抗真菌药Micafungin

据2002年3月的Marketletter杂志报道,日本藤泽(fujisawa)公司已经向美国FDA递交了其抗真菌药Micafungin(代号FK-463)的新药申请书(NDA),以期获得该药单独或与其他全身性抗真菌药物合并用于对目前临床常用抗真菌药不能耐受或已产生耐药菌的病人的治疗以及造血干细胞移植病人的预防用药.     

抗真菌药物的研究进展

综述抗真菌药物的进展、耐药性的研究及不良反应，系统论述抗真菌药物的研究现状。     

唑类抗真菌药物的药理学和毒理学研究进展

唑类抗真菌药在临床上广泛用于治疗深部真菌和浅表真菌感染,早期开发的咪唑类药物以克霉唑和酮康唑为代表,是治疗浅表性真菌感染的首选药物。此类药物可与人体细胞色素P450(CYP450)蛋白血红素辅基Fe原子配位结合,因而具有一定的肝毒性,并对肾上腺和性腺有一定的抑制作用,致使其     

抗真菌药物的研究进展

目的介绍20世纪90年代以来抗真菌药物的研究进展。方法综合分析国内外有关文献报道,分类进行综述。结果与结论目前的研究主要集中在对现有抗真菌药物的结构改造和发现新的抗真菌母核结构这两方面,而海洋药物也将成为研究开发的新热点。     

三唑类抗真菌药的药物动力学相互作用研究进展

目前,国内上市的三唑类抗真菌药（triazole antifungal,TAF）有氟康唑（fluconazole,FCZ）、伊曲康唑（itraconazole,ITZ）、伏立康唑（voriconazole,VRC）和泊沙康唑（posaconazole,POS）等,由于其具有高效低毒的特点,     

第二代三唑类抗真菌药物的研究进展

侵袭性真菌病的发病率和病死率逐年上升,新型抗真菌药物的研究和开发也越来越受到重视,尤其是三唑类抗真菌药物。本文综述国内外近期关于第二代三唑类抗真菌药物的研究进展,以期为未来临床真菌病的治疗及新药研发提供新的思路。     

环孢素与唑类抗真菌药物相互作用的研究进展

摘 要环抱素作为一种强效免疫抑制药,可以和唑类抗真菌药物联用来预防器官移植后引起的免疫排斥和侵袭性真菌感染,但两者联合应用会影响到各自的血药浓度并且可能会威胁到患者的生命安全。本文综述了环孢素与唑类抗真菌药物相互作用研究进展,为临床合理使用环孢素提供依据。     

抗真菌药物的耐药性研究进展

随着真菌感染的发生率逐年上升，抗真菌药物在临床上大量使用，真菌的耐药性迅速发展。真菌耐药性的发展是抗真菌感染治疗面临的又一难题，已引起各国学者的高度重视。本文着重介绍真菌对常用抗真菌药物耐药性的产生和发展过程，耐药机制，并提出控制其耐药性的对策。     

有机硫类抗真菌药物的研究进展

抗真菌药物(antifungal drugs)是一种用于治疗真菌感染的有效药物。近年来,天然抗真菌化合物的筛选和合成抗真菌药物的结构修饰促进了有机硫类抗真菌药物迅速发展。文中对天然有机硫类抗真菌化合物的研究进展进行了综述,同时从氮唑类、硫脲类和丙烯胺类以及硫色酮类等3类化合物的结构修饰方面综述了目前合成有机硫类抗真菌药物的研究进展。     

棘白霉素类抗真菌药的研究进展

棘白霉素类抗真菌药是一类新型抗真菌药，作用于真菌细胞壁，对于念珠菌属以及曲霉菌属均有效，而且安全性较高。目前开发的品种有卡泊芬净、米卡芬净、阿尼芬净，均已通过FDA认证上市。现从作用机制、抗菌活性、药动学、临床评价、药物相互作用和不良反应等几方面对其做一综述。     

抗真菌治疗新药研发进展

摘要：随着侵袭性真菌病例的增加和病原真菌耐药性日益严重,开发新型抗真菌药物的需求非常迫切。幸运的是针对致命 真菌威胁的新药正在涌现,给予了医生新的工具来对付那些难以解决的真菌感染。本文主要介绍了几种处在临床研究阶段的新 药,olorofim、fosmanogepix、rezafungin和ibrexafungerp的药物概况、临床适应症和药物作用机制等相关情况。     

The role of caspofungin and the echinocandins in the antifungal armamentarium

The echinocandins are a recently-developed class of antifungal agents that interfere with fungal cell wall synthesis through the inhibition of glucan synthesis. Although several intravenous preparations are in various stages of development, caspofungin is the only currently approved agent and no oral echinocandin derivatives are presently available. Caspofungin is approved for the treatment of invasive aspergillosis in patients who are refractory to, or intolerant of, other antifungal therapies. This agent has activity against most Candida species, and in a prospective randomized trial, was as effective as, and better tolerated than amphotericin B in the treatment of candidal esophagitis. Activity against the cyst form of Pneumocystis carinii has also been demonstrated. Caspofungin is administered in a daily intravenous dose, and is well tolerated. Concomitant use of this agent with cyclosporine is presently not recommended. Other echinocandin derivatives presently in phase II/III clinical development include micafungin and anidulafungin.     

新型抗真菌药物研究与临床应用

<正>近年来,随着免疫抑制剂、肾上腺皮质激素、广谱抗菌药物的广泛应用,骨髓移植和器官移植的开展、各种导管介入治疗的普遍采用及艾滋病的流行,系统性真菌感染的发病率逐年升高,临床迫切需要具有高效、低毒以及作用快速等特点的抗真菌     

The search for new antifungal drugs and strategies continues

Much of the research presented at the 4th Congress of the European Confederation of Medical Mycology involved new ways of combating the problem of resistance to antifungal agents. Among the possible ways forward in medical mycology are improvements in the bioavailability of existing agents, more clinical testing of new agents and further development of the lipid formulations of amphotericin B. A current major concern of clinicians is that they are now seeing the appearance of cross-resistance between a number of previously very effective antifungals drugs. New in vitro results of terbinafine were presented at this congress, along with the latest information on voriconazole. There is little doubt that the only way to combat emerging drug resistance is at a subcellular level. This will require a much more detailed understanding than we have at present of how fungi and yeasts work.     

Teaching old drugs new tricks: reincarnating immunosuppressants as antifungal drugs

Invasive fungal infections are rising worldwide as the number of immunocompromised patients increases. Unfortunately, our armamentarium of antifungal drugs is limited. Although current therapies are effective in treating some of the most prevalent infections, the development of novel treatments is vital because of emerging drug-resistant strains and species and because of the toxicity of certain current therapies. The immunosuppressive drugs CsA (cyclosporin A), FK-506 (tacrolimus) and rapamycin (sirolimus) exert potent antifungal effects against a variety of pathogenic fungi. These compounds are all currently in clinical use as immunosuppressive therapy to treat and prevent rejection of transplanted organs. Rapamycin is also in clinical trials as an antiproliferative agent for chemotherapy and invasive cardiology. Recent studies reveal a potent fungicidal synergism between azoles and the calcineurin inhibitors CsA and FK-506, and animal studies demonstrate that the CsA-fluconazole synergistic combination has therapeutic benefit. Less immunosuppressive analogs have been identified with potential to enhance current therapies, or as monotherapy without deleterious effects on the immune system. In summary, these highly successful pharmaceutical agents may find an even broader clinical application in combating infectious diseases.     

Advances in antifungal chemotherapy

The American Society for Microbiology sponsored the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), a premier annual scientific conference, in San Diego, California, September 24-27, 1998. At the ICAAC several sessions were held which focused on the pathogenesis of fungal disease, the in vitro susceptibility testing of new azole (voriconazole, Syn-2869, SCH-56592, carbendazim), echinocandin-like (FK-463, LY-303366, MK-0991), polyene (patricins) and established antifungal agents (fluconazole, itraconazole, amphotericin B, nystatin, terbinafine), the experimental in vivo activity of these new antifungal drugs in various animal models of fungal disease, and the clinical activity of fluconazole, itraconazole and liposomal amphotericin B formulations.     

抗真菌药物的研究进展

近20多年来，随着大量广谱抗生索的应用、骨髓和脏器的移植、皮质激素及免疫抑制剂的应用、艾滋病发病率的增加、各种导管的介入和真菌检测技术的提高，念珠菌血症和系统性曲霉感染逐渐增多。北京协和医院报道在四个不同年代败血症血培养的结果显示，1994～1995年真菌发生率为8．1％；2000年为6．7％。20年149例真菌感染的分析显示，真菌感染呈逐年上升的趋势。临床上已有耐氟康唑的念珠菌和耐两性霉紊B的曲霉存在。因此需夏新的抗真菌药物。目前即将推出和已上市的新药有：多烯类的制霉菌素脂质体、两性霉索B脂质体剂型AmBisome、两性霉素B脂质体复合物Abelect、两性霉素B胶样分散体Amphotec、伊曲康唑口服液和注射剂、伏立康唑注射剂和口服片剂以及卡泊芬净注射剂。各种新药均有其特点与不良反应，但总的是新药的开发和临床应用，将会对侵性真菌感染提供有力的治疗措施，真菌感染的治疗前景将会有进一步的改观。     

抗真菌药物联合治疗侵袭性真菌感染的研究进展

近些年,侵袭性真菌感染的发病率逐年增加。由于临床上单药治疗侵袭性真菌感染的效果欠佳,特别是耐药真菌的感染,可选择的药物极少,导致相关疾病的发病率和死亡率仍很高,故抗真菌药物的联合治疗得到了广大学者的青睐。总结了抗真菌药物联合治疗侵袭性真菌感染的机制,综述了针对中枢神经系统、肺部、血液系统、其他部位侵袭性真菌感染的联合用药情况,为临床合理使用抗菌药物提供参考依据。     

新型抗抑郁药物的研究进展

近年来对抑郁症发病机制和药物治疗靶标的研究取得了很大进展,围绕神经可塑性、神经发生、下丘脑-垂体-肾上腺(HPA)轴等后续神经系统适应性改变以及免疫系统变化,确定了谷氨酸受体、神经肽受体、糖皮质激素受体、褪黑激素受体和细胞因子受体等抗抑郁药物作用的新靶标。目前,已发现大量具有抗抑郁作用的新化合物,褪黑激素受体激动剂阿戈美拉丁、促肾上腺皮质激素释放激素受体拮抗剂喹硫平已经上市,神经激肽2受体拮抗剂沙瑞度坦、糖皮质激素受体拮抗剂米非司酮正在进行Ⅲ期临床研究,10余个药物进入临床研究阶段。本文对近5年新型抗抑郁药物的研究进展进行简要综述。