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Overview
- Description
- An ingredient used in a wide variety of medications, and is not an approved medication.
- Description
- An ingredient used in a wide variety of medications, and is not an approved medication.
- DrugBank ID
- DB11077
- Type
- Small Molecule
- Clinical Trials
- Phase 0
- 3
- Phase 1
- 3
- Phase 2
- 14
- Phase 3
- 8
- Phase 4
- 32
Identification
- Summary
Polyethylene glycol 400 is an ingredient used in a wide variety of medications, and is not an approved medication.
- Brand Names
- Blink Tears, Colirio Ocusan, Leader Lubricant Eye Drops, QC ultra lubricant eye, Systane, Tears Lubricant, Visine Dry Eye Relief
- Generic Name
- Polyethylene glycol 400
- DrugBank Accession Number
- DB11077
- Background
Polyethylene glycols (PEGs) are products made of condensed ethylene oxide and water that can contain various derivatives and have various functions. Because many PEG types are hydrophilic, they are favorably used as enhancers of penetration, and used heavily in topical dermatological preparations. PEGs, along with their many nonionic derivatives, are widely utilized in cosmetic products as surfactants, emulsifiers, cleansing agents, humectants, and skin conditioners.9
Polyethylene glycol 400 (PEG 400) is a low-molecular-weight grade of polyethylene glycol with a low-level toxicity. It is very hydrophilic, which renders it a useful ingredient in drug formulations to augment the solubility and bioavailability of weakly water-soluble drugs. It is used in ophthalmic solutions for the relief of burning, irritation and/or discomfort that follows dryness of the eye 7. PEG "400" indicates that the average molecular weight of the specific PEG is 400 10.
PEGylation occurs when PEGs are attached to numerous protein medications, allowing for greater solubility for selected drugs. Examples of PEGylated medications are PEG-interferon alpha (Pegintron) and PEG-filgrastim. In addition, PEG is available as a bowel preparation for colonoscopy procedures and as a laxative 10.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- 3,6,9,12,15,18,21-heptaoxatricosane-1,23-diol
- Octaethylene glycol
- PEG-400
- PEG-8
- Polyethylene glycol 400
- Polyethylene glycol 8
Pharmacology
- Indication
PEG-400 has been indicated for the temporary relief of burning and irritation due to dryness of the eye, andfor protection against further irritation and desiccation 14, 15, 16.
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 Constipation ••• ••• •••••••• Symptomatic treatment of Dry eyes ••• ••• •••••••• • ••••• - 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
PEG, when used as PEG-400 for eye lubrication provides relief of dry eye symptoms and prevents further irritation, thus protecting the eye from injury 15. PEG allows comfortable eye drop/natural tear instillation by offering improved spreading of the drop over the ocular surface with diminished blurring 14,15.
- Mechanism of action
PEG, depending on molecular weight, has various mechanisms of action 4, 5, 6, 7. For the purpose of Peg-400, the mechanism of action on the eye tissues will be the primary focus of discussion.
PEG-400 is considered a lacrimomimetic, or a synthetic ocular lubricant that improves one or more components of the lacrimal film by augmenting the tear volume and stability and by protecting the eye surface against desiccation 16. Hydroxypropyl-guar (HPG) is used along with polyethylene glycol 400 (PEG) and propylene glycol (PG) as a gelling agent that conforms to abnormalities of the tear film and existing irregularities on the ocular surface 16.
PEG provides lubrication and acts as a surfactant by coating the eye and interacting with propylene glycol and other solutions that help to act as surfactants on the eye mucosa 15. This allows for long-lasting, soothing effects 15.
Recent studies involving nanoparticle drug delivery have demonstrated that PEG can achieve sustained drug delivery. The delivery of drugs to mucosal surfaces is a significant challenge due to the presence of the protective mucus layer that acts to trap and quickly remove foreign particles. Nanoparticles designed to rapidly cross mucosal barriers (mucus-penetrating particles, “MPP”) have proven promising for augmenting drug distribution, and efficacy at various mucosal surfaces. Mucus- penetrating particles are heavily coated with polyethylene glycol (PEG), protecting the nanoparticle core from adhesion with mucus 17.
Polyethylene glycol, when free in solution, may also demonstrate attraction to the surfaces of various types of vesicles, cells or macromolecules, leading to polymer adsorption and subsequently either a repulsion or to an attraction, via bridging, of the surfaces or vesicles—again strongly depending on the temperature, molecular weight, and concentration of the polyethylene glycol. Low molecular weight polyethylene glycol (such as PEG-400) generally promotes cells or vesicles to adhere (depletion attraction), high molecular weight polyethylene glycol causes them to repel 18.
Target Actions Organism UEctonucleotide pyrophosphatase/phosphodiesterase family member 1 otherHumans UOxidoreductase HTATIP2 Not Available Humans - Absorption
PEG has low toxicity profile with an absorption of less than 0.5% 10.
Topical absorption of PEG occurs and, demonstrates a molecular weight dependence similar to that of PEG given orally. Absorption by this route is likely to be poor 12.
- Volume of distribution
Not Available
- Protein binding
Despite that fact that PEG is believed to be an excellent material to resist protein adsorption, there is a lack of quantitative evidence regarding interactions between proteins and PEG. A study has been performed that suggests that a large number of PEG molecules could associate with protein molecules 3.
- Metabolism
The metabolism of PEG involves the oxidation of the alcohol groups located on the PEG to a carboxylic acid. For example, the diacid and hydroxyl acid metabolites of PEG have been measured in the plasma and urine of burn patients and rabbits and in the bile of cats. In the isolated guinea pig liver and in rat/guinea pig in vitro, PEG has demonstrated to be sulfated. Evidence from experiments with PEG400 suggests that ethylene glycol is not formed as a metabolite of PEG in humans. Negligible amounts of oxalic acid are liberated after the metabolism of PEG 12.
The first phase of metabolism of PEG in mammals is regulated by the enzyme alcohol dehydrogenase. Liver cytochorome P450 enzymes may also play a role in the oxidation of PEG, although the evidence for this is not clear 12. Also, PEG has been shown to be metabolized by sulfotransferase enzymes. Although there is evidence that PEG can be metabolized to various phase 1 and phase 2 metabolites, the toxicology data presented above indicate that these metabolites are of very little toxicological concern. However, metabolism of PEG to the acid metabolite(s) has been implicated in the acidosis and hypercalcemia observed in patients after overdose 12. It is clear that these metabolites can be formed in multiple toxicology species and that the phase 1 metabolites are seen in animals and humans. These data indicate that humans and animals will be exposed to similar metabolites after administration of PEG 12. metabolic clearance of PEG decreases markedly as molecular weight increases. For PEG400, up to 25% of the dose may be metabolized in humans (Schaffer et al., 1950); similar results are also seen in the rabbit 12.
The absorption of PEG by the oral route is molecular weight- dependent. Urinary recovery data for PEG400 indicate that 50 to 60% of PEG with this molecular weight is absorbed from the intestine 12. In the case of PEG-400, up to 25% of the dose may be metabolized in humans. Similar results have also been obtained in studies on the rabbit 12.
- Route of elimination
Human excretion studies have demonstrated that 86% and 96% of PEG1000 and 6000 were excreted in the urine 12 h after intravenous administration. Specific data on PEG-400 are not available 12. In rats, urine PEG undergoes biliary excretion, and this process is depending on molecular weight, with hepatic clearance reaching a minimum at about 50 kDa molecular mass (in mouse)12.
- Half-life
Great than 24h 11.
- Clearance
In mice, lease than <10 % of the administered dose was cleared by the liver 12.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
PEG of different molecular weights by a range of routes has been studied extensively, and has not led to any major toxicities, and signs/symptoms of toxicity that do occur are only observed at a much higher than therapeutic dose 12.
LD50 = 157000 mg/kg, intragastric, guinea pigs MSDS LD50 = 28915 mg/kg, intragastric, mice, rats MSDS LD50 = 9708 mg/kg, intra-abdominal, rats MSDS LD50= 7312 mg/kg, intravenous, rats MSDS
- 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 softwareTenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Polyethylene glycol 400. - 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.- International/Other Brands
- CV single use lubricant eye drops / Good Neighbour Pharmacy Lubricant Eye Drops / Good Sense Lubricant Eye Drops
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Blink Gel Tears Solution / drops 2.5 mg/1mL Ophthalmic Bausch & Lomb Incorporated 2008-05-01 Not applicable US 
Blink Tears Solution / drops 2.5 mg/1mL Ophthalmic Bausch & Lomb Incorporated 2016-03-15 Not applicable US Blink Tears Solution / drops 2.5 mg/1mL Ophthalmic Johnson & Johnson Surgical Vision, Inc. 2008-03-17 2017-08-31 US Blink Tears Solution / drops 2.5 mg/1mL Ophthalmic Holopack Verpackungstechnik GmbH 2016-04-04 Not applicable US Blink Tears Solution / drops 2.5 mg/1mL Ophthalmic Bausch & Lomb Incorporated 2008-02-01 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Advance Relief Eye Drops Polyethylene glycol 400 (1000 mg/100mL) + Dextran 70 (100 mg/100mL) + Povidone (1000 mg/100mL) + Tetrahydrozoline hydrochloride (50 mg/100mL) Solution / drops Ophthalmic WinCo Foods, LLC 2015-01-09 Not applicable US Advanced relief Polyethylene glycol 400 (10 mg/1mL) + Dextran 70 (1 mg/1mL) + Povidone (10 mg/1mL) + Tetrahydrozoline hydrochloride (0.5 mg/1mL) Liquid Ophthalmic American Sales Company 2011-09-07 Not applicable US Advanced Relief Polyethylene glycol 400 (10 mg/1mL) + Dextran 70 (1 mg/1mL) + Povidone (10 mg/1mL) + Tetrahydrozoline hydrochloride (0.5 mg/1mL) Liquid Ophthalmic Kareway Product, Inc. 2018-05-30 Not applicable US Advanced relief Polyethylene glycol 400 (10 mg/1mL) + Dextran 70 (1 mg/1mL) + Povidone (10 mg/1mL) + Tetrahydrozoline hydrochloride (0.5 mg/1mL) Liquid Ophthalmic Samchundang Pharm. Co., Ltd. 2010-08-29 Not applicable US Advanced Relief Eye Drops Polyethylene glycol 400 (1 % w/v) + Dextran 70 (0.1 % w/v) + Povidone (1 % w/v) + Tetrahydrozoline hydrochloride (0.05 % w/v) Solution Ophthalmic Teva Italia S.R.L. 2010-08-30 Not applicable Canada 
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Dark Spot Corrector Polyethylene glycol 400 (.3 mg/15mg) Cream Topical Lange SAS 2012-09-17 Not applicable US Lightening Day Cream Polyethylene glycol 400 (2.5 mg/50mg) Cream Topical Lange SAS 2012-07-18 Not applicable US Peg Polyethylene glycol 400 (45 g/100g) + Polyethylene glycol (55 g/100g) Cream Topical Biocellerex, Inc. 2015-07-14 2016-01-05 US Sysfol Eye Drops Polyethylene glycol 400 (0.4 g/100mL) + Propylene glycol (0.3 g/100mL) Liquid Ophthalmic Unimed Pharmaceuticals, Inc. 2023-04-20 Not applicable US Sysfol Eye Drops Polyethylene glycol 400 (0.4 g/100mL) + Propylene glycol (0.3 g/100mL) Liquid Ophthalmic Unimed Pharmaceuticals, Inc. 2023-04-20 Not applicable US
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- B697894SGQ
- CAS number
- 25322-68-3
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Basit AW, Newton JM, Short MD, Waddington WA, Ell PJ, Lacey LF: The effect of polyethylene glycol 400 on gastrointestinal transit: implications for the formulation of poorly-water soluble drugs. Pharm Res. 2001 Aug;18(8):1146-50. [Article]
- Foulks GN: Clinical evaluation of the efficacy of PEG/PG lubricant eye drops with gelling agent (HP-Guar) for the relief of the signs and symptoms of dry eye disease: a review. Drugs Today (Barc). 2007 Dec;43(12):887-96. doi: 10.1358/dot.2007.43.12.1162080. [Article]
- Wu J, Wang Z, Lin W, Chen S: Investigation of the interaction between poly(ethylene glycol) and protein molecules using low field nuclear magnetic resonance. Acta Biomater. 2013 May;9(5):6414-20. doi: 10.1016/j.actbio.2013.01.006. Epub 2013 Jan 11. [Article]
- Polyethylene glyco [Link]
- SIGMA-ALDRICH PEG 400 [Link]
- Polyethylene glycol 400 (PEG400) affects the systemic exposure of oral drugs based on multiple mechanisms: taking berberine as an example [Link]
- Polyethylene glycol [Link]
- Polyethylene Glycol [Link]
- Safety Evaluation of Polyethylene Glycol (PEG) Compounds for Cosmetic Use [Link]
- PEG-400 [Link]
- Safety of Total Daily Doses of Polyethylene Glycol (PEG) 400 Administered Orally to Healthy Male Human Subjects [Link]
- PEGylated Proteins: Evaluation of Their Safety in the Absence of Definitive Metabolism Studies [Link]
- The Absorption and Excretion of a Liquid Polyethylene Glycol [Link]
- Polyethylene Glycol 400 [Link]
- Systane Mechanism of Action [Link]
- Ocular lubricants: what is the best choice? [Link]
- Impact of Surface Polyethylene Glycol (PEG) Density on Biodegradable Nanoparticle Transport in Mucus ex vivo and Distribution in vivo [Link]
- The different faces of poly(ethylene glycol) [Link]
- External Links
- MSDS
- Download (229 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 dataNot Available Completed Not Available Dry Eye Syndrome (DES) 2 somestatus stop reason just information to hide Not Available Completed Other Dry Eye Syndrome (DES) 1 somestatus stop reason just information to hide Not Available Completed Prevention Cataracts 1 somestatus stop reason just information to hide Not Available Completed Treatment Dry Eye Syndrome (DES) 5 somestatus stop reason just information to hide Not Available Completed Treatment Dry Eyes 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Liquid Ophthalmic Solution / drops Ophthalmic 2.5 mg/1mL Cream Dental 6 mg/60mg Cream Topical .3 mg/15mg Solution, gel forming / drops Ophthalmic Solution / drops Ophthalmic Solution / drops Ophthalmic 1 g/100mL Solution Ophthalmic Solution Conjunctival; Ophthalmic Cream Topical 2.5 mg/50mg Cream Topical Gel Ophthalmic Kit; solution Ophthalmic Solution Ophthalmic; Topical Kit; solution / drops Ophthalmic Solution / drops Ophthalmic 10 mg/1mL Liquid Topical Liquid Ophthalmic 1 % Solution Conjunctival; Topical Enema - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source boiling point (°C) >250 MSDS water solubility 100 % soluble 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
- Other
- General Function
- Nucleotide pyrophosphatase that generates diphosphate (PPi) and functions in bone mineralization and soft tissue calcification by regulating pyrophosphate levels (By similarity). PPi inhibits bone mineralization and soft tissue calcification by binding to nascent hydroxyapatite crystals, thereby preventing further growth of these crystals (PubMed:11004006). Preferentially hydrolyzes ATP, but can also hydrolyze other nucleoside 5' triphosphates such as GTP, CTP and UTP to their corresponding monophosphates with release of pyrophosphate, as well as diadenosine polyphosphates, and also 3',5'-cAMP to AMP (PubMed:25344812, PubMed:27467858, PubMed:28011303, PubMed:35147247, PubMed:8001561). May also be involved in the regulation of the availability of nucleotide sugars in the endoplasmic reticulum and Golgi, and the regulation of purinergic signaling (PubMed:27467858, PubMed:8001561). Inhibits ectopic joint calcification and maintains articular chondrocytes by repressing hedgehog signaling; it is however unclear whether hedgehog inhibition is direct or indirect (By similarity). Appears to modulate insulin sensitivity and function (PubMed:10615944). Also involved in melanogenesis (PubMed:28964717). Also able to hydrolyze 2',3'-cGAMP (cyclic GMP-AMP), a second messenger that activates TMEM173/STING and triggers type-I interferon production (PubMed:25344812). 2',3'-cGAMP degradation takes place in the lumen or extracellular space, and not in the cytosol where it is produced; the role of 2',3'-cGAMP hydrolysis is therefore unclear (PubMed:25344812). Not able to hydrolyze the 2',3'-cGAMP linkage isomer 3'-3'-cGAMP (PubMed:25344812)
- Specific Function
- 3',5'-cyclic-AMP phosphodiesterase activity
- Gene Name
- ENPP1
- Uniprot ID
- P22413
- Uniprot Name
- Ectonucleotide pyrophosphatase/phosphodiesterase family member 1
- Molecular Weight
- 104923.58 Da
References
- Impact of Surface Polyethylene Glycol (PEG) Density on Biodegradable Nanoparticle Transport in Mucus ex vivo and Distribution in vivo [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Oxidoreductase required for tumor suppression. NADPH-bound form inhibits nuclear import by competing with nuclear import substrates for binding to a subset of nuclear transport receptors. May act as a redox sensor linked to transcription through regulation of nuclear import. Isoform 1 is a metastasis suppressor with proapoptotic as well as antiangiogenic properties. Isoform 2 has an antiapoptotic effect
- Specific Function
- oxidoreductase activity
- Gene Name
- HTATIP2
- Uniprot ID
- Q9BUP3
- Uniprot Name
- Oxidoreductase HTATIP2
- Molecular Weight
- 27048.765 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of fatty acids and their oxygenated derivatives (oxylipins) (PubMed:10553002, PubMed:10660572, PubMed:15611369, PubMed:1739747, PubMed:7679927, PubMed:8914854). 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) (PubMed:10553002, PubMed:10660572, PubMed:15611369, PubMed:1739747, PubMed:7679927, PubMed:8914854). Catalyzes predominantly the oxidation of the terminal carbon (omega-oxidation) of saturated and unsaturated fatty acids, the catalytic efficiency decreasing in the following order: dodecanoic > tetradecanoic > (9Z)-octadecenoic > (9Z,12Z)-octadecadienoic > hexadecanoic acid (PubMed:10553002, PubMed:10660572). Acts as a major omega-hydroxylase for dodecanoic (lauric) acid in liver (PubMed:15611369, PubMed:1739747, PubMed:7679927, PubMed:8914854). Participates in omega-hydroxylation of (5Z,8Z,11Z,14Z)-eicosatetraenoic acid (arachidonate) to 20-hydroxyeicosatetraenoic acid (20-HETE), a signaling molecule acting both as vasoconstrictive and natriuretic with overall effect on arterial blood pressure (PubMed:10620324, PubMed:10660572, PubMed:15611369). Can also catalyze the oxidation of the penultimate carbon (omega-1 oxidation) of fatty acids with lower efficiency (PubMed:7679927). May contribute to the degradation of saturated very long-chain fatty acids (VLCFAs) such as docosanoic acid, by catalyzing successive omega-oxidations to the corresponding dicarboxylic acid, thereby initiating chain shortening (PubMed:18182499). Omega-hydroxylates (9R,10S)-epoxy-octadecanoate stereoisomer (PubMed:15145985). Plays a minor role in omega-oxidation of long-chain 3-hydroxy fatty acids (PubMed:18065749). Has little activity toward prostaglandins A1 and E1 (PubMed:7679927)
- Specific Function
- alkane 1-monooxygenase activity
- Gene Name
- CYP4A11
- Uniprot ID
- Q02928
- Uniprot Name
- Cytochrome P450 4A11
- Molecular Weight
- 59347.31 Da
References
- PEGylated Proteins: Evaluation of Their Safety in the Absence of Definitive Metabolism Studies [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the oxidation of long-chain primary alcohols and the oxidation of S-(hydroxymethyl) glutathione (PubMed:8460164). Also oxidizes long chain omega-hydroxy fatty acids, such as 20-HETE, producing both the intermediate aldehyde, 20-oxoarachidonate and the end product, a dicarboxylic acid, (5Z,8Z,11Z,14Z)-eicosatetraenedioate (PubMed:16081420). Class-III ADH is remarkably ineffective in oxidizing ethanol (PubMed:8460164). Required for clearance of cellular formaldehyde, a cytotoxic and carcinogenic metabolite that induces DNA damage (PubMed:33355142). Also acts as a S-nitroso-glutathione reductase by catalyzing the NADH-dependent reduction of S-nitrosoglutathione, thereby regulating protein S-nitrosylation (By similarity)
- Specific Function
- alcohol dehydrogenase (NAD+) activity, zinc-dependent
- Gene Name
- ADH5
- Uniprot ID
- P11766
- Uniprot Name
- Alcohol dehydrogenase class-3
- Molecular Weight
- 39723.945 Da
References
- PEGylated Proteins: Evaluation of Their Safety in the Absence of Definitive Metabolism Studies [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of a wide variety of acceptor molecules bearing a hydroxyl or an amine groupe. Sulfonation increases the water solubility of most compounds, and therefore their renal excretion, but it can also result in bioactivation to form active metabolites. Displays broad substrate specificity for small phenolic compounds. Plays an important role in the sulfonation of endogenous molecules such as steroid hormones and 3,3'-diiodothyronin (PubMed:10199779, PubMed:12471039, PubMed:16221673, PubMed:21723874, PubMed:22069470, PubMed:7834621). Mediates the sulfate conjugation of a variety of xenobiotics, including the drugs acetaminophen and minoxidil (By similarity). Mediates also the metabolic activation of carcinogenic N-hydroxyarylamines leading to highly reactive intermediates capable of forming DNA adducts, potentially resulting in mutagenesis (PubMed:7834621). May play a role in gut microbiota-host metabolic interaction. O-sulfonates 4-ethylphenol (4-EP), a dietary tyrosine-derived metabolite produced by gut bacteria. The product 4-EPS crosses the blood-brain barrier and may negatively regulate oligodendrocyte maturation and myelination, affecting the functional connectivity of different brain regions associated with the limbic system
- Specific Function
- 3'-phosphoadenosine 5'-phosphosulfate binding
- Gene Name
- SULT1A1
- Uniprot ID
- P50225
- Uniprot Name
- Sulfotransferase 1A1
- Molecular Weight
- 34165.13 Da
References
- PEGylated Proteins: Evaluation of Their Safety in the Absence of Definitive Metabolism Studies [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
- Johnson BM, Charman WN, Porter CJ: An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine. AAPS PharmSci. 2002;4(4):E40. doi: 10.1208/ps040440. [Article]
Drug created at December 03, 2015 16:51 / Updated at November 07, 2024 20:14