Investigational Drug Details
| Drug ID: | D381 |
| Drug Name: | Ursodeoxycholic acid |
| Synonyms: | (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; UDCA; Ursodeoxycholate; Ursodeoxycholic acid; Ursodiol |
| Type: | Chemical drug |
| DrugBank ID: | DB01586 |
| DrugBank Description: | Ursodeoxycholic acid is an epimer of . It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic. |
| PubChem ID: | 31401 |
| CasNo: | 128-13-2 |
| Repositioning for NAFLD: | Yes |
| SMILES: | C[C@]12[C@H]([C@H]3[C@H](CC2)[C@]2(C)[C@H](C[C@@H]3O)C[C@@H](CC2)O)CC[C@@H]1[C@@H](CCC(=O)O)C |
| Structure: |
|
| InChiKey: | RUDATBOHQWOJDD-UZVSRGJWSA-N |
| Molecular Weight: | 392.58 |
| DrugBank Targets: | Aldo-keto reductase family 1 member C2 inducer; Bile acid receptor |
| DrugBank MoA: | Ursodeoxycholic acid reduces elevated liver enzyme levels by facilitating bile flow through the liver and protecting liver cells. The main mechanism if anticholelithic. Although the exact process of ursodiol's anticholelithic action is not completely understood, it is thought that the drug is concentrated in bile and decreases biliary cholesterol by suppressing hepatic synthesis and secretion of cholesterol and by inhibiting its intestinal absorption. The reduced cholesterol saturation permits the gradual solubilization of cholesterol from gallstones, resulting in their eventual dissolution. |
| DrugBank Pharmacology: | Ursodiol (commonly known as ursodeoxycholic acid) is a product of metabolism of bacteria in the intestine. It is considered a secondary bile acid. The other type of bile acid, primary bile acids, are produced hepatically and subsequently stored in the gallbladder. When primary bile acids are secreted into the large intestine, they can be broken down into secondary bile acids by bacteria present in the intestine. Both types of bile acids assist in the metabolism of dietary fat. Ursodeoxycholic acid regulates cholesterol levels by slowing the rate at which the intestine is able to absorb cholesterol and also acts to break down micelles, which contain cholesterol. Because of this property, ursodeoxycholic acid is used to treat gall stones non-surgically. |
| DrugBank Indication: | The drug decreases the absorption of cholesterol and is used to dissolve (cholesterol) gallstones in patients as an alternative to a surgical procedure to remove the gallstones. |
| Targets: | AKR1C2 inducer |
| Therapeutic Category: | Anti-inflammatory |
| Clinical Trial Progress: | Phase 2 on-going (NCT05083390) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0137 | NCT01548079 | Not applicable | Completed | No Results Available | October 2008 | December 3, 2013 | Details |
| L0143 | NCT04977661 | Phase 4 | Completed | No Results Available | February 1, 2020 | July 27, 2021 | Details |
| L0269 | NCT05083390 | Phase 2 | Recruiting | No Results Available | July 8, 2019 | October 27, 2021 | Details |
| L0384 | NCT04910178 | Phase 4 | Recruiting | No Results Available | 25/05/2021 | 17 August 2021 | Details |
| L0446 | ChiCTR1900028204 | Phase 0 | Not Recruiting | No Results Available | 15/12/2019 | 16 December 2019 | Details |
| L0476 | EUCTR2018-003443-31-CZ | Phase 2 | Authorised | No Results Available | 05/03/2019 | 2 March 2022 | Details |
| L0553 | EUCTR2016-002965-67-NL | Phase 2 | Authorised | No Results Available | 29/03/2017 | 17 July 2017 | Details |
| L0600 | IRCT201407201155N21 | Not applicable | Not Recruiting | No Results Available | 22/09/2015 | 22 February 2018 | Details |
| L0618 | EUCTR2013-004605-38-AT | Phase 2 | Not Recruiting | No Results Available | 02/12/2014 | 14 November 2016 | Details |
| L0675 | JPRN-UMIN000004034 | Not applicable | Not Recruiting | No Results Available | 13/08/2010 | 2 April 2019 | Details |
| L0690 | EUCTR2007-004515-56-AT | Phase 3 | Not Recruiting | No Results Available | 25/03/2008 | 26 October 2020 | Details |
| L0691 | EUCTR2007-005531-28-SE | Not applicable | Not Recruiting | No Results Available | 15/02/2008 | 10 July 2015 | Details |
| L0754 | CTRI/2019/04/018550 | Not applicable | Not Recruiting | No Results Available | 10/04/2019 | 24 November 2021 | Details |
| L0780 | IRCT20180404039187N1 | Phase 2/Phase 3 | Recruiting | No Results Available | 22/11/2018 | 14 January 2019 | Details |
| L0787 | NCT03664596 | Not applicable | Not recruiting | No Results Available | 06/09/2018 | 16 February 2021 | Details |
| L0980 | NCT00470171 | Phase 2 | Not recruiting | No Results Available | 04/05/2007 | 19 February 2015 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T17 | Farnesoid X-activated receptor | NR1H4 | agonist | Nuclear hormone receptor | Q96RI1 | NR1H4_HUMAN | Details |
| T10 | Caspase-1 | CASP1 | inhibitor | Enzyme | P29466 | CASP1_HUMAN | Details |
| T07 | Bile acid receptor | NR1H4 | agonist | Nuclear hormone receptor | Q96RI1 | NR1H4_HUMAN | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00271 | 35159219 | Cells | S-Adenosylmethionine: From the Discovery of Its Inhibition of Tumorigenesis to Its Use as a Therapeutic Agent. | Details |
| A00474 | 35068796 | J Clin Exp Hepatol | A Current Understanding of Bile Acids in Chronic Liver Disease. | Details |
| A00594 | 35035690 | Am J Transl Res | Bile acid metabolism and liver fibrosis following treatment with bifid triple viable capsules in nonalcoholic fatty liver disease. | Details |
| A00604 | 35033554 | Eur J Pharmacol | Ursodesoxycholic acid is an FFA4 agonist and reduces hepatic steatosis via FFA4 signaling. | Details |
| A00760 | 34977519 | JHEP Rep | Pegbelfermin selectively reduces secondary bile acid concentrations in patients with non-alcoholic steatohepatitis. | Details |
| A00896 | 34938193 | Front Pharmacol | Ursodeoxycholic Acid Treatment Restores Gut Microbiota and Alleviates Liver Inflammation in Non-Alcoholic Steatohepatitic Mouse Model. | Details |
| A00941 | 34923459 | Wiad Lek | THE EFFECTIVENESS OF COMPLEX THERAPY WITH THE INCLUSION OF THE URSODEOXYCHOLIC ACID IN PATIENTS WITH NON-ALCOHOLIC FATTY LIVER DISEASE IN COMBINATION WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE. | Details |
| A01923 | 34560694 | Eur J Gastroenterol Hepatol | Healthcare practitioners' diagnostic and treatment practice patterns of nonalcoholic fatty liver disease in Poland: a cross-sectional survey. | Details |
| A01996 | 34535644 | Nat Commun | A phase 2, proof of concept, randomised controlled trial of berberine ursodeoxycholate in patients with presumed non-alcoholic steatohepatitis and type 2 diabetes. | Details |
| A02341 | 34411400 | Liver Int | Bile acid dysmetabolism in the gut-microbiota-liver axis under hepatitis C virus infection. | Details |
| A03036 | 34156011 | Wiad Lek | THE EFFECT OF COMPREHENSIVE TREATMENT OF PATIENTS WITH NON-ALCOHOLIC FATTY LIVER DISEASE IN COMBINATION WITH PREDIABETES ON THE LIPID PROFILE. | Details |
| A03701 | 33898959 | JHEP Rep | Potent suppression of hydrophobic bile acids by aldafermin, an FGF19 analogue, across metabolic and cholestatic liver diseases. | Details |
| A03905 | 33824248 | Korean J Gastroenterol | Efficacy and Safety of Biphenyl Dimethyl Dicarboxylate and Ursodeoxycholic Acid Combination in Chronic Hepatitis Related to Metabolic Syndrome Components. | Details |
| A04051 | 33776366 | World J Gastroenterol | Ursodeoxycholic acid as a means of preventing atherosclerosis, steatosis and liver fibrosis in patients with nonalcoholic fatty liver disease. | Details |
| A04068 | 33771699 | Pharmacol Res | Epigenetics in NAFLD/NASH: Targets and therapy. | Details |
| A04072 | 33769703 | Physiol Rep | ω-Imidazolyl-alkyl derivatives as new preclinical drug candidates for treating non-alcoholic steatohepatitis. | Details |
| A04120 | 33750416 | J Transl Med | LncRNA-Gm9795 promotes inflammation in non-alcoholic steatohepatitis via NF-[Formula: see text]B/JNK pathway by endoplasmic reticulum stress. | Details |
| A04188 | 33722778 | Clin Res Hepatol Gastroenterol | Efficacy and safety of obeticholic acid in liver disease-A systematic review and meta-analysis. | Details |
| A04443 | 33615207 | JHEP Rep | NASH-related increases in plasma bile acid levels depend on insulin resistance. | Details |
| A05097 | 33377363 | Asia Pac J Clin Nutr | Efficacy of ursodeoxycholic acid in nonalcoholic fatty liver disease: An updated meta-analysis of randomized controlled trials. | Details |