arsenic trioxide ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.76 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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 376.94 13.80 72 7630 861 50596561
Electrocardiogram QT prolonged 172.60 13.80 104 7598 51782 50545640
Febrile neutropenia 105.96 13.80 100 7602 97567 50499855
Hepatic function abnormal 89.62 13.80 58 7644 32623 50564799
Myelosuppression 47.20 13.80 28 7674 13489 50583933
Platelet count decreased 41.52 13.80 63 7639 100663 50496759
White blood cell count decreased 41.21 13.80 68 7634 116654 50480768
Neutrophil count decreased 35.03 13.80 39 7663 45987 50551435
Alanine aminotransferase increased 34.62 13.80 54 7648 88305 50509117
Disseminated intravascular coagulation 34.15 13.80 25 7677 17110 50580312
Leukaemia recurrent 33.79 13.80 11 7691 1243 50596179
Lower respiratory tract infection fungal 33.51 13.80 8 7694 287 50597135
Aspartate aminotransferase increased 31.02 13.80 48 7654 77950 50519472
Chromosomal deletion 28.82 13.80 5 7697 33 50597389
Haematopoietic neoplasm 28.20 13.80 5 7697 38 50597384
Leukocytosis 28.08 13.80 25 7677 22554 50574868
Idiopathic intracranial hypertension 23.68 13.80 10 7692 2339 50595083
Pericardial effusion 23.56 13.80 24 7678 25565 50571857
Acute myeloid leukaemia 23.48 13.80 19 7683 15055 50582367
Gamma-glutamyltransferase increased 22.36 13.80 25 7677 29598 50567824
Gambling 19.72 13.80 5 7697 231 50597191
Drug ineffective 19.64 13.80 62 7640 819271 49778151
Pyrexia 19.36 13.80 111 7591 380092 50217330
Blood lactate dehydrogenase increased 19.21 13.80 19 7683 19543 50577879
Sweat gland tumour 18.00 13.80 4 7698 104 50597318
Oedematous pancreatitis 17.19 13.80 5 7697 388 50597034
Blast cell count increased 17.15 13.80 5 7697 391 50597031
Laryngeal inflammation 17.05 13.80 4 7698 133 50597289
Ventricular extrasystoles 15.84 13.80 13 7689 10503 50586919
Intracranial pressure increased 15.34 13.80 9 7693 4243 50593179
Leukostasis syndrome 14.88 13.80 3 7699 48 50597374
Pneumonia 14.61 13.80 103 7599 378298 50219124
Humidity intolerance 13.93 13.80 4 7698 297 50597125

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 393.69 17.85 79 5264 1034 29568150
Electrocardiogram QT prolonged 242.98 17.85 122 5221 36015 29533169
Idiopathic intracranial hypertension 116.87 17.85 26 5317 569 29568615
Febrile neutropenia 103.95 17.85 114 5229 112126 29457058
Myelosuppression 78.20 17.85 40 5303 12187 29556997
Hyperleukocytosis 64.64 17.85 20 5323 1615 29567569
Hepatic function abnormal 58.88 17.85 52 5291 39207 29529977
Hypokalaemia 44.58 17.85 50 5293 50153 29519031
Platelet count decreased 38.16 17.85 68 5275 104604 29464580
Alanine aminotransferase increased 33.79 17.85 52 5291 70892 29498292
Acute myeloid leukaemia 33.33 17.85 26 5317 16487 29552697
Haematopoietic neoplasm 32.33 17.85 6 5337 50 29569134
Disseminated intravascular coagulation 30.99 17.85 27 5316 19953 29549231
Aspartate aminotransferase increased 27.34 17.85 43 5300 59682 29509502
Blood lactate dehydrogenase increased 24.01 17.85 23 5320 19186 29549998
White blood cell count increased 22.96 17.85 31 5312 37485 29531699
Hypomagnesaemia 21.99 17.85 21 5322 17447 29551737
Pneumonia 21.49 17.85 114 5229 320058 29249126
Pleural effusion 20.35 17.85 42 5301 71866 29497318
Blood alkaline phosphatase increased 19.75 17.85 25 5318 28381 29540803
Activated partial thromboplastin time prolonged 19.66 17.85 14 5329 7728 29561456
Leukaemia recurrent 19.48 17.85 8 5335 1469 29567715
Pancytopenia 19.47 17.85 45 5298 83123 29486061
White blood cell count decreased 19.40 17.85 45 5298 83317 29485867
Pericardial effusion 18.59 17.85 21 5322 21187 29547997

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 707.02 13.62 142 11245 1912 64485433
Electrocardiogram QT prolonged 312.71 13.62 187 11200 79261 64408084
Febrile neutropenia 201.23 13.62 204 11183 187453 64299892
Hepatic function abnormal 149.31 13.62 109 11278 64204 64423141
Myelosuppression 122.83 13.62 67 11320 23763 64463582
Idiopathic intracranial hypertension 121.65 13.62 36 11351 2557 64484788
Myelodysplastic syndrome transformation 98.73 13.62 23 11364 636 64486709
Platelet count decreased 86.49 13.62 126 11261 167585 64319760
Hyperleukocytosis 81.39 13.62 25 11362 2015 64485330
White blood cell count decreased 66.46 13.62 108 11279 157729 64329616
Haematopoietic neoplasm 60.48 13.62 11 11376 83 64487262
Alanine aminotransferase increased 58.33 13.62 95 11292 138936 64348409
Disseminated intravascular coagulation 57.85 13.62 47 11340 32301 64455044
Acute myeloid leukaemia 55.76 13.62 43 11344 27420 64459925
Aspartate aminotransferase increased 51.80 13.62 83 11304 119705 64367640
Neutrophil count decreased 45.66 13.62 62 11325 77134 64410211
Leukaemia recurrent 44.91 13.62 17 11370 2577 64484768
Leukocytosis 42.05 13.62 42 11345 37698 64449647
Pneumonia 41.03 13.62 201 11186 559375 63927970
Blood lactate dehydrogenase increased 40.94 13.62 39 11348 33039 64454306
Hypokalaemia 36.58 13.62 72 11315 121831 64365514
Pericardial effusion 33.64 13.62 38 11349 39216 64448129
White blood cell count increased 28.86 13.62 46 11341 65968 64421377
Pyrexia 28.44 13.62 182 11205 558462 63928883
Pleural effusion 26.83 13.62 65 11322 126494 64360851
Sepsis 24.72 13.62 93 11294 230248 64257097
Completed suicide 24.32 13.62 5 11382 224409 64262936
Gamma-glutamyltransferase increased 24.29 13.62 36 11351 48474 64438871
Lower respiratory tract infection fungal 23.92 13.62 8 11379 847 64486498
Chromosomal deletion 23.61 13.62 5 11382 88 64487257
Liver disorder 23.08 13.62 37 11350 53314 64434031
Pancytopenia 22.66 13.62 66 11321 143243 64344102
Blood alkaline phosphatase increased 21.62 13.62 37 11350 56242 64431103
Hypomagnesaemia 20.55 13.62 29 11358 37347 64449998
Drug ineffective 19.78 13.62 79 11308 840168 63647177
Neutropenia 19.59 13.62 89 11298 239535 64247810
Bone marrow failure 17.73 13.62 31 11356 47921 64439424
Protein total decreased 17.37 13.62 13 11374 7923 64479422
Ventricular extrasystoles 16.80 13.62 18 11369 17511 64469834
Central nervous system leukaemia 16.56 13.62 5 11382 380 64486965
Bronchopulmonary aspergillosis 15.54 13.62 18 11369 19067 64468278
Cytogenetic abnormality 15.03 13.62 6 11381 1048 64486297
Laryngeal inflammation 15.02 13.62 4 11383 193 64487152
Bone marrow necrosis 14.94 13.62 4 11383 197 64487148
Toxicity to various agents 14.75 13.62 26 11361 363487 64123858
Blast cell count increased 13.91 13.62 6 11381 1273 64486072

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:24852 insecticides
CHEBI has role CHEBI:35610 antineoplastic agents

Drug Use (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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1MG/ML **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** TRISENOX CEPHALON N021248 Sept. 25, 2000 DISCN INJECTABLE INJECTION Jan. 12, 2025 ARSENIC TRIOXIDE FOR USE IN COMBINATION WITH TRETINOIN FOR TREATMENT OF ADULTS WITH NEWLY-DIAGNOSED LOW-RISK ACUTE PROMYELOCYTIC LEUKEMIA (APL) WHOSE APL IS CHARACTERIZED BY THE PRESENCE OF THE T(15;17) TRANSLOCATION OR PML/RAR-ALPHA GENE EXPRESSION
2MG/ML TRISENOX CEPHALON N021248 Oct. 13, 2017 RX INJECTABLE INJECTION Jan. 12, 2025 ARSENIC TRIOXIDE FOR USE IN COMBINATION WITH TRETINOIN FOR TREATMENT OF ADULTS WITH NEWLY-DIAGNOSED LOW-RISK ACUTE PROMYELOCYTIC LEUKEMIA (APL) WHOSE APL IS CHARACTERIZED BY THE PRESENCE OF THE T(15;17) TRANSLOCATION OR PML/RAR-ALPHA GENE EXPRESSION

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

External reference:

IDSource
D02106 KEGG_DRUG
18330 RXNORM
C0052416 UMLSCUI
CHEBI:30621 CHEBI
CHEMBL2362016 ChEMBL_ID
CHEMBL1200978 ChEMBL_ID
DB01169 DRUGBANK_ID
D000077237 MESH_DESCRIPTOR_UI
14888 PUBCHEM_CID
S7V92P67HO UNII
15787 MMSL
40534 MMSL
71831 MMSL
d04720 MMSL
007172 NDDF
4021238 VANDF
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 29 sections
AllerstatI HUMAN OTC DRUG LABEL 9 44911-0178 LIQUID 12 [hp_X] ORAL unapproved homeopathic 9 sections
Vertitone HUMAN OTC DRUG LABEL 9 44911-0181 LIQUID 12 [hp_X] ORAL unapproved homeopathic 9 sections
Nightshade Antigens HUMAN OTC DRUG LABEL 10 44911-0350 LIQUID 12 [hp_X] ORAL unapproved homeopathic 9 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
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
Arsenic Trioxide HUMAN PRESCRIPTION DRUG LABEL 1 54879-027 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 27 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
Sleep Aid HUMAN OTC DRUG LABEL 14 57955-2640 LIQUID 59 [hp_X] ORAL unapproved homeopathic 9 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 28 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 68083-462 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