Current perspectives on echinocandin class drugs

Future Microbiology

Volumn 6, Issue 4, 2011, Pages 441-457

  Perlin, David S ^a  

^a PUBLIC HEALTH RESEARCH INSTITUTE   (United States)

Author keywords

anidulafungin; caspofungin; echinocandin; FKS; fungal infection; glucan synthase; MIC; micafungin

Indexed keywords

ANIDULAFUNGIN; BETA 1,3 GLUCAN; CALCINEURIN; CASPOFUNGIN; ECHINOCANDIN; ENFUMAFUNGIN; FKS PROTEIN; FUNGAL PROTEIN; GLUCAN SYNTHASE; HEAT SHOCK PROTEIN 90; MICAFUNGIN; MK 3118; UNCLASSIFIED DRUG;

ANTIFUNGAL RESISTANCE; AREA UNDER THE CURVE; ASPERGILLUS FUMIGATUS; BIOFILM; CANDIDA; CANDIDIASIS; CELL FUNCTION; CELL WALL; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG STRUCTURE; ENZYME SUBUNIT; FUNGAL STRAIN; FUNGAL VIRULENCE; FUNGICIDAL ACTIVITY; FUNGUS IMMUNITY; FUNGUS MUTATION; HUMAN; IC 50; MAXIMUM PLASMA CONCENTRATION; MICROBIAL SENSITIVITY TEST; MINIMUM INHIBITORY CONCENTRATION; MYCOSIS; NONHUMAN; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION; SINGLE DRUG DOSE; TARGET CELL;

ANTIFUNGAL AGENTS; ASPERGILLUS; CANDIDA; DRUG RESISTANCE, FUNGAL; ECHINOCANDINS; GLUCOSYLTRANSFERASES; HUMANS; MICROBIAL SENSITIVITY TESTS;

ASPERGILLUS; ASPERGILLUS FUMIGATUS; CANDIDA; FUNGI; MAMMALIA;

EID: 79955625171     PISSN: 17460913     EISSN: None     Source Type: Journal    
DOI: 10.2217/fmb.11.19     Document Type: Review

References (165)

1. Kurtz MB, Douglas CM: Lipopeptide inhibitors of fungal glucan synthase. J. Med. Vet. Mycol. 35(2), 79-86 (1997). (Pubitemid 27174580)
2. Denning DW: Echinocandins: a new class of antifungal. J. Antimicrob. Chemother. 49(6), 889-891 (2002). (Pubitemid 34692881)
3. Denning DW: Echinocandin antifungal drugs. Lancet 362(9390), 1142-1151 (2003). (Pubitemid 37222342)
4. Morrison VA: Echinocandin antifungals: review and update. Expert Rev. Anti Infect. Ther. 4(2), 325-342 (2006).
5. Douglas CM: Fungal b(1,3)-d-glucan synthesis. Med. Mycol. 39(Suppl. 1), 55-66 (2001).
6. Kurtz MB, Rex JH: Glucan synthase inhibitors as antifungal agents. Adv. Protein Chem. 56, 423-475 (2001). (Pubitemid 32367464)
7. Kurtz MB, Heath IB, Marrinan J, Dreikorn S, Onishi J, Douglas C: Morphological effects of lipopeptides against Aspergillus fumigatus correlate with activities against (1,3)-b-d-glucan synthase. Antimicrob. Agents Chemother. 38(7), 1480-1489 (1994). (Pubitemid 24203556)
8. Bowman JC, Hicks PS, Kurtz MB et al.: The antifungal echinocandin caspofungin acetate kills growing cells of Aspergillus fumigatus in vitro. Antimicrob. Agents Chemother. 46(9), 3001-3012 (2002).
9. Douglas CM: Understanding the microbiology of the Aspergillus cell wall and the efficacy of caspofungin. Med. Mycol. 44 (Suppl.) 95-99 (2006). (Pubitemid 44524092)
10. Pappas PG, Kauffman CA, Andes D et al.: Clinical practice guidelines for the management of candidiasis: 2009 update by the Infectious Diseases Society of America. Clin. Infect. Dis. 48(5), 503-535 (2009).
11. Pappas PG, Rotstein CM, Betts RF et al.: Micafungin versus caspofungin for treatment of candidemia and other forms of invasive candidiasis. Clin. Infect. Dis. 45(7), 883-893 (2007). (Pubitemid 47580382)
12. Reboli AC, Rotstein C, Pappas PG et al.: Anidulafungin versus fluconazole for invasive candidiasis. N. Engl. J. Med. 356(24), 2472-2482 (2007). (Pubitemid 46919773)
13. Bormann AM, Morrison VA: Review of the pharmacology and clinical studies of micafungin. Drug Des. Devel. Ther. 3, 295-302 (2009).
14. Temesgen Z, Barreto J, Vento S: Micafungin - the newest echinocandin. Drugs Today 45(6), 469-478 (2009).
15. Cross SA, Scott LJ: Micafungin: a review of its use in adults for the treatment of invasive and oesophageal candidiasis, and as prophylaxis against Candida infections. Drugs 68(15), 2225-2255 (2008).
16. Kim R, Khachikian D, Reboli AC: A comparative evaluation of properties and clinical efficacy of the echinocandins. Expert Opin. Pharmacother. 8(10), 1479-1492 (2007). (Pubitemid 47082698)
17. Morris MI, Villmann M: Echinocandins in the management of invasive fungal infections, Part 2. Am. J. Health Syst. Pharm. 63(19), 1813-1820 (2006). (Pubitemid 44477452)
18. Morris MI, Villmann M: Echinocandins in the management of invasive fungal infections, part 1. Am. J. Health Syst. Pharm. 63(18), 1693-1703 (2006). (Pubitemid 44413505)
19. Chandrasekar PH, Sobel JD: Micafungin: a new echinocandin. Clin. Infect. Dis. 42(8), 1171-1178 (2006).
20. Kartsonis N, DiNubile MJ, Bartizal K, Hicks PS, Ryan D, Sable CA: Efficacy of caspofungin in the treatment of esophageal candidiasis resistant to fluconazole. J. Acquir. Immune Defic. Syndr. 31(2), 183-187 (2002). (Pubitemid 35190573)
21. Posteraro B, Sanguinetti M, Fiori B et al.: Caspofungin activity against clinical isolates of azole cross-resistant Candida glabrata overexpressing efflux pump genes. J. Antimicrob. Chemother. 58(2), 458-461 (2006). (Pubitemid 44294967)
22. Pfaller MA, Diekema DJ, Messer SA, Hollis RJ, Jones RN: In vitro activities of caspofungin compared with those of fluconazole and itraconazole against 3,959 clinical isolates of Candida spp., including 157 fluconazole-resistant isolates. Antimicrob. Agents Chemother. 47(3), 1068-1071 (2003). (Pubitemid 36254236)
23. Bachmann SP, Patterson TF, Lopez-Ribot JL: In vitro activity of caspofungin (MK-0991) against Candida albicans clinical isolates displaying different mechanisms of azole resistance. J. Clin. Microbiol. 40(6), 2228-2230 (2002). (Pubitemid 34596413)
24. Ferreira JA, Carr JH, Starling CE, de Resende MA, Donlan RM: Biofilm formation and effect of caspofungin on biofilm structure of Candida species bloodstream isolates. Antimicrob. Agents Chemother. 53(10), 4377-4384 (2009).
25. Ramage G, Van de Walle K, Bachmann SP, Wickes BL, Lopez-Ribot JL: In vitro pharmacodynamic properties of three antifungal agents against preformed Candida albicans biofilms determined by time-kill studies. Antimicrob. Agents Chemother. 46(11), 3634-3636 (2002). (Pubitemid 35192940)
26. Bachmann SP, Van de Walle K, Ramage G et al.: In vitro activity of caspofungin against Candida albicans biofilms. Antimicrob. Agents Chemother. 46(11), 3591-3596 (2002). (Pubitemid 35192931)
27. Zaas AK: Echinocandins: a wealth of choice - how clinically different are they? Curr. Opin. Infect. Dis. 21(4), 426-432 (2008).
28. Zaas AK, Dodds Ashley ES, Alexander BD, Johnson MD, Perfect JR: Caspofungin for invasive candidiasis at a tertiary care medical center. Am. J. Med. 119(11), 993 E991-E996 (2006).
29. Goto N, Hara T, Tsurumi H et al.: Efficacy and safety of micafungin for treating febrile neutropenia in hematological malignancies. Am. J. Hematol. 85(11), 872-876 (2010).
30. Lehrnbecher T, Groll AH: Micafungin: a brief review of pharmacology, safety, and antifungal efficacy in pediatric patients. Pediatr. Blood Cancer 55(2), 229-232 (2010).
31. Manzoni P, Rizzollo S, Franco C et al.: Role of echinocandins in the management of fungal infections in neonates. J. Matern. Fetal Neonatal Med. 23(S3), 49-52 (2010).
32. Aikawa N, Kusachi S, Oda S, Takesue Y, Tanaka H: Clinical effects of micafungin, a novel echinocandin antifungal agent, on systemic fungal infections in surgery, emergency, and intensive-care medicine: evaluation using the AKOTT algorithm. J. Infect. Chemother. 15(4), 219-227 (2009).
33. Kuti EL, Kuti JL: Pharmacokinetics, antifungal activity and clinical efficacy of anidulafungin in the treatment of fungal infections. Expert Opin. Drug Metab. Toxicol. 6(10), 1287-1300 (2010).
34. Menichetti F: Anidulafungin, a new echinocandin: effectiveness and tolerability. Drugs 69 (Suppl. 1), 95-97 (2009).
35. Sucher AJ, Chahine EB, Balcer HE: Echinocandins: the newest class of antifungals. Ann. Pharmacother. 43(10), 1647-1657 (2009).
36. Vanden Bussche HL, Van Loo DA: A clinical review of echinocandins in pediatric patients. Ann. Pharmacother. 44(1), 166-177 (2010).
37. Venditti M: Clinical aspects of invasive candidiasis: endocarditis and other localized infections. Drugs 69 (Suppl. 1), 39-43 (2009).
38. Maschmeyer G, Glasmacher A: Pharmacological properties and clinical efficacy of a recently licensed systemic antifungal, caspofungin. Mycoses 48(4), 227-234 (2005). (Pubitemid 40973767)
39. Walsh TJ, Adamson PC, Seibel NL et al.: Pharmacokinetics, safety, and tolerability of caspofungin in children and adolescents. Antimicrob. Agents Chemother. 49(11), 4536-4545 (2005). (Pubitemid 41552583)
40. Heresi GP, Gerstmann DR, Reed MD et al.: The pharmacokinetics and safety of micafungin, a novel echinocandin, in premature infants. Pediatr. Infect. Dis. J. 25(12), 1110-1115 (2006). (Pubitemid 44900673)
41. Vazquez JA: The safety of anidulafungin. Expert Opin. Drug Saf. 5(6), 751-758 (2006). (Pubitemid 44669490)
42. Garcia-Effron G, Lee S, Park S, Cleary JD, Perlin DS: Effect of Candida glabrata FKS1 and FKS2 mutations on echinocandin sensitivity and kinetics of 1,3-b-d-glucan synthase: implication for the existing susceptibility breakpoint. Antimicrob. Agents Chemother. 53(9), 3690-3699 (2009).
43. Garcia-Effron G, Park S, Perlin DS: Correlating echinocandin MIC and kinetic inhibition of fks1 mutant glucan synthases for Candida albicans: implications for interpretive breakpoints. Antimicrob. Agents Chemother. 53(1), 112-122 (2009).
44. Perlin DS: Resistance to echinocandin-class antifungal drugs. Drug Resist. Update 10(3), 121-130 (2007). (Pubitemid 47031054)
45. Orlean PA: (1,3)-b-d-glucan synthase from budding and filamentous cultures of the dimorphic fungus Candida albicans. Eur. J. Biochem. 127(2), 397-403 (1982). (Pubitemid 13206485)
46. Andaluz E, Guillen A, Larriba G: Preliminary evidence for a glucan acceptor in the yeast Candida albicans. Biochem. J. 240(2), 495-502 (1986). (Pubitemid 17196141)
47. Lopez-Romero E, Ruiz-Herrera J: Biosynthesis of b-glucans by cell-free extracts from Saccharomyces cerevisiae. Biochim. Biophys. Acta. 500(2), 372-384 (1977). (Pubitemid 8229367)
48. Shematek EM, Braatz JA, Cabib E: Biosynthesis of the yeast cell wall. I: preparation and properties of b-(1 leads to 3) glucan synthetase. J. Biol. Chem. 255(3), 888-894 (1980). (Pubitemid 10108130)
49. Shematek EM, Cabib E: Biosynthesis of the yeast cell wall. II: regulation of b-(1 leads to 3)glucan synthetase by ATP and GTP. J. Biol. Chem. 255(3), 895-902 (1980). (Pubitemid 10108131)
50. Cabib E, Roberts R, Bowers B: Synthesis of the yeast cell wall and its regulation. Annu. Rev. Biochem. 51, 763-793 (1982).
51. Cabib E, Kang MS: Fungal 1,3-b-glucan synthase. Methods Enzymol. 138, 637-642 (1987).
52. Inoue SB, Takewaki N, Takasuka T et al.: Characterization and gene cloning of 1,3-b-D-glucan synthase from Saccharomyces cerevisiae. Eur. J. Biochem. 231(3), 845-854 (1995).
53. Inoue SB, Qadota H, Arisawa M, Anraku Y, Watanabe T, Ohya Y: Signaling toward yeast 1,3-b-glucan synthesis. Cell Struct. Funct. 21(5), 395-402 (1996). (Pubitemid 27068325)
54. Garcia-Effron G, Katiyar SK, Park S, Edlind TD, Perlin DS: A naturally occurring proline-to-alanine amino acid change in Fks1p in Candida parapsilosis, Candida orthopsilosis, and Candida metapsilosis accounts for reduced echinocandin susceptibility. Antimicrob. Agents Chemother. 52(7), 2305-2312 (2008). (Pubitemid 351915657)
55. Douglas CM, Foor F, Marrinan JA et al.: The Saccharomyces cerevisiae FKS1 (ETG1) gene encodes an integral membrane protein which is a subunit of 1,3-b-d-glucan synthase. Proc. Natl Acad. Sci. USA 91(26), 12907-12911 (1994).
56. Kondoh O, Tachibana Y, Ohya Y, Arisawa M, Watanabe T: Cloning of the RHO1 gene from Candida albicans and its regulation of b-1,3-glucan synthesis. J. Bacteriol. 179(24), 7734-7741 (1997). (Pubitemid 27525703)
57. Schimoler-O'Rourke R, Renault S, Mo W, Selitrennikoff CP: Neurospora crassa FKS protein binds to the (1,3)b-glucan synthase substrate, UDP-glucose. Curr. Microbiol. 46(6), 408-412 (2003). (Pubitemid 36918049)
58. Mio T, Adachi-Shimizu M, Tachibana Y et al.: Cloning of the Candida albicans homolog of Saccharomyces cerevisiae GSC1/ FKS1 and its involvement in b-1,3-glucan synthesis. J. Bacteriol. 179(13), 4096-4105 (1997). (Pubitemid 27291036)
59. Thompson JR, Douglas CM, Li W et al.: A glucan synthase FKS1 homolog in Cryptococcus neoformans is single copy and encodes an essential function. J. Bacteriol. 181(2), 444-453 (1999). (Pubitemid 29045134)
60. Mazur P, Morin N, Baginsky W et al.: Differential expression and function of two homologous subunits of yeast 1,3-b-d-glucan synthase. Mol. Cell Biol. 15(10), 5671-5681 (1995).
61. Mazur P, Baginsky W: In vitro activity of 1,3-b-d-glucan synthase requires the GTP-binding protein Rho1. J. Biol. Chem. 271(24), 14604-14609 (1996). (Pubitemid 26190367)
62. Edlind TD, Katiyar SK: The echinocandin "target" identified by cross-linking is a homolog of Pil1 and Lsp1, sphingolipid-dependent regulators of cell wall integrity signaling. Antimicrob. Agents Chemother. 48(11), 4491 (2004). (Pubitemid 39434927)
63. Radding JA, Heidler SA, Turner WW: Photoaffinity analog of the semisynthetic echinocandin LY303366: identification of echinocandin targets in Candida albicans. Antimicrob. Agents Chemother. 42(5), 1187-1194 (1998). (Pubitemid 28227918)
64. Pirri G, Giuliani A, Nicoletto SF, Pizzuto L, Rinaldi AC: Lipopeptides as anti-infectives: a practical perspective. Cent. Eur. J. Biol. 4, 258-273 (2009).
65. Paderu P, Park S, Perlin DS: Caspofungin uptake is mediated by a high-affinity transporter in Candida albicans. Antimicrob. Agents Chemother. 48(10), 3845-3849 (2004). (Pubitemid 39304613)
66. Niimi K, Maki K, Ikeda F et al.: Overexpression of Candida albicans CDR1, CDR2, or MDR1 does not produce significant changes in echinocandin susceptibility. Antimicrob. Agents Chemother. 50(4), 1148-1155 (2006).
67. Charlemagne D: Molecular and cellular level of action of digitalis. Herz 18(2), 79-85 (1993). (Pubitemid 23154851)
68. Zimbeck AJ, Iqbal N, Ahlquist AM et al.: FKS mutations and elevated echinocandin MIC values among Candida glabrata isolates from US population-based surveillance. Antimicrob. Agents Chemother. 54(12), 5042-5047 (2010).
69. Castanheira M, Woosley LN, Diekema DJ, Messer SA, Jones RN, Pfaller MA: Low prevalence of fks1 hot spot 1 mutations in a worldwide collection of Candida strains. Antimicrob. Agents Chemother. 54(6), 2655-2659 (2010).
70. Hakki M, Staab JF, Marr KA: Emergence of a Candida krusei isolate with reduced susceptibility to caspofungin during therapy. Antimicrob. Agents Chemother. 50(7), 2522-2524 (2006). (Pubitemid 43993195)
71. Katiyar S, Pfaller M, Edlind T: Candida albicans and Candida glabrata clinical isolates exhibiting reduced echinocandin susceptibility. Antimicrob. Agents Chemother. 50(8), 2892-2894 (2006). (Pubitemid 44198725)
72. Miller CD, Lomaestro BW, Park S, Perlin DS: Progressive esophagitis caused by Candida albicans with reduced susceptibility to caspofungin. Pharmacotherapy 26(6), 877-880 (2006). (Pubitemid 43807639)
73. Kahn JN, Garcia-Effron G, Hsu MJ, Park S, Marr KA, Perlin DS: Acquired echinocandin resistance in a Candida krusei isolate due to modification of glucan synthase. Antimicrob. Agents Chemother. 51(5), 1876-1878 (2007). (Pubitemid 46744179)
74. Cleary JD, Garcia-Effron G, Chapman SW, Perlin DS: Reduced Candida glabrata susceptibility secondary to an FKS1 mutation developed during candidemia treatment. Antimicrob. Agents Chemother. 52(6), 2263-2265 (2008). (Pubitemid 351758575)
75. Desnos-Ollivier M, Dromer F, Dannaoui E: Detection of caspofungin resistance in Candida spp. by Etest. J. Clin. Microbiol. 46(7), 2389-2392 (2008).
76. Garcia-Effron G, Kontoyiannis DP, Lewis RE, Perlin DS: Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies. Antimicrob. Agents Chemother. 52(11), 4181-4183 (2008).
77. Arendrup MC, Garcia-Effron G, Buzina W et al.: Breakthrough Aspergillus fumigatus and Candida albicans double infection during caspofungin treatment: laboratory characteristics and implication for susceptibility testing. Antimicrob. Agents Chemother. 53(3), 1185-1193 (2009).
78. Thompson GR 3rd, Wiederhold NP, Vallor AC, Villareal NC, Lewis JS 2nd, Patterson TF: Development of caspofungin resistance following prolonged therapy for invasive candidiasis secondary to Candida glabrata infection. Antimicrob. Agents Chemother. 52(10), 3783-3785 (2008).
79. Pfeiffer CD, Garcia-Effron G, Zaas AK, Perfect JR, Perlin DS, Alexander BD: Breakthrough invasive candidiasis in patients on micafungin. J. Clin. Microbiol. 48(7), 2373-2380 (2010).
80. Desnos-Ollivier M, Bretagne S, Raoux D, Hoinard D, Dromer F, Dannaoui E: Mutations in the fks1 gene in Candida albicans, C. tropicalis, and C. krusei correlate with elevated caspofungin MICs uncovered in AM3 medium using the method of the European Committee on Antibiotic Susceptibility Testing. Antimicrob. Agents Chemother. 52(9), 3092-3098 (2008).
81. Cowen LE: Hsp90 orchestrates stress response signaling governing fungal drug resistance. PLoS Pathog. 5(8), E1000471 (2009).
82. Kartsonis N, Killar J, Mixson L et al.: Caspofungin susceptibility testing of isolates from patients with esophageal candidiasis or invasive candidiasis: relationship of MIC to treatment outcome. Antimicrob. Agents Chemother. 49(9), 3616-3623 (2005). (Pubitemid 41233008)
83. Pfaller MA, Diekema DJ, Boyken L et al.: Effectiveness of anidulafungin in eradicating Candida species in invasive candidiasis. Antimicrob. Agents Chemother. 49(11), 4795-4797 (2005). (Pubitemid 41552623)
84. Pfaller MA, Diekema DJ, Ostrosky-Zeichner L et al.: Correlation of MIC with outcome for Candida species tested against caspofungin, anidulafungin, and micafungin: analysis and proposal for interpretive MIC breakpoints. J. Clin. Microbiol. 46(8), 2620-2629 (2008).
85. Park S, Kelly R, Kahn JN et al.: Specific substitutions in the echinocandin target Fks1p account for reduced susceptibility of rare laboratory and clinical Candida sp. isolates. Antimicrob. Agents Chemother. 49(8), 3264-3273 (2005). (Pubitemid 41060570)
86. Perlin DS: Antifungal drug resistance: do molecular methods provide a way forward? Curr. Opin. Infect. Dis. 22(6), 568-573 (2009).
87. Balajee SA, Gribskov JL, Hanley E, Nickle D, Marr KA: Aspergillus lentulus sp. nov., a new sibling species of A. fumigatus. Eukaryot. Cell 4(3), 625-632 (2005). (Pubitemid 40383765)
88. Alcazar-Fuoli L, Mellado E, Alastruey- Izquierdo A, Cuenca-Estrella M, Rodriguez-Tudela JL: Aspergillus section Fumigati: antifungal susceptibility patterns and sequence-based identification. Antimicrob. Agents Chemother. 52(4), 1244-1251 (2008). (Pubitemid 351521983)
89. Gardiner RE, Souteropoulos P, Park S, Perlin DS: Characterization of Aspergillus fumigatus mutants with reduced susceptibility to caspofungin. Med. Mycol. 43 (Suppl. 1), S299-S305 (2005). (Pubitemid 41038582)
90. Staab JF, Kahn JN, Marr KA: Differential Aspergillus lentulus echinocandin susceptibilities are Fksp-independent. Antimicrob. Agents Chemother. 54(12), 4992-4998 (2010).
91. Malani AN, Kauffman CA: Changing epidemiology of rare mould infections: implications for therapy. Drugs 67(13), 1803-1812 (2007). (Pubitemid 47347394)
92. Nett JE, Crawford K, Marchillo K, Ande DR: Role of Fks1p and matrix glucan in Candida albicans biofilm resistance to an echinocandin, pyrimidine, and polyene. Antimicrob. Agents Chemother. 54(8), 3505-3508 (2010).
93. Maligie MA, Selitrennikoff CP: Cryptococcus neoformans resistance to echinocandins: (1,3)b-glucan synthase activity is sensitive to echinocandins. Antimicrob. Agents Chemother. 49(7), 2851-2856 (2005). (Pubitemid 40917602)
94. Ikeda R, Sugita T, Jacobson ES, Shinoda T: Effects of melanin upon susceptibility of Cryptococcus to antifungals. Microbiol. Immunol. 47(4), 271-277 (2003). (Pubitemid 36460563)
95. Kahn JN, Hsu MJ, Racine F, Giacobbe R, Motyl M: Caspofungin susceptibility in Aspergillus and non-Aspergillus molds: inhibition of glucan synthase and reduction of b-D-1,3 glucan levels in culture. Antimicrob. Agents Chemother. 50(6), 2214-2216 (2006). (Pubitemid 43807547)
96. Stevens DA, Espiritu M, Parmar R: Paradoxical effect of caspofungin: reduced activity against Candida albicans at high drug concentrations. Antimicrob. Agents Chemother. 48(9), 3407-3411 (2004). (Pubitemid 39129338)
97. Chamilos G, Lewis RE, Albert N, Kontoyiannis DP: Paradoxical effect of echinocandins across Candida species in vitro: evidence for echinocandin- specific and candida species-related differences. Antimicrob. Agents Chemother. 51(6), 2257-2259 (2007). (Pubitemid 46903132)
98. Stevens DA, White TC, Perlin DS, Selitrennikoff CP: Studies of the paradoxical effect of caspofungin at high drug concentrations. Diagn. Microbiol. Infect. Dis. 51(3), 173-178 (2005). (Pubitemid 40568760)
99. Lesage G, Sdicu AM, Menard P, Shapiro J, Hussein S, Bussey H: Analysis of b-1,3- glucan assembly in Saccharomyces cerevisiae using a synthetic interaction network and altered sensitivity to caspofungin. Genetics 167(1), 35-49 (2004). (Pubitemid 38736368)
100. Wiederhold NP, Kontoyiannis DP, Prince RA, Lewis RE: Attenuation of the activity of caspofungin at high concentrations against Candida albicans: possible role of cell wall integrity and calcineurin pathways. Antimicrob. Agents Chemother. 49(12), 5146-5148 (2005). (Pubitemid 41778937)
101. Stevens DA, Ichinomiya M, Koshi Y, Horiuchi H: Escape of Candida from caspofungin inhibition at concentrations above the MIC (paradoxical effect) accomplished by increased cell wall chitin; evidence for b-1,6-glucan synthesis inhibition by caspofungin. Antimicrob. Agents Chemother. 50(9), 3160-3161 (2006). (Pubitemid 44396427)
102. Fortwendel JR, Zhao W, Bhabhra R et al.: A fungus-specific ras homolog contributes to the hyphal growth and virulence of Aspergillus fumigatus. Eukaryot. Cell 4(12), 1982-1989 (2005). (Pubitemid 41798304)
103. Wiederhold NP, Kontoyiannis DP, Chi J, Prince RA, Tam VH, Lewis RE: Pharmacodynamics of caspofungin in a murine model of invasive pulmonary aspergillosis: evidence of concentration-dependent activity. J. Infect. Dis. 190(8), 1464-1471 (2004). (Pubitemid 39332186)
104. Clemons KV, Stevens DA: Efficacy of micafungin alone or in combination against experimental pulmonary aspergillosis. Med. Mycol. 44(1), 69-73 (2006). (Pubitemid 43135558)
105. Klont RR, Mennink-Kersten MA, Ruegebrink D et al.: Paradoxical increase in circulating Aspergillus antigen during treatment with caspofungin in a patient with pulmonary aspergillosis. Clin. Infect. Dis. 43(3), E23-E25 (2006).
106. Lewis RE, Albert ND, Kontoyiannis DP: Comparison of the dose-dependent activity and paradoxical effect of caspofungin and micafungin in a neutropenic murine model of invasive pulmonary aspergillosis. J. Antimicrob. Chemother. 61(5), 1140-1144 (2008). (Pubitemid 351524462)
107. Cowen LE, Lindquist S: Hsp90 potentiates the rapid evolution of new traits: drug resistance in diverse fungi. Science 309(5744), 2185-2189 (2005). (Pubitemid 41396062)
108. Cowen LE, Carpenter AE, Matangkasombut O, Fink GR, Lindquist S: Genetic architecture of Hsp90-dependent drug resistance. Eukaryot. Cell 5(12), 2184-2188 (2006). (Pubitemid 44956829)
109. Cowen LE: The evolution of fungal drug resistance: modulating the trajectory from genotype to phenotype. Nat. Rev. Microbiol. 6(3), 187-198 (2008). (Pubitemid 351256314)
110. Steinbach WJ, Cramer RA Jr, Perfect BZ et al.: Calcineurin controls growth, morphology, and pathogenicity in Aspergillus fumigatus. Eukaryot. Cell 5(7), 1091-1103 (2006). (Pubitemid 44100707)
111. Semighini CP, Heitman J: Dynamic duo takes down fungal villains. Proc. Natl Acad. Sci. USA 106(9), 2971-2972 (2009).
112. Steinbach WJ, Singh N, Miller JL et al.: In vitro interactions between antifungals and immunosuppressants against Aspergillus fumigatus isolates from transplant and nontransplant patients. Antimicrob. Agents Chemother. 48(12), 4922-4925 (2004). (Pubitemid 39577709)
113. Cowen LE, Steinbach WJ: Stress, drugs, and evolution: the role of cellular signaling in fungal drug resistance. Eukaryot. Cell 7(5), 747-764 (2008). (Pubitemid 351968819)
114. Cramer RA Jr, Perfect BZ, Pinchai N et al.: Calcineurin target CrzA regulates conidial germination, hyphal growth, and pathogenesis of Aspergillus fumigatus. Eukaryot. Cell 7(7), 1085-1097 (2008). (Pubitemid 351969323)
115. Arendrup MC, Kahlmeter G, Rodriguez-Tudela JL, Donnelly JP: Breakpoints for susceptibility testing should not divide wild-type distributions of important target species. Antimicrob. Agents Chemother. 53(4), 1628-1629 (2009).
116. Turnidge J, Kahlmeter G, Kronvall G: Statistical characterisation of bacterial wild-type MIC value distributions and the determination of epidemiological cut-off values. Clin. Microbiol. Infect. 12(5), 418-425 (2006).
117. Turnidge J, Paterson DL: Setting and revising antibacterial susceptibility breakpoints. Clin. Microbiol. Rev. 20(3), 391-408 (2007). (Pubitemid 47175010)
118. Rodriguez-Tudela JL, Arendrup MC, Cuenca- Estrella M, Donnelly JP, Lass-Florl C: EUCAST breakpoints for antifungals. Drug News Perspect. 23(2), 93-97 (2010).
119. Pfaller MA, Boyken L, Hollis RJ, Messer SA, Tendolkar S, Diekema DJ: Global surveillance of in vitro activity of micafungin against Candida: a comparison with caspofungin by CLSI-recommended methods. J. Clin. Microbiol. 44(10), 3533-3538 (2006). (Pubitemid 46768811)
120. Pfaller MA, Boyken L, Hollis RJ et al.: In vitro susceptibility of invasive isolates of Candida spp. to anidulafungin, caspofungin, and micafungin: six years of global surveillance. J. Clin. Microbiol. 46(1), 150-156 (2008).
121. Rautemaa R, Richardson M, Pfaller MA, Perheentupa J, Saxen H: Activity of amphotericin B, anidulafungin, caspofungin, micafungin, posaconazole, and voriconazole against Candida albicans with decreased susceptibility to fluconazole from APECED patients on long-term azole treatment of chronic mucocutaneous candidiasis. Diagn. Microbiol. Infect. Dis. 62(2), 182-185 (2008).
122. Pfaller MA, Boyken L, Hollis RJ et al.: Wild-type minimum effective concentration distributions and epidemiologic cutoff values for caspofungin and Aspergillus spp. as determined by Clinical and Laboratory Standards Institute broth microdilution methods. Diagn. Microbiol. Infect. Dis. 67(1), 56-60 (2010).
123. Pfaller MA, Boyken L, Hollis RJ et al.: Wild-type MIC distributions and epidemiological cutoff values for the echinocandins and Candida spp. J. Clin. Microbiol. 48(1), 52-56 (2009).
124. Pfaller MA, Diekema DJ, Ostrosky-Zeichner L et al.: Correlation of MIC with outcome for Candida species tested against caspofungin, anidulafungin, and micafungin: analysis and proposal for interpretive MIC breakpoints. J. Clin. Microbiol. 46(8), 2620-2629 (2008).
125. Arendrup MC, Garcia-Effron G, Lass-Florl C et al.: Echinocandin susceptibility testing of Candida species: comparison of EUCAST EDef 7.1, CLSI M27-A3, Etest, disk diffusion, and agar dilution methods with RPMI and isosensitest media. Antimicrob. Agents Chemother. 54(1), 426-439 (2010).
126. Stein GE, El-Mortada M, Smith C, Dybas L, Prince R, Havlichek D: Fungicidal activity of anidulafungin in serum from patients does not correlate to its susceptible breakpoint against Candida spp. J. Antimicrob. Chemother. 65(2), 374-376 (2009).
127. Wiederhold NP, Grabinski JL, Garcia- Effron G, Perlin DS, Lee SA: Pyrosequencing to detect mutations in FKS1 that confer reduced echinocandin susceptibility in Candida albicans. Antimicrob. Agents Chemother. 52(11), 4145-4148 (2008).
128. Andes D, Diekema DJ, Pfaller MA, Bohrmuller J, Marchillo K, Lepak A: In vivo comparison of the pharmacodynamic targets for echinocandin drugs against Candida species. Antimicrob. Agents Chemother. 54(6), 2497-506 (2010).
129. Andes D, Diekema DJ, Pfaller MA et al.: In vivo pharmacodynamic characterization of anidulafungin in a neutropenic murine candidiasis model. Antimicrob. Agents Chemother. 52(2), 539-550 (2008). (Pubitemid 351170826)
130. Andes DR, Diekema DJ, Pfaller MA, Marchillo K, Bohrmueller J: In vivo pharmacodynamic target investigation for micafungin against Candida albicans and C. glabrata in a neutropenic murine candidiasis model. Antimicrob. Agents Chemother. 52(10), 3497-3503 (2008).
131. Pfaller MA, Diekema D, Andes D et al.:Clinical breakpoints for the Echinocandins and Candida, revisited. Presented at: Interscience Conference on Antimicrobial Agents and Chemotherapy. Poster M-369, MA, USA, 12-15 September 2010.
132. Bennett JE: Echinocandins for candidemia in adults without neutropenia. N. Engl. J. Med. 355(11), 1154-1159 (2006). (Pubitemid 44394921)
133. Hajdu R, Thompson R, Sundelof JG et al.: Preliminary animal pharmacokinetics of the parenteral antifungal agent MK-0991 (L-743,872). Antimicrob. Agents Chemother. 41(11), 2339-2344 (1997). (Pubitemid 27467537)
134. Hoang A: Caspofungin acetate: an antifungal agent. Am. J. Health Syst. Pharm. 58(13), 1206-1214 (2001). (Pubitemid 32622547)
135. Paderu P, Garcia-Effron G, Balashov S, Delmas G, Park S, Perlin DS: Serum differentially alters the antifungal properties of echinocandin drugs. Antimicrob. Agents Chemother. 51(6), 2253-2256 (2007). (Pubitemid 46903131)
136. Odabasi Z, Paetznick V, Rex JH, Ostrosky- Zeichner L: Effects of serum on in vitro susceptibility testing of echinocandins. Antimicrob. Agents Chemother. 51(11), 4214-4216 (2007). (Pubitemid 350057834)
137. Wiederhold NP, Najvar LK, Bocanegra R, Molina D, Olivo M, Graybill JR: In vivo efficacy of anidulafungin and caspofungin against Candida glabrata and association with in vitro potency in the presence of sera. Antimicrob. Agents Chemother. 51(5), 1616-1620 (2007). (Pubitemid 46744135)
138. Garcia-Effron G, Park S, Perlin DS: Improved detection of Candida spp. fks hot spot mutants using the CLSI M27-A3 document by the addition of bovine serum albumin (BSA). Antimicrob. Agents Chemother. DOI: 0:AAC.01350-10v1 (2011) (Epub ahead of print).
139. Arendrup MC, Rodriguez-Tudela JL, Park S et al.: Echinocandin susceptibility testing of Candida spp. using the EUCAST 1 EDef 7.1 and CLSI M27-A3 standard procedures: analysis of the influence of bovine serum albumin supplementation, storage time and drug lots. Antimicrob. Agents Chemother. 55(4), 1580-1587 (2011).
140. Ben-Ami R, Garcia-Effron G, Lewis RE et al.: The fitness and virulence cost of fks1 mutations causing echinocandin-resistance in Candida albicans. Proc. Natl Acad. Sci. USA (2010).
141. Wiederhold NP, Lewis JS 2nd: The echinocandin micafungin: a review of the pharmacology, spectrum of activity, clinical efficacy and safety. Expert Opin. Pharmacother. 8(8), 1155-1166 (2007). (Pubitemid 46929308)
142. Cappelletty D, Eiselstein-McKitrick K: The echinocandins. Pharmacotherapy 27(3), 369-388 (2007). (Pubitemid 46327905)
143. Vazquez JA: Anidulafungin: a new echinocandin with a novel profile. Clin. Ther. 27(6), 657-673 (2005). (Pubitemid 41583515)
144. Ernst EJ, Klepser ME, Pfaller MA: Postantifungal effects of echinocandin, azole, and polyene antifungal agents against Candida albicans and Cryptococcus neoformans. Antimicrob. Agents Chemother. 44(4), 1108-1111 (2000). (Pubitemid 30165304)
145. Chiller T, Farrokhshad K, Brummer E, Stevens DA: The interaction of human monocytes, monocyte-derived macrophages, and polymorphonuclear neutrophils with caspofungin (MK-0991), an echinocandin, for antifungal activity against Aspergillus fumigatus. Diagn. Microbiol. Infect. Dis. 39(2), 99-103 (2001). (Pubitemid 32206628)
146. Brown GD, Gordon S: Immune recognition. A new receptor for b-glucans. Nature 413(6851), 36-37 (2001). (Pubitemid 32843478)
147. Brown GD, Taylor PR, Reid DM et al.: Dectin-1 is a major b-glucan receptor on macrophages. J. Exp. Med. 196(3), 407-412 (2002). (Pubitemid 34875669)
148. Brown GD, Herre J, Williams DL, Willment JA, Marshall AS, Gordon S: Dectin-1 mediates the biological effects of b-glucans. J. Exp. Med. 197(9), 1119-1124 (2003). (Pubitemid 36570067)
149. Herre J, Willment JA, Gordon S, Brown GD: The role of Dectin-1 in antifungal immunity. Crit. Rev. Immunol. 24(3), 193-203 (2004). (Pubitemid 39410865)
150. Steele C, Rapaka RR, Metz A et al.: The b-glucan receptor dectin-1 recognizes specific morphologies of Aspergillus fumigatus. PLoS Pathog. 1(4), E42 (2005).
151. Wheeler RT, Fink GR: A drug-sensitive genetic network masks fungi from the immune system. PLoS Pathog. 2(4), E35 (2006).
152. Aimanianda V, Bayry J, Bozza S et al.: Surface hydrophobin prevents immune recognition of airborne fungal spores. Nature 460(7259), 1117-1121 (2009).
153. Hohl TM: Stage-specific innate immune recognition of Aspergillus fumigatus and modulation by echinocandin drugs. Med. Mycol. 12, 1-7 (2008).
154. Hohl TM, Rivera A, Lipuma L et al.: Inflammatory monocytes facilitate adaptive CD4 T cell responses during respiratory fungal infection. Cell Host Microbe 6(5), 470-481 (2009).
155. Hohl TM, Van Epps HL, Rivera A et al.: Aspergillus fumigatus triggers inflammatory responses by stage-specific b-glucan display. PLoS Pathog. 1(3), E30 (2005).
156. Hohl TM, Feldmesser M, Perlin DS, Pamer EG: Caspofungin modulates inflammatory responses to Aspergillus fumigatus through stage-specific effects on fungal b-glucan exposure. J. Infect. Dis. 198(2), 176-185 (2008). (Pubitemid 352019282)
157. Lamaris GA, Lewis RE, Chamilos G et al.: Caspofungin-mediated b-glucan unmasking and enhancement of human polymorphonuclear neutrophil activity against Aspergillus and non-Aspergillus hyphae. J. Infect. Dis. 198(2), 186-192 (2008). (Pubitemid 352019283)
158. Katragkou A, Kruhlak MJ, Simitsopoulou M et al.: Interactions between human phagocytes and Candida albicans biofilms alone and in combination with antifungal agents. J. Infect. Dis. 201(12), 1941-1949 (2010).
159. Schwartz RE, Smith SK, Onishi JC et al.: Isolation and structural determination of enfumafungin, a triterpene glycoside antifungal agent that is a specific inhibitor of glucan synthesis. J. Am. Chem. Soc. 122(20), 4882-4886 (2000). (Pubitemid 30347028)
160. Pelaez F, Cabello A, Platas G et al.: The discovery of enfumafungin, a novel antifungal compound produced by an endophytic Hormonema species biological activity and taxonomy of the producing organisms. Syst. Appl. Microbiol. 23(3), 333-343 (2000).
161. Wilkening R, Apgar J, Meng D et al.: Enfumafungin derivatives: orally active glucan synthase inhibitors. Presented at: 2010 Interscience Conference on Antimicrobial Agents and Chemotherapy. F1-846, MA, USA, 12-15 September 2010.
162. Peel M, Fan W, Mamai A et al.: Enfumafungin derivatives: orally active glucan synthase inhibitors. Presented at: Interscience Conference on Antimicrobial Agents and Chemotherapy. F1-845, MA, USA, 12-15 September 2010.
163. Motyl MR, Tan C, Liberator P et al.: MK-3118, an oral enfumafungin with potent in vitro activity against Candida and Aspergillus spp. In: Interscience Conference on Antimicrobial Agents and Chemotherapy. F1-847, MA, USA, 12-15 September 2010.
164. Flattery AM, Abruzzo GK, Gill C et al.: Evaluation of orally active enfumafungin derivative mk-3118 in mouse models of disseminated candidiasis. Presented at: Interscience Conference on Antimicrobial Agents and Chemotherapy. Boston, MA, USA, 12-15, September, 2010.
165. Flattery AM, Abruzzo GK, Gill C et al.: evaluation of enfumafungin derivative MK-3118 in two mouse models of disseminated aspergillosis. Presented at: Interscience Conference on Antimicrobial Agents and Chemotherapy. F1-849, MA, USA, 12-15 September, 2010.