All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

oteseconazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
systemic antifungal agents, miconazole derivatives	5510	1340593-59-0

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: oteseconazole vivijoa VT-1161

Oteseconazole is an azole metalloenzyme inhibitor targeting the fungal sterol, 14alpha demethylase(CYP51), an enzyme that catalyzes an early step in the biosynthetic pathway of ergosterol, a sterol required for fungal cell membrane formation and integrity. Inhibition of CYP51 results in the accumulation of 14-methylated sterols, some of which are toxic to fungi. Through the inclusion of a tetrazole metal-binding group, oteseconazole has a lower affinity for human CYP enzymes. Molecular weight: 527.40 Formula: C23H16F7N5O2 CLOGP: 4.97 LIPINSKI: 1 HAC: 7 HDO: 1 TPSA: 85.95 ALOGS: -5.06 ROTB: 9 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
21	mg	O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	4.020		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	2.065		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	36.058	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	3.499	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	0.770	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	2.890	%	High	1
herg	hERG pIC50	5.442	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	2.812	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	3.365	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	0.770	%	High	1
kinase-safety-class	ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PIK3CG	7
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	2.729		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	4.295		High	1
mppb	Mouse plasma protein binding (% unbound)	0.820		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	6.397		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	1
pppb	Pig plasma protein binding (% unbound)	1.370	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	2.065	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	6.650	%	High	1
rppb	Rat plasma protein binding (% unbound)	0.560	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	16.866	uM	High	1

Approvals:

Date	Agency	Company	Orphan
April 26, 2022	FDA	MYCOVIA PHARMACEUTICALS INC

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:

Source	Code	Description
ATC	J02AC06	ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE Triazole and tetrazole derivatives
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000935	Antifungal Agents
FDA CS	M0002083	Azoles
FDA EPC	N0000175487	Azole Antifungal
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
CHEBI has role	CHEBI:35718	antifungal agent
CHEBI has role	CHEBI:86327	antifungal drug

Related Drugs by ATC class:

J02AC Triazole and tetrazole derivatives 5 drugs

fluconazoleisavuconazoniumitraconazoleposaconazolevoriconazole

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

Disease	Relation	SNOMED_ID	DOID
Recurrent vulvovaginal candidiasis (RVVC)	indication	708126004
Lactation	contraindication	63158009
Pregnancy, function	contraindication	289908002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
150MG	VIVJOA	MYCOVIA PHARMS	N215888	April 26, 2022	RX	CAPSULE	ORAL	8754227	April 22, 2031	VIVJOA IS INDICATED TO REDUCE THE INCIDENCE OF RECURRENT VULVOVAGINAL CANDIDIASIS (RVVC) IN FEMALES WITH A HISTORY OF RVVC WHO ARE NOT OF REPRODUCTIVE POTENTIAL
150MG	VIVJOA	MYCOVIA PHARMS	N215888	April 26, 2022	RX	CAPSULE	ORAL	11247981	May 9, 2033	VIVJOA IS INDICATED TO REDUCE THE INCIDENCE OF RECURRENT VULVOVAGINAL CANDIDIASIS (RVVC) IN FEMALES WITH A HISTORY OF RVVC WHO ARE NOT OF REPRODUCTIVE POTENTIAL

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
150MG	VIVJOA	MYCOVIA PHARMS	N215888	April 26, 2022	RX	CAPSULE	ORAL	April 26, 2027	NEW CHEMICAL ENTITY
150MG	VIVJOA	MYCOVIA PHARMS	N215888	April 26, 2022	RX	CAPSULE	ORAL	April 26, 2032	GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN	INHIBITOR	IC50	4.19		SCIENTIFIC LITERATURE
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN	INHIBITOR	IC50	4		SCIENTIFIC LITERATURE
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN	INHIBITOR	IC50	4.14		SCIENTIFIC LITERATURE
Lanosterol 14-alpha demethylase	Enzyme		CP51_CANAL	INHIBITOR	Kd	7.41		SCIENTIFIC LITERATURE	DRUG LABEL

External reference:

ID	Source
CHEBI:188153	CHEBI
VT1	PDB_CHEM_ID
CHEMBL3311228	ChEMBL_ID
C000599187	MESH_SUPPLEMENTAL_RECORD_UI
DB13055	DRUGBANK_ID
4041587	VANDF
C4519300	UMLSCUI
D11785	KEGG_DRUG
10138	INN_ID
77050711	PUBCHEM_CID
40649	MMSL
d09883	MMSL
019048	NDDF
VHH774W97N	UNII
2602577	RXNORM
VHH774W97N	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
VIVJOA	HUMAN PRESCRIPTION DRUG LABEL	1	74695-823	CAPSULE	150 mg	ORAL	NDA	32 sections