Preclinical development of Ramizol, an antibiotic belonging to a new class, for the treatment of Clostridium difficile colitis

Journal of Antibiotics

Volumn 69, Issue 12, 2016, Pages 879-884

  Rao, Shasha ^a   Prestidge, Clive A ^a   Miesel, Lynn ^b   Sweeney, Deb ^c   Shinabarger, Dean L ^c   Boulos, Ramiz A ^d,e  

^a UNIVERSITY OF SOUTH AUSTRALIA   (Australia)

^b Eurofins Medinet Inc   (Germany)

^c Micromyx LLC   (United States)

^d FLINDERS UNIVERSITY   (Australia)

^e Boulos and Cooper Pharmaceuticals Pty Ltd   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIBIOTIC AGENT; FIDAXOMICIN; METRONIDAZOLE; MOXIFLOXACIN; RAMIZOL; RIFAXIMIN; UNCLASSIFIED DRUG; VANCOMYCIN; 1,3,5-TRIS(2'-(4'-BENZOIC ACID)VINYL)BENZENE; ANTIINFECTIVE AGENT; BENZOIC ACID DERIVATIVE; STILBENE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBACTERIAL ACTIVITY; ANTIBIOTIC RESISTANCE; ARTICLE; CLOSTRIDIUM DIFFICILE INFECTION; COLITIS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; IN VITRO STUDY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PRIORITY JOURNAL; RAT; SURVIVAL; SYRIAN HAMSTER; ANIMAL; CLOSTRIDIUM INFECTIONS; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECTS; MALE; MESOCRICETUS; MICROBIAL SENSITIVITY TEST; MICROBIOLOGY; MULTIDRUG RESISTANCE; PEPTOCLOSTRIDIUM DIFFICILE; PRECLINICAL STUDY; SPRAGUE DAWLEY RAT;

ANIMALS; ANTI-BACTERIAL AGENTS; BENZOATES; CLOSTRIDIUM DIFFICILE; CLOSTRIDIUM INFECTIONS; COLITIS; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE, MULTIPLE, BACTERIAL; MALE; MESOCRICETUS; MICROBIAL SENSITIVITY TESTS; RATS; RATS, SPRAGUE-DAWLEY; STILBENES;

EID: 85006724989     PISSN: 00218820     EISSN: 18811469     Source Type: Journal    
DOI: 10.1038/ja.2016.45     Document Type: Article

References (24)

1. US Department of Health and Human Services Center for Disease Control and Prevention. Antibiotic Resistance Threats in the United States (2013). http://www. cdc.gov/drugresistance/threat-report-2013/index.html.
2. Butler, M. S., Blaskovich, M. A. & Cooper, M. A. Antibiotics in the clinical pipeline in 2013. J. Antibiot. (Tokyo) 66, 571-591 (2013).
3. James,E.et al. A novel antimicrobial agent reduces oxidative stress in cells. RSC Adv. 3, 7277-7281 (2013).
4. Iscla,I.et al. A new antibiotic with potent activity targets MscL. J. Antibiot. (Tokyo) 68, 453-462 (2015).
5. Boulos, R. A. et al. Inspiration from old dyes: tris(stilbene) compounds as potent grampositive antibacterial agents. Chemistry 19, 17980-17988 (2013).
6. Rybak, M. J. The pharmacokinetic and pharmacodynamic properties of vancomycin. Clin. Infect. Dis. 42, S35-S39 (2006).
7. Waites, K. B. et al. Comparison of agar versus broth dilution techniques for determining antibiotic susceptibilities of Ureaplasma urealyticum. Diagn. Microbiol. Infect. Dis. 14, 265-271 (1991).
8. Wahid, M. H. et al. Aqueous based synthesis of antimicrobial-decorated graphene. J. Colloid Interface Sci. 443, 88-96 (2015).
9. Sanguinetti, M. C. & Tristani-Firouzi, M. hERG potassium channels and cardiac arrhythmia. Nature 23, 463-469 (2006).
10. Priest, B. T., Bell, I. M. & Garcia, M. Role of hERG potassium channel assays in drug development. Channels 2, 87-93 (2008).
11. Lannini, P. B. Cardiotoxicity of macrolides, ketolides and fluoroquinolones that prolong the QTc interval. Expert Opin. Drug Saf. 1, 121-128 (2002).
12. Surawicz, C. M. et al. The search for a better treatment for recurrent Clostridium difficile disease: use of high-dose vancomycin combined with Saccharomyces boulardii. Clin. Infect. Dis. 31, 1012-1017 (2000).
13. Clinical and Laboratory Standards Institute. Methods for Antimicrobial Susceptibility Testing of Anaerobic Bacteria; Approved Standard - Eighth Edition. CLSI document M11-A8 (CLSI, Wayne, PA, USA, 2012).
14. Schoemaker, H. & Langer, S. Z. [3H]Diltiazem binding to calcium channel antagonists recognition sites in rat cerebral cortex. Eur. J. Pharmacol. 111, 273-277 (1985).
15. Ehlert, F. J., Roeske, W. R., Itoga, E. & Yamamura, H. I. The binding of [3H] nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats. Life Sci. 30, 3656-3660 (1982).
16. Moresco, R. M., Govoni, S., Battaini, F., Trivulzio, S. & Trabucchi, M. Omegaconotoxin binding decreases in aged rat brain. Neurobiol. Aging 11, 433-436 (1990).
17. Gaines, K. L., Hamilton, S. & Boyd, III A. E. Characterization of the sulfonylurea receptor on beta cell membranes. J. Biol. Chem. 263, 2589-2592 (1988).
18. Finlayson, K., Turnbull, L., January, C. T., Sharkey, J. & Kelly, J. S. [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur. J. Pharmacol. 430, 147-148 (2001).
19. Catterall, W. A., Morrow, C. S., Daly, J. W. & Brown, C. B. Binding of batrachotoxinin A 20-alpha-benzoate to a receptor site associated with sodium channels in synaptic nerve ending particles. J. Biol. Chem. 256, 8922-8927 (1981).
20. Ochsner, U. A. et al. Inhibitory effect of REP3123 on toxin and spore formation in Clostridium difficile, and in vivo efficacy in a hamster gastrointestinal infection model. J. Antimicrob. Chemother. 63, 964-971 (2009).
21. Clostridium difficile ribotype 027 (BAA-1805), Hamster Colitis Model. Available at: https://www.eurofinspanlabs.com/Catalog/Products/ProductDetails.aspx? prodId=tkXBeXQXKFA%3D.
22. Montgomery, A. B., Rhomberg, P. R., Abuan, T., Walters, K. A. & Flamm, R. K. Amikacin-fosfomycin at a five-to-two ratio: characterization of mutation rates in microbial strains causing ventilator-associated pneumonia and interactions with commonly used antibiotics. Antimicrob. Agents Chemother. 58, 3708-3713 (2014).
23. Fung-Tomc, J., Huczko, E., Pearce, M. & Kessler, R. E. Frequency of in vitro resistance of Pseudomonas aeruginosa to cefepime, ceftazidime, and cefotaxime. Antimicrob. Agents Chemother. 32, 1443-1445 (1988).
24. Kaatz, G. W. et al. Efficacy of trovafloxacin against experimental Staphylococcus aureus endocarditis. Antimicrob. Agents Chemother. 42, 254-256 (1998).