カスポファンギン

カスポファンギン 化学特性,用途語,生産方法

• 効能

  抗真菌薬, 細胞壁合成阻害薬

• 使用

  Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat Aspergillus and Candida infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however in vitro resistance development to Caspofungin by Aspergillus species has not been studied.

• 定義

  ChEBI: A semisynthetic cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall.

• 抗菌性

  It is active against Aspergillus spp., Candida spp. and the cyst form of Pn. jirovecii.

• 獲得抵抗性

  This is rare, but resistant strains of C. albicans, C. glabrata and C. parapsilosis have been recovered from patients failing caspofungin treatment. These strains are typically cross-resistant to other echinocandins.

• 応用例（製薬）

  A semisynthetic lipopeptide derived from a fermentation product of Glarea lozoyensis. Formulated as the diacetate for intravenous infusion.

• 作用機序

  Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus species and Candida species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase.

• 薬物動態学

  C_max 70 mg 1-h infusion: c. 10 mg/L 1 h post infusion
  Plasma half-life: 9–11 h
  Volume of distribution: 0.15 L/kg
  Plasma protein binding: 97%
  Blood concentrations increase in proportion to dosage.
  Distribution
  The drug is widely distributed, the highest concentrations being found in the liver. Levels in the CSF are negligible.
  Metabolism and excretion
  It is slowly metabolized by the liver through non-enzymatic peptide hydrolysis and N-acetylation, and the two inactive metabolites are excreted in the feces and bile. No dosage adjustment is required in patients with renal impairment; however, a dose reduction to 35 mg following the 70 mg loading dose is recommended for patients with moderate hepatic impairment. Caspofungin is not cleared by hemodialysis.

• 臨床応用

  Candidemia and certain invasive forms of candidosis
  Esophageal candidosis
  Invasive aspergillosis unresponsive to other antifungal drugs
  Empirical treatment of presumed fungal infections in febrile neutropenic patients

• 副作用

  Occasional histamine-mediated infusion-related reactions, injection site reactions and transient abnormalities of liver enzymes have been reported. Rare cases of significant hepatic dysfunction, hepatitis or worsening liver failure have also been described.

カスポファンギン 生産企業

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カスポファンギン スペクトルデータ(¹HNMR)

162808-62-0, カスポファンギン キーワード