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

Stem definitionDrug idCAS RN
258 95233-18-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • 566C80
  • atovaquone
  • mepron
A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.
  • Molecular weight: 366.84
  • Formula: C22H19ClO3
  • CLOGP: 6.03
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 1
  • TPSA: 54.37
  • ALOGS: -5.66
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2.25 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 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) 58.41 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 23 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.15 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 63 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,NTRK2,PDK1,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,STK33,SYK,TEK,TTK,ULK1 49
kinase-selectivity-class ACVR2B,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,MAP2K6,MAPK12,MAPK7,STK33,TEK,TTK 14
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1

Approvals:

DateAgencyCompanyOrphan
Nov. 25, 1992 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
Pancytopenia 84.16 17.60 80 8945 120183 90499239
Malaria 83.45 17.60 15 9010 198 90619224
Febrile neutropenia 74.23 17.60 85 8940 158264 90461158
Agranulocytosis 73.69 17.60 45 8980 34957 90584465
Rash maculo-papular 69.65 17.60 46 8979 40887 90578535
Cytokine release syndrome 61.55 17.60 37 8988 27936 90591486
Cerebellar stroke 61.54 17.60 13 9012 411 90619011
Encephalopathy 57.59 17.60 43 8982 46401 90573021
Babesiosis 54.59 17.60 11 9014 274 90619148
Thrombocytopenia 54.32 17.60 84 8941 208641 90410781
Schizophrenia 52.83 17.60 27 8998 14887 90604535
Pyrexia 51.23 17.60 163 8862 660322 89959100
Neutropenia 50.98 17.60 85 8940 224819 90394603
Aspergillus infection 48.50 17.60 23 9002 10800 90608622
Pulmonary nocardiosis 48.30 17.60 12 9013 786 90618636
Hypomania 46.39 17.60 21 9004 8876 90610546
Thrombotic microangiopathy 45.83 17.60 25 9000 15718 90603704
Hepatocellular injury 45.55 17.60 31 8994 28927 90590495
Jaundice cholestatic 43.96 17.60 21 9004 10022 90609400
Hepatic cytolysis 43.72 17.60 31 8994 30885 90588537
Stevens-Johnson syndrome 42.80 17.60 30 8995 29346 90590076
Cholelithiasis 42.66 17.60 38 8987 52468 90566954
Toxic epidermal necrolysis 42.30 17.60 31 8994 32497 90586925
Systemic candida 36.71 17.60 15 9010 4944 90614478
Cytomegalovirus infection 36.06 17.60 26 8999 26576 90592846
Nocardiosis 34.44 17.60 12 9013 2558 90616864
Partial seizures 34.29 17.60 16 9009 7244 90612178
Multiple organ dysfunction syndrome 34.22 17.60 38 8987 68298 90551124
Plasma cell myeloma 34.06 17.60 30 8995 40798 90578624
Cutaneous nocardiosis 33.39 17.60 6 9019 79 90619343
Hepatotoxicity 32.99 17.60 31 8994 45811 90573611
Cell death 32.41 17.60 12 9013 3043 90616379
Platelet count decreased 31.31 17.60 52 8973 136917 90482505
Cytomegalovirus viraemia 30.59 17.60 15 9010 7571 90611851
Haemophagocytic lymphohistiocytosis 30.30 17.60 19 9006 15440 90603982
Pain 30.14 17.60 33 8992 996308 89623114
Sepsis 29.35 17.60 59 8966 179755 90439667
Burkholderia cepacia complex infection 27.70 17.60 6 9019 214 90619208
Bronchopulmonary aspergillosis 27.48 17.60 16 9009 11382 90608040
Asthma-chronic obstructive pulmonary disease overlap syndrome 26.93 17.60 12 9013 4887 90614535
Total lung capacity increased 26.64 17.60 12 9013 5009 90614413
Ischaemic stroke 26.30 17.60 20 9005 22146 90597276
Psychotic disorder 26.15 17.60 23 9002 31207 90588215
Rash morbilliform 25.83 17.60 11 9014 4018 90615404
Toxic skin eruption 25.07 17.60 17 9008 15757 90603665
Diarrhoea 24.84 17.60 169 8856 939021 89680401
Febrile bone marrow aplasia 24.36 17.60 14 9011 9724 90609698
Dermatitis acneiform 23.95 17.60 12 9013 6342 90613080
Drug reaction with eosinophilia and systemic symptoms 23.53 17.60 25 9000 42733 90576689
Off label use 23.27 17.60 188 8837 1102064 89517358
Drug resistance 22.69 17.60 21 9004 30428 90588994
Methaemoglobinaemia 22.60 17.60 10 9015 4005 90615417
Anaemia 21.91 17.60 81 8944 352721 90266701
Eosinophilia 21.89 17.60 20 9005 28513 90590909
Blood bilirubin increased 21.46 17.60 24 9001 43446 90575976
Cytopenia 21.27 17.60 16 9009 17433 90601989
Arthralgia 21.15 17.60 28 8997 778494 89840928
Lobular breast carcinoma in situ 20.88 17.60 4 9021 76 90619346
Vulval disorder 20.84 17.60 7 9018 1337 90618085
Colitis 20.80 17.60 30 8995 69912 90549510
Phyllodes tumour 20.50 17.60 4 9021 84 90619338
Myeloid maturation arrest 20.49 17.60 3 9022 9 90619413
Pneumocystis jirovecii pneumonia 20.30 17.60 17 9008 21599 90597823
Acute kidney injury 20.26 17.60 74 8951 320313 90299109
Vocal cord operation 20.03 17.60 4 9021 95 90619327
Joint swelling 19.65 17.60 13 9012 503287 90116135
Sinusitis 19.60 17.60 5 9020 343083 90276339
Evans syndrome 19.41 17.60 5 9020 379 90619043
Pharyngeal cyst 19.37 17.60 4 9021 113 90619309
Joint vibration 19.27 17.60 3 9022 15 90619407
Abdominal discomfort 19.09 17.60 12 9013 477316 90142106
Alopecia 19.05 17.60 13 9012 495058 90124364
Monoclonal immunoglobulin increased 18.95 17.60 5 9020 416 90619006
Pulmonary alveolar haemorrhage 18.78 17.60 10 9015 5988 90613434
Graft versus host disease 18.50 17.60 11 9014 8133 90611289
Sarcoidosis 18.16 17.60 12 9013 10661 90608761
Nasal polyps 17.95 17.60 12 9013 10868 90608554
Discomfort 17.73 17.60 3 9022 274332 90345090

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
Nocardiosis 183.19 16.69 65 11958 5125 42604187
IVth nerve paralysis 110.55 16.69 27 11996 564 42608748
Immune reconstitution inflammatory syndrome 107.61 16.69 54 11969 10089 42599223
Malacoplakia 93.96 16.69 26 11997 898 42608414
Cytokine release syndrome 90.31 16.69 85 11938 44442 42564870
Thrombocytopenia 88.51 16.69 177 11846 190102 42419210
Pneumocystis jirovecii pneumonia 88.37 16.69 66 11957 25115 42584197
IgA nephropathy 84.77 16.69 30 11993 2344 42606968
Immune effector cell-associated neurotoxicity syndrome 82.05 16.69 44 11979 9417 42599895
Thrombotic microangiopathy 80.96 16.69 51 11972 14731 42594581
Neutropenia 73.68 16.69 169 11854 199262 42410050
Hepatic cytolysis 71.88 16.69 60 11963 26784 42582528
Pancytopenia 70.27 16.69 122 11901 117621 42491691
Malaria 62.06 16.69 14 12009 204 42609108
Pulmonary nocardiosis 61.30 16.69 22 12001 1790 42607522
Cutaneous mucormycosis 60.33 16.69 17 12006 628 42608684
Pyrexia 59.74 16.69 244 11779 393798 42215514
Graft versus host disease 59.51 16.69 40 11983 12885 42596427
Cholestasis 55.87 16.69 57 11966 32822 42576490
Respiratory failure 51.05 16.69 112 11911 128020 42481292
Phalangeal hypoplasia 50.97 16.69 10 12013 70 42609242
Enterococcal infection 47.76 16.69 34 11989 12005 42597307
Encephalopathy 45.20 16.69 57 11966 41276 42568036
Drug reaction with eosinophilia and systemic symptoms 44.39 16.69 57 11966 42018 42567294
Septic shock 40.96 16.69 84 11939 91588 42517724
Klebsiella infection 40.40 16.69 30 11993 11302 42598010
Mucormycosis 39.99 16.69 25 11998 7118 42602194
Mixed liver injury 39.33 16.69 21 12002 4453 42604859
Drug resistance 38.67 16.69 48 11975 34200 42575112
Febrile neutropenia 37.20 16.69 126 11897 185577 42423735
Scrotal ulcer 37.05 16.69 11 12012 490 42608822
COVID-19 37.04 16.69 93 11930 115855 42493457
Gastrointestinal injury 35.54 16.69 13 12010 1116 42608196
Babesiosis 35.38 16.69 9 12014 223 42609089
Toxoplasmosis 34.48 16.69 14 12009 1593 42607719
Congenital foot malformation 34.04 16.69 10 12013 429 42608883
Parasite blood test positive 33.52 16.69 5 12018 3 42609309
Penile ulceration 31.96 16.69 11 12012 791 42608521
Mycobacterial infection 30.65 16.69 15 12008 2653 42606659
Agranulocytosis 30.00 16.69 40 11983 30572 42578740
Hepatocellular injury 29.68 16.69 35 11988 23643 42585669
Proteus infection 29.45 16.69 12 12011 1378 42607934
Persecutory delusion 29.29 16.69 16 12007 3548 42605764
Cytopenia 29.10 16.69 30 11993 17467 42591845
Staphylococcal skin infection 29.05 16.69 11 12012 1040 42608272
Acute kidney injury 27.91 16.69 188 11835 367149 42242163
Cellulitis staphylococcal 27.20 16.69 10 12013 871 42608441
Campylobacter test positive 26.89 16.69 6 12017 83 42609229
Plasmodium falciparum infection 26.75 16.69 6 12017 85 42609227
Escherichia infection 25.49 16.69 23 12000 11373 42597939
Varicella 24.89 16.69 12 12011 2053 42607259
Enterococcal bacteraemia 24.80 16.69 13 12010 2654 42606658
Off label use 24.55 16.69 281 11742 638054 41971258
Anal ulcer 24.44 16.69 10 12013 1161 42608151
Vocal cord paralysis 24.25 16.69 10 12013 1184 42608128
Myopia 23.50 16.69 10 12013 1281 42608031
Bacteraemia 23.44 16.69 32 11991 25008 42584304
Gastrointestinal tract mucosal pigmentation 23.30 16.69 8 12015 571 42608741
Alpha haemolytic streptococcal infection 22.77 16.69 11 12012 1891 42607421
Drug level increased 22.31 16.69 32 11991 26168 42583144
Vasogenic cerebral oedema 22.14 16.69 9 12014 1027 42608285
Human herpesvirus 8 infection 22.07 16.69 10 12013 1487 42607825
Device related bacteraemia 22.05 16.69 8 12015 671 42608641
Pneumonia fungal 21.53 16.69 19 12004 9127 42600185
Drug ineffective for unapproved indication 21.43 16.69 43 11980 46120 42563192
Meningoencephalitis amoebic 21.10 16.69 6 12017 229 42609083
Cytomegalovirus chorioretinitis 20.57 16.69 14 12009 4597 42604715
Myocardial infarction 20.29 16.69 5 12018 124004 42485308
Staphylococcal bacteraemia 20.20 16.69 20 12003 11101 42598211
Acanthamoeba infection 20.17 16.69 7 12016 516 42608796
Sepsis 20.16 16.69 110 11913 199224 42410088
Cutaneous malacoplakia 19.11 16.69 5 12018 139 42609173
Morganella infection 19.01 16.69 7 12016 612 42608700
Cytomegalovirus test positive 19.00 16.69 13 12010 4306 42605006
Haemophilus bacteraemia 18.81 16.69 5 12018 148 42609164
Cutaneous extramedullary haemopoiesis 18.23 16.69 3 12020 6 42609306
Anaemia megaloblastic 18.17 16.69 6 12017 380 42608932
Chylothorax 17.81 16.69 8 12015 1166 42608146
Histoplasmosis 17.45 16.69 9 12014 1778 42607534
Infectious pleural effusion 17.43 16.69 11 12012 3184 42606128

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
Nocardiosis 238.41 16.19 77 19207 7409 110562606
Cytokine release syndrome 164.02 16.19 119 19165 70187 110499828
Thrombocytopenia 145.57 16.19 236 19048 348649 110221366
Pancytopenia 140.86 16.19 178 19106 209435 110360580
Thrombotic microangiopathy 134.78 16.19 76 19208 29073 110540942
Neutropenia 134.51 16.19 237 19047 374383 110195632
Hepatic cytolysis 123.44 16.19 91 19193 54962 110515053
IVth nerve paralysis 120.54 16.19 27 19257 632 110569383
Febrile neutropenia 117.03 16.19 203 19081 316564 110253451
Pulmonary nocardiosis 112.90 16.19 34 19250 2595 110567420
Pneumocystis jirovecii pneumonia 112.74 16.19 78 19206 42657 110527358
Immune reconstitution inflammatory syndrome 105.20 16.19 53 19231 16173 110553842
Encephalopathy 104.15 16.19 97 19187 80958 110489057
Immune effector cell-associated neurotoxicity syndrome 103.87 16.19 51 19233 14731 110555284
Malacoplakia 98.51 16.19 26 19258 1226 110568789
Malaria 97.57 16.19 21 19263 406 110569609
Pyrexia 95.63 16.19 358 18926 897907 109672108
IgA nephropathy 94.38 16.19 31 19253 3142 110566873
Agranulocytosis 93.34 16.19 81 19203 61679 110508336
Graft versus host disease 84.14 16.19 48 19236 18758 110551257
Drug reaction with eosinophilia and systemic symptoms 73.81 16.19 81 19203 82014 110488001
Babesiosis 72.90 16.19 17 19267 478 110569537
Rash maculo-papular 71.58 16.19 76 19208 74146 110495869
Cholestasis 71.15 16.19 71 19213 64447 110505568
Respiratory failure 70.47 16.19 131 19153 215201 110354814
Hepatocellular injury 69.70 16.19 63 19221 50579 110519436
Acute kidney injury 66.39 16.19 252 19032 635178 109934837
Cutaneous mucormycosis 66.34 16.19 17 19267 713 110569302
Septic shock 64.77 16.19 106 19178 157422 110412593
Cytopenia 63.51 16.19 48 19236 30068 110539947
Drug resistance 62.09 16.19 62 19222 56312 110513703
Toxic epidermal necrolysis 56.32 16.19 59 19225 56668 110513347
Enterococcal infection 55.65 16.19 38 19246 20328 110549687
Mixed liver injury 54.49 16.19 31 19253 12048 110557967
Aspergillus infection 54.39 16.19 41 19243 25575 110544440
Pain 54.34 16.19 52 19232 954903 109615112
Sepsis 53.21 16.19 151 19133 327195 110242820
COVID-19 49.94 16.19 123 19161 244937 110325078
Off label use 47.06 16.19 432 18852 1499753 109070262
Cerebellar stroke 44.70 16.19 13 19271 879 110569136
Cytomegalovirus infection 44.28 16.19 51 19233 54393 110515622
Scrotal ulcer 43.45 16.19 11 19273 439 110569576
Haemophagocytic lymphohistiocytosis 42.90 16.19 39 19245 31520 110538495
Klebsiella infection 42.43 16.19 32 19252 19977 110550038
Mucormycosis 41.92 16.19 25 19259 10603 110559412
Rheumatoid arthritis 40.74 16.19 3 19281 299610 110270405
Arthralgia 39.24 16.19 47 19237 779585 109790430
Arthropathy 38.75 16.19 3 19281 287519 110282496
Penile ulceration 38.61 16.19 11 19273 691 110569324
Pneumonia fungal 36.73 16.19 26 19258 14728 110555287
Persecutory delusion 36.29 16.19 19 19265 6272 110563743
Joint swelling 36.13 16.19 16 19268 442829 110127186
Systemic candida 35.58 16.19 22 19262 9952 110560063
Parasite blood test positive 35.34 16.19 5 19279 4 110570011
Platelet count decreased 35.19 16.19 104 19180 230339 110339676
Hypomania 35.10 16.19 22 19262 10188 110559827
Gastrointestinal injury 35.02 16.19 13 19271 1890 110568125
Febrile bone marrow aplasia 34.98 16.19 27 19257 17438 110552577
Toxoplasmosis 34.76 16.19 15 19269 3224 110566791
Cytomegalovirus viraemia 34.57 16.19 27 19257 17737 110552278
Escherichia infection 33.49 16.19 30 19254 23786 110546229
Alopecia 33.37 16.19 11 19273 364742 110205273
Bacteraemia 33.28 16.19 39 19245 42351 110527664
Bronchopulmonary aspergillosis 33.16 16.19 33 19251 29830 110540185
Nasopharyngitis 32.56 16.19 14 19270 394347 110175668
Musculoskeletal stiffness 32.45 16.19 5 19279 279817 110290198
Jaundice cholestatic 32.39 16.19 24 19260 14584 110555431
Cutaneous nocardiosis 31.83 16.19 8 19276 310 110569705
Stevens-Johnson syndrome 31.70 16.19 40 19244 46861 110523154
Schizophrenia 31.70 16.19 28 19256 21798 110548217
Staphylococcal bacteraemia 31.69 16.19 25 19259 16663 110553352
Staphylococcal infection 31.38 16.19 49 19235 69895 110500120
Drug level increased 31.15 16.19 40 19244 47679 110522336
Plasmodium falciparum infection 31.04 16.19 7 19277 169 110569846
Fall 30.74 16.19 36 19248 603446 109966569
Lichenoid keratosis 30.67 16.19 17 19267 6285 110563730
Colitis 30.65 16.19 60 19224 102263 110467752
Drug ineffective for unapproved indication 30.44 16.19 60 19224 102778 110467237
Wound 30.08 16.19 3 19281 234434 110335581
Proteus infection 30.03 16.19 13 19271 2815 110567200
Toxic skin eruption 29.81 16.19 30 19254 27485 110542530
Hepatotoxicity 29.25 16.19 45 19239 63355 110506660
Cell death 29.22 16.19 16 19268 5775 110564240
Burkholderia cepacia complex infection 28.42 16.19 8 19276 481 110569534
Plasma cell myeloma 28.10 16.19 44 19240 62892 110507123
Staphylococcal skin infection 27.95 16.19 11 19273 1874 110568141
Hepatic function abnormal 27.53 16.19 53 19231 89242 110480773
Cellulitis staphylococcal 27.35 16.19 10 19274 1393 110568622
Hyperbilirubinaemia 27.10 16.19 30 19254 30641 110539374
Neutrophil count decreased 27.08 16.19 63 19221 120878 110449137
Campylobacter test positive 26.93 16.19 6 19278 137 110569878
Completed suicide 26.63 16.19 5 19279 242376 110327639
Acanthamoeba infection 26.50 16.19 8 19276 615 110569400
Cytomegalovirus test positive 26.32 16.19 16 19268 7020 110562995
Acute respiratory distress syndrome 26.31 16.19 39 19245 53159 110516856
Disseminated intravascular coagulation 26.00 16.19 34 19250 41252 110528763
COVID-19 pneumonia 25.61 16.19 32 19252 37111 110532904
Peripheral swelling 25.34 16.19 20 19264 404014 110166001
Pericarditis 25.21 16.19 4 19280 219110 110350905
Device related bacteraemia 24.85 16.19 9 19275 1221 110568794
Acute respiratory failure 24.85 16.19 46 19238 75214 110494801
Gamma-glutamyltransferase increased 24.83 16.19 41 19243 61268 110508747
Human herpesvirus 8 infection 24.56 16.19 10 19274 1861 110568154
Blood bilirubin increased 24.54 16.19 46 19238 75926 110494089
Anal ulcer 24.53 16.19 10 19274 1866 110568149
Enterococcal bacteraemia 24.39 16.19 13 19271 4448 110565567
Acute generalised exanthematous pustulosis 24.16 16.19 24 19260 21640 110548375
Anaemia megaloblastic 24.07 16.19 8 19276 841 110569174
Alpha haemolytic streptococcal infection 24.06 16.19 12 19272 3581 110566434
Haemophilus bacteraemia 23.81 16.19 6 19278 235 110569780
Sinusitis 23.75 16.19 11 19273 296677 110273338
Meningoencephalitis amoebic 23.74 16.19 6 19278 238 110569777
Contraindicated product administered 23.57 16.19 7 19277 248260 110321755
Varicella 23.56 16.19 12 19272 3743 110566272
Infectious pleural effusion 23.27 16.19 13 19271 4878 110565137
Drug eruption 23.25 16.19 37 19247 53622 110516393
Vocal cord paralysis 23.01 16.19 11 19273 2995 110567020
Phalangeal hypoplasia 22.84 16.19 4 19280 24 110569991
Lower respiratory tract infection 22.82 16.19 7 19277 243099 110326916
Total lung capacity increased 22.73 16.19 13 19271 5099 110564916
Myopia 22.69 16.19 10 19274 2261 110567754
Pancreatitis acute 22.67 16.19 39 19245 60235 110509780
Asthma-chronic obstructive pulmonary disease overlap syndrome 22.64 16.19 14 19270 6330 110563685
Cholelithiasis 22.51 16.19 40 19244 63382 110506633
Weight increased 22.48 16.19 24 19260 419620 110150395
Multiple organ dysfunction syndrome 21.76 16.19 67 19217 151643 110418372
Anti-cyclic citrullinated peptide antibody positive 21.68 16.19 3 19281 181981 110388034
Congenital foot malformation 21.62 16.19 4 19280 34 110569981
Bone marrow failure 21.19 16.19 37 19247 57811 110512204
Eosinophilia 21.15 16.19 37 19247 57899 110512116
Immunosuppressant drug level increased 21.06 16.19 17 19267 11707 110558308
Gastrointestinal tract mucosal pigmentation 20.88 16.19 8 19276 1269 110568746
Pneumonia 20.86 16.19 239 19045 876475 109693540
Pathogen resistance 20.50 16.19 20 19264 17652 110552363
Cutaneous malacoplakia 20.47 16.19 5 19279 172 110569843
Hypoaesthesia 20.40 16.19 15 19269 314208 110255807
Therapeutic product effect incomplete 20.02 16.19 7 19277 223798 110346217
Alanine aminotransferase increased 20.02 16.19 74 19210 183699 110386316
Pain in extremity 19.88 16.19 34 19250 487084 110082931
Rash morbilliform 19.76 16.19 14 19270 7937 110562078
Vulval disorder 19.65 16.19 7 19277 906 110569109
Fatigue 19.62 16.19 128 19156 1215830 109354185
Vasogenic cerebral oedema 19.56 16.19 9 19275 2249 110567766
Lobular breast carcinoma in situ 19.48 16.19 4 19280 61 110569954
Partial seizures 19.42 16.19 16 19268 11333 110558682
Folliculitis 19.42 16.19 3 19281 167650 110402365
Jaundice 19.29 16.19 36 19248 59200 110510815
Asthma 18.94 16.19 10 19274 250281 110319734
Cytomegalovirus chorioretinitis 18.76 16.19 13 19271 7115 110562900
Oesophagitis 18.63 16.19 24 19260 28691 110541324
Diffuse large B-cell lymphoma 18.45 16.19 18 19266 15880 110554135
Transplant rejection 18.29 16.19 22 19262 24545 110545470
Disseminated cryptococcosis 18.16 16.19 9 19275 2648 110567367
Phyllodes tumour 17.92 16.19 4 19280 92 110569923
Chills 17.72 16.19 73 19211 190507 110379508
Musculoskeletal pain 17.67 16.19 5 19279 183018 110386997
Joint vibration 17.59 16.19 3 19281 15 110570000
Pneumocystis test positive 17.57 16.19 4 19280 101 110569914
Vocal cord operation 17.53 16.19 4 19280 102 110569913
Disease recurrence 17.43 16.19 35 19249 60749 110509266
Pharyngeal cyst 17.42 16.19 4 19280 105 110569910
Histoplasmosis 17.27 16.19 9 19275 2944 110567071
Ischaemic stroke 17.25 16.19 28 19256 41235 110528780
Disseminated mucormycosis 17.03 16.19 8 19276 2094 110567921
Morganella infection 16.84 16.19 7 19277 1372 110568643
Injury 16.82 16.19 5 19279 177260 110392755
Parainfluenzae virus infection 16.69 16.19 12 19272 6962 110563053
Mouth ulceration 16.62 16.19 30 19254 48108 110521907
Pulmonary alveolar haemorrhage 16.59 16.19 19 19265 20131 110549884
Sleep disorder 16.47 16.19 7 19277 198637 110371378
Lymphopenia 16.45 16.19 27 19257 40143 110529872
Pneumocystis jirovecii infection 16.45 16.19 10 19274 4390 110565625
Mycobacterial infection 16.41 16.19 10 19274 4407 110565608

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC P01AX06 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTIPROTOZOALS
AGENTS AGAINST AMOEBIASIS AND OTHER PROTOZOAL DISEASES
Other agents against amoebiasis and other protozoal diseases
ATC P01BB51 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTIPROTOZOALS
ANTIMALARIALS
Biguanides
FDA EPC N0000175482 Antimalarial
FDA EPC N0000175485 Antiprotozoal
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000962 Antimalarials
MeSH PA D000977 Antiparasitic Agents
MeSH PA D000981 Antiprotozoal Agents
MeSH PA D004791 Enzyme Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35442 antiparasitic agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35718 antifungal agent
CHEBI has role CHEBI:38068 antimalarial
CHEBI has role CHEBI:38503 EC 1.6.5.3 [NADH:ubiquinone reductase (H<small><sup>+</small></sup>-translocating)] inhibitor
CHEBI has role CHEBI:77103 EC 1.3.5.2 [dihydroorotate dehydrogenase (quinone)] inhibitor
CHEBI has role CHEBI:77106 EC 1.10.2.2 (quinol—cytochrome-<em>c</em> reductase) inhibitor
CHEBI has role CHEBI:171664 antiamoebic agent

Related Drugs by ATC class:

P01AX Other agents against amoebiasis and other protozoal diseases 9 drugs
chiniofondihydroemetineemetinefumagillinmepacrinenitazoxanidephanquinonetenonitrozoletrimetrexate
P01BB Biguanides 3 drugs
chloroquinecycloguanilproguanil

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

DiseaseRelationSNOMED_IDDOID
Falciparum malaria indication 62676009 DOID:14067
Pneumocystosis jiroveci pneumonia indication 415125002 DOID:11339
Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention indication
Plasmodium Falciparum Malaria Prevention indication
Pneumocystis Carinii Pneumonia Prevention indication
Babesiosis off-label use 21061004 DOID:9643
Vivax malaria off-label use 27052006 DOID:12978
Toxoplasmosis off-label use 187192000 DOID:9965
Toxoplasmosis associated with acquired immunodeficiency syndrome off-label use 421666009
Toxoplasmosis Prevention off-label use
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Hyperglycemia contraindication 80394007 DOID:4195
Anemia due to enzyme deficiency contraindication 111577008
Disease of liver contraindication 235856003 DOID:409
Chronic diarrhea contraindication 236071009
Vomiting contraindication 422400008
Malabsorption States contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.18 acidic

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
ATP-binding cassette sub-family G member 2 Transporter IC50 6.64 CHEMBL
Dihydroorotate dehydrogenase (quinone), mitochondrial Enzyme IC50 5.03 WOMBAT-PK
Cytochrome b Enzyme INHIBITOR CHEMBL CHEMBL
Ubiquinol-cytochrome-c reductase complex core protein I, mitochondrial Enzyme WOMBAT-PK
Dihydroorotate dehydrogenase (quinone), mitochondrial Enzyme IC50 6.15 CHEMBL
Dihydroorotate dehydrogenase Enzyme Ki 4.57 CHEMBL
Dihydroorotate dehydrogenase Enzyme IC50 6.37 CHEMBL

External reference:

IDSource
4020594 VUID
N0000148284 NUI
D00236 KEGG_DRUG
114972 RXNORM
C0165603 UMLSCUI
CHEBI:575568 CHEBI
AOQ PDB_CHEM_ID
CHEMBL1450 ChEMBL_ID
DB01117 DRUGBANK_ID
D053626 MESH_DESCRIPTOR_UI
74989 PUBCHEM_CID
9695 IUPHAR_LIGAND_ID
6914 INN_ID
Y883P1Z2LT UNII
1907 MMSL
213467 MMSL
4227 MMSL
d01120 MMSL
4020594 VANDF
004112 NDDF
108718008 SNOMEDCT_US
386899002 SNOMEDCT_US
Y883P1Z2LT INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 0121-0956 SUSPENSION 750 mg ORAL ANDA 18 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 0121-1016 SUSPENSION 750 mg ORAL ANDA 17 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 0121-1016 SUSPENSION 750 mg ORAL ANDA 17 sections
MEPRON HUMAN PRESCRIPTION DRUG LABEL 1 0173-0547 SUSPENSION 750 mg ORAL NDA 26 sections
MEPRON HUMAN PRESCRIPTION DRUG LABEL 1 0173-0665 SUSPENSION 750 mg ORAL NDA 26 sections
MALARONE HUMAN PRESCRIPTION DRUG LABEL 2 0173-0675 TABLET, FILM COATED 250 mg ORAL NDA 25 sections
MALARONE HUMAN PRESCRIPTION DRUG LABEL 2 0173-0676 TABLET, FILM COATED 62.50 mg ORAL NDA 25 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0378-4160 TABLET, FILM COATED 62.50 mg ORAL ANDA 27 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0378-4162 TABLET, FILM COATED 250 mg ORAL ANDA 27 sections
ATOVAQUONE HUMAN PRESCRIPTION DRUG LABEL 1 0904-7459 SUSPENSION 750 mg ORAL ANDA 25 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 10544-909 TABLET, FILM COATED 250 mg ORAL ANDA 26 sections
Atovaquone Oral Suspension HUMAN PRESCRIPTION DRUG LABEL 1 10702-223 SUSPENSION 750 mg ORAL ANDA 23 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 17856-0631 SUSPENSION 750 mg ORAL ANDA 25 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 17856-8631 SUSPENSION 750 mg ORAL ANDA 25 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 31722-629 SUSPENSION 750 mg ORAL ANDA 26 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 33261-900 TABLET, FILM COATED 250 mg ORAL ANDA 22 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 42239-001 SUSPENSION 750 mg ORAL ANDA 17 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 42254-150 TABLET 250 mg ORAL ANDA 20 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 43063-393 TABLET, FILM COATED 250 mg ORAL ANDA 25 sections
Atovaquone and Proguanil HCl HUMAN PRESCRIPTION DRUG LABEL 2 50090-2980 TABLET, FILM COATED 250 mg ORAL NDA authorized generic 27 sections
ATOVAQUONE HUMAN PRESCRIPTION DRUG LABEL 1 50268-119 SUSPENSION 750 mg ORAL ANDA 22 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 51407-642 SUSPENSION 750 mg ORAL ANDA 26 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 51407-869 TABLET, FILM COATED 250 mg ORAL ANDA 27 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 54868-6393 TABLET, FILM COATED 250 mg ORAL ANDA 22 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 60687-534 SUSPENSION 750 mg ORAL ANDA 26 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 60687-534 SUSPENSION 750 mg ORAL ANDA 26 sections
Atovaquone HUMAN PRESCRIPTION DRUG LABEL 1 62135-528 SUSPENSION 750 mg ORAL ANDA 17 sections
Atovaquone and Proguanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 63187-879 TABLET, FILM COATED 250 mg ORAL ANDA 26 sections
Atovaquone and Proguanil HCl HUMAN PRESCRIPTION DRUG LABEL 2 63629-5531 TABLET, FILM COATED 250 mg ORAL NDA authorized generic 26 sections
ATOVAQUONE HUMAN PRESCRIPTION DRUG LABEL 1 65162-693 SUSPENSION 750 mg ORAL ANDA 23 sections