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Description
Curator's Comment: description was created based on several sources, including http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000920/WC500047919.pdf http://www.ema.europa.eu/docs/en_GB/document_library/Medicine_QA/2009/11/WC500014528.pdf https://www.medicines.org.uk/emc/medicine/24235 https://www.ncbi.nlm.nih.gov/pubmed/12537931

Tocophersolan (Vedrop, tocofersolan) or d-alpha-Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS) is a watersoluble derivative of the natural active (d-alpha) isomer of vitamin E. The active constituent of the medicinal product is essentially vitamin E (alpha tocopherol). Chronic congenital or hereditary cholestasis is a clinical condition where vitamin E deficiency results from an impaired bile secretion. Decreased intestinal absorption observed in chronic congenital or hereditary cholestatic patients is due to decreased bile secretion and the resulting decrease in intestinal cellular absorption. As a result, fatsoluble vitamins (i.e. vit. E) are not absorbed properly and deficiency can occur. Tocophersolan (Vedrop) is used to treat or prevent vitamin E deficiency (low vitamin E levels). It is used in children up to the age of 18 years who have congenital or hereditary chronic cholestasis and who cannot absorb vitamin E from the gut. Tocophersolan (Tocofersolan) can be absorbed from the gut in children who have difficulty absorbing fats and vitamin E from the diet. This can increase vitamin E levels in the blood and help to prevent neurological deterioration (problems in the nervous system) due to vitamin E deficiency. No treatment-related findings were reported, as all clinical observations and findings at autopsy were similar in treatment and control groups. In many of the studies, the LD50 was not determined as tocofersolan was well tolerated.

CNS Activity

Curator's Comment: Neurological symptoms were either improved or stabilized in 96% of patients with chronic congenital or hereditary cholestasis (pages 19-20)

Originator

Curator's Comment: Tocophersolan or d-a-tocopheryl polyethylene glycol succinate (TPGS, CAS Registry Number 9002-96-4) was invented by Eastman Kodak in 1950.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
Vedrop

Approved Use

Tocophersolan (Vedrop) is used to treat or prevent vitamin E deficiency (low vitamin E levels). The recommended total daily dose in paediatric patients suffering from congenital chronic cholestasis or hereditary chronic cholestasis is 0.34 ml/kg/day (17 mg/kg of d-alpha-tocopherol in the form of tocofersolan). The dose should be prescribed in ml.
Palliative
Vedrop

Approved Use

Tocophersolan (Vedrop) is used to treat or prevent vitamin E deficiency (low vitamin E levels). The recommended total daily dose in paediatric patients suffering from congenital chronic cholestasis or hereditary chronic cholestasis is 0.34 ml/kg/day (17 mg/kg of d-alpha-tocopherol in the form of tocofersolan). The dose should be prescribed in ml.
Palliative
Vedrop

Approved Use

Unknown
Palliative
Vedrop

Approved Use

Unknown
Palliative
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Treatment of cholestatic children with water-soluble vitamin E (alpha-tocopheryl polyethylene glycol succinate): effects on serum vitamin E, lipid peroxides, and polyunsaturated fatty acids.
1997 Feb
Final report on the safety assessment of Tocopherol, Tocopheryl Acetate, Tocopheryl Linoleate, Tocopheryl Linoleate/Oleate, Tocopheryl Nicotinate, Tocopheryl Succinate, Dioleyl Tocopheryl Methylsilanol, Potassium Ascorbyl Tocopheryl Phosphate, and Tocophersolan.
2002
Antioxidant capacity in Fasciola hepatica patients before and after treatment with triclabendazole alone or in combination with ascorbic acid (vitamin C) and tocofersolan (vitamin E).
2003
Determination of alpha-tocopherol in plasma by high performance liquid chromatography with fluorescence detection and stability of alpha-tocopherol under different conditions.
2004
Bioavailability of oral vitamin E formulations in adult volunteers and children with chronic cholestasis or cystic fibrosis.
2009 Oct
Guidelines for the diagnosis and management of chylomicron retention disease based on a review of the literature and the experience of two centers.
2010 Sep 29
Effect of hydrosoluble vitamin E on erythrocyte membrane lipid composition in patients with advanced cirrhosis: An open-label pilot trial.
2015 Aug
Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis.
2016 Dec
Efficacy of two vitamin E formulations in patients with abetalipoproteinemia and chylomicron retention disease.
2018 Sep

Sample Use Guides

In Vivo Use Guide
Curator's Comment: Tocophersolan (Vedrop) is given with or without water. This dose should be adjusted depending on the amount of vitamin E in the child’s blood. This should be checked regularly.
The recommended total daily dose in paediatric patients suffering from congenital chronic cholestasis or hereditary chronic cholestasis is 0.34 ml/kg/day (17 mg/kg of d-alpha-tocopherol in the form of tocofersolan). The dose should be prescribed in ml.
Route of Administration: Oral
In vitro studies using fibroblasts, enterocytes and Caco-2 cells conclude that Tocophersolan (tocofersolan) is taken up as the intact molecule and undergoes a slow hydrolysis reaction, intracellularly, to give PEG 1000 and Vitamin E (d-α tocopherol).
Substance Class Polymer
Created
by admin
on Sat Dec 16 03:42:45 UTC 2023
Edited
by admin
on Sat Dec 16 03:42:45 UTC 2023
Record UNII
O03S90U1F2
Record Status Validated (UNII)
Record Version
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Name Type Language
TOCOFERSOLAN
EMA EPAR   WHO-DD  
INN  
Preferred Name English
TOCOPHERSOLAN
USAN   INCI  
Preferred Name English
VITAMIN E POLYETHYLENE GLYCOL SUCCINATE
Common Name English
Mono-[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-6-chromanyl] succinate polyethylene glycol monoester
Common Name English
TPG-S
Code English
D-.ALPHA.-TOCOPHEROL POLYETHYLENE GLYCOL 1000 SUCCINATE
Common Name English
TOCOFERSOLAN [EMA EPAR]
Common Name English
(+)-.ALPHA.-TOCOPHERYL POLYETHYLENE GLYCOL 1000 SUCCINATE
Common Name English
LIQUI-E
Brand Name English
Tocofersolan [WHO-DD]
Common Name English
VEDROP
Brand Name English
tocofersolan [INN]
Common Name English
TOCOPHERSOLAN [II]
Common Name English
TPGS
Code English
VITAMIN E POLYETHYLENE GLYCOL 1000 SUCCINATE
Common Name English
TOCOPHERSOLAN [USAN]
Common Name English
TOCOPHERSOLAN [EMA EPAR]
Common Name English
POLY(OXY-1,2-ETHANEDIYL), .ALPHA.-(4-((3,4-DIHYDRO-2,5,7,8-TETRAMETHYL-2-(4,8,12-TRIMETHYLTRIDECYL)-2H-1-BENZOPYRAN-6-YL)OXY)-1,4-DIOXOBUTYL-.OMEGA.-HYDROXY-
Common Name English
TOCOPHERSOLAN [INCI]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 468414
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
FDA ORPHAN DRUG 22687
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
WHO-ATC A11HA08
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
EMA ASSESSMENT REPORTS VEDROP (AUTHORIZED: CHOLESTASIS)
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
NCI_THESAURUS C275
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
WHO-VATC QA11HA08
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
Code System Code Type Description
INN
1706
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
ChEMBL
CHEMBL2108106
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
NCI_THESAURUS
C67044
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
ChEMBL
CHEMBL2108812
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
EVMPD
SUB31955
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
WIKIPEDIA
TOCOFERSOLAN
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
SMS_ID
100000124318
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
MESH
C014225
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
CAS
9002-96-4
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
FDA UNII
O03S90U1F2
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
DRUG BANK
DB11635
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
RXCUI
159151
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY RxNorm
EPA CompTox
DTXSID1048623
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
DAILYMED
O03S90U1F2
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
DRUG CENTRAL
4280
Created by admin on Sat Dec 16 03:42:45 UTC 2023 , Edited by admin on Sat Dec 16 03:42:45 UTC 2023
PRIMARY
Display Structure of VITAMIN E POLYETHYLENE GLYCOL SUCCINATE
Related Record Type Details
TRANSPORTER -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY
TPGS enhances vitamin D absorbtion in chronic cholestatic liver disease of infancy and childhood (17). In 1999, the increased absorption of an anti-HIV protease inhibitor was suggested as a consequence of the drug’s solubility and permeability increase.
Name Property Type Amount Referenced Substance Defining Parameters References
HYDROPHILLIC-LIPOPHILLIC BALANCE (HLB) CHEMICAL
VISCOSITY PHYSICAL
MOL_WEIGHT:NUMBER AVERAGE CHEMICAL