General
Preferred name
osilodrostat
Synonyms
Osilodrostat (phosphate) ()
LCI699 ()
LCI699 (phosphate) ()
OSILODROSTAT PHOSPHATE ()
LCI699-NX ()
LCI-699 ()
LCI-699-NX ()
LCI699-AZA ()
Isturisa ()
P&D ID
PD046274
CAS
1304733-26-3
928134-65-0
1315449-72-9
Tags
available
drug
Approved by
EMA
PMDA
FDA
First approval
2020
Drug indication
Liver disease
Cushing disease
pituitary-dependent Cushing's disease
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Osilodrostat was designed as an inhibitor of aldosterone synthase (CYP11B2), but is also reported to inhibit the closely related enzyme, 11-beta-hydroxylase (CYP11B1) .
DESCRIPTION
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 . It is this latter action of osilodrostat that is harnessed for clinical utility in Cushing's disease. The drug is orally bioavailable.
(GtoPdb)
DESCRIPTION
Osilodrostat (LCI699) is a potent, orally active11¦Â-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS)[1][2][3].
PRICE
81
DESCRIPTION
Osilodrostat (LCI699) is a potent inhibitor of human 11??-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) with IC50 values ??of 2.5 and 0.7 nM, respectively, and has been approved by the FDA for the treatment of Cushing's disease.
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
20
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
NCATS Inxight Approved Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
34
Molecular Weight
227.09
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
0
Rotatable Bonds
1
Ring Count
3
Aromatic Ring Count
2
cLogP
2.43
TPSA
41.61
Fraction CSP3
0.23
Chiral centers
1.0
Largest ring
6.0
QED
0.75
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
Hydroxylase
Raf kinase B Inhibitors
Cytochrome P450 11B2 (Aldosterone Synthase) Inhibitors
Cytochrome P450 CYP11B1 (Steroid 11-beta Hydroxylase) Inhibitors
Cytochrome P450 inhibitor
Target
11¦Â-hydroxylase,aldosterone synthase
Mineralocorticoid Receptor
Member status
virtual
Pathway
Metabolic Enzyme/Protease
Vitamin D Related/Nuclear Receptor
Source data
