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

Stem definition	Drug id	CAS RN
antifungal antibiotics	4357	166663-25-8

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

anidulafungin
ecalta
eraxis
LY 303366
LY-303366

Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.

Molecular weight: 1140.25
Formula: C58H73N7O17
CLOGP: 2.80
LIPINSKI: 3
HAC: 24
HDO: 14
TPSA: 377.42
ALOGS: -4.31
ROTB: 14

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.10	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.05 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.30 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.57 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.21 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.16 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	40 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 20, 2007	EMA
Feb. 17, 2006	FDA	VICURON

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pathogen resistance	67.00	47.97	17	1080	5672	50598355
Multiple organ dysfunction syndrome	61.03	47.97	27	1070	50310	50553717
Morganella infection	56.76	47.97	10	1087	575	50603452
Haemodynamic instability	56.64	47.97	16	1081	8008	50596019
Haemostasis	50.51	47.97	8	1089	239	50603788

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Candida infection	99.05	42.16	37	1847	15188	29557455
Septic shock	88.78	42.16	53	1831	62507	29510136
Multiple organ dysfunction syndrome	88.34	42.16	53	1831	63063	29509580
Geotrichum infection	85.47	42.16	16	1868	429	29572214
Fungaemia	64.93	42.16	17	1867	2164	29570479
Enterococcal infection	64.52	42.16	23	1861	8245	29564398
Sepsis	53.67	42.16	55	1829	142627	29430016
Aortoenteric fistula	48.95	42.16	8	1876	94	29572549
Scedosporium infection	43.06	42.16	10	1874	775	29571868
Functional gastrointestinal disorder	42.19	42.16	12	1872	2078	29570565

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple organ dysfunction syndrome	136.40	39.67	74	2877	101339	64394442
Septic shock	128.22	39.67	72	2879	105365	64390416
Candida infection	104.86	39.67	43	2908	31376	64464405
Haemodynamic instability	76.82	39.67	28	2923	14884	64480897
Enterococcal infection	75.03	39.67	27	2924	13839	64481942
Geotrichum infection	73.25	39.67	15	2936	903	64494878
Sepsis	71.78	39.67	69	2882	230272	64265509
Fungaemia	70.49	39.67	19	2932	3766	64492015
Pathogen resistance	66.27	39.67	24	2927	12519	64483262
Immunosuppressant drug level increased	58.28	39.67	19	2932	7240	64488541
Trichosporon infection	50.63	39.67	11	2940	881	64494900
Aortoenteric fistula	49.77	39.67	8	2943	120	64495661
Morganella infection	49.31	39.67	11	2940	995	64494786
Drug ineffective	43.90	39.67	109	2842	840138	63655643
Haemostasis	43.58	39.67	8	2943	270	64495511
Graft versus host disease	42.97	39.67	18	2933	13795	64481986
Scedosporium infection	41.68	39.67	10	2941	1244	64494537

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	J02AX06	ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE Other antimycotics for systemic use
FDA CS	M0519359	Lipopeptides
FDA EPC	N0000175507	Echinocandin Antifungal
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000935	Antifungal Agents

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

Disease	Relation	SNOMED_ID	DOID
Candidiasis of the esophagus	indication	20639004	DOID:13146
Candidemia	indication	432261003
Candida Peritonitis	indication
Intra-Abdominal Candida Abscess	indication
Oropharyngeal Candidiasis	off-label use
Liver function tests abnormal	contraindication	166603001
Disease of liver	contraindication	235856003	DOID:409

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.55	acidic
pKa2	11.98	acidic
pKa3	13.18	acidic
pKa4	13.53	acidic
pKa5	13.86	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG/VIAL	ERAXIS	VICURON HOLDINGS	N021632	Nov. 14, 2006	RX	POWDER	INTRAVENOUS	Sept. 22, 2023	NEW PATIENT POPULATION
50MG/VIAL	ERAXIS	VICURON HOLDINGS	N021632	Feb. 17, 2006	RX	POWDER	INTRAVENOUS	Sept. 22, 2023	NEW PATIENT POPULATION

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Beta-1,3-glucan synthase catalytic subunit 1	Enzyme		O13428_CANAX	INHIBITOR	IC50	7.75		CHEMBL	CHEMBL

External reference:

ID	Source
4025092	VUID
N0000175344	NUI
D03211	KEGG_DRUG
4025092	VANDF
C1142738	UMLSCUI
CHEBI:55346	CHEBI
CHEMBL1631577	ChEMBL_ID
CHEMBL264241	ChEMBL_ID
CHEMBL413199	ChEMBL_ID
D000077612	MESH_DESCRIPTOR_UI
DB00362	DRUGBANK_ID
7795	INN_ID
9HLM53094I	UNII
166548	PUBCHEM_CID
341018	RXNORM
21218	MMSL
80828	MMSL
d05767	MMSL
011233	NDDF
421904007	SNOMEDCT_US
422157006	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ERAXIS	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0114	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	50 mg	INTRAVENOUS	NDA	32 sections
ERAXIS	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0116	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	100 mg	INTRAVENOUS	NDA	32 sections