ibrexafungerp 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5462 | 1207753-03-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | J02AX07 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE Other antimycotics for systemic use |
| 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 | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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) |
| EQ 150MG BASE | BREXAFEMME | SCYNEXIS | N214900 | June 1, 2021 | RX | TABLET | ORAL | 11534433 | June 10, 2039 | REDUCTION IN THE INCIDENCE OF RECURRENT VULVOVAGINAL CANDIDIASIS (RVVC) IN ADULT AND POST-MENARCHAL PEDIATRIC FEMALES |
| EQ 150MG BASE | BREXAFEMME | SCYNEXIS | N214900 | June 1, 2021 | RX | TABLET | ORAL | 11534433 | June 10, 2039 | TREATMENT OF ADULT AND POST-MENARCHAL PEDIATRIC FEMALES WITH VULVOVAGINAL CANDIDIASIS (VVC) |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 150MG BASE | BREXAFEMME | SCYNEXIS | N214900 | June 1, 2021 | RX | TABLET | ORAL | Nov. 30, 2025 | REDUCTION IN THE INCIDENCE OF RECURRENT VULVOVAGINAL CANDIDIASIS (RVVC) INADULT AND POST-MENARCHAL PEDIATRIC FEMALES |
| 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:
| 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 | 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:
| ID | Source |
|---|---|
| D11544 | KEGG_DRUG |
| A92JFM5XNU | UNII |
| 1965291-08-0 | SECONDARY_CAS_RN |
| C5206403 | UMLSCUI |
| CHEMBL4297513 | ChEMBL_ID |
| 46871657 | PUBCHEM_CID |
| DB12471 | DRUGBANK_ID |
| CHEMBL4298168 | ChEMBL_ID |
| 10597 | INN_ID |
| 018755 | NDDF |
| 018756 | NDDF |
| 4040654 | VANDF |
| 2560213 | RXNORM |
| 347181 | MMSL |
| 39565 | MMSL |
| d09756 | MMSL |
| C569338 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| BREXAFEMME | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75788-115 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 34 sections |
| BREXAFEMME | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75788-115 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 34 sections |
| BREXAFEMME | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75788-115 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 34 sections |