anidulafungin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antifungal antibiotics 4357 166663-25-8

Description:

MoleculeDescription

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:

DoseUnitRoute
0.10 g P

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
Sept. 20, 2007 EMA
Feb. 17, 2006 FDA VICURON

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
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 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
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 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
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:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-1,3-glucan synthase catalytic subunit 1 Enzyme INHIBITOR IC50 7.75 CHEMBL CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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