osilodrostat Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
enzyme inhibitors 5384 928134-65-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • osilodrostat
  • osilodrostat phosphate
  • LCI699-NX
  • LCI-699
  • isturisa
Osilodrostat is a cortisol synthesis inhibitor. It inhibits 11beta-hydroxylase (CYP11B1), the enzyme responsible for the final step of cortisol biosynthesis in the adrenal gland
  • Molecular weight: 227.24
  • Formula: C13H10FN3
  • CLOGP: 1.35
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 41.61
  • ALOGS: -2.81
  • ROTB: 1

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 9, 2020 EMA Novartis Europharm Limited
March 6, 2020 FDA RECORDATI RARE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Adrenal insufficiency 50.03 37.81 7 4 13117 46672934

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC H02CA02 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CORTICOSTEROIDS FOR SYSTEMIC USE
ANTIADRENAL PREPARATIONS
Anticorticosteroids

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pituitary-dependent Cushing's disease indication 190502001 DOID:3946

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.46 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL March 6, 2025 NEW CHEMICAL ENTITY
EQ 1MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL March 6, 2025 NEW CHEMICAL ENTITY
EQ 5MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL March 6, 2025 NEW CHEMICAL ENTITY
EQ 10MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL March 6, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH CUSHING’S DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 1MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL March 6, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH CUSHING’S DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 5MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL March 6, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH CUSHING’S DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Cytochrome P450 11B1, mitochondrial Enzyme INHIBITOR IC50 8.60 DRUG LABEL DRUG LABEL
Cytochrome P450 11B2, mitochondrial Enzyme INHIBITOR IC50 9.15 SCIENTIFIC LITERATURE

External reference:

IDSource
1315449-72-9 SECONDARY_CAS_RN
4039308 VANDF
C5243124 UMLSCUI
YSY PDB_CHEM_ID
CHEMBL3707393 ChEMBL_ID
CHEMBL3099695 ChEMBL_ID
DB11837 DRUGBANK_ID
C553306 MESH_SUPPLEMENTAL_RECORD_UI
D11061 KEGG_DRUG
8310 IUPHAR_LIGAND_ID
9818 INN_ID
5YL4IQ1078 UNII
44139752 PUBCHEM_CID
2286252 RXNORM
331593 MMSL
38191 MMSL
d09521 MMSL
018295 NDDF
018296 NDDF
863916001 SNOMEDCT_US
863938004 SNOMEDCT_US
863942001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Isturisa HUMAN PRESCRIPTION DRUG LABEL 1 55292-320 TABLET, COATED 1 mg ORAL NDA 26 sections
Isturisa HUMAN PRESCRIPTION DRUG LABEL 1 55292-321 TABLET, COATED 5 mg ORAL NDA 26 sections
Isturisa HUMAN PRESCRIPTION DRUG LABEL 1 55292-322 TABLET, COATED 10 mg ORAL NDA 26 sections