Scroll

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

Stem definition	Drug id	CAS RN
enzyme inhibitors	5384	928134-65-0

Description:

Molecule	Description
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

Molecule

Description

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:

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

Approvals:

Show entries

Search:

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

Showing 1 to 3 of 3 entries

Previous1Next

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:

Show entries

Search:

Source	Code	Description
ATC	H02CA02	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS CORTICOSTEROIDS FOR SYSTEMIC USE ANTIADRENAL PREPARATIONS Anticorticosteroids
FDA EPC	N0000193935	Cortisol Synthesis Inhibitor
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 MoA	N0000193936	Cytochrome P450 11B1 Inhibitors

Showing 1 to 8 of 8 entries

Previous1Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Hypercortisolism	indication	47270006
Pituitary-dependent Cushing's disease	indication	190502001	DOID:3946

Showing 1 to 2 of 2 entries

Previous1Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.46	Basic

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 10MG BASE	ISTURISA	RECORDATI RARE	N212801	March 6, 2020	DISCN	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	8609862	Jan. 13, 2031	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	8609862	Jan. 13, 2031	CUSHINGS DISEASE
EQ 5MG BASE	ISTURISA	RECORDATI RARE	N212801	March 6, 2020	RX	TABLET	ORAL	10709691	Oct. 12, 2035	CUSHINGS DISEASE

Showing 1 to 6 of 6 entries

Previous1Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE	ISTURISA	RECORDATI RARE	N212801	March 6, 2020	DISCN	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, 2025	NEW CHEMICAL ENTITY
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, 2025	NEW CHEMICAL ENTITY
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

Showing 1 to 6 of 6 entries

Previous1Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Cytochrome P450 11B1, mitochondrial	Enzyme	P15538	C11B1_HUMAN	INHIBITOR	IC50	8.60	DRUG LABEL	DRUG LABEL
Aromatase	Enzyme	P11511	CP19A_HUMAN		IC50	6.07	CHEMBL
Cytochrome P450 11B2, mitochondrial	Enzyme	P19099	C11B2_HUMAN	INHIBITOR	IC50	9.15	SCIENTIFIC LITERATURE
Cytochrome P450 11B2, mitochondrial	Enzyme		C11B2_MOUSE		IC50	6.68	CHEMBL
Cytochrome P450 11B1, mitochondrial	Enzyme		C11B1_RAT		IC50	6.30	CHEMBL
Cytochrome P450 11B2, mitochondrial	Enzyme		C11B2_RAT		IC50	6.96	CHEMBL

Showing 1 to 6 of 6 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
YSY	PDB_CHEM_ID
018295	NDDF
018296	NDDF
1315449-72-9	SECONDARY_CAS_RN
2286252	RXNORM
331593	MMSL
38191	MMSL
4039308	VANDF
44139752	PUBCHEM_CID
5YL4IQ1078	UNII

Showing 1 to 10 of 22 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

Showing 1 to 6 of 6 entries

Previous1Next