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二氢乳清酸脱氢酶抑制剂 F901318 对枝顶孢属和 prolificans 属具有很强的体外活性。

Dihydroorotate dehydrogenase inhibitor F901318 has potent in vitro activity against Scedosporium species and Lomentospora prolificans.

机构信息

Fungus Testing Laboratory, Department of Pathology, University of Texas Health Science Center at San Antonio, San Antonio, TX, USA.

F2G Limited, Manchester, UK.

出版信息

J Antimicrob Chemother. 2017 Jul 1;72(7):1977-1980. doi: 10.1093/jac/dkx065.

DOI:10.1093/jac/dkx065
PMID:28333310
Abstract

BACKGROUND

Scedosporium species and Lomentospora prolificans are increasing causes of invasive infections in immunocompromised hosts and many isolates are resistant to available antifungals. Our objective was to assess the in vitro potency of F901318, a member of the orotomide class of antifungals, against Scedosporium species and L. prolificans .

METHODS

The in vitro potency of F901318 was evaluated against 66 Scedosporium and 7 L. prolificans clinical isolates using the CLSI M38-A2 reference standard. Scedosporium species included Scedosporium apiospermum ( n  =   43), Scedosporium aurantiacum ( n  =   6), Scedosporium dehoogii ( n  =   2) and Scedosporium boydii ( n  =   15). Positive comparators included amphotericin B, caspofungin, posaconazole and voriconazole.

RESULTS

Against S. apiospermum and S. boydii F901318 geometric mean MICs/MECs (0.079 and 0.046 mg/L, respectively) were significantly lower than those observed with amphotericin (3.404 and 5.595 mg/L), posaconazole (1.937 and 1.823 mg/L), voriconazole (0.784 and 0.630 mg/L) and caspofungin (5.703 and 7.639 mg/L) ( P  <   0.001). Against S. aurantiacum and S. dehoogii the F901318 MIC range (0.12-0.5 mg/L) was also lower than those for the other antifungals (0.5 to >8 mg/L). F901318 also maintained activity against L. prolificans isolates (range 0.12-0.25 mg/L) in contrast to other antifungals, of which none demonstrated in vitro activity.

CONCLUSIONS

F901318 demonstrated potent in vitro activity against Scedosporium species and L. prolificans . This activity was maintained against isolates that had significantly reduced susceptibility to the other antifungals. Further studies are warranted to evaluate the in vivo efficacy of F901318 against Scedosporium species and L. prolificans .

摘要

背景

帚霉属和繁茂枝霉属是免疫功能低下宿主侵袭性感染的日益增多的原因,许多分离株对现有抗真菌药物具有耐药性。我们的目的是评估 F901318(一种属于奥托米德类抗真菌药物)对帚霉属和繁茂枝霉属的体外效力。

方法

使用 CLSI M38-A2 参考标准评估 F901318 对 66 株帚霉属和 7 株繁茂枝霉属临床分离株的体外效力。帚霉属包括棘孢木霉(n = 43)、橘青霉(n = 6)、德霍氏帚霉(n = 2)和博伊德帚霉(n = 15)。阳性对照包括两性霉素 B、卡泊芬净、泊沙康唑和伏立康唑。

结果

与两性霉素 B、泊沙康唑、伏立康唑和卡泊芬净相比,F901318 对棘孢木霉和博伊德帚霉的几何平均 MIC/MEC 值(分别为 0.079 和 0.046 mg/L)显著降低(分别为 3.404 和 5.595 mg/L、1.937 和 1.823 mg/L、0.784 和 0.630 mg/L 和 5.703 和 7.639 mg/L)(P < 0.001)。对于橘青霉和德霍氏帚霉,F901318 的 MIC 范围(0.12-0.5 mg/L)也低于其他抗真菌药物(0.5 至 >8 mg/L)。F901318 对繁茂枝霉属分离株也保持活性(范围 0.12-0.25 mg/L),而其他抗真菌药物则无体外活性。

结论

F901318 对帚霉属和繁茂枝霉属表现出强大的体外活性。这种活性在对其他抗真菌药物敏感性显著降低的分离株中得到维持。需要进一步研究评估 F901318 对帚霉属和繁茂枝霉属的体内疗效。

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