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Identification
- Summary
Tocofersolan is a derivative of alpha tocopherol used to treat vitamin E deficiencies.
- Brand Names
- Vedrop
- Generic Name
- Tocofersolan
- DrugBank Accession Number
- DB11635
- Background
D-Alpha-tocopheryl polyethylene glycol 1000 succinate (Tocofersolan, Vedrop), has been developed in Europe as an orally bioavailable source of vitamin E in children suffering from cholestasis 3. Cholestasis is the reduction or stoppage of bile flow, either to impaired secretion by hepatocytes (liver cells) or obstruction 4, 5.
Tocofersolan is a polyethylene glycol derivative of α-tocopherol and synthetic water-soluble version of Tocopherol. Tocofersolan is an oral treatment of vitamin E deficiency due to digestive malabsorption in pediatric patients with congenital chronic cholestasis or hereditary chronic cholestasis. It was approved by the European Medicines Agency (EMA) in June 2009 under the market name Vedrop. Moreover, the agent is capable of demonstrating antioxidant effects that make it a popular component to include in cosmetics and pharmaceuticals as well.
In addition to the above, tocofersolan has been studied as a promising application as an absorption enhancer in drug delivery MSDS.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- (+)-.ALPHA.-TOCOPHERYL POLYETHYLENE GLYCOL 1000 SUCCINATE
- D-.ALPHA.-TOCOPHEROL POLYETHYLENE GLYCOL 1000 SUCCINATE
- Mono-[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-6-chromanyl] succinate polyethylene glycol monoester
- 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-
- Tocofersolan
- Tocofersolano
- Tocofersolanum
- Tocophersolan
- TPG-S
- TPGS
- VITAMIN E POLYETHYLENE GLYCOL 1000 SUCCINATE
- VITAMIN E POLYETHYLENE GLYCOL SUCCINATE
Pharmacology
- Indication
Tocofersolan is indicated in vitamin E deficiency caused by digestive malabsorption in pediatric patients with congenital chronic cholestasis or hereditary chronic cholestasis from birth (full term newborns) up to 18 years of age 3.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Vitamin e deficiency •••••••••••• •••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Because of its increased solubility 4, 6, 9, this medication readily penetrates cells, unlike other types of vitamin E MSDS, which are strictly fat-soluble MSDS. Specific to cholestasis, tocofersolan normalizes vitamin E levels relieving the symptoms of deficiency because of its facilitation of vitamin E absorption 3, 8.
- Mechanism of action
Vitamin E is a major lipo-soluble antioxidant in humans. It acts as a free radical chain breaking molecule, halting the peroxidation of polyunsaturated fatty acids and it plays an important role in maintaining both the stability and integrity of cell membranes 3.
Target Actions Organism UATP-dependent translocase ABCB1 antagonistHumans - Absorption
The bioavailability of vitamin E from tocofersolan is unique from than that of other medicinal products 3.
Due to its amphipathic property in which it forms its own micelles, tocofersolan is readily taken up into enterocytes, even in the absence of bile salts; fat-soluble d-alpha-tocopherol is then released after hydrolysis. This formulation enhances the absorption of d-alpha-tocopherol compared to the administration of free d-alpha-tocopherol. Additionally, tocophersolan may enhance the absorption of water-insoluble agents and other fat-soluble vitamins 6.
Tocofersolan is a pro-drug; the active metabolite is the d-alpha-tocopherol. At low concentrations, tocofersolan forms micelles which improve the absorption of non-polar lipids such as other fat-soluble vitamins. Its required micellar concentration is low (0.04 to 0.06 mmol/l) 3.
A pharmacokinetic study of 12 healthy subjects compared tocofersolan with a water-miscible reference vitamin E after one single oral loading dose of 1200 IU (international units). The relative bioavailability of tocofersolan was found to be (Frel of 1.01 ± 1.74) with AUC0-t of 0.383 ± 0.203μM.h/mg, Cmax of 0.013 ± 0.006, Tmax of 6.0 h (6.0 – 24.0) 3.
For more information about Vitamin E metabolism, please visit the drug entry Tocopherol.
- Volume of distribution
Located principally on cell membranes, within mitochondria and microsomes, vitamin E is widely distributed throughout the body (red blood cells, brain, muscle, liver, platelets) and fat tissues are its primary reservoir 3.
- Protein binding
Highly bound to lipoproteins 3.
- Metabolism
The hydrolysis of tocofersolan occurs in the gut lumen. Tocofersolan is absorbed by cells, and the alpha-tocopherol moiety appears in chylomicrons in the lymph system in a manner that is identical to vitamin E absorbed from dietary sources. Cellular uptake does not require receptors, binding proteins or metabolic processes and does not occur by pinocytosis. Absorption of deuterated tocofersolan demonstrated a normal pattern in lipoproteins: alpha-tocopherol peaked first in chylomicrons, then peaked in very low- density lipoproteins (VLDL) and finally in low-density lipoproteins (LDL) and high-density lipoproteins (HDL)3.
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- Route of elimination
Vitamin E is primarily eliminated in the bile (75%) and feces, either as free tocopherol or in oxidized forms. Urine is a minor elimination route of vitamin E (as glucuronic-conjugate) 3.
- Half-life
29.7 h 3
- Clearance
Not Available
- Adverse Effects
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> 7 g/kg ( Rat ) 10
Common adverse reactions
The most commonly reported adverse reaction during treatment is diarrhea 3. High doses of Vitamin E may cause diarrhea, abdominal pain, and other gastrointestinal conditions. In the case of an overdose, symptomatic treatment should be provided 3. High doses of vitamin E have been reported to increase bleeding tendency in patients with Vitamin K deficiency, or patients taking oral anti-vitamins K treatment 3. Therefore, careful monitoring of the prothrombin time and international normalized ratio (INR) are advised. A possible adjustment of the dose of oral anticoagulant during and after treatment with Vedrop may be necessary 3.
Renal impairment
Data regarding patients with renal impairment are limited, this drug should be administered with caution and those with renal impairment or dehydration should be closely followed 3.
Hepatic impairment
This drug should be administered with caution in patients with liver impairment and under close monitoring of the liver function tests in such patients 3.
Hypersensitivity
Vedrop, the commercial form, contains sodium methyl parahydroxybenzoate (E219) and sodium ethyl parahydroxybenzoate (E215) which may cause allergic reactions, which are sometimes delayed 3.
Pregnancy
There is no current data on taking tocofersolan during pregnancy. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/ fetal development, parturition or postnatal development. Caution should be taken when prescribing this medication to pregnant women 3.
Breast-feeding
It is unknown whether tocofersolan is released into human breast milk. The excretion of tocofersolan in milk has not been studied in animals 3.
Fertility
No data is available 3.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Tocofersolan can be increased when it is combined with Abametapir. Amiodarone The metabolism of Tocofersolan can be decreased when combined with Amiodarone. Amprenavir The metabolism of Tocofersolan can be decreased when combined with Amprenavir. Apalutamide The serum concentration of Tocofersolan can be decreased when it is combined with Apalutamide. Aprepitant The metabolism of Tocofersolan can be decreased when combined with Aprepitant. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Vedrop Solution 50 mg/mL Oral Recordati Rare Diseases 2017-09-15 Not applicable EU 
Vedrop Solution 50 mg/mL Oral Recordati Rare Diseases 2017-09-15 Not applicable EU Vedrop Solution 50 mg/mL Oral Recordati Rare Diseases 2017-09-15 Not applicable EU - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aquasol E Tpgs Liquid 77iu/ml Liquid 77 unit / mL Oral Columbia Laboratories 1996-10-21 2009-07-17 Canada 
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image NESTABS ABC Prenatal Multi-vitamin/Mineral Supplement with DHA/EPA Tocofersolan (30 [iU]/1) + Ascorbic acid (120 mg/1) + Calcium (155 mg/1) + Calcium carbonate (45 mg/1) + Cholecalciferol (450 [iU]/1) + Choline bitartrate (55 mg/1) + Cyanocobalamin (10 ug/1) + Doconexent (120 mg/1) + Folic acid (1 mg/1) + Icosapent (180 mg/1) + Iron (32 mg/1) + Niacin (20 mg/1) + Potassium Iodide (100 ug/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (3 mg/1) + Thiamine chloride (3 mg/1) + Tocopherol (10 mg/1) + Zinc (10 mg/1) Capsule, gelatin coated; Kit; Tablet Oral WOMENS CHOICE PHARMACEUTICALS LLC 2011-02-01 2018-03-01 US 
Pre-Tabs DHA Prenatal Multi-vitamin/Mineral Supplement with DHA/EPA Tocofersolan (30 [iU]/1) + Calcium carbonate (45 mg/1) + Cholecalciferol (450 [iU]/1) + Choline bitartrate (55 mg/1) + Cyanocobalamin (10 ug/1) + Doconexent (230 mg/1) + Ferrous bisglycinate (32 mg/1) + Folic acid (1 mg/1) + Calcium formate (155 mg/1) + Icosapent (30 mg/1) + Nicotinamide (20 mg/1) + Potassium Iodide (100 ug/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (3 mg/1) + Sodium ascorbate (120 mg/1) + Thiamine mononitrate (3 mg/1) + Vitamin E (2 [iU]/1) + Zinc oxide (10 mg/1) Kit Oral DEREMETRX LLC 2014-06-15 Not applicable US
Categories
- ATC Codes
- A11HA08 — Tocofersolan
- Drug Categories
- Alimentary Tract and Metabolism
- Benzopyrans
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drug Carriers
- Heterocyclic Compounds, Fused-Ring
- Pyrans
- Vitamin E
- Vitamins
- Vitamins (Fat Soluble)
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- O03S90U1F2
- CAS number
- 9002-96-4
References
- General References
- Thebaut A, Nemeth A, Le Mouhaer J, Scheenstra R, Baumann U, Koot B, Gottrand F, Houwen R, Monard L, de Micheaux SL, Habes D, Jacquemin E: Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis. J Pediatr Gastroenterol Nutr. 2016 Dec;63(6):610-615. doi: 10.1097/MPG.0000000000001331. [Article]
- Roongpraiwan R, Suthutvoravut U, Feungpean B, Phuapradit P: Effect of oral vitamin E supplementation in children with cholestasis. J Med Assoc Thai. 2002 Nov;85 Suppl 4:S1199-205. [Article]
- EMA Summary Assessment Report [Link]
- Cholestasis [Link]
- Emedicine, Cholestasis [Link]
- Tocophersolan, PubChem [Link]
- Parmentier document [Link]
- Dosage and formulation issues: oral vitamin E therapy in children [Link]
- Scottish Medicines Document, Tocofersolan [Link]
- MSDS, Santa Cruz [Link]
- Vitamin E Regulatory Mechanisms [Link]
- α-TOCOPHEROL β-OXIDATION LOCALIZED TO RAT LIVER MITOCHONDRIA [Link]
- EMA Summary of Product Characteristics: Vedrop (tocofersolan) oral solution [Link]
- External Links
- PubChem Substance
- 347911221
- 159151
- Wikipedia
- Tocofersolan
- FDA label
- Download (345 KB)
- MSDS
- Download (160 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data3 Completed Treatment Hypobetalipoproteinemias 1 somestatus stop reason just information to hide 2 Withdrawn Treatment Short Bowel Syndrome (SBS) / Vitamin E Deficiency 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 500.000 UI Liquid Oral 77 unit / mL Capsule Oral 400.000 mg Solution Parenteral Capsule, gelatin coated; kit; tablet Oral Kit Oral Solution Oral 50 MG/ML - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 34-38 MSDS water solubility soluble at 1g/10 mL MSDS - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- Abc-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
- EMA Summary Assessment Report [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, eicosanoids and vitamins (PubMed:10660572, PubMed:10833273, PubMed:11997390, PubMed:17341693, PubMed:18574070, PubMed:18577768). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase). Catalyzes predominantly the oxidation of the terminal carbon (omega-oxidation) of long- and very long-chain fatty acids. Displays high omega-hydroxylase activity toward polyunsaturated fatty acids (PUFAs) (PubMed:18577768). Participates in the conversion of arachidonic acid to omega-hydroxyeicosatetraenoic acid (20-HETE), a signaling molecule acting both as vasoconstrictive and natriuretic with overall effect on arterial blood pressure (PubMed:10660572, PubMed:17341693, PubMed:18574070). Plays a role in the oxidative inactivation of eicosanoids, including both pro-inflammatory and anti-inflammatory mediators such as leukotriene B4 (LTB4), lipoxin A4 (LXA4), and several HETEs (PubMed:10660572, PubMed:10833273, PubMed:17341693, PubMed:18574070, PubMed:18577768, PubMed:8026587, PubMed:9799565). Catalyzes omega-hydroxylation of 3-hydroxy fatty acids (PubMed:18065749). Converts monoepoxides of linoleic acid leukotoxin and isoleukotoxin to omega-hydroxylated metabolites (PubMed:15145985). Contributes to the degradation of very long-chain fatty acids (VLCFAs) by catalyzing successive omega-oxidations and chain shortening (PubMed:16547005, PubMed:18182499). Plays an important role in vitamin metabolism by chain shortening. Catalyzes omega-hydroxylation of the phytyl chain of tocopherols (forms of vitamin E), with preference for gamma-tocopherols over alpha-tocopherols, thus promoting retention of alpha-tocopherols in tissues (PubMed:11997390). Omega-hydroxylates and inactivates phylloquinone (vitamin K1), and menaquinone-4 (MK-4, a form of vitamin K2), both acting as cofactors in blood coagulation (PubMed:19297519, PubMed:24138531)
- Specific Function
- 20-aldehyde-leukotriene b4 20-monooxygenase activity
- Gene Name
- CYP4F2
- Uniprot ID
- P78329
- Uniprot Name
- Cytochrome P450 4F2
- Molecular Weight
- 59852.825 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Binds alpha-tocopherol, enhances its transfer between separate membranes, and stimulates its release from liver cells (PubMed:7887897). Binds both phosphatidylinositol 3,4-bisphosphate and phosphatidylinositol 4,5-bisphosphate; the resulting conformation change is important for the release of the bound alpha-tocopherol (By similarity)
- Specific Function
- Lipid transfer activity
- Gene Name
- TTPA
- Uniprot ID
- P49638
- Uniprot Name
- Alpha-tocopherol transfer protein
- Molecular Weight
- 31749.305 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Receptor for different ligands such as phospholipids, cholesterol ester, lipoproteins, phosphatidylserine and apoptotic cells (PubMed:12016218, PubMed:12519372, PubMed:21226579). Receptor for HDL, mediating selective uptake of cholesteryl ether and HDL-dependent cholesterol efflux (PubMed:26965621). Also facilitates the flux of free and esterified cholesterol between the cell surface and apoB-containing lipoproteins and modified lipoproteins, although less efficiently than HDL. May be involved in the phagocytosis of apoptotic cells, via its phosphatidylserine binding activity (PubMed:12016218)
- Specific Function
- 1-phosphatidylinositol binding
- Gene Name
- SCARB1
- Uniprot ID
- Q8WTV0
- Uniprot Name
- Scavenger receptor class B member 1
- Molecular Weight
- 60877.385 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Plays a major role in cholesterol homeostasis (PubMed:22095670). Critical for the uptake of cholesterol across the plasma membrane of the intestinal enterocyte (PubMed:22095670). Involved in plant sterol absorption, it transports sitosterol, although at lower rates than cholesterol (By similarity). Is the direct molecular target of ezetimibe, a drug that inhibits cholesterol absorption and is approved for the treatment of hypercholesterolemia (PubMed:15928087). May have a function in the transport of multiple lipids and their homeostasis, thereby influencing lipid metabolism regulation (PubMed:15671032). May be involved in caveolin trafficking from the plasma membrane (By similarity). In addition, acts as a negative regulator of NPC2 and down-regulates its expression and secretion by inhibiting its maturation and accelerating its degradation (PubMed:22095670)
- Specific Function
- Cholesterol binding
- Gene Name
- NPC1L1
- Uniprot ID
- Q9UHC9
- Uniprot Name
- NPC1-like intracellular cholesterol transporter 1
- Molecular Weight
- 148726.52 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- ABCG5 and ABCG8 form an obligate heterodimer that mediates Mg(2+)- and ATP-dependent sterol transport across the cell membrane (PubMed:27144356). Plays an essential role in the selective transport of dietary plant sterols and cholesterol in and out of the enterocytes and in the selective sterol excretion by the liver into bile (PubMed:11099417, PubMed:11138003, PubMed:15054092, PubMed:27144356). Required for normal sterol homeostasis (PubMed:11099417, PubMed:11138003, PubMed:15054092). The heterodimer with ABCG8 has ATPase activity (PubMed:16893193, PubMed:20210363, PubMed:27144356)
- Specific Function
- Abc-type transporter activity
- Gene Name
- ABCG5
- Uniprot ID
- Q9H222
- Uniprot Name
- ATP-binding cassette sub-family G member 5
- Molecular Weight
- 72503.02 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- ABCG5 and ABCG8 form an obligate heterodimer that mediates Mg(2+)- and ATP-dependent sterol transport across the cell membrane. Plays an essential role in the selective transport of the dietary cholesterol in and out of the enterocytes and in the selective sterol excretion by the liver into bile (PubMed:11099417, PubMed:11452359, PubMed:15054092, PubMed:27144356). Required for normal sterol homeostasis (PubMed:11099417, PubMed:11452359, PubMed:15054092). The heterodimer with ABCG5 has ATPase activity (PubMed:16893193, PubMed:20210363, PubMed:27144356)
- Specific Function
- Abc-type transporter activity
- Gene Name
- ABCG8
- Uniprot ID
- Q9H221
- Uniprot Name
- ATP-binding cassette sub-family G member 8
- Molecular Weight
- 75678.03 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Catalyzes the translocation of specific phospholipids from the cytoplasmic to the extracellular/lumenal leaflet of membrane coupled to the hydrolysis of ATP (PubMed:24097981, PubMed:35974019). Thereby, participates in phospholipid transfer to apolipoproteins to form nascent high density lipoproteins/HDLs (PubMed:14754908). Transports preferentially phosphatidylcholine over phosphatidylserine (PubMed:24097981). May play a similar role in the efflux of intracellular cholesterol to apolipoproteins and the formation of nascent high density lipoproteins/HDLs (PubMed:10533863, PubMed:14754908, PubMed:24097981, PubMed:35974019). Translocates phospholipids from the outer face of the plasma membrane and forces it through its gateway and annulus into an elongated hydrophobic tunnel in its extracellular domain (PubMed:35974019)
- Specific Function
- Abc-type transporter activity
- Gene Name
- ABCA1
- Uniprot ID
- O95477
- Uniprot Name
- Phospholipid-transporting ATPase ABCA1
- Molecular Weight
- 254299.89 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Probable hydrophobic ligand-binding protein; may play a role in the transport of hydrophobic ligands like tocopherol, squalene and phospholipids
- Specific Function
- Lipid binding
- Gene Name
- SEC14L4
- Uniprot ID
- Q9UDX3
- Uniprot Name
- SEC14-like protein 4
- Molecular Weight
- 46643.385 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Carrier protein. Binds to some hydrophobic molecules and promotes their transfer between the different cellular sites. Binds with high affinity to alpha-tocopherol. Also binds with a weaker affinity to other tocopherols and to tocotrienols. May have a transcriptional activatory activity via its association with alpha-tocopherol. Probably recognizes and binds some squalene structure, suggesting that it may regulate cholesterol biosynthesis by increasing the transfer of squalene to a metabolic active pool in the cell
- Specific Function
- Phospholipid binding
- Gene Name
- SEC14L2
- Uniprot ID
- O76054
- Uniprot Name
- SEC14-like protein 2
- Molecular Weight
- 46144.9 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Probable hydrophobic ligand-binding protein; may play a role in the transport of hydrophobic ligands like tocopherol, squalene and phospholipids
- Specific Function
- Lipid binding
- Gene Name
- SEC14L3
- Uniprot ID
- Q9UDX4
- Uniprot Name
- SEC14-like protein 3
- Molecular Weight
- 46047.835 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Macrophage receptor that binds to the apolipoprotein B48 (APOB) of dietary triglyceride (TG)-rich lipoproteins (TRL) or to a like domain of APOB in hypertriglyceridemic very low density lipoprotein (HTG-VLDL). Binds and internalizes TRL when out of the context of the macrophage. May provide essential lipids to reticuloendothelial cells. Could also be involved in foam cell formation with elevated TRL and remnant lipoprotein (RLP). Mediates the rapid high-affinity uptake of chylomicrons (CM), HTG-VLDL, and trypsinized (tryp) VLDL devoid of APOE in vitro in macrophages
- Specific Function
- Very-low-density lipoprotein particle receptor activity
- Gene Name
- APOBR
- Uniprot ID
- Q0VD83
- Uniprot Name
- Apolipoprotein B receptor
- Molecular Weight
- 115633.15 Da
References
- Schmolz L, Birringer M, Lorkowski S, Wallert M: Complexity of vitamin E metabolism. World J Biol Chem. 2016 Feb 26;7(1):14-43. doi: 10.4331/wjbc.v7.i1.14. [Article]
Drug created at October 17, 2016 21:27 / Updated at September 28, 2023 05:40