 23910 131 90604400
Depression 24.38 22.15 26 23890 300575 90303956
Bone marrow transplant 24.35 22.15 9 23907 851 90603680
Klebsiella sepsis 24.16 22.15 11 23905 1770 90602761
Leukaemia cutis 24.01 22.15 6 23910 148 90604383
Serum ferritin increased 23.98 22.15 18 23898 7363 90597168
Myeloblast count increased 23.68 22.15 4 23912 11 90604520
Bacterial infection 23.56 22.15 30 23886 23414 90581117
Hypokalaemia 23.40 22.15 82 23834 131034 90473497
Dysplasia 23.40 22.15 10 23906 1384 90603147
Geotrichum infection 23.33 22.15 8 23908 608 90603923
Escherichia bacteraemia 23.25 22.15 16 23900 5719 90598812
Staphylococcal infection 23.19 22.15 44 23872 48395 90556136
Drug resistance 23.10 22.15 34 23882 30415 90574116
Klebsiella bacteraemia 23.06 22.15 12 23904 2580 90601951
Septic embolus 23.06 22.15 9 23907 988 90603543
Transfusion related complication 22.95 22.15 4 23912 14 90604517
Pulmonary haemorrhage 22.67 22.15 18 23898 7995 90596536
Pneumonia bacterial 22.62 22.15 22 23894 12768 90591763
Systemic mycosis 22.50 22.15 10 23906 1520 90603011
Aspiration bone marrow 22.37 22.15 6 23910 197 90604334

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
Febrile neutropenia 2239.60 17.72 1585 35092 184118 42400540
Myelosuppression 1216.46 17.72 624 36053 39837 42544821
Acute myeloid leukaemia 982.78 17.72 447 36230 21809 42562849
Acute myeloid leukaemia recurrent 722.66 17.72 219 36458 3293 42581365
Neutropenia 660.59 17.72 833 35844 198598 42386060
Pneumonia 568.36 17.72 1168 35509 420981 42163677
Death 531.86 17.72 1214 35463 469971 42114687
Neutrophil count decreased 495.57 17.72 421 36256 62994 42521664
Sepsis 442.84 17.72 688 35989 198646 42386012
Cytopenia 423.69 17.72 234 36443 17263 42567395
Thrombocytopenia 415.93 17.72 652 36025 189627 42395031
Platelet count decreased 400.30 17.72 542 36135 138039 42446619
Pancytopenia 380.94 17.72 487 36190 117256 42467402
Tumour lysis syndrome 339.45 17.72 221 36456 22010 42562648
Blast cell count increased 332.37 17.72 94 36583 1091 42583567
White blood cell count decreased 315.80 17.72 430 36247 109966 42474692
Pneumonia fungal 273.99 17.72 141 36536 9005 42575653
Anaemia 268.67 17.72 680 35997 279598 42305060
Infection 262.45 17.72 397 36280 111671 42472987
Transformation to acute myeloid leukaemia 244.90 17.72 73 36604 1032 42583626
Septic shock 243.92 17.72 345 36332 91327 42493331
Pyrexia 215.79 17.72 785 35892 393257 42191401
Bronchopulmonary aspergillosis 168.09 17.72 137 36540 19292 42565366
Myelodysplastic syndrome transformation 167.76 17.72 46 36631 472 42584186
Myelodysplastic syndrome 132.10 17.72 128 36549 22617 42562041
Acute febrile neutrophilic dermatosis 112.90 17.72 47 36630 1837 42582821
Chronic myelomonocytic leukaemia 104.83 17.72 35 36642 728 42583930
Bacteraemia 104.32 17.72 118 36559 24922 42559736
Product dose omission issue 102.57 17.72 8 36669 154357 42430301
Headache 99.17 17.72 41 36636 239328 42345330
Minimal residual disease 95.43 17.72 31 36646 590 42584068
Acute myeloid leukaemia refractory 93.16 17.72 22 36655 115 42584543
Allogenic stem cell transplantation 85.25 17.72 21 36656 135 42584523
Neutropenic sepsis 83.80 17.72 85 36592 15861 42568797
Haematotoxicity 79.66 17.72 70 36607 10915 42573743
Toxicity to various agents 77.51 17.72 51 36626 229085 42355573
Drug interaction 75.73 17.72 71 36606 266928 42317730
Somnolence 71.15 17.72 17 36660 141088 42443570
Inappropriate schedule of product administration 69.67 17.72 3 36674 95899 42488759
Anxiety 68.91 17.72 10 36667 118550 42466108
Febrile bone marrow aplasia 68.12 17.72 62 36615 10119 42574539
Completed suicide 66.97 17.72 4 36673 96461 42488197
Necrotising fasciitis 66.42 17.72 44 36633 4502 42580156
Bone marrow failure 65.87 17.72 109 36568 32984 42551674
Pyoderma gangrenosum 63.77 17.72 32 36645 1935 42582723
Blood product transfusion dependent 63.11 17.72 21 36656 432 42584226
Blood pressure increased 63.10 17.72 7 36670 101921 42482737
Disseminated intravascular coagulation 62.39 17.72 91 36586 24703 42559955
Corynebacterium bacteraemia 62.23 17.72 16 36661 125 42584533
Pain in extremity 61.98 17.72 26 36651 150578 42434080
Organising pneumonia 60.72 17.72 51 36626 7481 42577177
Drug hypersensitivity 58.65 17.72 8 36669 99381 42485277
Overdose 58.64 17.72 10 36667 105254 42479404
Arthralgia 57.65 17.72 55 36622 205183 42379475
Graft versus host disease 57.41 17.72 63 36614 12862 42571796
Tremor 56.73 17.72 8 36669 96921 42487737
Pain 56.43 17.72 77 36600 244771 42339887
Chloroma 54.42 17.72 20 36657 557 42584101
Off label use 50.94 17.72 800 35877 637535 41947123
Graft versus host disease in gastrointestinal tract 50.31 17.72 39 36638 5104 42579554
Pneumonitis 50.27 17.72 111 36566 41607 42543051
Cerebral haemorrhage 49.60 17.72 106 36571 38860 42545798
Weight decreased 49.32 17.72 64 36613 207884 42376774
Acute graft versus host disease in skin 49.26 17.72 45 36632 7379 42577279
Acute leukaemia 48.82 17.72 23 36654 1210 42583448
Dyspnoea 48.70 17.72 206 36471 442415 42142243
Dizziness 48.31 17.72 88 36589 249166 42335492
Muscle spasms 48.30 17.72 8 36669 86036 42498622
Pruritus 48.04 17.72 55 36622 188716 42395942
Disease progression 47.80 17.72 247 36430 143409 42441249
Graft versus host disease in skin 47.70 17.72 38 36639 5174 42579484
Weight increased 47.13 17.72 17 36660 107966 42476692
Granulocyte count decreased 46.41 17.72 24 36653 1546 42583112
Bacillus infection 46.01 17.72 19 36658 727 42583931
Myalgia 45.70 17.72 13 36664 96067 42488591
Myelofibrosis 45.49 17.72 25 36652 1822 42582836
Escherichia sepsis 44.45 17.72 38 36639 5709 42578949
Bacillus bacteraemia 43.92 17.72 13 36664 179 42584479
Condition aggravated 43.78 17.72 100 36577 260654 42324004
Agranulocytosis 43.33 17.72 87 36590 30525 42554133
Emphysematous cholecystitis 42.34 17.72 11 36666 90 42584568
Hypertension 42.23 17.72 49 36628 167155 42417503
Insomnia 41.75 17.72 25 36652 118228 42466430
Leukostasis syndrome 41.53 17.72 12 36665 151 42584507
Bone marrow disorder 41.13 17.72 24 36653 1962 42582696
Brain abscess 40.85 17.72 32 36645 4252 42580406
Pericarditis 40.79 17.72 54 36623 13390 42571268
Catheter site infection 40.64 17.72 28 36649 3055 42581603
Subdural haematoma 40.50 17.72 72 36605 23066 42561592
Differentiation syndrome 40.45 17.72 23 36654 1790 42582868
Leukaemia recurrent 39.72 17.72 23 36654 1853 42582805
Anal abscess 39.71 17.72 41 36636 7809 42576849
Staphylococcal sepsis 39.60 17.72 49 36628 11365 42573293
Fungal infection 39.29 17.72 65 36612 19657 42565001
Intentional product misuse 38.94 17.72 4 36673 61896 42522762
Full blood count decreased 38.61 17.72 66 36611 20494 42564164
Cardiac failure 38.53 17.72 188 36489 106668 42477990
Iron overload 38.42 17.72 21 36656 1514 42583144
Blood disorder 38.29 17.72 30 36647 3987 42580671
Leukocytosis 38.02 17.72 81 36596 29627 42555031
FLT3 gene mutation 37.57 17.72 7 36670 7 42584651
Neutropenic colitis 37.55 17.72 31 36646 4439 42580219
Depression 37.31 17.72 25 36652 111338 42473320
Enteritis infectious 37.23 17.72 21 36656 1610 42583048
Meningeal neoplasm 37.06 17.72 10 36667 96 42584562
Asthma 36.79 17.72 5 36672 62309 42522349
Aspergillus infection 36.79 17.72 56 36621 15781 42568877
Soft tissue infection 36.79 17.72 25 36652 2668 42581990
Hyperhidrosis 36.62 17.72 16 36661 90496 42494162
Cytarabine syndrome 34.86 17.72 8 36669 36 42584622
Therapy non-responder 33.84 17.72 112 36565 53247 42531411
Escherichia bacteraemia 33.75 17.72 31 36646 5118 42579540
Nasopharyngitis 33.74 17.72 15 36662 83981 42500677
Peripheral swelling 33.41 17.72 18 36659 90252 42494406
Fatigue 33.30 17.72 229 36448 435412 42149246
Musculoskeletal stiffness 33.25 17.72 5 36672 57760 42526898
Clostridium difficile colitis 33.24 17.72 63 36614 21189 42563469
Paraesthesia 33.02 17.72 11 36666 73448 42511210
Cellulitis 32.79 17.72 122 36555 61463 42523195
Haemoglobin abnormal 32.76 17.72 30 36647 4934 42579724
Joint swelling 32.72 17.72 9 36668 68013 42516645
Leukaemia 32.59 17.72 32 36645 5740 42578918
Myositis 32.34 17.72 51 36626 14815 42569843
Aeromonas infection 32.19 17.72 12 36665 348 42584310
Splenic infarction 31.86 17.72 22 36655 2409 42582249
Therapeutic product effect incomplete 31.69 17.72 133 36544 70806 42513852
Bacterial sepsis 31.25 17.72 33 36644 6449 42578209
Dehydration 31.21 17.72 46 36631 141721 42442937
Seizure 30.78 17.72 35 36642 120526 42464132
Juvenile chronic myelomonocytic leukaemia 30.60 17.72 7 36670 31 42584627
Malaise 30.47 17.72 88 36589 212068 42372590
Injection site reaction 30.23 17.72 51 36626 15670 42568988
Agitation 30.03 17.72 9 36668 64305 42520353
Klebsiella sepsis 29.78 17.72 22 36655 2679 42581979
Chest discomfort 29.52 17.72 9 36668 63607 42521051
Loss of personal independence in daily activities 29.40 17.72 4 36673 49812 42534846
Abdominal discomfort 29.35 17.72 14 36663 75241 42509417
Infusion related reaction 29.33 17.72 8 36669 60798 42523860
Wheezing 28.80 17.72 6 36671 54775 42529883
Feeling abnormal 28.76 17.72 12 36665 69774 42514884
Enterococcal infection 28.57 17.72 43 36634 11996 42572662
Pulmonary sepsis 27.81 17.72 23 36654 3301 42581357
Gait disturbance 27.79 17.72 26 36651 97974 42486684
Stenotrophomonas infection 27.65 17.72 24 36653 3680 42580978
Central nervous system leukaemia 27.64 17.72 11 36666 382 42584276
Memory impairment 27.45 17.72 5 36672 50217 42534441
Epistaxis 27.32 17.72 122 36555 66704 42517954
Lower motor neurone lesion 27.30 17.72 7 36670 54 42584604
Febrile infection 27.08 17.72 21 36656 2750 42581908
Septal panniculitis 26.97 17.72 7 36670 57 42584601
Cough 26.96 17.72 72 36605 178031 42406627
Rhabdomyolysis 26.82 17.72 17 36660 78002 42506656
Graft versus host disease in liver 26.73 17.72 17 36660 1622 42583036
Graft versus host disease in lung 26.72 17.72 13 36664 735 42583923
Transplant 26.53 17.72 14 36663 940 42583718
Ulcerative duodenitis 26.52 17.72 6 36671 25 42584633
Venoocclusive disease 26.50 17.72 24 36653 3891 42580767
Pneumonia bacterial 26.40 17.72 48 36629 15644 42569014
Administration site induration 26.36 17.72 5 36672 6 42584652
Haemophagocytic lymphohistiocytosis 26.04 17.72 52 36625 18170 42566488
Hypersensitivity 25.95 17.72 15 36662 72355 42512303
Oesophageal candidiasis 25.95 17.72 28 36649 5607 42579051
International normalised ratio increased 25.89 17.72 5 36672 48163 42536495
Cardiac tamponade 25.84 17.72 30 36647 6510 42578148
Palpitations 25.82 17.72 6 36671 50791 42533867
Multiple organ dysfunction syndrome 25.70 17.72 157 36520 96878 42487780
Myeloid leukaemia 25.34 17.72 11 36666 477 42584181
Bradycardia 25.04 17.72 22 36655 85462 42499196
Blast cells present 24.81 17.72 11 36666 502 42584156
Pericardial effusion 24.74 17.72 68 36609 29207 42555451
Dry mouth 24.02 17.72 3 36674 39876 42544782
Staphylococcal bacteraemia 23.98 17.72 38 36639 11083 42573575
Intracranial tumour haemorrhage 23.94 17.72 10 36667 394 42584264
Second primary malignancy 23.87 17.72 35 36642 9540 42575118
Sleep disorder 23.82 17.72 6 36671 48089 42536569
Respiratory failure 23.74 17.72 190 36487 127942 42456716
Rheumatoid arthritis 23.69 17.72 4 36673 42436 42542222
Disease risk factor 23.21 17.72 6 36671 48 42584610
Dyspepsia 22.86 17.72 4 36673 41348 42543310
Pseudomembranous colitis 22.78 17.72 20 36657 3113 42581545
Blood glucose increased 22.78 17.72 18 36659 73681 42510977
Vision blurred 22.51 17.72 9 36668 53690 42530968
Neutrophilic dermatosis 22.31 17.72 9 36668 324 42584334
Cord blood transplant therapy 22.29 17.72 6 36671 57 42584601
Haemoglobin decreased 22.18 17.72 192 36485 132279 42452379
Thrombosis 22.11 17.72 16 36661 68495 42516163
Product reconstitution quality issue 22.11 17.72 8 36669 213 42584445
Acute graft versus host disease 21.90 17.72 31 36646 8184 42576474
Aspiration bone marrow abnormal 21.81 17.72 7 36670 128 42584530
Lactic acidosis 21.74 17.72 6 36671 45255 42539403
Wrong technique in product usage process 21.74 17.72 5 36672 42630 42542028
Hyperleukocytosis 21.72 17.72 18 36659 2590 42582068
Balance disorder 21.64 17.72 7 36670 47638 42537020
Abdominal distension 21.57 17.72 18 36659 71717 42512941
Neutrophilic panniculitis 21.53 17.72 5 36672 24 42584634
Venous aneurysm 21.47 17.72 4 36673 4 42584654
Megakaryocytes decreased 21.47 17.72 4 36673 4 42584654
Acute myeloid leukaemia (in remission) 21.47 17.72 4 36673 4 42584654
Hypoaesthesia 21.41 17.72 18 36659 71445 42513213
Cytokine release syndrome 21.21 17.72 6 36671 44521 42540137
Administration site erythema 21.18 17.72 6 36671 70 42584588
Rash 20.90 17.72 146 36531 276808 42307850
Hypoglycaemia 20.63 17.72 13 36664 59841 42524817
Platelet disorder 20.21 17.72 16 36661 2158 42582500
Angiodysplasia 20.08 17.72 11 36666 796 42583862
Cystitis haemorrhagic 20.05 17.72 28 36649 7301 42577357
Plasma cell myeloma 19.90 17.72 8 36669 47570 42537088
Primary myelofibrosis 19.73 17.72 6 36671 91 42584567
Coronary artery disease 19.45 17.72 11 36666 53709 42530949
Muscular weakness 19.45 17.72 26 36651 83472 42501186
Colitis 19.01 17.72 85 36592 46487 42538171
Cardiac iron overload 18.96 17.72 4 36673 11 42584647
Pulmonary resection 18.63 17.72 6 36671 111 42584547
Eosinophilia 18.59 17.72 3 36674 32896 42551762
Loss of consciousness 18.39 17.72 32 36645 92322 42492336
General physical health deterioration 18.36 17.72 205 36472 151041 42433617
Urticaria 18.34 17.72 22 36655 74014 42510644
Euthyroid sick syndrome 18.18 17.72 3 36674 0 42584658
Injection site vasculitis 18.18 17.72 3 36674 0 42584658
Escherichia infection 18.09 17.72 34 36643 11362 42573296
Clostridium bacteraemia 18.04 17.72 7 36670 227 42584431
Leukopenia 17.96 17.72 118 36559 74628 42510030

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
Febrile neutropenia 4272.80 17.99 2367 52070 314400 110220462
Myelosuppression 2689.29 17.99 1178 53259 93162 110441700
Acute myeloid leukaemia recurrent 1388.97 17.99 352 54085 4787 110530075
Neutropenia 1375.98 17.99 1270 53167 373350 110161512
Acute myeloid leukaemia 1366.76 17.99 561 53876 37549 110497313
Death 1257.24 17.99 1625 52812 697244 109837618
Thrombocytopenia 1015.41 17.99 1042 53395 347843 110187019
Sepsis 904.20 17.99 951 53486 326395 110208467
Pneumonia 894.63 17.99 1565 52872 875149 109659713
Neutrophil count decreased 867.09 17.99 608 53829 120333 110414529
Platelet count decreased 776.22 17.99 746 53691 229697 110305165
Pancytopenia 773.79 17.99 714 53723 208899 110325963
Cytopenia 715.89 17.99 332 54105 29784 110505078
White blood cell count decreased 566.68 17.99 629 53808 228761 110306101
Anaemia 537.84 17.99 963 53474 546123 109988739
Tumour lysis syndrome 517.51 17.99 268 54169 30533 110504329
Blast cell count increased 511.53 17.99 126 54311 1511 110533351
Septic shock 509.21 17.99 499 53938 157029 110377833
Pyrexia 411.65 17.99 1166 53271 897099 109637763
Pneumonia fungal 405.38 17.99 180 54257 14574 110520288
Transformation to acute myeloid leukaemia 380.40 17.99 98 54339 1425 110533437
Bronchopulmonary aspergillosis 368.83 17.99 212 54225 29651 110505211
Bacteraemia 237.64 17.99 184 54253 42206 110492656
Pain 232.63 17.99 90 54347 954865 109579997
Headache 223.58 17.99 78 54359 882299 109652563
Infection 212.76 17.99 517 53920 361683 110173179
Arthralgia 197.29 17.99 69 54368 779563 109755299
Myelodysplastic syndrome transformation 186.76 17.99 49 54388 768 110534094
Acute febrile neutrophilic dermatosis 184.71 17.99 75 54362 4861 110530001
Allogenic stem cell transplantation 172.95 17.99 37 54400 222 110534640
Myelodysplastic syndrome 168.42 17.99 143 54294 37341 110497521
Joint swelling 163.22 17.99 15 54422 442830 110092032
Drug hypersensitivity 163.12 17.99 17 54420 454073 110080789
Bone marrow failure 162.41 17.99 170 54267 57678 110477184
Disease progression 161.33 17.99 365 54072 243669 110291193
Pneumonitis 156.95 17.99 191 54246 76340 110458522
Minimal residual disease 151.77 17.99 43 54394 910 110533952
Differentiation syndrome 148.30 17.99 56 54381 2988 110531874
Blood product transfusion dependent 144.09 17.99 36 54401 459 110534403
Neutropenic sepsis 143.70 17.99 120 54317 30626 110504236
Acute myeloid leukaemia refractory 141.13 17.99 32 54405 260 110534602
Weight increased 137.88 17.99 21 54416 419623 110115239
Granulocyte count decreased 137.19 17.99 57 54380 3917 110530945
Multiple organ dysfunction syndrome 135.61 17.99 257 54180 151453 110383409
Cerebral haemorrhage 131.36 17.99 161 54276 64807 110470055
Full blood count decreased 131.14 17.99 116 54321 31983 110502879
Agranulocytosis 129.67 17.99 156 54281 61604 110473258
Respiratory failure 127.99 17.99 309 54128 215023 110319839
Infusion related reaction 127.70 17.99 18 54419 381144 110153718
Arthropathy 127.15 17.99 3 54434 287519 110247343
Nasopharyngitis 124.49 17.99 22 54415 394339 110140523
Peripheral swelling 124.41 17.99 24 54413 404010 110130852
Product dose omission issue 120.97 17.99 10 54427 321772 110213090
Disseminated intravascular coagulation 120.68 17.99 124 54313 41162 110493700
Rheumatoid arthritis 119.33 17.99 7 54430 299606 110235256
Swelling 118.95 17.99 16 54421 351025 110183837
Anxiety 118.68 17.99 15 54422 345063 110189799
Subdural haematoma 118.53 17.99 116 54321 36338 110498524
Abdominal discomfort 117.93 17.99 25 54412 393833 110141029
Hypersensitivity 116.24 17.99 28 54409 403970 110130892
Febrile bone marrow aplasia 116.12 17.99 84 54353 17381 110517481
Organising pneumonia 114.57 17.99 77 54360 14166 110520696
Aspergillus infection 111.55 17.99 96 54341 25520 110509342
Escherichia sepsis 111.22 17.99 67 54370 10205 110524657
Musculoskeletal stiffness 110.04 17.99 7 54430 279815 110255047
Graft versus host disease 108.36 17.99 83 54354 18723 110516139
Systemic lupus erythematosus 107.56 17.99 4 54433 254334 110280528
Pain in extremity 107.10 17.99 53 54384 487065 110047797
Completed suicide 105.39 17.99 3 54434 242378 110292484
Contraindicated product administered 104.66 17.99 4 54433 248263 110286599
Maternal exposure during pregnancy 104.49 17.99 5 54432 254878 110279984
Alopecia 101.61 17.99 27 54410 364726 110170136
Off label use 99.44 17.99 1150 53287 1499035 109035827
Pruritus 98.43 17.99 85 54352 581475 109953387
Malaise 97.88 17.99 112 54325 671707 109863155
Dizziness 97.88 17.99 120 54317 698073 109836789
Dyspnoea 96.26 17.99 256 54181 1106616 109428246
Wound 94.82 17.99 5 54432 234432 110300430
Asthma 93.45 17.99 8 54429 250283 110284579
Wheezing 93.04 17.99 9 54428 255221 110279641
Paraesthesia 92.72 17.99 13 54424 276508 110258354
Hypertension 91.98 17.99 70 54367 510014 110024848
Hypoaesthesia 91.91 17.99 21 54416 314202 110220660
Cardiac failure 91.53 17.99 250 54187 187376 110347486
Acute graft versus host disease in skin 91.06 17.99 60 54377 10680 110524182
Soft tissue infection 90.24 17.99 46 54391 5061 110529801
Systemic candida 90.15 17.99 58 54379 9916 110524946
Fatigue 89.40 17.99 304 54133 1215654 109319208
Leukaemia 89.14 17.99 52 54385 7466 110527396
Cellulitis 88.26 17.99 193 54244 125823 110409039
Insomnia 87.50 17.99 34 54403 360556 110174306
Stenotrophomonas infection 87.08 17.99 47 54390 5811 110529051
Inappropriate schedule of product administration 86.80 17.99 3 54434 203634 110331228
Muscle spasms 86.71 17.99 16 54421 278141 110256721
Chloroma 86 17.99 27 54410 821 110534041
Corynebacterium bacteraemia 85.79 17.99 20 54417 186 110534676
Haematotoxicity 85.74 17.99 76 54361 21006 110513856
Necrotising fasciitis 83.45 17.99 50 54387 7541 110527321
Cord blood transplant therapy 83.10 17.99 17 54420 79 110534783
Acute leukaemia 82.84 17.99 32 54405 1817 110533045
Drug intolerance 82.37 17.99 49 54388 406463 110128399
Dry mouth 78.60 17.99 5 54432 199943 110334919
Therapy non-responder 78.11 17.99 211 54226 157096 110377766
Impaired healing 77.09 17.99 5 54432 196712 110338150
Pericardial effusion 76.44 17.99 116 54321 57101 110477761
Helicobacter infection 76.41 17.99 3 54434 181874 110352988
Blood pressure increased 76.08 17.99 17 54420 258356 110276506
Condition aggravated 74.91 17.99 156 54281 734680 109800182
Protothecosis 74.75 17.99 22 54415 535 110534327
Leukopenia 74.30 17.99 200 54237 148591 110386271
Enterococcal infection 74.16 17.99 69 54368 20297 110514565
Somnolence 73.90 17.99 27 54410 297422 110237440
Overdose 73.83 17.99 13 54424 233781 110301081
Abdominal pain upper 73.70 17.99 40 54397 349071 110185791
Blister 73.22 17.99 12 54425 227364 110307498
Leukocytosis 73.14 17.99 110 54327 53718 110481144
Graft versus host disease in skin 72.15 17.99 47 54390 8207 110526655
Memory impairment 71.62 17.99 7 54430 196937 110337925
Haemoglobin decreased 70.99 17.99 276 54161 248451 110286411
Myelofibrosis 70.48 17.99 33 54404 3018 110531844
Therapeutic product effect decreased 70.10 17.99 17 54420 244299 110290563
Discomfort 69.88 17.99 11 54426 214696 110320166
Pleural effusion 69.61 17.99 219 54218 177490 110357372
Staphylococcal bacteraemia 69.54 17.99 61 54376 16627 110518235
Staphylococcal sepsis 69.15 17.99 62 54375 17392 110517470
Mobility decreased 69.15 17.99 16 54421 237406 110297456
Graft versus host disease in gastrointestinal tract 68.60 17.99 47 54390 8921 110525941
Iron overload 68.06 17.99 29 54408 2122 110532740
Acute graft versus host disease 68.03 17.99 54 54383 12827 110522035
Type 2 diabetes mellitus 68.01 17.99 5 54432 177227 110357635
Toxicity to various agents 67.90 17.99 82 54355 480473 110054389
Graft versus host disease in liver 67.46 17.99 30 54407 2435 110532427
Sleep disorder 67.38 17.99 9 54428 198635 110336227
Neutropenic colitis 65.82 17.99 44 54393 8021 110526841
Bacillus infection 65.49 17.99 26 54411 1588 110533274
Injury 65.26 17.99 6 54431 177259 110357603
Pyoderma gangrenosum 65.26 17.99 38 54399 5438 110529424
Hepatic enzyme increased 64.54 17.99 39 54398 320853 110214009
Tremor 64.39 17.99 11 54426 202221 110332641
Exposure during pregnancy 63.46 17.99 5 54432 167419 110367443
Migraine 62.68 17.99 6 54431 171646 110363216
Leukaemia recurrent 60.61 17.99 30 54407 3101 110531761
Transplant 60.48 17.99 23 54414 1251 110533611
Blast cells present 58.77 17.99 21 54416 957 110533905
Gait disturbance 58.52 17.99 32 54405 278176 110256686
Klebsiella sepsis 58.07 17.99 32 54405 4121 110530741
Weight decreased 56.93 17.99 89 54348 467968 110066894
Venoocclusive liver disease 56.29 17.99 52 54385 15155 110519707
Pulmonary sepsis 56.04 17.99 34 54403 5244 110529618
Osteoarthritis 55.84 17.99 11 54426 182612 110352250
Bacterial sepsis 55.69 17.99 44 54393 10382 110524480
Sinusitis 55.66 17.99 39 54398 296649 110238213
Depression 55.32 17.99 45 54392 317290 110217572
Pneumonia bacterial 54.56 17.99 66 54371 26195 110508667
Folliculitis 53.63 17.99 9 54428 167644 110367218
Cardiovascular disorder 53.60 17.99 61 54376 22699 110512163
Anal abscess 53.50 17.99 45 54392 11593 110523269
Leukostasis syndrome 53.09 17.99 14 54423 224 110534638
Escherichia bacteraemia 52.38 17.99 42 54395 10122 110524740
Bursitis 51.81 17.99 3 54434 129915 110404947
C-reactive protein abnormal 51.70 17.99 3 54434 129692 110405170
Emphysematous cholecystitis 51.63 17.99 12 54425 110 110534752
Bacillus bacteraemia 51.59 17.99 14 54423 251 110534611
Pseudomonas infection 51.45 17.99 66 54371 27787 110507075
Hyperbilirubinaemia 50.98 17.99 69 54368 30602 110504260
Musculoskeletal pain 50.08 17.99 14 54423 183009 110351853
Chronic myelomonocytic leukaemia 49.78 17.99 19 54418 1044 110533818
Periorbital cellulitis 49.28 17.99 19 54418 1073 110533789
Clostridium difficile colitis 49.17 17.99 82 54355 43696 110491166
Epistaxis 48.61 17.99 158 54279 130214 110404648
Drug interaction 48.57 17.99 109 54328 500074 110034788
Intentional product misuse 47.60 17.99 5 54432 132899 110401963
Muscular weakness 47.48 17.99 32 54405 248436 110286426
FLT3 gene mutation 47.40 17.99 8 54429 8 110534854
Chest pain 47.26 17.99 70 54367 376305 110158557
Urticaria 46.52 17.99 53 54384 318804 110216058
Rash 46.48 17.99 227 54210 820737 109714125
Enteritis infectious 46.42 17.99 27 54410 3855 110531007
Fusarium infection 46.19 17.99 24 54413 2747 110532115
Pseudomonal bacteraemia 46.01 17.99 28 54409 4343 110530519
Loss of personal independence in daily activities 45.94 17.99 9 54428 150011 110384851
Haemoglobin abnormal 45.83 17.99 37 54400 9001 110525861
Gastrooesophageal reflux disease 45.26 17.99 16 54421 179960 110354902
Haemophagocytic lymphohistiocytosis 45.03 17.99 66 54371 31493 110503369
Fungal infection 44.03 17.99 85 54352 50721 110484141
Feeling abnormal 43.87 17.99 17 54420 180694 110354168
Brain abscess 43.71 17.99 32 54405 6742 110528120
Myalgia 43.35 17.99 28 54409 222353 110312509
Blood lactate dehydrogenase increased 43.20 17.99 78 54359 44256 110490606
Klebsiella infection 42.73 17.99 51 54386 19958 110514904
Granulocytopenia 42.33 17.99 41 54396 12674 110522188
COVID-19 pneumonia 42.28 17.99 70 54367 37073 110497789
Haemorrhage intracranial 41.94 17.99 61 54376 28908 110505954
Visual impairment 41.30 17.99 8 54429 134420 110400442
Road traffic accident 41.28 17.99 3 54434 107395 110427467
Splenic infarction 40.93 17.99 26 54411 4348 110530514
Febrile infection 40.53 17.99 26 54411 4422 110530440
Stress 40.33 17.99 3 54434 105345 110429517
Graft versus host disease in lung 39.68 17.99 17 54420 1261 110533601
Chest discomfort 39.56 17.99 18 54419 173830 110361032
Myeloid leukaemia 38.20 17.99 15 54422 890 110533972
Medication error 37.64 17.99 4 54433 105362 110429500
Pneumonia klebsiella 37.61 17.99 29 54408 6603 110528259
Platelet disorder 37.30 17.99 23 54414 3652 110531210
Acute graft versus host disease in intestine 37.20 17.99 27 54410 5612 110529250
Palpitations 36.99 17.99 16 54421 159196 110375666
Renal tubular disorder 36.80 17.99 30 54407 7399 110527463
Mucormycosis 36.76 17.99 35 54402 10593 110524269
Neutrophilic dermatosis 36.53 17.99 14 54423 778 110534084
Dry skin 36.21 17.99 5 54432 107648 110427214
Oesophageal candidiasis 36.18 17.99 36 54401 11498 110523364
Hyperhidrosis 35.94 17.99 24 54413 187274 110347588
Liver abscess 35.73 17.99 30 54407 7709 110527153
Pneumonia adenoviral 35.68 17.99 13 54424 627 110534235
Refractory anaemia with an excess of blasts 35.61 17.99 14 54423 833 110534029
Cardiac tamponade 34.93 17.99 35 54402 11272 110523590
Dyspepsia 34.63 17.99 26 54411 190939 110343923
Colitis 34.59 17.99 120 54317 102203 110432659
Myositis 34.56 17.99 58 54379 31058 110503804
Venoocclusive disease 34.35 17.99 27 54410 6323 110528539
Aeromonas infection 34.05 17.99 12 54425 525 110534337
Geotrichum infection 33.97 17.99 15 54422 1197 110533665
Hypercholesterolaemia 33.63 17.99 3 54434 90834 110444028
Enterocolitis 33.59 17.99 44 54393 18905 110515957
Constipation 33.42 17.99 295 54142 357491 110177371
Atypical pneumonia 33.28 17.99 29 54408 7833 110527029
Vision blurred 33.25 17.99 11 54426 129011 110405851
Adenoviral hepatitis 33.20 17.99 14 54423 998 110533864
Juvenile chronic myelomonocytic leukaemia 33.16 17.99 7 54430 39 110534823
Adverse drug reaction 33.03 17.99 6 54431 105553 110429309
Amnesia 32.96 17.99 6 54431 105402 110429460
Catheter site infection 32.85 17.99 29 54408 7971 110526891
Contusion 32.73 17.99 40 54397 233321 110301541
Cystitis haemorrhagic 32.69 17.99 35 54402 12174 110522688
Cough 32.68 17.99 117 54320 461524 110073338
Platelet count abnormal 32.46 17.99 26 54411 6256 110528606
Confusional state 32.38 17.99 120 54317 468560 110066302
COVID-19 31.72 17.99 218 54219 244842 110290020
Lower motor neurone lesion 31.66 17.99 7 54430 50 110534812
Gastrointestinal disorder 31.34 17.99 44 54393 241908 110292954
Cytarabine syndrome 31.20 17.99 8 54429 114 110534748
Primary myelofibrosis 31.18 17.99 9 54428 204 110534658
Cytogenetic abnormality 30.89 17.99 14 54423 1188 110533674
Flushing 30.60 17.99 7 54430 104729 110430133
White blood cell count abnormal 30.29 17.99 26 54411 6883 110527979
Blood pressure systolic increased 30.03 17.99 3 54434 82988 110451874
Interstitial lung disease 29.97 17.99 142 54295 139192 110395670
Acute erythroid leukaemia 29.80 17.99 10 54427 377 110534485
Acute graft versus host disease in liver 29.79 17.99 17 54420 2342 110532520
Pathogen resistance 29.74 17.99 40 54397 17632 110517230
Illness 29.66 17.99 3 54434 82168 110452694
Gingival bleeding 29.05 17.99 42 54395 19797 110515065
Second primary malignancy 29.04 17.99 40 54397 18028 110516834
Hypokalaemia 28.99 17.99 171 54266 182277 110352585
Feeling hot 28.89 17.99 5 54432 91101 110443761
Agitation 28.50 17.99 10 54427 113041 110421821
Ulcerative duodenitis 28.49 17.99 6 54431 33 110534829
Balance disorder 28.23 17.99 11 54426 116549 110418313
Tumour associated fever 28.19 17.99 13 54424 1148 110533714
Neutrophil count abnormal 28.15 17.99 22 54415 5110 110529752
Neutrophilic panniculitis 28.03 17.99 7 54430 89 110534773
Epstein-Barr virus infection reactivation 27.96 17.99 20 54417 4064 110530798
Pseudomonal sepsis 27.94 17.99 28 54409 9018 110525844
Nasal congestion 27.86 17.99 7 54430 98275 110436587
Phlebitis 27.75 17.99 29 54408 9812 110525050
Product quality issue 27.44 17.99 3 54434 77296 110457566
Aplasia 27.37 17.99 26 54411 7847 110527015
Bone marrow disorder 27.36 17.99 20 54417 4203 110530659
Sciatica 27.34 17.99 6 54431 92393 110442469
Erythema nodosum 27.08 17.99 24 54413 6629 110528233
Systemic mycosis 26.79 17.99 19 54418 3810 110531052
Bone marrow transplant 26.59 17.99 14 54423 1646 110533216
Lower limb fracture 26.56 17.99 3 54434 75345 110459517
Gene mutation 26.29 17.99 18 54419 3411 110531451
Hyperleukocytosis 26.25 17.99 18 54419 3421 110531441
Pulmonary haemorrhage 25.81 17.99 36 54401 16420 110518442
Leukaemia cutis 25.68 17.99 8 54429 237 110534625
Central nervous system leukaemia 25.67 17.99 10 54427 581 110534281
Tonsillitis bacterial 25.62 17.99 8 54429 239 110534623
Toxic neuropathy 25.49 17.99 12 54425 1111 110533751
Liver injury 25.37 17.99 22 54415 150391 110384471
Swelling face 25.36 17.99 7 54430 92314 110442548
Septal panniculitis 24.98 17.99 7 54430 142 110534720
Anorectal infection 24.88 17.99 10 54427 631 110534231
Fungaemia 24.86 17.99 22 54415 6064 110528798
Disease risk factor 24.80 17.99 8 54429 266 110534596
Incorrect dose administered 24.74 17.99 10 54427 103631 110431231
Granulocytes abnormal 24.68 17.99 8 54429 270 110534592
Heart rate increased 24.30 17.99 21 54416 143813 110391049
Malassezia infection 24.05 17.99 6 54431 76 110534786
Atrial fibrillation 23.88 17.99 194 54243 229448 110305414
Lactic acidosis 23.76 17.99 8 54429 92803 110442059
Skin infection 23.73 17.99 41 54396 22468 110512394
Granulocyte-colony stimulating factor level decreased 23.70 17.99 4 54433 4 110534858
Rhabdomyolysis 23.68 17.99 15 54422 120386 110414476
Aspiration bone marrow abnormal 23.52 17.99 7 54430 177 110534685
Chronic graft versus host disease 23.38 17.99 26 54411 9431 110525431
Vomiting 23.38 17.99 312 54125 910363 109624499
Escherichia infection 23.33 17.99 42 54395 23774 110511088
Back pain 23.07 17.99 99 54338 370897 110163965
Malignant neoplasm progression 23.00 17.99 156 54281 174411 110360451
Fungal sepsis 22.70 17.99 14 54423 2223 110532639
Pulmonary fibrosis 22.54 17.99 11 54426 102031 110432831
Dysplasia 22.49 17.99 13 54424 1835 110533027
Angiodysplasia 22.18 17.99 12 54425 1490 110533372
Platelet transfusion 21.97 17.99 15 54422 2831 110532031
Wound infection 21.92 17.99 10 54427 96455 110438407
Knee arthroplasty 21.88 17.99 3 54434 64945 110469917
Administration site induration 21.80 17.99 5 54432 43 110534819
Anal infection 21.78 17.99 7 54430 230 110534632
Acute myeloid leukaemia (in remission) 21.60 17.99 5 54432 45 110534817
Wrong technique in product usage process 21.55 17.99 8 54429 87340 110447522
Osteoporosis 21.48 17.99 8 54429 87144 110447718
Clonal evolution 21.36 17.99 7 54430 245 110534617
Splenomegaly 21.24 17.99 41 54396 24457 110510405
Neoplasm progression 21.17 17.99 75 54362 64520 110470342
Transfusion reaction 21.03 17.99 13 54424 2072 110532790
Portal vein cavernous transformation 20.95 17.99 6 54431 132 110534730
Venous aneurysm 20.93 17.99 4 54433 12 110534850
Ear infection 20.89 17.99 3 54434 62729 110472133
Myeloblast count increased 20.69 17.99 5 54432 55 110534807
Transplantation complication 20.66 17.99 8 54429 457 110534405
Haemorrhage subcutaneous 20.62 17.99 19 54418 5520 110529342
Injection site swelling 20.47 17.99 3 54434 61787 110473075
Bradycardia 20.41 17.99 28 54409 155489 110379373
Serum ferritin increased 20.21 17.99 27 54410 11820 110523042
Sinusitis fungal 20.20 17.99 14 54423 2706 110532156
Pseudomembranous colitis 20.14 17.99 20 54417 6371 110528491
Sinusitis aspergillus 20.09 17.99 7 54430 296 110534566
Diverticulitis 20.06 17.99 65 54372 53457 110481405
Ulcerative gastritis 19.97 17.99 6 54431 157 110534705
Tinnitus 19.92 17.99 3 54434 60537 110474325
Application site abscess 19.85 17.99 3 54434 0 110534862
Isocitrate dehydrogenase gene mutation 19.85 17.99 3 54434 0 110534862
Injection site vasculitis 19.84 17.99 4 54433 17 110534845
Swollen tongue 19.84 17.99 3 54434 60359 110474503
Hypoalbuminaemia 19.84 17.99 44 54393 28930 110505932
Heart rate decreased 19.73 17.99 8 54429 82748 110452114
Loss of consciousness 19.66 17.99 42 54395 196264 110338598
Pseudomonal skin infection 19.66 17.99 4 54433 18 110534844
Lung consolidation 19.63 17.99 25 54412 10451 110524411
Neck pain 19.59 17.99 19 54418 123111 110411751
Hypoglycaemia 19.55 17.99 17 54420 116087 110418775
Blast cell count decreased 19.48 17.99 4 54433 19 110534843
Aggression 19.33 17.99 3 54434 59207 110475655
Streptococcal bacteraemia 19.32 17.99 17 54420 4652 110530210
Aspiration bone marrow 19.32 17.99 6 54431 176 110534686
Acinetobacter bacteraemia 19.18 17.99 7 54430 339 110534523
Leukaemic infiltration extramedullary 19.07 17.99 7 54430 345 110534517
Pulmonary resection 18.76 17.99 6 54431 194 110534668
Lung infiltration 18.70 17.99 39 54398 24589 110510273
Staphylococcal infection 18.62 17.99 76 54361 69868 110464994
Transfusion related complication 18.56 17.99 4 54433 25 110534837
Skin maceration 18.22 17.99 6 54431 213 110534649
Subarachnoid haemorrhage 18.02 17.99 43 54394 29659 110505203

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01BC07 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
ANTIMETABOLITES
Pyrimidine analogues
FDA MoA N0000000233 Nucleic Acid Synthesis Inhibitors
CHEBI has role CHEBI:33231 antitubercular agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:231911 renoprotective agent
CHEBI has role CHEBI:233423 antifibrotic agent
MeSH PA D000963 Antimetabolites
MeSH PA D000964 Antimetabolites, Antineoplastic
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
FDA EPC N0000175595 Nucleoside Metabolic Inhibitor

Related Drugs by ATC class:

L01BC Pyrimidine analogues 9 drugs
capecitabinecarmofurcytarabinedecitabinefloxuridinefluorouracilgemcitabinetegafurtrifluridine

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

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009
Myelodysplastic syndrome indication 109995007
Chronic myelomonocytic leukemia indication 127225006
Hepatic failure contraindication 59927004
Kidney disease contraindication 90708001 DOID:557
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Advanced Malignant Neoplasm of Liver contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.32 acidic
pKa2 12.92 acidic
pKa3 13.79 acidic
pKa4 4.43 Basic
pKa5 2.98 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
200MG ONUREG BRISTOL N214120 Sept. 1, 2020 RX TABLET ORAL 12053482 May 14, 2029 CONTINUED TREATMENT OF ADULTS WITH ACUTE MYELOID LEUKEMIA WHO ACHIEVED FIRST COMPLETE REMISSION (CR) OR CR WITH INCOMPLETE BLOOD COUNT RECOVERY FOLLOWING INTENSIVE INDUCTION CHEMOTHERAPY AND ARE NOT ABLE TO COMPLETE INTENSIVE CURATIVE THERAPY
300MG ONUREG BRISTOL N214120 Sept. 1, 2020 RX TABLET ORAL 12053482 May 14, 2029 CONTINUED TREATMENT OF ADULTS WITH ACUTE MYELOID LEUKEMIA WHO ACHIEVED FIRST COMPLETE REMISSION (CR) OR CR WITH INCOMPLETE BLOOD COUNT RECOVERY FOLLOWING INTENSIVE INDUCTION CHEMOTHERAPY AND ARE NOT ABLE TO COMPLETE INTENSIVE CURATIVE THERAPY
200MG ONUREG BRISTOL N214120 Sept. 1, 2020 RX TABLET ORAL 8846628 June 3, 2030 CONTINUED TREATMENT OF ADULTS WITH ACUTE MYELOID LEUKEMIA WHO ACHIEVED FIRST COMPLETE REMISSION (CR) OR CR WITH INCOMPLETE BLOOD COUNT RECOVERY FOLLOWING INTENSIVE INDUCTION CHEMOTHERAPY AND ARE NOT ABLE TO COMPLETE INTENSIVE CURATIVE THERAPY
300MG ONUREG BRISTOL N214120 Sept. 1, 2020 RX TABLET ORAL 8846628 June 3, 2030 CONTINUED TREATMENT OF ADULTS WITH ACUTE MYELOID LEUKEMIA WHO ACHIEVED FIRST COMPLETE REMISSION (CR) OR CR WITH INCOMPLETE BLOOD COUNT RECOVERY FOLLOWING INTENSIVE INDUCTION CHEMOTHERAPY AND ARE NOT ABLE TO COMPLETE INTENSIVE CURATIVE THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
200MG ONUREG BRISTOL N214120 Sept. 1, 2020 RX TABLET ORAL Sept. 1, 2027 INDICATED FOR CONTINUED TREATMENT OF ADULT PATIENTS WITH ACUTE MYELOID LEUKEMIA WHO ACHIEVED FIRST COMPLETE REMISSION (CR) OR COMPLETE REMISSION WITH INCOMPLETE BLOOD COUNT RECOVERY (CRI) FOLLOWING INTENSIVE INDUCTION CHEMOTHERAPY AND ARE NOT ABLE TO COMPLETE INTENSIVE CURATIVE THERAPY
300MG ONUREG BRISTOL N214120 Sept. 1, 2020 RX TABLET ORAL Sept. 1, 2027 INDICATED FOR CONTINUED TREATMENT OF ADULT PATIENTS WITH ACUTE MYELOID LEUKEMIA WHO ACHIEVED FIRST COMPLETE REMISSION (CR) OR COMPLETE REMISSION WITH INCOMPLETE BLOOD COUNT RECOVERY (CRI) FOLLOWING INTENSIVE INDUCTION CHEMOTHERAPY AND ARE NOT ABLE TO COMPLETE INTENSIVE CURATIVE THERAPY
100MG/VIAL VIDAZA BRISTOL-MYERS N050794 May 19, 2004 RX POWDER INTRAVENOUS, SUBCUTANEOUS May 20, 2029 TREATMENT OF PEDIATRIC PATIENTS AGED ONE MONTH AND OLDER WITH NEWLY DIAGNOSED JUVENILE MYELOMONOCYTIC LEUKEMIA (JMML)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
DNA (cytosine-5)-methyltransferase 1 Enzyme INHIBITOR IC50 6.52 CHEMBL CHEMBL
DNA (cytosine-5)-methyltransferase 3A Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
4021468 VUID
N0000148852 NUI
D03021 KEGG_DRUG
1251 RXNORM
C0004475 UMLSCUI
CHEBI:2038 CHEBI
5AE PDB_CHEM_ID
CHEMBL1489 ChEMBL_ID
D001374 MESH_DESCRIPTOR_UI
DB00928 DRUGBANK_ID
6796 IUPHAR_LIGAND_ID
4520 INN_ID
M801H13NRU UNII
9444 PUBCHEM_CID
18639 MMSL
205981 MMSL
53994 MMSL
d05293 MMSL
4021468 VANDF
008661 NDDF
412328000 SNOMEDCT_US
412329008 SNOMEDCT_US
M801H13NRU INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 0143-9606 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine Human Prescription Drug Label 1 0781-3491 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 16714-927 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 16729-306 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 25 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 31722-365 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 43598-305 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 43598-305 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 43598-465 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 24 sections
AZACITIDINE AZACITIDINE HUMAN PRESCRIPTION DRUG LABEL 1 43598-678 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 43817-906 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 28 sections
AZACITIDINE Human Prescription Drug Label 1 55150-393 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 58458-002 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
VIDAZA HUMAN PRESCRIPTION DRUG LABEL 1 59572-102 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS NDA 26 sections
ONUREG HUMAN PRESCRIPTION DRUG LABEL 1 59572-730 TABLET, FILM COATED 200 mg ORAL NDA 30 sections
ONUREG HUMAN PRESCRIPTION DRUG LABEL 1 59572-740 TABLET, FILM COATED 300 mg ORAL NDA 30 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 60505-6271 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 26 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 63323-771 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 68001-313 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS NDA 17 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 68001-527 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 68001-620 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine Human Prescription Drug Label 1 69539-112 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 70069-857 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
AZACITIDINE HUMAN PRESCRIPTION DRUG LABEL 1 70121-1237 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 25 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 71288-115 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 25 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 71288-153 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 25 sections
AZACITIDINE HUMAN PRESCRIPTION DRUG LABEL 1 72485-201 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine Human Prescription Drug Label 1 72572-020 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 24 sections
Azacitidine HUMAN PRESCRIPTION DRUG LABEL 1 75907-225 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg SUBCUTANEOUS ANDA 24 sections
AZACITIDINE HUMAN PRESCRIPTION DRUG LABEL 1 83774-102 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 23 sections