Iclaprim, a diaminopyrimidine dihydrofolate reductase inhibitor for the potential treatment of antibiotic-resistant staphylococcal infections

Current Opinion in Investigational Drugs

Volumn 9, Issue 2, 2008, Pages 210-225

  Peppard, W J ^a   Schuenke, C D ^a  

^a FROEDTERT MEMORIAL LUTHERAN HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMOXICILLIN; AMOXICILLIN PLUS CLAVULANIC ACID; AMPICILLIN; AZITHROMYCIN; AZTREONAM; CEFAZOLIN; CEFTAZIDIME; CEFTRIAXONE; CEFUROXIME; CLARITHROMYCIN; COTRIMOXAZOLE; DIHYDROFOLATE REDUCTASE INHIBITOR; DOXYCYCLINE; ERYTHROMYCIN; GENTAMICIN; ICLAPRIM; IMIPENEM; KETOCONAZOLE; LEVOFLOXACIN; LINEZOLID; METRONIDAZOLE; PENICILLIN G; RIFAMPICIN; SULFADIAZINE; SULFAFURAZOLE; SULFAMETHOXAZOLE; TETRACYCLINE; TRIMETHOPRIM; TROVAFLOXACIN; VANCOMYCIN;

ANAPHYLAXIS; ANTIBIOTIC RESISTANCE; BONE MARROW SUPPRESSION; CLINICAL TRIAL; DIARRHEA; DRUG CONTRAINDICATION; DRUG METABOLISM; DRUG SYNTHESIS; ERYTHEMA; ERYTHEMA MULTIFORME; FEVER; GASTROINTESTINAL DISEASE; HEADACHE; HOSPITAL INFECTION; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LEUKOPENIA; MEGALOBLASTIC ANEMIA; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; NAUSEA; NEUROLOGIC DISEASE; NONHUMAN; PNEUMONIA; QT PROLONGATION; REVIEW; SKIN DISEASE; SKIN INFECTION; SKIN PRURITUS; SKIN STRUCTURE; STAPHYLOCOCCUS INFECTION; STEVENS JOHNSON SYNDROME; STRUCTURE ACTIVITY RELATION; THROMBOCYTOPENIA; TOXIC EPIDERMAL NECROLYSIS; VOMITING;

ANIMALS; ANTI-BACTERIAL AGENTS; CLINICAL TRIALS, PHASE I AS TOPIC; CLINICAL TRIALS, PHASE II AS TOPIC; CLINICAL TRIALS, PHASE III AS TOPIC; DRUG EVALUATION, PRECLINICAL; FOLIC ACID ANTAGONISTS; HUMANS; METHICILLIN RESISTANCE; MOLECULAR STRUCTURE; PATENTS AS TOPIC; PYRIMIDINES; STAPHYLOCOCCAL INFECTIONS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 38849190721     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (140)

1. 214387 Antibacterial activities of epiroprim, a new dihydrofolate reductase inhibitor, alone and in combination with dapsone. Locher HH, Schlunegger H, Hartman PG, Anghern P, Then RL ANTIMICROB AGENTS CHEMOTHER 1996 40 6 1376-1381
2. 270533 2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase. Rosowsky A, Papoulis AT, Queener SF J MED CHEM 1997 40 22 3694-3699
3. 354014 Drug development pipeline: Brodimorin. Helsinn Holding SA COMPANY COMUNICATION 2000 February 01
4. 414399 Arpida Research: R&D. Arpida Ltd COMPANY WORLD WIDE WEB SITE 2001 July 04
5. 430589 Arpida announces a sales and purchase agreement for an antibacterial compound from Roche. Arpida Ltd PRESS RELEASE 2001 November 01
6. 460270 Ertapenem once daily versus piperacillin-tazobactam 4 times per day for treatment of complicated skin and skin-structure infections in adults: Results of a prospective, randomized, double-blind multicenter study. Graham DR, Lucasti C, Malafaia O, Nichols RL, Holtom P, Perez NQ, McAdams A, Woods GL, Ceesay TP, Gesser R CLIN INFECT DIS 2002 34 11 1460-1468
7. 464845 AR-100, a novel diaminopyrimidine compound: In vitro activity against Gram-positive and Gram-negative bacterial pathogens. Then RL, Locher HH, Angehrn P ICAAC 2002 42 Abs F2018
8. 464848 AR-100, a novel diaminopyrimidine compound: Activity against selected Gram-positive and Gram-negative bacterial pathogens and synergy with other antibiotics. Hawser S, Weiss L, Fischer M, Gillessen D, Kompis I, Islam K ICAAC 2002 42 Abs F2019
9. 464850 AR-100, a novel diaminopyrimidine, can overcome TMP-resistance in staphylococci and streptococci. Hartmann PG, Kompis I, Jaeger J, Mukhija S, Islam K ICAAC 2002 42 Abs F2020
10. 464851 AR-100, a novel diaminopyrimidine compound: In vitro activity against pneumococci. Then RL, Hartman PG, Locher HH ICAAC 2002 42 Abs F2021
11. 464855 AR-100, a novel diaminopyrimidine: Activity against various clinical isolates of Gram-positive and Gram-negative bacteria. Gemmell CG, Middlemas G ICAAC 42 Abs F2022
12. 464856 AR-100, a novel diaminopyrimidine compound: Activity against streptococci. Good CE, Windau A, Bajaksouzian S, Jacobs MR, Appelbaum PC ICAAC 2002 42 Abs F2023
13. 464857 AR-100, a novel diaminopyrimidine compound: Activity against staphylococci and enterococci. Bajaksouzian S, Windau A, Appelbaum PC, Jacobs MR ICAAC 2002 42 Abs F2024
14. 464861 AR-100, a novel diaminopyrimidine compound: Activity against Enterobacteriaceae. Windau A, Bajaksouzian S, Appelbaum PC, Jacobs MR ICAAC 2002 42 Abs F2025
15. 464862 AR-100, a novel diaminopyrimidine compound: Activity against Haemophilus species and Moraxella catarrhalis. Jacobs MR, Windau A, Bajaksouzian S, Appelbaum PC ICAAC 2002 42 Abs F2026
16. 464865 AR-100, a novel diaminopyrimidine compound: Anti-anaerobe activity compared to other agents. Ednie L, Jacobs M, Appelbaum P ICAAC 2002 42 Abs F2027
17. 464867 AR-100, a novel diaminopyrimidine compound: Resistance studies in trimethoprim-sensitive and -resistant Staphylococcus aureus. Hawser S, Haldimann A, Parisi S, Gillessen D, Islam K ICAAC 2002 42 Abs F2028
18. 464869 AR-100, a novel diaminopyrimidine compound: In vivo efficacy in a murine model of staphylococcal septicaemia. Candiani GP, Romano G, Jabes D, Islam K ICAAC 2002 42 Abs F2030
19. 464905 AR-100, a novel diaminopyrimidine compound: Bactericidal activity and post-antibiotic effect on Gram-positive pathogens. Hawser S, Weiss L, Fischer M, Jaeger J, Greiveldinger S, Gillessen D, Kompis I, Islam K ICAAC 2002 42 Abs F2029
20. 484493 Randomized comparison of linezolid (PNU-100766) versus oxacillin-dicloxacillin for treatment of complicated skin and soft tissue infections. Stevens DL, Smith LG, Bruss JB, McConnell-Martin MA, Duvall SE, Todd WM, Hafkin B ANTIMICROB AGENTS CHEMOTHER 2000 44 12 3408-3413
21. 484509 Endocarditis caused by methicillin-resistant Staphylococcus aureus: Treatment failure with linezolid. Ruiz ME, Guerrero IC, Tuazon CU CLIN INFECT DIS 2002 35 8 1018-1020
22. 503381 PK/PD evaluation of iclaprim in two experimental mouse models. Fischer R, Lundsby K, Frimodt-Moeller N ICAAC 2003 43 Abs A305
23. 504034 In vitro activity of iclaprim, a novel diaminopyrimidine compound, against Chlamydia trachomatis and C pneumoniae. Hammerschlag MR, Kohlhoff S, Roblin PM, Reznik T, Hawser S, Islam K ICAAC 2003 43 Abs E2001
24. 504035 Activity of iclaprim against penicillin, erythromycin, trimethoprim/sulfamethoxazole or ciprofloxacin resistant Streptococcus pneumoniae from Canada. Zhanel GG, Palatnick LP, Hisanaga TL, Nichol KA, Hawser S, Islam K, Hoban DJ ICAAC 2003 43 Abs E2002
25. 504036 Activity of iclaprim and comparators against atypical bacterial respiratory pathogens. Morrissey I, Hawser S, Islam K, Williams L, Leakey A, Shackcloth J ICAAC 2003 43 Abs E2003
26. 504037 Iclaprim, a novel diaminopyrimidine antibiotic: In vitro and intracellular activity against Listeria monocytogenes. Hawser S, Fischer M, Weiss L, Scheidegger D, Bernardini F, Islam K ICAAC 2003 43 Abs E2004
27. 504038 In-vitro activities of iclaprim against trimethoprim-sensitive and -resistant enzymes. Parisi S, Haldimann A, Mainier C, Jaeger J, Greiveldinger S, Hawser S, Islam K ICAAC 2003 43 Abs E2005
28. 504040 In vitro activity of iclaprim (AR-100) against Gram-positive and Gram-negative bacteria. Milatovic D, Verhoef J, Fluit AC ICAAC 2003 43 Abs E2006
29. 532630 Iclaprim, a novel diaminopyrimidine with potent acitivity on trimethoprim sensitive and resistant bacteria. Schneider P, Hawser S, Islam K BIOORG MED CHEM LETT 2003 13 23 4217-4221
30. 544920 The safety and efficacy of daptomycin for the treatment of complicated skin and skin-structure infections. Arbeit RD, Maki D, Tally FP, Campanaro E, Eisenstein BI CLIN INFECT DIS 2004 38 12 1673-1681
31. 588617 New this month: Alimta MIMS (LONDON) 2005 January 01 6
32. 596645 Arpida announces further details of its proposed initial public offering on the SWX Swiss exchange. Arpida Ltd PRESS RELEASE 2005 April 20.
33. 617025 In vitro activity of a novel diaminopyrimidine compound, iclaprim, against Chlamydia trachomatis and C pneumoniae. Kohlhoff SA, Roblin PM, Reznik T, Haswer S, Islam K, Hammerschlag MR ANTIMICROB AGENTS CHEMOTHER 2004 48 5 1885-1886
34. 619252 FDA grants Arpida's injectable antibiotic Fast Track status for cSSSI. Arpida Ltd PRESS RELEASE 2005 August 24
35. 639635 Zyvox - linezolid injection, linezolid tablets, linezolid for oral suspension. Pfizer Inc DRUG DATASHEET WEBSITE 2005 November 01
36. 640082 Concentrations of iclaprim in plasma, epithelial lining fluid (ELF) alveolar macrophages (AM) and bronchial mucosa (BM) following a single 1.6 mg/kg intravenous infusion in healthy subjects. Hadvary P, Andrews JM, Honeybourne D, Ashby JP, Jevons GM, Fraise AP, Fry P, Wise R ICAAC 2005 45 Abs A9
37. 641604 Iclaprim: A new synthetic route to support clinical studies. Burri K, Greiveldinger-Poenaru S, Hoffner J, Jaeger J, Gillessen D, Islam K ICAAC 2005 45 Abs F1236
38. 641939 Efficacy and safety of intravenous iclaprim in complicated skin and skin structure infections: Results of a phase 2 study. Krievens D, Leighton A, Brandt R, Hadvary P, Hawser S, Gillessen D, Islam K ICAAC 2005 45 Abs L1579
39. 647448 Arpida confirms good bioavailability of iclaprim from an oral formulation. Arpida Ltd PRESS RELEASE 2006 January 25
40. 651644 Arpida presents additional clinical evidence of good bioavailability of oral iclaprim. Arpida Ltd PRESS RELEASE 2006 February 13
41. 747656 Arpida announces positive results in first phase III trial of iclaprim in complicated skin and skin structure infections. Arpida Ltd PRESS RELEASE 2006 November 30
42. 751655 Forest Laboratories to acquire Cerexa for $480 million. Forest Laboratories Inc PRESS RELEASE 2006 December 14
43. 764981 Arpida's lead antibiotic iclaprim is safe and well-tolerated in special populations with varying degrees of renal and hepatic impairment and obesity. Arpida Ltd PRESS RELEASE 2007 February 08
44. 777245 Arpida completes enrolment in phase III trial with intravenous iclaprim. Arpida LTd PRESS RELEASE 2007 March 22
45. 783738 NCT00303550: Study of intravenous (i.v.) iclaprim versus linezolid in complicated skin and skin structure infections [cSSSI] (ASSIST-2). CLINICALTRIALS.GOV 2007 March 26
46. 783739 NCT00299520: Phase 3 safety and efficacy study of i.v. iclaprim v linezolid in cSSSI (ASSIST-I). CLINICALTRIALS.GOV 2006 July 28
47. 784429 In vitro activity of iclaprim against Staphylococcus aureus, group A and group B streptococci. Hawser S, Lociuro S, Islam K ABS INT SYMP RESISTANT GRAM-POSITIVE INFECTIONS 2006 Abs CPLA34
48. 784432 In vitro spectrum of activity of iclaprim against various Gram-positive and Gram-negative pathogens. Hawser, S, Lociuro S, Islam K ABS INT SYMP RESISTANT GRAM-POSITIVE INFECTIONS 2006 Abs CPLA32
49. 784456 In vitro plasma fibrin clot models versus in vivo models of experimental endocarditis: Case study for diaminopyrimidine antibiotics iclaprim and trimethoprim-sulfamethoxazole. Hawser S, Entenza JM, Vouillamoz J, Moreilon P ABS INT SYMP RESISTANT GRAMPOSITIVE INFECTIONS 2006 Abs CPLA30
50. 806176 National Nosocomial Infections Surveillance (NNIS) System Report, data summary from January 1992 through June 2004, issued October 2004. AM J INFECT CONTROL 2004 32 8 470-485
51. 806184 Occurrence and antimicrobial susceptibility patterns of pathogens isolated from skin and soft tissue infections: Report from the SENTRY Antimicrobial Surveillance Program (United States and Canada, 2000). Rennie RP, Jones RN, Mutnick AH DIAGN MICROBIAL INFECT DIS 2003 45 4 287-293
52. 806264 Clinical and economic analysis of methicillin-susceptible and -resistant Staphylococcus aureus infections. Kopp BJ, Nix DE, Armstrong EP ANN PHARMACOTHER 2004 38 9 1377-13782
53. 806329 Adverse clinical and economic outcomes attributable to methicillin resistance among patients with Staphylococcus aureus surgical site infections. Engemann JJ, Carmeli Y, Cosgrove SE, Fowler VG, Bronstein MZ, Trivette SL, Briggs JP, Sexton DJ, Kaye KS CLIN INFECT DIS 2003 36 5 592-598
54. 806333 The economic impact of Staphylococcus aureus infections in New York city hospitals. Rubin RJ, Harrington CA, Poon A, Dietrich K, Greene JA, Moiduddin A EMERG INFECT DIS 1999 5 1 9-17
55. 806340 Practice guidelines for the diagnosis and management of skin and soft-tissue infections. Stevens DL, Bisno AL, Chambers HF, Everett ED, Dellinger P, Goldstein EJ, Gorbach SL, Hirschmann JV, Kaplan EL, Montoya JG, Wade JC CLIN INFECT DIS 2005 41 10 1373-1406
56. 806341 Analysis and presentation of cumulative antibiograms: A new consensus guideline from the clinical and laboratory standards institute. Barth RL, Weinstein MP CLIN INFECT DIS 2007 44 867-873
57. 806386 Treatment of hospitalized patients with complicated skin and skin structure infections: Double-blind, randomized, multicenter study of piperacillin-tazobactam versus ticarcillin-clavulanate. The piperacillin/ tazobactam skin and skin structure study group. Tan JS, Wishnow RM, Talan DA, Duncanson FP, Norden CW ANTIMICROB AGENTS CHEMOTHER 1993 37 8 1580-1586
58. 806390 Penicillins. Chambers HF IN: PRINCIPLES PRACTICE INFECT DIS, 5TH EDITION (EDS: MANDELL GL, BENNETT JE, DOLIN R), Churchill Livingstone, Philadelphia, PA, USA 2000 261-273
59. 806392 Cephalosporins. Karchmer AW IN: PRINCIPLES PRACTICE INFECT DIS, 5TH EDITION (EDS: MANDELL GL, BENNETT JE, DOLIN R), Churchill Livingstone, Philadelphia, PA, USA 2000 274-290
60. 806393 Other β-lactam antibiotics. Weiss ME, Adkinson NF IN: PRINCIPLES PRACTICE INFECT DIS, 5TH EDITION (EDS: MANDELL GL, BENNETT JE, DOLIN R), Churchill Livingstone, Philadelphia, PA, USA 2000 291-298
61. 806394 Treatment of hospitalized patients with complicated Gram-positive skin and skin structure infections: Two randomized, multicentre studies of quinupristin/dalfopristin versus cefazolin, oxacillin or vancomycin. Synercid Skin and Skin Structure Infection Group. Nichols RL, Graham DR, Barriere SL, Rodgers A, Wilson SE, Zervos M, Dunn DL, Kreter B J ANTIMICROB CHEMOTHER 1999 44 2 263-273
62. 806400 The efficacy and safety of tigecycline in the treatment of skin and skin-structure infections: Results of 2 double-blind phase 3 comparison studies with vancomycin-aztreonam. Ellis-Grosse EJ, Babinchak T, Dartois N, Rose G, Loh E CLIN INFECT DIS 2005 41 Suppl 5 S341-353
63. 806410 Dihydrofolate reductase inhibitors as antibacterial agents. Hawser S, Lociuro S, Islam K BIOCHEM PHARMACOL 2006 71 7 941-948
64. 806419 Dihydrofolate reductase as a therapeutic target. Schweitzer BI, Dicker AP, Bertino JR FASEB J 1990 4 8 2441-2452
65. 806557 FDA clears Arpida to start phase II pneumonia trial of iv iclaprim. Arpida Ltd PRESS RELEASE 2007 June 21
66. 806772 Successful treatment of a case of Proteus septicemia. Noall EWP, Sewards HFG, Waterworth PM Br Med J 1962 2 1101-1102
67. 806773 Trimethoprim, a sulphonamide potentiator. Bushby SRM, Hitchings GH BR J PHARMACOL 1968 33 1 72-90
68. 806774 Trimethoprim-sulfamethoxazole: An assessment of more than 12 years of use. Salter AJ REV INFECT DIS 1982 4 2 196-236
69. 806782 Treatment of uncomplicated urinary tract infections in an era of increasing antimicrobial resistance. Miller LG, Tang AW MAYO CLIN PROC 2004 79 8 1048-1054
70. 806785 Pneumocystis carinii pneumonia in Hong Kong: A 10 year retrospective study. Hui M, Kwok WT J MED MICROBIOL 2006 55 1 85-88
71. 806861 Enterobacter meningitis: Organism susceptibilities, antimicrobial therapy and related outcomes. Foster DR, Rhoney DH SURG NEUROL 2005 63 6 533-537
72. 806942 Treatment of community-associated methicillin-resistant Staphylococcus aureus infections. Kaplan SL PEDIATR INFECT DIS J 2005 24 5 457-458
73. 806943 Nocardial brain abscess: Treatment strategies and factors influencing outcome. Mamelak AN, Obana WG, Flaherty JF, Rosenblum ML NEUROSURGERY 1994 35 4 622-631
74. 806944 Xanthomonas maltophilia bacteremia: An analysis of 32 cases. Jang TN, Wang FD, Wang LS, Liu CY, Liu IM J FORMOS MED ASSOC 1992 91 12 1170-1176
75. 806949 Stenotrophomonas maltophilia: The significance and role as a nosocomial pathogen. Senol E J HOSP INFECT 2004 57 1 1-7
76. 807007 Chryseobacterium meningosepticum: An emerging pathogen among immunocompromised adults: Report of 6 cases and literature review. Bloch KC, Nadarajah R, Jacobs R MEDICINE 1997 76 1 30-41
77. 807014 Antimicrobial activities of dihydrofolate reductase inhibitors, used singly or in combination with dapsone, against Mycobacterium ulcerans. Dhople AM J ANTIMICROB CHEMOTHER 2001 47 1 93-96
78. 807015 Activity of epiroprim (Ro 11-8958), a dihydrofolate reductase inhibitor, alone and in combination with dapsone against Toxoplasma gondii. Chang HR, Arsenijevic D, Comte R, Polak A, Then RL, Pechère JC ANTIMICROB AGENTS CHEMOTHER 1994 38 8 1803-1807
79. 807023 Minireview: Trimethoprim resistance. Huovinen P ANTIMICROB AGENTS CHEMOTHER 1987 31 10 1451-1456
80. 807041 Minireview: Trimethoprim and sulfonamide resistance. Huovinen P, Sundstrom L, Swedberg G, Skold O ANTIMICROB AGENTS CHEMOTHER 1987 39 2 279-289
81. 807043 Resistance to trimethoprim and sulfonamides. Skold O VET RES 2001 32 3-4 261-273
82. 807048 Linezolid versus vancomycin in treatment of complicated skin and soft tissue infections. Weigelt J, Itani K, Stevens D, Lau W, Dryden M, Knirsch C ANTIMICROB AGENTS CHEMOTHER 2005 49 6 2260-2266
83. 807051 Linezolid eradicates MRSA better than vancomycin from surgical-site infections. Weigelt J, Kaafarani H, Itani K, Swanson R AM J SURG 2004 188 6 760-766
84. 807058 Linezolid compared with teicoplanin for the treatment of suspected or proven Gram-positive infections. Wilcox M, Nathwani D, Dryden M J ANTIMICROB CHEMOTHER 2004 53 2 335-344
85. 807073 AHA scientific statement on infective endocarditis: Diagnosis, antimicrobial therapy, and management of complications. Baddour LM, Wilson WR, Bayer AS, Fowler VG, Bolger AF, Levison ME, Ferrieri P, Gerber MA, Tani LY, Gewitz MH, Tong DC et al CIRCULATION 2005 111 3167-3184
86. 810851 Meropenem versus imipenem-cilastatin for the treatment of hospitalized patients with complicated skin and skin structure infections: Results of a multicenter, randomized, double-blind comparative study. Fabian TC, File TM, Embil JM, Krige JE, Klein S, Rose A, Melnick D, Soto NE SURG INFECT 2005 6 3 269-282
87. 811109 Effect of thymidine on the activity of diaminopyrimidine antibacterial agents: Generation and characterization of thymidine kinase-deficient Staphylococcus aureus mutants. Haldimann A, Hawser S, Bihr M, Fels S, Weiss L, Islam K, Lociuro S ICAAC 2006 46 Abs C1-940
88. 811731 Pharmacokinetic of single and multiple doses of iclaprim given by intravenous infusion in healthy volunteers. Brandt R, Irons S, MuBurney A, Norris V, Warrington S, Thomsen T, Hadvary P, Islam K ABS INT SYMP RESISTANT GRAM-POSITIVE INFECTIONS 2006 Abs CPLA33
89. 811978 Sustained clinical efficacy of sulfadoxine-pyrimethamine for uncomplicated falciparum malaria in Malawi after 10 years as first line treatment: Five year prospective study. Plowe CV, Kublin JG, Dzinjalamala FK, Kamwendo DS, Mukadam RA, Chimpeni P, Molyneux ME, Taylor TE BR MED J 2004 328 7439 545
90. 811979 Anticancer antifolates: Current status and future directions. McGuire JJ CURR PHARM DESIGN 2003 9 31 2593-2613
91. 811980 Inhibition of folate biosynthesis and function as a basis for chemotherapy. Hitchings GH, Burchall JJ ADV ENZYMOL RELAT AREAS MOL BIOL 1965 27 417-468
92. 811981 A large population-based follow-up study of trimethoprim-sulfamethoxazole, trimethoprim, and cephalexin for uncommon serious drug toxicity. Jick H, Derby LE PHARMACOTHERAPY 1995 5 4 428-432
93. 811983 Severe thrombocytopenia possibly associated with TMP/SMX therapy. Yamreudeewong W, Fosnocht BJ, Weixelman JM ANN PHARMACOTHER 2002 36 1 78-82
94. 811999 Trimethoprim/sulfamethoxazole-induced toxic epidermal necrolysis. See S, Mumford JM ANN PHARMACOTHER 2001 35 6 694-697
95. 812000 Adverse reactions to trimethoprim-sulfamethoxazole. Lawson DH, Paice BJ REV INFECT DIS 1982 4 2 429-433
96. 812002 Trimethoprim alone for treatment of urinary tract infection. Neu HC REV INFECT DIS 1982 4 2 366-371
97. 812005 Brodimoprim, a new bacterial dihydrofolate reductase inhibitor: A minireview. Periti P J CHEMOTHER 1995 7 3 221-223
98. 812010 Hospital-acquired and ventilator-associated pneumonia: What's new in diagnosis and treatment? Napolitano LM AM J SURG 2003 186 5A 4S-14S
99. 812014 Antimicrobial treatment of ventilator-associated pneumonia. Park DR RESPIR CARE 2005 50 7 932-952
100. 812016 Cost-effectiveness of linezolid versus vancomycin in mechanical ventilation-associated nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus. Machado AR, Arns Cda C, Follador W, Guerra A BRAZ J INFECT DIS 2005 9 3 191-200
101. 812027 Impact of linezolid on economic outcomes and determinants of cost in a clinical trial evaluating patients with MRSA complicated skin and soft-tissue infections. McKinnon PS, Sorensen SV, Liu LZ, Itani KM ANN PHARMACOTHER 2006 40 6 1017-1023
102. 812029 Clinical and economic outcomes of oral linezolid versus intravenous vancomycin in the treatment of MRSA-complicated, lower-extremity skin and soft-tissue infections caused by methicillin-resistant Staphylococcus aureus. Sharpe JN, Shively EH, Polk HC Jr AM J SURG 2005 189 4 425-428
103. 813114 Arpida reports positive results of second pivotal phase III trial with intravenous iclaprim in cSSSI. Arpida Ltd PRESS RELEASE 2007 July 15
104. 814954 The pharmacokinetic and pharmacodynamic properties of vancomycin. Rybak MJ CLIN INFECT DIS 2006 42 Suppl 1 S35-S39
105. 814955 Counterpoint: Vancomycin and Staphylococcus aureus - an antibiotic enters obsolescence. Deresinski S CLIN INFECT DIS 2007 44 12 1543-1548
106. 814956 The rationale for revising the Clinical and Laboratory Standards Institute vancomycin minimal inhibitory concentration interpretive criteria for Staphylococcus aureus. Tenover FC, Moellering RC Jr CLIN INFECT DIS 2007 44 9 1208-1215
107. 814958 Linezolid vs vancomycin: Analysis of two double-blind studies of patients with methicillin-resistant Staphylococcus aureus nosocomial pneumonia. Wunderink RG, Rello J, Cammarata SK, Croos-Dabrera RV, Kollef MH CHEST 2003 124 5 1789-1797
108. 14C]iclaprim in the marmoset. Brandt R, Harris SE, John BA, Jäger J, Islam K ICAAC 2007 47 Abs A-803
109. 844415 Activity of iclaprim against Legionella pneumophila. Morrissey I, Hawser S J ANTIMICROB CHEMOTHER 2007 60 4 905-906
110. 853354 Arpida's iclaprim has no effect on warfarin in phase I drug-drug interaction study. Arpida Ltd PRESS RELEASE 2007 November 20
111. 857244 In vitro activity of the novel diaminopyrimidine, iclaprim, in combination with folate inhibitors and other antimicrobials with different mechanisms of action. Laue H, Weiss L, Bernardi A, Hawser S, Lociuro S, Islam K J ANTIMICROB CHEMOTHER 2007 60 6 1391-1394
112. 857245 Effect of human plasma on the antimicrobial activity of iclaprim in vitro. Laue H, Valensise T, Seguin A, Hawser S, Lociuro S, Islam K J ANTIMICROB CHEMOTHER 2007 60 6 1388-1390
113. 857264 Comparative efficacy of iclaprim (ICL) against wild-type and thymidine kinase-deficient S. aureus in a mouse protection model. Murphy TM, Little S, Gordon L, McKenney D, Haldimann A, Hawser S, Lociuro S ICAAC 2007 47 Abs B-817
114. 857273 Antimicrobial activity of iclaprim tested against recent S. aureus clinical isolates: Results from the International Study of Iclaprim Susceptibility (ISIS). Sader HS, Fritsche TR, Islam K, Hawser S, Jones RN ICAAC 2007 47 Abs E-902
115. 857277 In-vitro activity of iclaprim against community acquired and nosocomial clinical isolates of Staphylococcus aureus. Mason E, Lamberth L, Hawser S, Lociuro S ICAAC 2007 47 Abs E-904
116. 857281 In vitro activity of iclaprim, a novel diaminopyrimidine, tested against β-hemolytic streptococci from the USA and Europe: Results from the International Study of Iclaprim Susceptibility (ISIS). Jones RN, Fritsche TR, Hawser S, Islam K, Sader HS ICAAC 2007 47 Abs E-911
117. 857285 Comparative evaluation of iclaprim potency and bactericidal activity tested against enterococci: Results from the International Study of Iclaprim Susceptibility (ISIS). Sader HS, Jones RN, Rhomberg P, Islam K, Hawser S, Fritsche TR ICAAC 2007 47 Abs E-910
118. 857291 Antimicrobial activity of a novel dihydrofolate reductase, iclaprim, tested against clinical strains of Enterobacteriaceae: Results from the International Study of Iclaprim Susceptibility (ISIS). Jones RN, Fritsche TR, Islam K, Hawser S, Sader HS ICAAC 2007 47 Abs E-909
119. 857296 In vitro activity of iclaprim against clinical isolates of Legionella pneumophila. Brown NP, Jones ME, Hawser S, Lociuro S, Sahm DF ICAAC 2007 47 Abs E-907
120. 857305 In-vitro activity of iclaprim and comparators against Chlamydia trachomatis. Donati M, Pignanelli S, Shurdhi A, Hawser S, Lociuro S, Cevenini R ICAAC 2007 47 Abs E-903
121. 857314 In-vitro activity of iclaprim and comparison agents tested against Neisseria gonorrhoeae including growth supplement effects. Biedenbach DJ, Sader HS, Fritsche TR, Hawser S, Lociuro S, Jones RN ICAAC 2007 47 Abs E-908
122. 857322 Bactericidal activity and post antibiotic effect of iclaprim (ICL) against Staphylococcus aureus (SA). Jones ME, Draghi DC, Grover PK, Hawser S, Islam K, Sahm DF ICAAC 2007 47 Abs E-906
123. 857375 Pharmacokinetics and metabolism of the potent dihydrofolate reductase inhibitor iclaprim mesylate in the rat. John BA, Henderson SJ, Harris SE, Irons SR, Cybulski ZR, McBurney A, Jäger J, Islam K, Brandt R ISSX MEET 2005 13 Abs 192
124. 857396 Interactions of iclaprim with human cytochrome P450 enzymes. Brandt R, Matthews A, Hall M, Islam K ICAAC 2007 47 Abs A-807
125. 857441 Tolerability and pharmacokinetics of single and repeat ascending doses of iclaprim in healthy adults. Brandt R, Warrington S, McBurney A, Islam K1 ICAAC 2007 47 Abs A-804
126. 857469 Absorption, pharmacokinetics, metabolism and excretion of iclaprim in healthy humans. Brandt R, John BA, Henderson SJ, Harris SE, Islam K ICAAC 2007 47 Abs A-805
127. 857503 Pharmacokinetics and bioavailability of iclaprim oral and intravenous formulations in humans. Brandt R, Neuenhofer D, Thomsen T, Hadváry P, Islam K ICAAC 2007 47 Abs A-806
128. 857543 Concentrations in plasma, epithelial lining fluid, alveolar macrophages and bronchial mucosa after a single intravenous dose of 1.6 mg/kg of iclaprim (AR-100) in healthy men. Andrews J, Honeybourne D, Ashby J, Jevons G, Fraise A, Fry P, Warrington S, Hawser S, Wise R J ANTIMICROB CHEMOTHER 2007 60 3 677-680
129. 857587 Evaluation of the effect of iclaprim on the QT interval in healthy volunteers. Hadváry P, Leighton A, Wargenau M, Thomsen T, Islam K IDSA 2007 45 Abs 432
130. 857645 Effect of iclaprim on the QT interval based on results of ASSIST-1. Hadváry P, Dankner W, Leighton A, Stevens D, Islam K IDSA 2007 45 Abs 1083
131. 857653 Microbiological efficacy of iclaprim against Staphylococcus aureus in complicated skin and skin structure infection (cSSSI): Preliminary results of ASSIST-1. Hawser S, Jones ME, Stevens D, Dankner W, Leighton A, Islam K, Hadváry P ICAAC 2007 47 Abs L-1142
132. 857655 Efficacy of iclaprim in complicated skin and skin structure infections: Preliminary results of ASSIST-1. Stevens D, Leighton A, Dankner W, Islam K, Hadváry P IDSA 2007 45 Abs 1079
133. 857658 Safety of iclaprim in complicated skin and skin structure infections: ASSIST-1 results. Leighton A, Dankner W, Stevens D, Islam K, Hadváry P IDSA 2007 45 Abs 1104
134. 860163 First patients enrolled in phase II trial with intravenous iclaprim in HAP/VAP/HCAP - progress of phase I programme with oral iclaprim - 'Rolling' NDA for intravenous iclaprim in cSSSI; electronic submission of first modules due before year-end 2007. Arpida Ltd PRESS RELEASE 2007 December 11
135. 866585 In vitro activity of iclaprim (formerly AR-100) against lower gastrointestinal tract isolates. Zhanel GG, Hisanaga TL, DeCorby MR, Laing MN, Nichol KA, Palatnick LP, Noreddin AM, Hawser S, Islam K, Hoban DJ ECCMID 2004 14 Abs R1915
136. 866646 Iclaprim, a novel diaminopyrimidine antibiotic: Synergy studies with different classes of antibiotics. Weiss L, Gilln D, Hawser S, Islam K ECCMID 2004 14 Abs P532
137. 866650 Anti-Pneumocystis activity of iclaprim, a reliable therapeutic alternative against Pneumocystis pneumonia. Aliouat EM, Dei-Cas N, Gantois N, Islam K, Hawser S ECCMID 2004 14 Abs P533
138. 866656 Pharmacokinetics of iclaprim in subjects with varying degree of hepatic or renal insufficiency or obesity. Hadváry P, de la Motte S, Klinger J, Islam K IDSA 2007 45 Abs 448
139. 866659 Influence of ketoconazole on the pharmacokinetics and safety of intravenous iclaprim. Hadváry P, Neuenhofer D, Brandt R, Ullmann U, Wargenau M, Thomsen T, Islam K JAHRESKONGRESS FÜR KLINISCHE PHARMAKOLOGIE (2007) 9 Abs K7
140. 867424 Arpida receives green light from US FDA for phase II efficacy trial with oral iclaprim. Arpida Ltd PRESS RELEASE 2008 January 14