anidulafungin 🐶 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 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:

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 71.17 43.61 18 1260 6380 63481364
Multiple organ dysfunction syndrome 69.51 43.61 30 1248 56722 63431022
Morganella infection 56.12 43.61 10 1268 661 63487083
Haemodynamic instability 55.64 43.61 16 1262 9174 63478570
Haemostasis 51.00 43.61 8 1270 242 63487502
Septic shock 46.77 43.61 24 1254 66605 63421139

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
Multiple organ dysfunction syndrome 132.38 40.56 74 2179 76492 34878186
Candida infection 96.64 40.56 38 2215 17677 34937001
Septic shock 83.83 40.56 54 2199 71780 34882898
Geotrichum infection 83.28 40.56 16 2237 488 34954190
Drug ineffective 65.92 40.56 110 2143 456641 34498037
Enterococcal infection 65.26 40.56 24 2229 9282 34945396
Fungaemia 61.97 40.56 17 2236 2551 34952127
Aortoenteric fistula 60.95 40.56 10 2243 119 34954559
Sepsis 56.28 40.56 61 2192 166500 34788178
Scedosporium infection 52.32 40.56 12 2241 870 34953808
Rectal perforation 47.84 40.56 10 2243 470 34954208
Haemodynamic instability 43.49 40.56 18 2235 9505 34945173
Systemic candida 43.20 40.56 14 2239 3712 34950966
Spinal cord disorder 42.02 40.56 10 2243 851 34953827
Functional gastrointestinal disorder 41.27 40.56 12 2241 2219 34952459

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 191.99 37.51 97 3399 120149 79620743
Septic shock 133.98 37.51 77 3419 122724 79618168
Candida infection 101.73 37.51 44 3452 38170 79702722
Haemodynamic instability 92.26 37.51 33 3463 17349 79723543
Sepsis 81.68 37.51 78 3418 269350 79471542
Enterococcal infection 76.63 37.51 28 3468 15632 79725260
Drug ineffective 74.15 37.51 152 3344 1080761 78660131
Geotrichum infection 72.89 37.51 15 3481 966 79739926
Pathogen resistance 67.79 37.51 25 3471 14317 79726575
Fungaemia 67.66 37.51 19 3477 4572 79736320
Aortoenteric fistula 63.09 37.51 10 3486 143 79740749
Immunosuppressant drug level increased 55.00 37.51 19 3477 9008 79731884
Systemic candida 52.31 37.51 17 3479 6689 79734203
Scedosporium infection 50.74 37.51 12 3484 1466 79739426
Trichosporon infection 49.75 37.51 11 3485 997 79739895
Morganella infection 48.53 37.51 11 3485 1116 79739776
Rectal perforation 45.35 37.51 10 3486 895 79739997
Mucormycosis 44.62 37.51 16 3480 8453 79732439
Graft versus host disease 42.24 37.51 18 3478 15008 79725884
Haemostasis 40.97 37.51 8 3488 394 79740498
Drug resistance 39.42 37.51 24 3472 42189 79698703
Spinal cord disorder 38.32 37.51 10 3486 1825 79739067

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

DiseaseRelationSNOMED_IDDOID
Candidiasis of the esophagus indication 20639004 DOID:13146
Disseminated candidiasis indication 70572005
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 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 0049-0114 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
ERAXIS HUMAN PRESCRIPTION DRUG LABEL 1 0049-0116 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS NDA 32 sections