Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C33H54O5 |
| Molecular Weight | 530.7789 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)CCC[C@@H](C)CCC[C@@H](C)CCC[C@]1(C)CCC2=C(C)C(OC(=O)CCC(O)=O)=C(C)C(C)=C2O1
InChI
InChIKey=IELOKBJPULMYRW-NJQVLOCASA-N
InChI=1S/C33H54O5/c1-22(2)12-9-13-23(3)14-10-15-24(4)16-11-20-33(8)21-19-28-27(7)31(25(5)26(6)32(28)38-33)37-30(36)18-17-29(34)35/h22-24H,9-21H2,1-8H3,(H,34,35)/t23-,24-,33-/m1/s1
| Molecular Formula | C33H54O5 |
| Molecular Weight | 530.7789 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000920/WC500047922.pdfCurator'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
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000920/WC500047922.pdf
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
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000920/WC500047922.pdf
Curator's Comment: Neurological symptoms were either improved or stabilized in 96% of patients with chronic congenital or hereditary cholestasis (pages 19-20)
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: GO:0016209 Sources: http://www.ncbi.nlm.nih.gov/pubmed/8387948 |
|||
Target ID: WP408 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Preventing | Vedrop Approved UseTocophersolan (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 UseTocophersolan (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 UseUnknown |
|||
| Palliative | Vedrop Approved UseUnknown |
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| Palliative | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Efficacy of two vitamin E formulations in patients with abetalipoproteinemia and chylomicron retention disease. | 2018-09 |
|
| Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis. | 2016-12 |
|
| Effect of hydrosoluble vitamin E on erythrocyte membrane lipid composition in patients with advanced cirrhosis: An open-label pilot trial. | 2015-08 |
|
| Guidelines for the diagnosis and management of chylomicron retention disease based on a review of the literature and the experience of two centers. | 2010-09-29 |
|
| Dosage and formulation issues: oral vitamin E therapy in children. | 2010-02 |
|
| Bioavailability of oral vitamin E formulations in adult volunteers and children with chronic cholestasis or cystic fibrosis. | 2009-10 |
|
| Determination of alpha-tocopherol in plasma by high performance liquid chromatography with fluorescence detection and stability of alpha-tocopherol under different conditions. | 2004 |
|
| 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 |
|
| 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 |
|
| 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. | 1997-02 |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000920/WC500047919.pdf
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 Use Guide
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000920/WC500047922.pdf
Curator's Comment: page 8
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 |
Chemical
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