ホスフルコナゾール

ホスフルコナゾール 価格

メーカー	製品番号	製品説明	CAS番号	包装	価格	更新時間	購入

ホスフルコナゾール 化学特性,用途語,生産方法

効能

抗真菌薬, エルゴステロール合成阻害薬

商品名

プロジフ (ファイザー)

説明

Fosfluconazole is a phosphate prodrug of fluconazole, and it was launched in Japan as an intravenous injection for the treatment of candidiasis and cryptococcosis infections. Fluconazole, a triazole antifungal agent, is a selective inhibitor of fungal cytochrome P450 sterol C-14 alpha-demethylation, and it is widely used for the treatment of patients with serious systemic fungal infections. Fluconazole is marketed in both oral and intravenous formulations, the latter being a dilute (2 mg/ mL) infusion in saline due to the relatively poor water solubility of the drug. In patients needing high doses (＞400 mg) of fluconazole, a drawback of the IV formulation is the requirement of a high-volume infusion, which is undesirable in critically ill patients in whom fluid overload must be avoided. Fosfluconazole is a prodrug with approximately 40-fold higher water solubility than fluconazole, thereby achieving a substantial reduction in infusion volume. It is prepared in three steps starting from fluconazole. In the first step, fluconazole is converted to its dibenzyl phosphite derivative by reaction with phosphorous trichloride and benzyl alcohol. Subsequent oxidation of the phosphite to the corresponding phosphate with hydrogen peroxide and cleavage of the benzyl protecting groups by hydrogenolysis affords fosfluconazole. In vitro, fosfluconazole is at least 25-fold less potent than fluconazole against single isolates of Candida species and Cryptococcus neoformans. In vivo, it is rapidly hydrolyzed to fluconazole by phosphatase enzymes and exhibits similar efficacy to fluconazole in experimental models of fungal disease. The hydrolysis potential of fosfluconazole was initially demonstrated in homogenates of kidney, lung and liver of rat, dog, and human. Subsequently, in clinical trials with healthy volunteers (n＝24), fosfluconazole was shown to hydrolyze rapidly and almost completely to provide a 97% mean bioavailability of fluconazole. Less than 1% of the administered dose of fosfluconazole was excreted unchanged in the urine, with the majority (85.6%) of the dose eliminated as fluconazole. The terminal half-life was about 2.3 hours, and the volume of distribution was 0.2 L/kg. The time to reach steady state drug levels with 500 mg daily dose was about 10 days, which could be shortened to 3 days by administering loading doses of 1000 mgs on days 1 and 2 followed by 500 mg daily. Further studies showed that hepatic or renal impairment did not significantly alter the pharmacokinetic profile of fosfluconazole. In phase III studies in patients with deep-seated mycosis due to Candida or Cryptococcus (n＝160), a 2-day loading dose regimen of fosfluconazole provided efficacy range of 73.8% (in Japanese patients) to 91.7% (patients of non-Japanese origin). The adverse events seen in these trials were similar to those previously known with fluconazole therapy and included rash (3.1%), abnormal liver function values (2.5%), asthma (1.9%), and lightheadedness (1.9%).

Originator

Pfizer (Japan)

brand name

Prodif

ホスフルコナゾール 上流と下流の製品情報

原材料

準備製品

ホスフルコナゾール 生産企業

名前	電話番号	電子メール	国籍	製品カタログ	優位度
Nanjing ChemLin Chemical Industry Co., Ltd.	025-83697070	product@chemlin.com.cn	CHINA	3012	60
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
SIMAGCHEM CORP	+86-13806087780	sale@simagchem.com	China	17367	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
Hefei Hirisun Pharmatech Co., Ltd	+8615056975894	shawn@hirisunpharm.com	CHINA	9923	58
Dayang Chem (Hangzhou) Co.,Ltd.	571-88938639 +8617705817739	info@dycnchem.com	CHINA	52867	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418684 +8618949823763	sales@tnjchem.com	China	25363	58

194798-83-9(ホスフルコナゾール)キーワード:

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• 194798-83-9
• 2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propyl dihydrogen phosphate
• Prodif
• Fosfluconazole, >=98%
• PHARMA PRODUCT FLUCONAZOLE USP 2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1,2,4-TRIAZOL-1-YL) PROPAN-2-OL
• Dihydrogen phosphate ester
• CS-969
• Fosfluconazole(INN)
• 1H-1,2,4-Triazole-1-ethanol, α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-ylmethyl)-, 1-(dihydrogen phosphate)
• 1H-1,2,4-Triazole-1-ethanol, a-(2,4-difluorophenyl)-a-(1H-1,2,4-triazol-1-ylmethyl)-,1-(dihydrogen phosphate)
• Fungal,Inhibitor,Fosfluconazole,inhibit
• 2-(2,4-Difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-yl dihydrogen phosphate (Efinaconazole?Impurity)
• Fosfluconazol
• ホスフルコナゾール
• ホスフルコナゾール (JAN)
• プロジフ
• りん酸二水素1-(2,4-ジフルオロフェニル)-2-(1H-1,2,4-トリアゾール-1-イル)-1-(1H-1,2,4-トリアゾール-1-イルメチル)エチル
• リン酸=二水素=1-(2,4-ジフルオロフェニル)-2-(1,2,4-トリアゾール-1-イル)-1-(1,2,4-トリアゾール-1-イルメチル)エチル
• りん酸α,α-ビス(1H-1,2,4-トリアゾール-1-イルメチル)-2,4-ジフルオロベンジル
• {[2-(2,4-ジフルオロフェニル)-1,3-ビス(1H-1,2,4-トリアゾール-1-イル)プロパン-2-イル]オキシ}ホスホン酸
• りん酸α,α-ビス[(1H-1,2,4-トリアゾール-1-イル)メチル]-2,4-ジフルオロベンジル
• フォスフルコナゾール
• 2,4-ジフルオロ-α,α-ビス(1H-1,2,4-トリアゾール-1-イルメチル)ベンゼンメタノール=二水素ホスファート
• ホスホフルコナゾール