Isavuconazole

製品コードS3722 バッチS372201

化学情報

	Synonyms	BAL-4815, RO-0094815	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₁₇F₂N₅OS
	分子量	437.47	CAS No.	241479-67-4
Solubility (25°C)*	体外	DMSO	87 mg/mL (198.87 mM)
		Ethanol	87 mg/mL (198.87 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Isavuconazole (BAL-4815, RO-0094815) is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi that inhibits cytochrome P450 (CYP)-dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis.
in vitro	Isavuconazole inhibits cytochrome P450 (CYP)–dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis. This blockade produces methylated sterols in the fungal membrane, altering its function and allowing the accumulation of ergosterol toxic precursors in the cytoplasm, which leads to cell death^[1].
in vivo	Isavuconazonium sulfate, the prodrug of isavuconazole, is available in both intravenous and oral formulations. After intravenous infusion, the prodrug is broken down quickly to the active component, isavuconazole, and an inactive cleavage product. Following oral administration, plasma concentrations of the active compound reach maximum concentrations (Cmax) by 2–3 hours; the prodrug and cleavage product are not measurable in plasma after oral administration. In healthy adult volunteers, isavuconazole exhibits linear and dose-proportional pharmacokinetics. The oral bioavailability of isavuconazole is 98%. Absorption of isavuconazole is not affected by food intake. In addition to excellent bioavailability, isavuconazole serum concentrations show low intersubject variability. In healthy volunteers, the Cmax at steady state was 2.5 ± 1.0 µg/mL. Isavuconazole has a large volume of distribution, is >99% protein bound, and has a long terminal half-life of 100-130 hours. Metabolism of isavuconazole takes place in the liver via the CYP enzyme family, specifically CYP3A4 and CYP3A5 isoenzymes^[1].

プロトコル(参考用のみ)

参考

[1] Miceli MH, et al. Clin Infect Dis. 2015, 61(10):1558-65.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Isavuconazonium Sulfate [ J Pharm Sci, 2023, 10.1016/j.xphs.2023.11.005]	PubMed: 37951471

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Isavuconazonium Sulfate [ J Pharm Sci, 2023, 10.1016/j.xphs.2023.11.005]

PubMed: 37951471

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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