arsenic trioxide ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
244 1327-53-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trisenox
  • arsenic trioxide
  • arsenic oxide
  • arsenious oxide
  • arsenious trioxide
  • white arsenic
Arsenic trioxide causes morphological changes and DNA fragmentation characteristic of apoptosis in NB4 human promyelocytic leukemia cells in vitro. Arsenic trioxide also causes damage or degradation of the fusion protein promyelocytic leukemia (PML)ยญ retinoic acid receptor (RAR)-alpha.
  • Molecular weight: 197.84
  • Formula: As2O3
  • CLOGP: -2.60
  • LIPINSKI: None
  • HAC: 3
  • HDO: 0
  • TPSA: 43.37
  • ALOGS:
  • ROTB: 2

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
7.50 mg P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.76 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility) 37 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,GRK2,GRK3,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K3,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 85
kinase-selectivity-class ACVR2B,AXL,CDK9,DYRK1B,EIF2AK3,GRK2,GSK3B,HIPK2,MAP2K6,MAP3K14,MAPK7,MAPK8,PIK3CB,PIK3CG,PRKDC,STK33,TEK,TGFBR1,TTK,UHMK1 20
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Nov. 14, 2019 EMA ACCORD HEALTHCARE SLU
Sept. 25, 2000 FDA CEPHALON

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
Differentiation syndrome 760.99 13.56 133 10854 1198 90616262
Electrocardiogram QT prolonged 203.10 13.56 120 10867 72336 90545124
Febrile neutropenia 96.38 13.56 107 10880 158242 90459218
Hepatic function abnormal 87.92 13.56 60 10927 46228 90571232
Intracranial pressure increased 54.37 13.56 23 10964 6788 90610672
White blood cell count decreased 50.30 13.56 80 10907 167029 90450431
Platelet count decreased 44.59 13.56 68 10919 136901 90480559
Alanine aminotransferase increased 43.20 13.56 62 10925 118276 90499184
Idiopathic intracranial hypertension 42.16 13.56 16 10971 3565 90613895
Aspartate aminotransferase increased 42.15 13.56 57 10930 102880 90514580
Disseminated intravascular coagulation 38.71 13.56 27 10960 21511 90595949
Lower respiratory tract infection fungal 35.91 13.56 8 10979 266 90617194
Leukaemia recurrent 34.56 13.56 11 10976 1456 90616004
Neutrophil count decreased 32.98 13.56 42 10945 71490 90545970
Pericardial effusion 31.64 13.56 30 10957 36803 90580657
Leukocytosis 30.03 13.56 27 10960 30963 90586497
Haematopoietic neoplasm 29.22 13.56 5 10982 39 90617421
Myelosuppression 28.80 13.56 34 10953 53557 90563903
Acute myeloid leukaemia 28.35 13.56 22 10965 20618 90596842
Systemic lupus erythematosus 28.08 13.56 5 10982 361891 90255569
Contraindicated product administered 23.62 13.56 5 10982 320134 90297326
Bone marrow necrosis 23.55 13.56 5 10982 132 90617328
Drug intolerance 22.76 13.56 13 10974 447578 90169882
Respiratory failure 21.97 13.56 46 10941 118372 90499088
Discomfort 20.83 13.56 4 10983 274331 90343129
Pyrexia 20.77 13.56 144 10843 660341 89957119
Gamma-glutamyltransferase increased 20.26 13.56 24 10963 37928 90579532
Gambling 20.25 13.56 5 10982 261 90617199
Blood lactate dehydrogenase increased 20.16 13.56 20 10967 25912 90591548
Wound 19.90 13.56 6 10981 302974 90314486
Chromosomal deletion 18.94 13.56 4 10983 103 90617357
VIth nerve paralysis 18.17 13.56 6 10981 892 90616568
Laryngeal inflammation 17.84 13.56 4 10983 137 90617323
Long QT syndrome 17.70 13.56 9 10978 4028 90613432
General physical health deterioration 17.09 13.56 11 10976 355104 90262356
Sweat gland tumour 17.05 13.56 4 10983 168 90617292
Blast cell count increased 16.85 13.56 5 10982 524 90616936
Infusion related reaction 16.18 13.56 16 10971 416764 90200696
Ventricular extrasystoles 15.80 13.56 13 10974 13237 90604223
Therapeutic product effect decreased 15.69 13.56 7 10980 277564 90339896
Chills 15.54 13.56 43 10944 131938 90485522
Arthropathy 15.48 13.56 13 10974 366229 90251231
Oedematous pancreatitis 14.90 13.56 5 10982 780 90616680
Leukostasis syndrome 14.57 13.56 3 10984 68 90617392
Hypoxia 14.46 13.56 29 10958 72370 90545090
Swelling 14.18 13.56 18 10969 419040 90198420
Blood cholesterol increased 13.87 13.56 4 10983 208008 90409452
Hyperaesthesia 13.81 13.56 11 10976 10691 90606769
Gastrointestinal disorder 13.70 13.56 7 10980 256680 90360780
Abdominal discomfort 13.70 13.56 23 10964 477305 90140155
Pleural effusion 13.70 13.56 37 10950 111954 90505506
Induced labour 13.68 13.56 5 10982 1003 90616457

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
Differentiation syndrome 695.21 17.15 136 7034 1677 42612488
Electrocardiogram QT prolonged 303.84 17.15 152 7018 47793 42566372
Idiopathic intracranial hypertension 125.94 17.15 29 7141 801 42613364
Hyperleukocytosis 105.78 17.15 32 7138 2576 42611589
Febrile neutropenia 74.65 17.15 121 7049 185582 42428583
Hepatic function abnormal 55.41 17.15 55 7115 51512 42562653
Myelosuppression 50.74 17.15 47 7123 40414 42573751
Disseminated intravascular coagulation 39.49 17.15 33 7137 24761 42589404
Acute myeloid leukaemia 38.32 17.15 31 7139 22225 42591940
Hypokalaemia 37.62 17.15 53 7117 71668 42542497
Alanine aminotransferase increased 34.58 17.15 57 7113 88349 42525816
Haematopoietic neoplasm 32.65 17.15 6 7164 51 42614114
Platelet count decreased 30.43 17.15 70 7100 138511 42475654
Bone marrow necrosis 27.56 17.15 7 7163 294 42613871
White blood cell count increased 23.15 17.15 33 7137 45054 42569111
Pericardial effusion 20.57 17.15 25 7145 29250 42584915
Periarthritis 20.56 17.15 8 7162 1372 42612793
Septic embolus 20.42 17.15 8 7162 1397 42612768
Aspartate aminotransferase increased 20.36 17.15 42 7128 77121 42537044
Extremity necrosis 19.64 17.15 9 7161 2310 42611855
Blood lactate dehydrogenase increased 19.52 17.15 23 7147 26058 42588107
Pneumonia 19.25 17.15 129 7041 422020 42192145
Testicular haemorrhage 18.80 17.15 5 7165 252 42613913
Leukaemia recurrent 18.18 17.15 8 7162 1868 42612297
Pericarditis 17.58 17.15 16 7154 13428 42600737
Jugular vein thrombosis 17.41 17.15 8 7162 2066 42612099
Drug ineffective 17.18 17.15 52 7118 630145 41984020

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
Differentiation syndrome 1395.78 13.41 259 15703 2785 110570552
Electrocardiogram QT prolonged 398.81 13.41 228 15734 108732 110464605
Febrile neutropenia 169.16 13.41 218 15744 316549 110256788
Idiopathic intracranial hypertension 147.84 13.41 44 15918 3908 110569429
Hepatic function abnormal 147.71 13.41 114 15848 89181 110484156
Hyperleukocytosis 123.06 13.41 37 15925 3402 110569935
Myelodysplastic syndrome transformation 98.42 13.41 23 15939 794 110572543
Platelet count decreased 82.14 13.41 131 15831 230312 110343025
Myelosuppression 75.41 13.41 80 15882 94260 110479077
Acute myeloid leukaemia 74.92 13.41 54 15908 38056 110535281
Disseminated intravascular coagulation 73.27 13.41 55 15907 41231 110532106
White blood cell count decreased 69.17 13.41 121 15841 229269 110344068
Alanine aminotransferase increased 68.97 13.41 107 15855 183666 110389671
Haematopoietic neoplasm 62.46 13.41 11 15951 85 110573252
Aspartate aminotransferase increased 55.68 13.41 90 15872 159846 110413491
Bone marrow necrosis 51.21 13.41 12 15950 419 110572918
Leukaemia recurrent 45.13 13.41 17 15945 3114 110570223
Pericardial effusion 44.79 13.41 48 15914 57169 110516168
Leukocytosis 41.85 13.41 45 15917 53783 110519554
Blood lactate dehydrogenase increased 39.74 13.41 40 15922 44294 110529043
Neutrophil count decreased 37.98 13.41 65 15897 120876 110452461
Intracranial pressure increased 35.67 13.41 21 15941 10514 110562823
Pneumonia 35.52 13.41 232 15730 876482 109696855
Hypokalaemia 30.96 13.41 76 15886 182372 110390965
White blood cell count increased 30.34 13.41 52 15910 96790 110476547
Pyrexia 26.24 13.41 220 15742 898045 109675292
Pleural effusion 25.99 13.41 70 15892 177639 110395698
Lower respiratory tract infection fungal 25.48 13.41 8 15954 849 110572488
Central nervous system leukaemia 23.94 13.41 7 15955 584 110572753
Treatment failure 20.85 13.41 7 15955 277227 110296110
Sepsis 20.83 13.41 98 15864 327248 110246089
Blood alkaline phosphatase increased 20.80 13.41 37 15925 70898 110502439
Gamma-glutamyltransferase increased 20.63 13.41 34 15928 61275 110512062
Lower respiratory tract infection 20.38 13.41 5 15957 243101 110330236
Testicular haemorrhage 19.63 13.41 5 15957 248 110573089
Ulnar neuritis 19.63 13.41 3 15959 8 110573329
Drug intolerance 19.46 13.41 18 15944 406494 110166843
Therapeutic reaction time decreased 19.13 13.41 11 15951 5268 110568069
Long QT syndrome 18.53 13.41 12 15950 7106 110566231
Pancytopenia 18.19 13.41 69 15893 209544 110363793
Systemic lupus erythematosus 18.14 13.41 7 15955 254331 110319006
Septic embolus 17.71 13.41 8 15954 2318 110571019
Wound 17.48 13.41 6 15956 234431 110338906
Contraindicated product administered 17.43 13.41 7 15955 248260 110325077
Staphylococcal infection 17.40 13.41 34 15928 69910 110503427
Blood cholesterol increased 17.13 13.41 3 15959 184782 110388555
Bone marrow failure 16.73 13.41 30 15932 57818 110515519
Extremity necrosis 16.73 13.41 9 15953 3793 110569544
Drug abuse 16.19 13.41 3 15959 177408 110395929
Chromosomal deletion 16.15 13.41 4 15958 177 110573160
Protein total decreased 16.04 13.41 13 15949 10877 110562460
Ventricular extrasystoles 15.99 13.41 18 15944 22623 110550714
Acute promyelocytic leukaemia 15.97 13.41 7 15955 1889 110571448
Respiratory failure 14.82 13.41 66 15896 215266 110358071
Arthropathy 14.64 13.41 12 15950 287510 110285827
Hypomagnesaemia 14.60 13.41 29 15933 60341 110512996
Hyperaesthesia 14.52 13.41 14 15948 14713 110558624
Hypoxia 14.14 13.41 46 15916 129469 110443868
Infusion related reaction 13.83 13.41 21 15941 381141 110192196
Neutropenia 13.82 13.41 97 15865 374523 110198814
Laryngeal inflammation 13.69 13.41 4 15958 333 110573004
Blast cell count increased 13.64 13.41 6 15956 1631 110571706
Oedematous pancreatitis 13.59 13.41 6 15956 1648 110571689

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XX27 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
MeSH PA D000970 Antineoplastic Agents
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:233423 antifibrotic agent

Related Drugs by ATC class:

L01XX Other antineoplastic agents 33 drugs

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

DiseaseRelationSNOMED_IDDOID
Acute promyelocytic leukemia, FAB M3 indication 110004001
Acute myelomonocytic leukemia, FAB M4 indication 110005000
Myelodysplastic syndrome off-label use 109995007
Hyperkalemia contraindication 14140009
Complete atrioventricular block contraindication 27885002
Torsades de pointes contraindication 31722008
Hypokalemia contraindication 43339004
Chronic heart failure contraindication 48447003
Kidney disease contraindication 90708001 DOID:557
Prolonged QT interval contraindication 111975006
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001
Congenital long QT syndrome contraindication 442917000




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Thioredoxin reductase 1, cytoplasmic Enzyme INHIBITOR CHEMBL CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.82 WOMBAT-PK
Somatostatin receptor type 2 GPCR Kd 4.60 CHEMBL

External reference:

IDSource
D02106 KEGG_DRUG
18330 RXNORM
C0052416 UMLSCUI
CHEBI:30621 CHEBI
CHEMBL5483015 ChEMBL_ID
DB01169 DRUGBANK_ID
D000077237 MESH_DESCRIPTOR_UI
14888 PUBCHEM_CID
S7V92P67HO UNII
15787 MMSL
40534 MMSL
71831 MMSL
d04720 MMSL
4021238 VANDF
007172 NDDF
400907001 SNOMEDCT_US
72251000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 0781-3498 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 28 sections
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 14789-600 INJECTION 1 mg INTRAVENOUS ANDA 31 sections
Arsenic Trioxide Human Prescription Drug Label 1 23155-869 INJECTION 1 mg INTRAVENOUS ANDA 31 sections
Arsenic Trioxide Human Prescription Drug Label 1 23155-869 INJECTION 1 mg INTRAVENOUS ANDA 31 sections
Arsenic Trioxide Human Prescription Drug Label 1 23155-870 INJECTION 2 mg INTRAVENOUS ANDA 31 sections
Arsenic Trioxide Human Prescription Drug Label 1 23155-870 INJECTION 2 mg INTRAVENOUS ANDA 31 sections
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 25021-226 INJECTION 1 mg INTRAVENOUS ANDA 31 sections
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 25021-227 INJECTION 2 mg INTRAVENOUS ANDA 31 sections
Sinus HP HUMAN OTC DRUG LABEL 11 44911-0629 LIQUID 30 [hp_X] ORAL unapproved drug other 9 sections
Jointox BB HUMAN OTC DRUG LABEL 17 44911-0642 LIQUID 30 [hp_C] ORAL unapproved drug other 9 sections
Arsenic trioxide HUMAN PRESCRIPTION DRUG LABEL 1 49315-005 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 1 sections
Arsenic trioxide HUMAN PRESCRIPTION DRUG LABEL 1 49315-007 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 1 sections
ARSENIC TRIOXIDE HUMAN PRESCRIPTION DRUG LABEL 1 50742-438 INJECTION 1 mg INTRAVENOUS ANDA 24 sections
7 Heavy Metal Detox HUMAN OTC DRUG LABEL 61 55146-007 LIQUID 12 [hp_X] ORAL unapproved homeopathic 9 sections
1 Detoxification HUMAN OTC DRUG LABEL 81 55146-011 LIQUID 12 [hp_X] ORAL unapproved homeopathic 9 sections
ARSENIC TRIOXIDE Human Prescription Drug Label 1 55150-366 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 28 sections
Hay Fever HUMAN OTC DRUG LABEL 55 55714-2562 LIQUID 15 [hp_X] ORAL unapproved homeopathic 10 sections
BronCare HUMAN OTC DRUG LABEL 29 55714-4840 PELLET 15 [hp_X] ORAL unapproved homeopathic 10 sections
Homeopathic Moon drops HUMAN OTC DRUG LABEL 9 57556-008 LOZENGE 30 [hp_X] ORAL unapproved drug other 6 sections
Homeopathic Moon drops HUMAN OTC DRUG LABEL 9 57556-008 LOZENGE 30 [hp_X] ORAL unapproved drug other 6 sections
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 63323-637 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 29 sections
Trisenox HUMAN PRESCRIPTION DRUG LABEL 1 63459-601 INJECTION, SOLUTION 2 mg INTRAVENOUS NDA 23 sections
Emvita 6 HUMAN OTC DRUG LABEL 5 66343-018 LIQUID 18 [hp_M] ORAL UNAPPROVED HOMEOPATHIC 10 sections
Arsenic Trioxide Human Prescription Drug Label 1 68083-462 INJECTION 2 mg INTRAVENOUS ANDA 28 sections
Arsenic Trioxide Human Prescription Drug Label 1 68083-535 INJECTION 1 mg INTRAVENOUS ANDA 28 sections
Arsenic trioxide HUMAN PRESCRIPTION DRUG LABEL 1 68382-997 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 26 sections
ARSENIC TRIOXIDE HUMAN PRESCRIPTION DRUG LABEL 1 69918-720 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 26 sections
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 70121-1483 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 27 sections
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 70121-1658 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 27 sections
Arsenic trioxide HUMAN PRESCRIPTION DRUG LABEL 1 70710-1610 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 26 sections