Biology:Levoketoconazole
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| Trade names | Recorlev |
| Other names | COR-003; (2S,4R)-ketoconazole; NormoCort |
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| Routes of administration | By mouth |
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| Formula | C26H28Cl2N4O4 |
| Molar mass | 531.43 g·mol−1 |
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Levoketoconazole, sold under the brand name Recorlev, is a steroidogenesis inhibitor that is used for the treatment of Cushing's syndrome.[2][3][4][5] Levoketoconazole was approved for medical use in the United States in December 2021.[6][7]
Levoketoconazole is the levorotatory or (2S,4R) enantiomer of ketoconazole,[3][4][5] and it is an inhibitor of the enzymes CYP11B1 (11β-hydroxylase), CYP17A1 (17α-hydroxylase/17,20-lyase), and CYP21A2 (21-hydroxylase).[2][3][5] It inhibits glucocorticoid biosynthesis and hence circulating levels of glucocorticoids, thereby treating Cushing's syndrome.[2][5] In addition to its increased potency, the drug is 12-fold less potent than racemic ketoconazole in inhibiting CYP7A1 (cholesterol 7α-hydroxylase), theoretically resulting in further reduced interference with bile acid production and metabolite elimination and therefore less risk of hepatotoxicity.[5] Levoketoconazole has also been found to inhibit CYP11A1 (cholesterol side-chain cleavage enzyme) and CYP51A1 (lanosterol-14α-demethylase), similarly but more potently relative to ketoconazole.[8]
References
- ↑ "Recorlev- levoketoconazole tablet". 12 January 2022. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d4c5fead-bc4a-fb02-e053-2a95a90ae4fc.
- ↑ 2.0 2.1 2.2 "Levoketoconazole - Strongbridge Biopharma". AdisInsight. Springer Nature Switzerland AG. http://adisinsight.springer.com/drugs/800037965.
- ↑ 3.0 3.1 3.2 Cushing's Disease: An Often Misdiagnosed and Not So Rare Disorder. Elsevier Science. 11 November 2016. pp. 113–. ISBN 978-0-12-804390-5. https://books.google.com/books?id=b21_CwAAQBAJ&pg=PA113.
- ↑ 4.0 4.1 Geer, Eliza B. (1 December 2016). The Hypothalamic-Pituitary-Adrenal Axis in Health and Disease: Cushing's Syndrome and Beyond. Springer. pp. 170–. ISBN 978-3-319-45950-9. https://books.google.com/books?id=Yw2kDQAAQBAJ&pg=PA170.
- ↑ 5.0 5.1 5.2 5.3 5.4 "Update on medical treatment for Cushing's disease". Clinical Diabetes and Endocrinology 2 (1): 16. 2016. doi:10.1186/s40842-016-0033-9. PMID 28702250.
- ↑ "Levoketoconazole: FDA-Approved Drugs". https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=214133.
- ↑ "Xeris Biopharma Announces U.S. FDA Approval of Recorlev (levoketoconazole) for the Treatment of Endogenous Hypercortisolemia in Adult Patients With Cushing's Syndrome" (Press release). Xeris Biopharma. 30 December 2021. Retrieved 3 January 2022 – via Business Wire.
- ↑ "Pharmacology of COR-003 (levoketoconazole), an investigational treatment for endogenous Cushing's syndrome.". Pituitary disorders—it’s not the anterior pituitary (posters). Endocrine Society. October 2016. pp. SAT-547-SAT-547. https://www.strongbridgebio.com/wp-content/uploads/strongbridge-poster-pharmology-cor-003.pdf. Retrieved 30 April 2017.
External links
- "Levoketoconazole". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/levoketoconazole.
- Clinical trial number NCT03277690 for "A Study to Assess the Safety and Efficacy of Levoketoconazole in the Treatment of Endogenous Cushing's Syndrome" at ClinicalTrials.gov
- Clinical trial number NCT01838551 for "Treatment for Endogenous Cushing's Syndrome (SONICS)" at ClinicalTrials.gov
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