Synonyms: Isturisa® | LCI-699 | LCI699
osilodrostat is an approved drug (EMA & FDA (2020))
Compound class:
Synthetic organic
Comment: Osilodrostat was designed as an inhibitor of aldosterone synthase (CYP11B2), but is also reported to inhibit the closely related enzyme, 11-beta-hydroxylase (CYP11B1) and hence as an inhibitor of cortisol biosynthesis [8]. It is this latter action of osilodrostat that is harnessed for clinical utility in Cushing's disease. The drug is orally bioavailable.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Amar L, Azizi M, Menard J, Peyrard S, Watson C, Plouin PF. (2010)
Aldosterone synthase inhibition with LCI699: a proof-of-concept study in patients with primary aldosteronism. Hypertension, 56 (5): 831-8. [PMID:20837883] |
2. Calhoun DA, White WB, Krum H, Guo W, Bermann G, Trapani A, Lefkowitz MP, Ménard J. (2011)
Effects of a novel aldosterone synthase inhibitor for treatment of primary hypertension: results of a randomized, double-blind, placebo- and active-controlled phase 2 trial. Circulation, 124 (18): 1945-55. [PMID:21986283] |
3. Daniel E, Newell-Price JD. (2015)
Therapy of endocrine disease: steroidogenesis enzyme inhibitors in Cushing's syndrome. Eur J Endocrinol, 172 (6): R263-80. [PMID:25637072] |
4. Duggan S. (2020)
Osilodrostat: First Approval. Drugs, 80 (5): 495-500. [PMID:32141023] |
5. Fleseriu M. (2015)
Medical Treatment of Cushing Disease: New Targets, New Hope. Endocrinol Metab Clin North Am, 44 (1): 51-70. [PMID:25732642] |
6. Fleseriu M, Petersenn S. (2015)
Medical therapy for Cushing's disease: adrenal steroidogenesis inhibitors and glucocorticoid receptor blockers. Pituitary, 18 (2): 245-52. [PMID:25560275] |
7. Wang HZ, Tian JB, Yang KH. (2015)
Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review. Eur Rev Med Pharmacol Sci, 19 (2): 296-304. [PMID:25683946] |
8. Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW. (2014)
Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors. J Med Chem, 57 (12): 5179-89. [PMID:24899257] |