Ursodeoxycholic acid 25mg/5ml oral suspension
Prescription only
Requires a prescription from a doctor or prescriber
Oral suspension
25mg/5ml
Oral
Drugs affecting intestinal secretions
Active ingredients:
Ursodeoxycholic acid
No active safety alerts
Official documents, adverse reaction reporting, and safety monitoring
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Official medicine documents
Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Ursodeoxycholic acid
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
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Suspected adverse reactions reported for Ursodeoxycholic acid
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
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WHO defined daily dose (DDD)
750 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Show details
Ursodeoxycholic acid 500mg capsules
Capsule
500mg
Same therapeutic group
Obeticholic acid 5mg tablets
Tablet
5mg
Same therapeutic group
Obeticholic acid 10mg tablets
Tablet
10mg
Same therapeutic group
Ursodeoxycholic acid 250mg tablets
Tablet
250mg
Same therapeutic group
Cholic acid 50mg capsules
Capsule
50mg
Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Clinical guidelines and formulary information
British National Formulary
Ursodeoxycholic acid
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(4)
Obeticholic acid for treating primary biliary cholangitis (TA443)
TA443
Technology appraisal
Updated Apr 2017Cystic fibrosis: diagnosis and management (NG78)
NG78
NICE guideline
Updated Oct 2017Odevixibat for treating progressive familial intrahepatic cholestasis (HST17)
HST17
Highly specialised technology
Updated Feb 2022Elafibranor for previously treated primary biliary cholangitis (TA1016)
TA1016
Technology appraisal
Updated Nov 2024Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Pharmacy stock checkers
Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
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These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
3.5 to 5.8 days
Mechanism
Endogenous hydrophobic bile acids such as deoxycholic acid and chenodeoxycholic acid can exert hepatotoxic effects.
Food interactions
1 warning
Human targets
4 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
5%
Normally, endogenous ursodeoxycholic acid constitutes a minor fraction (about 5%) of the total human bile acid pool.…
Half-life
3.5 to 5.8 days
The estimated half-life ranges from 3.5 to 5.8 days.
[A256277][A256678]
[A256277][A256678]
Protein binding
70%
Unconjugated ursodeoxycholic acid is at least 70% bound to plasma proteins in health individuals.…
Volume of distribution
The volume of distribution of ursodeoxycholic acid (UDCA) has not been determined; however, it is expected to be small since UDCA is mostly distributed…
Metabolism
Upon administration, ursodeoxycholic acid (UDCA) enters the portal vein and into the liver, where it undergoes conjugation with glycine or taurine.
[A256277]…
[A256277]…
Elimination
1%
Ursodeoxycholic acid is excreted primarily in the feces. Renal elimination is a minor elimination pathway.…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Ursodeoxycholic acid (UDCA), also known as ursodiol, is a naturally-occurring bile acid that constitutes a minor fraction of the human bile acid pool.[A256272][A256277] UDCA has been used to treat liver disease for decades: its first use in traditional medicine dates back more than a hundred years.[A256267][A256463] UDCA was first characterized in the bile of the Chinese black bear and is formed by 7b-epimerization of [chenodeoxycholic acid], which is a primary bile acid.[A256272] Due to its hydrophilicity, UDCA is less toxic than [cholic acid] or [chenodeoxycholic acid].[A256272]
UDCA was first approved by the FDA in 1987 for dissolution of gallstones and for primary biliary cirrhosis in 1996.[A256272] UDCA works by replacing the hydrophobic or more toxic bile acids from the bile acid pool.[A256272]
UDCA was first approved by the FDA in 1987 for dissolution of gallstones and for primary biliary cirrhosis in 1996.[A256272] UDCA works by replacing the hydrophobic or more toxic bile acids from the bile acid pool.[A256272]
Properties:
solid
Avg. mass: 392.57 Da
DrugBank indication
Ursodeoxycholic acid is indicated for the treatment of patients with primary biliary cholangitis.
[L44627]
It is used for the short-term treatment of radiolucent, noncalcified gallbladder stones in patients selected for elective cholecystectomy. It is also used to prevent gallstone formation in obese patients experiencing rapid weight loss.
[L44793]
[L44627]
It is used for the short-term treatment of radiolucent, noncalcified gallbladder stones in patients selected for elective cholecystectomy. It is also used to prevent gallstone formation in obese patients experiencing rapid weight loss.
[L44793]
Also known as(125)
(3alpha,5beta,7beta)-3,7-dihydroxycholan-24-oic acid
(3α,5β,7β)-3,7-dihydroxycholan-24-oic acid
3alpha,7beta-Dihydroxy-5beta-cholan-24-oic acid
Acide ursodesoxycholique
Acido ursodeossicolico
Acido ursodeoxicolico
Acidum ursodeoxycholicum
UDCA
Dosage forms(59)
Capsule (Oral) — 225 MG
Capsule (Oral) — 450 MG
Capsule, extended release (Oral) — 450 MG
Capsule, delayed release (Oral) — 225 MG
Capsule, delayed release (Oral) — 450 MG
Paste (Dental)
Capsule, extended release (Oral)
Capsule (Oral)
Molecular properties(19)
Drug interactions(262)
Known interactions with other medications. Always consult a healthcare professional.
The risk or severity of bleeding and bruising can be increased when Lepirudin is combined with Ursodeoxycholic acid.
Bivalirudin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Bivalirudin is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Alteplase is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Urokinase is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Reteplase is combined with Ursodeoxycholic acid.
Anistreplase
Unknown severity
The risk or severity of bleeding and bruising can be increased when Anistreplase is combined with Ursodeoxycholic acid.
Tenecteplase
Unknown severity
The risk or severity of bleeding and bruising can be increased when Tenecteplase is combined with Ursodeoxycholic acid.
Drotrecogin alfa
Unknown severity
The risk or severity of bleeding and bruising can be increased when Drotrecogin alfa is combined with Ursodeoxycholic acid.
Streptokinase
Unknown severity
The risk or severity of bleeding and bruising can be increased when Streptokinase is combined with Ursodeoxycholic acid.
Dicoumarol
Unknown severity
The risk or severity of bleeding and bruising can be increased when Dicoumarol is combined with Ursodeoxycholic acid.
Argatroban
Unknown severity
The risk or severity of bleeding and bruising can be increased when Argatroban is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Ardeparin is combined with Ursodeoxycholic acid.
Phenindione
Unknown severity
The risk or severity of bleeding and bruising can be increased when Phenindione is combined with Ursodeoxycholic acid.
Fondaparinux
Unknown severity
The risk or severity of bleeding and bruising can be increased when Fondaparinux is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Warfarin is combined with Ursodeoxycholic acid.
Pentosan polysulfate
Unknown severity
The risk or severity of bleeding and bruising can be increased when Pentosan polysulfate is combined with Ursodeoxycholic acid.
Phenprocoumon
Unknown severity
The risk or severity of bleeding and bruising can be increased when Phenprocoumon is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Heparin is combined with Ursodeoxycholic acid.
Enoxaparin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Ursodeoxycholic acid.
Acenocoumarol
Unknown severity
The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Ursodeoxycholic acid.
4-hydroxycoumarin
Unknown severity
The risk or severity of bleeding and bruising can be increased when 4-hydroxycoumarin is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Coumarin is combined with Ursodeoxycholic acid.
Ximelagatran
Unknown severity
The risk or severity of bleeding and bruising can be increased when Ximelagatran is combined with Ursodeoxycholic acid.
Desmoteplase
Unknown severity
The risk or severity of bleeding and bruising can be increased when Desmoteplase is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Ancrod is combined with Ursodeoxycholic acid.
Rivaroxaban
Unknown severity
The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Ursodeoxycholic acid.
Sulodexide
Unknown severity
The risk or severity of bleeding and bruising can be increased when Sulodexide is combined with Ursodeoxycholic acid.
Semuloparin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Semuloparin is combined with Ursodeoxycholic acid.
Idraparinux
Unknown severity
The risk or severity of bleeding and bruising can be increased when Idraparinux is combined with Ursodeoxycholic acid.
Astaxanthin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Astaxanthin is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Ursodeoxycholic acid.
Otamixaban
Unknown severity
The risk or severity of bleeding and bruising can be increased when Otamixaban is combined with Ursodeoxycholic acid.
Amediplase
Unknown severity
The risk or severity of bleeding and bruising can be increased when Amediplase is combined with Ursodeoxycholic acid.
Dabigatran etexilate
Unknown severity
The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Ursodeoxycholic acid.
Danaparoid
Unknown severity
The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Ursodeoxycholic acid.
Dalteparin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Dalteparin is combined with Ursodeoxycholic acid.
Tinzaparin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Tinzaparin is combined with Ursodeoxycholic acid.
(R)-warfarin
Unknown severity
The risk or severity of bleeding and bruising can be increased when (R)-warfarin is combined with Ursodeoxycholic acid.
Ethyl biscoumacetate
Unknown severity
The risk or severity of bleeding and bruising can be increased when Ethyl biscoumacetate is combined with Ursodeoxycholic acid.
Nadroparin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Nadroparin is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Ditazole is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Ursodeoxycholic acid.
Sodium citrate
Unknown severity
The risk or severity of bleeding and bruising can be increased when Sodium citrate is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Dextran is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Bemiparin is combined with Ursodeoxycholic acid.
Parnaparin
Unknown severity
The risk or severity of bleeding and bruising can be increased when Parnaparin is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Desirudin is combined with Ursodeoxycholic acid.
Antithrombin Alfa
Unknown severity
The risk or severity of bleeding and bruising can be increased when Antithrombin Alfa is combined with Ursodeoxycholic acid.
The risk or severity of bleeding and bruising can be increased when Protein C is combined with Ursodeoxycholic acid.
Antithrombin III human
Unknown severity
The risk or severity of bleeding and bruising can be increased when Antithrombin III human is combined with Ursodeoxycholic acid.
Showing 50 of 262 interactions
Food & lifestyle interactions
Take With Food
Take with food.
Toxicity & overdose
The oral LD50 in rats is >4600-5000 mg/kg.
[L44752][L44793]
It is over 7500 mg/kg for mice.
[L44793]
Ursodeoxycholic acid (UDCA) is associated with rare hepatotoxicities, such as jaundice, worsening pre-existing liver diseases, and hepatitis.
[A256272][A256277]
There have been no reports of accidental or intentional overdosage with UDCA. A single oral dose of UDCA at 1.5 g/kg was lethal in hamsters. Single oral doses of UDCA at 10 g/kg in mice and dogs and 5 g/kg in rats were not lethal.
Symptoms of acute toxicity were salivation and vomiting in dogs, while ataxia, dyspnea, ptosis, agonal convulsions and coma were observed in hamsters.
[L44627]
[L44752][L44793]
It is over 7500 mg/kg for mice.
[L44793]
Ursodeoxycholic acid (UDCA) is associated with rare hepatotoxicities, such as jaundice, worsening pre-existing liver diseases, and hepatitis.
[A256272][A256277]
There have been no reports of accidental or intentional overdosage with UDCA. A single oral dose of UDCA at 1.5 g/kg was lethal in hamsters. Single oral doses of UDCA at 10 g/kg in mice and dogs and 5 g/kg in rats were not lethal.
Symptoms of acute toxicity were salivation and vomiting in dogs, while ataxia, dyspnea, ptosis, agonal convulsions and coma were observed in hamsters.
[L44627]
How it works
Mechanism of action
Endogenous hydrophobic bile acids such as deoxycholic acid and chenodeoxycholic acid can exert hepatotoxic effects. Ursodeoxycholic acid is a hydrophilic bile acid that mediates its biological effects via several mechanisms. Ursodeoxycholic acid (UDCA) protects hepatocytes and cholangiocytes from bile acid-induced damage, such as reactive oxygen species (ROS)-induced inflammation and mitochondrial dysfunction.[A256267] UDCA was shown to reserve hepatocyte cell structures and stimulate anti-apoptotic pathways.[A256267][A256272][A256458][A256463] It was also shown to prevent the production of ROS by Kupffer cells and resident macrophages in the liver, thus attenuating oxidative stress in the liver.[A256267]
UDCA can also change the hydrophobicity index of the bile acid pool: following oral administration, UDCA forms a major fraction of the human bile acid pool and competitively displaces the hydrophobic or more toxic bile acids.[A256272][A256267] It increases the absorption of hydrophilic bile acids.[A256267] There are several proposed mechanisms of choleretic actions of UDCA: UDCA increases intracellular calcium levels, stimulating transport proteins and vesicular exocytosis in cholestatic hepatocytes.[A256267] UDCA may also upregulate the expression of membrane transport proteins like the chloride-bicarbonate anion exchanger (AE2),[A256267][A256458] which is involved in biliary secretion and is often observed to be defective in primary biliary cholangitis.[A256448] In rats, UDCA reduced hepatic expression of major histocompatibility complex (MHC) class I antigens, suggesting immunomodulating effects.[A256267] UDCA acts as a partial agonist at the bile acid receptor, also known as the farnesoid X receptor (FXR), and has negligible effects on cholesterol and lipid synthesis.[A256272]
UDCA can also change the hydrophobicity index of the bile acid pool: following oral administration, UDCA forms a major fraction of the human bile acid pool and competitively displaces the hydrophobic or more toxic bile acids.[A256272][A256267] It increases the absorption of hydrophilic bile acids.[A256267] There are several proposed mechanisms of choleretic actions of UDCA: UDCA increases intracellular calcium levels, stimulating transport proteins and vesicular exocytosis in cholestatic hepatocytes.[A256267] UDCA may also upregulate the expression of membrane transport proteins like the chloride-bicarbonate anion exchanger (AE2),[A256267][A256458] which is involved in biliary secretion and is often observed to be defective in primary biliary cholangitis.[A256448] In rats, UDCA reduced hepatic expression of major histocompatibility complex (MHC) class I antigens, suggesting immunomodulating effects.[A256267] UDCA acts as a partial agonist at the bile acid receptor, also known as the farnesoid X receptor (FXR), and has negligible effects on cholesterol and lipid synthesis.[A256272]
Pharmacodynamics
Ursodeoxycholic acid (UDCA) is a secondary bile acid with cytoprotectant, immunomodulating, and choleretic effects. It reduces the cholesterol fraction of biliary lipids.[A256267]
UDCA inhibits the absorption of cholesterol in the intestine and the secretion of cholesterol into bile, decreasing biliary cholesterol saturation.[A256267] UDCA increases bile acid flow and promotes the secretion of bile acids.[A256267][A256277][A256463]
UDCA inhibits the absorption of cholesterol in the intestine and the secretion of cholesterol into bile, decreasing biliary cholesterol saturation.[A256267] UDCA increases bile acid flow and promotes the secretion of bile acids.[A256267][A256277][A256463]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Normally, endogenous ursodeoxycholic acid constitutes a minor fraction (about 5%) of the total human bile acid pool. Following oral administration, the majority of ursodiol is absorbed by passive diffusion, and its absorption is incomplete. Once absorbed, ursodiol undergoes hepatic extraction to about 50% in the absence of liver disease.
As the severity of liver disease increases, the extent of extraction decreases. During chronic administration of ursodiol, it becomes a major biliary and plasma bile acid. At a chronic dose of 13 to 15 mg/kg/day, ursodiol constitutes 30-50% of biliary and plasma bile acids.
[L44627]
As the severity of liver disease increases, the extent of extraction decreases. During chronic administration of ursodiol, it becomes a major biliary and plasma bile acid. At a chronic dose of 13 to 15 mg/kg/day, ursodiol constitutes 30-50% of biliary and plasma bile acids.
[L44627]
Half-life
The estimated half-life ranges from 3.5 to 5.8 days.
[A256277][A256678]
[A256277][A256678]
Protein binding
Unconjugated ursodeoxycholic acid is at least 70% bound to plasma proteins in health individuals. There is no information regarding the protein binding of conjugated ursodeoxycholic acid.
[L44627]
[L44627]
Volume of distribution
The volume of distribution of ursodeoxycholic acid (UDCA) has not been determined; however, it is expected to be small since UDCA is mostly distributed in the bile in the gallbladder and small intestines.
[A256277][L44627]
[A256277][L44627]
Metabolism
Upon administration, ursodeoxycholic acid (UDCA) enters the portal vein and into the liver, where it undergoes conjugation with glycine or taurine.
[A256277]
UDCA is also decreased into bile. Glycine or taurine conjugates are absorbed in the small intestine via passive and active mechanisms. The conjugates can also be deconjugated in the ileum by intestinal enzymes, leading to the formation of free UDCA that can be reabsorbed and re-conjugated in the liver.
[L44627]
Nonabsorbed UDCA passes into the colon, where it undergoes 7-dehydroxylation by intestinal bacteria to lithocholic acid.
[A256728]
Some UDCA is epimerized to [chenodeoxycholic acid] via a 7-oxo intermediate.
Chenodeoxycholic acid also undergoes 7-dehydroxylation to form lithocholic acid. These metabolites are poorly soluble and excreted in the feces. A small portion of lithocholic acid is reabsorbed, conjugated in the liver with glycine or taurine, and sulfated at the 3 position.
The resulting sulfated lithocholic acid conjugates are excreted in bile and then lost in feces.
[L44627]
[A256277]
UDCA is also decreased into bile. Glycine or taurine conjugates are absorbed in the small intestine via passive and active mechanisms. The conjugates can also be deconjugated in the ileum by intestinal enzymes, leading to the formation of free UDCA that can be reabsorbed and re-conjugated in the liver.
[L44627]
Nonabsorbed UDCA passes into the colon, where it undergoes 7-dehydroxylation by intestinal bacteria to lithocholic acid.
[A256728]
Some UDCA is epimerized to [chenodeoxycholic acid] via a 7-oxo intermediate.
Chenodeoxycholic acid also undergoes 7-dehydroxylation to form lithocholic acid. These metabolites are poorly soluble and excreted in the feces. A small portion of lithocholic acid is reabsorbed, conjugated in the liver with glycine or taurine, and sulfated at the 3 position.
The resulting sulfated lithocholic acid conjugates are excreted in bile and then lost in feces.
[L44627]
Route of elimination
Ursodeoxycholic acid is excreted primarily in the feces. Renal elimination is a minor elimination pathway. With treatment, urinary excretion increases but remains less than 1% except in severe cholestatic liver disease.
[A256678][L44627]
[A256678][L44627]
Drug targets(4)
Proteins and enzymes this drug interacts with in the body
Aldo-keto reductase family 1 member C2
AKR1C2
inhibitor
Specific functionaldose reductase (NADPH) activity
Cellular location
Cytoplasm, cytosol
General function & pharmacology
Cytosolic aldo-keto reductase that catalyzes the NADH and NADPH-dependent reduction of ketosteroids to hydroxysteroids .
PMID:19218247
Most probably acts as a reductase in vivo since the oxidase activity measured in vitro is inhibited by physiological concentrations of NADPH .
PMID:14672942
Displays a broad positional specificity acting on positions 3, 17 and 20 of steroids and regulates the metabolism of hormones like estrogens and androgens .
PMID:10998348
Works in concert with the 5-alpha/5-beta-steroid reductases to convert steroid hormones into the 3-alpha/5-alpha and 3-alpha/5-beta-tetrahydrosteroids. Catalyzes the inactivation of the most potent androgen 5-alpha-dihydrotestosterone (5-alpha-DHT) to 5-alpha-androstane-3-alpha,17-beta-diol (3-alpha-diol) .
PMID:15929998 PMID:17034817 PMID:17442338 PMID:8573067
Also specifically able to produce 17beta-hydroxy-5alpha-androstan-3-one/5alphaDHT .
PMID:10998348
May also reduce conjugated steroids such as 5alpha-dihydrotestosterone sulfate .
PMID:19218247
Displays affinity for bile acids PMID:8486699
PMID:19218247
Most probably acts as a reductase in vivo since the oxidase activity measured in vitro is inhibited by physiological concentrations of NADPH .
PMID:14672942
Displays a broad positional specificity acting on positions 3, 17 and 20 of steroids and regulates the metabolism of hormones like estrogens and androgens .
PMID:10998348
Works in concert with the 5-alpha/5-beta-steroid reductases to convert steroid hormones into the 3-alpha/5-alpha and 3-alpha/5-beta-tetrahydrosteroids. Catalyzes the inactivation of the most potent androgen 5-alpha-dihydrotestosterone (5-alpha-DHT) to 5-alpha-androstane-3-alpha,17-beta-diol (3-alpha-diol) .
PMID:15929998 PMID:17034817 PMID:17442338 PMID:8573067
Also specifically able to produce 17beta-hydroxy-5alpha-androstan-3-one/5alphaDHT .
PMID:10998348
May also reduce conjugated steroids such as 5alpha-dihydrotestosterone sulfate .
PMID:19218247
Displays affinity for bile acids PMID:8486699
Biliverdin reductase A
BLVRA
activator
Specific functionbiliberdin reductase (NAD+) activity
Cellular location
Cytoplasm, cytosol
General function & pharmacology
Reduces the gamma-methene bridge of the open tetrapyrrole, biliverdin IXalpha, to bilirubin with the concomitant oxidation of a NADH or NADPH cofactor .
PMID:10858451 PMID:7929092 PMID:8424666 PMID:8631357
Does not reduce bilirubin IXbeta .
PMID:10858451
Uses the reactants NADH or NADPH depending on the pH; NADH is used at the acidic pH range (6-6.9) and NADPH at the alkaline range (8.5-8.7) .
PMID:7929092 PMID:8424666 PMID:8631357
NADPH, however, is the probable reactant in biological systems PMID:7929092
PMID:10858451 PMID:7929092 PMID:8424666 PMID:8631357
Does not reduce bilirubin IXbeta .
PMID:10858451
Uses the reactants NADH or NADPH depending on the pH; NADH is used at the acidic pH range (6-6.9) and NADPH at the alkaline range (8.5-8.7) .
PMID:7929092 PMID:8424666 PMID:8631357
NADPH, however, is the probable reactant in biological systems PMID:7929092
Solute carrier family 23 member 2
SLC23A2
activator
Specific functionL-ascorbate
Cellular location
Cell membrane
General function & pharmacology
Sodium/ascorbate cotransporter .
PMID:10471399 PMID:10556521
Mediates electrogenic uptake of vitamin C, with a stoichiometry of 2 Na(+) for each ascorbate PMID:10471399
PMID:10471399 PMID:10556521
Mediates electrogenic uptake of vitamin C, with a stoichiometry of 2 Na(+) for each ascorbate PMID:10471399
Bile acid receptor
NR1H4
partial agonist
Specific functionbile acid binding
Cellular location
Nucleus
General function & pharmacology
Ligand-activated transcription factor. Receptor for bile acids (BAs) such as chenodeoxycholic acid (CDCA), lithocholic acid, deoxycholic acid (DCA) and allocholic acid (ACA). Plays a essential role in BA homeostasis through the regulation of genes involved in BA synthesis, conjugation and enterohepatic circulation.
Also regulates lipid and glucose homeostasis and is involved innate immune response .
PMID:10334992 PMID:10334993 PMID:21383957 PMID:22820415
The FXR-RXR heterodimer binds predominantly to farnesoid X receptor response elements (FXREs) containing two inverted repeats of the consensus sequence 5'-AGGTCA-3' in which the monomers are spaced by 1 nucleotide (IR-1) but also to tandem repeat DR1 sites with lower affinity, and can be activated by either FXR or RXR-specific ligands. It is proposed that monomeric nuclear receptors such as NR5A2/LRH-1 bound to coregulatory nuclear responsive element (NRE) halfsites located in close proximity to FXREs modulate transcriptional activity (By similarity). In the liver activates transcription of the corepressor NR0B2 thereby indirectly inhibiting CYP7A1 and CYP8B1 (involved in BA synthesis) implicating at least in part histone demethylase KDM1A resulting in epigenomic repression, and SLC10A1/NTCP (involved in hepatic uptake of conjugated BAs).
Activates transcription of the repressor MAFG (involved in regulation of BA synthesis) (By similarity). Activates transcription of SLC27A5/BACS and BAAT (involved in BA conjugation), ABCB11/BSEP (involved in bile salt export) by directly recruiting histone methyltransferase CARM1, and ABCC2/MRP2 (involved in secretion of conjugated BAs) and ABCB4 (involved in secretion of phosphatidylcholine in the small intestine) .
PMID:12754200 PMID:15471871 PMID:17895379
Activates transcription of SLC27A5/BACS and BAAT (involved in BA conjugation), ABCB11/BSEP (involved in bile salt export) by directly recruiting histone methyltransferase CARM1, and ABCC2/MRP2 (involved in secretion of conjugated BAs) and ABCB4 (involved in secretion of phosphatidylcholine in the small intestine) .
PMID:10514450 PMID:15239098 PMID:16269519
In the intestine activates FGF19 expression and secretion leading to hepatic CYP7A1 repression .
PMID:12815072 PMID:19085950
The function also involves the coordinated induction of hepatic KLB/beta-klotho expression (By similarity). Regulates transcription of liver UGT2B4 and SULT2A1 involved in BA detoxification; binding to the UGT2B4 promoter seems to imply a monomeric transactivation independent of RXRA .
PMID:12806625 PMID:16946559
Modulates lipid homeostasis by activating liver NR0B2/SHP-mediated repression of SREBF1 (involved in de novo lipogenesis), expression of PLTP (involved in HDL formation), SCARB1 (involved in HDL hepatic uptake), APOE, APOC1, APOC4, PPARA (involved in beta-oxidation of fatty acids), VLDLR and SDC1 (involved in the hepatic uptake of LDL and IDL remnants), and inhibiting expression of MTTP (involved in VLDL assembly .
PMID:12554753 PMID:12660231 PMID:15337761
Increases expression of APOC2 (promoting lipoprotein lipase activity implicated in triglyceride clearance) .
PMID:11579204
Transrepresses APOA1 involving a monomeric competition with NR2A1 for binding to a DR1 element .
PMID:11927623 PMID:21804189
Also reduces triglyceride clearance by inhibiting expression of ANGPTL3 and APOC3 (both involved in inhibition of lipoprotein lipase) .
PMID:12891557
Involved in glucose homeostasis by modulating hepatic gluconeogenesis through activation of NR0B2/SHP-mediated repression of respective genes.
Modulates glycogen synthesis (inducing phosphorylation of glycogen synthase kinase-3) (By similarity). Modulates glucose-stimulated insulin secretion and is involved in insulin resistance .
PMID:20447400
Involved in intestinal innate immunity. Plays a role in protecting the distal small intestine against bacterial overgrowth and preservation of the epithelial barrier (By similarity).
Down-regulates inflammatory cytokine expression in several types of immune cells including macrophages and mononuclear cells .
PMID:21242261
Mediates trans-repression of TLR4-induced cytokine expression; the function seems to require its sumoylation and prevents N-CoR nuclear receptor corepressor clearance from target genes such as IL1B and NOS2 .
PMID:19864602
Involved in the TLR9-mediated protective mechanism in intestinal inflammation. Plays an anti-inflammatory role in liver inflammation; proposed to inhibit pro-inflammatory (but not antiapoptotic) NF-kappa-B signaling) (By similarity)
Also regulates lipid and glucose homeostasis and is involved innate immune response .
PMID:10334992 PMID:10334993 PMID:21383957 PMID:22820415
The FXR-RXR heterodimer binds predominantly to farnesoid X receptor response elements (FXREs) containing two inverted repeats of the consensus sequence 5'-AGGTCA-3' in which the monomers are spaced by 1 nucleotide (IR-1) but also to tandem repeat DR1 sites with lower affinity, and can be activated by either FXR or RXR-specific ligands. It is proposed that monomeric nuclear receptors such as NR5A2/LRH-1 bound to coregulatory nuclear responsive element (NRE) halfsites located in close proximity to FXREs modulate transcriptional activity (By similarity). In the liver activates transcription of the corepressor NR0B2 thereby indirectly inhibiting CYP7A1 and CYP8B1 (involved in BA synthesis) implicating at least in part histone demethylase KDM1A resulting in epigenomic repression, and SLC10A1/NTCP (involved in hepatic uptake of conjugated BAs).
Activates transcription of the repressor MAFG (involved in regulation of BA synthesis) (By similarity). Activates transcription of SLC27A5/BACS and BAAT (involved in BA conjugation), ABCB11/BSEP (involved in bile salt export) by directly recruiting histone methyltransferase CARM1, and ABCC2/MRP2 (involved in secretion of conjugated BAs) and ABCB4 (involved in secretion of phosphatidylcholine in the small intestine) .
PMID:12754200 PMID:15471871 PMID:17895379
Activates transcription of SLC27A5/BACS and BAAT (involved in BA conjugation), ABCB11/BSEP (involved in bile salt export) by directly recruiting histone methyltransferase CARM1, and ABCC2/MRP2 (involved in secretion of conjugated BAs) and ABCB4 (involved in secretion of phosphatidylcholine in the small intestine) .
PMID:10514450 PMID:15239098 PMID:16269519
In the intestine activates FGF19 expression and secretion leading to hepatic CYP7A1 repression .
PMID:12815072 PMID:19085950
The function also involves the coordinated induction of hepatic KLB/beta-klotho expression (By similarity). Regulates transcription of liver UGT2B4 and SULT2A1 involved in BA detoxification; binding to the UGT2B4 promoter seems to imply a monomeric transactivation independent of RXRA .
PMID:12806625 PMID:16946559
Modulates lipid homeostasis by activating liver NR0B2/SHP-mediated repression of SREBF1 (involved in de novo lipogenesis), expression of PLTP (involved in HDL formation), SCARB1 (involved in HDL hepatic uptake), APOE, APOC1, APOC4, PPARA (involved in beta-oxidation of fatty acids), VLDLR and SDC1 (involved in the hepatic uptake of LDL and IDL remnants), and inhibiting expression of MTTP (involved in VLDL assembly .
PMID:12554753 PMID:12660231 PMID:15337761
Increases expression of APOC2 (promoting lipoprotein lipase activity implicated in triglyceride clearance) .
PMID:11579204
Transrepresses APOA1 involving a monomeric competition with NR2A1 for binding to a DR1 element .
PMID:11927623 PMID:21804189
Also reduces triglyceride clearance by inhibiting expression of ANGPTL3 and APOC3 (both involved in inhibition of lipoprotein lipase) .
PMID:12891557
Involved in glucose homeostasis by modulating hepatic gluconeogenesis through activation of NR0B2/SHP-mediated repression of respective genes.
Modulates glycogen synthesis (inducing phosphorylation of glycogen synthase kinase-3) (By similarity). Modulates glucose-stimulated insulin secretion and is involved in insulin resistance .
PMID:20447400
Involved in intestinal innate immunity. Plays a role in protecting the distal small intestine against bacterial overgrowth and preservation of the epithelial barrier (By similarity).
Down-regulates inflammatory cytokine expression in several types of immune cells including macrophages and mononuclear cells .
PMID:21242261
Mediates trans-repression of TLR4-induced cytokine expression; the function seems to require its sumoylation and prevents N-CoR nuclear receptor corepressor clearance from target genes such as IL1B and NOS2 .
PMID:19864602
Involved in the TLR9-mediated protective mechanism in intestinal inflammation. Plays an anti-inflammatory role in liver inflammation; proposed to inhibit pro-inflammatory (but not antiapoptotic) NF-kappa-B signaling) (By similarity)
Metabolizing enzymes(1)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP3A7Cytochrome P450 3A7 · Cytochrome P450 3A Subfamily
inducer
Transporters(7)
Proteins that transport this drug across cell membranes
Bile salt export pump
ABCB11
substrate
inhibitor
inducer
Specific functionABC-type bile acid transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner .
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
Solute carrier organic anion transporter family member 1A2
SLCO1A2
substrate
inhibitor
inducer
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane .
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:19129463 PMID:7557095
Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) .
PMID:11159893 PMID:12568656 PMID:19129463 PMID:23918469 PMID:25560245 PMID:9539145
Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision .
PMID:25560245
Involved in the uptake of clinically used drugs .
PMID:17301733 PMID:20686826 PMID:27777271
Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) .
PMID:19129463 PMID:20358049
Also transports prostaglandin E2 .
PMID:19129463
Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
ATP-binding cassette sub-family C member 2
ABCC2
inducer
Specific functionABC-type glutathione S-conjugate transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
ATP-dependent transporter of the ATP-binding cassette (ABC) family that binds and hydrolyzes ATP to enable active transport of various substrates including many drugs, toxicants and endogenous compound across cell membranes. Transports a wide variety of conjugated organic anions such as sulfate-, glucuronide- and glutathione (GSH)-conjugates of endo- and xenobiotics substrates .
PMID:10220572 PMID:10421658 PMID:11500505 PMID:16332456
Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification .
PMID:10421658
Also mediates hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 .
PMID:11500505
Transports sulfated bile salt such as taurolithocholate sulfate .
PMID:16332456
Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors .
PMID:10220572 PMID:11500505 PMID:12441801
Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine PMID:10220572 PMID:11500505
PMID:10220572 PMID:10421658 PMID:11500505 PMID:16332456
Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification .
PMID:10421658
Also mediates hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 .
PMID:11500505
Transports sulfated bile salt such as taurolithocholate sulfate .
PMID:16332456
Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors .
PMID:10220572 PMID:11500505 PMID:12441801
Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine PMID:10220572 PMID:11500505
ATP-binding cassette sub-family C member 4
ABCC4
inhibitor
Specific function15-hydroxyprostaglandin dehydrogenase (NAD+) activity
Cellular location
Basolateral cell membrane
General function & pharmacology
ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes physiological compounds and xenobiotics from cells. Transports a range of endogenous molecules that have a key role in cellular communication and signaling, including cyclic nucleotides such as cyclic AMP (cAMP) and cyclic GMP (cGMP), bile acids, steroid conjugates, urate, and prostaglandins .
PMID:11856762 PMID:12523936 PMID:12835412 PMID:12883481 PMID:15364914 PMID:15454390 PMID:16282361 PMID:17959747 PMID:18300232 PMID:26721430
Mediates the ATP-dependent efflux of glutathione conjugates such as leukotriene C4 (LTC4) and leukotriene B4 (LTB4) too. The presence of GSH is necessary for the ATP-dependent transport of LTB4, whereas GSH is not required for the transport of LTC4 .
PMID:17959747
Mediates the cotransport of bile acids with reduced glutathione (GSH) .
PMID:12523936 PMID:12883481 PMID:16282361
Transports a wide range of drugs and their metabolites, including anticancer, antiviral and antibiotics molecules .
PMID:11856762 PMID:12105214 PMID:15454390 PMID:17344354 PMID:18300232
Confers resistance to anticancer agents such as methotrexate PMID:11106685
PMID:11856762 PMID:12523936 PMID:12835412 PMID:12883481 PMID:15364914 PMID:15454390 PMID:16282361 PMID:17959747 PMID:18300232 PMID:26721430
Mediates the ATP-dependent efflux of glutathione conjugates such as leukotriene C4 (LTC4) and leukotriene B4 (LTB4) too. The presence of GSH is necessary for the ATP-dependent transport of LTB4, whereas GSH is not required for the transport of LTC4 .
PMID:17959747
Mediates the cotransport of bile acids with reduced glutathione (GSH) .
PMID:12523936 PMID:12883481 PMID:16282361
Transports a wide range of drugs and their metabolites, including anticancer, antiviral and antibiotics molecules .
PMID:11856762 PMID:12105214 PMID:15454390 PMID:17344354 PMID:18300232
Confers resistance to anticancer agents such as methotrexate PMID:11106685
Ileal sodium/bile acid cotransporter
SLC10A2
inhibitor
Specific functionbile acid
Cellular location
Membrane
General function & pharmacology
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine .
PMID:7592981 PMID:9458785 PMID:9856990
Transports various bile acids, unconjugated or conjugated, such as cholate and taurocholate .
PMID:7592981 PMID:9458785 PMID:9856990
Also responsible for bile acid transport in the renal proximal tubules, a salvage mechanism that helps conserve bile acids (Probable). Works collaboratively with the Na(+)-taurocholate cotransporting polypeptide (NTCP), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
PMID:7592981 PMID:9458785 PMID:9856990
Transports various bile acids, unconjugated or conjugated, such as cholate and taurocholate .
PMID:7592981 PMID:9458785 PMID:9856990
Also responsible for bile acid transport in the renal proximal tubules, a salvage mechanism that helps conserve bile acids (Probable). Works collaboratively with the Na(+)-taurocholate cotransporting polypeptide (NTCP), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
Hepatic sodium/bile acid cotransporter
SLC10A1
substrate
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
As a major transporter of conjugated bile salts from plasma into the hepatocyte, it plays a key role in the enterohepatic circulation of bile salts necessary for the solubilization and absorption of dietary fat and fat-soluble vitamins .
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It is strictly dependent on the extracellular presence of sodium .
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It exhibits broad substrate specificity and transports various bile acids, such as taurocholate, cholate, as well as non-bile acid organic compounds, such as estrone sulfate .
PMID:14660639 PMID:34060352
Works collaboratively with the ileal transporter (NTCP2), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It is strictly dependent on the extracellular presence of sodium .
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It exhibits broad substrate specificity and transports various bile acids, such as taurocholate, cholate, as well as non-bile acid organic compounds, such as estrone sulfate .
PMID:14660639 PMID:34060352
Works collaboratively with the ileal transporter (NTCP2), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
Chloride anion exchanger
SLC26A3
upregulator
Specific functionbicarbonate transmembrane transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Mediates chloride-bicarbonate exchange with a chloride bicarbonate stoichiometry of 2:1 in the intestinal epithelia .
PMID:16606687 PMID:19321737 PMID:22159084 PMID:22627094
Plays a role in the chloride and bicarbonate homeostasis during sperm epididymal maturation and capacitation (By similarity)
PMID:16606687 PMID:19321737 PMID:22159084 PMID:22627094
Plays a role in the chloride and bicarbonate homeostasis during sperm epididymal maturation and capacitation (By similarity)
Scientific references(8)
Achufusi T.G.O., Safadi A.O., Mahabadi N.
ursodeoxycholic acid. doi: 10.
18578/bnf
388810079
Authors unspecified
Ursodiol, Ursodeoxycholic Acid. Papich Handbook of Veterinary Drugs. 2021;:955-956. doi: 10.
1016/b978-0-323-70957-6
00561-6
Kotb M.A.
Molecular mechanisms of ursodeoxycholic acid toxicity & side effects: ursodeoxycholic acid freezes regeneration & induces hibernation mode.
International Journal Molecular Science
201213(7):8882-8914. doi: 10.3390/ijms13078882. Epub 2012 Jul 17
Trampert D.C., van de Graaf S.F.J., Jongejan A., Oude Elferink R.P.J., Beuers U.
Hepatobiliary acid-base homeostasis: Insights from analogous secretory epithelia.
Journal Hepatol
2021 Feb74(2):428-441. doi: 10.1016/j.jhep.2020.10.010. Epub 2020 Oct 24
Festi D., Montagnani M., Azzaroli F., Lodato F., Mazzella G., Roda A., Di Biase A.R., Roda E., Simoni P., Colecchia A.
Clinical efficacy and effectiveness of ursodeoxycholic acid in cholestatic liver diseases.
Curr Clinical Pharmacology
2007 May2(2):155-77. doi: 10.2174/157488407780598171
Paumgartner G., Beuers U.
Ursodeoxycholic acid in cholestatic liver disease: mechanisms of action and therapeutic use revisited.
Hetersology
2002 Sep36(3):525-31. doi: 10.1053/jhep.2002.36088
Angulo P.
Use of ursodeoxycholic acid in patients with liver disease.
Curr Gastroenterol Reports
2002 Feb4(1):37-44. doi: 10.1007/s11894-002-0036-9
Hofmann A.F.
Pharmacology of ursodeoxycholic acid, an enterohepatic drug.
Scand Journal Gastroenterol Suppl
1994204:1-15. doi: 10.3109/00365529409103618
ATC classification(1 code)
ATC A05AA02
Affected organisms(1)
Humans and other mammals
International brands(9)
Experimental properties(2)
Commercial products(140)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Ursodeoxycholic acid
Additional database identifiers
Drugs Product Database (DPD)
952
ChemSpider
29131
BindingDB
53721
PDB
IU5
ZINC
ZINC000003914809
HUGO Gene Nomenclature Committee (HGNC)
HGNC:385
GenAtlas
AKR1C2
GeneCards
AKR1C2
GenBank Gene Database
U05598
GenBank Protein Database
531160
UniProt Accession
AK1C2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1062
GenAtlas
BLVRA
GeneCards
BLVRA
GenBank Gene Database
X93086
GenBank Protein Database
1246749
UniProt Accession
BIEA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10973
GeneCards
SLC23A2
UniProt Accession
S23A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:7967
GenAtlas
NR1H4
GeneCards
NR1H4
GenBank Gene Database
U68233
GenBank Protein Database
1546084
Guide to Pharmacology
603
UniProt Accession
NR1H4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:17450
GeneCards
CYP3A43
GenBank Gene Database
AF319634
GenBank Protein Database
12642642
UniProt Accession
CP343_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2638
GenAtlas
CYP3A5
GeneCards
CYP3A5
GenBank Gene Database
J04813
GenBank Protein Database
181346
Guide to Pharmacology
1338
UniProt Accession
CP3A5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2640
GeneCards
CYP3A7
GenBank Gene Database
D00408
GenBank Protein Database
220149
UniProt Accession
CP3A7_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:42
GenAtlas
ABCB11
GeneCards
ABCB11
GenBank Gene Database
AF091582
GenBank Protein Database
3873243
Guide to Pharmacology
778
UniProt Accession
ABCBB_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10956
GeneCards
SLCO1A2
GenBank Gene Database
U21943
GenBank Protein Database
885978
Guide to Pharmacology
1219
UniProt Accession
SO1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:53
GenAtlas
ABCC2
GeneCards
ABCC2
GenBank Gene Database
U63970
GenBank Protein Database
1764162
Guide to Pharmacology
780
UniProt Accession
MRP2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:55
GenAtlas
ABCC4
GeneCards
ABCC4
GenBank Gene Database
AF071202
GenBank Protein Database
3335173
Guide to Pharmacology
782
UniProt Accession
MRP4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10906
GeneCards
SLC10A2
GenBank Gene Database
U10417
GenBank Protein Database
595399
Guide to Pharmacology
960
UniProt Accession
NTCP2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10905
GeneCards
SLC10A1
GenBank Gene Database
L21893
GenBank Protein Database
410214
Guide to Pharmacology
959
UniProt Accession
NTCP_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3018
GeneCards
SLC26A3
UniProt Accession
S26A3_HUMAN
International reference pricing
10 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $0.92/tablet
To $6.30/tablet
Pms-Ursodiol C 250 mg Tablet
$0.92/tablet
Urso 250 mg Tablet
$1.42/tablet
Pms-Ursodiol C 500 mg Tablet
$1.75/tablet
Ursodiol 250 mg tablet
$2.68/tablet
Urso Ds 500 mg Tablet
$2.69/tablet
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)