osilodrostat 🐶 Veterinary Use | 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: 1.36
  • 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:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Jan. 9, 2020 EMA Novartis Europharm Limited
March 6, 2020 FDA RECORDATI RARE
March 23, 2021 PMDA Recordati Rare Diseases Japan K.K.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H02CA02 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CORTICOSTEROIDS FOR SYSTEMIC USE
ANTIADRENAL PREPARATIONS
Anticorticosteroids
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
FDA MoA N0000182138 Cytochrome P450 1A2 Inhibitors
FDA MoA N0000182140 Cytochrome P450 2C19 Inhibitors
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000190115 Cytochrome P450 3A5 Inhibitors
FDA EPC N0000193935 Cortisol Synthesis Inhibitor
FDA MoA N0000193936 Cytochrome P450 11B1 Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hypercortisolism indication 47270006
Pituitary-dependent Cushing's disease indication 190502001 DOID:3946




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 DISCN TABLET ORAL 8609862 Jan. 13, 2031 CUSHINGS DISEASE
EQ 1MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL 8609862 Jan. 13, 2031 CUSHINGS DISEASE
EQ 5MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL 8609862 Jan. 13, 2031 CUSHINGS DISEASE
EQ 10MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 DISCN TABLET ORAL 10709691 Oct. 12, 2035 CUSHINGS DISEASE
EQ 1MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL 10709691 Oct. 12, 2035 CUSHINGS DISEASE
EQ 5MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 RX TABLET ORAL 10709691 Oct. 12, 2035 CUSHINGS DISEASE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE ISTURISA RECORDATI RARE N212801 March 6, 2020 DISCN 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 DISCN 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
Aromatase Enzyme IC50 6.07 CHEMBL
Cytochrome P450 11B2, mitochondrial Enzyme INHIBITOR IC50 9.15 SCIENTIFIC LITERATURE
Cytochrome P450 11B2, mitochondrial Enzyme IC50 6.68 CHEMBL
Cytochrome P450 11B1, mitochondrial Enzyme IC50 6.30 CHEMBL
Cytochrome P450 11B2, mitochondrial Enzyme IC50 6.96 CHEMBL

External reference:

IDSource
5YL4IQ1078 UNII
1315449-72-9 SECONDARY_CAS_RN
C4330903 UMLSCUI
YSY PDB_CHEM_ID
CHEMBL3099695 ChEMBL_ID
44139752 PUBCHEM_CID
DB11837 DRUGBANK_ID
CHEMBL3707393 ChEMBL_ID
9818 INN_ID
D11061 KEGG_DRUG
8310 IUPHAR_LIGAND_ID
018295 NDDF
018296 NDDF
863916001 SNOMEDCT_US
863938004 SNOMEDCT_US
863942001 SNOMEDCT_US
4039308 VANDF
2286252 RXNORM
331593 MMSL
38191 MMSL
d09521 MMSL
C553306 MESH_SUPPLEMENTAL_RECORD_UI

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