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

Stem definitionDrug idCAS RN
5462 1207753-03-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ibrexafungerp
  • ibrexafungerp citrate
  • brexafemme
  • SCY-078
  • MK-3118
Ibrexafungerp, a triterpenoid antifungal agent, inhibits glucan synthase, an enzyme involved in the formation of 1,3-beta-D-glucan, an essential component of the fungal cell wall. Ibrexafungerp has concentration-dependent fungicidal activity against Candida species as measured by time kill studies. Ibrexafungerp retains in vitro antifungal activity when tested at pH 4.5 (the normal vaginal pH).
  • Molecular weight: 730.05
  • Formula: C44H67N5O4
  • CLOGP: 6.03
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 2
  • TPSA: 125.38
  • ALOGS: -6.32
  • ROTB: 9

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 1, 2021 FDA SCYNEXIS

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:

SourceCodeDescription
FDA CS M0022020 Triterpenes
FDA MoA N0000020027 Glucan Synthase Inhibitors
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents
FDA EPC N0000193966 Triterpenoid Antifungal

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Vulvovaginal candidiasis indication 72605008 DOID:2272
Candidiasis of vagina indication 72934000
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 150MG BASE BREXAFEMME SCYNEXIS N214900 June 1, 2021 RX TABLET ORAL 8188085 Aug. 28, 2030 TREATMENT OF ADULT AND POST-MENARCHAL PEDIATRIC FEMALES WITH VULVOVAGINAL CANDIDIASIS (VVC)
EQ 150MG BASE BREXAFEMME SCYNEXIS N214900 June 1, 2021 RX TABLET ORAL 10370406 Jan. 19, 2035 TREATMENT OF ADULT AND POST-MENARCHAL PEDIATRIC FEMALES WITH VULVOVAGINAL CANDIDIASIS (VVC)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 150MG BASE BREXAFEMME SCYNEXIS N214900 June 1, 2021 RX TABLET ORAL June 1, 2026 NEW CHEMICAL ENTITY
EQ 150MG BASE BREXAFEMME SCYNEXIS N214900 June 1, 2021 RX TABLET ORAL June 1, 2031 GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-1,3-glucan synthase catalytic subunit 1 Enzyme INHIBITOR IC50 8.35 SCIENTIFIC LITERATURE DRUG LABEL
1,3-Beta-D-glucan-UDP glucosyltransferase Enzyme INHIBITOR IC50 7.83 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
1,3-Beta-D-glucan-UDP glucosyltransferase Enzyme INHIBITOR IC50 8.97 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
D11544 KEGG_DRUG
A92JFM5XNU UNII
C5206403 UMLSCUI
CHEMBL4297513 ChEMBL_ID
46871657 PUBCHEM_CID
DB12471 DRUGBANK_ID
CHEMBL4298168 ChEMBL_ID
2560213 RXNORM
347181 MMSL
39565 MMSL
d09756 MMSL
4040654 VANDF
018755 NDDF
018756 NDDF
C569338 MESH_SUPPLEMENTAL_RECORD_UI
10597 INN_ID
1965291-08-0 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BREXAFEMME HUMAN PRESCRIPTION DRUG LABEL 1 75788-115 TABLET, FILM COATED 150 mg ORAL NDA 29 sections