Obeticholic Acid—A Pharmacological and Clinical Review
Obeticholic acid (OCA) or 6-alpha-ethyl-chenodeoxycholic acid is a semisynthetic modified bile acid derivative that acts on the farnesoid X receptor (FXR) as an agonist with a higher potency than bile acid. The FXR is a nuclear receptor highly expressed in the liver and small intestine and regulates...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-02-01
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| Series: | Future Pharmacology |
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| Online Access: | https://www.mdpi.com/2673-9879/3/1/17 |
| _version_ | 1797611580233351168 |
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| author | Caezaan Keshvani Jonathan Kopel Hemant Goyal |
| author_facet | Caezaan Keshvani Jonathan Kopel Hemant Goyal |
| author_sort | Caezaan Keshvani |
| collection | DOAJ |
| description | Obeticholic acid (OCA) or 6-alpha-ethyl-chenodeoxycholic acid is a semisynthetic modified bile acid derivative that acts on the farnesoid X receptor (FXR) as an agonist with a higher potency than bile acid. The FXR is a nuclear receptor highly expressed in the liver and small intestine and regulates bile acid, cholesterol, glucose metabolism, inflammation, and apoptosis. The FXR group of bile acid receptors is currently under investigation for their potential role in the treatment of primary biliary cirrhosis (PBC), non-alcoholic steatohepatitis (NASH), and primary sclerosing cholangitis (PSC). Recent clinical studies suggest OCA may work synergistically with lipid modifying medications to further improve long-term outcomes with primary sclerosing cholangitis. Specifically, OCA can improve clinical outcomes in NASH patients with their different histological, metabolic, and biochemical issues as well as improve morbidity and mortality in patients suffering from PBC, PSC, or liver disease. This improvement is noted in both improved histological examination and reduced need for transplantation. In this review, we examine the pharmacology of OCA towards the treatment of PBC refractory and steatohepatitis (NASH). In addition, we examine future directions and applications of OCA for PBC, PSC, NASH, and NAFLD. |
| first_indexed | 2024-03-11T06:30:43Z |
| format | Article |
| id | doaj.art-21e77bb19b344c958c028085f3930f54 |
| institution | Directory Open Access Journal |
| issn | 2673-9879 |
| language | English |
| last_indexed | 2024-03-11T06:30:43Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Future Pharmacology |
| spelling | doaj.art-21e77bb19b344c958c028085f3930f542023-11-17T11:13:34ZengMDPI AGFuture Pharmacology2673-98792023-02-013123825110.3390/futurepharmacol3010017Obeticholic Acid—A Pharmacological and Clinical ReviewCaezaan Keshvani0Jonathan Kopel1Hemant Goyal2Department of Medicine, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USADepartment of Medicine, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USAInstructor in Medicine, Division of Gastroenterology, Hepatology and Nutrition, The University of Texas Health Science Center at Houston, Houston, TX 77030, USAObeticholic acid (OCA) or 6-alpha-ethyl-chenodeoxycholic acid is a semisynthetic modified bile acid derivative that acts on the farnesoid X receptor (FXR) as an agonist with a higher potency than bile acid. The FXR is a nuclear receptor highly expressed in the liver and small intestine and regulates bile acid, cholesterol, glucose metabolism, inflammation, and apoptosis. The FXR group of bile acid receptors is currently under investigation for their potential role in the treatment of primary biliary cirrhosis (PBC), non-alcoholic steatohepatitis (NASH), and primary sclerosing cholangitis (PSC). Recent clinical studies suggest OCA may work synergistically with lipid modifying medications to further improve long-term outcomes with primary sclerosing cholangitis. Specifically, OCA can improve clinical outcomes in NASH patients with their different histological, metabolic, and biochemical issues as well as improve morbidity and mortality in patients suffering from PBC, PSC, or liver disease. This improvement is noted in both improved histological examination and reduced need for transplantation. In this review, we examine the pharmacology of OCA towards the treatment of PBC refractory and steatohepatitis (NASH). In addition, we examine future directions and applications of OCA for PBC, PSC, NASH, and NAFLD.https://www.mdpi.com/2673-9879/3/1/17obeticholic acidnon-alcoholic fatty liver diseasemetabolic syndromebiliary cirrhosisprimary biliary cholangitisnon-alcoholic steatohepatitis |
| spellingShingle | Caezaan Keshvani Jonathan Kopel Hemant Goyal Obeticholic Acid—A Pharmacological and Clinical Review Future Pharmacology obeticholic acid non-alcoholic fatty liver disease metabolic syndrome biliary cirrhosis primary biliary cholangitis non-alcoholic steatohepatitis |
| title | Obeticholic Acid—A Pharmacological and Clinical Review |
| title_full | Obeticholic Acid—A Pharmacological and Clinical Review |
| title_fullStr | Obeticholic Acid—A Pharmacological and Clinical Review |
| title_full_unstemmed | Obeticholic Acid—A Pharmacological and Clinical Review |
| title_short | Obeticholic Acid—A Pharmacological and Clinical Review |
| title_sort | obeticholic acid a pharmacological and clinical review |
| topic | obeticholic acid non-alcoholic fatty liver disease metabolic syndrome biliary cirrhosis primary biliary cholangitis non-alcoholic steatohepatitis |
| url | https://www.mdpi.com/2673-9879/3/1/17 |
| work_keys_str_mv | AT caezaankeshvani obeticholicacidapharmacologicalandclinicalreview AT jonathankopel obeticholicacidapharmacologicalandclinicalreview AT hemantgoyal obeticholicacidapharmacologicalandclinicalreview |