Peringatan Keamanan

During clinical studies, no cases of rezafungin overdose were reported. Since rezafungin is highly protein bound, it is not anticipated to be dialyzable. In non-clinical studies, rezafungin did not show evidence of mutagenicity in a standard battery of assays, and did not affect mating or fertility in male or female rats given up to 45 mg/kg of rezafungin intravenously (6 times the clinical exposure) every 3 days. At doses greater or equal than 30 mg/kg of rezafungin, male mice presented lower sperm motility, and at 45 mg/kg, they had mild/moderate hypospermia and no detectable motile sperm. In rats given 45 mg/kg of rezafungin intravenously every 3 days for 3 months, males showed minimal tubular degeneration/atrophy in the testes and cellular debris in the epididymides at the end of the study. The carcinogenicity of rezafungin has not been evaluated in non-clinical studies.L45633

Rezafungin

DB16310

small molecule approved investigational

Deskripsi

Rezafungin is an echinocandin antifungal drug.A258393,L45633 Unlike other echinocandins such as caspofungin and micafungin, rezafungin has long?acting pharmacokinetics and a high stability that allows for it to have long dosing intervals maintaining high plasma exposure. Rezafungin has a half-life higher than 130 hours and can be administered once a week instead of daily. It can only be administered intravenously but does not reach therapeutic concentrations in the central nervous system, eye and urine.A258393,A258398 Rezafungin is active against Candida albicans, Candida glabrata, Candida parapsilosis and Candida tropicalis, as well as other Candida and Aspergillus spp.A258398,L45633

Clinical studies have shown that rezafungin is non-inferior to caspofungin for the treatment of candidaemia and invasive candidiasis.A258403 In March 2023, the FDA approved rezafungin for injection for the treatment of candidemia and invasive candidiasis in adults with limited or no alternative treatment options.L45633,L45658

Struktur Molekul 2D

Berat 1226.411
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Rezafungin has a terminal half-life of 152 hours.[L45633]
Volume Distribusi Rezafungin has a volume of distribution of 67 L.[L45633]
Klirens (Clearance) Rezafungin has an elimination clearance of 0.35 L/hr.[L45633]

Absorpsi

Between 50 mg (0.125 times the approved maximum recommended loading dose) and 400 mg and with single or multiple doses, the Cmax and AUC of rezafungin increase in a dose-proportional manner. In patients with candidemia and invasive candidias given an initial 400 mg loading dose of rezafungin, followed by a 200 mg dose once weekly, the Cmax, AUC from time zero to 168 hours post-dose (AUC0-168) and Cmin on day 1 were 19.2 mcg/mL, 827 mcg?h/mL and 2.4 mcg/mL, respectively. In the same group of patients, the Cmax, AUC0-168 and Cmin on day 15 were 11.8 mcg/mL, 667 mcg?h/mL and 2.2 mcg/mL, respectively. Compared to healthy subjects, the AUC0-168 and Cmax were 30% and 19% lower in patients with candidemia. Age, sex, race, weight and hepatic impairment did not have a clinically significant effect on rezafungin pharmacokinetics.L45633

Metabolisme

Rezafungin is metabolized by hydroxylation of the terphenyl, pentyl ether side chain, to form three hydroxylated metabolite isomers: 2’-, 3?-, or 4’-hydroxylpentyl rezafungin. Rezafungin can also be metabolized through a reaction that involves the loss of the pentyl group via O-dealkylation, forming despentyl-rezafungin. There is minimal subsequent conjugation (sulfation) of the hydroxyl metabolites.A258408 Rezafungin is not metabolized in the liver and is not expected to be a clinically relevant substrate of CYP450 enzymes.L45633

Rute Eliminasi

Rezafungin is mainly eliminated through fecal excretion. In healthy subjects, 74.3% was recovered in feces primarily as rezafungin, while 25.7% was recovered in urine primarily as inactive metabolites of rezafungin.L45633

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

1,3-beta-glucan synthase component FKS1 fksA
1,3-beta-glucan synthase component GSC2 GSC2

Referensi & Sumber

Synthesis reference: Hughes, D., et al. (2022). Synthesis of echinocandin antifungal agent. (U.S. Patent No. 11,524,980 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/34/d5/c2/1a8cdcfb3fe3db/US11524980.pdf
Artikel (PubMed)
  • PMID: 36855391
    Lamoth F: Novel Therapeutic Approaches to Invasive Candidiasis: Considerations for the Clinician. Infect Drug Resist. 2023 Feb 22;16:1087-1097. doi: 10.2147/IDR.S375625. eCollection 2023.
  • PMID: 31763045
    Miesel L, Lin KY, Ong V: Rezafungin treatment in mouse models of invasive candidiasis and aspergillosis: Insights on the PK/PD pharmacometrics of rezafungin efficacy. Pharmacol Res Perspect. 2019 Nov 20;7(6):e00546. doi: 10.1002/prp2.546. eCollection 2019 Dec.
  • PMID: 36442484
    Thompson GR 3rd, Soriano A, Cornely OA, Kullberg BJ, Kollef M, Vazquez J, Honore PM, Bassetti M, Pullman J, Chayakulkeeree M, Poromanski I, Dignani C, Das AF, Sandison T, Pappas PG: Rezafungin versus caspofungin for treatment of candidaemia and invasive candidiasis (ReSTORE): a multicentre, double-blind, double-dummy, randomised phase 3 trial. Lancet. 2023 Jan 7;401(10370):49-59. doi: 10.1016/S0140-6736(22)02324-8. Epub 2022 Nov 25.
  • PMID: 34662192
    Ong V, Wills S, Watson D, Sandison T, Flanagan S: Metabolism, Excretion, and Mass Balance of (14)C-Rezafungin in Animals and Humans. Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0139021. doi: 10.1128/AAC.01390-21. Epub 2021 Oct 18.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Rezzayo
    Injection, powder, for solution • 200 mg • Intravenous • EU • Approved
  • Rezzayo
    Injection, powder, lyophilized, for solution • 200 mg/1 • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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