tocofersolan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4280 59-02-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tocophersolan
  • .ALPHA.-TOCOPHEROL, D-
  • alpha-tocopherol
  • alpha-D-Tocopherol
  • syntopherol
  • ALPHA-TOCOPHEROL, D-
  • .ALPHA.-TOCOPHEROL
  • d-alpha-tocopherol
  • alpha-tocopherol, dl-
  • .Alpha.-tocopherol, DL-
  • tocofersolan
  • vedrop
A natural tocopherol and one of the most potent antioxidant tocopherols. It exhibits antioxidant activity by virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus. It has four methyl groups on the 6-chromanol nucleus. The natural d form of alpha-tocopherol is more active than its synthetic dl-alpha-tocopherol racemic mixture.
  • Molecular weight: 430.72
  • Formula: C29H50O2
  • CLOGP: 12
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 1
  • TPSA: 29.46
  • ALOGS: -7.79
  • ROTB: 12

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None 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
Muscle spasticity 148.88 13.54 93 21977 17091 50565963
Therapy cessation 120.53 13.54 96 21974 25915 50557139
Macular degeneration 112.51 13.54 73 21997 14315 50568739
Ear pain 93.46 13.54 86 21984 28197 50554857
Night sweats 91.86 13.54 92 21978 33482 50549572
Body temperature increased 82.30 13.54 84 21986 31257 50551797
Respiratory disorder 75.45 13.54 80 21990 31107 50551947
Peripheral swelling 74.66 13.54 228 21842 205708 50377346
Electric shock 71.99 13.54 24 22046 1004 50582050
Back pain 66.55 13.54 229 21841 219801 50363253
Insomnia 58.17 13.54 188 21882 174677 50408377
Abdominal pain upper 56.39 13.54 175 21895 159134 50423920
Pneumonia aspiration 55.42 13.54 68 22002 30936 50552118
Toxicity to various agents 54.29 13.54 13 22057 212486 50370568
Diarrhoea 54.07 13.54 439 21631 588037 49995017
Gastrooesophageal reflux disease 51.25 13.54 107 21963 76321 50506733
Intervertebral discitis 49.92 13.54 24 22046 2632 50580422
Presbyacusis 48.91 13.54 24 22046 2752 50580302
Pleural thickening 47.38 13.54 23 22047 2576 50580478
Asthenia 45.23 13.54 265 21805 318777 50264277
Blood magnesium increased 45.14 13.54 23 22047 2857 50580197
Pleural fibrosis 44.42 13.54 24 22046 3360 50579694
Post-traumatic stress disorder 44.23 13.54 26 22044 4277 50578777
Systemic lupus erythematosus 43.87 13.54 5 22065 140617 50442437
Drug interaction 42.40 13.54 17 22053 199604 50383450
Temperature intolerance 41.86 13.54 31 22039 7508 50575546
Urticaria 40.99 13.54 137 21933 129424 50453630
Deafness neurosensory 40.59 13.54 25 22045 4476 50578578
Sinusitis 39.44 13.54 163 21907 170395 50412659
Epigastric discomfort 36.84 13.54 26 22044 5844 50577210
Fatigue 35.65 13.54 467 21603 707134 49875920
Incorrect route of product administration 35.08 13.54 42 22028 18624 50564430
Weight decreased 32.09 13.54 185 21885 221060 50361994
Demyelination 31.72 13.54 24 22046 6002 50577052
Maternal exposure during pregnancy 31.71 13.54 15 22055 159763 50423291
Headache 31.43 13.54 348 21722 506187 50076867
Bone cyst 31.25 13.54 16 22054 2008 50581046
Cyst 30.78 13.54 32 22038 12155 50570899
Glossodynia 29.63 13.54 7 22063 115562 50467492
Multiple sclerosis 28.91 13.54 40 22030 20453 50562601
Infective pulmonary exacerbation of cystic fibrosis 27.98 13.54 25 22045 7884 50575170
General physical health deterioration 27.31 13.54 14 22056 142420 50440634
Synovitis 27.20 13.54 10 22060 123855 50459199
Progressive multifocal leukoencephalopathy 27.01 13.54 29 22041 11428 50571626
Balance disorder 26.29 13.54 79 21991 70511 50512543
Pain in extremity 26.21 13.54 206 21864 272659 50310395
Low turnover osteopathy 25.79 13.54 18 22052 3976 50579078
Osteosclerosis 25.65 13.54 17 22053 3450 50579604
Dry eye 25.18 13.54 48 22022 32047 50551007
Exposure during pregnancy 24.57 13.54 11 22059 121004 50462050
Osteopenia 23.68 13.54 33 22037 16985 50566069
Product dose omission issue 23.62 13.54 149 21921 183689 50399365
Coordination abnormal 23.41 13.54 27 22043 11507 50571547
Pruritus 22.43 13.54 205 21865 283363 50299691
Neuropathy peripheral 21.96 13.54 92 21978 96665 50486389
Acute kidney injury 21.33 13.54 42 22028 228016 50355038
Wound 20.88 13.54 10 22060 105784 50477270
Hernia 20.49 13.54 23 22047 9520 50573534
Osteoarthritis 20.31 13.54 71 21999 68535 50514519
Glaucoma 19.74 13.54 29 22041 15657 50567397
Coma 19.63 13.54 62 22008 56817 50526237
Constipation 18.81 13.54 142 21928 185566 50397488
Spinal epidural haematoma 18.78 13.54 9 22061 980 50582074
Depressed mood 18.69 13.54 44 22026 33979 50549075
Cardiac arrest 17.95 13.54 7 22063 83644 50499410
Somnolence 17.70 13.54 122 21948 154863 50428191
Throat irritation 17.59 13.54 40 22030 30199 50552855
Skin lesion 17.41 13.54 37 22033 26690 50556364
Ageusia 16.92 13.54 23 22047 11560 50571494
Joint swelling 15.81 13.54 170 21900 245116 50337938
Underdose 15.50 13.54 30 22040 20248 50562806
Febrile neutropenia 15.41 13.54 12 22058 97655 50485399
Deformity 15.14 13.54 18 22052 7922 50575132
Body height decreased 15.05 13.54 19 22051 8889 50574165
Pancytopenia 15.03 13.54 9 22061 84021 50499033
Dry mouth 14.82 13.54 56 22014 56122 50526932
Adrenal insufficiency 14.66 13.54 24 22046 14219 50568835
White blood cell count decreased 14.60 13.54 94 21976 116628 50466426
Dysgeusia 13.96 13.54 43 22027 38873 50544181
Flatulence 13.95 13.54 36 22034 29422 50553632
Depression 13.77 13.54 121 21949 165302 50417752

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
Infective pulmonary exacerbation of cystic fibrosis 75.20 16.69 35 7432 6201 29560859
Fractional exhaled nitric oxide increased 61.05 16.69 15 7452 361 29566699
Therapy cessation 54.75 16.69 38 7429 14424 29552636
Secretion discharge 45.75 16.69 22 7445 4188 29562872
Plantar fasciitis 39.09 16.69 14 7453 1267 29565793
Sensation of foreign body 38 16.69 15 7452 1775 29565285
Nasopharyngitis 36.74 16.69 59 7408 59606 29507454
Myoglobin blood increased 36.43 16.69 15 7452 1980 29565080
Appendicolith 28.45 16.69 15 7452 3465 29563595
Brain natriuretic peptide increased 28.39 16.69 16 7451 4214 29562846
Product dose omission issue 27.38 16.69 69 7398 96314 29470746
Weight decreased 25.64 16.69 90 7377 150815 29416245
Chest discomfort 24.98 16.69 43 7424 45940 29521120
Muscle spasms 24.42 16.69 52 7415 65030 29502030
Constipation 23.79 16.69 73 7394 114087 29452973
Fatigue 22.13 16.69 146 7321 316675 29250385
Sleep apnoea syndrome 20.95 16.69 24 7443 17575 29549485
Cardiac disorder 20.43 16.69 35 7432 37228 29529832
Diarrhoea 17.86 16.69 144 7323 332554 29234506
Appendicitis 17.86 16.69 16 7451 8763 29558297
Carcinoid crisis 17.19 16.69 5 7462 232 29566828

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
Muscle spasticity 162.50 13.43 91 23150 16578 64458913
Therapy cessation 159.68 13.43 115 23126 32374 64443117
Ear pain 103.44 13.43 80 23161 25056 64450435
Night sweats 93.48 13.43 88 23153 35958 64439533
Peripheral swelling 90.43 13.43 219 23022 208934 64266557
Respiratory disorder 83.91 13.43 83 23158 36028 64439463
Body temperature increased 79.19 13.43 81 23160 36585 64438906
Infective pulmonary exacerbation of cystic fibrosis 77.55 13.43 50 23191 11746 64463745
Electric shock 74.28 13.43 24 23217 1105 64474386
Toxicity to various agents 69.99 13.43 22 23219 363491 64112000
Insomnia 68.84 13.43 191 23050 197645 64277846
Back pain 65.90 13.43 219 23022 249952 64225539
Completed suicide 64.97 13.43 4 23237 224410 64251081
Abdominal pain upper 61.88 13.43 170 23071 174860 64300631
Drug interaction 61.17 13.43 27 23214 362056 64113435
Diarrhoea 54.59 13.43 445 22796 722259 63753232
Fatigue 53.88 13.43 456 22785 748274 63727217
Presbyacusis 51.78 13.43 23 23218 2552 64472939
Post-traumatic stress disorder 49.43 13.43 26 23215 4179 64471312
Sinusitis 48.86 13.43 139 23102 145789 64329702
Urticaria 48.05 13.43 139 23102 147178 64328313
Pleural thickening 47.51 13.43 22 23219 2688 64472803
Blood magnesium increased 46.79 13.43 23 23218 3208 64472283
Intervertebral discitis 45.77 13.43 24 23217 3833 64471658
Temperature intolerance 44.65 13.43 31 23210 8224 64467267
Gastrooesophageal reflux disease 43.53 13.43 94 23147 83049 64392442
Headache 42.03 13.43 330 22911 529137 63946354
Pleural fibrosis 41.89 13.43 23 23218 4027 64471464
Pain 36.50 13.43 331 22910 553180 63922311
Acute kidney injury 35.97 13.43 67 23174 449173 64026318
Asthenia 35.71 13.43 270 22971 427774 64047717
Epigastric discomfort 35.49 13.43 25 23216 6786 64468705
Product dose omission issue 35.03 13.43 151 23090 194596 64280895
Deafness neurosensory 34.62 13.43 24 23217 6350 64469141
Dry eye 34.12 13.43 47 23194 28972 64446519
Joint swelling 33.51 13.43 160 23081 215222 64260269
Weight decreased 33.33 13.43 196 23045 285543 64189948
Demyelination 33.12 13.43 24 23217 6810 64468681
Bone cyst 32.90 13.43 16 23225 2181 64473310
Pain in extremity 32.87 13.43 204 23037 302881 64172610
Multiple sclerosis 32.39 13.43 37 23204 18904 64456587
Osteopenia 29.39 13.43 32 23209 15508 64459983
Cyst 28.59 13.43 28 23213 11999 64463492
Osteosclerosis 28.55 13.43 17 23224 3469 64472022
Incorrect route of product administration 27.79 13.43 38 23203 23260 64452231
Pruritus 27.11 13.43 199 23042 312201 64163290
Pneumonia aspiration 25.47 13.43 62 23179 59209 64416282
Progressive multifocal leukoencephalopathy 25.25 13.43 32 23209 18200 64457291
Interstitial lung disease 24.85 13.43 3 23238 97729 64377762
Deformity 23.65 13.43 19 23222 6278 64469213
Depressed mood 23.35 13.43 48 23193 40964 64434527
Throat irritation 23.18 13.43 42 23199 32669 64442822
Bradycardia 22.98 13.43 7 23234 118212 64357279
Cardio-respiratory arrest 22.75 13.43 4 23237 98389 64377102
Intentional overdose 22.29 13.43 3 23238 89941 64385550
Cardiac arrest 22.27 13.43 14 23227 154050 64321441
Neuropathy peripheral 21.78 13.43 92 23149 117433 64358058
Arthralgia 21.66 13.43 249 22992 442011 64033480
Lower respiratory tract infection 21.53 13.43 79 23162 94535 64380956
Appendicolith 21.08 13.43 14 23227 3455 64472036
Nausea 20.60 13.43 397 22844 785403 63690088
Flatulence 19.43 13.43 41 23200 35625 64439866
Balance disorder 19.03 13.43 70 23171 83856 64391635
Febrile neutropenia 18.80 13.43 24 23217 187633 64287858
Coordination abnormal 18.75 13.43 25 23216 14939 64460552
Constipation 18.69 13.43 144 23097 229193 64246298
Glaucoma 18.50 13.43 26 23215 16322 64459169
Systemic lupus erythematosus 18.28 13.43 3 23238 77609 64397882
Skin lesion 17.67 13.43 40 23201 36442 64439049
Septic shock 17.55 13.43 8 23233 105429 64370062
Blood cholesterol increased 17.03 13.43 48 23193 50018 64425473
General physical health deterioration 16.75 13.43 30 23211 204395 64271096
Cardiac failure 16.56 13.43 14 23227 132359 64343132
Low density lipoprotein increased 16.52 13.43 17 23224 7723 64467768
Overdose 16.41 13.43 20 23221 159546 64315945
Dry skin 16.39 13.43 48 23193 51113 64424378
Blood pressure increased 16.15 13.43 112 23129 172440 64303051
Hernia 16.05 13.43 22 23219 13496 64461995
Spinal epidural haematoma 15.52 13.43 8 23233 1234 64474257
Pulmonary embolism 15.41 13.43 18 23223 146338 64329153
Cataract 15.38 13.43 47 23194 51215 64424276
Body height decreased 15.07 13.43 16 23225 7538 64467953
Maternal exposure during pregnancy 14.86 13.43 8 23233 95876 64379615
Nasopharyngitis 14.81 13.43 121 23120 195952 64279539
Pancytopenia 14.69 13.43 18 23223 143291 64332200
C-reactive protein increased 14.59 13.43 8 23233 94901 64380590
Underdose 14.43 13.43 30 23211 25799 64449692
Eye disorder 14.36 13.43 25 23216 18844 64456647
Muscle spasms 14.06 13.43 93 23148 140930 64334561
Dysgeusia 13.99 13.43 43 23198 47004 64428487
Bone hypertrophy 13.87 13.43 5 23236 321 64475170
Cough 13.82 13.43 168 23073 301980 64173511
Cystic fibrosis lung 13.54 13.43 4 23237 136 64475355
Hyperkalaemia 13.52 13.43 10 23231 101119 64374372

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A11HA08 ALIMENTARY TRACT AND METABOLISM
VITAMINS
OTHER PLAIN VITAMIN PREPARATIONS
Other plain vitamin preparations
CHEBI has role CHEBI:22586 antioxidants
CHEBI has role CHEBI:22587 antiviral agents
CHEBI has role CHEBI:27027 trace elements
CHEBI has role CHEBI:37700 protein kinase C inhibitors
CHEBI has role CHEBI:50249 anticoagulants
CHEBI has role CHEBI:50733 Dietary Supplement
CHEBI has role CHEBI:50846 Immunologic factor
CHEBI has role CHEBI:50855 antiatherogenic drug
CHEBI has role CHEBI:76924 plant metabolites
CHEBI has role CHEBI:84735 algal metabolites
MeSH PA D000975 Antioxidants
MeSH PA D018977 Micronutrients
MeSH PA D020011 Protective Agents
MeSH PA D014815 Vitamins

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Obstruction of bile duct indication 30144000
Vitamin E deficiency indication 54137008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.06 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
Glutathione S-transferase P Enzyme IC50 6.30 CHEMBL
Alpha-tocopherol transfer protein Transporter Kd 5.62 CHEMBL

External reference:

IDSource
N0000011305 NUI
10191-41-0 SECONDARY_CAS_RN
4017771 VANDF
CHEBI:18145 CHEBI
VIV PDB_CHEM_ID
CHEMBL2108106 ChEMBL_ID
D06174 KEGG_DRUG
CHEMBL47 ChEMBL_ID
CHEMBL3989727 ChEMBL_ID
C014225 MESH_SUPPLEMENTAL_RECORD_UI
DB11635 DRUGBANK_ID
N9PR3490H9 UNII
71406 PUBCHEM_CID
DB00163 DRUGBANK_ID
159151 RXNORM
11960 MMSL
009945 NDDF
116776001 SNOMEDCT_US
259666007 SNOMEDCT_US
768524003 SNOMEDCT_US
D024502 MESH_DESCRIPTOR_UI
C0606070 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CitraNatal Harmony 3.0 HUMAN PRESCRIPTION DRUG LABEL 8 0178-0796 CAPSULE, GELATIN COATED 30 [iU] ORAL unapproved drug other 10 sections
CitraNatal Harmony HUMAN PRESCRIPTION DRUG LABEL 8 0178-0798 CAPSULE, GELATIN COATED 30 [iU] ORAL UNAPPROVED DRUG OTHER 11 sections
CitraNatal Harmony HUMAN PRESCRIPTION DRUG LABEL 8 0178-0799 CAPSULE, GELATIN COATED 30 [iU] ORAL Unapproved drug other 11 sections
CitraNatal Harmony HUMAN PRESCRIPTION DRUG LABEL 8 0178-0812 CAPSULE, GELATIN COATED 30 [iU] ORAL Unapproved drug other 11 sections
CitraNatal Medley HUMAN PRESCRIPTION DRUG LABEL 8 0178-0896 CAPSULE, GELATIN COATED 15 [iU] ORAL unapproved drug other 10 sections
VitafolOne HUMAN PRESCRIPTION DRUG LABEL 16 0642-0070 CAPSULE, GELATIN COATED 9 mg ORAL unapproved drug other 14 sections
Vitafol Caplet HUMAN PRESCRIPTION DRUG LABEL 12 0642-0072 CAPSULE 10 [iU] ORAL UNAPPROVED DRUG OTHER 13 sections
Vitafol OB Caplet HUMAN PRESCRIPTION DRUG LABEL 15 0642-0079 TABLET 30 [iU] ORAL Unapproved drug other 14 sections
Vitafol Plus HUMAN PRESCRIPTION DRUG LABEL 17 0642-0092 CAPSULE, LIQUID FILLED 10 [iU] ORAL UNAPPROVED DRUG OTHER 13 sections
Strovite Forte Caplet HUMAN PRESCRIPTION DRUG LABEL 19 0642-0204 TABLET, COATED 60 [iU] ORAL UNAPPROVED DRUG OTHER 15 sections
Reaphirm Plant Source DHA HUMAN PRESCRIPTION DRUG LABEL 16 0642-3010 CAPSULE, GELATIN COATED 20 [iU] ORAL unapproved drug other 7 sections
Quflora Pediatric HUMAN PRESCRIPTION DRUG LABEL 14 15370-103 TABLET, CHEWABLE 15 [iU] ORAL UNAPPROVED DRUG OTHER 12 sections
Quflora Pediatric HUMAN PRESCRIPTION DRUG LABEL 14 15370-104 TABLET, CHEWABLE 15 [iU] ORAL UNAPPROVED DRUG OTHER 12 sections
Quflora Pediatric HUMAN PRESCRIPTION DRUG LABEL 14 15370-105 TABLET, CHEWABLE 15 [iU] ORAL UNAPPROVED DRUG OTHER 12 sections
C-Nate DHA HUMAN PRESCRIPTION DRUG LABEL 13 23359-105 CAPSULE, GELATIN COATED 30 [iU] ORAL unapproved drug other 15 sections
PNV-Omega HUMAN PRESCRIPTION DRUG LABEL 13 42192-332 CAPSULE, GELATIN COATED 10 [iU] ORAL unapproved drug other 12 sections
Prenaissance HUMAN PRESCRIPTION DRUG LABEL 9 42192-341 CAPSULE, LIQUID FILLED 30 [iU] ORAL UNAPPROVED DRUG OTHER 10 sections
Kimchi Vitaminchewable multivitamin HUMAN OTC DRUG LABEL 11 52102-1001 TABLET, CHEWABLE 1.88 mg ORAL unapproved drug other 2 sections
Floriva HUMAN PRESCRIPTION DRUG LABEL 16 52796-173 TABLET, CHEWABLE 20 [iU] ORAL UNAPPROVED DRUG OTHER 6 sections
Floriva HUMAN PRESCRIPTION DRUG LABEL 16 52796-174 TABLET, CHEWABLE 20 [iU] ORAL UNAPPROVED DRUG OTHER 6 sections
Floriva HUMAN PRESCRIPTION DRUG LABEL 16 52796-177 TABLET, CHEWABLE 20 [iU] ORAL UNAPPROVED DRUG OTHER 7 sections
TRICARE PRENATAL DHA ONE HUMAN PRESCRIPTION DRUG LABEL 17 67112-401 CAPSULE, GELATIN COATED 30 [iU] ORAL unapproved drug other 12 sections
AntiphlamineCoin Plaster HUMAN OTC DRUG LABEL 7 69642-1600 PATCH 0.31 mg TOPICAL unapproved drug other 9 sections
Acne C-Patch HUMAN OTC DRUG LABEL 1 70236-103 PATCH 0.06 g TOPICAL unapproved drug other 8 sections
PRENATE DHA HUMAN PRESCRIPTION DRUG LABEL 10 75854-312 CAPSULE, GELATIN COATED 40 [iU] ORAL unapproved drug other 13 sections
DR. WALTONS BABY POWDER HUMAN OTC DRUG LABEL 2 76271-001 POWDER 5.20 g TOPICAL OTC monograph not final 8 sections
SOLNARA Everything Blood circulation Nattokinase(Control blood pressure and Improve blood circulation) HUMAN OTC DRUG LABEL 6 82559-8751 POWDER 0.10 g ORAL unapproved drug other 9 sections
Dechangling HUMAN OTC DRUG LABEL 12 82570-009 POWDER 2 g TOPICAL unapproved drug other 8 sections
De Haomian HUMAN OTC DRUG LABEL 5 82570-014 POWDER 7 g TOPICAL unapproved drug other 8 sections
Debaochun HUMAN OTC DRUG LABEL 7 82570-016 POWDER 2 dL TOPICAL unapproved drug other 8 sections