LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of CYP11B1;Inhibitor of CYP11B2
Product Description
Information
Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B) , an enzyme catalyzing the final step of cortisol synthesis.
Targets
11β-hydroxylase 2.5 nM
In vitro
LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1.
In vivo
LCI699 is a potent inhibitor of 11β-hydroxylase (CYP11B1), the enzyme that catalyzes the final step of cortisol synthesis, and has a half-life of ∼4 hours. It decreases blood pressure (BP) in patients with essential hypertension and primary aldosteronism. Treatment with LCI699 is well tolerated, it is demonstrated efficacy with a satisfactory safety and tolerability profile in the proof-of-concept study in Cushing\'s disease. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism.
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.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]
4.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]
5.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]
6.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]
7.Fleseriu M. (2015) Medical Treatment of Cushing Disease: New Targets, New Hope.. Endocrinol Metab Clin North Am, 44 (1):(51-70). [PMID:25732642]
8.Duggan S. (2020) Osilodrostat: First Approval.. Drugs, 80 (5):(495-500). [PMID:32141023]
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K2228505