Levoketoconazole

Levoketoconazole

Levoketoconazole

Chemical compound

Levoketoconazole, sold under the brand name Recorlev, is a steroidogenesis inhibitor that is used for the treatment of Cushing's syndrome.[3][4][5][6] Levoketoconazole was approved for medical use in the United States in December 2021.[7][8]

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Levoketoconazole is the levorotatory or (2S,4R) enantiomer of ketoconazole,[4][5][6] and it is an inhibitor of the enzymes CYP11B1 (11β-hydroxylase), CYP17A1 (17α-hydroxylase/17,20-lyase), and CYP21A2 (21-hydroxylase).[3][4][6] It inhibits glucocorticoid biosynthesis and hence circulating levels of glucocorticoids, thereby treating Cushing's syndrome.[3][6] 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.[6] 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.[9]

References

  1. [1]
    "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  2. [2]
    "Recorlev- levoketoconazole tablet". DailyMed. 12 January 2022. Retrieved 20 February 2022.
  3. [3]
    "Levoketoconazole - Strongbridge Biopharma". AdisInsight. Springer Nature Switzerland AG.
  4. [4]
    Laws Jr ER, Pace L (11 November 2016). Cushing's Disease: An Often Misdiagnosed and Not So Rare Disorder. Elsevier Science. pp. 113–. ISBN 978-0-12-804390-5.
  5. [5]
    Geer EB (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.
  6. [6]
    Cuevas-Ramos D, Lim DS, Fleseriu M (2016). "Update on medical treatment for Cushing's disease". Clinical Diabetes and Endocrinology. 2 (1): 16. doi:10.1186/s40842-016-0033-9. PMC 5471955. PMID 28702250.
  7. [7]
    "Levoketoconazole: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 3 January 2022.
  8. [8]
    "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.
  9. [9]
    Thieroff-Ekerdt R, Lavin P, Abou-Gharbia M, France N (October 2016). Pharmacology of COR-003 (levoketoconazole), an investigational treatment for endogenous Cushing's syndrome (PDF). Pituitary disorders—it’s not the anterior pituitary (posters). Endocrine Society. pp. SAT-547–SAT-547. Archived from the original (PDF) on 20 September 2020. Retrieved 30 April 2017.
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