生物活性

• 描述Anidulafungin, a new echinocandin, has potent activity against candida species. Anidulafungin was shown to be noninferior to fluconazole in the treatment of invasive candidiasis^[3]. As other echinocandins, it inhibits a selective target, 1,3- beta-D-glucan synthesis, a major structural component of the fungal cell wall which is not present in mammalian cells, this avoiding toxicity problems. It has fungicidal activity against many Candida spp., including fluconazole-resistant, and fungistatic activity against other yeast and moulds such as Aspergillus spp. As it does not interact with amphotericin B and voriconazole, cyclosporine, tacrolimus and other drugs, it can be used in combination with other antifungal agents and co-administered with immunosuppressant drugs. It is generally well-tolerated in clinical trials. Its most frequent adverse events are nausea, vomiting, moderate diarrhea, transient elevation of hepatic enzymes and headache^[4]. A 48 hours exposure of human erythrocytes to Anidulafungin (1.5 - 6 µg/ml) significantly increased hemolysis and the percentage of annexin-V-binding cells, and significantly decreased forward scatter. Anidulafungin (6 µg/ml) slightly, but significantly inceased Fluo3-fluorescence and the effect of Anidulafungin on annexin-V-binding was slightly, but significantly blunted by removal of extracellular Ca2+^[5]. In obese and normal-weight subjects, weight influenced both of the anidulafungin pharmacokinetic parameters clearance and volume of distribution, implying a lower exposure to anidulafungin in (morbidly) obese individuals^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01236261	-	-	Completed	-	Spain ... more >> Hospital Sant Joan de Dèu Esplugues de Llobregat, Barcelona, Spain, 08950 Hospital Fundación de Alcorcón Alcorcón, Madrid, Spain, 28922 Hospital Puerta de Hierro Majadahonda Majadahonda, Madrid, Spain, 28222 Hospital San Juan de Dios del Aljarafe Bormujos, Seville, Spain, 41930 Hospital de Cruces Baracaldo, Vizcaya, Spain, 48903 Hospital de Basurto Basurto, Vizcaya, Spain, 48013 Hospital de Galdakao-Usansolo Galdakao, Vizcaya, Spain, 48960 Hospital del Mar Barcelona, Spain, 08003 Hospital de Barcelona Barcelona, Spain, 08034 Hospital Vall d'Hebrón Barcelona, Spain, 08035 Hospital Clinic i Provincial Barcelona, Spain, 08036 Hospital de la Santa Creu i Sant Pau Barcelona, Spain, 08041 Hospital de la Princesa Madrid, Spain, 28006 Hospital Gregorio Marañon Madrid, Spain, 28007 Hospital del Niño Jesús Madrid, Spain, 28009 Hospital Infanta Leonor Madrid, Spain, 28032 Hospital Ramon y Cajal Madrid, Spain, 28034 Fundación Jiménez Díaz Madrid, Spain, 28040 Hospital Clínico San Carlos Madrid, Spain, 28040 Hospital 12 de Octubre Madrid, Spain, 28041 Hospital La Paz Madrid, Spain, 28046 Hospital Virgen de Macarena Seville, Spain, 41009 Clínica Sagrado Corazón Seville, Spain, 41013 Hospital Virgen del Rocío Seville, Spain, 41013 Hospital Nuestra Señora de Valme Seville, Spain, 41014 Hospital La Fe Valencia, Spain, 46009 Hospital Clínico de Valencia Valencia, Spain, 46010 Hospital General de Valencia Valencia, Spain, 46014 Hospital Doctor Peset Valencia, Spain, 46017 Collapse <<
  NCT00491426	-	-	Completed	-	United States, California ... more >> University of California at San Diego La Jolla, California, United States, 92103 United States, District of Columbia Children's National Medical Center Washington, District of Columbia, United States, 20010 United States, Kentucky Kosair Children's Hospital Louisville, Kentucky, United States, 40202 United States, Michigan Children's Hospital of Michigan, Wayne State University Detroit, Michigan, United States, 48201 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27705 United States, Texas University of Texas Southwestern Medical Center Dallas, Texas, United States, 75235 Collapse <<
  NCT01174147	-	-	Completed	-	-

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• 参考文献

• [1] Locke JB, Almaguer AL, et al. Characterization of In Vitro Resistance Development to the Novel Echinocandin CD101 in Candida Species. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6100-7.

  [2] Zhanel GG, Karlowsky JA, et al. In vitro activity of a new semisynthetic echinocandin, LY-303366, against systemic isolates of Candida species, Cryptococcus neoformans, Blastomyces dermatitidis, and Aspergillus species. Antimicrob Agents Chemother. 1997 Apr;41(4):863-5.

  [3] Reboli AC, Rotstein C, Pappas PG, et al. Anidulafungin versus fluconazole for invasive candidiasis. N Engl J Med. 2007;356(24):2472‐2482

  [4] Gobernado M, Cantón E. Anidulafungina [Anidulafungin]. Rev Esp Quimioter. 2008;21(2):99‐114

  [5] Peter T, Bissinger R, Liu G, Lang F. Anidulafungin-Induced Suicidal Erythrocyte Death. Cell Physiol Biochem. 2016;38(6):2272‐2284

  [6] Wasmann RE, Ter Heine R, van Dongen EP, et al. Pharmacokinetics of Anidulafungin in Obese and Normal-Weight Adults. Antimicrob Agents Chemother. 2018;62(7):e00063-18. Published 2018 Jun 26

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