Peringatan Keamanan

Data regarding overdoses of ibrexafungerp are not readily available, however patients did take higher than recommended doses in clinical trials without significant adverse effects.L34349 Patients experiencing an overdose of ibrexafungerp may experience and increased risk and severity of adverse effects. Patients should be treated with symptomatic and supportive measures.L34349

Ibrexafungerp

DB12471

small molecule approved investigational

Deskripsi

Ibrexafungerp, also known as SCY-078 or MK-3118, is a novel enfumafungin derivative oral triterpene antifungal approved for the treatment of vulvovaginal candidiasis (VVC), also known as a vaginal yeast infection.A235384,L34349 It was developed out of a need to treat fungal infections that may have become resistant to echinocandins or azole antifungals.A235384 Ibrexafungerp is orally bioavailable compared to the echinocandins caspofungin, micafungin, and anidulafungin; which can only be administered parenterally.A235384,A235389 Similar to echinocandins, ibrexafungerp targets the fungal ?-1,3-glucan synthase, which is not present in humans, limiting the chance of renal or hepatic toxicity.A235414,L34349

Ibrexafungerp was granted FDA approval on 1 June 2021.L34349

Struktur Molekul 2D

Berat 730.051
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life of ibrexafungerp is approximately 20 hours.[A235614,L34349]
Volume Distribusi The volume of distribution at steady state is approximately 600 L.[L34349]
Klirens (Clearance) Clearance values of 53.6 L/h and 56.1 L/h have been reported.[A235614]

Absorpsi

Ibrexafungerp given at a dose of 300 mg twice daily reaches a Cmax of 435 ng/mL, with a Tmax of 4-6 hours, and an AUC0-24 of 6832 h\*ng/mL.A235614,L34349

Metabolisme

Ibrexafungerp is hydroxylated by CYP3A4 before glucuronide or sulfate conjugation of the hydroxyl group before elimination.A235619,L34349

Rute Eliminasi

90% of a radiolabelled oral dose of ibrexafungerp is recovered in the feces, with 51% as the unchanged parent drug.L34349 1% of a radiolabelled oral dose is recovered in the urine.L34349

Interaksi Makanan

1 Data
  • 1. Take with or without food. A high fat meal increases the AUC by 38% and Cmax by 32%, which is not considered significant.

Interaksi Obat

130 Data
Dicoumarol The therapeutic efficacy of Dicoumarol can be increased when used in combination with Ibrexafungerp.
Phenindione The therapeutic efficacy of Phenindione can be increased when used in combination with Ibrexafungerp.
Warfarin The therapeutic efficacy of Warfarin can be increased when used in combination with Ibrexafungerp.
Phenprocoumon The therapeutic efficacy of Phenprocoumon can be increased when used in combination with Ibrexafungerp.
Acenocoumarol The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Ibrexafungerp.
4-hydroxycoumarin The therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Ibrexafungerp.
Coumarin The therapeutic efficacy of Coumarin can be increased when used in combination with Ibrexafungerp.
(R)-warfarin The therapeutic efficacy of (R)-warfarin can be increased when used in combination with Ibrexafungerp.
Ethyl biscoumacetate The therapeutic efficacy of Ethyl biscoumacetate can be increased when used in combination with Ibrexafungerp.
Fluindione The therapeutic efficacy of Fluindione can be increased when used in combination with Ibrexafungerp.
Clorindione The therapeutic efficacy of Clorindione can be increased when used in combination with Ibrexafungerp.
Diphenadione The therapeutic efficacy of Diphenadione can be increased when used in combination with Ibrexafungerp.
Tioclomarol The therapeutic efficacy of Tioclomarol can be increased when used in combination with Ibrexafungerp.
(S)-Warfarin The therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Ibrexafungerp.
Efavirenz The serum concentration of Ibrexafungerp can be decreased when it is combined with Efavirenz.
Bexarotene The serum concentration of Ibrexafungerp can be decreased when it is combined with Bexarotene.
Bosentan The serum concentration of Ibrexafungerp can be decreased when it is combined with Bosentan.
Nafcillin The serum concentration of Ibrexafungerp can be decreased when it is combined with Nafcillin.
Modafinil The serum concentration of Ibrexafungerp can be decreased when it is combined with Modafinil.
Etravirine The serum concentration of Ibrexafungerp can be decreased when it is combined with Etravirine.
Avasimibe The serum concentration of Ibrexafungerp can be decreased when it is combined with Avasimibe.
Echinacea The serum concentration of Ibrexafungerp can be decreased when it is combined with Echinacea.
Dexamethasone acetate The serum concentration of Ibrexafungerp can be decreased when it is combined with Dexamethasone acetate.
Nelfinavir The serum concentration of Ibrexafungerp can be increased when it is combined with Nelfinavir.
Terfenadine The serum concentration of Ibrexafungerp can be increased when it is combined with Terfenadine.
Ritonavir The serum concentration of Ibrexafungerp can be increased when it is combined with Ritonavir.
Voriconazole The serum concentration of Ibrexafungerp can be increased when it is combined with Voriconazole.
Ergotamine The serum concentration of Ibrexafungerp can be increased when it is combined with Ergotamine.
Delavirdine The serum concentration of Ibrexafungerp can be increased when it is combined with Delavirdine.
Methimazole The serum concentration of Ibrexafungerp can be increased when it is combined with Methimazole.
Conivaptan The serum concentration of Ibrexafungerp can be increased when it is combined with Conivaptan.
Tipranavir The serum concentration of Ibrexafungerp can be increased when it is combined with Tipranavir.
Telithromycin The serum concentration of Ibrexafungerp can be increased when it is combined with Telithromycin.
Ketoconazole The serum concentration of Ibrexafungerp can be increased when it is combined with Ketoconazole.
Atazanavir The serum concentration of Ibrexafungerp can be increased when it is combined with Atazanavir.
Econazole The serum concentration of Ibrexafungerp can be increased when it is combined with Econazole.
Nefazodone The serum concentration of Ibrexafungerp can be increased when it is combined with Nefazodone.
Itraconazole The serum concentration of Ibrexafungerp can be increased when it is combined with Itraconazole.
Clarithromycin The serum concentration of Ibrexafungerp can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Ibrexafungerp can be increased when it is combined with Saquinavir.
Posaconazole The serum concentration of Ibrexafungerp can be increased when it is combined with Posaconazole.
Darunavir The serum concentration of Ibrexafungerp can be increased when it is combined with Darunavir.
Danazol The serum concentration of Ibrexafungerp can be increased when it is combined with Danazol.
Lopinavir The serum concentration of Ibrexafungerp can be increased when it is combined with Lopinavir.
Ditiocarb The serum concentration of Ibrexafungerp can be increased when it is combined with Ditiocarb.
Nilotinib The serum concentration of Ibrexafungerp can be increased when it is combined with Nilotinib.
Telaprevir The serum concentration of Ibrexafungerp can be increased when it is combined with Telaprevir.
Lonafarnib The serum concentration of Ibrexafungerp can be increased when it is combined with Lonafarnib.
Boceprevir The serum concentration of Ibrexafungerp can be increased when it is combined with Boceprevir.
Elvitegravir The serum concentration of Ibrexafungerp can be increased when it is combined with Elvitegravir.
Stiripentol The serum concentration of Ibrexafungerp can be increased when it is combined with Stiripentol.
Curcumin The serum concentration of Ibrexafungerp can be increased when it is combined with Curcumin.
Ribociclib The serum concentration of Ibrexafungerp can be increased when it is combined with Ribociclib.
Danoprevir The serum concentration of Ibrexafungerp can be increased when it is combined with Danoprevir.
Troleandomycin The serum concentration of Ibrexafungerp can be increased when it is combined with Troleandomycin.
Indinavir The serum concentration of Ibrexafungerp can be increased when it is combined with Indinavir.
Amprenavir The serum concentration of Ibrexafungerp can be increased when it is combined with Amprenavir.
Amiodarone The serum concentration of Ibrexafungerp can be increased when it is combined with Amiodarone.
Midostaurin The serum concentration of Ibrexafungerp can be decreased when it is combined with Midostaurin.
Phenytoin The serum concentration of Ibrexafungerp can be decreased when it is combined with Phenytoin.
Pentobarbital The serum concentration of Ibrexafungerp can be decreased when it is combined with Pentobarbital.
Carbamazepine The serum concentration of Ibrexafungerp can be decreased when it is combined with Carbamazepine.
Mitotane The serum concentration of Ibrexafungerp can be decreased when it is combined with Mitotane.
Primidone The serum concentration of Ibrexafungerp can be decreased when it is combined with Primidone.
Rimexolone The serum concentration of Ibrexafungerp can be decreased when it is combined with Rimexolone.
Rifampin The serum concentration of Ibrexafungerp can be decreased when it is combined with Rifampicin.
Phenobarbital The serum concentration of Ibrexafungerp can be decreased when it is combined with Phenobarbital.
Dexamethasone The serum concentration of Ibrexafungerp can be decreased when it is combined with Dexamethasone.
Fosphenytoin The serum concentration of Ibrexafungerp can be decreased when it is combined with Fosphenytoin.
St. John's Wort The serum concentration of Ibrexafungerp can be decreased when it is combined with St. John's Wort.
Enzalutamide The serum concentration of Ibrexafungerp can be decreased when it is combined with Enzalutamide.
Lumacaftor The serum concentration of Ibrexafungerp can be decreased when it is combined with Lumacaftor.
Apalutamide The serum concentration of Ibrexafungerp can be decreased when it is combined with Apalutamide.
Cyclosporine The metabolism of Ibrexafungerp can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Ibrexafungerp can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Ibrexafungerp can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Ibrexafungerp can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Ibrexafungerp can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Ibrexafungerp can be decreased when combined with Isradipine.
Diltiazem The metabolism of Ibrexafungerp can be decreased when combined with Diltiazem.
Clozapine The metabolism of Ibrexafungerp can be decreased when combined with Clozapine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Ibrexafungerp.
Ciprofloxacin The metabolism of Ibrexafungerp can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Ibrexafungerp can be decreased when combined with Nicardipine.
Verapamil The metabolism of Ibrexafungerp can be decreased when combined with Verapamil.
Aprepitant The metabolism of Ibrexafungerp can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Ibrexafungerp can be decreased when combined with Isoniazid.
Primaquine The metabolism of Ibrexafungerp can be decreased when combined with Primaquine.
Miconazole The metabolism of Ibrexafungerp can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Ibrexafungerp can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Ibrexafungerp can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Ibrexafungerp can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Ibrexafungerp can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Ibrexafungerp can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Ibrexafungerp can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Ibrexafungerp can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Ibrexafungerp can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Ibrexafungerp can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Ibrexafungerp can be decreased when combined with Linagliptin.
Indalpine The metabolism of Ibrexafungerp can be decreased when combined with Indalpine.

Target Protein

1,3-beta-glucan synthase component GSC2 GSC2
GTP-binding protein RHO1 RHO1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28137806
    Wring SA, Randolph R, Park S, Abruzzo G, Chen Q, Flattery A, Garrett G, Peel M, Outcalt R, Powell K, Trucksis M, Angulo D, Borroto-Esoda K: Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis. Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: AAC.02068-16. doi: 10.1128/AAC.02068-16. Print 2017 Apr.
  • PMID: 21787240
    Hector RF, Bierer DE: New beta-glucan inhibitors as antifungal drugs. Expert Opin Ther Pat. 2011 Oct;21(10):1597-610. doi: 10.1517/13543776.2011.603899. Epub 2011 Jul 25.
  • PMID: 30051576
    Kuhnert E, Li Y, Lan N, Yue Q, Chen L, Cox RJ, An Z, Yokoyama K, Bills GF: Enfumafungin synthase represents a novel lineage of fungal triterpene cyclases. Environ Microbiol. 2018 Sep;20(9):3325-3342. doi: 10.1111/1462-2920.14333. Epub 2018 Sep 13.
  • PMID: 30885896
    Larkin EL, Long L, Isham N, Borroto-Esoda K, Barat S, Angulo D, Wring S, Ghannoum M: A Novel 1,3-Beta-d-Glucan Inhibitor, Ibrexafungerp (Formerly SCY-078), Shows Potent Activity in the Lower pH Environment of Vulvovaginitis. Antimicrob Agents Chemother. 2019 Apr 25;63(5). pii: AAC.02611-18. doi: 10.1128/AAC.02611-18. Print 2019 May.
  • PMID: 16835448
    Ha YS, Covert SF, Momany M: FsFKS1, the 1,3-beta-glucan synthase from the caspofungin-resistant fungus Fusarium solani. Eukaryot Cell. 2006 Jul;5(7):1036-42. doi: 10.1128/EC.00030-06.
  • PMID: 26190298
    Perlin DS: Mechanisms of echinocandin antifungal drug resistance. Ann N Y Acad Sci. 2015 Sep;1354:1-11. doi: 10.1111/nyas.12831. Epub 2015 Jul 17.
  • PMID: 29947477
    Wring S, Murphy G, Atiee G, Corr C, Hyman M, Willett M, Angulo D: Clinical Pharmacokinetics and Drug-Drug Interaction Potential for Coadministered SCY-078, an Oral Fungicidal Glucan Synthase Inhibitor, and Tacrolimus. Clin Pharmacol Drug Dev. 2019 Jan;8(1):60-69. doi: 10.1002/cpdd.588. Epub 2018 Jun 27.
  • PMID: 32854252
    Ghannoum M, Arendrup MC, Chaturvedi VP, Lockhart SR, McCormick TS, Chaturvedi S, Berkow EL, Juneja D, Tarai B, Azie N, Angulo D, Walsh TJ: Ibrexafungerp: A Novel Oral Triterpenoid Antifungal in Development for the Treatment of Candida auris Infections. Antibiotics (Basel). 2020 Aug 25;9(9). pii: antibiotics9090539. doi: 10.3390/antibiotics9090539.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Brexafemme
    Tablet, film coated • 150 mg/1 • Oral • US • Approved
International Brands
  • Brexafemme — Scynexis, Inc.

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