Perlin David S
Public Health Research Institute, New Jersey Medical School, Rutgers, The State University of New Jersey, Newark, NJ, 07103, USA,
Drugs. 2014 Sep;74(14):1573-85. doi: 10.1007/s40265-014-0286-5.
This article addresses the emergence of echinocandin resistance among Candida species, mechanisms of resistance, factors that promote resistance and confounding issues surrounding standard susceptibility testing. Fungal infections remain a significant cause of global morbidity and mortality, especially among patients with underlying immunosupression. Antifungal therapy is a critical component of patient management for acute and chronic diseases. Yet, therapeutic choices are limited due to only a few drug classes available to treat systemic disease. Moreover, the problem is exacerbated by the emergence of antifungal resistance, which has resulted in difficult to manage multidrug resistant strains. Echinocandin drugs are now the preferred choice to treat a range of candidiasis. These drugs target and inhibit the fungal-specific enzyme glucan synthase, which is responsible for the biosynthesis of a key cell wall polymer. Therapeutic failures involving acquisition of resistance among susceptible organisms like Candida albicans is largely a rare event. However, in recent years, there is an alarming trend of increased resistance among strains of Candida glabrata, which in many cases are also resistant to azole drugs. Echinocandin resistance is always acquired during therapy and the mechanism of resistance is well established to involve amino acid changes in "hot-spot" regions of the Fks subunits carrying the catalytic portion of glucan synthase. These changes significantly decrease the sensitivity of the enzyme to drug resulting in higher MIC values. A range of drug responses, from complete to partial refractory response, is observed depending on the nature of the amino acid substitution, and clinical responses are recapitulated in pharmacodynamic models of infection. The cellular processes promoting the formation of resistant Fks strains involve complex stress response pathways, which yield a variety of adaptive compensatory genetic responses. Stress-adapted cells become drug tolerant and can form stable drug resistant FKS mutations with continued drug exposure. A major concern for resistance detection is that classical broth microdilution techniques show significant variability among clinical microbiology laboratories for certain echinocandin drugs and Candida species. The consequence is that susceptible strains are misclassified according to established clinical breakpoints, and this has led to confusion in the field. Clinical factors that appear to promote echinocandin resistance include the expanding use of antifungal agents for empiric therapy and prophylaxis. Furthermore, host reservoirs such as biofilms in the gastrointestinal tract or intra-abdominal infections can seed development of resistant organisms during therapy. A fundamental understanding of the primary molecular resistance mechanism, along with cellular and clinical factors that promote resistance emergence, is critical to develop better diagnostic tools and therapeutic strategies to overcome and prevent echinocandin resistance.
本文探讨了念珠菌属中棘白菌素耐药性的出现、耐药机制、促进耐药性的因素以及围绕标准药敏试验的混杂问题。真菌感染仍然是全球发病和死亡的重要原因,尤其是在有潜在免疫抑制的患者中。抗真菌治疗是急性和慢性疾病患者管理的关键组成部分。然而,由于治疗全身性疾病的药物种类有限,治疗选择受到限制。此外,抗真菌耐药性的出现加剧了这一问题,导致出现难以管理的多重耐药菌株。棘白菌素类药物现在是治疗多种念珠菌病的首选药物。这些药物靶向并抑制真菌特异性酶葡聚糖合酶,该酶负责一种关键细胞壁聚合物的生物合成。在白色念珠菌等易感微生物中获得耐药性导致治疗失败的情况在很大程度上是罕见事件。然而,近年来,光滑念珠菌菌株的耐药性呈惊人的上升趋势,在许多情况下,这些菌株对唑类药物也耐药。棘白菌素耐药性总是在治疗过程中获得的,其耐药机制已明确涉及携带葡聚糖合酶催化部分的Fks亚基“热点”区域的氨基酸变化。这些变化显著降低了酶对药物的敏感性,导致更高的最低抑菌浓度(MIC)值。根据氨基酸取代的性质,观察到一系列从完全到部分难治性反应的药物反应,并且在感染的药效学模型中重现了临床反应。促进耐药性Fks菌株形成的细胞过程涉及复杂的应激反应途径,产生多种适应性补偿性遗传反应。适应应激的细胞对药物产生耐受性,并且在持续接触药物的情况下可以形成稳定的耐药性FKS突变。耐药性检测的一个主要问题是,对于某些棘白菌素类药物和念珠菌属,经典的肉汤微量稀释技术在临床微生物实验室之间显示出显著差异。结果是,根据既定的临床断点,易感菌株被错误分类,这在该领域导致了混乱。似乎促进棘白菌素耐药性的临床因素包括抗真菌药物在经验性治疗和预防中的广泛使用。此外,宿主储存库,如胃肠道中的生物膜或腹腔内感染,可在治疗期间播散耐药菌的发展。对主要分子耐药机制以及促进耐药性出现的细胞和临床因素的基本了解,对于开发更好的诊断工具和治疗策略以克服和预防棘白菌素耐药性至关重要。