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

Stem definitionDrug idCAS RN
antineoplastics, daunorubicin derivatives 1414 58957-92-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • idarubicin
  • 4-Demethoxydaunomycin
  • 4-Demethoxydaunorubicin
  • demethoxydaunorubicin
  • idarubicin hydrochloride
  • idarubicin HCl
An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.
  • Molecular weight: 497.50
  • Formula: C26H27NO9
  • CLOGP: 0.84
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 5
  • TPSA: 176.61
  • ALOGS: -2.81
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 3 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.43 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 28 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 38 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 24 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.08 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 16 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 10 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.495 Moderate 0.75
caco2-efflux Caco-2 efflux ratio (BA/AB) 13.740 Moderate 0.75
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 15.417 10^-6 cm/s Moderate 0.75
dh-clint Dog hepatocyte intrinsic clearance 3.963 uL/min/10^6 cells Moderate 0.75
dppb Dog plasma protein binding (% unbound) 16.630 % Moderate 0.75
fcs-ppb Fetal calf serum protein binding (% unbound) 15.160 % Moderate 0.75
herg hERG pIC50 4.729 pIC50 Moderate 0.75
hh-clint Human hepatocyte intrinsic clearance 2.399 uL/min/10^6 cells Moderate 0.75
hlm-clint Human liver microsomal intrinsic clearance 3.334 uL/min/mg protein Moderate 0.75
hppb Human plasma protein binding (% unbound) 10.070 % Moderate 0.75
kinase-safety-class ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,KDR,KIT,MAP2K6,MAP3K14,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 46
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 39.355 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 18.323 Moderate 0.75
mh-clint Mouse hepatocyte intrinsic clearance 8.091 Moderate 0.75
mppb Mouse plasma protein binding (% unbound) 11.890 Moderate 0.75
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 33.420 Moderate 0.75
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
pppb Pig plasma protein binding (% unbound) 15.130 % Moderate 0.75
rat-kpuu-brain Rat brain Kpuu 0.018 % High 1
rh-clint Rat hepatocyte intrinsic clearance 5.610 uL/min/10^6 cells Moderate 0.75
rh-fuinc Rat hepatocyte fraction unbound in incubation 54.140 % Moderate 0.75
rppb Rat plasma protein binding (% unbound) 9.320 % Moderate 0.75
solubility-dd Solubility at pH 7.4 in DMSO 22.699 uM Moderate 0.75

Approvals:

DateAgencyCompanyOrphan
Sept. 27, 1990 FDA

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 774.21 37.95 331 6801 158018 90463297
Myelosuppression 234.26 37.95 104 7028 53487 90567828
Acute myeloid leukaemia recurrent 214.19 37.95 46 7086 2011 90619304
Neutropenia 202.56 37.95 156 6976 224748 90396567
Differentiation syndrome 198.02 37.95 40 7092 1291 90620024
Mucosal inflammation 196.06 37.95 94 7038 57531 90563784
Geotrichum infection 175.88 37.95 32 7100 584 90620731
Fusarium infection 169.82 37.95 34 7098 1048 90620267
Acute myeloid leukaemia 169.35 37.95 63 7069 20577 90600738
Sepsis 168.96 37.95 128 7004 179686 90441629
Septic shock 165.19 37.95 95 7037 84065 90537250
Thrombocytopenia 154.19 37.95 129 7003 208596 90412719
Pancytopenia 148.18 37.95 101 7031 120162 90501153
Neutropenic colitis 148.02 37.95 39 7093 4104 90617211
Second primary malignancy 144.44 37.95 47 7085 10331 90610984
Multiple organ dysfunction syndrome 139.05 37.95 79 7053 68257 90553058
Neoplasm recurrence 137.41 37.95 35 7097 3224 90618091
Bone marrow failure 120.05 37.95 56 7076 32165 90589150
Acute lymphocytic leukaemia recurrent 113.62 37.95 29 7103 2692 90618623
Pseudomonas infection 109.68 37.95 42 7090 14823 90606492
Leukaemia recurrent 88.42 37.95 21 7111 1446 90619869
Bronchopulmonary aspergillosis 86.94 37.95 33 7099 11365 90609950
Pneumonia fungal 82.48 37.95 28 7104 7003 90614312
Gene mutation 80.64 37.95 21 7111 2109 90619206
Myelodysplastic syndrome 76.82 37.95 36 7096 20867 90600448
Neurotoxicity 72.85 37.95 35 7097 21432 90599883
Neutropenic sepsis 69.02 37.95 32 7100 18098 90603217
Leukoerythroblastosis 68.65 37.95 13 7119 297 90621018
Aspergillus infection 67.22 37.95 27 7105 10796 90610519
Haemophagocytic lymphohistiocytosis 61.08 37.95 28 7104 15431 90605884
Mucormycosis 60.10 37.95 19 7113 3802 90617513
Dysplasia 58.90 37.95 15 7117 1379 90619936
Lower respiratory tract infection fungal 57.61 37.95 11 7121 263 90621052
Endophthalmitis 56.30 37.95 19 7113 4666 90616649
Febrile bone marrow aplasia 56.04 37.95 23 7109 9715 90611600
Disseminated intravascular coagulation 55.10 37.95 29 7103 21509 90599806
Pneumatosis intestinalis 53.68 37.95 17 7115 3420 90617895
Dedifferentiated liposarcoma 52.95 37.95 8 7124 42 90621273
Off label use 51.37 37.95 196 6936 1102056 89519259
Pathogen resistance 49.55 37.95 20 7112 8095 90613220
Bacteraemia 48.60 37.95 27 7105 22273 90599042
Pain 48.14 37.95 10 7122 996331 89624984
Ejection fraction decreased 47.10 37.95 28 7104 26225 90595090
Ventricular hypokinesia 46.34 37.95 17 7115 5324 90615991
Fungal infection 45.84 37.95 33 7099 42628 90578687
Chloroma 45.80 37.95 9 7123 251 90621064
Hyperbilirubinaemia 45.10 37.95 22 7110 13914 90607401
Nephropathy toxic 43.99 37.95 21 7111 12667 90608648
Subclavian vein thrombosis 43.83 37.95 13 7119 2103 90619212
Posterior reversible encephalopathy syndrome 43.16 37.95 25 7107 22314 90599001
Fungaemia 41.89 37.95 14 7118 3336 90617979
Arthralgia 41.54 37.95 6 7126 778516 89842799
Tumour lysis syndrome 40.33 37.95 19 7113 11133 90610182
Respiratory failure 40.10 37.95 48 7084 118370 90502945
Enterococcal bacteraemia 40.01 37.95 12 7120 2016 90619299
Enterococcal infection 39.16 37.95 18 7114 9973 90611342
Haematopoietic neoplasm 38.75 37.95 6 7126 38 90621277

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 558.38 30.72 390 8453 185313 42427179
Acute myeloid leukaemia recurrent 259.73 30.72 72 8771 3440 42609052
Myelosuppression 187.18 30.72 112 8731 40349 42572143
Neutropenia 184.07 30.72 216 8627 199215 42413277
Pancytopenia 183.49 30.72 169 8674 117574 42494918
Bone marrow failure 154.04 30.72 92 8751 33001 42579491
Fungal infection 150.44 30.72 76 8767 19646 42592846
Bronchopulmonary aspergillosis 139.84 30.72 72 8771 19357 42593135
Acute myeloid leukaemia 133.41 30.72 73 8770 22183 42590309
Differentiation syndrome 124.10 30.72 35 8808 1778 42610714
Mucormycosis 113.62 30.72 46 8797 7097 42605395
Thrombocytopenia 112.81 30.72 166 8677 190113 42422379
Septic shock 107.88 30.72 113 8730 91559 42520933
Cytomegalovirus infection reactivation 102.92 30.72 49 8794 11129 42601363
Myelodysplastic syndrome 102.59 30.72 62 8781 22683 42589809
Fusarium infection 100.72 30.72 29 8814 1587 42610905
Venoocclusive liver disease 91.32 30.72 44 8799 10258 42602234
Graft versus host disease 84.69 30.72 45 8798 12880 42599612
Aspergillus infection 84.12 30.72 48 8795 15789 42596703
Febrile bone marrow aplasia 74.00 30.72 38 8805 10143 42602349
Second primary malignancy 73.26 30.72 37 8806 9538 42602954
Sepsis 72.63 30.72 140 8703 199194 42413298
Pyrexia 69.85 30.72 209 8634 393833 42218659
Neutropenic colitis 68.38 30.72 28 8815 4442 42608050
Pneumonia fungal 66.07 30.72 34 8809 9112 42603380
Aeromonas infection 64.62 30.72 15 8828 345 42612147
Hyperbilirubinaemia 55.99 30.72 41 8802 20594 42591898
Neoplasm progression 53.68 30.72 46 8797 28954 42583538
Geotrichum infection 52.79 30.72 14 8829 563 42611929
Chronic graft versus host disease 51.17 30.72 25 8818 6000 42606492
Mucosal inflammation 49.49 30.72 56 8787 49318 42563174
Rash maculo-papular 49.04 30.72 49 8794 37454 42575038
Rhabdomyosarcoma recurrent 48.03 30.72 10 8833 136 42612356
Fatigue 43.64 30.72 18 8825 435623 42176869
Device related infection 43.41 30.72 35 8808 20244 42592248
Infection 41.05 30.72 79 8764 111989 42500503
Acute graft versus host disease in skin 40.75 30.72 23 8820 7401 42605091
Adenomatous polyposis coli 40.21 30.72 9 8834 175 42612317
Premature ageing 39.66 30.72 8 8835 92 42612400
Stenotrophomonas infection 39.55 30.72 18 8825 3686 42608806
Pain 39.44 30.72 3 8840 244845 42367647
Neoplasm recurrence 38.07 30.72 16 8827 2708 42609784
Drug resistance 38.03 30.72 41 8802 34207 42578285
Enamel anomaly 37.79 30.72 9 8834 232 42612260
Haematopoietic neoplasm 37.70 30.72 7 8836 50 42612442
Dizziness 37.61 30.72 4 8839 249250 42363242
Tooth hypoplasia 37.11 30.72 9 8834 251 42612241
Reticulocytosis 35.83 30.72 9 8834 291 42612201
Acute respiratory distress syndrome 35.12 30.72 37 8806 30071 42582421
Respiratory failure 34.88 30.72 80 8763 128052 42484440
Poikiloderma 34.82 30.72 9 8834 327 42612165
Systemic mycosis 33.29 30.72 14 8829 2373 42610119
Leukaemia recurrent 33.01 30.72 13 8830 1863 42610629
Off label use 32.23 30.72 234 8609 638101 41974391
Large granular lymphocytosis 31.96 30.72 8 8835 255 42612237
Anti-platelet antibody positive 31.49 30.72 8 8835 271 42612221
Bacteraemia 31.41 30.72 32 8811 25008 42587484
Escherichia bacteraemia 31.12 30.72 17 8826 5132 42607360
Recurrent cancer 30.87 30.72 12 8831 1661 42610831

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 1272.01 27.63 696 14940 316071 110257592
Acute myeloid leukaemia recurrent 398.43 27.63 101 15535 5038 110568625
Myelosuppression 383.44 27.63 210 15426 94130 110479533
Neutropenia 362.90 27.63 348 15288 374272 110199391
Differentiation syndrome 302.35 27.63 73 15563 2971 110570692
Fusarium infection 298.73 27.63 71 15565 2700 110570963
Bone marrow failure 283.57 27.63 146 15490 57702 110515961
Acute myeloid leukaemia 283.35 27.63 128 15508 37982 110535681
Septic shock 268.92 27.63 203 15433 157325 110416338
Thrombocytopenia 253.71 27.63 278 15358 348607 110225056
Pancytopenia 243.79 27.63 216 15420 209397 110364266
Neutropenic colitis 219.50 27.63 70 15566 7995 110565668
Sepsis 212.53 27.63 246 15390 327100 110246563
Geotrichum infection 211.50 27.63 46 15590 1166 110572497
Second primary malignancy 208.68 27.63 83 15553 17985 110555678
Bronchopulmonary aspergillosis 205.27 27.63 95 15541 29768 110543895
Fungal infection 186.81 27.63 106 15530 50700 110522963
Mucosal inflammation 186.69 27.63 134 15502 96007 110477656
Myelodysplastic syndrome transformation 170.86 27.63 36 15600 781 110572882
Myelodysplastic syndrome 164.77 27.63 88 15548 37396 110536267
Pneumonia fungal 147.11 27.63 61 15575 14693 110558970
Aspergillus infection 141.07 27.63 70 15566 25546 110548117
Mucormycosis 141.01 27.63 54 15582 10574 110563089
Neoplasm recurrence 140.67 27.63 45 15591 5187 110568476
Venoocclusive liver disease 122.30 27.63 54 15582 15153 110558510
Multiple organ dysfunction syndrome 110.11 27.63 121 15515 151589 110422074
Acute lymphocytic leukaemia recurrent 108.72 27.63 38 15598 5749 110567914
Hyperbilirubinaemia 107.37 27.63 62 15574 30609 110543054
Cytomegalovirus infection reactivation 106.61 27.63 52 15584 18281 110555382
Graft versus host disease 105.35 27.63 52 15584 18754 110554909
Pyrexia 102.99 27.63 319 15317 897946 109675717
Febrile bone marrow aplasia 99.94 27.63 49 15587 17416 110556247
Pain 92.07 27.63 13 15623 954942 109618721
Pathogen resistance 90.55 27.63 46 15590 17626 110556037
Pseudomonas infection 88.79 27.63 53 15583 27800 110545863
Drug resistance 81.60 27.63 66 15570 56308 110517355
Leukaemia recurrent 80.36 27.63 26 15610 3105 110570558
Respiratory failure 78.06 27.63 122 15514 215210 110358453
Arthralgia 76.55 27.63 10 15626 779622 109794041
Haematopoietic neoplasm 76.26 27.63 13 15623 83 110573580
Bacteraemia 75.22 27.63 56 15580 42334 110531329
Neoplasm progression 73.77 27.63 66 15570 64529 110509134
Rash maculo-papular 73.45 27.63 70 15566 74152 110499511
Fatigue 68.48 27.63 44 15592 1215914 109357749
Aeromonas infection 64.37 27.63 15 15621 522 110573141
Pneumonia 64.05 27.63 269 15367 876445 109697218
Dizziness 63.83 27.63 11 15625 698182 109875481
Haemophagocytic lymphohistiocytosis 63.51 27.63 45 15591 31514 110542149
Acute respiratory distress syndrome 62.02 27.63 55 15581 53143 110520520
Stenotrophomonas infection 61.03 27.63 25 15611 5833 110567830
Fungaemia 60.11 27.63 25 15611 6061 110567602
Cytopenia 58.44 27.63 42 15594 30074 110543589
Fall 56.27 27.63 9 15627 603473 109970190
Acute graft versus host disease in skin 55.15 27.63 28 15608 10712 110562951
Dysplasia 54.25 27.63 17 15619 1831 110571832
Agranulocytosis 53.18 27.63 54 15582 61706 110511957
Chronic graft versus host disease 52.51 27.63 26 15610 9431 110564232
Myocarditis 51.74 27.63 39 15597 30016 110543647
Disseminated intravascular coagulation 50.76 27.63 44 15592 41242 110532421
Malaise 50.69 27.63 16 15620 671803 109901860
Drug ineffective 50.02 27.63 376 15260 1520164 109053499
Off label use 48.79 27.63 370 15266 1499815 109073848
Tumour lysis syndrome 48.71 27.63 38 15598 30763 110542900
Weight decreased 48.38 27.63 5 15631 468052 110105611
Product use in unapproved indication 47.45 27.63 155 15481 447222 110126441
Drug hypersensitivity 46.55 27.63 5 15631 454085 110119578
Pulmonary haemorrhage 46.51 27.63 29 15607 16427 110557236
Peripheral swelling 45.38 27.63 3 15633 404031 110169632
Neutropenic infection 44.88 27.63 17 15619 3228 110570435
Aplasia 44.77 27.63 22 15614 7851 110565812
Chloroma 43.40 27.63 12 15624 836 110572827
Dyspnoea 43.27 27.63 56 15580 1106816 109466847
Lower respiratory tract infection fungal 43.27 27.63 12 15624 845 110572818
Enterococcal bacteraemia 42.96 27.63 18 15618 4443 110569220
Escherichia bacteraemia 42.23 27.63 23 15613 10141 110563522
Premature ageing 42.11 27.63 8 15628 100 110573563
Neurotoxicity 42.11 27.63 40 15596 42167 110531496
Abdominal discomfort 41.24 27.63 4 15632 393854 110179809
Cytarabine syndrome 41.14 27.63 8 15628 114 110573549
Leukaemia cutis 41.08 27.63 9 15627 236 110573427
Transformation to acute myeloid leukaemia 40.53 27.63 13 15623 1510 110572153
Cytomegalovirus infection 40.44 27.63 44 15592 54400 110519263
Hidradenitis 40.38 27.63 18 15618 5162 110568501
Gastrointestinal mucormycosis 40.30 27.63 11 15625 730 110572933
Ventricular hypokinesia 40.12 27.63 23 15613 11191 110562472
Posterior reversible encephalopathy syndrome 39.44 27.63 35 15601 33826 110539837
Ejection fraction decreased 39.37 27.63 38 15598 40842 110532821
Rhabdomyosarcoma recurrent 38.87 27.63 8 15628 154 110573509
Device related infection 38.56 27.63 37 15599 39482 110534181
Adenomatous polyposis coli 38.41 27.63 9 15627 321 110573342
Neutropenic sepsis 38.26 27.63 33 15603 30713 110542950
Leukoerythroblastosis 38.01 27.63 9 15627 336 110573327
Chromosomal deletion 37.99 27.63 8 15628 173 110573490
T-cell type acute leukaemia 37.88 27.63 9 15627 341 110573322
Pain in extremity 37.80 27.63 11 15625 487107 110086556
Cardiomyopathy 37.76 27.63 34 15602 33491 110540172
Tooth hypoplasia 37.70 27.63 9 15627 348 110573315
Weight increased 37.46 27.63 7 15629 419637 110154026
Pruritus 37.01 27.63 18 15618 581542 109992121
Recurrent cancer 37.00 27.63 15 15621 3408 110570255
Insomnia 36.87 27.63 4 15632 360586 110213077
Streptococcal bacteraemia 35.67 27.63 16 15620 4653 110569010
Enamel anomaly 35.61 27.63 8 15628 236 110573427
Haematotoxicity 35.50 27.63 27 15609 21055 110552608
Systemic mycosis 35.37 27.63 15 15621 3814 110569849
Poikiloderma 34.84 27.63 9 15627 483 110573180
Pneumatosis intestinalis 34.60 27.63 19 15617 8510 110565153
Urticaria 34.01 27.63 3 15633 318854 110254809
Leukaemia 34 27.63 18 15618 7500 110566163
Drug intolerance 33.78 27.63 8 15628 406504 110167159
Hypoaesthesia 33.40 27.63 3 15633 314220 110259443
Swelling 33.22 27.63 5 15631 351036 110222627
Alpha haemolytic streptococcal infection 32.94 27.63 14 15622 3579 110570084
Anti-platelet antibody positive 32.74 27.63 8 15628 342 110573321
Infective aneurysm 32.71 27.63 11 15625 1481 110572182
Infusion related reaction 32.68 27.63 7 15629 381155 110192508
Reticulocytosis 32.49 27.63 9 15627 631 110573032
Pulmonary mucormycosis 32.46 27.63 12 15624 2131 110571532
Graft versus host disease in skin 32.42 27.63 18 15618 8236 110565427
Klebsiella infection 32.32 27.63 25 15611 19984 110553679
Haemorrhagic pneumonia 31.75 27.63 7 15629 189 110573474
Granulocyte count decreased 31.59 27.63 14 15622 3960 110569703
Central nervous system infection 31.10 27.63 11 15625 1721 110571942
Necrotising fasciitis 31.04 27.63 17 15619 7574 110566089
Graft versus host disease in gastrointestinal tract 31.03 27.63 18 15618 8950 110564713
Colitis 30.33 27.63 53 15583 102270 110471393
Blood bilirubin increased 30.24 27.63 45 15591 75927 110497736
Retinal haemorrhage 30.07 27.63 18 15618 9483 110564180
Endophthalmitis 29.84 27.63 17 15619 8170 110565493
Large granular lymphocytosis 29.53 27.63 8 15628 516 110573147
Philadelphia chromosome positive 29.46 27.63 9 15627 891 110572772
Coombs direct test positive 29.40 27.63 8 15628 525 110573138
Subclavian vein thrombosis 29.21 27.63 12 15624 2820 110570843
Central nervous system leukaemia 28.58 27.63 8 15628 583 110573080
Gamma-glutamyltransferase increased 28.35 27.63 39 15597 61270 110512393
Cardiac failure acute 28.27 27.63 25 15611 24053 110549610
Nausea 28.01 27.63 86 15550 1235604 109338059
Pleural effusion 27.95 27.63 71 15565 177638 110396025

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01DB06 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
CYTOTOXIC ANTIBIOTICS AND RELATED SUBSTANCES
Anthracyclines and related substances
FDA CS M0028312 Anthracyclines
FDA MoA N0000000176 Topoisomerase Inhibitors
FDA EPC N0000175414 Anthracycline Topoisomerase Inhibitor
MeSH PA D000903 Antibiotics, Antineoplastic
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D059005 Topoisomerase II Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

L01DB Anthracyclines and related substances 10 drugs
aclarubicinamrubicindaunorubicindoxorubicinepirubicinmitoxantronepirarubicinpixantronevalrubicinzorubicin

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

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009
Acute promyelocytic leukemia, FAB M3 indication 110004001
Pericarditis contraindication 3238004 DOID:1787
Enterocolitis contraindication 43752006
Conduction disorder of the heart contraindication 44808001
Chronic heart failure contraindication 48447003
Myocarditis contraindication 50920009 DOID:820
Gastrointestinal perforation contraindication 51875005
Acute infectious disease contraindication 63171007
Cardiomyopathy contraindication 85898001 DOID:0050700
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Bone marrow depression contraindication 307762000
Breastfeeding (mother) contraindication 413712001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.01 acidic
pKa2 9.88 acidic
pKa3 11.6 acidic
pKa4 8.73 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
DNA topoisomerase 2-alpha Enzyme INHIBITOR IC50 8.59 CHEMBL CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK

External reference:

IDSource
4019784 VUID
N0000147874 NUI
D01747 KEGG_DRUG
57852-57-0 SECONDARY_CAS_RN
4019569 VANDF
4019784 VANDF
C0020789 UMLSCUI
DM5 PDB_CHEM_ID
CHEMBL1117 ChEMBL_ID
CHEMBL1200976 ChEMBL_ID
D015255 MESH_DESCRIPTOR_UI
DB01177 DRUGBANK_ID
7083 IUPHAR_LIGAND_ID
5174 INN_ID
ZRP63D75JW UNII
42890 PUBCHEM_CID
5650 RXNORM
45101 MMSL
4865 MMSL
d00256 MMSL
003556 NDDF
004819 NDDF
108786002 SNOMEDCT_US
108788001 SNOMEDCT_US
372539000 SNOMEDCT_US
CHEBI:42068 CHEBI
ZRP63D75JW INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Idamycin PFS HUMAN PRESCRIPTION DRUG LABEL 1 0013-2576 SOLUTION 1 mg INTRAVENOUS NDA 28 sections
Idamycin PFS HUMAN PRESCRIPTION DRUG LABEL 1 0013-2586 SOLUTION 1 mg INTRAVENOUS NDA 28 sections
Idamycin PFS HUMAN PRESCRIPTION DRUG LABEL 1 0013-2596 SOLUTION 1 mg INTRAVENOUS NDA 28 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9217 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9218 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9219 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9306 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9307 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9308 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71288-184 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71288-185 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Idarubicin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71288-186 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections